Trimetazidine
Trimetazidine
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Trimetazidine

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Trimetazidine

Trimetazidine (IUPAC: 1-(2,3,4-trimethoxybenzyl)piperazine) is a drug used in the treatment of angina pectoris, a condition characterized by chest pain due to reduced blood flow to the heart. Developed and first marketed by Laboratoires Servier (France), it is described as the first cytoprotective anti-ischemic agent. Trimetazidine is an antianginal metabolic drug of the fatty acid oxidation inhibitor class; it shifts cardiac energy metabolism from fatty acid utilization toward glucose oxidation, thereby improving the efficiency of energy production in ischemic conditions.

The drug has also become controversial as a performance-enhancing drug, with multiple doping scandals linked to its use at successive Olympic Games.

Trimetazidine is prescribed primarily as a long-term treatment for angina pectoris. In some countries, including France, it has also been used for tinnitus and dizziness. The drug is typically administered twice daily. In 2012, the European Medicines Agency (EMA) completed a review of its benefits and risks and recommended restricting trimetazidine-containing medicines to use only as an add-on therapy for angina pectoris when first-line antianginal agents are insufficient or not tolerated.

Controlled studies in patients with angina have shown that trimetazidine increases coronary flow reserve, delays the onset of exercise-induced ischemia, stabilizes blood pressure without significantly affecting heart rate, reduces the frequency of angina attacks, and decreases the need for symptomatic nitrate use.

Trimetazidine has also been reported to improve left ventricular function in patients with coronary heart disease and diabetes.

As of 2023, it is under investigation for the treatment of bipolar depression.

Although developed for medical use in the 1970s, trimetazidine was only added to the World Anti-Doping Agency (WADA) list of prohibited substances in 2014 under the category of "hormone and metabolic modulators." Its use is prohibited at all times, both in and out of competition.

In 2014, Chinese Olympic swimmer Sun Yang tested positive for trimetazidine, four months after it had been added to the banned list. He was suspended for three months by the Chinese Swimming Association. Later that year, WADA reclassified trimetazidine from a "stimulant" to a "modulator of cardiac metabolism."[permanent dead link]

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