Preduktal MB, 35 mg 60 pcs

Trimetazidine prevents decrease in intracellular concentration of adenosine triphosphate (ATP) by preserving energy metabolism of cells under hypoxia.

Thereby, the drug ensures normal functioning of membrane ion channels, transmembrane transport of potassium and sodium ions and preservation of cellular homeostasis.

. Trimetazidine inhibits fatty acid oxidation through selective inhibition of the enzyme 3-ketoacyl-CoA-thiolase (3- CAT) mitochondrial long-chain fatty acid isoform, which leads to increased glucose oxidation and accelerated glucose-oxidized glycolysis, which is responsible for myocardial protection from ischemia.

The switch of energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine.

Trimetazidine has been experimentally confirmed to have the following properties:

• maintains energy metabolism of cardiac and neurosensory tissues during ischemia;
• reduces the severity of intracellular acidosis and changes in transmembrane ion flow occurring during ischemia;
• reduces the extent of myocardial damage;
• does not directly affect hemodynamic parameters.

In patients with angina pectoris, trimetazidine:

• increases coronary reserve, thereby delaying the onset of exercise-induced ischemia beginning on day 15 of therapy;
• limits exercise-induced blood pressure fluctuations without significant changes in heart rate;
• significantly reduces the frequency of angina attacks and the need to take short-acting nitroglycerin;
• improves left ventricular contractile function in patients with coronary dysfunction.

In a 2-month clinical trial, the addition of 35 mg modified-release trimetazidine tablets to 50 mg atenolol therapy 12 hours after oral administration was shown to significantly delay the onset of ischemic ST-segment depression on loading tests.

Pharmacokinetics

Trimetazidine is rapidly absorbed after oral administration and reaches maximum plasma concentration approximately 5 hours later.

After 24 hours, the plasma concentration remains at a level greater than 75% of the concentration determined after 11 hours. The equilibrium state is reached after 60 hours. Food intake does not affect the bioavailability of trimetazidine.

The volume of distribution is 4.8 l/kg, which indicates good distribution of trimetazidine in tissues (the degree of binding to plasma proteins is quite low, about 16 %in vitro).

Trimetazidine is mainly excreted by the kidneys, mainly unchanged.
The elimination half-life in young healthy volunteers is about 7 hours, in patients older than 65 years – about 12 hours.

The renal clearance of trimetazidine directly correlates with creatinine clearance (CK), hepatic clearance decreases with patient age.

In elderly patients taking a daily dose of 2 tablets of trimetazidine in two doses, increased plasma exposure has not been shown to have any more pronounced effects than placebo.

Indications

Cardiology: long-term therapy of coronary heart disease: prevention of stable angina attacks in mono- or combined therapy. ENT diseases: treatment of vestibulo-cochlear disorders of ischemic nature, such as dizziness, tinnitus, hearing disorders.

Ophthalmology: chorioretinal disorders with ischemic components.

Active ingredient

Composition

Active ingredient:

Trimetazidine dihydrochloride 35 mg;

Auxiliary substances:

calcium hydrophosphate dihydrate – 80.9 mg;

povidone – 8.7 mg;

hypromellose – 74 mg;

Magnesium stearate – 1 mg;

Silicon dioxide colloid – 0.4 mg;

Macrogol 6000 – 0.1317 mg;

Shell:

N5361 rose-coated dry premix consisting of titanium dioxide – 0.6908 mg, iron oxide red dye – 0.0103 mg, glycerol – 0.2191 mg, hypromellose – 3.6414 mg, magnesium stearate – 0.2191 mg, macrogol 6000 – 0.0876 mg;

How to take, the dosage

Overly, whole, without chewing, with water, 1 tablet 2 times a day, morning and evening, with meals.

The duration of treatment is determined by the doctor.

The maximum daily dose is 70 mg.

Special Instructions

Preductal® MV is not indicated for the management of 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 procedure) should be reviewed and adapted.

Preductal® MB may cause or worsen 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.

If movement disorders such as parkinsonian symptoms, restless legs, tremor, unsteadiness in the Romberg posture and wobbly gait occur, Preductal®MV should be permanently discontinued.

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

There may be cases of falls associated with unsteadiness in the Romberg posture and a “wobbly” gait or a marked decrease in BP, especially in patients taking hypotensive medications (see “Adverse Effects”).

Preduptal® MV should be administered with caution in patients in whom its exposure may be increased:

– in moderate renal impairment (see “Pharmacokinetics and pharmacokinetics”). “Pharmacokinetics” and “Dosage and administration”);

– in elderly patients over 75 years of age (see “Dosage and administration”).

Impact on the ability to drive vehicles and perform work requiring high psychomotor reactions. No effect of drug Preduktal® MB on hemodynamic parameters was revealed during the clinical trials, however during the post-registration period there were cases of dizziness and somnolence (see “Adverse reactions”), which can affect the ability to drive vehicles and perform work requiring high rate of physical and mental reactions.

Contraindications

Side effects

Digestive system: often – abdominal pain, diarrhea, dyspepsia, nausea, vomiting; unspecified frequency – constipation.

General disorders: often – asthenia.

CNS disorders: frequently – dizziness, headache; unspecified frequency – parkinsonian symptoms (tremor, akinesia, increased tone), unsteadiness in Romberg posture and “wobbly” gait, “restless” legs syndrome, other related motor disorders, usually reversible after discontinuation of therapy, sleep disorders (insomnia, somnolence).

Skin and subcutaneous fat: frequently – skin rash, itching, urticaria; unspecified frequency – acute generalized exanthematous pustulosis, Quincke’s edema.

Systems: rarely – palpitation, extrasystole, tachycardia, marked BP decrease, orthostatic hypotension, which may be accompanied by general weakness, dizziness or loss of balance, especially with simultaneous use of hypotensive drugs, flushes to the skin.

Blood and lymphatic system disorders: unspecified frequency – agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

Hepatic and biliary tract disorders: unspecified frequency – hepatitis.

Similarities