Trimetazidine

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 Recommendation
<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. Patient Counselling This drug may cause dizziness or drowsiness, if affected, do not drive or operate machinery. Monitoring Parameters Monitor renal function.

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.

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.
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).

Oral: Store below 30°C.

Anti-Anginal Drugs

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