Each modified release film-coated tablet contains Trimetazidine dihydrochloride 35 mg.
Pharmacology: Pharmacodynamics: In patients with ischemic heart disease, Trimetazidine acts as a metabolic agent, preserving the myocardial high-energy phosphate intracellular levels. Anti-ischemic effects are achieved without concomitant hemodynamic effects.
Pharmacokinetics: After oral administration, maximum concentration is found, on average, 5 hours after taking the tablet. Over 24 hours the plasma concentration remains at levels above or equal to 75% of the maximum concentration for 11 hours. Steady state is reached by the 60th hour, at the latest. The pharmacokinetic characteristics of Trimetazidine (Vastarel MR) are not influenced by meals. The apparent distribution volume is 4.8 L/kg; protein binding is low: in vitro measurements give value of 16%. Trimetazidine (Vastarel MR) is eliminated primarily in the urine, mainly in the unchanged form. The elimination half-life of Trimetazidine (Vastarel MR) is an average of 7 hours in healthy young volunteers and 12 hours in subjects aged more than 65 years. Total clearance of trimetazidine is the result of major renal clearance which is directly correlated to creatinine clearance and, to a lesser extent, to liver clearance which is reduced with age.
Trimetazidine is indicated in adults as add-on therapy for the symptomatic treatment of patients with stable angina pectoris who are inadequately controlled by or intolerant to first-line antianginal therapies.
One tablet twice daily, that is once in the morning and once in the evening, during meals.
The benefit of the treatment should be assessed after three months and trimetazidine should be discontinued if there is no treatment response.
Patients with renal impairment: In patients with moderate renal impairment (creatinine clearance 30-60 ml/min), the recommended dose is one 35 mg tablet in the morning during breakfast.
Elderly patients: Elderly patients may have increased trimetazidine exposure due to age-related decrease in renal function. In patients with moderate renal impairment (creatinine clearance 30-60 ml/min), the recommended dose is one tablet of 35 mg in the morning during breakfast. Dose titration in elderly patients should be exercised with caution.
Pediatric population: The safety and efficacy of Trimetazidine (Vastarel MR) in children aged below 18 years have not been established. No data are available.
Missed dose: Resume treatment normally. Do not take a double dose to compensate for the single dose that the patient forgot to take.
Limited information is available on trimetazidine overdose. Treatment should be symptomatic.
Hypersensitivity to Trimetazidine or to any of the other ingredients of Trimetazidine (Vastarel MR).
Parkinson disease, parkinsonian symptoms, tremors, restless leg syndrome, and other related movement disorders.
Severe renal impairment (creatinine clearance <30ml/min).
This medicinal product is not a curative treatment for angina attacks, nor an initial treatment for unstable angina pectoris or myocardial infarction, nor in the pre-hospital phase or during the first days of hospitalization.
In the event of an angina attack, the coronaropathy should be reevaluated and an adaptation of the treatment considered (medicinal treatment and possibly revascularization).
This medicinal product can aggravate or cause symptoms similar to those of Parkinson's disease (tremor, difficulty in making movements, rigidity of limbs), which should be investigated and reported to the doctor, especially in elderly patients. In doubtful cases, patients should be referred to a neurologist for appropriate investigations.
The occurrence of movement disorders such as parkinsonian symptoms, restless leg syndrome, tremors, gait instability should lead to definitive withdrawal of Trimetazidine (Vastarel MR).
These cases have a low incidence and are usually reversible after treatment discontinuation. The majority of the patients recovered within 4 months after Trimetazidine (Vastarel MR) withdrawal. If parkinsonian symptoms persist more than 4 months after drug discontinuation, a neurologist's opinion should be sought.
Falls may occur following a drop in blood pressure or a loss of balance, in particular in patients taking antihypertensive treatment (see description of side effects).
Caution should be exercised in patients with moderate renal impairment and elderly (>75 years old).
Driving and using machines: Trimetazidine (Vastarel MR) does not have hemodynamic effects in clinical studies, however cases of dizziness and drowsiness have been observed in post-marketing experience, which may affect ability to drive and use machines.
Use in Children: Trimetazidine (Vastarel MR) must not be administered to children aged below 18 years.
Pregnancy: There are no data from the use of trimetazidine in pregnant women. Animal studies do not indicate direct or indirect harmful effects with respect to reproductive toxicity. As a precautionary measure, it is preferable to avoid the use of Trimetazidine (Vastarel MR) during pregnancy.
Breastfeeding: It is unknown whether trimetazidine/metabolites are excreted in human milk. A risk to the newborns/infants cannot be excluded. Trimetazidine (Vastarel MR) should not be used during breastfeeding.
As with all medicines, Trimetazidine (Vastarel MR) is likely to have side effects, although not everyone may be prone to them.
The table as follows includes the adverse reactions from spontaneous notifications and scientific literature.
Very common (≥1/10); common (≥1/100,<1/10); uncommon (≥1/1000, <1/100); rare (≥1/10000, <1/1000); very rare (<1/10000); not known (cannot be estimated from the available data). (See table.)
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Reporting of Adverse Drug Reaction:
Seek medical attention immediately at the first sign of any adverse drug reaction.
No drug interaction has been reported.
Store at temperatures not exceeding 30°C.
C01EB15 - trimetazidine ; Belongs to the class of other cardiac preparations.
MR tab 35 mg (pink, film-coated, lenticular) x 60's.