Nitroglycerin: Rapid-Acting Relief for Angina Pectoris
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Nitroglycerin is a cornerstone medication in the management of angina pectoris, a condition characterized by chest pain due to myocardial ischemia. As an organic nitrate, its primary mechanism of action is venous and arterial vasodilation, which reduces cardiac preload and afterload, thereby decreasing myocardial oxygen demand. This vasodilatory effect also improves coronary blood flow by dilating epicardial coronary arteries and collateral vessels. Available in sublingual tablets, sprays, ointments, patches, and intravenous formulations, nitroglycerin offers flexible administration tailored to both acute prophylaxis and long-term therapeutic strategies. Its rapid onset of action, particularly in sublingual forms, makes it an indispensable agent for the immediate relief of anginal attacks and for prophylactic use prior to anticipated physical or emotional exertion.
Features
- Active Ingredient: Glyceryl trinitrate
- Available Formulations: Sublingual tablets, translingual spray, topical ointment, transdermal patches, extended-release capsules, and intravenous solution
- Mechanism of Action: Nitric oxide donor causing venous and arterial vasodilation
- Onset of Action: Sublingual/translingual: 1–3 minutes; Topical: 15–60 minutes; Transdermal: 30–60 minutes
- Duration of Effect: Sublingual: 30–60 minutes; Transdermal: 8–14 hours (with patch-free interval)
- Metabolism: Extensive first-pass metabolism in the liver via glutathione-organic nitrate reductase
- Elimination Half-life: 1–4 minutes
- Prescription Status: Prescription-only medication in most jurisdictions
Benefits
- Provides rapid relief from acute anginal episodes, often within minutes of administration
- Reduces frequency and severity of angina attacks with prophylactic use
- Decreases myocardial oxygen demand through reduction in preload and afterload
- Improves exercise tolerance and quality of life in patients with chronic stable angina
- Offers multiple administration routes for tailored therapeutic approaches
- May be used in acute coronary syndromes under careful hemodynamic monitoring
Common use
Nitroglycerin is primarily indicated for the prevention and treatment of angina pectoris caused by coronary artery disease. In clinical practice, it is used for acute relief of anginal pain, prophylaxis before activities known to provoke angina, and as part of chronic management regimens for stable angina. The sublingual formulation is most commonly employed for immediate relief during acute attacks, while transdermal patches and ointments are typically used for prolonged prophylaxis. In hospital settings, intravenous nitroglycerin is utilized for the management of unstable angina, acute myocardial infarction (particularly with associated hypertension or heart failure), and perioperative hypertension control during cardiac surgery. Off-label uses include the treatment of anal fissures (as topical ointment), Raynaud’s phenomenon, and esophageal spasm, though evidence for these applications varies.
Dosage and direction
Sublingual Tablets: Place 0.3–0.6 mg tablet under the tongue at the first sign of an anginal attack. Dose may be repeated every 5 minutes for up to 3 doses within 15 minutes. If pain persists after 3 doses, seek emergency medical attention.
Translingual Spray: Spray 1–2 metered doses (0.4 mg each) onto or under the tongue. Do not inhale. Repeat every 5 minutes as needed, up to 3 doses within 15 minutes.
Topical Ointment: Apply 1/2 to 2 inches (15–50 mm) of 2% ointment every 8 hours, typically using dose-measuring paper. Spread thinly on clean, dry, hairless skin (usually chest); do not rub in. Rotate application sites.
Transdermal Patches: Apply one patch (0.1–0.8 mg/hour) to clean, dry, hairless skin daily. Remove after 12–14 hours to provide a 10–12 hour nitrate-free interval to prevent tolerance.
Extended-Release Capsules: 2.5–9 mg orally every 8–12 hours, taken on an empty stomach.
Intravenous Administration: Initiate at 5 mcg/min, titrating upward by 5 mcg/min every 3–5 minutes until desired hemodynamic response. Maintenance doses typically range from 10–200 mcg/min.
All patients should receive thorough education on proper administration techniques, especially the importance of sitting down when taking sublingual/translingual doses to prevent orthostatic hypotension.
Precautions
Patients should be advised that nitroglycerin may cause dizziness, lightheadedness, or syncope, particularly upon initiation or dose escalation. These effects are more pronounced when standing quickly from a sitting or lying position. Alcohol consumption may potentiate these effects. Headache is common, especially during initial therapy, and typically diminishes with continued use. Patients should not use phosphodiesterase-5 inhibitors (sildenafil, tadalafil, vardenafil) within 24 hours (48 hours for tadalafil) of nitroglycerin administration due to risk of severe hypotension. Tolerance to the antianginal and hemodynamic effects may develop with continuous exposure; implementing a nitrate-free interval of 10–14 hours daily helps prevent this. Sublingual tablets should be kept in their original glass container and protected from light, moisture, and heat to maintain stability. Patients should replace sublingual tablets every 3-6 months once the bottle is opened to ensure potency.
Contraindications
Nitroglycerin is contraindicated in patients with known hypersensitivity to organic nitrates or any component of the formulation. Absolute contraindications include concurrent use with phosphodiesterase-5 inhibitors due to the risk of profound hypotension. Additional contraindications include severe anemia, increased intracranial pressure (due to potential for further elevation), closed-angle glaucoma (though open-angle glaucoma is not a contraindication), and hypotension (systolic BP <90 mmHg). It is contraindicated in patients with marked bradycardia or tachycardia and in those who have taken recreational drugs known to contain phosphodiesterase inhibitors. Right ventricular infarction represents a relative contraindication due to dependence on preload.
Possible side effect
Common (≥1%): Headache (most frequent, often dose-related), dizziness, lightheadedness, orthostatic hypotension, flushing, nausea, vomiting, syncope (particularly with initial doses), reflex tachycardia.
Less common (<1%): Cutaneous vasodilation with flushing, weakness, palpitations, dry mouth, rash, contact dermatitis (with topical forms), methemoglobinemia (especially with high doses or renal impairment), blurred vision, diaphoresis.
Rare: Severe hypotension leading to cardiovascular collapse, paradoxical bradycardia, exacerbation of angina (particularly with withdrawal), neurological effects including confusion, restlessness, and seizures (typically with overdose situations). Transdermal formulations may cause localized skin reactions including erythema, pruritus, and contact dermatitis.
Drug interaction
Phosphodiesterase-5 inhibitors (sildenafil, tadalafil, vardenafil): Contraindicated combination; may cause severe, potentially fatal hypotension.
Antihypertensive agents: Additive hypotensive effects with calcium channel blockers, beta-blockers, ACE inhibitors, ARBs, diuretics, and other vasodilators.
Alcohol: Potentiates vasodilation and hypotensive effects.
Tricyclic antidepressants, antipsychotics: May enhance hypotensive effects.
Aspirin: May increase nitroglycerin bioavailability.
Heparin: Intravenous nitroglycerin may reduce anticoagulant effect of heparin; monitoring of PTT recommended.
Sympathomimetics: May reduce antianginal efficacy of nitroglycerin.
Dihydroergotamine: Nitroglycerin may enhance the vasoconstrictive effects.
Riociguat: Concomitant use may result in additive hypotensive effects.
Missed dose
For scheduled dosing regimens (ointments, patches, capsules), apply or take the missed dose as soon as remembered unless it is almost time for the next dose. Do not double doses to make up for a missed dose. For sublingual tablets or spray used as needed for acute angina, there is no scheduled dosing, so the “missed dose” concept does not apply. Patients should be instructed to take nitroglycerin at the first sign of angina rather than waiting for pain to become severe. If using prophylactically before anticipated exertion, take approximately 5-10 minutes before activity.
Overdose
Nitroglycerin overdose manifests primarily as vasodilation with severe hypotension, paradoxical bradycardia, syncope, methemoglobinemia, nausea, vomiting, diaphoresis, visual disturbances, flushing, headache, dizziness, and palpitations. Severe overdose may lead to cyanosis, tachypnea, syncope, coma, seizures, and cardiovascular collapse. Treatment is primarily supportive with elevation of legs to promote venous return. Intravenous fluids should be administered cautiously to avoid pulmonary edema. If severe hypotension persists despite positioning and fluids, alpha-adrenergic agonists such as phenylephrine or norepinephrine may be considered. Methylene blue (1-2 mg/kg IV over 5 minutes) is indicated for methemoglobinemia (>30% or symptomatic). Hemodialysis is not effective due to extensive protein binding and rapid metabolism.
Storage
Store at controlled room temperature (20-25°C or 68-77°F). Protect from light, moisture, and heat. Keep sublingual tablets in their original glass container with cotton removed and tightly capped. Do not transfer to other containers. Translingual spray should be kept with the protective cap on when not in use. Transdermal patches should be kept in their protective pouch until use. Do not freeze. Keep all medications out of reach of children and pets. Properly discard expired medication or medication that is no longer needed.
Disclaimer
This information is for educational purposes only and does not constitute medical advice. Individual patient needs may vary. Always consult with a qualified healthcare professional before starting, stopping, or changing any medication regimen. Do not disregard professional medical advice or delay seeking it because of something you have read here. The prescribing physician should be consulted regarding any questions about diagnosis or treatment. In case of emergency, seek immediate medical attention or contact poison control.
Reviews
“After my MI, nitroglycerin has been a lifesaver during angina episodes. The sublingual tablets work within minutes, though the headaches can be intense initially.” - John D., 68
“As a cardiologist, I’ve prescribed nitroglycerin for decades. Its rapid action and multiple formulations make it invaluable for both acute and prophylactic angina management.” - Dr. Eleanor M., Cardiologist
“The transdermal patch system has significantly improved my quality of life with stable angina. The nitrate-free interval prevents tolerance development.” - Margaret T., 72
“Emergency responders rely on nitroglycerin for rapid relief of cardiac chest pain. Its predictable pharmacokinetics make it a cornerstone of pre-hospital care.” - Paramedic, 12 years experience
“While effective, patients need careful education about proper storage and the critical importance of avoiding PDE5 inhibitors. The safety concerns are real and potentially fatal.” - Clinical Pharmacist