Trimetazidine-Biocom MB, 35 mg 30 pcs

Pharmacotherapeutic group: antihypoxant drug.

ATC code C01EB15

Pharmacological properties

Pharmacodynamics

Trimetazidine has antianginal, antihypoxic effect. By directly influencing cardiomyocytes and brain neurons it optimizes their metabolism and function. Cytoprotective effect is due to increased energy potential, activation of oxidative decarboxylation and rationalization of oxygen consumption (enhancement of aerobic glycolysis and blockade of fatty acid oxidation). It supports myocardial contractility, prevents decrease in intracellular ATP and phosphocreatinine content. Under acidosis, it normalizes the functioning of ion channels, prevents the accumulation of calcium and sodium in cardiomyocytes and normalizes the intracellular content of potassium ions.

Creases intracellular acidosis and phosphate concentration caused by myocardial ischemia and reperfusion. Prevents damaging action of free radicals, maintains integrity of cell membranes, prevents activation of neutrophils in ischemic area, increases duration of electric potential, decreases release of creatine phosphokinase from cells and intensity of ischemic myocardial damage.

In angina pectoris it reduces the frequency of attacks (nitrates consumption decreases), after 2 weeks of treatment the tolerance to physical load increases, blood pressure fluctuations decrease. Hearing and results of vestibular tests of patients improve, dizziness and tinnitus decrease.

In case of vascular eye pathology, it restores functional activity of the retina.

Pharmacokinetics

After oral administration of the drug, trimetazidine is quickly and almost completely absorbed from the gastrointestinal tract. Bioavailability is 90%. Time of reaching maximum concentration in blood plasma is 2 hours. Maximum concentration after a single dose of 35 mg of trimetazidine is about 55 ng/ml. Easily penetrates through histohematic barriers. The half-life (T1/2) is 4.5-5 hours. Blood plasma protein binding is 16%. It is excreted by kidneys (about 60% unchanged).

Pharmacokinetics in special groups of patients

Patients with renal dysfunction

Pharmacokinetics in special groups of patients

Exposure to trimetazidine was on average 2.4-fold increased in patients with moderate renal impairment (creatinine clearance (CK) 30-60 mL/min) and on average 4-fold increased in patients with severe renal impairment (CK less than 30 mL/min) compared with patients with normal renal function.

No differences were found regarding safety in this patient population compared to the general population.

Elderly Patients

In patients older than 75 years, increased exposure to trimetazidine may be observed due to age-related decline in renal function.

Indications

Active ingredient

Composition

1 coated modified-release tablet contains:

the active substance: trimetazidine dihydrochloride – 35.00 mg;

excipients: calcium hydrophosphate dihydrate – 79.93 mg, hypromellose (hydroxypropyl methylcellulose) – 57.40 mg, prosolv (silicified microcrystalline cellulose) – 20.50 mg, potato starch – 3.07 mg, colloidal silicon dioxide (aerosil) – 2.05 mg, magnesium stearate – 2.05 mg;

coating composition: Hypromellose (hydroxypropyl methylcellulose) – 3.476 mg, macrogol (polyethylene glycol) – 0.524 mg, titanium dioxide E 171 – 0.976 mg, iron oxide red dye E 172 – 0.024 mg.

How to take, the dosage

Overly, with meals.

The recommended dosing regimen is 2 tablets (70 mg) per day, in 2 doses. The course of treatment is according to the doctor’s recommendation.

Patients with renal impairment

In patients with moderate renal impairment (CKR 30-60 ml/min), the daily dose is 35 mg in the morning with breakfast.

Elderly patients

In patients over 75 years of age, increased exposure to trimetazidine may be observed due to age-related decreases in renal function.

Dose selection in patients over 75 years of age should be done with caution.

Special Instructions

The drug is not intended to control angina attacks and is not indicated for initial therapy of unstable angina or myocardial infarction in the pre-hospital phase or in the first days of hospitalization.

In the event of an angina attack, treatment (drug therapy or revascularization) should be reviewed and adapted.

Trimetazidine-Biocom MB may cause or worsen the symptoms of parkinsonism (tremor, akinesia, increased tone), therefore patients, especially elderly patients, should be monitored regularly. In doubtful cases, patients should be referred to a neurologist for appropriate evaluation.

Trimetazidine-Biocom MB should be permanently withdrawn if movement disorders such as parkinsonian symptoms, restless legs syndrome, tremor, unsteadiness in the Romberg posture and wobbly gait occur.

These cases are rare and symptoms usually disappear after discontinuation of therapy: in most patients within 4 months of discontinuation. If the parkinsonian symptoms persist longer than 4 months after discontinuation, a neurologist should be consulted.

There may be some falls associated with unsteadiness in the Romberg pose and a “wobbly” gait, or a marked decrease in BP, particularly in patients taking hypotensive medications (see section “Adverse effects”).

Trimetazidine-Biocom MB should be administered with caution in patients who may have increased exposure to:

– In moderate renal impairment (see “Pharmacological properties” and “Dosage and administration” sections).

– In elderly patients older than 75 years (see section “Pharmacological properties”).

Impact on the ability to drive vehicles and perform work requiring high-speed psychomotor reactions

With regard to the possibility of developing adverse reactions in the central nervous system when taking trimetazidine (see section “Adverse effects”), caution should be exercised when driving vehicles and performing work requiring high-speed physical and mental reactions.

Contraindications

– Parkinson’s disease, Parkinsonian symptoms, tremor, restless legs syndrome and other related movement disorders;

– Severe renal impairment (CKR below 30 ml/min);

– Age under 18 years (effectiveness and safety not established).

With caution

– Severe hepatic impairment (clinical data are limited);

Side effects

Overly, with meals.

The recommended dosing regimen is 2 tablets (70 mg) per day, in 2 doses. The course of treatment is according to the doctor’s recommendation.

Patients with renal impairment

In patients with moderate renal impairment (CKR 30-60 ml/min), the daily dose is 35 mg in the morning with breakfast.

Elderly patients

In patients over 75 years of age, increased exposure to trimetazidine may be observed due to age-related decreases in renal function.

Dose selection in patients over 75 years of age should be done with caution.

Overdose

Limited information is available on trimetazidine overdose. In case of overdose symptomatic therapy should be administered.

Pregnancy use

There are no data on the use of Trimetazidine-Biocom MB in pregnant women. Animal studies have shown no direct or indirect reproductive toxicity. Reproductive toxicity studies have shown no effect of Trimetazidine on the reproductive function of rats of either sex. As a precautionary measure, Trimetazidine-Biocom MB is not recommended for use during pregnancy.

There are no data on excretion of trimetazidine or its metabolites into breast milk. The risk to the newborn/infant cannot be excluded. Trimetazidine-Biocom MB should not be used during breastfeeding.

Similarities