Trimetazidine is indicated for the symptomatic treatment of stable angina in adults with insufficient efficacy or intolerance to first-line antianginal drugs.
active substance: trimetazidine;
1 tablet contains 20 mg of trimetazidine dihydrochloride;
auxiliary substances: corn starch, lactose monohydrate, microcrystalline cellulose, colloidal anhydrous silicon dioxide, talc, calcium stearate, sepifilm 752 white.
Energoton Dosage form
Basic physical and chemical properties: round tablets with a biconvex surface, film-coated, white.
Cardiological agents. Trimetazidine.
ATX code С01Е В15.
Mechanism of action.
By preserving energy metabolism in cells suffering from hypoxia or ischemia, trimetazidine prevents a decrease in the level of intracellular adenosine triphosphoric acid (ATP), thereby ensuring the proper functioning of ion pumps and transmembrane sodium-potassium flow while maintaining cellular homeostasis.
Trimetazidine inhibits β-oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase (3-CAT), which increases glucose oxidation. In cells under ischemic conditions, the process of obtaining energy by oxidizing glucose requires less oxygen compared to the process of obtaining energy by β-oxidation of fatty acids. Strengthening the glucose oxidation process optimizes the energy processes in cells and, accordingly, maintains a sufficient energy metabolism under conditions of ischemia.
In patients with coronary artery disease, trimetazidine acts as a metabolic agent, maintaining intracellular levels of high-energy phosphate in the myocardium. The effects are achieved without concomitant hemodynamic effects.
The maximum concentration of trimetazidine in the blood is observed on average 5 hours after taking the pill. During the day, the concentration in the blood plasma is stable: within 11 hours after taking the tablet, the concentration of trimetazidine in the blood plasma is at least 75% of the maximum concentration. The state of stable concentration is established at the latest at the 60th hour. Food intake does not affect the pharmacokinetic characteristics of trimetazidine. The volume of distribution is 4.8 l / kg; protein binding is low: according to in vitro measurements – 16%.
Trimetazidine is excreted mainly in the urine, mainly in unchanged form. The half-life is on average 7 hours for healthy young volunteers and 12 hours for those over 65 years of age. Complete elimination of trimetazidine is the result of renal clearance, which directly correlates with creatinine clearance and, to a lesser extent, is the result of hepatic clearance, which decreases with age.
Special patient groups.
Elderly patients. In elderly patients, an increase in the concentration of trimetazidine is possible due to an age-related decrease in renal function.
Renal dysfunction. The concentration of trimetazidine in the blood increases in patients with moderate renal impairment (creatinine clearance – 30-60 ml / min) and in patients with severe renal impairment (creatinine clearance <30 ml / min).
For adults, trimetazidine is indicated for the symptomatic treatment of stable angina pectoris with insufficient efficacy or intolerance to first-line antianginal drugs.
Hypersensitivity to the active substance or to any of the excipients of the drug.
Parkinson’s disease, parkinsonism symptoms, tremors, restless legs syndrome and other movement disorders related to the above.
Severe renal impairment (creatinine clearance <30 ml / min).
Interaction with other medicinal products and other forms of interaction
Interaction with other drugs has not been identified. In particular, trimetazidine can be administered in combination with heparin, calciparin, vitamin K antagonists, oral lipid-lowering drugs, acetylsalicylic acid, β-blocker drugs, calcium antagonists, digitalis drugs (trimetazidine does not affect plasma digoxin levels).