Nitroglycerin 0.4 MG Sublingual Tablet

Generic Name: NITROGLYCERIN
Brand Name: NITROGLYCERIN
  • Substance Name(s):
  • NITROGLYCERIN

WARNINGS

The benefits of sublingual nitroglycerin in patients with acute myocardial infarction or congestive heart failure have not been established.

If one elects to use nitroglycerin in these conditions, careful clinical or hemodynamic monitoring must be used because of the possibility of hypotension and tachycardia.

DRUG INTERACTIONS

Drug Interactions Concomitant use of Nitroglycerin with soluble guanylate cyclase stimulators is contraindicated (see CONTRAINDICATIONS ).

Concomitant use of nitrates and alcohol may cause hypotension.

The vasodilatory and hemodynamic effects of nitroglycerin may be enhanced by concomitant administration of aspirin.

Intravenous administration of nitroglycerin decreases the thrombolytic effect of alteplase.

Therefore, caution should be observed in patients receiving sublingual nitroglycerin during alteplase therapy.

Intravenous nitroglycerin reduces the anticoagulant effect of heparin and activated partial thromboplastin times (APTT) should be monitored in patients receiving heparin and intravenous nitroglycerin.

It is not known if this effect occurs following single sublingual nitroglycerin doses.

Tricyclic antidepressants (amitriptyline, desipramine, doxepin, others) and anticholinergic drugs may cause dry mouth and diminished salivary secretions.

This may make dissolution of sublingual nitroglycerin difficult.

Increasing salivation with chewing gum or artificial saliva products may prove useful in aiding dissolution of sublingual nitroglycerin.

Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and subsequently increases its oral bioavailability.

Ergotamine is known to precipitate angina pectoris.

Therefore, patients receiving sublingual nitroglycerin should avoid ergotamine and related drugs or be monitored for symptoms of ergotism if this is not possible.

Administration of nitroglycerin is contraindicated in patients who are using PDE-5 inhibitors (e.g., sildenafil citrate, tadalafil, vardenafil hydrochloride).

These compounds have been shown to potentiate the hypotensive effects of organic nitrates.

A decrease in therapeutic effect of sublingual nitroglycerin may result from use of long-acting nitrates.

OVERDOSAGE

Hemodynamic Effects The effects of nitroglycerin overdose are generally the results of nitroglycerin’s capacity to induce vasodilatation, venous pooling, reduced cardiac output, and hypotension.

These hemodynamic changes may have protean manifestations, including increased intracranial pressure, with any or all of persistent throbbing headache, confusion, and moderate fever; vertigo; palpitations; tachycardia; visual disturbances; nausea and vomiting (possibly with colic and even bloody diarrhea); syncope (especially in the upright posture); dyspnea, later followed by reduced ventilatory effort; diaphoresis, with the skin either flushed or cold and clammy; heart block and bradycardia; paralysis; coma; seizures; and death.

No specific antagonist to the vasodilator effects of nitroglycerin is known, and no intervention has been subject to controlled study as a therapy of nitroglycerin overdose.

Because the hypotension associated with nitroglycerin overdose is the result of venodilatation and arterial hypovolemia, prudent therapy in this situation should be directed toward increase in central fluid volume.

Passive elevation of the patient’s legs may be sufficient, but intravenous infusion of normal saline or similar fluid may also be necessary.

The use of epinephrine or other arterial vasoconstrictors in this setting is likely to do more harm than good.

In patients with renal disease or congestive heart failure, therapy resulting in central volume expansion is not without hazard.

Treatment of nitroglycerin overdose in these patients may be subtle and difficult, and invasive monitoring may be required.

Methemoglobinemia Methemoglobinemia has been rarely reported in association with organic nitrates.

The diagnosis should be suspected in patients who exhibit signs of impaired oxygen delivery despite adequate cardiac output and adequate arterial PO2.

Classically, methemoglobinemic blood is described as chocolate brown, without color change on exposure to air.

If methemoglobinemia is present, intravenous administration of methylene blue, 1 to 2 mg/kg of body weight, may be required.

DESCRIPTION

Nitroglycerin tablets are stabilized sublingual compressed tablets that contain 0.3 mg, 0.4 mg, or 0.6 mg nitroglycerin; as well as lactose monohydrate, NF; glyceryl monostearate, NF; pregelatinized starch, NF; calcium stearate, NF powder; and silicon dioxide, colloidal, NF.

Nitroglycerin, an organic nitrate, is a vasodilating agent.

The chemical name for nitroglycerin is 1, 2, 3 propanetriol trinitrate and the chemical structure is: C3H5N309 Molecular weight: 227.09 Chemical Structure

HOW SUPPLIED

Nitroglycerin tablets are supplied as white, round, flat-faced tablets in 3 strengths (0.3 mg, 0.4 mg, and 0.6 mg) in bottles containing 100 tablets each, with color-coded labels, and in color-coded Patient Convenience Packages of 4 bottles of 25 tablets each.

0.3 mg: Coded “N” on one side and “3” on the other.

NDC 59762-4921-1—Bottle of 100 tablets 0.4 mg: Coded “N” on one side and “4” on the other.

NDC 59762-3304-3—Convenience Package NDC 59762-3304-1—Bottle of 100 tablets 0.6 mg: Coded “N” on one side and “6” on the other.

NDC 59762-0489-1—Bottle of 100 tablets Store at Controlled Room Temperature 20°–25°C (68°–77°F) [see USP].

GERIATRIC USE

Geriatric Use Clinical studies of nitroglycerin tablets did not include sufficient numbers of subjects aged 65 and over to determine whether they respond differently from younger subjects.

Other reported clinical experience has not identified differences in responses between the elderly and younger patients.

In general, dose selection for an elderly patient should be cautious, usually starting at the low end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy.

MECHANISM OF ACTION

Mechanism of Action 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.

These events lead to dephosphorylation of myosin light chains, which regulate the contractile state in smooth muscle, and result in vasodilatation.

INDICATIONS AND USAGE

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

PEDIATRIC USE

Pediatric Use The safety and effectiveness of nitroglycerin in pediatric patients have not been established.

PREGNANCY

Pregnancy Category B Animal reproduction and teratogenicity studies have not been conducted with nitroglycerin sublingual tablets.

However, teratology studies conducted in rats and rabbits with topically applied nitroglycerin ointment at dosages up to 80 mg/kg/day and 240 mg/kg/day, respectively revealed no toxic effects on dams or fetuses.

There are no adequate and well-controlled studies in pregnant women.

Nitroglycerin should be given to a pregnant woman only if clearly needed.

NUSRING MOTHERS

Nursing Mothers It is not known whether nitroglycerin is excreted in human milk.

Because many drugs are excreted in human milk, caution should be exercised when nitroglycerin is administered to a nursing woman.

INFORMATION FOR PATIENTS

Information for Patients Nitroglycerin is a sublingual tablet and should not be chewed, crushed, or swallowed.

If possible, patients should sit down when taking nitroglycerin tablets and should use caution when returning to a standing position.

This eliminates the possibility of falling due to lightheadedness or dizziness.

One tablet should be dissolved under the tongue or in the buccal pouch at the first sign of an acute anginal attack.

The dose may be repeated approximately every 5 minutes, until relief is obtained.

If chest pain persists after a total of 3 tablets in a 15-minute period, or if the pain is different than is typically experienced, prompt medical attention is recommended.

Nitroglycerin may be used prophylactically 5 to 10 minutes prior to engaging in activities that might precipitate an acute attack.

Nitroglycerin may produce a burning or tingling sensation when administered sublingually; however, the ability to produce a burning or tingling sensation should not be considered a reliable method for determining the potency of the tablets.

Headaches can sometimes accompany treatment with nitroglycerin.

In patients who get these headaches, the headaches may be a marker of the activity of the drug.

Treatment with nitroglycerin may be associated with lightheadedness upon standing, especially just after rising from a recumbent or seated position.

This effect may be more frequent in patients who have also consumed alcohol.

Nitroglycerin should be kept in the original glass container and must be tightly capped after each use to prevent loss of tablet potency.

DOSAGE AND ADMINISTRATION

One tablet should be dissolved under the tongue or in the buccal pouch at the first sign of an acute anginal attack.

The dose may be repeated approximately every 5 minutes until relief is obtained.

If the pain persists after a total of 3 tablets in a 15-minute period, or if the pain is different than is typically experienced, prompt medical attention is recommended.

Nitroglycerin tablets may be used prophylactically 5 to 10 minutes prior to engaging in activities that might precipitate an acute attack.

During administration the patient should rest, preferably in the sitting position.

No dosage adjustment is required in patients with renal failure.