Trimetazidine

Trimetazidine.svg

Trimetazidine is a metabolic agent used primarily in the management of angina pectoris and other cardiovascular diseases. It is classified as a cytoprotective drug, which means it helps to protect cells from damage, particularly in conditions where there is a lack of oxygen.

Mechanism of Action

Trimetazidine works by inhibiting the enzyme 3-ketoacyl-CoA thiolase (3-KAT) in the fatty acid oxidation pathway. This inhibition shifts the energy production from fatty acid oxidation to glucose oxidation, which is more oxygen-efficient. By optimizing the energy production in myocardial cells, trimetazidine helps to maintain proper cellular function during episodes of ischemia.

Clinical Uses

Trimetazidine is primarily used for the treatment of stable angina pectoris. It is often prescribed as an adjunct therapy to other anti-anginal medications such as beta-blockers, calcium channel blockers, and nitrates. Additionally, it has been investigated for use in other conditions such as heart failure, tinnitus, and dizziness.

Side Effects

Common side effects of trimetazidine include nausea, vomiting, dizziness, and headache. Rare but serious side effects can include extrapyramidal symptoms and Parkinsonism, particularly in elderly patients.

Contraindications

Trimetazidine is contraindicated in patients with Parkinson's disease, severe renal impairment, and hypersensitivity to the drug. It should be used with caution in patients with hepatic impairment.

Pharmacokinetics

Trimetazidine is well absorbed after oral administration, with peak plasma concentrations occurring within 2-3 hours. It is primarily excreted unchanged in the urine, with a half-life of approximately 6 hours.

History

Trimetazidine was first developed in the 1960s and has been used in clinical practice since the 1970s. It is marketed under various brand names worldwide and is available in both immediate-release and modified-release formulations.

Regulatory Status

Trimetazidine is approved for use in many countries, but its use is restricted in some regions due to concerns about its safety profile. For example, the European Medicines Agency (EMA) has recommended restrictions on its use in patients with movement disorders.

Research

Ongoing research is exploring the potential benefits of trimetazidine in other conditions such as diabetic cardiomyopathy, chronic kidney disease, and neurodegenerative diseases.

See Also

• Angina pectoris
• Cardiovascular disease
• Metabolic agent
• Cytoprotection