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Active ingredient: Aspirin - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Anti-Inflammatory Agents, Non-Steroidal
  • Cyclooxygenase Inhibitors
  • Fibrinolytic Agents
  • Anticoagulants
  • Salicylates

Dosage Forms

  • Tablet (enteric-coated)
  • Tablet

Brands / Synonyms

2-Acetoxybenzenecarboxylic acid; 2-Acetoxybenzoic acid; 2-Carboxyphenyl acetate; 8-hour Bayer; A.S.A.; A.S.A. Empirin; Acenterine; Acesal; Acetal; Acetal (VAN); Acetaminophen, Aspirin and Codeine; Aceticyl; Acetilsalicilico; Acetilum acidulatum; Acetisal; Acetol; Acetol (VAN); Acetonyl; Acetophen; Acetosal; Acetosalic acid; Acetosalin; Acetoxybenzoic acid; Acetylin; Acetylsal; Acetylsalicylate; Acetylsalicylic acid; Acetylsalicylsaure; Acetylsalicylsaure (GERMAN); Acetysalicylic acid; Acide acetylsalicylique; Acide acetylsalicylique (FRENCH); Acido acetilsalicilico; Acido O-acetil-benzoico; Acidum acetylsalicylicum; Acimetten; Acisal; Acylpyrin; Adiro; Aggrenox; ASA; ASA (VAN); Asagran; Asatard; Ascoden-30; Aspalon; Aspec; Aspergum; Aspirdrops; Aspirin (VAN); Aspirine; Aspro; Asteric; Bayer; Bayer Extra Strength Aspirin For Migraine Pain; Benaspir; Benzoic acid, 2-(acetyloxy)-; Bi-prin; Bialpirina; Bialpirinia; Bufferin; Butalbital, Aspirin, and Caffeine; Butalbital, Aspirin, Caffeine, and Codeine; Caprin; Carisoprodol and Aspirin; Cemirit; Claradin; Clariprin; Colfarit; Contrheuma retard; Coricidin; Crystar; Decaten; Delgesic; Dolean pH 8; Duramax; Easprin; ECM; Ecolen; Ecotrin; Empirin; Endydol; Entericin; Enterophen; Enterosarein; Enterosarine; Entrophen; Equagesic; Extren; Fiorinal; Fiorinal with Codeine; Globentyl; Globoid; Helicon; Idragin; Kyselina 2-acetoxybenzoova; Kyselina acetylsalicylova; Lemascorb; Levius; Liqui-Cee; Measurin; Micristin; Neuronika; Norgesic; Novid; Nu-seals; Nu-seals aspirin; O-accetylsalicylic acid; o-Acetoxybenzoic acid; O-Acetylsalicylic acid; o-Carboxyphenyl acetate ; Oxycodone and Aspirin; Percodan; Persistin; Pharmacin; Pirseal; Planavit C; Polopiryna; Premaspin; Rheumintabletten; Rhodine; Rhonal; Salacetin; Salcetogen; Saletin; Salicylic acid acetate; Salicylic acid, acetate; Salicylic acid, acetyl-; Solfrin; Solprin; Solprin acid; Solpyron; Soma Compound with Codeine; Spira-Dine; St. Joseph; St. Joseph Aspirin for Adults; Supac; Tasprin; Temperal; Triaminicin; Triple-sal; Vanquish; Xaxa; Yasta

Indications

For use in the temporary relief of various forms of pain, inflammation associated with various conditions (including rheumatoid arthritis, juvenile rheumatoid arthritis, systemic lupus erythematosus, osteoarthritis, and ankylosing spondylitis), and is also used to reduce the risk of death and/or nonfatal myocardial infarction in patients with a previous infarction or unstable angina pectoris.

Pharmacology

Aspirin (acetylsalicylic acid) is an analgesic, antipyretic, antirheumatic, and anti-inflammatory agent. Aspirin's mode of action as an antiinflammatory and antirheumatic agent may be due to inhibition of synthesis and release of prostaglandins. Aspirin appears to produce analgesia by virtue of both a peripheral and CNS effect. Peripherally, Aspirin acts by inhibiting the synthesis and release of prostaglandins. Acting centrally, it would appear to produce analgesia at a hypothalamic site in the brain, although the mode of action is not known. Aspirin also acts on the hypothalamus to produce antipyresis; heat dissipation is increased as a result of vasodilation and increased peripheral blood flow. Aspirin's antipyretic activity may also be related to inhibition of synthesis and release of prostaglandins.

Mechanism of Action

The analgesic, antipyretic, and anti-inflammatory effects of aspirin are due to actions by both the acetyl and the salicylate portions of the intact molecule as well as by the active salicylate metabolite. Aspirin directly and irreversibly inhibits the activity of both types of cyclo-oxygenase (COX-1 and COX-2) to decrease the formation of precursors of prostaglandins and thromboxanes from arachidonic acid. This makes aspirin different from other NSAIDS (such as diclofenac and ibuprofen) which are reversible inhibitors. Salicylate may competitively inhibit prostaglandin formation. Aspirin's antirheumatic (nonsteroidal anti-inflammatory) actions are a result of its analgesic and anti-inflammatory mechanisms; the therapeutic effects are not due to pituitary-adrenal stimulation. The platelet aggregation–inhibiting effect of aspirin specifically involves the compound's ability to act as an acetyl donor to the platelet membrane; the nonacetylated salicylates have no clinically significant effect on platelet aggregation. Aspirin affects platelet function by inhibiting the enzyme prostaglandin cyclooxygenase in platelets, thereby preventing the formation of the aggregating agent thromboxane A2. This action is irreversible; the effects persist for the life of the platelets exposed. Aspirin may also inhibit formation of the platelet aggregation inhibitor prostacyclin (prostaglandin I2) in blood vessels; however, this action is reversible.

Absorption

Absorption is generally rapid and complete following oral administration but may vary according to specific salicylate used, dosage form, and other factors such as tablet dissolution rate and gastric or intraluminal pH.

Toxicity

Oral, mouse: LD50 = 250 mg/kg; Oral, rabbit: LD50 = 1010 mg/kg; Oral, rat: LD50 = 200 mg/kg. Effects of overdose include: tinnitus, abdominal pain, hypokalemia, hypoglycemia, pyrexia, hyperventilation, dysrhythmia, hypotension, hallucination, renal failure, confusion, seizure, coma, and death.

Biotrnasformation / Drug Metabolism

Aspirin is rapidly hydrolyzed primarily in the liver to salicylic acid, which is conjugated with glycine (forming salicyluric acid) and glucuronic acid and excreted largely in the urine.

Contraindications

Aspirin should not be used in patients who have previously exhibited hypersensitivity to aspirin and/or nonsteroidal antiinflammatory agents. Aspirin should not be given to patients with a recent history of gastrointestinal bleeding or in patients with bleeding disorders (e.g., hemophilia).

Drug Interactions

Uricosuric Agents: Aspirin may decrease the effects of probenecid, sulfinpyrazone, and phenylbutazone.
Alcohol: Has a synergistic effect with aspirin in causing gastrointestinal bleeding.
Corticosteroids: Concomitant administration with aspirin may increase the risk of gastrointestinal ulceration and may reduce serum salicylate levels.
Pyrazolone Derivatives (phenylbutazone, oxyphenbutazone, and possibly dipyrone): Concomitant administration with aspirin may increase the risk of gastrointestinal ulceration.
Nonsteroidal Antiinflammatory Agents: Aspirin is contraindicated in patients who are hypersensitive to nonsteroidal anti-inflammatory agents.
Urinary Alkalinizers: Decrease aspirin effectiveness by increasing the rate of salicylate renal excretion.
Phenobarbital: Decreases aspirin effectiveness by enzyme induction.
Phenytoin: Serum phenytoin levels may be increased by aspirin.
Propranolol: May decrease aspirin's anti-inflammatory action by competing for the same receptors. Antacids: Enteric Coated Aspirin should not be given concurrently with antacids, since an increase in the pH of the stomach may effect the enteric coating of the tablets.

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