Dosing & Uses
Dosage Forms & Strengths
ointment
- 2%
Angina Pectoris (Long-Term Prophylaxis)
0.5-2 inches applied in am and 6 hours later to truncal skin
Congestive Heart Failure
1.5 inches, increase by 0.5-1 inch up to 4 inches, q4hr
Safety and efficacy not established
Interactions
Interaction Checker
No Results

Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor

Adverse Effects
Frequency Not Defined
Headache
Hypotension
Tachycardia
Dizziness
Lightheadedness
Blurred vision
Flushing
Nausea/vomiting
Nervousness
Xerostomia
Topical allergic reactions
Serious
- Methemoglobinemia (rare)
- Syncope
- Prolonged bleeding time
- Exfoliative dermatitis
- Unstable angina
- Rebound hypertension
- Thrombocytopenia
Warnings
Contraindications
Hypersensitivity to organic nitrates
Recent use (within several days) of PDE-5 inhibitors (eg, avanafil, sildenafil, tadalafil, or vardenafil)
Riociguat; coadministration may cause hypotension
Cautions
Use caution in alcohol use, increased ICP (head trauma, cerebral hemorrhage-potential contraindication), hyperthyroidism, hypertrophic cardiomyopathy, increased IOP, hypotension, volume depletion, or low systolic BP
Do not change brands unintentionally as not all are bioequivalent
Treat drug-induced headache with aspirin or acetaminophen
Provide nitrate-free interval (10-12 hr or overnight) to avoid development of tolerance
Discontinue if blurred vision develops
Do not apply with fingers; do not rub or massage
Use supportive treatment in overdose
Amplification of vasodilatory effects of nitroglycerin by sildenafil can result in severe hypotension; time course and dose dependence of this interaction not studied; appropriate supportive care has not been studied, but seems reasonable to treat this as a nitrate overdose, with elevation of extremities and with central volume expansion
Benefits of transdermal nitroglycerin in patients with acute myocardial infarction or congestive heart failure not established; if one elects to use nitroglycerin in these conditions, use careful clinical or hemodynamic monitoring to avoid hazards of hypotension and tachycardia
Severe hypotension, particularly with upright posture, may occur with even small doses; use drug with caution in patients who may be volume depleted or who, for whatever reason, are already hypotensive; hypotension induced by therapy may be accompanied by paradoxical bradycardia and increased angina pectoris
Nitrate therapy may aggravate angina caused by hypertrophic cardiomyopathy
Effect of therapy on exercise tolerance, although still observable, may become somewhat blunted; in industrial workers who have had long-term exposure to unknown (presumably high) doses of organic nitrates, tolerance clearly occurs; chest pains, acute myocardial infarction, and even sudden death have occurred during temporary withdrawal of nitrates from these workers, demonstrating existence of true physical dependence
During nitrate-free intervals in some clinical trials, anginal attacks have been more easily provoked than before treatment, and patients have demonstrated hemodynamic rebound and decreased exercise tolerance; importance of these observations to routine, clinical use of transdermal nitroglycerin not known
Pregnancy & Lactation
Pregnancy Category: C
Lactation: not known whether the drug crosses into breast milk, use caution
Pregnancy Categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk. C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done. D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk. X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist. NA: Information not available.Pharmacology
Mechanism of Action
Organic nitrate which causes systemic venodilation, decreasing preload
Cellular mechanism: nitrate enters vascular smooth muscle and converted to nitric oxide (NO) leading to activation of cGMP & vasodilation
Relaxes smooth muscle via dose-dependent dilation of arterial and venous beds to reduce both preload and afterload, and myocardial O2 demand
Also improves coronary collateral circulation
Lower BP, increase HR, occasional paradoxical bradycardia
Pharmacokinetics
Half-Life elimination: 1-4 min
Antianginal effects: 30 min
Hemodynamic effects: Within 1 hr
Duration antianginal effects: Up to 7 hr (topical)
Hemodynamic effects: 3-6 hr
Peak Plasma Time: 3-4 hr
Protein Bound: 60%
Vd: 3 L/kg
Metabolism: Mainly in liver, extrahepatic sites: vascular wall, RBC
Metabolites: 1,3-glyceryl dinitrate, 1,2-glyceryl dinitrate, and glyceryl mononitrate (inactive)
Clearance: 5.5-11 L/min
Excretion: Urine
Dialyzable: No
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Patient Handout
Formulary
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