Aspirin 100 mg, glycine 45 mg.
Each tablet contains aspirin 100 mg and glycine (aminoacetic acid) 45 mg.
Antiplatelet, antithrombotic.
Pharmacology: Metabolism of arachidonic acid via the enzyme cyclooxygenase produces mainly thromboxane (TxA2) in platelets and prostacyclin (PGI2) in the vascular endothelium. TxA2 causes vasoconstriction and induces platelet aggregation and PGI2 causes vasodilation and has a platelet anti-aggregatory effect. Platelet cyclooxygenase is more sensitive to aspirin inhibition and can only be regenerated with the formation of new platelets. Acetylsalicylic acid can therefore have a selective inhibitory effect on thromboxane production and hence on platelet aggregation. In vitro and ex vivo studies have shown that at low doses (100 mg), there is a differential effect between the inhibitory action of aspirin on platelet cyclooxygenase and the cyclooxygenase in the blood vessels. At these doses, there is complete inhibition of platelet aggregation induced by collagen, ADP and arachidonic acid. The anti-inflammatory, antipyretic and analgesic actions of aspirin are also thought to be mediated via inhibition of prostaglandin biosynthesis.
Pharmacokinetics: After oral administration of aspirin-glycine, aspirin is generally well absorbed from the gastrointestinal tract, partly from the stomach and mainly from the small intestine. Time to peak plasma levels is within 15 min.
Salicylate is 80-90% bound to plasma protein especially albumin, at clinical concentrations of salicylate.
Aspirin is converted to salicylic acid (salicylate) in many tissues but primarily in the gastrointestinal mucosa and the liver.
Salicylates are excreted predominantly by the kidneys. Most of the administered dose can be recovered in the urine as free salicylate (10%) or metabolites (75% as salicyluric acid). Excretion of free salicylate is extremely variable, 85% of ingested aspirin in alkaline urine, 5% in acidic urine.
Patients with impaired renal function require dosage adjustment.
The plasma elimination half-life for aspirin is approximately 30 min. The half-life of salicylate is therapeutically more important and is dose-dependent, increasing as the plasma concentration increases. At low doses, the elimination half-life is 2-3 hrs and at high doses 13-30 hrs.
Plasma ASA rather than SA is required for antiplatelet effect and this can best be achieved with soluble aspirin and aspirin-glycine formulations where first-pass metabolism in the gastrointestinal tract is minimised.
Conditions where modification of platelet behaviour is considered beneficial, including transient ischaemic attacks, secondary prevention of myocardial infarction, and for prophylaxis against stroke, vascular occlusion and deep vein thrombosis.
Adults: 1 tab daily or as required. Dissolve on tongue or take with a glass of water.
Usual procedures for aspirin overdosage should be followed, including general supportive measures and gastric lavage if necessary.
Patients suffering from active peptic ulceration or haemophilia or known to be allergic to aspirin.
Use in pregnancy: There is clinical and epidemiological evidence of the safety of aspirin in pregnancy, but it may prolong labour and contribute to maternal and neonatal bleeding and is best avoided in the last trimester of pregnancy.
Use in children: Not recommended.
Use in the elderly: Elderly patients do not tolerate aspirin as well as younger patients. They may experience tinnitus, nausea, anorexia and gastrointestinal irritation though this would be less likely at the doses recommended for antiplatelet action.
Use in pregnancy: There is clinical and epidemiological evidence of the safety of aspirin in pregnancy, but it may prolong labour and contribute to maternal and neonatal bleeding and is best avoided in the last trimester of pregnancy.
Unwanted effects are those of soluble aspirin. It may precipitate bronchospasm, and induce attacks of asthma in susceptible subjects; may also induce gastrointestinal haemorrhage, occasionally major.
Aspirin may enhance the effects of anticoagulants and inhibit the action of uricosuric.
B01AC06 - acetylsalicylic acid ; Belongs to the class of platelet aggregation inhibitors excluding heparin. Used in the treatment of thrombosis.
Cardiprin 100 tab
30's;90's
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