Wincardia Mechanism of Action


KCK Pharma


Full Prescribing Info
Pharmacology: Pharmacodynamics: Acetylsalicylic acid is an analgesic, anti-inflammatory, antipyretic and an inhibitor of platelet aggregation. It prolongs the bleeding time. It inhibits fatty acid cyclo-oxygenase by acetylation of the active site of the enzyme, and most of its pharmacological effects are due to inhibition of the formation of cyclo-oxygenase products including thromboxanes, prostaglandins and prostacyclin.
Acetylsalicylic acid has an active metabolite (salicylate) which, in addition to possessing some antiinflammatory properties in its own right, also has important effects on respiration, acid-base balance and the stomach. Salicylates stimulate respiration by a direct effect on the medulla, and at high concentrations, uncouple oxidative phosphorylation in muscle, increasing oxygen consumption and carbon dioxide production. Hyperventilation causes respiratory alkalosis which is compensated by renal excretion of bicarbonate.
Glycine is used to reduce gastric irritation.
Pharmacokinetics: Absorption: In general, immediate Acetylsalicylic acid is well and completely absorbed from the gastrointestinal (GI) tract. Following absorption, Acetylsalicylic acid is hydrolyzed to salicylic acid with peak plasma levels of salicylic acid occurring within 1-2 hours of dosing. The rate of absorption from the GI tract is dependent upon the dosage form, the presence or absence of food, gastric PH (the presence or absence of GI antacids or buffering agents), and other physiologic factors. Enteric coated Acetylsalicylic acid products are erratically absorbed from the GI tract.
Metabolism: Acetylsalicylic acid is rapidly hydrolyzed in the plasma to salicylic acid such that plasma levels of Acetylsalicylic acid are essentially undetectable 1-2 hours after dosing. Salicylic acid is primarily conjugated in the liver to form salicyluric acid, a phenolic glucuronide, an acyl glucuronide, and a number of minor metabolites. Salicylic acid has a plasma half-life of approximately 6 hours. Salicylate metabolism is saturable and total body clearance decreases at higher serum concentrations due to the limited ability of the liver to form both salicyluric acid and phenolic glucuronide. Following toxic doses (10-20 grams (g)), the plasma half-life may be increased to over 20 hours.
Distribution: Salicylic acid is widely distributed to all tissues and fluids in the body including the central nervous system (CNS), breast milk and fetal tissues. The highest concentrations are found in the plasma, liver, renal cortex, heart and lungs.
Excretion: The elimination of salicylic acid is constant in relation to plasma concentration. Renal excretion of unchanged drug depends upon urine pH. As urinary pH rises above 6.5, the renal clearance of free salicylate increases from 5 percent to 80 percent.
Elimination Half-life: Salicylic acid: approximately 6 h.
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