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.
Instructions for use PREDUCTAL® MR (PREDUCTAL MR)
An antianginal drug that improves myocardial metabolism in ischemic conditions. 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 Na+-K+ flux while maintaining cellular homeostasis.
Trimetazidine inhibits fatty acid β-oxidation by inhibiting long-chain 3-ketoacyl CoA thiolase (3-CAT), which increases glucose oxidation. In ischemic cells, energy requirements are met by glucose oxidation, which requires less oxygen consumption than β-oxidation. Enhanced glucose oxidation optimizes cellular energy processes, and thereby maintains proper energy metabolism during ischemia.
In patients with coronary artery disease, trimetazidine acts as a metabolic agent that preserves the intracellular level of high-energy phosphates in cardiomyocytes. The anti-ischemic effect is not accompanied by an effect on hemodynamics.
Clinical efficacy and safety
Clinical studies have shown the effectiveness and safety of trimetazidine in patients with angina pectoris, both in monotherapy and in combination when other antianginal drugs are insufficiently effective.
In a randomized, double-blind, placebo-controlled trial involving 426 patients (TRIMPOL-II), trimetazidine (60 mg/day) plus metoprolol 100 mg/day (50 mg twice a day) for 12 weeks statistically significantly improved parameters. stress tests and clinical symptoms compared with placebo:
- the total duration of the stress tests was +20.1 s, p=0.023, the total load performed was +0.54 MET, p=0.001, the time until the development of ST segment depression by 1 mm was +33.4 s, p=0.003, the time until the onset of an angina attack was +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 randomized, double-blind, placebo-controlled study of 223 patients (Sellier), the addition of trimetazidine 35 mg (1 modified-release tablet) twice daily to atenolol 50 mg (once daily) for 8 weeks significantly increased the time before the development of 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. A significant difference was also proven for the time of onset of angina attacks (p=0.049). There was no significant difference between groups for other secondary endpoints (total exercise test duration, total exercise capacity, and clinical endpoints).
In a three-month, randomized, double-blind study of 1962 patients (the Vasco study), two doses of trimetazidine (70 mg/day and 140 mg/day) given in addition to atenolol 50 mg/day were studied in comparison with placebo. In the general population, including patients with or without clinical symptoms, no benefit was observed for trimetazidine on ergometric (total duration of stress tests, time to 1 mm ST segment depression, time to onset of angina) and clinical endpoints. However, in a post-hoc analysis of a subgroup of symptomatic patients (n=1574), trimetazidine (140 mg) significantly improved total exercise test time (+23.8 sec versus +13.1 sec placebo; p=0.001) and time to onset of angina (+46.3 sec versus +32.5 with placebo; p=0.005).
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.
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
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<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 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).
Pharmacokinetics
Suction
Trimetazidine has a linear pharmacokinetic profile and reaches Cmax in plasma 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 Cmax. An equilibrium state is achieved after taking the 3rd dose (after 3 days). Food intake does not affect the bioavailability of trimetazidine when taking Preductal® OD 80 mg.
Distribution
Vd 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. T1/2 in young healthy volunteers is about 7 hours, in patients over 65 years old - about 12 hours.
Renal clearance of trimetazidine directly correlates with creatinine clearance; hepatic clearance decreases with patient age.
Pharmacokinetics in special groups of patients
Patients over 75 years of age may experience increased exposure to trimetazidine due to age-related decline in renal function. A special study was conducted in a population of patients over 75 years of age using trimetazidine tablets at a dose of 35 mg 2 times a day. An analysis conducted by the kinetic population method showed an average twofold increase in plasma exposure in patients with severe renal failure (creatinine clearance less than 30 ml/min) compared with patients with creatinine clearance more than 60 ml/min.
No safety differences were found in patients over 75 years of age compared with the general population.
Trimetazidine exposure was increased on average by 2.4 times in patients with moderate renal failure (creatinine clearance 30-60 ml/min), and on average by 4 times in patients with severe renal failure (creatinine clearance less than 30 ml/min) compared with healthy volunteers with normal renal function. No significant safety differences were observed in this patient population compared with the general population.
The pharmacokinetics of trimetazidine in children and adolescents under 18 years of age have not been studied.
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 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.
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 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.
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 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.
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 |
“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.
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 MV
The drug preductal MB (active ingredient - trimetazidine) belongs to the group of antihypoxants: it improves energy metabolism (primarily the myocardium) and increases the body's resistance to hypoxia. This drug is used mainly in cardiology to treat coronary heart disease and prevent attacks of stable angina, but in some cases it may be in demand in otolaryngology and ophthalmology. Preductal MB is an original drug produced by the pharmaceutical company and its many subsidiaries. The mechanism of its action is realized at the cellular level through a positive effect on ischemic myocardial cells. Preductal MB maintains the intracellular concentration of ATP at the proper level, ensuring the normal operation of ion channels in membranes, the transport of potassium and sodium ions through them, and the constancy of the internal state of the cell. The drug suppresses the oxidation of fatty acids, while simultaneously promoting the oxidation of glucose, which protects the myocardium from the development of ischemia. The transfer of energy metabolism from the oxidation of fatty acids to glycolytic “rails” is, in fact, the main “highlight” of the CF preductal, which underlies its pharmacological action. During clinical trials, a number of positive qualities were observed in the drug. It regulated the energy metabolism of the heart during ischemia, mitigated the consequences of disturbances in the acid-base balance within cells, prevented changes in ion transport through membranes characteristic of ischemia, and reduced the extent of ischemic damage to the myocardium. In patients suffering from angina, preductal MV increases the ability of the coronary vessels to increase blood flow in accordance with the urgent needs of the heart (due to this, the development of ischemia caused by physical activity is inhibited), reduces the amplitude of blood pressure fluctuations provoked by physical activity, without significantly changing the heart rate; reduces the frequency of angina attacks, increases the functional characteristics of the left ventricle.
All these advantages in the pharmacological “summary” of the CF preductal allow us to look with optimism at the outpatient chart of patients suffering from angina pectoris. Preductal MB is produced in tablets with a modified release of the active substance and fully meets the high requirements that are imposed today on modern antianginal drugs, such as: high anti-ischemic effectiveness, maintained thanks to the dosage form throughout the day and a favorable safety profile.
The dosage form of CF preductal should be discussed separately. The active ingredient in the tablet is evenly distributed in methylhydroxypropylcellulose. When it enters the gastrointestinal tract, this hydrophilic matrix swells to form a gel-like substance, which ensures a slow, controlled release of trimetazidine into the blood, and, consequently, stability of the anti-ischemic effect. Thanks to the original dosage form, the effective concentration of the drug in the blood is 31% higher than that of the short-acting dosage form. This is very important, especially in the morning, when the risk of developing acute manifestations of ischemia is highest.
Preductal MB should be taken without chewing and with plenty of water. Dose and frequency of administration: 1 tablet. 2 times a day in the morning and evening during meals. The duration of treatment is determined by the doctor. In conclusion, it should be noted that Preductal CF is not used for the direct relief of angina attacks and is not intended for the initial course of treatment of unstable angina.
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 extended action 80 mg 30 pcs. Pharmstandard-Leksredstva OJSC/LLC SERVIER RUS
838 rub. order - Preductal OD capsules extended action 80 mg 60 pcs. Servier Rus LLC
RUB 1,446 order
Pharmacy Dialogue
- Preductal OD (caps.prolon.high.80mg No.60)FS.-Leksredstva
RUB 1,490 order
- Preductal OD extended release capsules 80 mg No. 30FS.-Leksredstva
RUB 815 order
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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
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Preductal MB tab. with mod. release cover captivity. about. 35 mg per blister. in pack No. 30x2 (trimetazidine)
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Preductal® MR, film-coated tablets, modified release Trimetazidine dihydrochloride
Compound
The active substance is trimetazidine hydrochloride. Each tablet contains 35 mg trimetazidine dihydrochloride.
Other Ingredients:
Tablet core: calcium hydrogen phosphate dihydrate; hypromellose 4000; povidone; colloidal anhydrous silicon dioxide, magnesium stearate.
Film coating: titanium dioxide (E 171), glycerol, hypromellose, macrogol 6000, red iron oxide (E 172), magnesium stearate.
What PREDUCTAL MR looks like and contents of the package
Modified release film-coated tablet. Biconvex tablets, pink, film-coated. 60 tablets per box.
What is Preductal MR and in what cases is it used?
This drug is used in adults to treat angina (chest pain caused by coronary artery disease) in combination with other drugs
Before you start taking Preductal MR
In what cases should you not take PREDUCTAL MR?
- if you are allergic to trimetazidine or any of the other components of PREDUCTAL MR (see section 6),
- if you have Parkinson's disease: a brain disease that leads to movement disorders (shaking, stiff body posture, slow movements and shuffling, gait disturbance),
- if you have severe kidney disease.
Warnings and Precautions for Use
Talk to your doctor or pharmacist before taking Preductal MR. This medicine is not intended to relieve attacks of angina or as initial treatment for unstable angina. This drug is not used to treat myocardial infarction.
If you have an attack of angina, inform your doctor. You may be prescribed examinations, and treatment may be adjusted. If you are in any doubt, you should ask your doctor or pharmacist for advice.
This drug may cause or worsen symptoms such as trembling, stiff posture, gait disturbance, slow movements, and shuffling, especially in older patients, which should be monitored and reported to the doctor, who may re-evaluate treatment.
Falls may also occur, which may be due to low blood pressure or loss of balance (see description of possible side effects).
Children and teenagers
Preductal MR is not recommended for use by children under 18 years of age.
Taking other medications
No interactions with other medications were noted.
Always tell your doctor or pharmacist what medicines you are taking.
have recently taken, or may have taken.
Taking PREDUCTAL MR with food and drinks
Preductal MR can be taken with food and drinks.
Pregnancy and breastfeeding
It is preferable not to take this drug during pregnancy. If you find out that you are pregnant while taking the drug, you should consult your doctor, as only he can judge the need to continue your treatment.
Due to the lack of data on the excretion of the drug into breast milk, breastfeeding is not recommended during treatment with Preductal MR. Check with your doctor or pharmacist before starting any medication.
If you are pregnant or breastfeeding, or think you are or may become pregnant, talk to your doctor before taking this drug.
Driving vehicles and operating machinery
While taking this drug, you may experience dizziness and drowsiness, which may affect your ability to operate machines.
How to take Preductal MR
When taking PREDUCTAL MR, always strictly follow your doctor's instructions. If you are in doubt about taking the medicine correctly, you should consult your doctor or pharmacist.
The recommended dose is one tablet twice a day in the morning and evening with meals. If you have kidney problems or are over 75 years of age, your doctor may adjust the recommended dose.
PREDUCTAL MR is intended for oral administration. The tablet is swallowed with a glass of water during meals.
If you take more PREDUCTAL MR than recommended
If you take too many tablets, tell your doctor or pharmacist immediately.
If you forget to take PREDUCTAL MR
If you forget to take PREDUCTAL MR, take your next dose at the usual time. Do not double the next dose to replace a forgotten dose.
If you stop taking PREDUCTAL MR
Your doctor will tell you how long to continue treatment. You should consult your doctor before stopping this drug.
If you have any questions about using this medicine, ask your doctor or pharmacist.
Possible side effects
Like all medicines, PREDUCTAL MR can cause side effects, although not everyone gets them.
The frequency of possible side effects is determined according to the following system:
- very common (occurs in more than 1 patient out of 10);
- common (occurs in 1-10 patients out of 100)
- uncommon (affects 1-10 patients out of 1000);
- rare (occurs in 1-10 patients out of 10,000);
- very rare (occurs in less than 1 patient in 10,000)
— unknown frequency (impossible to estimate from available data).
Common
Dizziness, headache, abdominal pain, diarrhea, dyspepsia, feeling of malaise, vomiting, rash, itching, urticaria and feeling of weakness.
Rare
Fast or irregular heartbeat (also called fluttering), extra heart beats, faster heart rate, drop in blood pressure when standing up which may be caused by dizziness, mild dizziness or fainting, malaise (a general feeling of being unwell), dizziness, falls, flushing
Unknown frequency
Extrapyramidal symptoms (unusual movements including trembling and shaking of the hands and fingers, undulating body movements, shuffling gait, and stiffness of the arms and legs) are usually reversible when treatment is stopped.
Sleep disturbances (difficulty falling asleep, drowsiness), constipation, severe generalized red skin rash with blistering, swelling of the face, lips, mouth, tongue or throat, which may cause difficulty swallowing or breathing.
A severe decrease in the number of white blood cells in the blood, which makes infection more likely, and a decrease in platelets, which increases the risk of bleeding and bruising.
Liver disease (nausea, vomiting, loss of appetite, general feeling of illness, fever, itching, yellowing of the skin and eyes, light-colored feces, dark-colored urine).
If you notice any unwanted effects, tell your doctor. This includes effects not listed in this leaflet.
About storing Preductal MR
Keep out of the reach and sight of children. Store at a temperature not exceeding 30°C.
Do not take PREDUCTAL MR after the expiration date indicated on the carton. When indicating the expiration date, we mean the last day of the specified month.
This medicine does not require special storage conditions.
Medicines should not be disposed of in wastewater or sewer systems. Ask your pharmacist how to dispose of finished medications. These measures are aimed at protecting the environment.
Packing
Box contains 60 tablets (PVC/aluminium):
2 blisters of 30 modified-release film-coated tablets together with an insert leaflet are placed in a cardboard box.
Vacation conditions
A medical product available with a doctor's prescription.
Marketing Authorization Holder and Manufacturers
Marketing authorization holder
Les Laboratoires Servier (Jle Laboratoires Servier) 50, rue Carnot
92284 Suresnes cedex France - France
Manufacturers
Les Laboratoires Servier Industrie 905, route de Saran 45520 Gidy France
Or
Anpharm Przedsiebiorstwo Farmaceutyczne SA 03-236 Warsawa, ul. Annopol 6B Poland
For any questions about this medicinal product, please contact your local Marketing Authorization Holder office.
BELARUS
Myasnikova St., 70, office 303 220030 Minsk, Republic of Belarus Tel.: +375
Date of last approval of the insert: 2012