Trimetazidine

Oral
Stable angina

CrCl (mL/min)	Dosage
<30	Contraindicated.
30-60	As conventional tab: 20 mg bid. As modified-release tab: 35 mg once daily.

Should be taken with food.

Parkinson's disease, parkinsonian symptoms, restless leg syndrome, tremors, and other related movement disorders. Severe renal impairment (CrCl <30 mL/min). Lactation.

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.

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.

This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.

Monitor renal function.

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).

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

Store below 30°C.

Anti-Anginal Drugs

C01EB15 - trimetazidine ; Belongs to the class of other cardiac preparations.

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.