PharmaceuticalMetabolic modulatorWADA-bannedAnti-anginalFatty-acid oxidation inhibitor

Trimetazidine

Also known as TMZ · Vastarel · Preductal

Written by enwyReviewed 5 Aug 20262 sources0 comments

An anti-anginal metabolic agent that partially inhibits fatty-acid oxidation, shifting cardiac energy production toward glucose. Prescribed for stable angina in Europe and Asia, it is WADA-banned and has produced high-profile positive tests, including Kamila Valieva at the 2022 Winter Olympics.

01 Overview

Trimetazidine (TMZ) inhibits the mitochondrial enzyme long-chain 3-ketoacyl-CoA thiolase (3-KAT), the terminal enzyme of beta-oxidation. By partially blocking fatty-acid oxidation it promotes glucose oxidation, which yields more ATP per unit of oxygen and preserves cellular energy during ischaemia without altering heart rate or blood pressure. It is a well-studied second-line anti-anginal.

Because the metabolic shift is theoretically ergogenic and TMZ was repeatedly detected in athletes, WADA moved it to the fully prohibited 'S4 hormone and metabolic modulators' category. Its use in sport is banned in and out of competition.

02 Mechanism

Partially inhibits mitochondrial 3-ketoacyl-CoA thiolase (3-KAT), reducing fatty-acid oxidation and favouring more oxygen-efficient glucose oxidation, preserving ATP during ischaemia.

03 Dosing

Tier	Dose	Route	Notes
Angina (IR)	20 mg	Oral	20 mg three times daily with meals.

04 Effects

Effect	Magnitude	Evidence
Reduced angina frequencyReduces frequency of anginal attacks and improves exercise tolerance as add-on therapy.	moderate	Clinical
Anti-ischaemic myocardial protectionPreserves myocardial energy metabolism during ischaemia without haemodynamic effects.		Clinical
Claimed endurance efficiencyTheoretical exercise-efficiency benefit is the doping rationale; robust ergogenic data in healthy athletes are lacking.		Anecdotal

05 Side effects

Effect	Severity	Frequency	Evidence
Gastrointestinal upsetNausea, dyspepsia and abdominal discomfort.	Mild	Common	Clinical
Parkinsonian symptoms / movement disorderTremor, gait instability and restless-legs-type symptoms; contraindicated in Parkinson's disease.	Moderate	Rare	Clinical
Doping sanctionWADA-prohibited (S4); positive tests carry lengthy bans.	Severe	For competing athletes	Clinical

06 Legal status

Prescription medicine

Licensed for angina as second-line; WADA-prohibited in sport. · as of Jan 2026

United States

Not FDA-approved

Not approved in the US; WADA-prohibited. · as of Jan 2026

07 References

Trimetazidine: a review of its use in stable angina and other coronary conditionsDrugs, 2003

WADA Prohibited List — S4 Hormone and Metabolic ModulatorsWorld Anti-Doping Agency

08 Discussion0 comments

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This page is reference information, not medical advice. Doses and protocols are documented as they appear in the clinical literature and in practice — describing them is not a recommendation to use them. Countermeasures listed here are not a substitute for a physician. Legal status varies by jurisdiction and changes.