Trimetazidine


Thông tin thuốc gốc
Chỉ định và Liều dùng
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.
Suy thận
CrCl (mL/min) Dosage
<30 Contraindicated.
30-60 As conventional tab: 20 mg bid. As modified-release tab: 35 mg once daily.
Cách dùng
Should be taken with food.
Chống chỉ định
Parkinson's disease, parkinsonian symptoms, restless leg syndrome, tremors, and other related movement disorders. Severe renal impairment (CrCl <30 mL/min). Lactation.
Thận trọng
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.
Tác dụng không mong muốn
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.
Thông tin tư vấn bệnh nhân
This drug may cause drowsiness or dizziness, if affected, do not drive or operate machinery.
Chỉ số theo dõi
Monitor renal function.
Tác dụng
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).
Đặc tính

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)

Bảo quản
Store below 30°C.
Phân loại MIMS
Thuốc chống đau thắt ngực
Phân loại ATC
C01EB15 - trimetazidine ; Belongs to the class of other cardiac preparations.
Tài liệu tham khảo
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.

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