Kj. Mcclellan et Gl. Plosker, Trimetazidine - A review of its use in stable angina pectoris and other coronary conditions, DRUGS, 58(1), 1999, pp. 143-157
The orally administered antianginal agent trimetazidine increases cell tole
rance to ischaemia by maintaining cellular homeostasis. In theory, this cyt
oprotective activity should limit myocyte loss during ischaemia in patients
with angina pectoris.
Data from studies in patients with coronary artery disease indicate that, u
nlike the effects of other antianginals, the anti-ischaemic effects of trim
etazidine 20mg are not associated with alterations in haemadynamic determin
ants of myocardial oxygen consumption such as heart rate, systolic blood pr
essure and the rate-pressure product. Furthermore, limited evidence suggest
s trimetazidine may improve left ventricular function in patients with chro
nic coronary artery disease or ischaemic cardiomyopathy and in patients exp
eriencing acute periods of ischaemia when undergoing percutaneous translumi
nal coronary angioplasty.
Clinical studies have shown that oral trimetazidine 20mg 3 times daily redu
ces the frequency of anginal attacks and nitroglycerin use and increases ex
ercise capacity when used as monotherapy in patients with angina pectoris.
Its clinical effects are broadly similar to those of nifedipine 40 mg/day a
nd propranolol 120 to 160 mg/day but, unlike these agents, trimetazidine do
es not affect the rate-pressure product during peak exercise or at rest.
Adjunctive trimetazidine 60 mg/day reduces the frequency of anginal attacks
and nitroglycerin use and improves exercise capacity in patients with angi
na pectoris not sufficiently controlled by conventional antianginal agents.
Furthermore, the drug appears to be more effective than isosorbide dinitra
te 30 mg/day when used adjunctively in patients with angina pectoris poorly
controlled by propranolol 120 mg/day.
The tolerability profile of trimetazidine 60 mg/day was similar to that of
placebo when used as add-on therapy in patients with angina pectoris insuff
iciently controlled by other antianginal agents and was superior to that of
either nifedipine 30 mg/day or propranolol 120 to 160 mg/day when used as
monotherapy, The most frequently reported adverse events in trimetazidine r
ecipients were gastrointestinal disorders, although the incidence of these
events was low.
Conclusions: Trimetazidine is an effective and well tolerated anti-ischaemi
c agent which, in addition to providing symptom relief and functional impro
vement in patients with angina pectoris, has a cytoprotective action during
ischaemia. The drug is suitable for initial use as monotherapy in patients
with angina pectoris and, because of its different mechanism of action, as
adjunctive therapy in those with symptoms not sufficiently controlled by n
itrates, beta-blockers or calcium antagonists. The role of trimetazidine in
other coronary conditions has yet to be clearly established.