Trimetazidine tablets po modified release 35mg №10×6

Name:
Trimetazidine MV 35mg №60
Description:
Round coated tablets, pink, with a biconvex surface. The main active ingredient Trimetazidine Release form tablets Dosage 35 mg Pharmacological action Pharmacodynamics Trimetazidine prevents a decrease in the intracellular concentration of adenosine triphosphate (ATP) by maintaining energy metabolism in cells subjected to hypoxia or ischemia. This ensures the correct operation of ion pumps and transmembrane transport of sodium and potassium, maintaining cellular homeostasis. Trimetazidine inhibits α-oxidation of fatty acids by inhibiting the long chain 3-ketoacyl-CoA thiolase in mitochondria, which leads to an increase in glucose oxidation. In an ischemic cell, less oxygen is required to obtain energy by oxidizing glucose than in the process of α-oxidation. Potentiation of glucose oxidation optimizes energy processes within the cell, thereby maintaining proper energy metabolism in ischemic conditions. Pharmacodynamic effects In patients with ischemic heart disease, trimetazidine acts as a metabolic agent, maintaining the level of high-energy phosphate in the cell. Anti-ischemic effects are achieved without concomitant hemodynamic effects. Clinical efficacy and safety Clinical studies have demonstrated the efficacy and safety of trimetazidine in patients with angina pectoris, both in monotherapy and in combination with insufficient effect of other antianginal agents. Pharmacokinetics After oral administration, trimetazidine is rapidly absorbed and reaches its maximum plasma concentration in approximately 5 hours. For 24 hours, the plasma concentration remains at levels above or equal to 75% of the maximum concentration for 11 hours. The equilibrium state is reached after 60 hours. Food intake does not affect the pharmacokinetic properties of the drug. The volume of distribution is 4.8 l / kg, which explains the good diffusion in the tissue (the degree of protein binding is quite low, about 16% in vitro). Trimetazidine is excreted from the body mainly in the urine, in an almost unchanged form. The half-life is about 7 hours in healthy young volunteers, in patients over 65 years old – about 12 hours. Renal clearance of trimetazidine is directly correlated with creatinine clearance, and hepatic clearance decreases with age. Pharmacokinetics in elderly patients In elderly patients, an increased exposure to trimetazidine may occur due to age-related decline in renal function. A special study was conducted with the participation of elderly patients (over 75 years old) using the drug (PM) Trimetazidine, with a modified release of 35 mg, twice a day. Population-based kinetic analysis showed an average two-fold increase in plasma trimetazidine exposure in patients with severe renal impairment (creatinine clearance less than 30 ml/min) compared with elderly patients with creatinine clearance greater than 60 ml/min. No special features regarding the safety of use in elderly patients in comparison with the general population were found. Pharmacokinetics in patients with reduced renal function The exposure of trimetazidine was increased by an average of 2.4 times in patients with moderate renal insufficiency (creatinine clearance 30–60 ml / min), and by an average of 4 times in patients with severe renal insufficiency (clearance creatinine < 30 ml/min) compared with healthy volunteers with normal kidney function. No special features regarding the safety of use in this patient population but compared with the general population were found. Pharmacokinetics in children The pharmacokinetics of trimetazidine in children (< 18 years) have not been studied. Indications for use: Trimetazidine is indicated for the symptomatic treatment of adult patients with stable angina pectoris as adjunctive therapy when first-line antianginal therapy fails or is intolerable. Dosage and administration Take orally during meals with liquid. Adults: one tablet 2 times a day - in the morning and in the evening (70 mg / day). After three months of treatment, the clinical effect should be evaluated. In case of insufficient effectiveness of the drug, it should be discontinued. Patients with impaired renal function In patients with moderate renal impairment (creatinine clearance 30-60 ml / min), the recommended dose is 1 tablet (35 mg) in the morning with breakfast. Elderly patients Elderly patients may experience an increased exposure to trimetazidine due to age-related decline in renal function. In patients with moderate renal impairment (creatinine clearance 30-60 ml / min), the recommended dose is 1 tablet (35 mg) in the morning with breakfast. It is necessary to carefully select the dose in elderly patients. Use during pregnancy and lactation There are no data on the use of trimetazidine by pregnant women. Animal studies have shown no direct or indirect harmful effects on the reproductive system. As a precautionary measure, trimetazidine is not recommended during pregnancy. Breastfeeding It is not known whether trimetazidine is excreted in breast milk. A risk to neonates/children cannot be excluded. Trimetazidine should not be used during breastfeeding. Precautions Trimetazidine is not indicated for the relief of angina attacks, nor is it indicated as initial treatment for unstable angina or myocardial infarction. Trimetazidine should not be taken before hospitalization and during the first days of hospitalization. At an attack of angina, the pathology of the coronary vessels should be re-evaluated and the treatment used (medical treatment and possibly revascularization) adjusted. Trimetazidine may cause or worsen the symptoms of parkinsonism (tremor, akinesia, increased muscle tone), patients should be monitored regularly, especially elderly patients. In doubtful cases, the patient should be referred to a neurologist for an appropriate examination. The development of movement disorders, such as symptoms of parkinsonism, restless legs syndrome, tremor, unsteadiness when walking, may lead to the final decision to cancel trimetazidine. The frequency of development of movement disorders is low, usually they are reversible. In most cases, after stopping trimetazidine, patients recovered within 4 months. If the symptoms of parkinsonism persist for more than 4 months after discontinuation of the drug, a consultation with a neurologist is necessary. With unsteady walking or low muscle tone, especially when using antihypertensive therapy, the patient may fall. With caution, trimetazidine should be prescribed to patients with moderate renal impairment and elderly patients over 75 years of age, since in such patients there is a possibility of an increase in the elimination time of trimetazidine from the body. Children The safety and efficacy of Trimetazidine in children under 18 years of age have not been established. There are no data on use in children. Interaction with other drugs There were no interactions with other drugs. Contraindications Hypersensitivity to the active substance or to any of the excipients. Parkinson's disease, parkinson's syndrome, restless legs syndrome and other movement disorders. Severe renal failure (creatinine clearance less than 30 ml / min). Active ingredient: trimetazidine dihydrochloride - 35 mg; excipients: hypromellose (type 2208) (Metocel K100M Premium), hypromellose (type 2208) (Metocel K15M Premium), anhydrous colloidal silicon dioxide, magnesium stearate; microcrystalline cellulose, opadry 200 F (polyvinyl alcohol, partially hydrolyzed; titanium dioxide E 171; talc, macrogol 3350; methacrylic acid copolymer type C; iron oxide yellow E 172; iron oxide red E172; sodium bicarbonate E 500ii; iron oxide black E 172 ). Overdose Data on trimetazidine overdose are limited. In case of overdose, symptomatic treatment is necessary. Side effectsAccording to the frequency of occurrence, adverse reactions are divided into the following groups: very frequent (? 1/10), frequent (? 1/100, <1/10), infrequent (? 1/1000, <1/100), rare (? 1 /10000, <1/1000), very rare (<1/10000), with an unknown frequency (it is impossible to determine the frequency of occurrence from the available data). Nervous system disorders: often: dizziness, headache; with an unknown frequency: symptoms of parkinsonism (tremor, akinesia, increased muscle tone), restless legs syndrome, unsteadiness when walking and other motor disorders, usually reversible; sleep disturbance (drowsiness, insomnia). Cardiac disorders: rarely: palpitations, extrasystole, tachycardia. Vascular disorders: rarely: arterial hypotension; orthostatic hypotension, which may be associated with malaise, dizziness, or falling, especially in patients taking antihypertensive treatment; redness of the face. Gastrointestinal disorders: often: abdominal pain, diarrhea, dyspepsia, nausea and vomiting; with an unknown frequency: constipation. Liver and biliary tract disorders: Not known: Hepatitis. Skin and subcutaneous tissue disorders: often: rash, itching, urticaria; with an unknown frequency: acute generalized exanthematous pustulosis, Quincke's edema. General disorders and disorders at the injection site: often: asthenia. Blood and lymphatic system disorders: with an unknown frequency: agranulocytosis, thrombocytopenia, thrombocytopenic purpura. Storage conditions In a place protected from light and moisture, at a temperature not exceeding 30 C. Keep out of the reach of children. for Trimetazidine tablets p/o modified release 35mg №10x6