Acetylsalicylic acid

Acetylsalicylic acid

Mechanism of action

Antiplatelet agent.

Irreversible non-selective COX inhibitor. 

Inhibition of COX-1 in platelets blocks thromboxane A2 synthesis and inhibits platelet aggregation for the whole life of a platelet (about 10 days). 

Inhibition of COX-2 in tissues reduces synthesis of prostaglandins, which results in the antipyretic, analgesic, and anti-inflammatory effect of acetylsalicylic acid.

Indications and dose

Pharmacokinetics

Onset of action

  • Antiplatelet: 60 minutes
  • Anti-inflamatory: 30 minutes

Duration of action

  • Antiplatelet: 10 days (life of the platelet)
  • Anti-inflamatory: 6–12 hours

Half-life of elimination:

  • ASA: 13–19 minutes
  • Salicylate: 3.5–4.5 hours

Metabolism

  • ASA → plasma hydrolyzation → salicylic acid
  • Salicylate → hepatic metabolism, metabolism in other tissues

Elimination: Kidneys

Medicinal forms

Tablets = 75 mg, 100 mg, 300 mg, 400 mg, 500 mg

1 vial = 500 mg (powder for solution for injection - dilute in 5 ml F1/1)

Side-effects

Gastric and duodenal ulcers

Bleeding (inhibition of platelet aggregation)

Dyspepsia

Urticaria

Salicylism (dizziness, tinnitus, deafness, sweating, nausea, vomiting, headache, confusion)

References

  1. Pharm 101: Aspirin • LITFL • Top 200 Drugs
  2. Aspirin: Uses, Interactions, Mechanism of Action | DrugBank Online
  3. Aspirin | Circulation (ahajournals.org)
  4. https://www.medicines.org.uk/emc/search?q=Acetylsalicylic+