Included in the formulation
АТХ:C.01.E.B Other drugs for the treatment of heart disease
C.01.E.B.15 Trimetazidine
Pharmacodynamics:Selective inhibition of 3-ketoacyl-CoA-thiolase, a key enzyme of β-oxidation of fatty acids, leads to switching of energy metabolism to glucose oxidation, optimization of metabolism in cardiomyocytes and neurons of the brain.Reduction of intracellular acidosis and phosphate content caused by myocardial ischemia and reperfusion.
Pharmacokinetics:Absorption - 90%. The maximum concentration after a single oral intake of 20 mg of trimetazidine is about 55 ng / ml. The time to reach the maximum concentration 2 hours The volume distribution of 4.8 l / kg, penetrates the blood-brain barrier, the placenta. Relationship with plasma proteins 16%. Half-life ~ 4.5-5 hours Elimination by the kidneys (about 60% unchanged).
Indications:Long-term therapy of ischemic heart disease: prevention of angina attacks (monotherapy or as part of combination therapy); treatment of cochlear-vestibular disorders of ischemic nature (including dizziness, tinnitus, hearing impairment); chorioretinal vascular disorders with ischemic component.
VII.H30-H36.H35.0 Background retinopathy and retinal vascular changes
VIII.H80-H83.H81 Violations of the vestibular function
VIII.H90-H95.H93.0 Degenerative and vascular diseases of the ear
IX.I20-I25.I20 Angina pectoris [angina pectoris]
Contraindications:Hypersensitivity, pregnancy, breast-feeding.
Carefully:Hypersensitivity.
Pregnancy and lactation:Adequate and well-controlled studies in humans and animals have not been conducted. Contraindicated in the use.
Category of recommendations for FDA is not defined.
Dosing and Administration:Take inside a daily dose of 40-60 mg per day, the frequency of reception 2-3 times a day. When taken in modified release forms - 35 mg 2 times a day during meals.
Side effects:Possible: allergic reactions (including skin rash, itching).
Rarely: nausea, vomiting, gastralgia.
Interaction:Not described.
Special instructions:The drug is not intended for relief of angina attacks. The meta-analysis of the Cochrane review confirmed the low efficacy of trimetazidine in the treatment of stable angina compared with placebo. The comparison was made on the basis of the decrease in the frequency of anginal attacks [the weighted mean difference was -1.44; 95% CI (-2.10) - (-0.79), according to 12 studies combining 692 participants], a decrease in the frequency of nitroglycerin intake [the weighted mean difference was -1.47; 95% CI (-2.20) - (- 0.73), according to 10 studies combining 667 participants]. There is no information on the effect of treatment with trimetazidine on clinically relevant outcomes.The available information is too scarce to give advice on the use of trimetazidine in monotherapy or in combination with traditional antianginal agents. Patients should be informed about treatment options, rather than offering a single therapy based on the physician's preferences. Decisions at the local level need to be made taking into account all the multiple factors, such as epidemiological data, price structure and existing clinical practice.