Как пишется аспирин по латински

Содержание

Химическое название

2-(Ацетилокси)бензойная кислота

Фармакологическая группа вещества Ацетилсалициловая кислота

Фармакологическое действие

Характеристика

Белые мелкие игольчатые кристаллы или легкий кристаллический порошок без запаха или со слабым запахом, слабокислого вкуса. Мало растворим в воде при комнатной температуре, растворим в горячей воде, легко растворим в этаноле, растворах едких и углекислых щелочей.

Фармакология

Применение вещества Ацетилсалициловая кислота

Противопоказания

Гиперчувствительность, в т.ч. «аспириновая» триада, «аспириновая» астма; геморрагический диатез (гемофилия, болезнь Виллебранда, телеангиоэктазия), расслаивающая аневризма аорты, сердечная недостаточность, острые и рецидивирующие эрозивно-язвенные заболевания ЖКТ, желудочно-кишечное кровотечение, острая почечная или печеночная недостаточность, исходная гипопротромбинемия, дефицит витамина К, тромбоцитопения, тромботическая тромбоцитопеническая пурпура, дефицит глюкозо-6-фосфатдегидрогеназы, беременность (I и III триместр), грудное вскармливание, детский и подростковый возраст до 15 лет при применении в качестве жаропонижающего средства (риск развития синдрома Рейе у детей с лихорадкой на фоне вирусных заболеваний).

Ограничения к применению

Гиперурикемия, нефролитиаз, подагра, язвенная болезнь желудка и двенадцатиперстной кишки (в анамнезе), тяжелые нарушения функции печени и почек, бронхиальная астма, ХОБЛ, полипоз носа, неконтролируемая артериальная гипертензия.

Применение при беременности и кормлении грудью

Побочные действия вещества Ацетилсалициловая кислота

Взаимодействие

Усиливает токсичность метотрексата, снижая его почечный клиренс, эффекты наркотических анальгетиков (кодеин), пероральных противодиабетических препаратов, гепарина, непрямых антикоагулянтов, тромболитиков и ингибиторов агрегации тромбоцитов, снижает эффект урикозурических ЛС (бензбромарон, сульфинпиразон), гипотензивных средств, диуретиков (спиронолактон, фуросемид). Парацетамол, кофеин повышают риск развития побочных явлений. Глюкокортикоиды, этанол и этанолсодержащие ЛС усиливают негативное воздействие на слизистую оболочку ЖКТ и увеличивают клиренс. Повышает концентрацию дигоксина, барбитуратов, солей лития в плазме. Антациды, содержащие магний и/или алюминий, замедляют и ухудшают всасывание ацетилсалициловой кислоты. Миелотоксические ЛС усиливают проявления гематотоксичности ацетилсалициловой кислоты.

Передозировка

Способ применения и дозы

Меры предосторожности

Торговые названия с действующим веществом Ацетилсалициловая кислота

Торговое название	Цена за упаковку, руб.
АСК-кардио	от 54.00 до 166.00
Аспикор®	30.00
Аспирин®	393.00
Аспирин® Кардио	от 263.00 до 318.00
Аспирин® Экспресс	от 325.00 до 334.00
Ацекардол®	от 21.00 до 28.00
Ацетилсалициловая кислота	от 5.60 до 29.00
Ацетилсалициловая кислота Кардио	от 52.00 до 91.00
Ацетилсалициловая кислота Медисорб	от 19.00 до 38.00
Ацетилсалициловая кислота Реневал	137.00
Ацетилсалициловая кислота-УБФ	от 15.00 до 15.00
КардиАСК®	от 46.00 до 117.00
САНОВАСК®	от 77.00 до 79.00
Тромбопол®	от 41.50 до 44.00
Тромбостен	от 148.00 до 148.00
Упсарин УПСА®	от 196.90 до 266.00

аспирин

Aspirin

Clinical data
Pronunciation	acetylsalicylic acid
Trade names	Bayer Aspirin, others
Other names	2-acetoxybenzoic acid acetylsalicylate acetylsalicylic acid o-acetylsalicylic acid
AHFS/Drugs.com	Monograph
MedlinePlus	a682878
License data	EU EMA: by INN US DailyMed: Acetylsalicylic_acid US FDA: Aspirin
Pregnancy category	AU: C[1]
Routes of administration	By mouth, rectal
ATC code	A01AD05 (WHO) B01AC06 (WHO), N02BA01 (WHO)
Legal status
Legal status	AU: OTC / Schedule 2, 4, 5, 6[2][3] UK: General sales list (GSL, OTC) US: OTC / Rx-only
Pharmacokinetic data
Bioavailability	80–100%[4]
Protein binding	80–90%[5]
Metabolism	Liver (CYP2C19 and possibly CYP3A), some is also hydrolysed to salicylate in the gut wall.[5]
Elimination half-life	Dose-dependent; 2–3 h for low doses (100 mg or less), 15–30 h for large doses.[5]
Excretion	Urine (80–100%), sweat, saliva, feces[4]
Identifiers
IUPAC name Aspirin
CAS Number	50-78-2
PubChem CID	2244
IUPHAR/BPS	4139
DrugBank	DB00945
ChemSpider	2157
UNII	R16CO5Y76E
KEGG	D00109  C01405
ChEBI	CHEBI:15365
ChEMBL	ChEMBL25
PDB ligand	AIN (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID5020108
ECHA InfoCard	100.000.059
Chemical and physical data
Formula	C9H8O4
Molar mass	180.159 g·mol−1
3D model (JSmol)	Interactive image
Density	1.40 g/cm3
Melting point	136 °C (277 °F) [6]
Boiling point	140 °C (284 °F) (decomposes)
Solubility in water	3 g/L
SMILES O=C(C)Oc1ccccc1C(=O)O
InChI InChI=1S/C9H8O4/c1-6(10)13-8-5-3-2-4-7(8)9(11)12/h2-5H,1H3,(H,11,12)  Key:BSYNRYMUTXBXSQ-UHFFFAOYSA-N
(verify)

Aspirin, also known as acetylsalicylic acid (ASA), is a nonsteroidal anti-inflammatory drug (NSAID) used to reduce pain, fever, and/or inflammation, and as an antithrombotic.^[7] Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, pericarditis, and rheumatic fever.^[7]

Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk.^[7] For pain or fever, effects typically begin within 30 minutes.^[7] Aspirin works similarly to other NSAIDs but also suppresses the normal functioning of platelets.^[7]

One common adverse effect is an upset stomach.^[7] More significant side effects include stomach ulcers, stomach bleeding, and worsening asthma.^[7] Bleeding risk is greater among those who are older, drink alcohol, take other NSAIDs, or are on other blood thinners.^[7] Aspirin is not recommended in the last part of pregnancy.^[7] It is not generally recommended in children with infections because of the risk of Reye syndrome.^[7] High doses may result in ringing in the ears.^[7]

A precursor to aspirin found in the bark of the willow tree (genus Salix) has been used for its health effects for at least 2,400 years.^[8][9] In 1853, chemist Charles Frédéric Gerhardt treated the medicine sodium salicylate with acetyl chloride to produce acetylsalicylic acid for the first time.^[10] Over the next 50 years, other chemists established the chemical structure and devised more efficient production methods.^{[10]: 69–75}

Aspirin is available without medical prescription as a proprietary or generic medication^[7] in most jurisdictions. It is one of the most widely used medications globally, with an estimated 40,000 tonnes (44,000 tons) (50 to 120 billion pills)^{[clarification needed]} consumed each year,^[8][11] and is on the World Health Organization’s List of Essential Medicines.^[12] In 2020, it was the 36th most commonly prescribed medication in the United States, with more than 17 million prescriptions.^[13][14]

Brand vs. generic name[edit]

In 1897, scientists at the Bayer company began studying acetylsalicylic acid as a less-irritating replacement medication for common salicylate medicines.^{[10]: 69–75 [15]} By 1899, Bayer had named it «Aspirin» and sold it around the world.^[16]

Aspirin’s popularity grew over the first half of the 20th century, leading to competition between many brands and formulations.^[17] The word Aspirin was Bayer’s brand name; however, their rights to the trademark were lost or sold in many countries.^[17] The name is ultimately a blend of the prefix a(cetyl) + spir Spiraea, the meadowsweet plant genus from which the acetylsalicylic acid was originally derived at Bayer + -in, the common chemical suffix.

Chemical properties[edit]

Aspirin decomposes rapidly in solutions of ammonium acetate or the acetates, carbonates, citrates, or hydroxides of the alkali metals. It is stable in dry air, but gradually hydrolyses in contact with moisture to acetic and salicylic acids. In solution with alkalis, the hydrolysis proceeds rapidly and the clear solutions formed may consist entirely of acetate and salicylate.^[18]

Like flour mills, factories producing aspirin tablets must control the amount of the powder that becomes airborne inside the building, because the powder-air mixture can be explosive. The National Institute for Occupational Safety and Health (NIOSH) has set a recommended exposure limit in the United States of 5 mg/m³ (time-weighted average).^[19] In 1989, the Occupational Safety and Health Administration (OSHA) set a legal permissible exposure limit for aspirin of 5 mg/m³, but this was vacated by the AFL-CIO v. OSHA decision in 1993.^[20]

Synthesis[edit]

The synthesis of aspirin is classified as an esterification reaction. Salicylic acid is treated with acetic anhydride, an acid derivative, causing a chemical reaction that turns salicylic acid’s hydroxyl group into an ester group (R-OH → R-OCOCH₃). This process yields aspirin and acetic acid, which is considered a byproduct of this reaction. Small amounts of sulfuric acid (and occasionally phosphoric acid) are almost always used as a catalyst. This method is commonly demonstrated in undergraduate teaching labs.^[21]

Reaction between acetic acid and salicylic acid can also form aspirin but this esterification reaction is reversible and the presence of water can lead to hydrolysis of the aspirin. So, an anhydrous reagent is preferred.^[22]

Reaction mechanism

Formulations containing high concentrations of aspirin often smell like vinegar^[23] because aspirin can decompose through hydrolysis in moist conditions, yielding salicylic and acetic acids.^[24]

Physical properties[edit]

Aspirin, an acetyl derivative of salicylic acid, is a white, crystalline, weakly acidic substance, which melts at 136 °C (277 °F),^[6] and decomposes around 140 °C (284 °F).^[25] Its acid dissociation constant (pK_a) is 3.5 at 25 °C (77 °F).^[26]

Polymorphism[edit]

Polymorphism, or the ability of a substance to form more than one crystal structure, is important in the development of pharmaceutical ingredients. Many drugs receive regulatory approval for only a single crystal form or polymorph. For a long time, only one crystal structure for aspirin was known. That aspirin might have a second crystalline form was suspected since the 1960s. The elusive second polymorph was first discovered by Vishweshwar and coworkers in 2005,^[27] and fine structural details were given by Bond et al.^[28] A new crystal type was found during experiments after co-crystallization of aspirin and levetiracetam from hot acetonitrile. The form II is only stable at 100 K and reverts to form I at ambient temperature. In the (unambiguous) form I, two salicylic molecules form centrosymmetric dimers through the acetyl groups with the (acidic) methyl proton to carbonyl hydrogen bonds, and in the newly claimed form II, each salicylic molecule forms the same hydrogen bonds with two neighboring molecules instead of one. With respect to the hydrogen bonds formed by the carboxylic acid groups, both polymorphs form identical dimer structures.^[27]

Mechanism of action[edit]

Discovery of the mechanism[edit]

In 1971, British pharmacologist John Robert Vane, then employed by the Royal College of Surgeons in London, showed aspirin suppressed the production of prostaglandins and thromboxanes.^[29][30] For this discovery he was awarded the 1982 Nobel Prize in Physiology or Medicine, jointly with Sune Bergström and Bengt Ingemar Samuelsson.^[31]

Prostaglandins and thromboxanes[edit]

Aspirin’s ability to suppress the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the cyclooxygenase (COX; officially known as prostaglandin-endoperoxide synthase, PTGS) enzyme required for prostaglandin and thromboxane synthesis. Aspirin acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the PTGS enzyme (Suicide inhibition). This makes aspirin different from other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors.

Low-dose aspirin use irreversibly blocks the formation of thromboxane A₂ in platelets, producing an inhibitory effect on platelet aggregation during the lifetime of the affected platelet (8–9 days). This antithrombotic property makes aspirin useful for reducing the incidence of heart attacks in people who have had a heart attack, unstable angina, ischemic stroke or transient ischemic attack.^[32] 40 mg of aspirin a day is able to inhibit a large proportion of maximum thromboxane A₂ release provoked acutely, with the prostaglandin I2 synthesis being little affected; however, higher doses of aspirin are required to attain further inhibition.^[33]

Prostaglandins, local hormones produced in the body, have diverse effects, including the transmission of pain information to the brain, modulation of the hypothalamic thermostat, and inflammation. Thromboxanes are responsible for the aggregation of platelets that form blood clots. Heart attacks are caused primarily by blood clots, and low doses of aspirin are seen as an effective medical intervention to prevent a second acute myocardial infarction.^[34]

COX-1 and COX-2 inhibition[edit]

At least two different types of cyclooxygenases, COX-1 and COX-2, are acted on by aspirin. Aspirin irreversibly inhibits COX-1 and modifies the enzymatic activity of COX-2. COX-2 normally produces prostanoids, most of which are proinflammatory. Aspirin-modified PTGS2 (prostaglandin-endoperoxide synthase 2) produces lipoxins, most of which are anti-inflammatory.^{[35][verification needed]} Newer NSAID drugs, COX-2 inhibitors (coxibs), have been developed to inhibit only PTGS2, with the intent to reduce the incidence of gastrointestinal side effects.^[11]

Several COX-2 inhibitors, such as rofecoxib (Vioxx), have been withdrawn from the market, after evidence emerged that PTGS2 inhibitors increase the risk of heart attack and stroke.^[36][37] Endothelial cells lining the microvasculature in the body are proposed to express PTGS2, and, by selectively inhibiting PTGS2, prostaglandin production (specifically, PGI2; prostacyclin) is downregulated with respect to thromboxane levels, as PTGS1 in platelets is unaffected. Thus, the protective anticoagulative effect of PGI2 is removed, increasing the risk of thrombus and associated heart attacks and other circulatory problems. Since platelets have no DNA, they are unable to synthesize new PTGS once aspirin has irreversibly inhibited the enzyme, an important difference as compared with reversible inhibitors.

Furthermore, aspirin, while inhibiting the ability of COX-2 to form pro-inflammatory products such as the prostaglandins, converts this enzyme’s activity from a prostaglandin-forming cyclooxygenase to a lipoxygenase-like enzyme: aspirin-treated COX-2 metabolizes a variety of polyunsaturated fatty acids to hydroperoxy products which are then further metabolized to specialized proresolving mediators such as the aspirin-triggered lipoxins, aspirin-triggered resolvins, and aspirin-triggered maresins. These mediators possess potent anti-inflammatory activity. It is proposed that this aspirin-triggered transition of COX-2 from cyclooxygenase to lipoxygenase activity and the consequential formation of specialized proresolving mediators contributes to the anti-inflammatory effects of aspirin.^[38][39][40]

Additional mechanisms[edit]

Aspirin has been shown to have at least three additional modes of action. It uncouples oxidative phosphorylation in cartilaginous (and hepatic) mitochondria, by diffusing from the inner membrane space as a proton carrier back into the mitochondrial matrix, where it ionizes once again to release protons.^[41] Aspirin buffers and transports the protons. When high doses are given, it may actually cause fever, owing to the heat released from the electron transport chain, as opposed to the antipyretic action of aspirin seen with lower doses. In addition, aspirin induces the formation of NO-radicals in the body, which have been shown in mice to have an independent mechanism of reducing inflammation. This reduced leukocyte adhesion is an important step in the immune response to infection; however, evidence is insufficient to show aspirin helps to fight infection.^[42] More recent data also suggest salicylic acid and its derivatives modulate signalling through NF-κB.^[43] NF-κB, a transcription factor complex, plays a central role in many biological processes, including inflammation.^[44][45][46]

Aspirin is readily broken down in the body to salicylic acid, which itself has anti-inflammatory, antipyretic, and analgesic effects. In 2012, salicylic acid was found to activate AMP-activated protein kinase, which has been suggested as a possible explanation for some of the effects of both salicylic acid and aspirin.^[47][48] The acetyl portion of the aspirin molecule has its own targets. Acetylation of cellular proteins is a well-established phenomenon in the regulation of protein function at the post-translational level. Aspirin is able to acetylate several other targets in addition to COX isoenzymes.^[49][50] These acetylation reactions may explain many hitherto unexplained effects of aspirin.^[51]

Pharmacokinetics[edit]

Acetylsalicylic acid is a weak acid, and very little of it is ionized in the stomach after oral administration. Acetylsalicylic acid is quickly absorbed through the cell membrane in the acidic conditions of the stomach. The increased pH and larger surface area of the small intestine causes aspirin to be absorbed more slowly there, as more of it is ionized. Owing to the formation of concretions, aspirin is absorbed much more slowly during overdose, and plasma concentrations can continue to rise for up to 24 hours after ingestion.^[52][53][54]

About 50–80% of salicylate in the blood is bound to human serum albumin, while the rest remains in the active, ionized state; protein binding is concentration-dependent. Saturation of binding sites leads to more free salicylate and increased toxicity. The volume of distribution is 0.1–0.2 L/kg. Acidosis increases the volume of distribution because of enhancement of tissue penetration of salicylates.^[54]

As much as 80% of therapeutic doses of salicylic acid is metabolized in the liver. Conjugation with glycine forms salicyluric acid, and with glucuronic acid to form two different glucuronide esters. The conjugate with the acetyl group intact is referred to as the acyl glucuronide; the deacetylated conjugate is the phenolic glucuronide. These metabolic pathways have only a limited capacity. Small amounts of salicylic acid are also hydroxylated to gentisic acid. With large salicylate doses, the kinetics switch from first-order to zero-order, as metabolic pathways become saturated and renal excretion becomes increasingly important.^[54]

Salicylates are excreted mainly by the kidneys as salicyluric acid (75%), free salicylic acid (10%), salicylic phenol (10%), and acyl glucuronides (5%), gentisic acid (< 1%), and 2,3-dihydroxybenzoic acid.^[55] When small doses (less than 250 mg in an adult) are ingested, all pathways proceed by first-order kinetics, with an elimination half-life of about 2.0 h to 4.5 h.^[56][57] When higher doses of salicylate are ingested (more than 4 g), the half-life becomes much longer (15 h to 30 h),^[58] because the biotransformation pathways concerned with the formation of salicyluric acid and salicyl phenolic glucuronide become saturated.^[59] Renal excretion of salicylic acid becomes increasingly important as the metabolic pathways become saturated, because it is extremely sensitive to changes in urinary pH. A 10- to 20-fold increase in renal clearance occurs when urine pH is increased from 5 to 8. The use of urinary alkalinization exploits this particular aspect of salicylate elimination.^[60] It was found that short-term aspirin use in therapeutic doses might precipitate reversible acute kidney injury when the patient was ill with glomerulonephritis or cirrhosis.^[61] Aspirin for some patients with chronic kidney disease and some children with congestive heart failure was contraindicated.^[61]

History[edit]

Medicines made from willow and other salicylate-rich plants appear in clay tablets from ancient Sumer as well as the Ebers Papyrus from ancient Egypt.^{[10]: 8–13 [17]} Hippocrates referred to the use of salicylic tea to reduce fevers around 400 BC, and willow bark preparations were part of the pharmacopoeia of Western medicine in classical antiquity and the Middle Ages.^[17] Willow bark extract became recognized for its specific effects on fever, pain, and inflammation in the mid-eighteenth century.^[62] By the nineteenth century, pharmacists were experimenting with and prescribing a variety of chemicals related to salicylic acid, the active component of willow extract.^{[10]: 46–55}

In 1853, chemist Charles Frédéric Gerhardt treated sodium salicylate with acetyl chloride to produce acetylsalicylic acid for the first time;^{[10]: 46–48} in the second half of the 19th century, other academic chemists established the compound’s chemical structure and devised more efficient methods of synthesis. In 1897, scientists at the drug and dye firm Bayer began investigating acetylsalicylic acid as a less-irritating replacement for standard common salicylate medicines, and identified a new way to synthesize it.^{[10]: 69–75} By 1899, Bayer had dubbed this drug Aspirin and was selling it globally.^[16]: 27 The word Aspirin was Bayer’s brand name, rather than the generic name of the drug; however, Bayer’s rights to the trademark were lost or sold in many countries. Aspirin’s popularity grew over the first half of the 20th century leading to fierce competition with the proliferation of aspirin brands and products.^[17]

Aspirin’s popularity declined after the development of acetaminophen/paracetamol in 1956 and ibuprofen in 1962. In the 1960s and 1970s, John Vane and others discovered the basic mechanism of aspirin’s effects,^{[10]: 226–231} while clinical trials and other studies from the 1960s to the 1980s established aspirin’s efficacy as an anti-clotting agent that reduces the risk of clotting diseases.^{[10]: 247–257} The initial large studies on the use of low-dose aspirin to prevent heart attacks that were published in the 1970s and 1980s helped spur reform in clinical research ethics and guidelines for human subject research and US federal law, and are often cited as examples of clinical trials that included only men, but from which people drew general conclusions that did not hold true for women.^[63][64][65]

Aspirin sales revived considerably in the last decades of the 20th century, and remain strong in the 21st century with widespread use as a preventive treatment for heart attacks and strokes.^{[10]: 267–269}

Trademark[edit]

Bayer lost its trademark for Aspirin in the United States in actions taken between 1918 and 1921 because it had failed to use the name for its own product correctly and had for years allowed the use of «Aspirin» by other manufacturers without defending the intellectual property rights.^[66] Today, aspirin is a generic trademark in many countries.^[67][68] Aspirin, with a capital «A», remains a registered trademark of Bayer in Germany, Canada, Mexico, and in over 80 other countries, for acetylsalicylic acid in all markets, but using different packaging and physical aspects for each.^[69][70]

Compendial status[edit]

• United States Pharmacopeia^[71]
• British Pharmacopoeia^[72]

Medical use[edit]

Aspirin is used in the treatment of a number of conditions, including fever, pain, rheumatic fever, and inflammatory conditions, such as rheumatoid arthritis, pericarditis, and Kawasaki disease.^[7] Lower doses of aspirin have also been shown to reduce the risk of death from a heart attack, or the risk of stroke in people who are at high risk or who have cardiovascular disease, but not in elderly people who are otherwise healthy.^{[73][74][75][76][77]} There is some evidence that aspirin is effective at preventing colorectal cancer, though the mechanisms of this effect are unclear.^[78] In the United States, the selective initiation of low-dose aspirin, based on an individualised assessment, has been deemed reasonable for the primary prevention of cardiovascular disease in people aged between 40 and 59 who have a 10% or greater risk of developing cardiovascular disease over the next 10 years and are not at an increased risk of bleeding.^[79]

Pain[edit]

Aspirin is an effective analgesic for acute pain, although it is generally considered inferior to ibuprofen because aspirin is more likely to cause gastrointestinal bleeding.^[80] Aspirin is generally ineffective for those pains caused by muscle cramps, bloating, gastric distension, or acute skin irritation.^[81] As with other NSAIDs, combinations of aspirin and caffeine provide slightly greater pain relief than aspirin alone.^[82] Effervescent formulations of aspirin relieve pain faster than aspirin in tablets,^[83] which makes them useful for the treatment of migraines.^[84] Topical aspirin may be effective for treating some types of neuropathic pain.^[85]

Aspirin, either by itself or in a combined formulation, effectively treats certain types of a headache, but its efficacy may be questionable for others. Secondary headaches, meaning those caused by another disorder or trauma, should be promptly treated by a medical provider. Among primary headaches, the International Classification of Headache Disorders distinguishes between tension headache (the most common), migraine, and cluster headache. Aspirin or other over-the-counter analgesics are widely recognized as effective for the treatment of tension headache.^[86] Aspirin, especially as a component of an aspirin/paracetamol/caffeine combination, is considered a first-line therapy in the treatment of migraine, and comparable to lower doses of sumatriptan. It is most effective at stopping migraines when they are first beginning.^[87]

Fever[edit]

Like its ability to control pain, aspirin’s ability to control fever is due to its action on the prostaglandin system through its irreversible inhibition of COX.^[88] Although aspirin’s use as an antipyretic in adults is well established, many medical societies and regulatory agencies, including the American Academy of Family Physicians, the American Academy of Pediatrics, and the Food and Drug Administration, strongly advise against using aspirin for treatment of fever in children because of the risk of Reye’s syndrome, a rare but often fatal illness associated with the use of aspirin or other salicylates in children during episodes of viral or bacterial infection.^[89][90][91] Because of the risk of Reye’s syndrome in children, in 1986, the US Food and Drug Administration (FDA) required labeling on all aspirin-containing medications advising against its use in children and teenagers.^[92]

Inflammation[edit]

Aspirin is used as an anti-inflammatory agent for both acute and long-term inflammation,^[93] as well as for treatment of inflammatory diseases, such as rheumatoid arthritis.^[7]

Heart attacks and strokes[edit]

Aspirin is an important part of the treatment of those who have had a heart attack.^[94] It is generally not recommended for routine use by people with no other health problems, including those over the age of 70.^[95]

The 2009 Antithrombotic Trialists’ Collaboration published in Lancet evaluated the efficacy and safety of low dose aspirin in secondary prevention. In those with prior ischaemic stroke or acute myocardial infarction, daily low dose aspirin was associated with a 19% relative risk reduction of serious cardiovascular events (non-fatal myocardial infarction, non-fatal stroke, or vascular death). This did come at the expense of a 0.19% absolute risk increase in gastrointestinal bleeding; however, the benefits outweigh the hazard risk in this case.^[96] Data from early trials of aspirin in primary prevention suggested low dose aspirin is more beneficial for people <70 kg and high dose aspirin is more beneficial for those ≥70 kg.^[97] However, more recent trials have suggested lower dose aspirin is not more efficacious in people with a low body weight and more evidence is required to determine the effect of higher dose aspirin in people with a high body weight.^{[98][99][100]}

After percutaneous coronary interventions (PCIs), such as the placement of a coronary artery stent, a U.S. Agency for Healthcare Research and Quality guideline recommends that aspirin be taken indefinitely.^[101] Frequently, aspirin is combined with an ADP receptor inhibitor, such as clopidogrel, prasugrel, or ticagrelor to prevent blood clots. This is called dual antiplatelet therapy (DAPT). Duration of DAPT was advised in the United States and European Union guidelines after the CURE ^[102] and PRODIGY ^[103] studies . In 2020, the systematic review and network meta-analysis from Khan et al.^[104] showed promising benefits of short-term (< 6 months) DAPT followed by P2Y12 inhibitors in selected patients, as well as the benefits of extended-term (> 12 months) DAPT in high risk patients. In conclusion, the optimal duration of DAPT after PCIs should be personalized after outweighing each patient’s risks of ischemic events and risks of bleeding events with consideration of multiple patient-related and procedure-related factors. Moreover, aspirin should be continued indefinitely after DAPT is complete.^{[105][106][107]}

The status of the use of aspirin for the primary prevention in cardiovascular disease is conflicting and inconsistent, with recent changes from previously recommending it widely decades ago, and that some referenced newer trials in clinical guidelines show less of benefit of adding aspirin alongside other anti-hypertensive and cholesterol lowering therapies.^[95][108] The ASCEND study demonstrated that in high-bleeding risk diabetics with no prior cardiovascular disease, there is no overall clinical benefit (12% decrease in risk of ischaemic events v/s 29% increase in GI bleeding) of low dose aspirin in preventing the serious vascular events over a period of 7.4 years. Similarly, the results of the ARRIVE study also showed no benefit of same dose of aspirin in reducing the time to first cardiovascular outcome in patients with moderate risk of cardiovascular disease over a period of five years. Aspirin has also been suggested as a component of a polypill for prevention of cardiovascular disease.^[109][110] Complicating the use of aspirin for prevention is the phenomenon of aspirin resistance.^[111][112] For people who are resistant, aspirin’s efficacy is reduced.^[113] Some authors have suggested testing regimens to identify people who are resistant to aspirin.^[114]

As of April 2022, the United States Preventive Services Task Force (USPSTF) determined that there was a «small net benefit» for patients aged 40-59 with a 10% or greater 10-year cardiovascular disease (CVD) risk, and «no net benefit» for patients aged over 60.^{[115][116][117]} Determining the net benefit was based on balancing the risk reduction of taking aspirin for heart attacks and ischaemic strokes, with the increased risk of gastrointestinal bleeding, intracranial bleeding, and hemorrhagic strokes. Their recommendations state that age changes the risk of the medicine, with the magnitude of the benefit of aspirin coming from starting at a younger age, while the risk of bleeding, while small, increases with age, particular for adults over 60, and can be compounded by other risk factors such as diabetes and a history of gastrointestinal bleeding. As a result, the USPSTF suggests that «people ages 40 to 59 who are at higher risk for CVD should decide with their clinician whether to start taking aspirin; people 60 or older should not start taking aspirin to prevent a first heart attack or stroke.» Primary prevention guidelines from September 2019 made by the American College of Cardiology and the American Heart Association state they might consider aspirin for patients aged 40-69 with a higher risk of atherosclerotic CVD, without an increased bleeding risk, while stating they would not recommend aspirin for patients aged over 70 or adults of any age with an increased bleeding risk.^[95] They state a CVD risk estimation and a risk discussion should be done before starting on aspirin, while stating aspirin should be used «infrequently in the routine primary prevention of (atherosclerotic CVD) because of lack of net benefit». As of August 2021, the European Society of Cardiology made similar recommendations; considering aspirin specifically to patients aged less than 70 at high or very high CVD risk, without any clear contraindications, on a case-by-case basis considering both ischemic risk and bleeding risk.^[108]

Cancer prevention[edit]

Aspirin may reduce the overall risk of both getting cancer and dying from cancer.^[118] There is substantial evidence for lowering the risk of colorectal cancer (CRC),^{[78][119][120][121]} but aspirin must be taken for at least 10–20 years to see this benefit.^[122] It may also slightly reduce the risk of endometrial cancer,^[123] breast cancer, and prostate cancer.^[124]

Some conclude the benefits are greater than the risks due to bleeding in those at average risk.^[118] Others are unclear if the benefits are greater than the risk.^[125][126] Given this uncertainty, the 2007 United States Preventive Services Task Force (USPSTF) guidelines on this topic recommended against the use of aspirin for prevention of CRC in people with average risk.^[127] Nine years later however, the USPSTF issued a grade B recommendation for the use of low-dose aspirin (75 to 100 mg/day) «for the primary prevention of CVD [cardiovascular disease] and CRC in adults 50 to 59 years of age who have a 10% or greater 10-year CVD risk, are not at increased risk for bleeding, have a life expectancy of at least 10 years, and are willing to take low-dose aspirin daily for at least 10 years».^[128]

A meta-analysis through 2019 said that there was an association between taking aspirin and lower risk of cancer of the colorectum, esophagus, and stomach.^[129]

In 2021, the U.S. Preventive services Task Force raised questions about the use of aspirin in cancer prevention. It notes the results of the 2018 ASPREE (Aspirin in Reducing Events in the Elderly) Trial, in which the risk of cancer-related death was higher in the aspirin-treated group than in the placebo group.^[130]

Psychiatry[edit]

Bipolar disorder[edit]

Aspirin, along with several other agents with anti-inflammatory properties, has been repurposed as an add-on treatment for depressive episodes in subjects with bipolar disorder in light of the possible role of inflammation in the pathogenesis of severe mental disorders.^[131] However, meta-analytic evidence is based on very few studies and does not suggest any efficacy of aspirin in the treatment of bipolar depression.^[131] Thus, notwithstanding the biological rationale, the clinical perspectives of aspirin and anti-inflammatory agents in the treatment of bipolar depression remain uncertain.^[131]

Dementia[edit]

Although cohort and longitudinal studies have shown low-dose aspirin has a greater likelihood of reducing the incidence of dementia, numerous randomised controlled trials have not validated this.^[132][133]

Other uses[edit]

Aspirin is a first-line treatment for the fever and joint-pain symptoms of acute rheumatic fever. The therapy often lasts for one to two weeks, and is rarely indicated for longer periods. After fever and pain have subsided, the aspirin is no longer necessary, since it does not decrease the incidence of heart complications and residual rheumatic heart disease.^[134][135] Naproxen has been shown to be as effective as aspirin and less toxic, but due to the limited clinical experience, naproxen is recommended only as a second-line treatment.^[134][136]

Along with rheumatic fever, Kawasaki disease remains one of the few indications for aspirin use in children^[137] in spite of a lack of high quality evidence for its effectiveness.^[138]

Low-dose aspirin supplementation has moderate benefits when used for prevention of pre-eclampsia.^[139][140] This benefit is greater when started in early pregnancy.^[141]

Aspirin has also demonstrated anti-tumoral effects, via inhibition of the PTTG1 gene, which is often overexpressed in tumors.^[142]

Resistance[edit]

For some people, aspirin does not have as strong an effect on platelets as for others, an effect known as aspirin-resistance or insensitivity. One study has suggested women are more likely to be resistant than men,^[143] and a different, aggregate study of 2,930 people found 28% were resistant.^[144]
A study in 100 Italian people found, of the apparent 31% aspirin-resistant subjects, only 5% were truly resistant, and the others were noncompliant.^[145]
Another study of 400 healthy volunteers found no subjects who were truly resistant, but some had «pseudoresistance, reflecting delayed and reduced drug absorption».
^[146]

Meta-analysis and systematic reviews have concluded that laboratory confirmed aspirin resistance confers increased rates of poorer outcomes in cardiovascular and neurovascular diseases.^{[147][144][148][149][150][151]} Although the majority of research conducted has surrounded cardiovascular and neurovascular, there is emerging research into the risk of aspirin resistance after orthopaedic surgery where aspirin is used for venous thromboembolism prophylaxis.^[152] Aspirin resistance in orthopaedic surgery, specifically after total hip and knee arthroplasties, is of interest as risk factors for aspirin resistance are also risk factors for venous thromboembolisms and osteoarthritis; the sequalae of requiring a total hip or knee arthroplasty. Some of these risk factors include obesity, advancing age, diabetes mellitus, dyslipidaemia and inflammatory diseases.^[152]

Dosages[edit]

Adult aspirin tablets are produced in standardised sizes, which vary slightly from country to country, for example 300 mg in Britain and 325 mg (or 5 grains) in the United States. Smaller doses are based on these standards, e.g., 75 mg and 81 mg tablets. The 81-milligram (1+1⁄4-grain) tablets are commonly called «baby aspirin» or «baby-strength», because they were originally – but no longer – intended to be administered to infants and children.^[153] No medical significance occurs due to the slight difference in dosage between the 75 mg and the 81 mg tablets. The dose required for benefit appears to depend on a person’s weight.^[97] For those weighing less than 70 kilograms (154 lb), low dose is effective for preventing cardiovascular disease; for patients above this weight, higher doses are required.^[97]

In general, for adults, doses are taken four times a day for fever or arthritis,^[154] with doses near the maximal daily dose used historically for the treatment of rheumatic fever.^[155] For the prevention of myocardial infarction (MI) in someone with documented or suspected coronary artery disease, much lower doses are taken once daily.^[154]

March 2009 recommendations from the USPSTF on the use of aspirin for the primary prevention of coronary heart disease encourage men aged 45–79 and women aged 55–79 to use aspirin when the potential benefit of a reduction in MI for men or stroke for women outweighs the potential harm of an increase in gastrointestinal hemorrhage.^{[156][157][needs update]} The WHI study of postmenopausal women found that aspirin resulted in a 25% lower risk of death from cardiovascular disease and a 14% lower risk of death from any cause, though there was no significant difference between 81 mg and 325 mg aspirin doses.^[158] The 2021 ADAPTABLE study also showed no significant difference in cardiovascular events or major bleeding between 81 mg and 325 mg doses of aspirin in patients (both men and women) with established cardiovascular disease.^[159]

Low-dose aspirin use was also associated with a trend toward lower risk of cardiovascular events, and lower aspirin doses (75 or 81 mg/day) may optimize efficacy and safety for people requiring aspirin for long-term prevention.^[157]

In children with Kawasaki disease, aspirin is taken at dosages based on body weight, initially four times a day for up to two weeks and then at a lower dose once daily for a further six to eight weeks.^[160]

Adverse effects[edit]

In October 2020, the US Food and Drug Administration (FDA) required the drug label to be updated for all nonsteroidal anti-inflammatory medications to describe the risk of kidney problems in unborn babies that result in low amniotic fluid.^[161][162] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.^[161][162] One exception to the recommendation is the use of low-dose 81 mg aspirin at any point in pregnancy under the direction of a health care professional.^[162]

Contraindications[edit]

Aspirin should not be taken by people who are allergic to ibuprofen or naproxen,^[163][164] or who have salicylate intolerance^[165][166] or a more generalized drug intolerance to NSAIDs, and caution should be exercised in those with asthma or NSAID-precipitated bronchospasm. Owing to its effect on the stomach lining, manufacturers recommend people with peptic ulcers, mild diabetes, or gastritis seek medical advice before using aspirin.^[163][167] Even if none of these conditions is present, the risk of stomach bleeding is still increased when aspirin is taken with alcohol or warfarin.^[163][164] People with hemophilia or other bleeding tendencies should not take aspirin or other salicylates.^[163][167] Aspirin is known to cause hemolytic anemia in people who have the genetic disease glucose-6-phosphate dehydrogenase deficiency, particularly in large doses and depending on the severity of the disease.^[168] Use of aspirin during dengue fever is not recommended owing to increased bleeding tendency.^[169] People with kidney disease, hyperuricemia, or gout should not take aspirin because it inhibits the kidneys’ ability to excrete uric acid, thus may exacerbate these conditions. Aspirin should not be given to children or adolescents to control cold or influenza symptoms, as this has been linked with Reye’s syndrome.^[170]

Gastrointestinal[edit]

Aspirin use has been shown to increase the risk of gastrointestinal bleeding.^[171] Although some enteric-coated formulations of aspirin are advertised as being «gentle to the stomach», in one study, enteric coating did not seem to reduce this risk.^[171] Combining aspirin with other NSAIDs has also been shown to further increase this risk.^[171] Using aspirin in combination with clopidogrel or warfarin also increases the risk of upper gastrointestinal bleeding.^[172]

Blockade of COX-1 by aspirin apparently results in the upregulation of COX-2 as part of a gastric defense.^[173] Several trials suggest that the simultaneous use of a COX-2 inhibitor with aspirin may increase the risk of gastrointestinal injury.^[174][175] However, currently available evidence has been unable to prove that this effect is consistently repeatable in everyday clinical practice.^[176] More dedicated research is required to provide greater clarity on the subject.^[176] Therefore, caution should be exercised if combining aspirin with any «natural» supplements with COX-2-inhibiting properties, such as garlic extracts, curcumin, bilberry, pine bark, ginkgo, fish oil, resveratrol, genistein, quercetin, resorcinol, and others.^{[citation needed]}

In addition to enteric coating, «buffering» is the other main method companies have used to try to mitigate the problem of gastrointestinal bleeding. Buffering agents are intended to work by preventing the aspirin from concentrating in the walls of the stomach, although the benefits of buffered aspirin are disputed.^{[citation needed]} Almost any buffering agent used in antacids can be used; Bufferin, for example, uses magnesium oxide. Other preparations use calcium carbonate.^[177] Gas-forming agents in effervescent tablet and powder formulations can also double as a buffering agent, one example being sodium bicarbonate found in Alka-Seltzer.^[178]

Taking it with vitamin C has been investigated as a method of protecting the stomach lining. Taking equal doses of vitamin C and aspirin may decrease the amount of stomach damage that occurs compared to taking aspirin alone.^[179][180]

Retinal vein occlusion[edit]

It is a widespread habit among eye specialists (ophthalmologists) to prescribe aspirin as an add-on medication for patients with retinal vein occlusion (RVO), such as central retinal vein occlusion (CRVO) and branch retinal vein occlusion (BRVO). The reason of this widespread use is the evidence of its proven effectiveness in major systemic venous thrombotic disorders, and it has been assumed that may be similarly beneficial in various types of retinal vein occlusion.

However, a large-scale investigation based on data of nearly 700 patients showed «that aspirin or other antiplatelet aggregating agents or anticoagulants adversely influence the visual outcome in patients with CRVO and hemi-CRVO, without any evidence of protective or beneficial effect».^[181] Several expert groups, including the Royal College of Ophthalmologists, recommended against the use of antithrombotic drugs (incl. aspirin) for patients with RVO.^[182]

Central effects[edit]

Large doses of salicylate, a metabolite of aspirin, cause temporary tinnitus (ringing in the ears) based on experiments in rats, via the action on arachidonic acid and NMDA receptors cascade.^[183]

Reye’s syndrome[edit]

Reye’s syndrome, a rare but severe illness characterized by acute encephalopathy and fatty liver, can occur when children or adolescents are given aspirin for a fever or other illness or infection. From 1981 to 1997, 1207 cases of Reye’s syndrome in people younger than 18 were reported to the US Centers for Disease Control and Prevention (CDC). Of these, 93% reported being ill in the three weeks preceding the onset of Reye’s syndrome, most commonly with a respiratory infection, chickenpox, or diarrhea. Salicylates were detectable in 81.9% of children for whom test results were reported.^[184] After the association between Reye’s syndrome and aspirin was reported, and safety measures to prevent it (including a Surgeon General’s warning, and changes to the labeling of aspirin-containing drugs) were implemented, aspirin taken by children declined considerably in the United States, as did the number of reported cases of Reye’s syndrome; a similar decline was found in the United Kingdom after warnings against pediatric aspirin use were issued.^[184] The US Food and Drug Administration recommends aspirin (or aspirin-containing products) should not be given to anyone under the age of 12 who has a fever,^[170] and the UK National Health Service recommends children who are under 16 years of age should not take aspirin, unless it is on the advice of a doctor.^[185]

Skin[edit]

For a small number of people, taking aspirin can result in symptoms including hives, swelling, and headache.^[186] Aspirin can exacerbate symptoms among those with chronic hives, or create acute symptoms of hives.^[187] These responses can be due to allergic reactions to aspirin, or more often due to its effect of inhibiting the COX-1 enzyme.^[187][188] Skin reactions may also tie to systemic contraindications, seen with NSAID-precipitated bronchospasm,^[187][188] or those with atopy.^[189]

Aspirin and other NSAIDs, such as ibuprofen, may delay the healing of skin wounds.^[190] Earlier findings from two small, low-quality trials suggested a benefit with aspirin (alongside compression therapy) on venous leg ulcer healing time and leg ulcer size,^{[191][192][193]} however larger, more recent studies of higher quality have been unable to corroborate these outcomes.^[194][195] As such, further research is required to clarify the role of aspirin in this context.

Other adverse effects[edit]

Aspirin can induce swelling of skin tissues in some people. In one study, angioedema appeared one to six hours after ingesting aspirin in some of the people. However, when the aspirin was taken alone, it did not cause angioedema in these people; the aspirin had been taken in combination with another NSAID-induced drug when angioedema appeared.^[196]

Aspirin causes an increased risk of cerebral microbleeds having the appearance on MRI scans of 5 to 10 mm or smaller, hypointense (dark holes) patches.^[197][198]

A study of a group with a mean dosage of aspirin of 270 mg per day estimated an average absolute risk increase in intracerebral hemorrhage (ICH) of 12 events per 10,000 persons.^[199] In comparison, the estimated absolute risk reduction in myocardial infarction was 137 events per 10,000 persons, and a reduction of 39 events per 10,000 persons in ischemic stroke.^[199] In cases where ICH already has occurred, aspirin use results in higher mortality, with a dose of about 250 mg per day resulting in a relative risk of death within three months after the ICH around 2.5 (95% confidence interval 1.3 to 4.6).^[200]

Aspirin and other NSAIDs can cause abnormally high blood levels of potassium by inducing a hyporeninemic hypoaldosteronic state via inhibition of prostaglandin synthesis; however, these agents do not typically cause hyperkalemia by themselves in the setting of normal renal function and euvolemic state.^[201]

Use of low-dose aspirin before a surgical procedure has been associated with an increased risk of bleeding events in some patients, however, ceasing aspirin prior to surgery has also been associated with an increase in major adverse cardiac events. An analysis of multiple studies found a three-fold increase in adverse events such as myocardial infarction in patients who ceased aspirin prior to surgery. The analysis found that the risk is dependent on the type of surgery being performed and the patient indication for aspirin use.^[202]

On 9 July 2015, the US Food and Drug Administration (FDA) toughened warnings of increased heart attack and stroke risk associated with nonsteroidal anti-inflammatory drugs (NSAID).^[203] Aspirin is an NSAID but is not affected by the new warnings.^[203]

Overdose[edit]

Aspirin overdose can be acute or chronic. In acute poisoning, a single large dose is taken; in chronic poisoning, higher than normal doses are taken over a period of time. Acute overdose has a mortality rate of 2%. Chronic overdose is more commonly lethal, with a mortality rate of 25%;^[204] chronic overdose may be especially severe in children.^[205] Toxicity is managed with a number of potential treatments, including activated charcoal, intravenous dextrose and normal saline, sodium bicarbonate, and dialysis.^[206] The diagnosis of poisoning usually involves measurement of plasma salicylate, the active metabolite of aspirin, by automated spectrophotometric methods. Plasma salicylate levels in general range from 30 to 100 mg/L after usual therapeutic doses, 50–300 mg/L in people taking high doses and 700–1400 mg/L following acute overdose. Salicylate is also produced as a result of exposure to bismuth subsalicylate, methyl salicylate, and sodium salicylate.^[207][208]

Interactions[edit]

Aspirin is known to interact with other drugs. For example, acetazolamide and ammonium chloride are known to enhance the intoxicating effect of salicylates, and alcohol also increases the gastrointestinal bleeding associated with these types of drugs.^[163][164] Aspirin is known to displace a number of drugs from protein-binding sites in the blood, including the antidiabetic drugs tolbutamide and chlorpropamide, warfarin, methotrexate, phenytoin, probenecid, valproic acid (as well as interfering with beta oxidation, an important part of valproate metabolism), and other NSAIDs. Corticosteroids may also reduce the concentration of aspirin. Other NSAIDs, such as ibuprofen and naproxen, may reduce the antiplatelet effect of aspirin.^[209][210] Although limited evidence suggests this may not result in a reduced cardioprotective effect of aspirin.^[209] Analgesic doses of aspirin decrease sodium loss induced by spironolactone in the urine, however this does not reduce the antihypertensive effects of spironolactone.^[211] Furthermore, antiplatelet doses of aspirin are deemed too small to produce an interaction with spironolactone.^[212] Aspirin is known to compete with penicillin G for renal tubular secretion.^[213] Aspirin may also inhibit the absorption of vitamin C.^{[214][215][unreliable medical source?][216]}

Research[edit]

The ISIS-2 trial demonstrated that aspirin at doses of 160 mg daily for one month, decreased the mortality by 21% of participants with a suspected myocardial infarction in the first five weeks.^[217] A single daily dose of 324 mg of aspirin for 12 weeks has a highly protective effect against acute myocardial infarction and death in men with unstable angina.^[218]

Bipolar disorder[edit]

Aspirin has been repurposed as an add-on treatment for depressive episodes in subjects with bipolar disorder.^[131] However, meta-analytic evidence is based on very few studies and does not suggest any efficacy of aspirin in the treatment of bipolar depression.^[131] Thus, notwithstanding the biological rationale, the clinical perspectives of aspirin and anti-inflammatory agents in the treatment of bipolar depression remain uncertain.^[131]

Infectious diseases[edit]

Several studies investigated the anti-infective properties of aspirin for bacterial, viral and parasitic infections. Aspirin was demonstrated to limit platelet activation induced by Staphylococcus aureus and Enterococcus faecalis and to reduce streptococcal adhesion to heart valves. In patients with tuberculous meningitis, the addition of aspirin reduced the risk of new cerebral infarction [RR = 0.52 (0.29-0.92)]. A role of aspirin on bacterial and fungal biofilm is also being supported by growing evidence.^[219]

Cancer prevention[edit]

Aspirin might weakly reduce the risk of breast cancer per a 2020 meta-analysis.^[220]

In gardening[edit]

There are a many anecdotal reportings that aspirin can improve plant’s growth and resistance^[221][222] though most research involved salicylic acid instead of aspirin.^[223]

Veterinary medicine[edit]

Aspirin is sometimes used in veterinary medicine as an anticoagulant or to relieve pain associated with musculoskeletal inflammation or osteoarthritis. Aspirin should only be given to animals under the direct supervision of a veterinarian, as adverse effects—including gastrointestinal issues—are common. An aspirin overdose in any species may result in salicylate poisoning, characterized by hemorrhaging, seizures, coma, and even death.^[224]

Dogs are better able to tolerate aspirin than cats are.^[225] Cats metabolize aspirin slowly because they lack the glucuronide conjugates that aid in the excretion of aspirin, making it potentially toxic if dosing is not spaced out properly.^[224][226] No clinical signs of toxicosis occurred when cats were given 25 mg/kg of aspirin every 48 hours for 4 weeks,^[225] but the recommended dose for relief of pain and fever and for treating blood clotting diseases in cats is 10 mg/kg every 48 hours to allow for metabolization.^[224][227]

See also[edit]

• Fluoroaspirin

References[edit]

Further reading[edit]

• McTavish, Jan R. (Fall 1987). «What’s in a name? Aspirin and the American Medical Association». Bulletin of the History of Medicine. 61.3: 343–366. JSTOR 44442097. On loss of patent in the US in 1917.

External links[edit]

• «Aspirin». Drug Information Portal. U.S. National Library of Medicine.
• Ling G (2005). «Aspirin». How Products Are Made. Vol. 1. Thomson Gale.

Aspirin

Clinical data
Pronunciation	acetylsalicylic acid
Trade names	Bayer Aspirin, others
Other names	2-acetoxybenzoic acid acetylsalicylate acetylsalicylic acid o-acetylsalicylic acid
AHFS/Drugs.com	Monograph
MedlinePlus	a682878
License data	EU EMA: by INN US DailyMed: Acetylsalicylic_acid US FDA: Aspirin
Pregnancy category	AU: C[1]
Routes of administration	By mouth, rectal
ATC code	A01AD05 (WHO) B01AC06 (WHO), N02BA01 (WHO)
Legal status
Legal status	AU: OTC / Schedule 2, 4, 5, 6[2][3] UK: General sales list (GSL, OTC) US: OTC / Rx-only
Pharmacokinetic data
Bioavailability	80–100%[4]
Protein binding	80–90%[5]
Metabolism	Liver (CYP2C19 and possibly CYP3A), some is also hydrolysed to salicylate in the gut wall.[5]
Elimination half-life	Dose-dependent; 2–3 h for low doses (100 mg or less), 15–30 h for large doses.[5]
Excretion	Urine (80–100%), sweat, saliva, feces[4]
Identifiers
IUPAC name Aspirin
CAS Number	50-78-2
PubChem CID	2244
IUPHAR/BPS	4139
DrugBank	DB00945
ChemSpider	2157
UNII	R16CO5Y76E
KEGG	D00109  C01405
ChEBI	CHEBI:15365
ChEMBL	ChEMBL25
PDB ligand	AIN (PDBe, RCSB PDB)
CompTox Dashboard (EPA)	DTXSID5020108
ECHA InfoCard	100.000.059
Chemical and physical data
Formula	C9H8O4
Molar mass	180.159 g·mol−1
3D model (JSmol)	Interactive image
Density	1.40 g/cm3
Melting point	136 °C (277 °F) [6]
Boiling point	140 °C (284 °F) (decomposes)
Solubility in water	3 g/L
SMILES O=C(C)Oc1ccccc1C(=O)O
InChI InChI=1S/C9H8O4/c1-6(10)13-8-5-3-2-4-7(8)9(11)12/h2-5H,1H3,(H,11,12)  Key:BSYNRYMUTXBXSQ-UHFFFAOYSA-N
(verify)

Aspirin, also known as acetylsalicylic acid (ASA), is a nonsteroidal anti-inflammatory drug (NSAID) used to reduce pain, fever, and/or inflammation, and as an antithrombotic.^[7] Specific inflammatory conditions which aspirin is used to treat include Kawasaki disease, pericarditis, and rheumatic fever.^[7]

Aspirin is also used long-term to help prevent further heart attacks, ischaemic strokes, and blood clots in people at high risk.^[7] For pain or fever, effects typically begin within 30 minutes.^[7] Aspirin works similarly to other NSAIDs but also suppresses the normal functioning of platelets.^[7]

One common adverse effect is an upset stomach.^[7] More significant side effects include stomach ulcers, stomach bleeding, and worsening asthma.^[7] Bleeding risk is greater among those who are older, drink alcohol, take other NSAIDs, or are on other blood thinners.^[7] Aspirin is not recommended in the last part of pregnancy.^[7] It is not generally recommended in children with infections because of the risk of Reye syndrome.^[7] High doses may result in ringing in the ears.^[7]

A precursor to aspirin found in the bark of the willow tree (genus Salix) has been used for its health effects for at least 2,400 years.^[8][9] In 1853, chemist Charles Frédéric Gerhardt treated the medicine sodium salicylate with acetyl chloride to produce acetylsalicylic acid for the first time.^[10] Over the next 50 years, other chemists established the chemical structure and devised more efficient production methods.^{[10]: 69–75}

Aspirin is available without medical prescription as a proprietary or generic medication^[7] in most jurisdictions. It is one of the most widely used medications globally, with an estimated 40,000 tonnes (44,000 tons) (50 to 120 billion pills)^{[clarification needed]} consumed each year,^[8][11] and is on the World Health Organization’s List of Essential Medicines.^[12] In 2020, it was the 36th most commonly prescribed medication in the United States, with more than 17 million prescriptions.^[13][14]

Brand vs. generic name[edit]

In 1897, scientists at the Bayer company began studying acetylsalicylic acid as a less-irritating replacement medication for common salicylate medicines.^{[10]: 69–75 [15]} By 1899, Bayer had named it «Aspirin» and sold it around the world.^[16]

Aspirin’s popularity grew over the first half of the 20th century, leading to competition between many brands and formulations.^[17] The word Aspirin was Bayer’s brand name; however, their rights to the trademark were lost or sold in many countries.^[17] The name is ultimately a blend of the prefix a(cetyl) + spir Spiraea, the meadowsweet plant genus from which the acetylsalicylic acid was originally derived at Bayer + -in, the common chemical suffix.

Chemical properties[edit]

Aspirin decomposes rapidly in solutions of ammonium acetate or the acetates, carbonates, citrates, or hydroxides of the alkali metals. It is stable in dry air, but gradually hydrolyses in contact with moisture to acetic and salicylic acids. In solution with alkalis, the hydrolysis proceeds rapidly and the clear solutions formed may consist entirely of acetate and salicylate.^[18]

Like flour mills, factories producing aspirin tablets must control the amount of the powder that becomes airborne inside the building, because the powder-air mixture can be explosive. The National Institute for Occupational Safety and Health (NIOSH) has set a recommended exposure limit in the United States of 5 mg/m³ (time-weighted average).^[19] In 1989, the Occupational Safety and Health Administration (OSHA) set a legal permissible exposure limit for aspirin of 5 mg/m³, but this was vacated by the AFL-CIO v. OSHA decision in 1993.^[20]

Synthesis[edit]

The synthesis of aspirin is classified as an esterification reaction. Salicylic acid is treated with acetic anhydride, an acid derivative, causing a chemical reaction that turns salicylic acid’s hydroxyl group into an ester group (R-OH → R-OCOCH₃). This process yields aspirin and acetic acid, which is considered a byproduct of this reaction. Small amounts of sulfuric acid (and occasionally phosphoric acid) are almost always used as a catalyst. This method is commonly demonstrated in undergraduate teaching labs.^[21]

Reaction between acetic acid and salicylic acid can also form aspirin but this esterification reaction is reversible and the presence of water can lead to hydrolysis of the aspirin. So, an anhydrous reagent is preferred.^[22]

Reaction mechanism

Formulations containing high concentrations of aspirin often smell like vinegar^[23] because aspirin can decompose through hydrolysis in moist conditions, yielding salicylic and acetic acids.^[24]

Physical properties[edit]

Aspirin, an acetyl derivative of salicylic acid, is a white, crystalline, weakly acidic substance, which melts at 136 °C (277 °F),^[6] and decomposes around 140 °C (284 °F).^[25] Its acid dissociation constant (pK_a) is 3.5 at 25 °C (77 °F).^[26]

Polymorphism[edit]

Polymorphism, or the ability of a substance to form more than one crystal structure, is important in the development of pharmaceutical ingredients. Many drugs receive regulatory approval for only a single crystal form or polymorph. For a long time, only one crystal structure for aspirin was known. That aspirin might have a second crystalline form was suspected since the 1960s. The elusive second polymorph was first discovered by Vishweshwar and coworkers in 2005,^[27] and fine structural details were given by Bond et al.^[28] A new crystal type was found during experiments after co-crystallization of aspirin and levetiracetam from hot acetonitrile. The form II is only stable at 100 K and reverts to form I at ambient temperature. In the (unambiguous) form I, two salicylic molecules form centrosymmetric dimers through the acetyl groups with the (acidic) methyl proton to carbonyl hydrogen bonds, and in the newly claimed form II, each salicylic molecule forms the same hydrogen bonds with two neighboring molecules instead of one. With respect to the hydrogen bonds formed by the carboxylic acid groups, both polymorphs form identical dimer structures.^[27]

Mechanism of action[edit]

Discovery of the mechanism[edit]

In 1971, British pharmacologist John Robert Vane, then employed by the Royal College of Surgeons in London, showed aspirin suppressed the production of prostaglandins and thromboxanes.^[29][30] For this discovery he was awarded the 1982 Nobel Prize in Physiology or Medicine, jointly with Sune Bergström and Bengt Ingemar Samuelsson.^[31]

Prostaglandins and thromboxanes[edit]

Aspirin’s ability to suppress the production of prostaglandins and thromboxanes is due to its irreversible inactivation of the cyclooxygenase (COX; officially known as prostaglandin-endoperoxide synthase, PTGS) enzyme required for prostaglandin and thromboxane synthesis. Aspirin acts as an acetylating agent where an acetyl group is covalently attached to a serine residue in the active site of the PTGS enzyme (Suicide inhibition). This makes aspirin different from other NSAIDs (such as diclofenac and ibuprofen), which are reversible inhibitors.

Low-dose aspirin use irreversibly blocks the formation of thromboxane A₂ in platelets, producing an inhibitory effect on platelet aggregation during the lifetime of the affected platelet (8–9 days). This antithrombotic property makes aspirin useful for reducing the incidence of heart attacks in people who have had a heart attack, unstable angina, ischemic stroke or transient ischemic attack.^[32] 40 mg of aspirin a day is able to inhibit a large proportion of maximum thromboxane A₂ release provoked acutely, with the prostaglandin I2 synthesis being little affected; however, higher doses of aspirin are required to attain further inhibition.^[33]

Prostaglandins, local hormones produced in the body, have diverse effects, including the transmission of pain information to the brain, modulation of the hypothalamic thermostat, and inflammation. Thromboxanes are responsible for the aggregation of platelets that form blood clots. Heart attacks are caused primarily by blood clots, and low doses of aspirin are seen as an effective medical intervention to prevent a second acute myocardial infarction.^[34]

COX-1 and COX-2 inhibition[edit]

At least two different types of cyclooxygenases, COX-1 and COX-2, are acted on by aspirin. Aspirin irreversibly inhibits COX-1 and modifies the enzymatic activity of COX-2. COX-2 normally produces prostanoids, most of which are proinflammatory. Aspirin-modified PTGS2 (prostaglandin-endoperoxide synthase 2) produces lipoxins, most of which are anti-inflammatory.^{[35][verification needed]} Newer NSAID drugs, COX-2 inhibitors (coxibs), have been developed to inhibit only PTGS2, with the intent to reduce the incidence of gastrointestinal side effects.^[11]

Several COX-2 inhibitors, such as rofecoxib (Vioxx), have been withdrawn from the market, after evidence emerged that PTGS2 inhibitors increase the risk of heart attack and stroke.^[36][37] Endothelial cells lining the microvasculature in the body are proposed to express PTGS2, and, by selectively inhibiting PTGS2, prostaglandin production (specifically, PGI2; prostacyclin) is downregulated with respect to thromboxane levels, as PTGS1 in platelets is unaffected. Thus, the protective anticoagulative effect of PGI2 is removed, increasing the risk of thrombus and associated heart attacks and other circulatory problems. Since platelets have no DNA, they are unable to synthesize new PTGS once aspirin has irreversibly inhibited the enzyme, an important difference as compared with reversible inhibitors.

Furthermore, aspirin, while inhibiting the ability of COX-2 to form pro-inflammatory products such as the prostaglandins, converts this enzyme’s activity from a prostaglandin-forming cyclooxygenase to a lipoxygenase-like enzyme: aspirin-treated COX-2 metabolizes a variety of polyunsaturated fatty acids to hydroperoxy products which are then further metabolized to specialized proresolving mediators such as the aspirin-triggered lipoxins, aspirin-triggered resolvins, and aspirin-triggered maresins. These mediators possess potent anti-inflammatory activity. It is proposed that this aspirin-triggered transition of COX-2 from cyclooxygenase to lipoxygenase activity and the consequential formation of specialized proresolving mediators contributes to the anti-inflammatory effects of aspirin.^[38][39][40]

Additional mechanisms[edit]

Aspirin has been shown to have at least three additional modes of action. It uncouples oxidative phosphorylation in cartilaginous (and hepatic) mitochondria, by diffusing from the inner membrane space as a proton carrier back into the mitochondrial matrix, where it ionizes once again to release protons.^[41] Aspirin buffers and transports the protons. When high doses are given, it may actually cause fever, owing to the heat released from the electron transport chain, as opposed to the antipyretic action of aspirin seen with lower doses. In addition, aspirin induces the formation of NO-radicals in the body, which have been shown in mice to have an independent mechanism of reducing inflammation. This reduced leukocyte adhesion is an important step in the immune response to infection; however, evidence is insufficient to show aspirin helps to fight infection.^[42] More recent data also suggest salicylic acid and its derivatives modulate signalling through NF-κB.^[43] NF-κB, a transcription factor complex, plays a central role in many biological processes, including inflammation.^[44][45][46]

Aspirin is readily broken down in the body to salicylic acid, which itself has anti-inflammatory, antipyretic, and analgesic effects. In 2012, salicylic acid was found to activate AMP-activated protein kinase, which has been suggested as a possible explanation for some of the effects of both salicylic acid and aspirin.^[47][48] The acetyl portion of the aspirin molecule has its own targets. Acetylation of cellular proteins is a well-established phenomenon in the regulation of protein function at the post-translational level. Aspirin is able to acetylate several other targets in addition to COX isoenzymes.^[49][50] These acetylation reactions may explain many hitherto unexplained effects of aspirin.^[51]

Pharmacokinetics[edit]

Acetylsalicylic acid is a weak acid, and very little of it is ionized in the stomach after oral administration. Acetylsalicylic acid is quickly absorbed through the cell membrane in the acidic conditions of the stomach. The increased pH and larger surface area of the small intestine causes aspirin to be absorbed more slowly there, as more of it is ionized. Owing to the formation of concretions, aspirin is absorbed much more slowly during overdose, and plasma concentrations can continue to rise for up to 24 hours after ingestion.^[52][53][54]

About 50–80% of salicylate in the blood is bound to human serum albumin, while the rest remains in the active, ionized state; protein binding is concentration-dependent. Saturation of binding sites leads to more free salicylate and increased toxicity. The volume of distribution is 0.1–0.2 L/kg. Acidosis increases the volume of distribution because of enhancement of tissue penetration of salicylates.^[54]

As much as 80% of therapeutic doses of salicylic acid is metabolized in the liver. Conjugation with glycine forms salicyluric acid, and with glucuronic acid to form two different glucuronide esters. The conjugate with the acetyl group intact is referred to as the acyl glucuronide; the deacetylated conjugate is the phenolic glucuronide. These metabolic pathways have only a limited capacity. Small amounts of salicylic acid are also hydroxylated to gentisic acid. With large salicylate doses, the kinetics switch from first-order to zero-order, as metabolic pathways become saturated and renal excretion becomes increasingly important.^[54]

Salicylates are excreted mainly by the kidneys as salicyluric acid (75%), free salicylic acid (10%), salicylic phenol (10%), and acyl glucuronides (5%), gentisic acid (< 1%), and 2,3-dihydroxybenzoic acid.^[55] When small doses (less than 250 mg in an adult) are ingested, all pathways proceed by first-order kinetics, with an elimination half-life of about 2.0 h to 4.5 h.^[56][57] When higher doses of salicylate are ingested (more than 4 g), the half-life becomes much longer (15 h to 30 h),^[58] because the biotransformation pathways concerned with the formation of salicyluric acid and salicyl phenolic glucuronide become saturated.^[59] Renal excretion of salicylic acid becomes increasingly important as the metabolic pathways become saturated, because it is extremely sensitive to changes in urinary pH. A 10- to 20-fold increase in renal clearance occurs when urine pH is increased from 5 to 8. The use of urinary alkalinization exploits this particular aspect of salicylate elimination.^[60] It was found that short-term aspirin use in therapeutic doses might precipitate reversible acute kidney injury when the patient was ill with glomerulonephritis or cirrhosis.^[61] Aspirin for some patients with chronic kidney disease and some children with congestive heart failure was contraindicated.^[61]

History[edit]

Medicines made from willow and other salicylate-rich plants appear in clay tablets from ancient Sumer as well as the Ebers Papyrus from ancient Egypt.^{[10]: 8–13 [17]} Hippocrates referred to the use of salicylic tea to reduce fevers around 400 BC, and willow bark preparations were part of the pharmacopoeia of Western medicine in classical antiquity and the Middle Ages.^[17] Willow bark extract became recognized for its specific effects on fever, pain, and inflammation in the mid-eighteenth century.^[62] By the nineteenth century, pharmacists were experimenting with and prescribing a variety of chemicals related to salicylic acid, the active component of willow extract.^{[10]: 46–55}

In 1853, chemist Charles Frédéric Gerhardt treated sodium salicylate with acetyl chloride to produce acetylsalicylic acid for the first time;^{[10]: 46–48} in the second half of the 19th century, other academic chemists established the compound’s chemical structure and devised more efficient methods of synthesis. In 1897, scientists at the drug and dye firm Bayer began investigating acetylsalicylic acid as a less-irritating replacement for standard common salicylate medicines, and identified a new way to synthesize it.^{[10]: 69–75} By 1899, Bayer had dubbed this drug Aspirin and was selling it globally.^[16]: 27 The word Aspirin was Bayer’s brand name, rather than the generic name of the drug; however, Bayer’s rights to the trademark were lost or sold in many countries. Aspirin’s popularity grew over the first half of the 20th century leading to fierce competition with the proliferation of aspirin brands and products.^[17]

Aspirin’s popularity declined after the development of acetaminophen/paracetamol in 1956 and ibuprofen in 1962. In the 1960s and 1970s, John Vane and others discovered the basic mechanism of aspirin’s effects,^{[10]: 226–231} while clinical trials and other studies from the 1960s to the 1980s established aspirin’s efficacy as an anti-clotting agent that reduces the risk of clotting diseases.^{[10]: 247–257} The initial large studies on the use of low-dose aspirin to prevent heart attacks that were published in the 1970s and 1980s helped spur reform in clinical research ethics and guidelines for human subject research and US federal law, and are often cited as examples of clinical trials that included only men, but from which people drew general conclusions that did not hold true for women.^[63][64][65]

Aspirin sales revived considerably in the last decades of the 20th century, and remain strong in the 21st century with widespread use as a preventive treatment for heart attacks and strokes.^{[10]: 267–269}

Trademark[edit]

Bayer lost its trademark for Aspirin in the United States in actions taken between 1918 and 1921 because it had failed to use the name for its own product correctly and had for years allowed the use of «Aspirin» by other manufacturers without defending the intellectual property rights.^[66] Today, aspirin is a generic trademark in many countries.^[67][68] Aspirin, with a capital «A», remains a registered trademark of Bayer in Germany, Canada, Mexico, and in over 80 other countries, for acetylsalicylic acid in all markets, but using different packaging and physical aspects for each.^[69][70]

Compendial status[edit]

• United States Pharmacopeia^[71]
• British Pharmacopoeia^[72]

Medical use[edit]

Aspirin is used in the treatment of a number of conditions, including fever, pain, rheumatic fever, and inflammatory conditions, such as rheumatoid arthritis, pericarditis, and Kawasaki disease.^[7] Lower doses of aspirin have also been shown to reduce the risk of death from a heart attack, or the risk of stroke in people who are at high risk or who have cardiovascular disease, but not in elderly people who are otherwise healthy.^{[73][74][75][76][77]} There is some evidence that aspirin is effective at preventing colorectal cancer, though the mechanisms of this effect are unclear.^[78] In the United States, the selective initiation of low-dose aspirin, based on an individualised assessment, has been deemed reasonable for the primary prevention of cardiovascular disease in people aged between 40 and 59 who have a 10% or greater risk of developing cardiovascular disease over the next 10 years and are not at an increased risk of bleeding.^[79]

Pain[edit]

Aspirin is an effective analgesic for acute pain, although it is generally considered inferior to ibuprofen because aspirin is more likely to cause gastrointestinal bleeding.^[80] Aspirin is generally ineffective for those pains caused by muscle cramps, bloating, gastric distension, or acute skin irritation.^[81] As with other NSAIDs, combinations of aspirin and caffeine provide slightly greater pain relief than aspirin alone.^[82] Effervescent formulations of aspirin relieve pain faster than aspirin in tablets,^[83] which makes them useful for the treatment of migraines.^[84] Topical aspirin may be effective for treating some types of neuropathic pain.^[85]

Aspirin, either by itself or in a combined formulation, effectively treats certain types of a headache, but its efficacy may be questionable for others. Secondary headaches, meaning those caused by another disorder or trauma, should be promptly treated by a medical provider. Among primary headaches, the International Classification of Headache Disorders distinguishes between tension headache (the most common), migraine, and cluster headache. Aspirin or other over-the-counter analgesics are widely recognized as effective for the treatment of tension headache.^[86] Aspirin, especially as a component of an aspirin/paracetamol/caffeine combination, is considered a first-line therapy in the treatment of migraine, and comparable to lower doses of sumatriptan. It is most effective at stopping migraines when they are first beginning.^[87]

Fever[edit]

Like its ability to control pain, aspirin’s ability to control fever is due to its action on the prostaglandin system through its irreversible inhibition of COX.^[88] Although aspirin’s use as an antipyretic in adults is well established, many medical societies and regulatory agencies, including the American Academy of Family Physicians, the American Academy of Pediatrics, and the Food and Drug Administration, strongly advise against using aspirin for treatment of fever in children because of the risk of Reye’s syndrome, a rare but often fatal illness associated with the use of aspirin or other salicylates in children during episodes of viral or bacterial infection.^[89][90][91] Because of the risk of Reye’s syndrome in children, in 1986, the US Food and Drug Administration (FDA) required labeling on all aspirin-containing medications advising against its use in children and teenagers.^[92]

Inflammation[edit]

Aspirin is used as an anti-inflammatory agent for both acute and long-term inflammation,^[93] as well as for treatment of inflammatory diseases, such as rheumatoid arthritis.^[7]

Heart attacks and strokes[edit]

Aspirin is an important part of the treatment of those who have had a heart attack.^[94] It is generally not recommended for routine use by people with no other health problems, including those over the age of 70.^[95]

The 2009 Antithrombotic Trialists’ Collaboration published in Lancet evaluated the efficacy and safety of low dose aspirin in secondary prevention. In those with prior ischaemic stroke or acute myocardial infarction, daily low dose aspirin was associated with a 19% relative risk reduction of serious cardiovascular events (non-fatal myocardial infarction, non-fatal stroke, or vascular death). This did come at the expense of a 0.19% absolute risk increase in gastrointestinal bleeding; however, the benefits outweigh the hazard risk in this case.^[96] Data from early trials of aspirin in primary prevention suggested low dose aspirin is more beneficial for people <70 kg and high dose aspirin is more beneficial for those ≥70 kg.^[97] However, more recent trials have suggested lower dose aspirin is not more efficacious in people with a low body weight and more evidence is required to determine the effect of higher dose aspirin in people with a high body weight.^{[98][99][100]}

After percutaneous coronary interventions (PCIs), such as the placement of a coronary artery stent, a U.S. Agency for Healthcare Research and Quality guideline recommends that aspirin be taken indefinitely.^[101] Frequently, aspirin is combined with an ADP receptor inhibitor, such as clopidogrel, prasugrel, or ticagrelor to prevent blood clots. This is called dual antiplatelet therapy (DAPT). Duration of DAPT was advised in the United States and European Union guidelines after the CURE ^[102] and PRODIGY ^[103] studies . In 2020, the systematic review and network meta-analysis from Khan et al.^[104] showed promising benefits of short-term (< 6 months) DAPT followed by P2Y12 inhibitors in selected patients, as well as the benefits of extended-term (> 12 months) DAPT in high risk patients. In conclusion, the optimal duration of DAPT after PCIs should be personalized after outweighing each patient’s risks of ischemic events and risks of bleeding events with consideration of multiple patient-related and procedure-related factors. Moreover, aspirin should be continued indefinitely after DAPT is complete.^{[105][106][107]}

The status of the use of aspirin for the primary prevention in cardiovascular disease is conflicting and inconsistent, with recent changes from previously recommending it widely decades ago, and that some referenced newer trials in clinical guidelines show less of benefit of adding aspirin alongside other anti-hypertensive and cholesterol lowering therapies.^[95][108] The ASCEND study demonstrated that in high-bleeding risk diabetics with no prior cardiovascular disease, there is no overall clinical benefit (12% decrease in risk of ischaemic events v/s 29% increase in GI bleeding) of low dose aspirin in preventing the serious vascular events over a period of 7.4 years. Similarly, the results of the ARRIVE study also showed no benefit of same dose of aspirin in reducing the time to first cardiovascular outcome in patients with moderate risk of cardiovascular disease over a period of five years. Aspirin has also been suggested as a component of a polypill for prevention of cardiovascular disease.^[109][110] Complicating the use of aspirin for prevention is the phenomenon of aspirin resistance.^[111][112] For people who are resistant, aspirin’s efficacy is reduced.^[113] Some authors have suggested testing regimens to identify people who are resistant to aspirin.^[114]

As of April 2022, the United States Preventive Services Task Force (USPSTF) determined that there was a «small net benefit» for patients aged 40-59 with a 10% or greater 10-year cardiovascular disease (CVD) risk, and «no net benefit» for patients aged over 60.^{[115][116][117]} Determining the net benefit was based on balancing the risk reduction of taking aspirin for heart attacks and ischaemic strokes, with the increased risk of gastrointestinal bleeding, intracranial bleeding, and hemorrhagic strokes. Their recommendations state that age changes the risk of the medicine, with the magnitude of the benefit of aspirin coming from starting at a younger age, while the risk of bleeding, while small, increases with age, particular for adults over 60, and can be compounded by other risk factors such as diabetes and a history of gastrointestinal bleeding. As a result, the USPSTF suggests that «people ages 40 to 59 who are at higher risk for CVD should decide with their clinician whether to start taking aspirin; people 60 or older should not start taking aspirin to prevent a first heart attack or stroke.» Primary prevention guidelines from September 2019 made by the American College of Cardiology and the American Heart Association state they might consider aspirin for patients aged 40-69 with a higher risk of atherosclerotic CVD, without an increased bleeding risk, while stating they would not recommend aspirin for patients aged over 70 or adults of any age with an increased bleeding risk.^[95] They state a CVD risk estimation and a risk discussion should be done before starting on aspirin, while stating aspirin should be used «infrequently in the routine primary prevention of (atherosclerotic CVD) because of lack of net benefit». As of August 2021, the European Society of Cardiology made similar recommendations; considering aspirin specifically to patients aged less than 70 at high or very high CVD risk, without any clear contraindications, on a case-by-case basis considering both ischemic risk and bleeding risk.^[108]

Cancer prevention[edit]

Aspirin may reduce the overall risk of both getting cancer and dying from cancer.^[118] There is substantial evidence for lowering the risk of colorectal cancer (CRC),^{[78][119][120][121]} but aspirin must be taken for at least 10–20 years to see this benefit.^[122] It may also slightly reduce the risk of endometrial cancer,^[123] breast cancer, and prostate cancer.^[124]

Some conclude the benefits are greater than the risks due to bleeding in those at average risk.^[118] Others are unclear if the benefits are greater than the risk.^[125][126] Given this uncertainty, the 2007 United States Preventive Services Task Force (USPSTF) guidelines on this topic recommended against the use of aspirin for prevention of CRC in people with average risk.^[127] Nine years later however, the USPSTF issued a grade B recommendation for the use of low-dose aspirin (75 to 100 mg/day) «for the primary prevention of CVD [cardiovascular disease] and CRC in adults 50 to 59 years of age who have a 10% or greater 10-year CVD risk, are not at increased risk for bleeding, have a life expectancy of at least 10 years, and are willing to take low-dose aspirin daily for at least 10 years».^[128]

A meta-analysis through 2019 said that there was an association between taking aspirin and lower risk of cancer of the colorectum, esophagus, and stomach.^[129]

In 2021, the U.S. Preventive services Task Force raised questions about the use of aspirin in cancer prevention. It notes the results of the 2018 ASPREE (Aspirin in Reducing Events in the Elderly) Trial, in which the risk of cancer-related death was higher in the aspirin-treated group than in the placebo group.^[130]

Psychiatry[edit]

Bipolar disorder[edit]

Aspirin, along with several other agents with anti-inflammatory properties, has been repurposed as an add-on treatment for depressive episodes in subjects with bipolar disorder in light of the possible role of inflammation in the pathogenesis of severe mental disorders.^[131] However, meta-analytic evidence is based on very few studies and does not suggest any efficacy of aspirin in the treatment of bipolar depression.^[131] Thus, notwithstanding the biological rationale, the clinical perspectives of aspirin and anti-inflammatory agents in the treatment of bipolar depression remain uncertain.^[131]

Dementia[edit]

Although cohort and longitudinal studies have shown low-dose aspirin has a greater likelihood of reducing the incidence of dementia, numerous randomised controlled trials have not validated this.^[132][133]

Other uses[edit]

Aspirin is a first-line treatment for the fever and joint-pain symptoms of acute rheumatic fever. The therapy often lasts for one to two weeks, and is rarely indicated for longer periods. After fever and pain have subsided, the aspirin is no longer necessary, since it does not decrease the incidence of heart complications and residual rheumatic heart disease.^[134][135] Naproxen has been shown to be as effective as aspirin and less toxic, but due to the limited clinical experience, naproxen is recommended only as a second-line treatment.^[134][136]

Along with rheumatic fever, Kawasaki disease remains one of the few indications for aspirin use in children^[137] in spite of a lack of high quality evidence for its effectiveness.^[138]

Low-dose aspirin supplementation has moderate benefits when used for prevention of pre-eclampsia.^[139][140] This benefit is greater when started in early pregnancy.^[141]

Aspirin has also demonstrated anti-tumoral effects, via inhibition of the PTTG1 gene, which is often overexpressed in tumors.^[142]

Resistance[edit]

For some people, aspirin does not have as strong an effect on platelets as for others, an effect known as aspirin-resistance or insensitivity. One study has suggested women are more likely to be resistant than men,^[143] and a different, aggregate study of 2,930 people found 28% were resistant.^[144]
A study in 100 Italian people found, of the apparent 31% aspirin-resistant subjects, only 5% were truly resistant, and the others were noncompliant.^[145]
Another study of 400 healthy volunteers found no subjects who were truly resistant, but some had «pseudoresistance, reflecting delayed and reduced drug absorption».
^[146]

Meta-analysis and systematic reviews have concluded that laboratory confirmed aspirin resistance confers increased rates of poorer outcomes in cardiovascular and neurovascular diseases.^{[147][144][148][149][150][151]} Although the majority of research conducted has surrounded cardiovascular and neurovascular, there is emerging research into the risk of aspirin resistance after orthopaedic surgery where aspirin is used for venous thromboembolism prophylaxis.^[152] Aspirin resistance in orthopaedic surgery, specifically after total hip and knee arthroplasties, is of interest as risk factors for aspirin resistance are also risk factors for venous thromboembolisms and osteoarthritis; the sequalae of requiring a total hip or knee arthroplasty. Some of these risk factors include obesity, advancing age, diabetes mellitus, dyslipidaemia and inflammatory diseases.^[152]

Dosages[edit]

Adult aspirin tablets are produced in standardised sizes, which vary slightly from country to country, for example 300 mg in Britain and 325 mg (or 5 grains) in the United States. Smaller doses are based on these standards, e.g., 75 mg and 81 mg tablets. The 81-milligram (1+1⁄4-grain) tablets are commonly called «baby aspirin» or «baby-strength», because they were originally – but no longer – intended to be administered to infants and children.^[153] No medical significance occurs due to the slight difference in dosage between the 75 mg and the 81 mg tablets. The dose required for benefit appears to depend on a person’s weight.^[97] For those weighing less than 70 kilograms (154 lb), low dose is effective for preventing cardiovascular disease; for patients above this weight, higher doses are required.^[97]

In general, for adults, doses are taken four times a day for fever or arthritis,^[154] with doses near the maximal daily dose used historically for the treatment of rheumatic fever.^[155] For the prevention of myocardial infarction (MI) in someone with documented or suspected coronary artery disease, much lower doses are taken once daily.^[154]

March 2009 recommendations from the USPSTF on the use of aspirin for the primary prevention of coronary heart disease encourage men aged 45–79 and women aged 55–79 to use aspirin when the potential benefit of a reduction in MI for men or stroke for women outweighs the potential harm of an increase in gastrointestinal hemorrhage.^{[156][157][needs update]} The WHI study of postmenopausal women found that aspirin resulted in a 25% lower risk of death from cardiovascular disease and a 14% lower risk of death from any cause, though there was no significant difference between 81 mg and 325 mg aspirin doses.^[158] The 2021 ADAPTABLE study also showed no significant difference in cardiovascular events or major bleeding between 81 mg and 325 mg doses of aspirin in patients (both men and women) with established cardiovascular disease.^[159]

Low-dose aspirin use was also associated with a trend toward lower risk of cardiovascular events, and lower aspirin doses (75 or 81 mg/day) may optimize efficacy and safety for people requiring aspirin for long-term prevention.^[157]

In children with Kawasaki disease, aspirin is taken at dosages based on body weight, initially four times a day for up to two weeks and then at a lower dose once daily for a further six to eight weeks.^[160]

Adverse effects[edit]

In October 2020, the US Food and Drug Administration (FDA) required the drug label to be updated for all nonsteroidal anti-inflammatory medications to describe the risk of kidney problems in unborn babies that result in low amniotic fluid.^[161][162] They recommend avoiding NSAIDs in pregnant women at 20 weeks or later in pregnancy.^[161][162] One exception to the recommendation is the use of low-dose 81 mg aspirin at any point in pregnancy under the direction of a health care professional.^[162]

Contraindications[edit]

Aspirin should not be taken by people who are allergic to ibuprofen or naproxen,^[163][164] or who have salicylate intolerance^[165][166] or a more generalized drug intolerance to NSAIDs, and caution should be exercised in those with asthma or NSAID-precipitated bronchospasm. Owing to its effect on the stomach lining, manufacturers recommend people with peptic ulcers, mild diabetes, or gastritis seek medical advice before using aspirin.^[163][167] Even if none of these conditions is present, the risk of stomach bleeding is still increased when aspirin is taken with alcohol or warfarin.^[163][164] People with hemophilia or other bleeding tendencies should not take aspirin or other salicylates.^[163][167] Aspirin is known to cause hemolytic anemia in people who have the genetic disease glucose-6-phosphate dehydrogenase deficiency, particularly in large doses and depending on the severity of the disease.^[168] Use of aspirin during dengue fever is not recommended owing to increased bleeding tendency.^[169] People with kidney disease, hyperuricemia, or gout should not take aspirin because it inhibits the kidneys’ ability to excrete uric acid, thus may exacerbate these conditions. Aspirin should not be given to children or adolescents to control cold or influenza symptoms, as this has been linked with Reye’s syndrome.^[170]

Gastrointestinal[edit]

Aspirin use has been shown to increase the risk of gastrointestinal bleeding.^[171] Although some enteric-coated formulations of aspirin are advertised as being «gentle to the stomach», in one study, enteric coating did not seem to reduce this risk.^[171] Combining aspirin with other NSAIDs has also been shown to further increase this risk.^[171] Using aspirin in combination with clopidogrel or warfarin also increases the risk of upper gastrointestinal bleeding.^[172]

Blockade of COX-1 by aspirin apparently results in the upregulation of COX-2 as part of a gastric defense.^[173] Several trials suggest that the simultaneous use of a COX-2 inhibitor with aspirin may increase the risk of gastrointestinal injury.^[174][175] However, currently available evidence has been unable to prove that this effect is consistently repeatable in everyday clinical practice.^[176] More dedicated research is required to provide greater clarity on the subject.^[176] Therefore, caution should be exercised if combining aspirin with any «natural» supplements with COX-2-inhibiting properties, such as garlic extracts, curcumin, bilberry, pine bark, ginkgo, fish oil, resveratrol, genistein, quercetin, resorcinol, and others.^{[citation needed]}

In addition to enteric coating, «buffering» is the other main method companies have used to try to mitigate the problem of gastrointestinal bleeding. Buffering agents are intended to work by preventing the aspirin from concentrating in the walls of the stomach, although the benefits of buffered aspirin are disputed.^{[citation needed]} Almost any buffering agent used in antacids can be used; Bufferin, for example, uses magnesium oxide. Other preparations use calcium carbonate.^[177] Gas-forming agents in effervescent tablet and powder formulations can also double as a buffering agent, one example being sodium bicarbonate found in Alka-Seltzer.^[178]

Taking it with vitamin C has been investigated as a method of protecting the stomach lining. Taking equal doses of vitamin C and aspirin may decrease the amount of stomach damage that occurs compared to taking aspirin alone.^[179][180]

Retinal vein occlusion[edit]

It is a widespread habit among eye specialists (ophthalmologists) to prescribe aspirin as an add-on medication for patients with retinal vein occlusion (RVO), such as central retinal vein occlusion (CRVO) and branch retinal vein occlusion (BRVO). The reason of this widespread use is the evidence of its proven effectiveness in major systemic venous thrombotic disorders, and it has been assumed that may be similarly beneficial in various types of retinal vein occlusion.

However, a large-scale investigation based on data of nearly 700 patients showed «that aspirin or other antiplatelet aggregating agents or anticoagulants adversely influence the visual outcome in patients with CRVO and hemi-CRVO, without any evidence of protective or beneficial effect».^[181] Several expert groups, including the Royal College of Ophthalmologists, recommended against the use of antithrombotic drugs (incl. aspirin) for patients with RVO.^[182]

Central effects[edit]

Large doses of salicylate, a metabolite of aspirin, cause temporary tinnitus (ringing in the ears) based on experiments in rats, via the action on arachidonic acid and NMDA receptors cascade.^[183]

Reye’s syndrome[edit]

Reye’s syndrome, a rare but severe illness characterized by acute encephalopathy and fatty liver, can occur when children or adolescents are given aspirin for a fever or other illness or infection. From 1981 to 1997, 1207 cases of Reye’s syndrome in people younger than 18 were reported to the US Centers for Disease Control and Prevention (CDC). Of these, 93% reported being ill in the three weeks preceding the onset of Reye’s syndrome, most commonly with a respiratory infection, chickenpox, or diarrhea. Salicylates were detectable in 81.9% of children for whom test results were reported.^[184] After the association between Reye’s syndrome and aspirin was reported, and safety measures to prevent it (including a Surgeon General’s warning, and changes to the labeling of aspirin-containing drugs) were implemented, aspirin taken by children declined considerably in the United States, as did the number of reported cases of Reye’s syndrome; a similar decline was found in the United Kingdom after warnings against pediatric aspirin use were issued.^[184] The US Food and Drug Administration recommends aspirin (or aspirin-containing products) should not be given to anyone under the age of 12 who has a fever,^[170] and the UK National Health Service recommends children who are under 16 years of age should not take aspirin, unless it is on the advice of a doctor.^[185]

Skin[edit]

For a small number of people, taking aspirin can result in symptoms including hives, swelling, and headache.^[186] Aspirin can exacerbate symptoms among those with chronic hives, or create acute symptoms of hives.^[187] These responses can be due to allergic reactions to aspirin, or more often due to its effect of inhibiting the COX-1 enzyme.^[187][188] Skin reactions may also tie to systemic contraindications, seen with NSAID-precipitated bronchospasm,^[187][188] or those with atopy.^[189]

Aspirin and other NSAIDs, such as ibuprofen, may delay the healing of skin wounds.^[190] Earlier findings from two small, low-quality trials suggested a benefit with aspirin (alongside compression therapy) on venous leg ulcer healing time and leg ulcer size,^{[191][192][193]} however larger, more recent studies of higher quality have been unable to corroborate these outcomes.^[194][195] As such, further research is required to clarify the role of aspirin in this context.

Other adverse effects[edit]

Aspirin can induce swelling of skin tissues in some people. In one study, angioedema appeared one to six hours after ingesting aspirin in some of the people. However, when the aspirin was taken alone, it did not cause angioedema in these people; the aspirin had been taken in combination with another NSAID-induced drug when angioedema appeared.^[196]

Aspirin causes an increased risk of cerebral microbleeds having the appearance on MRI scans of 5 to 10 mm or smaller, hypointense (dark holes) patches.^[197][198]

A study of a group with a mean dosage of aspirin of 270 mg per day estimated an average absolute risk increase in intracerebral hemorrhage (ICH) of 12 events per 10,000 persons.^[199] In comparison, the estimated absolute risk reduction in myocardial infarction was 137 events per 10,000 persons, and a reduction of 39 events per 10,000 persons in ischemic stroke.^[199] In cases where ICH already has occurred, aspirin use results in higher mortality, with a dose of about 250 mg per day resulting in a relative risk of death within three months after the ICH around 2.5 (95% confidence interval 1.3 to 4.6).^[200]

Aspirin and other NSAIDs can cause abnormally high blood levels of potassium by inducing a hyporeninemic hypoaldosteronic state via inhibition of prostaglandin synthesis; however, these agents do not typically cause hyperkalemia by themselves in the setting of normal renal function and euvolemic state.^[201]

Use of low-dose aspirin before a surgical procedure has been associated with an increased risk of bleeding events in some patients, however, ceasing aspirin prior to surgery has also been associated with an increase in major adverse cardiac events. An analysis of multiple studies found a three-fold increase in adverse events such as myocardial infarction in patients who ceased aspirin prior to surgery. The analysis found that the risk is dependent on the type of surgery being performed and the patient indication for aspirin use.^[202]

On 9 July 2015, the US Food and Drug Administration (FDA) toughened warnings of increased heart attack and stroke risk associated with nonsteroidal anti-inflammatory drugs (NSAID).^[203] Aspirin is an NSAID but is not affected by the new warnings.^[203]

Overdose[edit]

Aspirin overdose can be acute or chronic. In acute poisoning, a single large dose is taken; in chronic poisoning, higher than normal doses are taken over a period of time. Acute overdose has a mortality rate of 2%. Chronic overdose is more commonly lethal, with a mortality rate of 25%;^[204] chronic overdose may be especially severe in children.^[205] Toxicity is managed with a number of potential treatments, including activated charcoal, intravenous dextrose and normal saline, sodium bicarbonate, and dialysis.^[206] The diagnosis of poisoning usually involves measurement of plasma salicylate, the active metabolite of aspirin, by automated spectrophotometric methods. Plasma salicylate levels in general range from 30 to 100 mg/L after usual therapeutic doses, 50–300 mg/L in people taking high doses and 700–1400 mg/L following acute overdose. Salicylate is also produced as a result of exposure to bismuth subsalicylate, methyl salicylate, and sodium salicylate.^[207][208]

Interactions[edit]

Aspirin is known to interact with other drugs. For example, acetazolamide and ammonium chloride are known to enhance the intoxicating effect of salicylates, and alcohol also increases the gastrointestinal bleeding associated with these types of drugs.^[163][164] Aspirin is known to displace a number of drugs from protein-binding sites in the blood, including the antidiabetic drugs tolbutamide and chlorpropamide, warfarin, methotrexate, phenytoin, probenecid, valproic acid (as well as interfering with beta oxidation, an important part of valproate metabolism), and other NSAIDs. Corticosteroids may also reduce the concentration of aspirin. Other NSAIDs, such as ibuprofen and naproxen, may reduce the antiplatelet effect of aspirin.^[209][210] Although limited evidence suggests this may not result in a reduced cardioprotective effect of aspirin.^[209] Analgesic doses of aspirin decrease sodium loss induced by spironolactone in the urine, however this does not reduce the antihypertensive effects of spironolactone.^[211] Furthermore, antiplatelet doses of aspirin are deemed too small to produce an interaction with spironolactone.^[212] Aspirin is known to compete with penicillin G for renal tubular secretion.^[213] Aspirin may also inhibit the absorption of vitamin C.^{[214][215][unreliable medical source?][216]}

Research[edit]

The ISIS-2 trial demonstrated that aspirin at doses of 160 mg daily for one month, decreased the mortality by 21% of participants with a suspected myocardial infarction in the first five weeks.^[217] A single daily dose of 324 mg of aspirin for 12 weeks has a highly protective effect against acute myocardial infarction and death in men with unstable angina.^[218]

Bipolar disorder[edit]

Aspirin has been repurposed as an add-on treatment for depressive episodes in subjects with bipolar disorder.^[131] However, meta-analytic evidence is based on very few studies and does not suggest any efficacy of aspirin in the treatment of bipolar depression.^[131] Thus, notwithstanding the biological rationale, the clinical perspectives of aspirin and anti-inflammatory agents in the treatment of bipolar depression remain uncertain.^[131]

Infectious diseases[edit]

Several studies investigated the anti-infective properties of aspirin for bacterial, viral and parasitic infections. Aspirin was demonstrated to limit platelet activation induced by Staphylococcus aureus and Enterococcus faecalis and to reduce streptococcal adhesion to heart valves. In patients with tuberculous meningitis, the addition of aspirin reduced the risk of new cerebral infarction [RR = 0.52 (0.29-0.92)]. A role of aspirin on bacterial and fungal biofilm is also being supported by growing evidence.^[219]

Cancer prevention[edit]

Aspirin might weakly reduce the risk of breast cancer per a 2020 meta-analysis.^[220]

In gardening[edit]

There are a many anecdotal reportings that aspirin can improve plant’s growth and resistance^[221][222] though most research involved salicylic acid instead of aspirin.^[223]

Veterinary medicine[edit]

Aspirin is sometimes used in veterinary medicine as an anticoagulant or to relieve pain associated with musculoskeletal inflammation or osteoarthritis. Aspirin should only be given to animals under the direct supervision of a veterinarian, as adverse effects—including gastrointestinal issues—are common. An aspirin overdose in any species may result in salicylate poisoning, characterized by hemorrhaging, seizures, coma, and even death.^[224]

Dogs are better able to tolerate aspirin than cats are.^[225] Cats metabolize aspirin slowly because they lack the glucuronide conjugates that aid in the excretion of aspirin, making it potentially toxic if dosing is not spaced out properly.^[224][226] No clinical signs of toxicosis occurred when cats were given 25 mg/kg of aspirin every 48 hours for 4 weeks,^[225] but the recommended dose for relief of pain and fever and for treating blood clotting diseases in cats is 10 mg/kg every 48 hours to allow for metabolization.^[224][227]

See also[edit]

• Fluoroaspirin

References[edit]

Further reading[edit]

• McTavish, Jan R. (Fall 1987). «What’s in a name? Aspirin and the American Medical Association». Bulletin of the History of Medicine. 61.3: 343–366. JSTOR 44442097. On loss of patent in the US in 1917.

External links[edit]

• «Aspirin». Drug Information Portal. U.S. National Library of Medicine.
• Ling G (2005). «Aspirin». How Products Are Made. Vol. 1. Thomson Gale.

Состав Аспирина

В состав таблеток входят 500 мг ацетилсалициловой кислоты (АСК), а также кукурузный крахмал и микрокристаллическая целлюлоза.

Форма выпуска

Форма выпуска препарата — таблетки.

Фармакологическое действие

Препарат снимает воспаление и боль, а также действует как антипиретик и дезагрегант.

Фармакологическая группа: НПВС — производные салициловой кислоты.

Фармакодинамика и фармакокинетика

Что такое Аспирин?

Активное вещество препарата — ацетилсалициловая кислота (иногда ее ошибочно называют “ацетиловая кислота”) — относится к группе нестероидных противовоспалительных ЛС, механизм действия которых реализуется за счет необратимой инактивации энзима COX, играющего важную роль в синтезе тромбоксанов и Pg.

Таким образом, на вопрос ацетилсалициловая кислота — это аспирин или нет, можно с уверенностью ответить, что Аспирин и ацетилсалициловая кислота — одно и то же .

Природный источник Аспирина: кора Sаlix аlba (ивы белой).

Химическая формула Аспирина: C₉H₈O₄.

Фармакодинамика

Пероральный прием АСК в дозе от 300 мг до 1 г способствует облегчению боли (в том числе мышечной и суставной) и состояний, которые сопровождаются легкой лихорадкой (например, при простуде или гриппе). Аналогичные дозы АСК назначаются от температуры.

Свойства АСК позволяют применять препарат также при острых и хронических воспалительных заболеваниях. В списке показаний, от чего помогает Аспирин, перечисляются остеоартриты, ревматоидный артрит, болезнь Бехтерева.

При указанных заболеваниях применяются, как правило, более высокие, чем, например, при температуре или при простуде, дозы. Для облегчения состояния взрослому, в зависимости от особенностей течения болезни, назначают от 4 до 8 г АСК в сутки.

За счет блокирования синтеза тромбоксана А2 АСК подавляет агрегацию тромбоцитов. Это делает целесообразным ее применение при большом количестве заболеваний сосудов. Суточная доза при такого рода патологиях варьируется в пределах от 75 до 300 мг.

Фармакокинетика

После приема таблетки Аспирина АСК быстро и полностью всасывается из ЖКТ. Во время и после абсорбции она биотрансформируется в салициловую кислоту (СК) — основной, фармакологически активный метаболит.

ТСмах АСК — 10-20 минут, салицилатов — от 20 минут до 2 часов. АСК и СК полностью связываются в крови с плазменным белками и быстро распределяются в организме. СК проникает через плаценту и попадает в грудное молоко.

В метаболизме СК участвует печень. Продуктами метаболизма вещества являются: гентизиновая, гентизинмочевая, салицилмочевая кислоты, а также салицилацил и салицилфенол глюкурониды.

Кинетика выведения СК зависит от дозы, поскольку метаболизм ограничен активностью печеночных ферментов. Т1/2 также дозозависимая величина: в случае применения низких доз Т1/2 — от 2 до 3 часов, в случае применения высоких доз — увеличивается до 15 часов.

Выводятся СК и продукты ее метаболизм главным образом почками.

Показания к применению Аспирина

Аспирин (АСК) — это симптоматическое средство, которое применяется при состояниях, сопровождающихся болью, воспалением и лихорадкой.

Показания к применению:

• головная боль;
• зубная боль;
• альгодисменорея;
• боль в горле, причиной которой является простуда;
• мышечная и суставная боль;
• боль в спине;
• ОРВИ и простуда;
• умеренные боли при воспалении суставов.

Противопоказания на Аспирин

Противопоказания делятся на абсолютные и относительные.

Прием препарата категорически запрещен при аллергии на АСК или любые другие нестероидные противовоспалительным ЛС (Анальгин, Парацетамол и пр.), а также при состояниях, которые характеризуются повышенной склонностью к кровотечению.

Относительными являются следующие противопоказания:

• одновременный прием антикоагулянтов;
• недостаточность цитозольного фермента G6PD;
• бронхиальная астма;
• нарушение функции почек;
• хронические болезни желудка и двенадцатиперстной кишки;
• сахарный диабет;
• подагра;
• детский возраст до 12 лет;
• беременность;
• лактация.

При наличии относительных противопоказаний Аспирин Байер можно принимать только после того, как это одобрит доктор.

Побочные действия

Побочные действия:

• реакции гиперчувствительности (высыпания на коже, бронхоспазм);
• снижение уровня тромбоцитов в крови;
• боли в желудке.

Частое и длительное применение АСК в отдельных случаях может сопровождаться развитием кровотечения из ЖКТ, признаками которого являются:

• дегтеобразный стул;
• анемия;
• общая слабость;
• упорные боли в животе.

Появление подобных симптомов требует прекращения приема Аспирина и немедленного обращения к врачу.

Продолжительное лечение высокими дозами АСК также может спровоцировать:

• повреждение юкстагломерулярного аппарата (околоклубочкового комплекса) почек;
• образование оксалатных и/или уратных конкрементов в мочевыводящих путях и почках;
• почечную недостаточность;
• повреждение инсулярного аппарата ПЖЖ;
• нарушение синтеза гликогена (в некоторых случаях вплоть до развития сахарного диабета);
• тромбоцитоз;
• дистрофию миокарда;
• гемолитическую анемию, эритроцитопению, гиперпротромбинемию, нейтрофильный лейкоцитоз;
• снижение проницаемости капилляров (возможно повышение АД и ухудшение трофики тканей);
• гемолиз эритроцитов (у больных с недостаточностью G6PD);
• нарушение обмена меди и цинка;
• дисбактериоз ротовой полости.

Таблетки Аспирин, инструкция по применению

В инструкции по применению Аспирина указывается, что таблетки следует принимать внутрь после еды с достаточным количеством жидкости.

Максимальная продолжительность лечения препаратом без консультации врача — 5 дней.

В качестве одноразовой дозы взрослым назначают от 300 мг до 1 г АСК. Повторный прием возможен через 4-8 часов. Допустимый верхний предел суточной дозы — 4 г.

Аспирин: как пить для профилактики болезней сердца и сосудов?

Систематический обзор различных исследований показал, что применение Аспирина после перенесенного инфаркта миокарда позволяет снизить на 31% частоту нефатальных инфарктов, на 39% — частоту нефатальных инсультов, на 25% — частоту рецидивирующих инсультов и инфарктов, а также на 15% — сосудистой смерти.

При этом положительный эффект АСК не зависит от пола, возраста, наличия сахарного диабета и показателей артериального давления.

В ходе исследований было установлено, что после инфаркта миокарда АСК должна назначаться немедленно, а лечение должно продолжаться до тех пор, пока не будут выявлены специфические противопоказания. Оптимальная дозировка для профилактики сосудов — 160-325 мг/сут.

Чем запивать Аспирин?

Запивать таблетки Аспирина рекомендуется молоком, киселем или гидрокарбонатно-натриевой минеральной водой.

Аспирин для разжижения крови: разжижает ли кровь АСК?

АСК является дезагрегантом. Это свойство препарата позволяет применять его при состояниях, когда нужно создать препятствия для индуцированной или спонтанной агрегации тромбоцитов.

Существует 2 группы кроверазжижающих препаратов: без АСК и на основе этого вещества. Препараты, разжижающие кровь, без АСК — это антикоагулянты. Лекарства, основой которых является АСК, относятся к группе антиагрегантов.

На вопрос, разжижает кровь или нет Аспирин, врачи отвечают, что смысл воздействия дезагрегантов (и, в частности, АСК) заключается в в том, что они понижают способность тромбоцитов склеиваться, а это в свою очередь снижает риск образования тромбов.

Для чего нужен Аспирин? В инструкции и в Википедии на этот счет приводятся следующие рекомендации: препарат следует назначать пациентам с высоким сердечно-сосудистым риском, людям, перенесшим инфаркт миокарда, а также в острый период ишемического инсульта, при нарушениях кровообращения в головном мозге и иных проявлениях атеросклероза.

Елена Малышева про препарат говорит следующее: “Лекарство от старости. Нет тромбов в сосудах, хороший кровоток в мозге, в сердце, в ногах, в руках. В коже!”. Также она отмечает, что средство снижает риск атеросклероза и защищает организм от рака.

Советы относительно того, как принимать Аспирин для разжижения крови правильно, следующие: оптимальной дозой лекарства в случае его применения для профилактики сосудистых осложнений является доза, равная 75-100 мг/сут. Именно такая доза считается наиболее хорошо сбалансированной в соотношении безопасности/эффективности.

Западные врачи не практикуют применение Аспирина для разжижения крови, тем не менее, в России его для этих целей рекомендуют довольно часто. Зная о пользе АСК для сосудов, некоторые люди начинают принимать препарат бесконтрольно.

Медики же не устают напоминать о том, что перед тем как пить Аспирин для очищения сосудистых стенок от холестерина и “размягчения” крови, необходимо получить одобрение врача.

Чем вреден Аспирин? Исследования, которые проводились учеными в 70-х годах XX века, показали, что препараты АСК оказывают влияние на вязкость крови, тем самым способствуя уменьшению нагрузки на сердечную мышцу и препятствуя повышению АД.

Однако для достижения этих эффектов обычно достаточно 50-75 мг вещества в сутки. Регулярное же превышение рекомендуемой профилактической дозы может дать прямо противоположные результаты и нанести организму вред.

Иными словами, прием АСК для разжижения крови, если нет никаких признаков болезней сердца, на организме сказывается отрицательно.

Чем заменить АСК?

Нередко пациенты задаются вопросом, что разжижает кровь кроме Аспирина. В качестве альтернативы лекарствам можно использовать отдельные продукты, разжижающие кровь, — аналоги антиагрегантов.

Основными из них являются те, в которых содержатся салициловая кислота, витамин Е и йод. Растительными заменителями Аспирина считаются солодка, шалфей, алоэ, конский каштан. Также для разжижения крови хорошо вводить в рацион вишню, апельсины, клюкву, изюм, виноград, мандарины, чернику, тимьян, мяту, имбирь и карри.

Мясо, рыба и молочные продукты не способствуют разжижению крови, однако регулярное употребление рыбы способствует улучшению картины крови. Кровь становится менее вязкой и в том случае, когда организм получает достаточное количество витамина D.

Беременным женщинам разжижать кровь рекомендуется при помощи баклажанов, кабачков, капусты, репчатого лука, хрена, стручкового перца, лимонов, гранатов, смородины, клюквы, калины.

Понижает или повышает давление Аспирин? Аспирин от головной боли

Аспирин от головной боли в особенности эффективен, если причиной боли является повышенное внутричерепное давление (ВЧД). Это связано с тем, что АСК оказывает кроверазжижающее действие и таким образом способствует снижению ВЧД.

Взрослым при головной боли (в зависимости от ее интенсивности) обычно назначают принимать от 0,25 до 1 г АСК через каждые 6-8 часов.

Как принимать для профилактики Аспирин при варикозе?

Действие АСК направлено на подавление функции тромбоцитов. Как следствие, при варикозе регулярное применение препарата способствует снижению риска тромбообразования.

Тем не менее, врачи на вопрос “Можно ли пить каждый день Аспирин?” отвечают, что злоупотреблять этим препаратом при варикозной болезни все же не стоит. Оптимальный способ применения средства — специальные лечебные компрессы.

Для приготовления компресса рекомендуется залить 200 мл спирта (водки) размолотые таблетки Аспирина (10 штук) и настоять лекарство в течение 48 часов. Компрессы прикладывают к области расширенных вен ежедневно, на ночь. Такая процедура при варикозной болезни помогает устранить болевой синдром.

Чем полезен Аспирин в косметологии?

В косметологии АСК применяется для волос (в частности, в качестве средства от перхоти), для лечения прыщей и улучшения кожи. Эффективность средства подтверждают большое количество положительных отзывов и картинки, на которых можно оценить внешний вид лица до и после применения Аспирина.

Для кожи лица АСК используют в составе кремов для ежедневного ухода, а также в составе масок. Польза такого лечения для лица заключается в том, что с кожи достаточно быстро — в течение нескольких часов — исчезают воспаления и покраснения и спадает отек тканей.

Кроме того, маски для лица с Аспирином способствуют отшелушиванию слоя отмерших клеток и очистке пор от подкожного сала.

На вопрос, как помогает от прыщей на лице Аспирин, косметологи отвечают, что свойство очищать поры обусловлено подсушивающим действием и хорошей растворимостью в жирах, благодаря которой АСК может проникать достаточно глубоко в забитые кожным салом поры.

Легкий пилинг гарантируется за счет зернистой структуры растворенного препарата. При этом средство не травмирует здоровые участки кожи. Это обусловлено тем, что, АСК работает несколько иначе, чем абразивные скрабы, отшелушивающий эффект которых реализуется за счет наличия в их составе грубых частичек.

Действие АСК, в отличие от таких средств, направлено на ослабление клейких связей между клетками, что в свою очередь помогает удалять мертвые клетки с поверхности кожи, не повреждая молодые здоровые клетки в более глубоких слоях.

Самый простой рецепт против прыщей — положить на воспалившееся место половинку таблетки препарата.

Также можно добавить измельченные таблетки Аспирина в крем. Для приготовления состава, 4 таблетки препарата помещают в миску и капают на них водой. Когда лекарство начнет растворяться, его растирают пальцами до кашицеобразной консистенции и затем при помощи шпателя перемешивают с 2 ст. ложками крема.

Чтобы средство от прыщей имело более тонкую текстуру, к смеси можно влить до 1 ст. ложки теплой воды. Крем наносят на лицо, а через 15 минут смывают теплой водой.

Аспирин от прыщей можно использовать и в сочетании со свежевыжатым соком лимона.

Рецепт такой маски из Аспирина против прыщей простой: 6 таблеток препарата растирают с лимонным с соком до получения однородной массы (отзывы позволяют сделать вывод, что процесс растворения таблеток может растянуться минут на 10), а затем полученную пасту наносят точечно на прыщи и оставляют подсыхать.

Удалять пасту с кожи для нейтрализации кислоты рекомендуется раствором питьевой соды.

Хорошие отзывы и о маске для лица с Аспирином и медом. Для приготовления лечебного состава, нужно поместить в мисочку 3 таблетки (используется не шипучий Аспирин УПСА, а обычные таблетки) и капнуть на них водой. Когда таблетки станут рыхлыми, к ним добавляют 0,5-1 ч. ложку меда и тщательно перемешивают.

Если мед слишком густой, можно добавить к смеси несколько капель воды. Маску наносят на сухую кожу на 15 минут, а затем аккуратно, круговыми движениями умывают лицо теплой водой.

Больше всего подходит маска из меда и Аспирина для увядающей, жирной и пористой кожи, но косметологи говорят, что можно использовать такую маску с медом и от прыщей.

Хороша маска от прыщей с Аспирином и глиной. Для ее приготовления нужно взять 6 таблеток АСК, 2 ч. ложки косметической глины (голубой или белой) и небольшое количество теплой воды.

Все ингредиенты размешивают в удобной емкости до получения кашицы, после чего состав на 15 минут наносят при помощи ватного диска на лицо. При появлении неприятных ощущений (жжения, зуда) маску можно смыть раньше. После процедуры кожу рекомендуется протереть смоченным в отваре ромашки или череды спонжем.

Для устранения мелких акне и черных точек Аспирин используют в сочетании с газированной минеральной водой и черной косметической глиной. На 1 ст. ложку глины нужно брать 1 таблетку АСК. Вначале глину разводят минеральной водой, затем к полученной кашице добавляют Аспирин.

Состав наносят на кожу тонким слоем. Время воздействия — 20 минут. Крем после процедуры рекомендуется накладывать не раньше чем через 10-15 минут (это даст коже “подышать”).

Эффективны от прыщей Левомицетин, календула и Аспирин в виде болтушки. Для приготовления средства к 40 мл настойки календулы добавляют по 4 таблетки каждого препарата и хорошо взбалтывают флакончик. Раствор используют для протирания лица.

Чистку лица с помощью Аспирина проводят с использованием только лишь таблеток в чистом виде. Следует помнить, что в продаже имеются разные виды АСК. Однако для пилинга следует использовать таблетки без дополнительного покрытия, Аспирин в оболочке для этих целей не используют.

Размокшую таблетку препарата кладут на ватный диск, а затем круговыми движениями наносят на кожу лица на 3 минуты и затем смывают теплой водой.

От черных точек, против прыщей (комедонов) и для профилактики появления угревой сыпи можно использовать Аспирин в составе маски с кофе и глиной. На 2 ст. ложки белой или голубой косметической глины рекомендуется использовать 1 ч. ложку натурального кофе среднего помола и 4 таблетки АСК.

К готовой смеси небольшими порциями вливают газированную минеральную воду в количестве, необходимом для получения густой кашицы. На кожу средство наносят медленными массирующими движениями, покрывая все участки, кроме области верхнего и нижнего века. Время воздействия — 20 минут, после этого маску смывают. Чтобы усилить эффект, проблемные зоны можно протереть кубиком льда.

Аспирин для волос применяется главным образом как средство от перхоти. Самым простым способом лечения болезней волос является использование шампуня с АСК.

Для приготовления целебного состава, в отдельную емкость отмеряют необходимое для одного мытья головы количество шампуня (лучше, если он будет содержать минимум красителей и отдушек), а затем добавляют в него 2 измельченные таблетки АСК (без покрытия).

Передозировка

Симптомами передозировки средней тяжести являются: шум в ушах, тошнота, нарушение слуха, рвота, спутанность сознания, головокружение, головная боль. Перечисленные явления исчезают при снижении дозы препарата.

Тяжелая передозировка Аспирином сопровождается гипервентиляцией, лихорадкой, метаболическим ацидозом, респираторным алкалозом, кетозом, кардиогенным шоком, комой, выраженной гипогликемией, дыхательной недостаточностью.

В подобных случаях больного госпитализируют. Лечение включает прием активированного угля, лаваж, контроль КЩР, форсированный щелочной диурез для получения значений рН мочи в пределах 7.5-8.0, компенсацию потери жидкости, гемодиализ, симптоматическую терапию.

Взаимодействие

АСК усиливает эффекты нестероидных противовоспалительных ЛС (по этой причине врачи не рекомендуют принимать Аспирин с другими препаратами этой группы, например, одновременно с Парацетамолом), ненаркотических анальгетиков, пероральных гипогликемических ЛС, непрямых антикоагулянтов, Гепарина, тромболитиков, подавляющих агрегацию тромбоцитов, трийодтиронина, сульфаниламидов.

Снижает эффекты диуретиков, урикозурических препаратов, гипотензивных средств.

ГКС, алкоголь и содержащие этанол препараты усиливают повреждающее действие АСК на слизистую оболочку пищеварительного канала, повышают риск развития желудочных и кишечных кровотечений.

АСК повышает плазменную концентрацию препаратов Li, барбитуратов и дигоксина.

Всасывание АСК ухудшается и замедляется при одновременном приеме препарата с содержащими гидроксид Al и/или Mg антацидами.

Условия продажи

Без рецепта.

Рецепт на латинском на препарат (образец): Rp.: Tab. Acidi acetylsalicylici 0,1 №10 D. S. При подозрении на ОИМ принимать по 1 таблетке 2 раза в день.

Условия хранения

Таблетки должны храниться в недоступном для детей, защищенном от света и влаги месте.

Срок годности

Пять лет.

Особые указания

АСК может вызвать реакции повышенной чувствительности (например, приступ бронхиальной астмы (БА) или бронхоспазм). Факторами риска являются наличие в анамнезе БА, полипов носа, лихорадки, бронхо-легочных заболеваний в хронической форме, случаев аллергии (кожные проявления аллергии, аллергические риниты).

АСК способна повысить склонность к кровоточивости, что обусловлено ее ингибирующим воздействием на агрегацию тромбоцитов. Это нужно учитывать, назначая препарат пациентам, которым предстоит хирургическое вмешательство (в том числе небольшое, например, удаление зуба).

Прием препарата прекращают за 5-7 дней до операции. Врач должен быть проинформирован о том, что перед хирургическим вмешательством пациент принимал Аспирин.

АСК уменьшает выведение мочевой кислоты из организма, что у предрасположенных пациентов может спровоцировать острый приступ подагры.

Аспирин — польза или вред?

АСК широко применяется в качестве обезболивающего, жаропонижающего и противовоспалительного средства. В более низких дозах она применяется для профилактики развития сосудистых осложнений.

На сегодняшний день АСК — это единственный дезагрегант, эффективность которого при использовании в остром периоде ишемического инсульта (инфаркта мозга) подкреплена данными доказательной медицины.

При регулярном приеме АСК существенно снижается риск колоректального рака, а также рака простаты, легких, пищевода и горла.

Важной особенностью АСК является то, что она необратимо подавляет COX — фермент, который задействован в синтезе тромбоксанов и Pg. Действуя как ацетилирующий агент, АСК присоединяется к остатку серина в активном центре COX ацетильную группу. Это отличает препарат от других НПВП (в частности, от ибупрофена и диклофенака), которые относятся к группе обратимых ингибиторов COX.

Бодибилдеры используют комбинацию “Аспирин-Кофеин-Бронхолитин” в качестве жиросжигателя (такая смесь считается прародителем всех сжигателей жира). Домохозяйки нашли применение АСК и в быту: средство нередко применяется для удаления пятен пота с белой одежды и для полива пораженной грибком почвы.

Можно использовать АСК и для цветов: измельченную таблетку Аспирина добавляют в воду, когда хотят подольше сохранить срезанные растения.

Некоторые женщины используют таблетки Аспирина как противозачаточное средство: таблетку вводят интравагинально за 10-15 минут до ПА или же растворяют ее в воде и затем спринцуются полученным раствором.

Действенность такого способа предохранения от беременности исследованиям не подвергалась, однако, право на его существование гинекологами не отрицается. При этом врачи отмечают, что эффективность контрацепции с применением АСК всего лишь около 10%.

Также бытует мнение, что при помощи Аспирина можно прервать беременность. Врачи таких способов, конечно, не приветствуют, а советуют в случае, если беременность не запланирована и нежелательна, все-таки своевременно обращаться за помощью в медицинские учреждения.

Несмотря на большое количество полезных свойств, препарат имеет и дурную славу. Подавление активности СОХ провоцирует нарушение целостности стенок пищеварительного канала и является фактором развития язвенной болезни.

Также опасной АСК может быть для детей до 12 лет. В случае применения при наличии у ребенка вирусной инфекции препарат может стать причиной синдрома Рея — заболевания, представляющего угрозу для жизни маленьких пациентов.

Аналоги Аспирина

Совпадения по коду АТХ 4-го уровня:

Структурные аналоги: Ацетилсалициловая кислота, Аспирин УПСА, Тромбо Асс, Таспир, Флуспирин, Аспровит, Аспирин “Йорк” (или “американский аспирин” — по-другому как называется этот препарат).

Чем можно заменить Аспирин?

Аналоги с близким механизмом действия: Аспирин Комплекс, Аскофен-П, Цитрапар, Натрия салицилат, Кофицил-Плюс, Аспровит-С, Аспагель, Алька-Прим, АнГрикапс, Цефекон Н.

Что лучше: Аспирин или Аспирин Кардио?

На вопрос, чем отличается Аспирин и Аспирина Кардио, врачи отвечают, что отличиями препаратов являются дозировка активного вещества (меньшая в Аспирине Кардио) и то, что таблетки Аспирин Кардио выпускаются в специальной кишечнорастворимой оболочке, которая защищает слизистую пищеварительного канала от агрессивного действия АСК.

Аспирин и Аспирин Кардио имеют разные показания к применению. Первый (в нем содержится 500 мг АСК) применяется в качестве обезболивающего, жаропонижающего и противовоспалительного средства, Аспирин Кардио, концентрация АСК в котором 100 или 300 мг/таб., назначают для профилактики и лечения:

• тромбозов и эмболии после АКШ, трансдермальной внутрисосудистой коронарной ангиопластики и других операций на сосудах;
• инфаркта миокарда;
• нестабильной стенокардии;
• проходящих нарушений кровотока в мозге и инсульта на преморбидной стадии;
• тромбоза коронарных артерий у относящихся к группе риска пациентов;
• мигрени (в том числе для долговременной профилактики).

Можно ли давать детям Аспирин?

Детям Аспирин рекомендуется давать с 12-тилетнего возраста.

Давать детям при температуре, поднимающейся на фоне вирусной инфекции препараты, в которых содержится АСК, запрещено, поскольку АСК действует на те же структуры печени и мозга, что и некоторые вирусы.

Таким образом, сочетание Аспирина и вирусной инфекции может стать причиной развития синдрома Рея — заболевания, при котором поражаются головной мозг и печень, и от которого умирает примерно каждый пятый маленький пациент.

Риск развития синдрома Рея повышается в случаях, когда АСК используется как сопутствующее ЛС, однако доказательств причинно-следственной связи в подобных случаях нет. Одним из признаков синдрома Рея является продолжительная рвота.

Как одноразовая доза детям до трех лет обычно дается 100 мг, детям четырех-шести лет — 200 мг, а детям семи-девяти лет — 300 мг АСК.

Рекомендованная доза для ребенка — 60 мг/кг/сут., разделенные на 4-6 приемов, или 15 мг/кг через каждые 6 часов или 10 мг/кг через каждые 4 часа. У детей, не достигших трехлетнего возраста, препарат в данной лекарственной форме не применяется.

Совместимость с алкоголем

Можно ли пить с алкоголем Аспирин?

Аспирин и алкоголь несовместимы. Имеются описания случаев, когда прием даже 40 г алкоголя в сочетании с препаратом сопровождался развитием желудочных кровотечений и тяжелых аллергических реакций.

Помогает ли от похмелья Аспирин?

Аспирин при похмелье весьма эффективен, благодаря способности АСК препятствовать агрегации тромбоцитов (как спонтанной, так и индуцированной).

На вопрос, можно ли пить с похмелья Аспирин, врачи отвечают, что препарат лучше употреблять не после алкоголя, а примерно за 2 часа до планируемого застолья. Это позволит предотвратить микротромбирование в мелких кровеносных сосудах мозга и — отчасти — отек тканей.

При похмелье лучше всего принимать быстро растворимый Аспирин, например, Упсарин УПСА. Последний меньше раздражает слизистую ЖКТ, а содержащаяся в нем лимонная кислота активирует переработку недоокисленных продуктов распада алкоголя. Оптимальная дозировка — 500 мг на каждые 35 кг массы тела.

Аспирин при беременности

Можно ли пить Аспирин при беременности на ранних сроках?

Применение салицилатов в первые три месяца в отдельных ретроспективных эпидемиологических исследованиях ассоциировалось с повышенным риском развития врожденных дефектов (включая пороки сердца и расщепление твердого неба).

Тем не менее, при длительном применении препарата в терапевтических дозах, которые не превышают 150 мг/сут., этот риск оказался низким. У 32 тысяч пар “мать-ребенок” в ходе исследований не было выявлено связи между применением Аспирина и увеличением количества врожденных пороков развития.

Во время беременности АСК следует принимать только после оценки соотношения риск для ребенка/польза для матери. В случае необходимости продолжительного применения Аспирина, суточная доза АСК не должна превышать 150 мг.

Аспирин для беременных в 3 триместре

В последние месяцы беременности прием высоких (более 300 мг/сут.) доз салицилатов может стать причиной перенашивания беременности и ослабления схваток во время родов.

Кроме того, лечение Аспирином в таких дозах может привести к преждевременному закрытию у ребенка ductus arteriosus (кардиопульмональной токсичности).

Применение высоких доз АСК незадолго до родов может спровоцировать внутричерепное кровотечение, в особенности у недоношенных детей.

Исходя из этого, кроме исключительных случаев, обусловленных акушерскими и кардиологическими медицинскими показаниями с использованием специального мониторинга, применение АСК в последнем триместре беременности противопоказано.

Можно ли при грудном вскармливании Аспирин?

Салицилаты и продукты их метаболизма в небольшом количестве проникают в молоко. Поскольку побочные эффекты у младенцев после случайного применения препарата не отмечались, прерывать ГВ, как правило, не требуется.

При необходимости длительного лечения препаратом в высоких дозах необходимо решить вопрос о прекращении кормления грудью.

Отзывы об Аспирине

Аспирин — это лекарство, знакомое каждому. Его эффективность клинически апробирована, а профиль безопасности и механизм действия досконально изучены. ВОЗ включила АСК в список важнейших препаратов.

Свойства АСК позволяют использовать Аспирин для купирования боли и воспаления, для снижения повышенной температуры и ВЧД, а также для профилактики сосудистых осложнений.

Наряду с отзывами об использовании АСК по прямому назначению женщины оставляют также хорошие отзывы о чистке лица с Аспирином и отзывы о применении препарата для волос. Немало положительных отзывов и о маске “Аспирин с медом”, которая в косметологии используется как средство от прыщей.

Аспирин хорошо лечит воспаленные элементы, снимает отек тканей и способствует отшелушиванию отмерших клеток, мед для кожи лица полезен тем, что, проникая в глубокие слои, прекрасно питает и очищает кожу, предотвращает испарение влаги из кожи, обладает вяжущим, подтягивающим и тонизирующим действием.

Цена Аспирина, сколько стоят таблетки

Цена Аспирина 500 мг №10 в России — 225 руб. Цена Аспирина Кардио 300 мг №20 — от 80 руб., 100 мг №28 — от 130 руб. Купить шипучий Аспирин Байер можно в среднем за 200 руб. (цена за 10 таблеток), Упсарин УПСА — от 170 руб. за 16 таблеток.

Стоимость препарата Тромбо Асс — от 45 руб.

АСПИРИН

Аспирин
Действующее вещество
›› Ацетилсалициловая кислота (Acetylsalicylic acid)
Латинское название
Aspirin
АТХ:
›› N02BA01 Ацетилсалициловая кислота
Фармакологическая группа: НПВС — Производные салициловой кислоты
Нозологическая классификация (МКБ-10)
›› K08.8.0* Боль зубная
›› M25.5 Боль в суставе
›› M79.1 Миалгия
›› N94.6 Дисменорея неуточненная
›› R50.0 Лихорадка с ознобом
›› R51 Головная боль
Состав и форма выпуска
Таблетки1 табл.ацетилсалициловая кислота100 мгвспомогательные вещества: целлюлозный порошок — 10 мг; крахмал — 10 мг в блистере 10 шт.; в коробке 2 блистера.
Фармакологическое действие
Фармакологическое действие — анальгезирующее, жаропонижающее, противовоспалительное, антиагрегационное.
Показания
болевой синдром различной локализации (суставные, мышечные, головная, менструальные, зубная боли);
лихорадочные состояния.
Противопоказания
Абсолютные:
состояния, сопровождающиеся повышенной склонностью к кровотечению;
отмеченная ранее повышенная чувствительность к салицилатам и другим НПВС.
Относительные:
Аспирин 100 мг следует принимать только после консультации врача при следующих состояниях и заболеваниях:
одновременная терапия антикоагулянтами (производные кумарина, гепарин);
недостаточность глюкозо-6-фосфатдегидрогеназы;
бронхиальная астма;
хронические заболевания желудка и двенадцатиперстной кишки;
нарушение функции почек;
подагра;
сахарный диабет;
беременность;
лактация;
детский возраст до 12 лет.
Применение при беременности и кормлении грудью
Так как ацетилсалициловая кислота может проходить через плацентарный барьер и проникать в материнское молоко, применение Аспирина 100 мг при лактации и беременности, особенно в первом и последнем триместрах, возможно только после консультации врача.
Побочные действия
Аллергические реакции (бронхоспазм, кожная сыпь).
Боли в желудке.
Снижение числа тромбоцитов в крови.
При частом и длительном применении в редких случаях возможно развитие желудочно-кишечного кровотечения, которое сопровождается упорными болями в животе, черным (дегтеобразным) стулом, общей слабостью, анемией.При появлении подобных симптомов рекомендуется прекратить прием препарата и немедленно обратиться к врачу.
Взаимодействие
При одновременном назначении аспирина с антикоагулянтами (производными кумарина, гепарином) возрастает риск желудочно-кишечных кровотечений.
Аспирин может потенцировать нежелательные побочные эффекты кортикостероидов, других НПВС, сахаропонижающих (сульфонамиды) и противоопухолевых (метотрексат) препаратов.
Передозировка
Основные симптомы, которые могут наблюдаться при передозировке аспирина (более 3000 мг): головокружение, шум в ушах.
Способ применения и дозы
Внутрь. Взрослым разовая доза — 100 мг, рекомендуемая суточная доза — 300 мг (3 табл. в день). Аспирин 100 мг желательно принимать после еды, запивая достаточным количеством воды. Курс лечения не должен превышать 7–10 дней при отсутствии нежелательных побочных явлений. Более продолжительная терапия требует консультации лечащего врача. Назначение Аспирина 100 мг детям возможно только после консультации врача с учетом возможного риска развития синдрома Рейе — очень редкого, угрожающего жизни состояния, сопровождающегося развитием энцефалопатии и жировой дегенерации печени. Рекомендуемые дозы для детей: от 2 до 3 лет — 100 мг/сут (1 табл.), от 4 до 6 лет — 200 мг/сут (2 табл.), от 7 до 9 лет — 300 мг/сут (3 табл.).
Особые указания
В случаях, когда суточная доза превышает 300 мг, рекомендуется использовать препараты: Аспирин-С, содержащий 400 мг ацетилсалициловой кислоты, или Аспирин 500 мг.
Срок годности
5 лет
Условия хранения
Список Б.: В сухом, защищенном от света месте.
Словарь медицинских препаратов.2005.
Синонимы:
анопирин, апо-аса, аспилайт, аспирин упса, аспирин-директ, аспирин-кардио, аспиринчик, кислота ацетилсалициловая, лекарство, лекарство (повышение температуры, лихорадка)

АСПИРИН 1000 →← АСПИЗОЛ

Синонимы слова «АСПИРИН»:

АНОПИРИН, АПО-АСА, АСПИЛАЙТ, АСПИРИН УПСА, АСПИРИН-ДИРЕКТ, АСПИРИН-КАРДИО, АСПИРИНЧИК, КИСЛОТА АЦЕТИЛСАЛИЦИЛОВАЯ, ЛЕКАРСТВО, <<ЛЕКАРСТВО

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