Description

Simple

A painkiller used to treat pain, fever, inflammation, and migraines, as well as reduce the risk of heart attacks, strokes, and other events.

Clinical

A salicylate used to treat pain, fever, inflammation, migraines, and reducing the risk of major adverse cardiovascular events.

Overview

Also known as _Aspirin_, acetylsalicylic acid (ASA) is a commonly used drug for the treatment of pain and fever due to various causes. Acetylsalicylic acid has both anti-inflammatory and antipyretic effects. This drug also inhibits platelet aggregation and is used in the prevention of blood clots stroke, and myocardial infarction (MI) [FDA label].

Interestingly, the results of various studies have demonstrated that long-term use of acetylsalicylic acid may decrease the risk of various cancers, including colorectal, esophageal, breast, lung, prostate, liver and skin cancer [15]. Aspirin is classified as a _non-selective cyclooxygenase (COX) inhibitor_ [11, 14] and is available in many doses and forms, including chewable ta... Read more

Pharmacology

Indication

**Pain, fever, and inflammation**

Acetylsalicylic acid (ASA), in the regular tablet form (immediate-release), is indicated to relieve pain, fever, and inflammation associated with many conditions, including the flu, the common cold, neck and back pain, dysmenorrhea, headache, tooth pain, sprains,... Read more

Pharmacodynamic

**Effects on pain and fever**

Acetylsalicylic acid disrupts the production of prostaglandins throughout the body by targeting cyclooxygenase-1 (COX-1) and cyclooxygenase-2 (COX-2) [ Read more

Mechanism of action

Acetylsalicylic acid (ASA) blocks prostaglandin synthesis. It is non-selective for COX-1 and COX-2 enzymes [9, Read more

Absorption


Absorption is generally rapid and complete following oral administration but absorption may be variable depending on the route, dosage form, and other factors including but not limited to the rate of tablet dissolution, gastric contents, gastric emptying time, and gastric pH [FDA label].

**Deta... Read more

Protein binding

50% to 90% of a normal therapeutic concentration salicylate (a main metabolite of acetylsalicylic acid [FDA label]) binds plasma proteins, particularly albumin, while acetylsalicylic acid itself binds negligibly [FDA label]. Acetylsalicylic acid has the ability to bind to and acetylate many proteins... Read more

Volume of distribution

This drug is distributed to body tissues shortly after administration. It is known to cross the placenta. The plasma contains high levels of salicylate, as well as tissues such as spinal, peritoneal and synovial fluids, saliva and milk. The kidney, liver, heart, and lungs are also found to be rich i... Read more

Clearance

The clearance rate of acetylsalicylic acid is extremely variable, depending on several factors [6]. Dosage adjustments may be required in patient... Read more

Half life

The half-life of ASA in the circulation ranges from 13 - 19 minutes. Blood concentrations drop rapidly after complete absorption. The half-life of the salicylate ranges between 3.5 and 4.5 hours [FDA label].

Route of elimination

Excretion of salicylates occurs mainly through the kidney, by the processes of glomerular filtration and tubular excretion, in the form of free salicylic acid, salicyluric acid, and, additionally, phenolic and acyl glucuronides [FDA label].

Salicylate can be found in the urine soon after adminis... Read more

Toxicity

**Lethal doses**

Acute oral LD50 values have been reported as over 1.0 g/kg in humans, cats, and dogs, 0.92 g/kg - 1.48 g/kg in albino rats, 1.19 g/kg in guinea pigs, 1.1 g/kg in mice, and 1.8 g/kg in rabbit models [FDA label].

**Acute toxicity**

Salicylate toxicity is a problem that may de... Read more

Adverse Effects

Contraindications

  • Regions: Canada
  • Patient Conditions:
      • Name: Hypersensitivity to analgesics
      • Drugbank Id: DBCOND0119127
  • Regions: Canada
  • Patient Conditions:
      • Name: Hypersensitivity to antipyretics
      • Drugbank Id: DBCOND0119126
  • Regions: Canada
  • Patient Conditions:
      • Name: Hypersensitivity to acetylsalicylic acid
      • Drugbank Id: DBCOND0119125
  • Regions: Canada
  • Patient Conditions:
      • Name: Salicylate hypersensitivity
      • Drugbank Id: DBCOND0119124
  • Regions: Canada
  • Patient Conditions:
      • Name: Dose equal to 15mg/week or more
      • Drugbank Id: DBCOND0119123
  • With Drugs:
      • Name: Methotrexate
      • Drugbank Id: DB00563
  • Regions: US
  • Patient Conditions:
      • Name: History of asthma
      • Drugbank Id: DBCOND0107635
  • Patient Conditions Associated With:
      • Name: NSAID use
      • Drugbank Id: DBCOND0021294
      • Related Concepts:
          • Name: Antiinflammatory therapy
          • Drugbank Id: DBCOND0025182
      • Name: Salicylate use
      • Drugbank Id: DBCOND0119122
  • Regions: US
  • Patient Conditions:
      • Name: Congestive Heart Failure(CHF)
      • Drugbank Id: DBCOND0072976
  • Regions: US
  • Patient Conditions:
      • Name: Renal failure/acute renal failure
      • Drugbank Id: DBCOND0102751
  • Regions: Canada
  • Patient Conditions:
      • Name: Severe Hepatic Impairment
      • Drugbank Id: DBCOND0070791
      • Modification Of:
        • Base:
          • Name: Heptic Impairment
          • Drugbank Id: DBCOND0072269
        • Severity:
          • Includes:
            • severe
  • Regions: US
  • Patient Conditions:
      • Name: Acute hepatic failure
      • Drugbank Id: DBCOND0013188
      • Modification Of:
        • Base:
          • Name: Hepatic Failure
          • Drugbank Id: DBCOND0042778
        • Severity:
          • Includes:
            • acute
  • Regions: US
  • Patient Conditions:
      • Name: Hemorrhagic diathesis
      • Drugbank Id: DBCOND0102909
  • Route:
    • Oral
  • Dose Form:
    • Tablet
  • Regions: US
  • Patient Conditions:
      • Name: History of gastrointestinal ulcers
      • Drugbank Id: DBCOND0119121
  • Regions: US
  • Patient Conditions:
      • Name: Active peptic ulcer disease
      • Drugbank Id: DBCOND0107876
      • Modification Of:
        • Condition Status: active
        • Base:
          • Name: Peptic Ulcer Disease
          • Drugbank Id: DBCOND0045072
  • Regions: US
  • Patient Conditions:
      • Name: Third trimester of pregnancy
      • Drugbank Id: DBCOND0108315
  • Regions: US
  • Patient Conditions:
      • Name: Nasal Polyps
      • Drugbank Id: DBCOND0004147
  • Regions: US
  • Patient Conditions:
      • Name: Rhinitis
      • Drugbank Id: DBCOND0014062
  • Regions: US
  • Patient Conditions:
      • Name: Asthma
      • Drugbank Id: DBCOND0013565
  • Regions: US
  • Patient Conditions:
      • Name: Hypersensitivity to NSAIDS (nonsteroidal anti-inflammatory drugs)
      • Drugbank Id: DBCOND0119120

Food Interactions

  • Avoid alcohol. Alcohol increases the risk of gastrointestinal bleeding.
  • Take after a meal. This reduces irritating gastrointestinal effects.
  • Take with a full glass of water.

Interactions

Type in a drug name to check for interaction with Acetylsalicylic acid
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  • Paracetamol(acetaminophen)
  • Paxil(paroxetine)
  • Pamelor(nortriptyline)
  • Panadol(acetaminophen)
  • Patanol(olopatadine ophthalmic)
  • Pataday(olopatadine ophthalmic)
  • Parnate(tranylcypromine)
  • Pazeo(olopatadine ophthalmic)
(1,2,6,7-3H)Testosterone
(1,2,6,7-3H)Testosterone may increase the anticoagulant activities of Acetylsalicylic acid.
(R)-warfarin
Acetylsalicylic acid may increase the anticoagulant activities of (R)-warfarin.
(S)-Warfarin
Acetylsalicylic acid may increase the anticoagulant activities of (S)-Warfarin.
1-benzylimidazole
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 1-benzylimidazole.
1-Testosterone
1-Testosterone may increase the anticoagulant activities of Acetylsalicylic acid.
18-methyl-19-nortestosterone
18-methyl-19-nortestosterone may increase the anticoagulant activities of Acetylsalicylic acid.
2,4-thiazolidinedione
The risk or severity of hypoglycemia can be increased when Acetylsalicylic acid is combined with 2,4-thiazolidinedione.
2,5-Dimethoxy-4-ethylamphetamine
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 2,5-Dimethoxy-4-ethylamphetamine.
2,5-Dimethoxy-4-ethylthioamphetamine
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 2,5-Dimethoxy-4-ethylthioamphetamine.
3,5-Diiodotyrosine
3,5-Diiodotyrosine may increase the anticoagulant activities of Acetylsalicylic acid.
4-Bromo-2,5-dimethoxyamphetamine
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 4-Bromo-2,5-dimethoxyamphetamine.
4-hydroxycoumarin
Acetylsalicylic acid may increase the anticoagulant activities of 4-hydroxycoumarin.
4-Hydroxytestosterone
4-Hydroxytestosterone may increase the anticoagulant activities of Acetylsalicylic acid.
4-Methoxyamphetamine
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 4-Methoxyamphetamine.
5-methoxy-N,N-dimethyltryptamine
The risk or severity of hypertension can be increased when Acetylsalicylic acid is combined with 5-methoxy-N,N-dimethyltryptamine.
5beta-dihydrotestosterone
5beta-dihydrotestosterone may increase the anticoagulant activities of Acetylsalicylic acid.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline
The risk or severity of bleeding and hemorrhage can be increased when 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline is combined with Acetylsalicylic acid.
Abacavir
Acetylsalicylic acid may decrease the excretion rate of Abacavir which could result in a higher serum level.
Abatacept
The metabolism of Acetylsalicylic acid can be increased when combined with Abatacept.
Abciximab
Acetylsalicylic acid may increase the antiplatelet activities of Abciximab.
21 References
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  2. 2 . Sneader W: The discovery of aspirin: a reappraisal. BMJ. 2000 Dec 23-30;321(7276):1591-4.PubMed: 11124191
  3. 3 . Aukerman G, Knutson D, Miser WF: Management of the acute migraine headache. Am Fam Physician. 2002 Dec 1;66(11):2123-30.PubMed: 12484694
  4. 4 . Authors unspecified: Randomised trial of intravenous streptokinase, oral aspirin, both, or neither among 17,187 cases of suspected acute myocardial infarction: ISIS-2. ISIS-2 (Second International Study of Infarct Survival) Collaborative Group. Lancet. 1988 Aug 13;2(8607):349-60.PubMed: 2899772
  5. 5 . Dorsch MP, Lee JS, Lynch DR, Dunn SP, Rodgers JE, Schwartz T, Colby E, Montague D, Smyth SS: Aspirin resistance in patients with stable coronary artery disease with and without a history of myocardial infarction. Ann Pharmacother. 2007 May;41(5):737-41. Epub 2007 Apr 24.PubMed: 17456544
  6. 6 . Levy G: Clinical pharmacokinetics of aspirin. Pediatrics. 1978 Nov;62(5 Pt 2 Suppl):867-72.PubMed: 724339
  7. 7 . Authors unspecified: Guidance document: management priorities in salicylate toxicity. J Med Toxicol. 2015 Mar;11(1):149-52. doi: 10.1007/s13181-013-0362-3.PubMed: 25715929
  8. 8 . Durnas C, Cusack BJ: Salicylate intoxication in the elderly. Recognition and recommendations on how to prevent it. Drugs Aging. 1992 Jan-Feb;2(1):20-34.PubMed: 1554971
  9. 9 . Flower R: What are all the things that aspirin does? BMJ. 2003 Sep 13;327(7415):572-3. doi: 10.1136/bmj.327.7415.572.PubMed: 12969898
  10. 10 . Hall MN, Campos H, Li H, Sesso HD, Stampfer MJ, Willett WC, Ma J: Blood levels of long-chain polyunsaturated fatty acids, aspirin, and the risk of colorectal cancer. Cancer Epidemiol Biomarkers Prev. 2007 Feb;16(2):314-21.PubMed: 17301265
  11. 11 . Vane JR, Botting RM: The mechanism of action of aspirin. Thromb Res. 2003 Jun 15;110(5-6):255-8.PubMed: 14592543
  12. 12 . Vane JR, Bakhle YS, Botting RM: Cyclooxygenases 1 and 2. Annu Rev Pharmacol Toxicol. 1998;38:97-120. doi: 10.1146/annurev.pharmtox.38.1.97.PubMed: 9597150
  13. 13 . Varga Z, Sabzwari SRA, Vargova V: Cardiovascular Risk of Nonsteroidal Anti-Inflammatory Drugs: An Under-Recognized Public Health Issue. Cureus. 2017 Apr 8;9(4):e1144. doi: 10.7759/cureus.1144.PubMed: 28491485
  14. 14 . Ornelas A, Zacharias-Millward N, Menter DG, Davis JS, Lichtenberger L, Hawke D, Hawk E, Vilar E, Bhattacharya P, Millward S: Beyond COX-1: the effects of aspirin on platelet biology and potential mechanisms of chemoprevention. Cancer Metastasis Rev. 2017 Jun;36(2):289-303. doi: 10.1007/s10555-017-9675-z.PubMed: 28762014
  15. 15 . Alfonso L, Ai G, Spitale RC, Bhat GJ: Molecular targets of aspirin and cancer prevention. Br J Cancer. 2014 Jul 8;111(1):61-7. doi: 10.1038/bjc.2014.271. Epub 2014 May 29.PubMed: 24874482
  16. 16 . Tsoi KKF, Ho JMW, Chan FCH, Sung JJY: Long-term use of low-dose aspirin for cancer prevention: A 10-year population cohort study in Hong Kong. Int J Cancer. 2018 Dec 21. doi: 10.1002/ijc.32083.PubMed: 30575949
  17. 17 . Li D, Wang P, Yu Y, Huang B, Zhang X, Xu C, Zhao X, Yin Z, He Z, Jin M, Liu C: Tumor-preventing activity of aspirin in multiple cancers based on bioinformatic analyses. PeerJ. 2018 Sep 26;6:e5667. doi: 10.7717/peerj.5667. eCollection 2018.PubMed: 30280037
  18. 18 . Hasan Arif; Sandeep Aggarwal (2018). Salicylic Acid (Aspirin): StatPearls. StatPearls Publishing.
  19. 19 . Mayo Clinic website: Salicylate Link
  20. 20 . FDA Approved Products: Aspirin (acetylsalicylic acid) oral tablets Link
  21. 21 . Durlaza FDA label File