Antianginal and anti-ischaemic.
Pharmacology: Carvidon: Trimetazidine belongs to a new class of compounds that display anti-ischaemic effects without inducing haemodynamic changes and improves the status of the ischaemic myocardium. It exerts its antianginal effects through a direct cytoprotective action on the myocardium, thereby, avoiding the side effects of impaired left ventricular function, excessive peripheral vasodilation and other disadvantages associated with the use of comparative antianginal agents.
Carvidon-MR: Mechanism of Action: There are several possible mechanisms of action by which trimetazidine promotes preservation of membrane structures and cellular function, thereby allowing the ischaemic myocardial cell to more rapidly restore its energy reserves. The main mechanisms are: Limitation of intracellular acidosis; improvement in transmembrane ion exchanges and calcium overload; prevention of excessive free radical production; inhibition of the inflammatory reaction and preservation of mitochondrial function.
Pharmacokinetics: Trimetazidine is >95% non-ionized at physiological pH, permitting the drug to pass through lipoprotein membranes. It is rapidly and completely absorbed from the gastrointestinal tract after oral ingestion. Cmax is 1.8 hrs and plasma half-life is 6 hrs. Plasma protein-binding is low and the volume of distribution is 320 L. Four pathways of metabolism are known but metabolism is not extensive, with 51% of unchanged drug eliminated in urine. Elimination is rapid (t½=6 hrs) and predominantly renal. Sixty percent of the drug is excreted unchanged in the urine. Food intake does not interfere with the pharmacokinetics of trimetazidine.
Carvidon: Treatment of ischaemic heart disease (angina pectoris, sequelae of infarction).
Carvidon-MR: Treatment of coronary insufficiency, angina pectoris, sequelae of infarction and in ischaemia of neurosensorial tissue.
Carvidon: 1 tab thrice daily with meals. Trimetazidine can be combined with calcium-channel blockers or β-blockers.
Carvidon-MR: 1 tab twice daily.
Impaired Renal and Hepatic Function: No dosage adjustment is required in patients with impaired renal and hepatic functions.
Trimetazidine is extremely safe, the maximum tolerated dosage being 2000 times the therapeutic dosage.
Hypersensitivity to trimetazidine.
Appropriate dosage reduction may be necessary in patients with major kidney failure or severe liver failure.
Use in pregnancy: There is insufficient evidence to recommend the use of trimetazidine in pregnancy. Animal studies do not reveal any teratogenic effect.
Use in lactation: There is no information on the secretion of trimetazidine into breast milk. However, breastfeeding should be discontinued if the use of trimetazidine is considered essential.
Use in children: There is no experience with trimetazidine in children.
Use in pregnancy: There is insufficient evidence to recommend the use of trimetazidine in pregnancy. Animal studies do not reveal any teratogenic effect.
Use in lactation: There is no information on the secretion of trimetazidine into breast milk. However, breastfeeding should be discontinued if the use of trimetazidine is considered essential.
The most commonly encountered side effects are gastric discomfort, nausea, headache and vertigo. However, the side effects are mild and nonspecific.
No drug interactions have been reported. In particular, no interactions have been reported between trimetazidine and β-blockers, calcium antagonists, nitrates, heparin, hypolipidaemic agents or digitalis preparation.
Carvidon: Store below 25°C, in a dry place.
Carvidon-MR: Store in a cool, dry place.
C01EB15 - trimetazidine ; Belongs to the class of other cardiac preparations.
Carvidon: Tab 20 mg x 10 x 10's.
Carvidon-MR: Tab 35 mg (modified-release, film-coated) x 10 x 10's.
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