Preductal tablets: instructions for use, indications, price, analogues and reviews about the medicine

Pharmacodynamics and pharmacokinetics

The main substance trimetazidine is able to prevent a decrease in the concentration of adenosine triphosphate inside cells, due to the preservation of energy metabolism at the cellular level in a state of hypoxia. At the same time, as Wikipedia reports, the normal operation of membrane ion channels, transmembrane transport of potassium or sodium ions is ensured, and cellular homeostasis is maintained.

The drug Preductal activates several complex processes in the body, due to which the myocardium from possible ischemia.

The pharmacological properties of trimetazidine make it possible to switch energy metabolism from the oxidation of fatty acids to glucose.

In general, during ischemia, trimetazidine is characterized by:

providing support for cardiac energy metabolism and neurosensory tissues;
decreased severity of intracellular acidosis and some changes related to transmembrane ion flow;
reducing the level of infiltration and migration of polynuclear neutrophils in the area of ischemic and reperfused cardiac tissue;
reducing the size of myocardial damage.

In this case, there is no direct effect on hemodynamic parameters.

As for the treatment of patients suffering from angina , what usually happens:

an increase in coronary reserve, which slows down the development of ischemia caused by physical activity;
limiting fluctuations in blood pressure during physical activity, without having a particular effect on the heart rate;
reducing the frequency of angina attacks and the need for short-acting nitroglycerin;
improvement of contractile function of the left ventricle in ischemic dysfunction.

After oral administration, Preductal tablets are rapidly absorbed, followed by reaching a maximum concentration in the blood plasma after approximately 5 hours. At the same time, its concentration is maintained throughout the day. Eating food does not affect the bioavailability of the drug. The main substance is well distributed in tissues and body fluids.

The drug is excreted mainly through the kidneys, in unchanged form.

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).

Contraindications

Taking Preductal is contraindicated if:

sensitivity to it;
Parkinson's disease , symptoms of parkinsonism , tremor , restless legs syndrome and other movement disorders;
severe renal failure ;
under 18 years of age;
lactation , pregnancy .

Caution is necessary when prescribing the drug to patients with severe or moderate hepatic and renal insufficiency.

Preductal OD caps prolong 80 mg x30

Preductal OD caps 80 mg x30, ATX code: C01EB15 (Trimetazidine) Active substance: trimetazidine Rec.INN registered by WHO

Dosage form

PREDUCTAL® OD

caps. with extended release 80 mg: 27, 30 or 60 pcs.reg. No.: LP-003410 dated 01/13/16 - Valid

Release form, composition and packaging

Extended-release hard gelatin capsules, No. 2, with a white body and an orange-red cap, a white logo* printed on the cap, the contents of the capsule are spherical granules of white or almost white color.

1 cap.#

trimetazidine dihydrochloride (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.

Composition of the film shell of the granules: ethylcellulose - 8 mg, tributylacetyl citrate - 1.2 mg, talc - 12 mg. Composition of the mixture 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.

* 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).

Clinical and pharmacological group: Antianginal drug that improves myocardial metabolism in conditions of ischemia Pharmacotherapeutic group: Antianginal drug

pharmachologic effect

Pharmacokinetics,

Indications

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

ICD-10 codes,

Dosage regimen

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 use of the drug. If no improvement occurs during this time, use of Preductal® OD should be discontinued.

The duration of treatment is determined by the doctor.

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.

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.

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").

The safety and effectiveness of trimetazidine in patients under 18 years of age have not been established. No data available.

Side effect

Adverse reactions, defined as adverse events at least possibly related to treatment with trimetazidine, are listed in the following gradation: 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), unspecified frequency (frequency cannot be calculated from available data).

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 disorders (insomnia, drowsiness).

From the cardiovascular system: rarely - a feeling of palpitations, extrasystole, tachycardia, a marked decrease in blood pressure, orthostatic hypotension, which may be accompanied by general weakness, dizziness or loss of balance, especially with the 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.

From the hematopoietic system: unspecified frequency - agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

From the skin and subcutaneous fat: often - skin rash, itching, urticaria, unspecified frequency - Quincke's edema, acute generalized exanthematous pustulosis.

General disorders: often - asthenia.

Contraindications for use

- severe renal failure (creatinine clearance less than 30 ml/min),

- Parkinson's disease, symptoms of parkinsonism, tremor, restless legs syndrome and other related movement disorders,

- fructose/sucrose intolerance, glucose-galactose malabsorption syndrome, sucrase/isomaltase deficiency and other enzymopathies associated with intolerance to sucrose, which is part of the drug,

- age under 18 years (due to lack of sufficient clinical data),

- hypersensitivity to any of the components of the drug.

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 "Dosage regimen" and "Special Instructions").

Use during pregnancy and breastfeeding

There are no data on the use of Preductal® OD in pregnant women. Animal studies have not shown any direct or indirect reproductive toxicity. Reproductive toxicity studies have shown no effect of trimetazidine on reproductive function in rats of either sex. As a precautionary measure, it is not recommended to use Preductal® OD during pregnancy.

There is no data on the excretion of trimetazidine or its metabolites into breast milk. Risk to the newborn/child cannot be excluded. If it is necessary to use the drug Preductal® OD during lactation, breastfeeding should be stopped.

Use in hepatic impairment Caution should be exercised when treating patients with severe hepatic impairment due to the fact that the available data are limited and cannot completely exclude the absence of an effect of hepatic impairment on the metabolism of trimetazidine.

Use for impaired renal function 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.

Use in children The safety and effectiveness of trimetazidine in patients under 18 years of age have not been established. No data available.

Use in Elderly Patients Patients over 75 years of age may experience increased trimetazidine exposure due to age-related decline in renal function. Dose selection in patients over 75 years of age should be done with caution. ,

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, the patient should be referred to a neurologist for appropriate examination.

If movement disorders appear, such as symptoms of parkinsonism, restless leg syndrome, tremor, “unsteady” 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 increased exposure may occur:

- in case of 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.

Impact 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.

Overdose

There is only very limited information on trimetazidine overdose.

Treatment: in case of overdose, symptomatic therapy should be carried out.

Drug interactions

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

Conditions for dispensing from pharmacies The drug is dispensed with a prescription. ,

Storage conditions and periods

The drug should be stored out of the reach of children at a temperature not exceeding 25°C. Shelf life: 2 years.

Side effects

When taking Preductal, various undesirable reactions may develop that affect the functioning of the digestive, nervous, cardiovascular, circulatory, lymphatic and other systems.

This manifests itself as: abdominal pain, diarrhea , nausea, vomiting, constipation , dyspepsia , dizziness , headaches , tachycardia , irregular heartbeat, and so on.

Possible side effects on the skin: rash, itching and urticaria .

Preductal tablets, instructions for use (Method and dosage)

Instructions for use of Preductal recommend taking the tablets orally, in their entirety, with plenty of water.

This medicine is prescribed in a daily dosage of one tablet taken twice a day. Preferably in the morning and evening, along with food.

Detailed instructions for Preductal indicate that the duration of treatment is determined by the doctor. In this case, the drug can be taken in a maximum daily dosage of up to 70 mg.

It should be noted that the instructions for use of Preductal MR highlight the treatment of special groups of patients. Therefore, for example, for people with kidney failure, Preductal is prescribed in a daily dosage of 35 mg. It is better to take the medicine in the morning, along with breakfast.

During treatment of patients over 75 years of age, it is possible that increased exposure to trimetazidine may develop due to age-related decline in kidney function. The dosage of Preductal for this group of patients is selected only by a doctor.

PREDUCTAL OD CAPS PROL DAY-YA 80MG N30

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.

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, trimetazidine:

— increases coronary reserve, thereby slowing down the onset of ischemia caused by physical activity, 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 the contractile function of the left ventricle in patients with ischemic dysfunction.

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 to perform the load +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<0.001, number of angina attacks per week -0.73, p=0.014 and consumption of short-acting nitrates per week -0.63, p=0.032, 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 (+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 in 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 before the development of an angina attack (+46.3 s compared with +32.5 for placebo; p = 0.005).

special instructions

It has been established that Preductal is not designed to relieve attacks of angina, so it is not recommended for use for the treatment of unstable angina , as well as myocardial infarction at the initial stage or in the first days of hospitalization.

The fact is that Preductal often causes or intensifies symptoms of parkinsonism , for example, tremor , akinesia and increased tone. For this reason, regular monitoring of patients is required. If the treatment is in doubt, then an appropriate examination by a neurologist is necessary.

If movement disorders appear, for example: symptoms of parkinsonism , restless legs syndrome, tremors , instability and “wobbly” gait, you must immediately stop taking the pills. Such cases occur quite rarely and usually the symptoms disappear after discontinuation of the drug.

dizziness and drowsiness may occur . Therefore, during the treatment period, you should drive vehicles and perform work that requires quick reactions with the utmost caution.

Preductal® OD

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.

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, trimetazidine:

— increases coronary reserve, thereby slowing down the onset of ischemia caused by physical activity, 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 the contractile function of the left ventricle in patients with ischemic dysfunction.

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 exercise tests, total exercise time, time to 1 mm ST segment depression, time to angina attack, number of angina attacks per week, and short-acting nitrate intake per week, without hemodynamic changes.

In a study of 223 patients with stable angina, adding 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 during exercise tests in a subgroup of patients compared with placebo. A significant difference was also shown for the time of development of angina attacks. 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 (70 mg/day and 140 mg/day) was added to atenolol 50 mg/day compared with placebo. In the general population, including both asymptomatic and symptomatic patients with angina, trimetazidine did not demonstrate benefit on ergometric and clinical endpoints. However, in a retrospective analysis of a subgroup of patients with symptomatic angina, trimetazidine (140 mg) significantly improved total exercise test time and time to onset of angina.

Analogues of Preductal

Level 4 ATX code matches:
Vazonat

Phosphaden

Hawthorn fruit

Meldonium

Angiosil Retard

Ranexa

Lily of the valley tincture

Neocardil

Rimecore

Triductane

ATF-Long

Hawthorn tincture

Triductan MV

Trimectal MV

Trimectal

Neoton

Predisin

Trimetazidine

Tivortin Aspartate

Metamax

The drug Preductal and its analogues ATP-Long , Triductan , Kratal and Trimetazidine can only be sold with a prescription. Similar drugs are prescribed by a doctor, and you can choose a substitute only with a responsible approach.

The price of analogues may differ depending on the country and city, so it is better to find out the price of a specific medicine at the pharmacy.

Reviews about Preductal

Numerous reviews of Preductal indicate that it should be taken with extreme caution. However, some users think differently, although they don’t even know exactly why the pills are prescribed by doctors.

Sometimes some specialists in the field of cardiology also show distrust of Preductal. Therefore, reviews from cardiologists are varied. The fact is that the effect of Preductal has not been fully studied and more than one forum contains discussions on this topic. According to some experts, its effectiveness is equal to dietary supplements. Doctors prescribe a drug to improve the condition of the myocardium, constantly monitoring the patient’s condition, and if a positive result does not occur, they make an adequate replacement.

Interestingly, many patients who suffer from coronary heart disease and angina report that they feel significant improvement when treated with this drug. They also note a reduction in the number of attacks, which is what the medicine helps best with.

Thus, it becomes clear that Preductal cannot be the only and main treatment, but it can significantly improve a person’s well-being. Such drugs help normalize metabolism and the functioning of the heart muscle, so they are also considered “vitamins for the heart.” Even if they do not restore heart health, they significantly improve the functioning of the body, preventing the development of any malfunctions and disorders.

Preductal od 80mg 60 pcs. extended-release capsules laboratory servier

pharmachologic effect

Antiangial agent.

Composition and release form Preductal od 80 mg 60 pcs. extended-release capsules laboratory servier

Capsules - 1 capsule:

Active ingredient: trimetazidine dihydrochloride - 80.00 mg;
Excipients: sugar spheres (sucrose, corn starch) (710-850 microns), hypromellose;
film coating: ethylcellulose, tributylacetyl citrate, talc; mixture for dusting granules: talc, magnesium stearate;
Capsule body: titanium dioxide (E 171), gelatin; capsule cover: titanium dioxide (E 171), red iron oxide (E 172), gelatin;
Ink: Shellac, Titanium dioxide, Simethicone, Propylene glycol, Ammonium hydroxide.

10 capsules per blister made of cold-formed foil (PA/Al/PVC) and printed varnished aluminum foil. 3 or 6 blisters with instructions for medical use in a cardboard pack.

9 capsules per blister made of cold-formed foil (PA/Al/PVC) and printed varnished aluminum foil. 3 blisters with instructions for medical use per cardboard pack.

Description of the dosage form

Hard gelatin capsules No. 2 with a white body and an orange-red cap. The lid has a white logo printed on it. Capsule contents: spherical granules of white or almost white color.

Directions for use and doses

Orally, 1 capsule 1 time per day, in the morning, during breakfast.

Capsules should be taken whole, without chewing, with water.

The benefit of treatment can be assessed after three months of taking the drug. Taking the drug Preductal® OD should be stopped if no improvement has occurred during this time.

The duration of treatment is determined by the doctor.

Special groups

Patients with impaired renal function

In patients with moderate renal impairment (creatinine clearance 30-60 ml/min), a dose reduction is recommended, i.e. 1 tablet containing 35 mg trimetazidine per day.

Patients with liver dysfunction

Caution should be exercised when treating patients with severe hepatic impairment due to the fact that the available data are limited and cannot completely exclude the absence of an influence of impaired liver function on the metabolism of trimetazidine.

Elderly patients

Elderly patients may experience increased trimetazidine exposure due to age-related decline in renal function. In patients with moderate renal impairment (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.

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.

Pharmacodynamics

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.

Pharmacodynamic properties:

supports energy metabolism of the heart and neurosensory tissues during ischemia;
reduces the severity of intracellular acidosis and changes in 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 ischemia caused by physical activity, starting from the 15th day of therapy;
limits exercise-induced blood pressure fluctuations 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.

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 exercise tests, total exercise time, time to 1 mm ST segment depression, time to angina attack, number of angina attacks per week, and short-acting nitrate intake per week, without hemodynamic changes.

Pharmacokinetics

Absorption

After oral administration of the Preductal® OD capsule, trimetazidine has a linear pharmacokinetic profile and reaches maximum plasma concentration approximately 14 hours after administration. In the intervals between doses of the drug (i.e., within 24 hours), the concentration of trimetazidine in the blood plasma for 15 hours after taking the drug remains at a level of at least 75% of the maximum concentration.

An equilibrium state is achieved after taking the 3rd dose (after 3 days). Food intake does not affect the bioavailability of trimetazidine when taking the drug Preductal® OD 80 mg.

Distribution

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).

Removal

Trimetazidine is excreted mainly by the kidneys, mainly unchanged. The half-life in young healthy volunteers is about 7 hours, in patients over 65 years of age - about 12 hours.

Renal clearance of trimetazidine directly correlates with creatinine clearance (CC), hepatic clearance decreases with patient age.

Special groups

Elderly patients

A special clinical study conducted in a population of elderly patients using a dose of trimetazidine MB 35 mg, 2 tablets per day (in 2 divided doses), showed an increase in plasma levels of the drug according to population pharmacokinetic analysis.

Elderly patients may experience increased trimetazidine exposure due to age-related decline in renal function. A special pharmacokinetic study involving elderly patients (75-84 years) or very elderly (> 85 years) patients showed that moderate renal impairment (creatinine clearance 30-60 ml/min) increased trimetazidine exposure by 1.0 and 1.3 times, respectively, compared with younger patients (30-65 years) with moderate renal impairment.

Patients with impaired renal function

Trimetazidine exposure was increased on average by 1.7 times in patients with moderate renal impairment (creatinine clearance 30-60 ml/min), and on average by 3.1 times in patients with severe renal failure (creatinine clearance below 30 ml/min ) compared to healthy volunteers with normal kidney function.

No significant safety differences were observed in this patient population compared with the general population.

Use in children and adolescents

The pharmacokinetics of trimetazidine in children and adolescents under 18 years of age have not been studied.

Indications for use Preductal od 80 mg 60 pcs. extended-release capsules laboratory servier

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

Contraindications

Hypersensitivity to the active substance or any of the excipients included in the drug.

Parkinson's disease, parkinsonian symptoms, tremors, restless legs syndrome and other related movement disorders.

Severe renal failure (creatinine clearance below 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, prescribing the drug is not recommended for patients under 18 years of age.

Pregnancy and breastfeeding period.

Carefully:

Patients with severe liver failure (from 10 to 15 points on the Child-Pugh scale).

Patients with moderate renal impairment (creatinine clearance 30-60 ml/min).

Patients over 75 years of age.

Application Preductal od 80 mg 60 pcs. extended-release capsules laboratory servier during pregnancy and lactation

Pregnancy

There are no data on the use of trimetazidine in pregnant women. Animal studies have not revealed any direct or indirect negative effects on reproductive function.

The use of the drug Preductal® OD during pregnancy is contraindicated.

Breastfeeding period

There are no data on the excretion of trimetazidine or its metabolites into breast milk. Risk to the newborn/child cannot be excluded. If necessary

When using the drug Preductal® OD during lactation, breastfeeding should be stopped.

Fertility

Reproductive toxicity studies did not reveal any effect of the drug on male or female rats.

special instructions

The drug 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.

In the event of an attack of angina, the degree of damage to the coronary arteries should be re-evaluated and, if necessary, treatment should be adapted (drug therapy or a possible revascularization procedure). Trimetazidine may 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, gait instability, trimetazidine 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 trimetazidine. If symptoms of parkinsonism persist more than 4 months after discontinuation of the drug, you should consult a neurologist. Falls associated with gait instability or hypotension may occur, especially in patients taking antihypertensive drugs.

Trimetazidine should be prescribed with caution to patients who may have increased exposure:

In cases of moderate renal dysfunction.

In elderly patients over 75 years of age.

The drug contains sucrose, so the drug is not recommended for patients with fructose intolerance, glucose-galactose malabsorption syndrome and sucrase-isomaltase deficiency.

Impact on the ability to drive vehicles and operate machinery

Clinical studies did not reveal the effect of trimetazidine on hemodynamic parameters, however, during post-registration use, cases of dizziness and drowsiness were observed, which may affect the ability to drive vehicles and perform work that requires an increased speed of physical and mental reactions.

Overdose

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

Side effects Preductal od 80 mg 60 pcs. extended-release capsules laboratory servier

Adverse reactions, defined as adverse events that are at least possibly related to treatment with trimetazidine, are listed as follows: very often (≥1/10); often (≥1/100,

MedDRA Classes and Organ Systems	Adverse reactions	Frequency
Nervous system disorders	Dizziness	Often
	Headache	Often
	Symptoms of parkinsonism (tremor, akinesia, increased tone), gait instability, restless legs syndrome, other associated movement disorders, usually reversible after cessation of therapy	Unspecified frequency
	Sleep disorders (insomnia, drowsiness)	Unspecified frequency
Hearing and labyrinth disorders	Vertigo	Unspecified frequency
Heart disorders	Feeling of heartbeat	Rarely
	Extrasystole	Rarely
	Tachycardia	Rarely
Vascular disorders	Arterial hypotension, orthostatic hypotension, which may be accompanied by general malaise, dizziness or falling, especially when taking antihypertensive drugs simultaneously	Rarely
Vascular disorders	“Rushes” of blood to the skin of the face	Rarely
Gastrointestinal disorders	Abdominal pain	Often
	Diarrhea	Often
	Dyspepsia	Often
	Nausea	Often
	Vomit	Often
	Constipation	Unspecified frequency
Skin and subcutaneous tissue disorders	Skin rash	Often
	Itchy skin	Often
	Hives	Often
	Acute generalized exanthematous pustulosis (AGEP)	Unspecified frequency
	Angioedema	Unspecified frequency
General and administration site disorders	Asthenia	Often
Blood and lymphatic system disorders	Agranulocytosis	Unspecified frequency
	Thrombocytopenia	Unspecified frequency
	Thrombocytopenic purpura	Unspecified frequency
Disorders of the liver and biliary tract	Hepatitis	Unspecified frequency

Drug interactions

There were no interactions with other drugs.

Preductal price, where to buy

The price of Preductal OD in pharmacies is about 800 rubles for 30 tablets and 1,400 rubles for 60 tablets of 80 mg. You can buy Preductal in Moscow in almost any pharmacy with a prescription.

You can buy Preductal MR in Ukraine at a cost of 180 UAH.

Online pharmacies in RussiaRussia
Online pharmacies in UkraineUkraine
Online pharmacies in KazakhstanKazakhstan

ZdravCity

Preductal OD capsules long-acting 80 mg 60 pcs. Servier Rus LLC
RUB 1,461 order
Preductal OD capsules extended action 80 mg 30 pcs. Pharmstandard-Leksredstva OJSC/LLC SERVIER RUS
RUB 849 order

Pharmacy Dialogue

Preductal OD (caps.prolon.high.80mg No.60)FS.-Leksredstva
1400 rub. order
Preductal OD extended release capsules 80 mg No. 30FS.-Leksredstva
RUR 821 order

Pharmacy24

Preductal MR 35 mg N60 tablets Lab.Serv e Industries, France/Anfarm Pidp.Pharmac.
AT, Poland/TOV Serdiks, Russia 176 UAH.order

PaniPharmacy

Preductal MR tablets Preductal MR film-coated tablets 35 mg No. 60 France, Servier Industrie
199 UAH order