Nitroglycerin Medisorb (Tablets) Instructions for Use

Marketing Authorization Holder

Medisorb, JSC (Russia)

ATC Code

C01DA02 (Nitroglycerin)

Active Substance

Nitroglycerin

Nitroglycerin (USP United States Pharmacopeia)

Dosage Form

Nitroglycerin Medisorb

Sublingual tablets 0.5 mg

Dosage Form, Packaging, and Composition

Sublingual tablets

100 pcs. – cases – cardboard packs (100 pcs.) – Over-the-counter
100 pcs. – tubes – cardboard packs (100 pcs.) – Over-the-counter
40 pcs. – cases – cardboard packs (40 pcs.) – Over-the-counter
40 pcs. – tubes – cardboard packs (40 pcs.) – Over-the-counter
50 pcs. – cases – cardboard packs (50 pcs.) – Over-the-counter
50 pcs. – tubes – cardboard packs (50 pcs.) – Over-the-counter

Clinical-Pharmacological Group

Peripheral vasodilator. Anti-anginal drug

Pharmacotherapeutic Group

Drugs for the treatment of heart diseases; vasodilators for the treatment of heart diseases; organic nitrates

Pharmacological Action

Peripheral vasodilator with a predominant effect on venous vessels. Anti-anginal agent. The mechanism of action is associated with the release of the active substance nitric oxide in vascular smooth muscle. Nitric oxide causes activation of guanylate cyclase and increases the level of cGMP, which ultimately leads to smooth muscle relaxation.

Under the influence of glyceryl trinitrate, arterioles and precapillary sphincters relax to a lesser extent than large arteries and veins. This is partly due to reflex reactions, as well as less intense formation of nitric oxide from active substance molecules in the walls of arterioles.

The action of nitroglycerin (glyceryl trinitrate) is mainly associated with 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 total peripheral vascular resistance). Promotes redistribution of coronary blood flow to ischemic subendocardial areas of the myocardium. Increases exercise tolerance in patients with coronary artery disease, angina pectoris. In heart failure, it promotes myocardial unloading mainly by reducing preload. Reduces pressure in the pulmonary circulation.

Pharmacokinetics

After oral administration, it is absorbed from the gastrointestinal tract and undergoes the first-pass effect through the liver. With sublingual administration, this effect is absent, and the therapeutic concentration in blood plasma is achieved within a few minutes. It is metabolized in the liver with the participation of nitrate reductase. Among the metabolites of nitroglycerin, dinitro derivatives can cause pronounced vasodilation; it is possible that they determine the therapeutic effect of nitroglycerin (glyceryl trinitrate) when taken orally.

Plasma protein binding is 60%. T_1/2 after oral administration is 4 hours, with sublingual administration – 20 minutes, after intravenous administration – 1-4 minutes. It is excreted mainly by the kidneys.

Indications

For sublingual and buccal use: relief and prevention of angina attacks; as an emergency treatment for acute myocardial infarction and acute left ventricular failure at the prehospital stage.

For oral administration: relief and prevention of angina attacks, rehabilitation treatment after myocardial infarction.

For intravenous administration: acute myocardial infarction, including complicated by acute left ventricular failure; unstable angina; pulmonary edema.

For topical application: prevention of angina attacks.

ICD codes

Dosage Regimen

Administer sublingually, buccally, orally, topically, or intravenously. Titrate the dose and regimen individually based on indication and clinical presentation.

For sublingual administration to relieve an acute angina attack, place one 0.5 mg tablet under the tongue at the first sign of an attack. Do not swallow the tablet. Allow it to dissolve completely in the sublingual pocket. Do not eat, drink, or smoke until the tablet is fully dissolved.

If chest pain persists, administer a second 0.5 mg tablet after 5 minutes. Do not exceed three tablets within a 15-minute period. Seek immediate emergency medical assistance if pain continues after three doses.

For prophylaxis of angina attacks prior to anticipated physical or emotional stress, administer one 0.5 mg tablet sublingually 5 to 10 minutes before the activity.

For buccal administration, place the tablet between the lip and gum or between the cheek and gum. Allow it to dissolve slowly. Do not crush or chew the tablet.

Monitor for signs of arterial hypotension, especially after the initial dose. The patient should be in a sitting or recumbent position during and immediately after administration to mitigate hypotensive effects.

To prevent the development of tolerance with chronic use, maintain a daily nitrate-free interval of 10 to 12 hours. Schedule dosing to provide this period of low nitrate exposure, typically overnight.

Store tablets in the original glass container. Keep it tightly closed and protected from light and moisture. Do not transfer tablets to other containers. Discard any unused tablets 6 months after opening the original container, as the potency decreases.

Adverse Reactions

From the cardiovascular system dizziness, headache, tachycardia, skin flushing, feeling of heat, arterial hypotension; rarely (especially with overdose) – collapse, cyanosis.

From the digestive system nausea, vomiting.

From the central nervous system rarely (especially with overdose) – anxiety, psychotic reactions.

Allergic reactions rarely – skin rash, itching.

Local reactions mild itching, burning, skin redness.

Other methemoglobinemia.

Contraindications

Shock, collapse, arterial hypotension (systolic BP <100 mm Hg, diastolic BP <60 mm Hg), acute myocardial infarction with severe arterial hypotension, hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, toxic pulmonary edema, increased intracranial pressure (including in hemorrhagic stroke, after a recent head injury), closed-angle glaucoma with high intraocular pressure, hypersensitivity to nitrates.

Use in Pregnancy and Lactation

The use of nitroglycerin (glyceryl trinitrate) during pregnancy and lactation (breastfeeding) is possible only in cases where the intended benefit to the mother outweighs the potential risk to the fetus or infant.

Use in Hepatic Impairment

Use with caution in severe liver dysfunction (parenterally).

Use in Renal Impairment

Use with caution in severe renal dysfunction (parenterally).

Geriatric Use

Use with caution in elderly patients.

Special Precautions

Use with caution in patients with severe cerebral atherosclerosis, cerebrovascular accidents, a tendency to orthostatic hypotension, with severe anemia, in elderly patients, as well as in hypovolemia and severe liver and kidney dysfunction (parenterally).

With prolonged use, the development of tolerance to the action of nitrates is possible. To prevent the occurrence of tolerance, it is recommended to observe a 10-12 hour break in their use during each 24-hour cycle.

If an angina attack occurs during topical application of nitroglycerin (glyceryl trinitrate), it should be relieved by taking glyceryl trinitrate under the tongue.

Avoid alcohol consumption during treatment.

Effect on ability to drive vehicles and operate machinery

Glyceryl trinitrate may reduce the speed of psychomotor reactions, which should be taken into account when driving vehicles or engaging in other potentially hazardous activities.

Drug Interactions

With simultaneous use with vasodilators, ACE inhibitors, calcium channel blockers, beta-blockers, diuretics, tricyclic antidepressants, MAO inhibitors, ethanol, ethanol-containing drugs, it is possible to enhance the hypotensive effect of glyceryl trinitrate.

With simultaneous use with beta-blockers, calcium channel blockers, the antianginal effect is enhanced.

With simultaneous use with sympathomimetics, a decrease in the antianginal effect of glyceryl trinitrate is possible, which, in turn, can reduce the pressor effect of sympathomimetics (as a result, arterial hypotension is possible).

With simultaneous use of agents with anticholinergic activity (including tricyclic antidepressants, disopyramide), hyposalivation, dry mouth develops.

There is limited data that acetylsalicylic acid, used as an analgesic, increases the concentration of nitroglycerin (glyceryl trinitrate) in blood plasma. This may be accompanied by an increase in the hypotensive effect and headaches.

In a number of studies, a decrease in the vasodilating effect of nitroglycerin (glyceryl trinitrate) was observed against the background of long-term therapy with acetylsalicylic acid.

It is believed that an enhancement of the antiplatelet effect of acetylsalicylic acid is possible against the background of the use of nitroglycerin (glyceryl trinitrate).

With simultaneous use with nitroglycerin, the action of acetylcholine, histamine, and norepinephrine decreases.

Against the background of intravenous administration of nitroglycerin, a decrease in the anticoagulant effect of heparin is possible.

With simultaneous use, an increase in the bioavailability of dihydroergotamine and a decrease in the antianginal effect of nitroglycerin (glyceryl trinitrate) are possible.

With simultaneous use with procainamide, an increase in the hypotensive effect and the development of collapse are possible.

With simultaneous use with rizatriptan, sumatriptan, the risk of coronary artery spasm increases; with sildenafil – the risk of severe arterial hypotension and myocardial infarction; with quinidine – orthostatic collapse is possible; with ethanol – sharp weakness and dizziness.

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

Over-the-Counter

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.