Medical Dialogues
  • Dermatology
Login Register
This site is intended for healthcare professionals only
Login Register
  • MD Brand Connect
  • Vaccine Hub
  • MDTV
    • Breaking News
    • Medical News Today
    • Health News Today
    • Latest
    • Journal Club
    • Medico Legal Update
    • Latest Webinars
    • MD Shorts
    • Health Dialogues
  • Fact Check
  • Health Dialogues
Medical Dialogues
  • Medical News & Guidelines
      • Anesthesiology
      • Cardiology and CTVS
      • Critical Care
      • Dentistry
      • Dermatology
      • Diabetes and Endocrinology
      • ENT
      • Gastroenterology
      • Medicine
      • Nephrology
      • Neurology
      • Obstretics-Gynaecology
      • Oncology
      • Ophthalmology
      • Orthopaedics
      • Pediatrics-Neonatology
      • Psychiatry
      • Pulmonology
      • Radiology
      • Surgery
      • Urology
      • Laboratory Medicine
      • Diet
      • Nursing
      • Paramedical
      • Physiotherapy
  • Health news
      • Doctor News
      • Government Policies
      • Hospital & Diagnostics
      • International Health News
      • Medical Organization News
      • Medico Legal News
      • NBE News
      • NMC News
  • Fact Check
      • Bone Health Fact Check
      • Brain Health Fact Check
      • Cancer Related Fact Check
      • Child Care Fact Check
      • Dental and oral health fact check
      • Diabetes and metabolic health fact check
      • Diet and Nutrition Fact Check
      • Eye and ENT Care Fact Check
      • Fitness fact check
      • Gut health fact check
      • Heart health fact check
      • Kidney health fact check
      • Medical education fact check
      • Men's health fact check
      • Respiratory fact check
      • Skin and hair care fact check
      • Vaccine and Immunization fact check
      • Women's health fact check
  • AYUSH
    • Ayurveda
    • Homeopathy
    • Siddha
    • Unani
    • Yoga
  • State News
      • Andaman and Nicobar Islands
      • Andhra Pradesh
      • Arunachal Pradesh
      • Assam
      • Bihar
      • Chandigarh
      • Chattisgarh
      • Dadra and Nagar Haveli
      • Daman and Diu
      • Delhi
      • Goa
      • Gujarat
      • Haryana
      • Himachal Pradesh
      • Jammu & Kashmir
      • Jharkhand
      • Karnataka
      • Kerala
      • Ladakh
      • Lakshadweep
      • Madhya Pradesh
      • Maharashtra
      • Manipur
      • Meghalaya
      • Mizoram
      • Nagaland
      • Odisha
      • Puducherry
      • Punjab
      • Rajasthan
      • Sikkim
      • Tamil Nadu
      • Telangana
      • Tripura
      • Uttar Pradesh
      • Uttrakhand
      • West Bengal
  • Medical Education
      • Ayush Education News
      • Dentistry Education News
      • Medical Admission News
      • Medical Colleges News
      • Medical Courses News
      • Medical Universities News
      • Nursing education News
      • Paramedical Education News
      • Study Abroad
  • Industry
      • Health Investment News
      • Health Startup News
      • Medical Devices News
      • Pharma News
      • Pharmacy Education News
      • Industry Perspective
  • MDTV
      • Health Dialogues MDTV
      • Health News today MDTV
      • Latest Videos MDTV
      • Latest Webinars MDTV
      • MD shorts MDTV
      • Medical News Today MDTV
      • Medico Legal Update MDTV
      • Top Videos MDTV
      • Health Perspectives MDTV
      • Journal Club MDTV
      • Medical Dialogues Show
This site is intended for healthcare professionals only
LoginRegister
Medical Dialogues
LoginRegister
  • Home
  • Medical news & Guidelines
    • Anesthesiology
    • Cardiology and CTVS
    • Critical Care
    • Dentistry
    • Dermatology
    • Diabetes and Endocrinology
    • ENT
    • Gastroenterology
    • Medicine
    • Nephrology
    • Neurology
    • Obstretics-Gynaecology
    • Oncology
    • Ophthalmology
    • Orthopaedics
    • Pediatrics-Neonatology
    • Psychiatry
    • Pulmonology
    • Radiology
    • Surgery
    • Urology
    • Laboratory Medicine
    • Diet
    • Nursing
    • Paramedical
    • Physiotherapy
  • Health news
    • Doctor News
    • Government Policies
    • Hospital & Diagnostics
    • International Health News
    • Medical Organization News
    • Medico Legal News
    • NBE News
    • NMC News
  • Fact Check
    • Bone Health Fact Check
    • Brain Health Fact Check
    • Cancer Related Fact Check
    • Child Care Fact Check
    • Dental and oral health fact check
    • Diabetes and metabolic health fact check
    • Diet and Nutrition Fact Check
    • Eye and ENT Care Fact Check
    • Fitness fact check
    • Gut health fact check
    • Heart health fact check
    • Kidney health fact check
    • Medical education fact check
    • Men's health fact check
    • Respiratory fact check
    • Skin and hair care fact check
    • Vaccine and Immunization fact check
    • Women's health fact check
  • AYUSH
    • Ayurveda
      • Ayurveda Giuidelines
      • Ayurveda News
    • Homeopathy
      • Homeopathy Guidelines
      • Homeopathy News
    • Siddha
      • Siddha Guidelines
      • Siddha News
    • Unani
      • Unani Guidelines
      • Unani News
    • Yoga
      • Yoga Guidelines
      • Yoga News
  • State News
    • Andaman and Nicobar Islands
    • Andhra Pradesh
    • Arunachal Pradesh
    • Assam
    • Bihar
    • Chandigarh
    • Chattisgarh
    • Dadra and Nagar Haveli
    • Daman and Diu
    • Delhi
    • Goa
    • Gujarat
    • Haryana
    • Himachal Pradesh
    • Jammu & Kashmir
    • Jharkhand
    • Karnataka
    • Kerala
    • Ladakh
    • Lakshadweep
    • Madhya Pradesh
    • Maharashtra
    • Manipur
    • Meghalaya
    • Mizoram
    • Nagaland
    • Odisha
    • Puducherry
    • Punjab
    • Rajasthan
    • Sikkim
    • Tamil Nadu
    • Telangana
    • Tripura
    • Uttar Pradesh
    • Uttrakhand
    • West Bengal
  • Medical Education
    • Ayush Education News
    • Dentistry Education News
    • Medical Admission News
    • Medical Colleges News
    • Medical Courses News
    • Medical Universities News
    • Nursing education News
    • Paramedical Education News
    • Study Abroad
  • Industry
    • Health Investment News
    • Health Startup News
    • Medical Devices News
    • Pharma News
      • CDSCO (Central Drugs Standard Control Organisation) News
    • Pharmacy Education News
    • Industry Perspective
OverviewMechanism of ActionHow To UseUsesBenfitsIndicationsDosage StrengthsDosage FormsDietary RestrictionsContraindicationsWarnings and Precautions for usingAdverse ReactionsOverdosage Clinical Pharmacology Clinical StudiesAuthored by Reviewed by References
Trimetazidine

Trimetazidine

Indications, Uses, Dosage, Drugs Interactions, Side effects
Trimetazidine
Medicine Type :
Allopathy
Prescription Type:
Prescription Required
Approval :
DCGI (Drugs Controller General of India)
Schedule
Schedule H
Pharmacological Class:
Fatty acid oxidation inhibitors,
Therapy Class:
Antianginal,

Trimetazidine is an antianginal agent belonging to the Fatty acid oxidation inhibitors.

Trimetazidine is used in the symptomatic treatment of stable angina pectoris.

Trimetazidine is rapidly absorbed from the gastrointestinal tract with a volume of distribution of 4.8 L/kg with plasma protein binding of 16% and gets partially metabolized in the liver (<40% metabolized) into 8 metabolites with unknown activity and gets excreted via urine (79-84%; >60% as unchanged drug) with elimination half-life: Approx 5-6 hours (immediate-release tab); 7 hours (modified-release tab and prolonged-release cap).

The Tmax of Trimetazidine was about <2 hours (immediate-release tab); 2-6 hours (modified-release tab); approx 14 hours (prolonged-release cap)and Cmax was about 91.2 µg/L.

The common side effects are dizziness, drowsiness, headache, weakness, Nausea, strong irregular heartbeat, swelling, and dizziness upon standing.

Trimetazidine is available in a dosage form, such as tablets.

Trimetazidine is available in Japan, Russia, France, and India.

Trimetazidine inhibits β-oxidation of fatty acids by blocking long-chain 3-ketoacyl-CoA thiolase, with the effect of enhancing glucose oxidation, resulting in the 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 ischemia or hypoxia, thus ensuring the proper functioning of ionic pumps and transmembrane Na-K flow without changing hemodynamic parameters.

Trimetazidine is available in a dosage form, such as a tablet.

Trimetazidine tablets were taken orally with or without food.

Trimetazidine is used in the symptomatic treatment of stable angina pectoris.

Trimetazidine selectively inhibits long-chain 3-ketoacyl coenzyme A thiolase, an enzyme responsible for mitochondrial beta-oxidation of long-chain fatty acids. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis, and improves the mechanical resistance of the sarcolemma.

Trimetazidine is approved for its use in the following clinical indications:

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 bid. As modified-release tab: 35 mg bid. A prolonged-release cap: 80 mg once daily.

Trimetazidine is available in various dosage strengths: 20mg, 35 mg, and 80 mg.

Trimetazidine is available in a dosage form, such as a tablet.

  • CrCl 30-60 mL/minute:
  • Immediate-release tablet: Initial and maximum dose: 20 mg twice daily
  • Modified release tablet: Initial and maximum dose: 35 mg once daily (preferably in the morning)
  • CrCl <30 mL/minute: Use is contraindicated

Trimetazidine is approved for the treatment of Angina pectoris

Eat plenty of fruits, vegetables, and whole grains. Choose lean proteins, such as skinless chicken, fish, and beans. Eat non-fat or low-fat dairy products, such as skim milk and low-fat yogurt. Avoid foods that contain high levels of sodium (salt).

Trimetazidine may be contraindicated in the following.

Parkinson’s disease, parkinsonian symptoms, restless leg syndrome, tremors, and other related movement disorders.

Severe renal impairment (CrCl <30 mL/min). Lactation.

Pregnancy Warning

This medicine is not recommended for use in pregnant women unless absolutely necessary. All the risks and benefits should be discussed with the doctor before taking this medicine.

Food Warning

Salt Substitutes: Those who are taking Trimetazidine should avoid sodium, calcium, and magnesium-rich foods. The salts may reduce the blood-pressure-lowering effect of Trimetazidine.

The adverse reactions related to the molecule Trimetazidine can be categorized as

  • Common Adverse Effects: Haemorrhage, potential risk of transmission of infection, embolism including pulmonary or cholesterol embolism, infusion reactions (e.g., fever, chills, rigors). Rarely allergic reactions (e.g., bronchospasm, rash). Gastrointestinal disorders: Gingival bleeding, gastrointestinal or retroperitoneal hemorrhage, nausea, vomiting.
  • Less Common Adverse Effects: Headache, and dizziness. Skin and subcutaneous tissue disorders: Rash, urticaria, pruritus.
  • Rare Adverse Effects: Palpitations, extrasystoles, tachycardia, arterial hypotension, orthostatic hypotension, and flushing.

The clinically relevant drug interactions of Trimetazidine are briefly summarized here.

Trimetazidine should be used with caution with sedatives or hypnotics (buspirone), strong painkillers, some allergy medications (chlorphenamine), certain antidepressants (fluoxetine and lithium), medicines to lower blood pressure (methyldopa), medicines to treat Parkinson’s disease (levodopa, pramipexole, ropinirole), medicines to treat epilepsy (phenobarbital, carbamazepine, phenytoin, rifampicin, primidone, oxcarbazepine, ethosuximide, valproate).

Symptoms: Hypertension, acute heart failure, bradycardia, heart block, AV block, cardiogenic shock, bronchospasm, trouble breathing and consciousness, coma, nausea, vomiting, generalized convulsions, cyanosis (manifest in 20 minutes – 2 hours after taking metoprolol).

Treatment: gastric lavage, the symptomatic therapy: atropine sulfate injection (IV fast 0.5-2 mg) if bradycardia and a violation of AV conduction; glucagon (1-10 mg IV, then IV infusion 2-2.5 mg / h) and dobutamine in the case of reduction of myocardial contractility; agonists (noradrenaline, adrenaline, etc.) when arterial hypotension; diazepam (IV slowly) to eliminate seizures; beta-agonists inhalation or IV jet injection of aminophylline to relieve broncho spastic reactions; cardio acceleration.

Pharmacodynamics:

Trimetazidine is indicated for the symptomatic treatment of stable angina pectoris in patients inadequately controlled or intolerant to first-line therapies. Patients should be counseled regarding the risk of use with reduced renal or hepatic function, worsening of extrapyramidal symptoms or other movement disorders, and risk of falls

Pharmacokinetics:

  • Absorption

In elderly patients, a 35 mg oral modified release tablet reaches a mean Cmax of 115 µg/L, with a Tmax of 2.0-5.0 hours, and a mean AUC0-12 of 1104 h*µg/L. In young, healthy patients, the same dose reaches a mean Cmax of 91.2 µg/L, with a Tmax of 2.0-6.0 hours, and an AUC0-12h 720 h*µg/L.

  • Distribution:

The volume of distribution: 4.8 L/kg. Plasma protein binding: 16%.

  • Metabolism:

Trimetazidine can be oxidized at the piperazine ring to form trimetazidine ketopiperazine. Trimetazidine can also be N-formylated, N-acetylated, or N-methylated at the piperazine ring to form N-formyltrimetazidine, N-acetyltrimetazidine, and N-methyltrimetazidine respectively. Alternatively, trimetazidine can be demethylated at the 2, 3, or 4 positions of the 2,3,4-trimethoxybenzyl moiety to form 2-desmethyltrimetazidine, 3-desmethyltrimetazidine, or 4-desmethyltrimetazidine. The desmethyltrimetazidine metabolites can undergo sulfate conjugation or glucuronidation prior to elimination.

  • Elimination

Trimetazidine is 79-84% eliminated in the urine, with 60% as the unchanged parent compound. In a study of 4 healthy subjects, individual metabolites made up 0.01-1.4% of the dose recovered in urine. In the urine, 2-desmethyltrimetazidine made up 0-1.4% of the recovered dose, 3- and 4-desmethyltrimetazidine made up 0.039-0.071% each, N-methyltrimetazidine made up 0.015-0.11%, trimetazidine ketopiperazine made up 0.011-0.4%, N-formyltrimetazidine made up 0.035-0.42%, N-acetyltrimetazidine made up 0.016-0.19%, desmethyl trimetazidine O-sulphate made up 0.01-0.65% and an unknown metabolite made up0.026-0.67%.


There are some clinical studies of the drug Trimetazidine mentioned below:
  1. https://clinicaltrials.gov/ct2/show/NCT00532493
  2. https://pubmed.ncbi.nlm.nih.gov/29414272/
  3. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3538493/
           4. https://ajp.psychiatryonline.org/doi/10.1176/appi.ajp.2018.17080913


    • https://reference.medscape.com/drug/cardura-xl-Trimetazidine -342343
    • https://www.mims.com/india/drug/info/Trimetazidine ?type=full&mtype=generic
    • https://go.drugbank.com/drugs/DB00590
    • https://www.rxlist.com/consumer_Trimetazidine _cardura/drugs-condition.htm
    undefined
    Parthika Patel
    Parthika Patel has completed her Graduated B.Pharm from SSR COLLEGE OF PHARMACY and done M.Pharm in Pharmaceutics. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
    undefined
    Dr JUHI SINGLA
    Dr JUHI SINGLA has completed her MBBS from Era’s Lucknow Medical college and done MD pharmacology from SGT UNIVERSITY Gurgaon. She can be contacted at editorial@medicaldialogues.in. Contact no. 011-43720751
    Published on: 31 Oct 2022 1:26 PM GMT
    © 2022 All Rights Reserved.
    Powered By: Hocalwire
    X
    We use cookies for analytics, advertising and to improve our site. You agree to our use of cookies by continuing to use our site. To know more, see our Cookie Policy and Cookie Settings.Ok