Preductal OD capsules with prolonged release 80 mg 30 pcs. in Moscow

Preductal OD capsules with prolonged release 80 mg 30 pcs. in Moscow

Trimetazidine prevents a decrease in intracellular adenosine triphosphate (ATP) concentration by maintaining the energy metabolism of cells in a state of hypoxia. Thus, the drug ensures the normal functioning of membrane ion channels, the transmembrane transport of potassium and sodium ions and the preservation of cellular homeostasis.

Trimetazidine inhibits the oxidation of fatty acids due to the selective inhibition of the enzyme 3-ketoacyl-CoA thiolase (3-CAT) of the mitochondrial long-chain isoform of fatty acids, which leads to increased oxidation of glucose and acceleration of glycolysis with oxidation of glucose, which determines the protection of the myocardium from ischemia. The switch of energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine.

Pharmacodynamic properties:

• supports energy metabolism of the heart and neurosensory tissues during ischemia;
• reduces the severity of intracellular acidosis and changes in the transmembrane ion flow that occur during ischemia;
• reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused heart tissues;
• reduces the size of myocardial damage;
• does not have a direct effect on hemodynamic parameters.

In patients with angina, trimetazidine:

• increases coronary reserve thereby slowing down the onset of exercise-induced ischemia starting from the 15th day of therapy;
• limits fluctuations in blood pressure caused by physical activity without significant changes in heart rate;
• significantly reduces the frequency of angina attacks and the need for short-acting nitroglycerin;
• improves contractile function of the left ventricle in patients with ischemic dysfunction.

The results of clinical studies have confirmed the effectiveness and safety of trimetazidine in patients with stable angina, both in monotherapy and as part of combination therapy when the effect of other antianginal drugs is insufficient.

In a study of 426 patients with stable angina, adding trimetazidine (60 mg/day) to metoprolol 100 mg/day (50 mg twice daily) for 12 weeks statistically significantly improved exercise test scores and clinical symptoms compared with placebo: the total duration of stress tests was +201 s p=0023 total time for performing the load +054 METs p=0001 time until the development of ST segment depression by 1 mm +334 s p=0003 time until the development of an angina attack +339 s p<0001 number of angina attacks per week -073 p=0014 and consumption of short-acting nitrates per week -063 p=0032 without hemodynamic changes.

In a study of 223 patients with stable angina, the addition of trimetazidine 35 mg twice daily to atenolol 50 mg once daily for 8 weeks increased the time to development of ischemic ST segment depression by 1 mm (+344 with p=003) during stress tests in a subgroup of patients (n=173) compared with placebo 12 hours after taking the drug. This difference was also shown for the time of development of angina attacks (p=0049). There were no significant differences between groups for other secondary endpoints (total duration of exercise tests, total exercise time and clinical endpoints).

In a study of 1962 patients with stable angina, trimetazidine at two doses (70 mg/day and 140 mg/day) was added to atenolol 50 mg/day compared with placebo. In the general population, including patients with both asymptomatic and symptomatic angina, trimetazidine did not demonstrate benefit on ergometric (total duration of stress tests, time to onset of ischemic ST-segment depression by 1 mm and time to onset of angina) and clinical endpoints. However, in a post-hoc analysis of a subgroup of patients with symptomatic angina (n=1574), trimetazidine (140 mg) significantly improved total exercise test time (+238 s versus +131 s for placebo; P=.0001) and time to onset of angina ( +463 s versus +325 for placebo; p=0005).

Preductal OD (caps.prolon.high.80mg No.60)

A country

Russia
The country of production may vary depending on the batch of goods. Please check with the operator for detailed information when confirming your order.

Compound

For 1 caps.# trimetazidine dihydrochloride (in granules) 80 mg. #1 extended-release hard capsule contains: trimetazidine dihydrochloride film-coated granules: 144.85 mg. Excipients: sugar spheres** (710-850 microns) - 36.68 mg, hypromellose - 6.4 mg. Film shell composition: ethylcellulose - 8 mg, tributylacetyl citrate - 1.2 mg, talc - 12 mg. Composition for dusting granules: talc - 0.43 mg, magnesium stearate - 0.14 mg. Hard gelatin capsule No. 2 with a white body and an orange-red cap, with a white logo printed on the cap*: 61,000 mg. Composition of the capsule body: titanium dioxide (E171) - 0.732 mg, gelatin*** - 35.868 mg. Composition of the capsule cap: titanium dioxide (E171) - 0.122 mg, red iron oxide (E172) - 0.366 mg, gelatin*** - 23.912 mg. 9 pcs. - blisters (3) - cardboard packs. 10 pieces. - blisters (3) - cardboard packs. 10 pieces. - blisters (6) - cardboard packs. * The logo and inscription on the capsule are printed with white ink containing shellac, titanium dioxide, simethicone, propylene glycol, ammonium hydroxide. The total amount of ink per capsule is approximately 0.15 mg. ** Composition of sugar spheres: sucrose - no more than 92% (in terms of dry matter), corn starch. May also contain starch hydrolysis products and dyes. *** Contains an average of 14.5% water (mass loss on drying).

pharmachologic effect

Mechanism of action. Trimetazidine prevents a decrease in intracellular adenosine triphosphate (ATP) concentration by maintaining the energy metabolism of cells in a state of hypoxia. Thus, the drug ensures the normal functioning of membrane ion channels, transmembrane transport of potassium and sodium ions and the preservation of cellular homeostasis. Trimetazidine inhibits the oxidation of fatty acids due to the selective inhibition of the enzyme 3-ketoacyl-CoA thiolase (3-CAT) of the mitochondrial long-chain isoform of fatty acids, which leads to increased oxidation of glucose and acceleration of glycolysis with oxidation of glucose, which determines the protection of the myocardium from ischemia. The switch of energy metabolism from fatty acid oxidation to glucose oxidation underlies the pharmacological properties of trimetazidine. Pharmacodynamic properties - supports the energy metabolism of the heart and neurosensory tissues during ischemia; — reduces the severity of intracellular acidosis and changes in the transmembrane ion flow that occur during ischemia; - reduces the level of migration and infiltration of polynuclear neutrophils in ischemic and reperfused heart tissues; - reduces the size of myocardial damage; - does not have a direct effect on hemodynamic parameters. In patients with angina pectoris, trimetazidine increases coronary reserve, thereby slowing the onset of exercise-induced ischemia, starting from the 15th day of therapy; limits fluctuations in blood pressure caused by physical activity without significant changes in heart rate; significantly reduces the frequency of angina attacks and the need for short-acting nitroglycerin; improves contractile function of the left ventricle in patients with ischemic dysfunction. The results of clinical studies have confirmed the effectiveness and safety of trimetazidine in patients with stable angina, both in monotherapy and as part of combination therapy when the effect of other antianginal drugs is insufficient. In a study of 426 patients with stable angina, the addition of trimetazidine (60 mg/day) to metoprolol 100 mg/day (50 mg twice daily) for 12 weeks statistically significantly improved exercise test scores and clinical symptoms compared with placebo: total duration of stress tests was +20.1 s, p=0.023, total time of exercise +0.54 METs, p=0.001, time to development of ST segment depression by 1 mm +33.4 s, p=0.003, time to development of angina attack + 33.9 s, p In a study of 223 patients with stable angina, the addition of trimetazidine 35 mg twice daily to atenolol 50 mg once daily for 8 weeks increased the time to development of ischemic depression ST segment by 1 mm (+34.4 s, p = 0.03) during stress tests in a subgroup of patients (n = 173), compared with placebo, 12 hours after taking the drug. This difference was also shown for the time of development of angina attacks (p=0.049). There were no significant differences between groups for other secondary endpoints (total exercise test duration, total exercise time, and clinical endpoints). In a study of 1962 patients with stable angina, trimetazidine at two doses (70 mg/day and 140 mg/day) was added to atenolol 50 mg/day versus placebo. In the general population, including patients with both asymptomatic and symptomatic angina, trimetazidine did not demonstrate benefit on ergometric (total duration of exercise tests, time to ischemic ST-segment depression of 1 mm, and time to onset of angina) and clinical endpoints. . However, in a post-hoc analysis of a subgroup of patients with symptomatic angina (n=1574), trimetazidine (140 mg) significantly improved total exercise test time (+23.8 s versus +13.1 s for placebo; p=0.001) and time to angina onset (+46.3 s versus +32.5 for placebo; p=0.005).

Indications for use

- long-term therapy of coronary artery disease: prevention of attacks of stable angina as part of mono- or combination therapy.

Mode of application

The drug is taken orally, 1 capsule 1 time/day, in the morning, during breakfast. Capsules should be taken whole, without chewing, with water. Evaluation of the benefit of treatment can be carried out after 3 months of taking the drug. Taking Preductal® OD should be stopped if there is no improvement within this time. The duration of treatment is determined by the doctor. Special groups of patients. Patients with renal failure. In patients with moderate renal failure (creatinine clearance 30-60 ml/min) (see sections “Pharmacokinetics” and “Special instructions”), a dose reduction is recommended, i.e. 1 tablet containing 35 mg trimetazidine per day. Patients with impaired liver function. Caution should be exercised when treating patients with severe hepatic impairment (see section "Special Instructions") due to the fact that the available data are limited and do not allow us to completely exclude the lack of influence of liver dysfunction on the metabolism of trimetazidine. Patients over 75 years of age. In patients over 75 years of age, increased exposure to trimetazidine may occur due to age-related decline in renal function (see Pharmacokinetics section). In patients with moderate renal failure (creatinine clearance 30-60 ml/min), a dose reduction is recommended, i.e. 1 tablet containing 35 mg trimetazidine per day. Dose selection in patients over 75 years of age should be done with caution (see section "Special Instructions"). Patients under 18 years of age. The safety and effectiveness of trimetazidine in patients under 18 years of age have not been established. No data available.

Interaction

Not observed. The patient must inform the doctor about all medications taken.

Side effect

Adverse reactions, defined as adverse events at least possibly related to treatment with trimetazidine, are given in the following gradation: very often (? 1/10); often (?1/100, From the central nervous system: often - dizziness, headache; unspecified frequency - symptoms of parkinsonism (tremor, akinesia, increased tone), "unsteadiness" of gait, restless legs syndrome, other associated motor disorders, usually reversible after cessation of therapy. Sleep disturbances (insomnia, drowsiness). From the cardiovascular system: rarely - palpitations, extrasystole, tachycardia, marked decrease in blood pressure, orthostatic hypotension, which may be accompanied by general weakness, dizziness or loss of balance, especially with simultaneous use of antihypertensive drugs, "flushes" of blood to the skin of the face. From the digestive system: often - abdominal pain, diarrhea, dyspepsia, nausea, vomiting; unspecified frequency - constipation. From the liver and biliary tract: unspecified frequency - hepatitis. With from the hematopoietic and lymphatic systems: unspecified frequency - agranulocytosis, thrombocytopenia, thrombocytopenic purpura. From the skin and subcutaneous fat: often - skin rash, itching, urticaria; unspecified frequency - acute generalized exanthematous pustulosis, Quincke's edema. General disorders: often - asthenia.

Contraindications

- hypersensitivity to any of the components of the drug; - Parkinson's disease, symptoms of parkinsonism, tremor, restless legs syndrome and other associated movement disorders; - severe renal failure (creatinine clearance less than 30 ml/min); - fructose/sucrose intolerance, the presence of glucose-galactose malabsorption syndrome, sucrase-isomaltase deficiency and other enzymopathies associated with intolerance to sucrose, which is part of the drug; - due to the lack of sufficient clinical data, the drug is not recommended for patients under 18 years of age; The drug should be prescribed with caution to patients with severe liver failure (from 10 to 15 points on the Child-Pugh scale), moderate renal failure (creatinine clearance 30-60 ml/min), patients over 75 years of age (see sections "Regimen" dosing" and "Special instructions").

Overdose

There is only very limited information on trimetazidine overdose. In case of overdose, symptomatic therapy should be carried out.

special instructions

Preductal® OD is not intended for the relief of angina attacks and is not indicated for the initial course of treatment of unstable angina or myocardial infarction in the prehospital stage or in the first days of hospitalization. If an attack of angina occurs, treatment (drug therapy or revascularization procedure) should be reviewed and adapted. Preductal® OD can cause or worsen symptoms of parkinsonism (tremor, akinesia, increased tone), so patients should be regularly monitored, especially the elderly. In doubtful cases, patients should be referred to a neurologist for appropriate examination. If movement disorders appear, such as symptoms of parkinsonism, restless legs syndrome, tremor, unsteadiness of gait, Preductal® OD should be permanently discontinued. Such cases are rare and symptoms usually resolve after discontinuation of therapy: in most patients, within 4 months after discontinuation of the drug. If symptoms of parkinsonism persist more than 4 months after discontinuation of the drug, you should consult a neurologist. There may be cases of falls associated with instability in the Romberg position and “wobbly” gait or a pronounced decrease in blood pressure, especially in patients taking antihypertensive drugs (see section “Side effects”). Preductal® OD should be prescribed with caution to patients in whom its exposure may increase: - with moderate renal failure (see sections “Pharmacological action” and “Dosage regimen”); - in elderly patients over 75 years of age (see section "Dosage regimen"). The drug contains sucrose, so the drug is not recommended for patients with fructose intolerance, glucose-galactose malabsorption syndrome and sucrase-isomaltase deficiency. Influence on the ability to drive vehicles and operate machinery. During clinical studies, no effect of trimetazidine on hemodynamic parameters was revealed, however, during the period of post-registration use, cases of dizziness and drowsiness were observed (see section “Side effects”). These symptoms can affect the ability to drive vehicles and perform work that requires increased speed of physical and mental reactions.

Dispensing conditions in pharmacies

On prescription