Adult: As adjunctive therapy for the symptomatic treatment of patients who are inadequately controlled by or intolerant of 1st-line antianginal therapies: As conventional tab: 20 mg tid. As modified-release tab: 35 mg bid. As prolonged-release cap: 80 mg once daily.
Renal Impairment
CrCl (mL/min)
Dosage
<30
Contraindicated.
30-60
As conventional tab: 20 mg bid. As modified-release tab: 35 mg once daily.
Administration
Should be taken with food.
Contraindications
Parkinson's disease, parkinsonian symptoms, restless leg syndrome, tremors, and other related movement disorders. Severe renal impairment (CrCl <30 mL/min). Lactation.
Special Precautions
Patient predisposed to closed-angle glaucoma (when using modified-release tab). Not indicated as a treatment for angina attacks, as initial treatment for unstable angina or MI, nor in the pre-hospital phase or during the 1st days of hospitalisation. Mild to moderate renal impairment. Elderly (particularly >75 years old). Avoid use during pregnancy.
Adverse Reactions
Significant: New-onset or worsening of parkinsonian symptoms (e.g. akinesia, hypertonia, tremor). Cardiac disorders: Rarely, palpitations, extrasystoles, tachycardia. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, dyspepsia. General disorders and administration site conditions: Asthenia. Nervous system disorders: Headache, dizziness. Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus. Vascular disorders: Rarely, arterial hypotension, orthostatic hypotension, flushing.
Patient Counseling Information
This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.
Monitoring Parameters
Monitor renal function.
Action
Description: Trimetazidine inhibits β-oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase, with the effect of enhancing glucose oxidation, resulting in more efficient production of ATP with less oxygen demand. It prevents a decrease in intracellular ATP levels by preserving energy metabolism in cells exposed to ischaemia or hypoxia, thus ensuring the proper functioning of ionic pumps and transmembrane Na-K flow without changing haemodynamic parameters. Pharmacokinetics: Absorption: Rapidly absorbed from the gastrointestinal tract. Time to peak plasma concentration: <2 hours (immediate-release tab); 2-6 hours (modified-release tab); approx 14 hours (prolonged-release cap). Distribution: Volume of distribution: 4.8 L/kg. Plasma protein binding: 16%. Metabolism: Partially metabolised in the liver (<40% metabolised) into 8 metabolites with unknown activity. Excretion: Via urine (79-84%; >60% as unchanged drug). Elimination half-life: Approx 5-6 hours (immediate-release tab); 7 hours (modified-release tab and prolonged-release cap).
C01EB15 - trimetazidine ; Belongs to the class of other cardiac preparations.
References
Anon. Trimetazidine. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 04/02/2022.Buckingham R (ed). Trimetazidine Hydrochloride. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 04/02/2022.Trimetazidine Stella Modified Release Tablets 35 mg (Stellapharm J.V. Co Ltd). MIMS Hong Kong. http://www.mims.com/hongkong. Accessed 18/02/2022.Vastarel 20 mg Film-Coated Tablet (Zuellig Pharma Corporation). MIMS Philippines. http://www.mims.com/philippines. Accessed 04/02/2022.Vastarel 20 mg, Film-Coated Tablet (Servier Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/02/2022.Vastarel MR, Modified Release Film-Coated Tablets (Servier Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/02/2022.Vastarel XR 80 mg, Prolonged-Release Hard Capsule (Servier Malaysia Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my. Accessed 04/02/2022.