Pharmacodynamics. Due to the preservation of energy metabolism in cells experiencing hypoxia or ischemia, trimetazidine prevents a decrease in intracellular ATP levels, 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 conditions of ischemia, the process of obtaining energy through the oxidation of glucose requires less oxygen compared to the process of obtaining energy through β-oxidation of fatty acids.
Strengthening the glucose oxidation process optimizes energy processes in cells and, accordingly, supports energy metabolism under conditions of ischemia.
In patients with coronary artery disease, trimetazidine acts as a metabolic agent, maintaining intracellular levels of high-energy phosphates in the myocardium. The effects are achieved without concomitant hemodynamic changes.
Clinical studies have demonstrated the efficacy and safety of using trimetazidine for the treatment of patients with stable angina pectoris, both in monotherapy and in the case of addition to other preparations with insufficient efficacy.
The TRIMPOL-II randomized, double-blind, placebo-controlled trial demonstrated that the addition of trimetazidine 60 mg / day to metoprolol 100 mg (50 mg twice daily) for 12 weeks resulted in a significant improvement in exercise test scores and clinical symptoms compared with those when using a placebo.
Pharmacokinetics. After oral administration, trimetazidine is rapidly absorbed in the digestive tract. Cmax in blood plasma is reached in 2 hours and is 55 ng / ml after a single dose of 20 mg. The stage of equilibrium concentration in blood plasma begins 24–36 hours after the start of treatment. The volume of distribution is 4.8 l / kg of body weight. Plasma protein binding is low, ≈16% according to in vitro measurements. Trimetazidine is excreted mainly in the urine, mainly unchanged. T½ is ≈6 hours. In elderly patients, due to age-related decline in renal function, the concentration of trimetazidine in the body may increase.
Pharmacokinetics of Triductan MB. Cmax of trimetazidine in the blood is observed on average 5 hours after administration. During the day, the concentration in the blood plasma is stable: within 11 hours after administration, the concentration of trimetazidine in the blood plasma is ≥75% Cmax. The state of equilibrium concentration is established later, at the 60th hour. Food intake does not affect the pharmacokinetic characteristics of Triductan MB. The volume of distribution is 4.8 l / kg, protein binding is low and amounts to 16%. Trimetazidine is excreted mainly in the urine, mostly unchanged.
T½ averages 7 hours for healthy young volunteers and 12 hours for the elderly. The complete elimination of trimetazidine is the result of renal clearance, which is directly related to creatinine clearance and, to a lesser extent, to hepatic clearance, which decreases with age.
Impaired renal function. 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).
Symptomatic treatment of adult patients with stable angina pectoris with insufficient efficacy or intolerance to first-line antianginal preparations.
Triductan is prescribed orally 1 tablet 3 times a day with meals. after 3 months of treatment, it is necessary to evaluate its results, and in the absence of an effect, trimetazidine should be canceled.
Special patient groups.
Patients with impaired renal function. Patients with moderate renal impairment (creatinine clearance - 30-60 ml / min) are recommended to use 1 tablet 2 times a day: in the morning and in the evening with meals.
Elderly patients. Elderly patients are more sensitive to the action of trimetazidine due to age-related decline in renal function. For persons with moderate renal impairment (creatinine clearance - 30-60 ml / min), the recommended dose is 1 tablet 2 times a day: in the morning and in the evening with meals. For elderly patients, dose titration should be done with caution.
Triduktan MV is prescribed orally 1 tablet 2 times a day in the morning and in the evening with meals, drinking plenty of water. The duration of treatment is determined by the doctor individually, depending on the nature and course of the disease. If necessary, the treatment regimen can be revised after 3 months.
Special patient groups
Patients with impaired renal function. For patients with moderate renal impairment (creatinine clearance 30-60 ml / min), the recommended dose is 1 tablet per day in the morning with meals.
Elderly patients. Elderly patients are more sensitive to the action of trimetazidine due to age-related decline in renal function. For patients with moderate renal impairment (creatinine clearance - 30-60 ml / min), the recommended dose is 1 tablet per day in the morning with meals.
For elderly patients, dose titration should be done with caution.
Increased individual sensitivity to trimetazidine or to any of the components of the preparation.
Parkinson's disease, parkinsonism symptoms, tremors, restless legs syndrome and other movement disorders related to the above.
Severe renal failure (creatinine clearance 30 ml / min).
Usually, treatment with triductan is well tolerated. Adverse reactions, which have been identified as side effects that may be associated with the use of trimetazidine, are listed below.
From the nervous system: headache, dizziness, symptoms of parkinsonism (tremor, akinesia, muscle hypertonicity), gait instability, restless legs syndrome and other movement disorders related to the above, which are reversible after preparation withdrawal, may occur; sleep disorders (insomnia, drowsiness).
Cardiac disorders: palpitation, extrasystole, tachycardia.
Vascular disorders: arterial hypotension, orthostatic hypotension, which may be associated with malaise, dizziness or falling (in particular in patients using antihypertensive preparations), facial redness.
From the digestive tract: abdominal pain, dyspepsia, diarrhea, nausea, vomiting, constipation.
From the hepatobiliary system: hepatitis.
Skin and subcutaneous tissue disorders: rash, itching, urticaria, acute generalized exanthematous pustular rash, angioedema.
From the blood and lymphatic system: agranulocytosis, thrombocytopenia, thrombocytopenic purpura.
General disorders: asthenia.
The preparation should not be used to relieve angina attacks. it should not be prescribed for unstable angina or myocardial infarction as primary therapy in the prehospital phase or in the early days of hospitalization.
In the event of an attack of unstable angina pectoris against the background of current therapy, it is necessary to revise the course of the disease and adjust the treatment (preparation therapy and the possibility of revascularization).
Trimetazidine can cause or worsen the course of symptoms of parkinsonism (tremor, akinesia, muscle hypertonicity), which should be monitored regularly, especially in elderly patients. In doubtful cases, patients should be referred to a neurologist for appropriate examination.
With the appearance of movement disorders, such as symptoms of parkinsonism, tremors, restless legs syndrome, unsteadiness of gait, it is necessary to discontinue the preparation. These cases have a low incidence and usually disappear after discontinuation of treatment, in most patients within 4 months after discontinuation of trimetazidine. If the symptoms of parkinsonism persist for 4 months after discontinuation of the preparation, it is necessary to consult a neurologist.
Falls associated with gait instability or arterial hypotension are possible, especially in patients with antihypertensive preparations.
Use with caution in patients with moderate renal impairment; elderly people (over 75 years old).
The presence of sunset yellow (E110) and ponceau 4R (E124) dyes in the preparation can cause allergic reactions.
To achieve a modified (sustained) release of the active substance, a special tablet structure (matrix) has been developed. The active substance, which provides the therapeutic effect of Triductan MB, is gradually released from the tablet as it passes through the digestive system. However, in some cases, the scaffold structure of the matrix may exit the body in the form of a tablet. This feature does not affect the therapeutic properties of the preparation.
Use during pregnancy and lactation. There are no data on the use of the preparation during pregnancy. It is not known whether trimetazidine and its metabolites pass into breast milk. Triduktan is not recommended for use during pregnancy and lactation.
Children. The safety and effectiveness of trimetazidine in children have not been established. No data available.
The ability to influence the reaction rate when driving or operating machinery. Trimetazidine does not affect hemodynamics. Cases of dizziness and drowsiness have been recorded (see SIDE EFFECTS), which can affect the ability to drive vehicles or work with mechanisms.
Triduktan. the interaction of the preparation triductan with other preparations that would lead to a negative effect has not been described.
The use of Triductan in combination with nitrates, β-adrenergic receptor blockers or calcium antagonists provides an additional therapeutic effect in patients with angina pectoris.
Trimetazidine can be prescribed in combination with heparin, vitamin K antagonists (without potentiating their action), as well as with ACE inhibitors, oral lipid-lowering preparations, acetylsalicylic acid.
Triduktan MV. To date, no interactions with other preparationshave been reported. Trimetazidine can be prescribed in combination with heparin, calciparin, vitamin K antagonists, oral lipid-lowering preparations, acetylsalicylic acid, β-adrenergic receptor blockers, calcium antagonists, digitalis preparations (trimetazidine does not affect the level of digoxin in plasma), and other preparations.
Data on trimetazidine overdose are limited. symptomatic treatment.
In its original packaging at a temperature not exceeding 25 ° C.
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