Acetylsalicylic acid
Acetylsalicylic acid (Acidum acetylsalicilicum, Aspirin, ACC, Thrombo ASS). It exerts anti-inflammatory, anti-pyretic, analgesic effects.
Indications: fever, headache, migraine, neuralgias and as an anti-rheumatic drug.
Anti-inflammatory effect is usually observed in 1-2 days after the beginning of the drug intake. Acute inflammation is usually over within several days. In case of chronic course the effect develops slowlier and may not always be complete.
At present acetylsalicylic acid is frequently used as an effective antiaggregant in doses 100—150 mg a day for the prevention of coronary artery thrombosis at ischemic heart disease, for the prevention of ischemic stroke.
Pharmacokinetics. Taken orally, it is quickly and almost fully absorbed, penetrates easily into numerous tissues, undergoes biotransformation in the wall of intestines and in liver with the formation of salicylic acid and other active metabolites, gets excreted by kidneys in an unchanged form.
Specific side effects of acetylsalicylic acid are irritation and ulceration of gastric mucosa, bronchospasm – “aspirin asthma”. The bronchospasm is caused by the activation of lipoxygenase pathway of arachidonic acid metabolism.
Contraindications: hypersensitivity, age under 5, glucose 6-phosphate dehydrogenase deficiency (risk of hemolysis), GIT diseases, risk of bleeding, renal dysfunction, BA, last trimester of pregnancy (the risk of weak delivery activity), lactation (if taken more than 300 mg a day).
Interaction. The action of anticoagulants (coumarin derivatives, heparin), hypoglycemic drugs (sulphonylurea derivatives), thrombolytic drugs and other inhibitors of platelet aggregation is intensified. The risk of gastric hemorrhages becomes higher if it is taken together with glucocorticoids. Side effects of Methotrexate are intensified.
Paracetomol, caffeine, antihistamine drugs increase the risk of acetylsalicylic acid side effects.
Dosage form: tab. – 0,25 and 0,5 g.
