Molsidomine-Lekpharm (Tablets) Instructions for Use

Marketing Authorization Holder

Lekpharm, SOOO (Republic of Belarus)

ATC Code

C01DX12 (Molsidomine)

Active Substance

Molsidomine (Rec.INN WHO registered)

Dosage Forms

	Molsidomine-Lekpharm	Tablets 2 mg: 30 pcs.
		Tablets 4 mg: 30 pcs.

Dosage Form, Packaging, and Composition

Tablets white or almost white, round, flat-cylindrical in shape with a bevel and a score on one side.

Excipients: magnesium stearate – 1 mg, crospovidone (type B) – 1 mg, lactose monohydrate – 96 mg.

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

Tablets white or almost white, round, flat-cylindrical in shape with a bevel and a score on one side.

Excipients: magnesium stearate – 2 mg, crospovidone (type B) – 2 mg, lactose monohydrate – 192 mg.

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

Clinical-Pharmacological Group

Peripheral vasodilator. Anti-anginal drug

Pharmacotherapeutic Group

Vasodilating agent

Pharmacological Action

An antianginal agent from the group of sydnonimines. The action of molsidomine is realized through nitric oxide (NO) formed during its metabolism, which stimulates soluble guanylate cyclase.

This leads to the accumulation of cGMP, which promotes relaxation of the smooth muscles of the vascular wall. Molsidomine causes a decrease in venous pressure, end-diastolic pressure in the ventricles, and pressure in the pulmonary artery.

It reduces myocardial oxygen demand. It dilates large coronary arteries and improves collateral circulation in coronary atherosclerosis. In chronic heart failure, molsidomine reduces ventricular dilation.

Pharmacokinetics

After oral administration, Molsidomine is almost completely (90%) absorbed from the gastrointestinal tract. Food intake does not affect the extent and rate of absorption. Plasma protein binding is about 10%.

It is metabolized in the liver to form active metabolites (mainly linsidomine, i.e., SIN-1 A, which releases NO), which are then inactivated. Molsidomine and its metabolites are mainly excreted in the urine (90%).

T_1/2 increases with impaired liver function.

Indications

Prevention and long-term treatment of stable angina pectoris in adults in case of insufficient effectiveness, contraindications to the use, or intolerance of other antianginal drugs (such as beta-blockers and/or calcium channel blockers), as well as in older patients.

ICD codes

Dosage Regimen

Determine the dosage individually based on clinical response and tolerability.

Initiate therapy with a low dose and titrate upwards gradually to minimize adverse effects such as headache.

For the 2 mg tablet, the typical starting dose is one tablet (2 mg) taken two to three times daily.

For the 4 mg tablet, the typical starting dose is half a tablet (2 mg) taken two to three times daily; use the score line for accurate division.

The maximum single dose is 4 mg.

The maximum daily dose is 12 mg, administered in two or three divided doses.

Administer tablets orally with a sufficient amount of water, with or without food.

For elderly patients and patients with hepatic impairment or renal impairment, initiate treatment at the lowest possible dose and adjust carefully.

In patients with arterial hypotension, use with caution and monitor blood pressure closely.

Regularly reassess the need for continued antianginal therapy.

Adverse Reactions

From the cardiovascular system: at the beginning of treatment, headaches may occur (which cease during therapy); rarely – facial flushing, orthostatic hypertension.

From the digestive system: nausea, diarrhea, loss of appetite may occur.

Contraindications

Hypersensitivity to molsidomine; cardiogenic shock, pronounced arterial hypotension, decreased central venous pressure, glaucoma; simultaneous use of nitric oxide donors in any form and stimulators of soluble guanylate cyclase (riociguat) due to the high risk of arterial hypotension.

Use in Pregnancy and Lactation

Use during pregnancy and breastfeeding is contraindicated.

Use in Hepatic Impairment

Elderly patients with impaired liver function require dose adjustment.

Use in Renal Impairment

Elderly patients with impaired renal function require dose adjustment.

Pediatric Use

Used in adult patients.

Geriatric Use

Elderly patients with impaired liver or kidney function and arterial hypotension require dose adjustment.

Special Precautions

Use with special caution in patients after a recent myocardial infarction.

Elderly patients with impaired liver or kidney function and arterial hypotension require dose adjustment.

Effect on the ability to drive vehicles and mechanisms

During the use of molsidomine (especially at the beginning of treatment), one should refrain from engaging in potentially hazardous activities that require increased attention and rapid psychomotor reactions.

Drug Interactions

With simultaneous use with antihypertensive and vasodilating agents, an enhancement of the antihypertensive effect is possible.

Simultaneous use of molsidomine may potentiate the antihypertensive effect of soluble guanylate cyclase stimulators (such as riociguat) with the development of severe arterial hypotension.

With simultaneous use with acetylsalicylic acid, the antiplatelet effect of acetylsalicylic acid is enhanced.

With simultaneous use with ethanol, the risk of arterial hypotension increases.

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.