nitroglycerin topical (Rx)

Brand and Other Names:Nitrol, Nitro Bid, more...NitroBid Topical, glyceryl trinitrate topical, Topical Nitroglycerin
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Dosing & Uses

AdultPediatric

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

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Interactions

Interaction Checker

and nitroglycerin topical

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      Serious - Use Alternative

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            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
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            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

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            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.

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            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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            Formulary

            FormularyPatient Discounts

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            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
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            Medscape prescription drug monographs are based on FDA-approved labeling information, unless otherwise noted, combined with additional data derived from primary medical literature.