Brand and Other Names:Nitrol, Nitro Bid, more...NitroBid Topical, glyceryl trinitrate topical, Topical Nitroglycerin
- Classes: Nitrates, Angina
Dosing & Uses
Dosage Forms & Strengths
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
Serious - Use Alternative
Significant - Monitor Closely
Frequency Not Defined
Topical allergic reactions
- Methemoglobinemia (rare)
- Prolonged bleeding time
- Exfoliative dermatitis
- Unstable angina
- Rebound hypertension
Hypersensitivity to organic nitrates
Recent use (within several days) of PDE-5 inhibitors (eg, avanafil, sildenafil, tadalafil, or vardenafil) may cause dangerously low hypotension; the time course of the interaction appears to be related to the PDE-5 inhibitor half-life
Riociguat; coadministration may cause hypotension
Narrow angle glaucoma (controversial: may not be clinically significant)
Alcohol use, incr ICP (head trauma, cerebral hemorrhage-potential contraindication), hyperthyroidism, hypertrophic cardiomyopathy, increase IOP, hypotension, volume depletion, 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
Pregnancy & Lactation
Pregnancy Category: C
Lactation: not known whether the drug crosses into breast milk, use caution
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.
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
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
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|1||This drug is available at the lowest co-pay. Most commonly, these are generic drugs.|
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|4||This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.|
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