Olicard^® 40 Retard (Capsules) Instructions for Use

ATC Code

C01DA14 (Isosorbide mononitrate)

Active Substance

Isosorbide mononitrate (Rec.INN registered by WHO)

Clinical-Pharmacological Group

Peripheral vasodilator. Anti-anginal drug

Pharmacotherapeutic Group

Vasodilating agent – nitrate

Pharmacological Action

Peripheral vasodilator with a predominant effect on venous vessels, an antianginal agent. It causes a decrease in myocardial oxygen demand due to a reduction in preload (dilation of peripheral veins and decreased blood flow to the right atrium) and afterload (decrease in systemic vascular resistance), and also has a direct coronary vasodilating effect.

It promotes the redistribution of coronary blood flow to areas with reduced blood supply. It increases exercise tolerance in patients with coronary artery disease and angina pectoris. In heart failure, it promotes myocardial unloading by reducing preload. It reduces pressure in the pulmonary circulation.

Pharmacokinetics

After oral administration, isosorbide-5-mononitrate is rapidly and completely absorbed from the gastrointestinal tract. Bioavailability is 90-100%. Plasma concentration is directly proportional to the dose.

Isosorbide-5-mononitrate is almost completely biotransformed in the liver to form inactive metabolites.

It is excreted by the kidneys mainly in the form of metabolites, 2% unchanged. The elimination half-life (T_1/2) is 4-5 hours.

Indications

Coronary artery disease: prevention of angina attacks, including after myocardial infarction.

Chronic heart failure – as additional symptomatic therapy in combination with cardiac glycosides and/or diuretics when they are insufficiently effective.

ICD codes

Dosage Regimen

Administer Olicard^® 40 Retard capsules orally, swallowed whole with a sufficient amount of liquid. Do not chew or crush the capsules.

Initiate therapy with a low dose and titrate individually based on clinical response and tolerability. The standard maintenance dose for the prophylaxis of angina pectoris is one 40 mg capsule once or twice daily.

For twice-daily administration, take the second capsule no later than 8 hours after the first dose to ensure a daily nitrate-free interval and prevent the development of tolerance.

In patients with chronic heart failure, use as adjunctive therapy. The dose must be carefully titrated to avoid a pronounced decrease in blood pressure.

In elderly patients and those with severe hepatic or renal impairment, initiate treatment with particular caution and at the lower end of the dosing range. Monitor blood pressure and heart rate closely during dose adjustment.

Abrupt discontinuation of therapy may provoke a withdrawal syndrome, characterized by an increase in angina attacks. Gradually reduce the dosage under medical supervision when terminating treatment.

Adverse Reactions

From the cardiovascular system: often – tachycardia, orthostatic hypotension; infrequently – “paradoxical” increase in angina attacks; collapse (sometimes accompanied by bradyarrhythmia and syncope); frequency unknown – pronounced decrease in blood pressure.

From the nervous system: very often – “nitrate” headache; often – drowsiness, dizziness; rarely – cerebral ischemia.

From the digestive system: infrequently – nausea, vomiting; very rarely – heartburn.

From the skin and subcutaneous tissues: infrequently – skin allergic reactions (including rash), flushing; very rarely – angioedema, Stevens-Johnson syndrome; frequency unknown – exfoliative dermatitis.

General disorders: often – asthenia, development of tolerance (including cross-tolerance to other nitrates). To prevent the development of tolerance, continuous use of high doses of isosorbide mononitrate should be avoided.

Long-term use of isosorbide mononitrate can cause transient hypoxemia due to relative redistribution of blood flow to hypoventilated alveolar areas (in patients with coronary artery disease – can lead to myocardial ischemia).

Contraindications

Hypersensitivity to isosorbide dinitrate, other nitrates; acute circulatory disorders (shock, collapse); cardiogenic shock (if measures to maintain end-diastolic pressure are not being taken); hypertrophic obstructive cardiomyopathy; constrictive pericarditis; cardiac tamponade; severe arterial hypotension (systolic blood pressure below 90 mm Hg); severe hypovolemia; severe anemia; severe aortic and subaortic stenosis, severe mitral stenosis; cerebral hemorrhage; simultaneous use of PDE5 inhibitors (including sildenafil, vardenafil, tadalafil); simultaneous use with the soluble guanylate cyclase stimulator riociguat; age under 18 years (efficacy and safety not established).

With caution: low left ventricular filling pressure, including in acute myocardial infarction, impaired left ventricular function; aortic and/or mitral stenosis; diseases accompanied by increased intracranial pressure; closed-angle glaucoma; tendency to orthostatic disorders of vascular regulation, severe renal and/or hepatic insufficiency, hypothyroidism, inadequate and malnutrition; pregnancy, breastfeeding period.

Use in Pregnancy and Lactation

Use during pregnancy and lactation (breastfeeding) is possible in cases where the expected benefit of therapy for the mother outweighs the potential risk to the fetus or child.

If use during lactation is necessary, the issue of discontinuing breastfeeding should be decided.

Use in Hepatic Impairment

Should be used with caution in patients with severe hepatic insufficiency.

Use in Renal Impairment

Should be used with caution in patients with severe renal insufficiency.

Pediatric Use

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

Special Precautions

Not used for relief of angina attacks. Use with caution in increased intracranial pressure.

During therapy, monitoring of blood pressure and heart rate is necessary.

During the use of isosorbide mononitrate, alcohol consumption should be avoided.

Effect on the ability to drive vehicles and mechanisms

During treatment, it is not recommended to drive vehicles and engage in other potentially hazardous activities that require quick psychomotor reactions.

Drug Interactions

With simultaneous use with adsorbents, astringents and coating agents, the absorption of isosorbide mononitrate is reduced.

With simultaneous use with anticholinergic agents, memory and attention disorders are possible in elderly patients.

With simultaneous use of vasodilators, calcium channel blockers, tricyclic antidepressants, ethanol, an increase in the hypotensive effect is possible.

With simultaneous use with antihypertensive drugs, beta-blockers, neuroleptics, PDE inhibitors (including sildenafil, vardenafil, tadalafil), an increase in the hypotensive effect is possible.

With simultaneous use with dihydroergotamine, an increase in the concentration and enhancement of the effect of dihydroergotamine is possible.

With simultaneous use with norepinephrine, the therapeutic effect of norepinephrine is reduced.

Simultaneous use of isosorbide mononitrate with riociguat, a soluble guanylate cyclase stimulator, is contraindicated, as it may cause hypotension.

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.