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Trimetazidine (Tablets) Instructions for Use

ATC Code

C01EB15 (Trimetazidine)

Active Substance

Trimetazidine (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Drug improving metabolism of the myocardium and neurosensory organs under ischemic conditions

Pharmacotherapeutic Group

Antihypoxant

Pharmacological Action

An agent that normalizes the energy metabolism of cells subjected to hypoxia or ischemia. It prevents the decrease in intracellular ATP content, ensures the normal functioning of membrane ion channels, transmembrane transfer of potassium and sodium ions, and the preservation of cellular homeostasis.

Trimetazidine slows down the oxidation of fatty acids by selectively inhibiting long-chain 3-ketoacyl-CoA thiolase, which leads to increased glucose oxidation and restoration of the coupling between glycolysis and oxidative decarboxylation and has been shown to provide protection of the myocardium from ischemia. The switching of fatty acid oxidation to glucose oxidation underlies the antianginal action of trimetazidine.

Trimetazidine maintains the energy metabolism of the heart and neurosensory organs during episodes of ischemia; reduces the degree of intracellular acidosis and the extent of changes in transmembrane ion flow occurring during ischemia; reduces the level of migration and infiltration of polymorphonuclear neutrophils in ischemic and reperfused heart tissues, reduces the size of myocardial damage; while it does not affect hemodynamics.

Pharmacokinetics

Trimetazidine is rapidly and almost completely absorbed from the gastrointestinal tract. Vd is 4.8 L/kg. It easily passes through histohematic barriers. Plasma protein binding is about 16%.

T1/2 is 4.5-5 hours. It is excreted by the kidneys, mainly unchanged.

Indications

Long-term therapy of coronary artery disease: prevention of attacks of stable angina pectoris as part of mono- or combination therapy.

ICD codes

ICD-10 code Indication
I20 Angina pectoris
ICD-11 code Indication
BA40.Z Angina pectoris, unspecified

Dosage Regimen

The method of application and dosage regimen for a specific drug depend on its form of release and other factors. The optimal dosage regimen is determined by the doctor. It is necessary to strictly adhere to the compliance of the dosage form of a specific drug with the indications for use and dosage regimen.

Administer Trimetazidine tablets orally with water during meals.

The standard total daily dose is 40 mg to 70 mg.

Divide the total daily dose into two or three separate administrations.

A common regimen is one 20 mg tablet taken three times daily with breakfast, lunch, and dinner.

For the modified-release formulation, the typical dose is one 35 mg tablet taken twice daily, in the morning and evening.

Adhere strictly to the twice-daily or three-times-daily schedule to maintain stable plasma concentrations.

The duration of therapy is determined individually based on the patient’s clinical response and the severity of ischemic symptoms.

Continue treatment for as long as clinically required; regularly reassess the need for ongoing therapy.

Do not use for the acute relief of an angina attack.

In patients with moderate renal impairment (creatinine clearance 30-60 mL/min), monitor treatment response closely.

This medication is contraindicated in patients with severe renal impairment (creatinine clearance less than 30 mL/min).

Use with caution in patients over 75 years of age and those with severe hepatic impairment.

Adverse Reactions

From the digestive system: frequently – abdominal pain, diarrhea, dyspepsia, nausea, vomiting; frequency unknown – constipation.

From the nervous system: frequently – dizziness, headache; infrequently – paresthesia; frequency unknown – symptoms of parkinsonism (tremor, akinesia, increased tone), instability in the Romberg position and unsteady gait, restless legs syndrome (usually reversible after discontinuation of therapy), insomnia, drowsiness.

From the hearing organ and labyrinthine disorders: frequency unknown – vertigo.

From the skin and subcutaneous tissues: frequently – skin rash, itching, urticaria; frequency unknown – acute severe skin adverse reactions, including drug reaction with eosinophilia and systemic symptoms (DRESS syndrome) and acute generalized exanthematous pustulosis, which can be fatal.

Allergic reactions frequency unknown – angioedema.

From the cardiovascular system: rarely – palpitations, extrasystole, tachycardia, marked decrease in blood pressure, orthostatic hypotension (may be accompanied by general weakness, dizziness or loss of balance, especially when taking antihypertensive drugs simultaneously), flushing.

From the hematopoietic system: frequency unknown – agranulocytosis, thrombocytopenia, thrombocytopenic purpura.

From the liver and biliary tract: frequency unknown – hepatitis.

Other: frequently – asthenia.

Contraindications

Hypersensitivity to trimetazidine; Parkinson’s disease, symptoms of parkinsonism, tremor, restless legs syndrome and other related movement disorders; severe renal failure (creatinine clearance less than 30 ml/min); children and adolescents under 18 years of age; pregnancy, lactation (breastfeeding).

With caution

Patients with moderate renal failure (creatinine clearance 30-60 ml/min), patients with severe hepatic insufficiency (10 to 15 points on the Child-Pugh scale); patients over 75 years of age.

Use in Pregnancy and Lactation

Trimetazidine is contraindicated for use during pregnancy and lactation (breastfeeding).

Use in Hepatic Impairment

Should be used with caution in patients with severe hepatic insufficiency (10 to 15 points on the Child-Pugh scale).

Use in Renal Impairment

Contraindicated in severe renal failure (creatinine clearance less than 30 ml/min). Should be used with caution in patients with moderate renal failure (creatinine clearance 30-60 ml/min).

Pediatric Use

Contraindicated for use in children and adolescents under 18 years of age.

Geriatric Use

Should be used with caution in patients over 75 years of age.

Special Precautions

It is not intended for the relief of angina attacks and is not indicated for the initial course of therapy for unstable angina or myocardial infarction at the pre-hospital stage or in the first days of hospitalization.

Influence on the ability to drive vehicles and mechanisms

During the use of trimetazidine, patients should exercise caution when driving vehicles and mechanisms, as well as when engaging in other potentially hazardous activities that require increased concentration and speed of psychomotor reactions.

Storage Conditions

Store at 2°C (36°F) to 25°C (77°F). Keep in original packaging, protected from light. Keep out of reach of children.

Dispensing Status

Rx Only

Important Safety Information

This information is for educational purposes only and does not replace professional medical advice. Always consult your doctor before use. Dosage and side effects may vary. Use only as prescribed.

Medical Disclaimer

Brand (or Active Substance), Marketing Authorisation Holder, Dosage Form

Marketing Authorization Holder

Okasa Pharma, Ltd. (India)

Dosage Form

Bottle Rx Icon Trimetazidine Coated tablets 20 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Coated tablets 1 tab.
Trimetazidine dihydrochloride 20 mg

10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (6) – cardboard packs.

Marketing Authorization Holder

Alsi Pharma, JSC (Russia)

Contact Information

ALSI Pharma JSC (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Film-coated tablets, 20 mg: 10, 20, 30, 40, 50, 60, or 100 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets red in color, biconvex in shape.

1 tab.
Trimetazidine dihydrochloride 20 mg

Excipients : lactose monohydrate – 81 mg, povidone – 3 mg, crospovidone – 3 mg, magnesium stearate – 1 mg, polyvinyl alcohol – 1.8 mg, macrogol (polyethylene glycol) – 900 mcg, talc – 700 mcg, titanium dioxide – 200 mcg, Ponceau 4R dye – 180 mcg, Sunset Yellow dye – 10 mcg, aluminum lake – 710 mcg.

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (4) – cardboard packs.
10 pcs. – contour cell packs (5) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
100 pcs. – polymer jars (1) – cardboard packs.

Marketing Authorization Holder

Belmedpreparaty RUP (Republic of Belarus)

Dosage Form

Bottle Rx Icon Trimetazidine Film-coated tablets, 20 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets white in color, round, biconvex in shape.

1 tab.
Trimetazidine dihydrochloride 20 mg
(calculated as 100% substance)

Excipients : potato starch 14 mg, calcium stearate 1 mg, lactose monohydrate – to obtain a tablet weighing 98 mg (without coating).

Coating composition: hypromellose 2910 0.99 mg, polysorbate 80 0.25 mg, titanium dioxide 0.48 mg, talc 0.28 mg

10 pcs. – contour cell packs (3) – cardboard packs.

Marketing Authorization Holder

Borisov Plant Of Medical Preparations, PJSC (Republic Of Belarus)

Dosage Form

Bottle Rx Icon Trimetazidine Extended-release film-coated tablets, 35 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Extended-release film-coated tablets pink in color, round, with a biconvex surface.

1 tab.
Trimetazidine dihydrochloride 35 mg

Excipients : hypromellose (type 2208) (hydroxypropyl methylcellulose) (Methocel K100M Premium) – 31.5 mg, hypromellose (type 2208) (hydroxypropyl methylcellulose) (Methocel K15M Premium) – 31.5 mg, colloidal anhydrous silicon dioxide – 1.05 mg, magnesium stearate – 1.05 mg, microcrystalline cellulose – to a core weight of 210 mg, Opadry F200 – 5 mg.

Composition of Opadry series 200F code 240002 (pink) polyvinyl alcohol, partially hydrolyzed – 35%, titanium dioxide (E171) – 24.24%, talc – 23.88%, macrogol 3350 (polyethylene glycol) – 12%, methacrylic acid copolymer type C – 4%, yellow iron oxide dye (E172) – 0.37%; red iron oxide dye (E172) – 0.36%; sodium bicarbonate (E500ii) – 0.12%; black iron oxide dye (E172) – 0.03%.

10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.

Marketing Authorization Holder

ZiO-Health CJSC (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Modified-release coated tablets, 35 mg: 10, 14, 20, 28, 30, 500, 1000, 1400, 2000, 2800, 3000, 40004200, 5000, 5600, or 7000 pcs.

Dosage Form, Packaging, and Composition

Modified-release coated tablets 1 tab.
Trimetazidine dihydrochloride 35 mg

10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (1) – cardboard packs.
10 pcs. – blisters (100) – cardboard packs.
10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (300) – cardboard packs.
10 pcs. – blisters (400) – cardboard packs.
10 pcs. – blisters (500) – cardboard packs.
14 pcs. – blisters (1) – cardboard packs.
14 pcs. – blisters (2) – cardboard packs.
14 pcs. – blisters (100) – cardboard packs.
14 pcs. – blisters (200) – cardboard packs.
14 pcs. – blisters (300) – cardboard packs.
14 pcs. – blisters (400) – cardboard packs.
14 pcs. – blisters (500) – cardboard packs.
10 pcs. – blisters (200) – cardboard packs.
500 pcs. – polymer jars (1) – cardboard packs.
1000 pcs. – polymer jars (1) – cardboard packs.

Marketing Authorization Holder

Canonpharma Production, CJS (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Film-coated tablets 20 mg: 10, 20, 30, 60, 90, or 120 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets pink in color, round, biconvex; on the cross-section – white or almost white.

1 tab.
Trimetazidine dihydrochloride 20 mg

Excipients : hyprolose (hydroxypropylcellulose) – 0.7 mg, corn starch – 16 mg, colloidal silicon dioxide (aerosil) – 3.13 mg, lactose monohydrate – 89.47 mg, magnesium stearate – 0.7 mg.

Coating composition Selecote AQ-01673 – 6 mg (hypromellose (hydroxypropyl methylcellulose) – 2.4 mg, macrogol 400 (polyethylene glycol 400) – 0.6 mg, macrogol 6000 (polyethylene glycol 6000) – 0.6 mg, Ponceau 4R dye – 0.6 mg, titanium dioxide – 1.8 mg).

10 pcs. – contour cell packs (1) – cardboard packs.
10 pcs. – contour cell packs (2) – cardboard packs.
10 pcs. – contour cell packs (3) – cardboard packs.
10 pcs. – contour cell packs (6) – cardboard packs.
30 pcs. – contour cell packs (1) – cardboard packs.
30 pcs. – contour cell packs (2) – cardboard packs.
30 pcs. – contour cell packs (3) – cardboard packs.
30 pcs. – contour cell packs (4) – cardboard packs.

Marketing Authorization Holder

Novosibkhimpharm, JSC (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Film-coated tablets, 20 mg: 20, 30, 40, or 60 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets 1 tab.
Trimetazidine dihydrochloride 20 mg

10 pcs. – blisters (3) – cardboard packs.
10 pcs. – blisters (2) – cardboard packs.
10 pcs. – blisters (4) – cardboard packs.
10 pcs. – blisters (6) – cardboard packs.
20 pcs. – polymer jars (1) – cardboard packs.
40 pcs. – polymer jars (1) – cardboard packs.
60 pcs. – polymer jars (1) – cardboard packs.

Marketing Authorization Holder

Ozon, LLC (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Coated tablets 20 mg: 10, 14, 20, 28, 30, 40, 50, or 60 pcs.

Dosage Form, Packaging, and Composition

Coated tablets 1 tab.
Trimetazidine dihydrochloride 20 mg

10 pcs. – contour cell packs (1) – cardboard boxes.
10 pcs. – contour cell packs (2) – cardboard boxes.
10 pcs. – contour cell packs (3) – cardboard boxes.
10 pcs. – contour cell packs (4) – cardboard boxes.
10 pcs. – contour cell packs (5) – cardboard boxes.
10 pcs. – contour cell packs (6) – cardboard boxes.
10 pcs. – polymer containers (1) – cardboard packs.
14 pcs. – polymer containers (1) – cardboard packs.
20 pcs. – polymer containers (1) – cardboard packs.
28 pcs. – polymer containers (1) – cardboard packs.
30 pcs. – polymer containers (1) – cardboard packs.
40 pcs. – polymer containers (1) – cardboard packs.
50 pcs. – polymer containers (1) – cardboard packs.

Marketing Authorization Holder

Tatkhimpharmpreparaty, JSC (Russia)

Dosage Form

Bottle Rx Icon Trimetazidine Film-coated tablets, 20 mg: 30 or 60 pcs.

Dosage Form, Packaging, and Composition

Film-coated tablets 1 tab.
Trimetazidine dihydrochloride 20 mg

10 pcs. – blisters (3) – carton packs.
10 pcs. – blisters (6) – carton packs.
15 pcs. – blisters (2) – carton packs.
15 pcs. – blisters (4) – carton packs.

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