Nitrosol SR 2.6MG Tablet

Nitrosol SR is indicated for acute relief of an attack or prophylaxis of angina pectoris due to coronary artery disease.

Nitrosol SR, an organic nitrate, is a vasodilator which has effects on both arteries and veins. This is a metered dose spray containing Nitrosol SR. Nitrosol SR delivers Nitrosol SR (400 mcg per spray, 200 metered sprays) in the form of spray droplets under the tongue.

The principal pharmacological action of nitroglycerin is relaxation of vascular smooth muscle, producing a vasodilator effect on both peripheral arteries and veins with more prominent effects on the latter. Dilation of the post-capillary vessels, including large veins, promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular enddiastolic pressure (pre-load). Arteriolar relaxation reduces systemic vascular resistance and arterial pressure (after-load).

Nitroglycerin forms free radical nitric oxide (NO), which activates guanylate cyclase, resulting in an increase of guanosine 3’5’-monophosphate (cyclic GMP) in smooth muscle and other tissues. This eventually leads to dephosphorylation of myosin light chains, which regulates thecontractile state in smooth muscle and results in vasodilation.

Absorption: Nitroglycerin is rapidly absorbed and is often used in emergency situations for this reason.

Distribution: The volume of distribution of Nitroglycerin is 3 L/kg.

Metabolism: Nitroglycerin is rapidly metabolized in the liver by hepatic enzymes to di-nitrates and mononitrates.

Elimination: Nitroglycerin is excreted by the renal route, primarily as the 2 di-nitro-metabolites.

Sublingual tablet: One tablet (0.5 mg) should be dissolved under the tongue at the first sign of an acute anginal attack. The dose may be repeated approximately every five minutes, until relief is obtained. If the pain persists after a total of 3 tablets in a 15-minute period, prompt medical attention is recommended.

Sustained release tablet: Dosage should always to be adjusted according to the requirement and response obtained by the individual patient and the severity of the anginal pain.

• 2.6 mg: 1 tablet 2 times a day before meal (in the morning, at noon). If necessary the doses may be raised gradually 2 or 3 tablets 2 times daily.
• 6.4 mg: One tablet twice daily. Or as directed by the registered physician

Spray: At the onset of an attack, one metered dose spray or two metered dose sprays should be administered under the tongue. A spray may be repeated approximately every 5 minutes as needed. Maximum of 3 metered sprays are recommended within a 15-minute period. If chest pain persists after a total of 3 sprays, prompt medical attention is recommended. May be used prophylactically 5 minutes to 10 minutes before engaging in activities that might precipitate an acute attack

Priming of Nitroglycerin Spray: Before you use Nitroglycerin Spray for the first time, you must prime it. To prime your Nitroglycerin Spray, follow the below steps:

1. Remove the plastic cap from the container.
2. Hold the container upright and facing away from yourself and others. Press down on the
3. top of the grooved button 5 times.
4. Your Nitroglycerin Spray is now primed. You are ready to take your first dose.
5. If you do not use your Nitroglycerin Spray withi 6 weeks, you will need to prime it again by pressing down on the top of the groove button 1 time.
6. If you do not use your Nitroglycerin Spray within 3 months, you will need to re-prime it by pressing down on the top of the grooved button up to 5 times.

Giving a dose of Nitroglycerin Spray:

1. It is best to use Nitroglycerin Spray while you are resting and in a sitting position.
2. Hold your Nitroglycerin Spray container upright with your index finger on top of the grooved button.
3. Open your mouth and bring the Nitroglycerin Spray container as close to your mouth as possible.
4. Press down on the top of the grooved button firmly with your index finger to release the spray under your tongue. (See Figure C). The grooved button can help you make sure the canister is turned to the correct position if you are administering the spray in the dark.
5. Release the grooved button and close your mouth right away. Avoid swallowing right after using Nitroglycerin Spray. Do not spit out Nitroglycerin Spray or rinse your mouth for 5 to 10 minutes after using Nitroglycerin Spray.
6. If a second dose of Nitroglycerin Spray is needed, repeat Steps 3 through 5 above.
7. Replace the plastic cap

Special Instruction:

1. Nitroglycerin Spray is for use under the tongue. Do not inhale Nitroglycerin Spray.
2. You should not use more than 3 sprays of Nitroglycerin Spray within 15 minutes.
3. Get emergency medical help right away if you still have chest pain after using a total of 3 sprays of Nitroglycerin Spray.
4. Do not shake the container of Nitroglycerin Spray.
5. Do not spray Nitroglycerin Spray toward flames.

Patients receiving antihypertensive drugs, beta-adrenergic blockers or phenothiazines and nitrates should be observed for possible additive hypotensive effects. Concomitant use of nitrates and alcohol may cause hypotension. The vasodilatory and hemodynamic effects of Nitrosol SR may be enhanced by concomitant administration of Aspirin.

It is contraindicated for patients who are using PDE5 inhibitors (Sildenafil, Vardenafil & Tadalafil), patients who have severe anemia, increased intracranial pressure, hypersensitivity to it or to other nitrates or nitrites & acute circulatory failure or shock.

Most common adverse reactions are headache, flushing and hypotension.

There is no evidence relating to the safety of nitrates in pregnancy and lactation. Nitrates should be administered to pregnant women and nursing mothers unless considered essential by the physician. It is not known whether Nitroglycerin is excreted in human milk.

Only the smallest dose is required for effective control of the acute anginal attack. Excessive use may lead to
the development of tolerance. Nitrosol SR should be used with caution in patients who may be volume-depleted or are already hypotensive.

Safety and effectiveness of Nitrosol SR in pediatric patients have not been established.

In the event of accidental or deliberate over dosage, toxic effects of Nitrosol SR include vomiting, restlessness, hypotension, cyanosis, methemoglobinemia, tachycardia and syncope.

Nitrates: Coronary vasodilators

Keep out of reach of children. Store in a dry place, below 25°C temperature and protected from light.