Instructions for use Triductan MB film-coated tablets with modified release 35 mg blister No. 60
Composition
active ingredient: trimetazidine;
1 tablet contains trimetazidine dihydrochloride 35 mg;
excipients: mannitol (E 421), microcrystalline cellulose, montan glycol wax, magnesium stearate, ammonium methacrylate copolymer (type B), coating for applying the shell Opadry II Pink (iron oxide red (E 172), polyethylene glycol, iron oxide yellow (E 172), polyvinyl alcohol, talc, titanium dioxide (E 171), iron oxide black (E 172).
Dosage form
Modified-release film-coated tablets.
Main physicochemical properties: round tablets with a biconvex surface, coated with a pink film coating.
Pharmacotherapeutic group
Cardiological drugs. Trimetazidine.
ATX code C01E B15.
Pharmacological properties
Pharmacodynamics
By preserving energy metabolism in cells exposed to hypoxia or ischemia, trimetazidine prevents a decrease in intracellular ATP levels, thereby ensuring the proper functioning of ion pumps and transmembrane sodium-potassium flux 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 oxidation of glucose requires less oxygen compared to the process of obtaining energy by β-oxidation of fatty acids.
Enhancing the process of glucose oxidation optimizes energy processes in cells and accordingly supports energy metabolism in conditions of ischemia.
In patients with coronary heart disease, trimetazidine acts as a metabolic agent, preserving intracellular levels of high-energy phosphates in the myocardium. The effects are achieved without concomitant hemodynamic changes.
Pharmacokinetics
The maximum concentration of trimetazidine in the blood is observed on average 5 hours after taking the tablet. The concentration in the blood plasma is stable throughout the day: within 11 hours after taking the tablet, the concentration of trimetazidine in the blood plasma is equal to or higher than 75% of the maximum concentration.
The steady state concentration is established, at the latest, by 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 and is 16%.
Trimetazidine is excreted mainly in the urine, mostly in unchanged form.
The elimination half-life of the drug is on average 7 hours for healthy young volunteers and 12 hours for elderly people. The complete elimination of trimetazidine is the result of renal clearance, which is directly related to creatinine clearance and, to a lesser extent, hepatic clearance, which decreases with age. In elderly patients, due to decreased renal function, an increase in trimetazidine plasma concentrations is observed, which requires dose adjustment.
Renal impairment: The concentration of trimetazidine in the blood increases in patients with moderate renal insufficiency (creatinine clearance - 30-60 ml/min) and in patients with severe renal insufficiency (creatinine clearance < 30 ml/min).
Indication
Symptomatic treatment of adult patients with stable angina pectoris when first-line antianginal drugs are ineffective or intolerant.
Contraindication
increased individual sensitivity to trimetazidine or to any of the components of the drug; Parkinson's disease, parkinsonism symptoms, tremor, restless legs syndrome and other movement disorders; severe renal failure (creatinine clearance < 30 ml/min).
Interaction with other medicinal products and other types of interactions
No interactions with other drugs have been reported so far. Trimetazidine can be administered in combination with heparin, calciparin, vitamin K antagonists, oral lipid-lowering drugs, acetylsalicylic acid, beta-blockers, calcium antagonists, digitalis drugs (trimetazidine does not affect the level of digoxin in the blood plasma), and other antianginal drugs.
Application features
The drug 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 stage or in the first days of hospitalization.
In the event of an attack of unstable angina during current therapy, it is necessary to review the course of the disease and adjust the patient's treatment (drug therapy and the possibility of revascularization).
Trimetazidine may cause or worsen parkinsonian symptoms (tremor, akinesia, muscle hypertonia), which should be monitored regularly, especially in elderly patients. In doubtful cases, patients should be referred to a neurologist for appropriate examination.
The incidence of motor disorders is low. They are generally reversible, disappearing after discontinuation of trimetazidine in most patients within 4 months. If parkinsonism symptoms persist for more than 4 months after discontinuation of the drug, a neurologist should be consulted.
Falls may occur due to gait instability or hypotension, especially in patients taking antihypertensive medications.
It should be used with caution in patients:
with moderate renal impairment; elderly patients (≥ 75 years of age).
To achieve a modified (delayed) release of the active substance, a special tablet structure (matrix) has been developed. The active substance, which provides the therapeutic effect of the drug, is gradually released from the tablet as it passes through the digestive system. However, in some cases, the skeleton structure of the matrix can exit the human body in the form of a tablet. This feature does not affect the therapeutic properties of the drug.
Ability to influence reaction speed when driving vehicles or other mechanisms
Trimetazidine does not affect hemodynamics. There have been reports of dizziness and drowsiness, which may affect the ability to drive or operate machinery.
Use during pregnancy or breastfeeding
Due to the lack of clinical data, the use of the drug is not recommended during pregnancy or breastfeeding.
Method of administration and doses
The drug is taken orally, 1 tablet 2 times a day: in the morning and in the evening, during meals, with sufficient 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 reviewed after 3 months.
Special patient groups.
Patients with renal impairment.
For patients with moderate renal impairment (creatinine clearance 30-60 ml/min), the recommended dose is 1 tablet per day in the morning with a meal.
Elderly patients.
Elderly patients are more sensitive to the effects 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 food.
For elderly patients, dose titration should be done with caution.
Children
The safety and effectiveness of trimetazidine in children have not been established.
Data is missing.
Overdose
There is limited data on overdose with trimetazidine. Treatment is symptomatic.
Adverse reactions
Adverse reactions that have been identified as possible adverse reactions related to the use of trimetazidine are listed with the following frequency: very common (≥1/10); common (≥1/100, <1/10); uncommon (≥1/1000, <1/100); rare (≥1/10,000, <1/1000); very rare (<1/10,000); frequency unknown (cannot be estimated from the available information):
Nervous system: often - headache, dizziness; frequency unknown - possible occurrence of parkinsonism symptoms (tremor, akinesia, muscle hypertonia), gait instability, restless legs syndrome and other movement disorders related to the above, which are reversible after drug withdrawal; sleep disorders (insomnia, drowsiness); hearing and vestibular system: frequency unknown - vertigo. Cardiac disorders: rarely - palpitations, extrasystole, tachycardia; vascular system: rarely - arterial hypotension, orthostatic hypotension, which may be associated with malaise, dizziness or falls (in particular in patients taking antihypertensive drugs), facial flushing; digestive tract: often - abdominal pain, diarrhea, dyspepsia, nausea and vomiting; frequency unknown - constipation; Hepatobiliary system: frequency unknown - hepatitis; Skin and subcutaneous tissue disorders: common - rash, itching, urticaria; frequency unknown - acute generalized exanthematous pustular rash, angioedema; Blood and lymphatic system disorders: frequency unknown - agranulocytosis, thrombocytopenia, thrombocytopenic purpura; General disorders: common - asthenia.
Expiration date
3 years.
Storage conditions
Store out of the reach of children, in the original packaging at a temperature not exceeding 25 ºС.
Packaging
20 tablets in a blister, 3 blisters in a cardboard pack.
Vacation category
According to the recipe.
Producer
"Pharma Start" LLC.
Location of the manufacturer and its business address
Ukraine, 03124, Kyiv, Vaclav Havel Boulevard, 8.
