Trimetazidine


Generic Medicine Info
Indications and Dosage
Oral
Stable angina
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).
Chemical Structure

Chemical Structure Image
Trimetazidine

Source: National Center for Biotechnology Information. PubChem Database. Trimetazidine, CID=21109, https://pubchem.ncbi.nlm.nih.gov/compound/Trimetazidine (accessed on Jan. 23, 2020)

Storage
Store below 30°C.
MIMS Class
Anti-Anginal Drugs
ATC Classification
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.

Disclaimer: This information is independently developed by MIMS based on Trimetazidine from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2022 MIMS. All rights reserved. Powered by MIMS.com
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