nitroglycerin transmucosal (Discontinued)Brand and Other Names:glyceryl trinitrate transmucosal, Nitrogard, more...Transmucosal Nitroglycerin

 
 
 

Dosing & Uses

AdultPediatricGeriatric

Angina Pectoris (Long-Term Prophylaxis)

Initially: 1 mg between lip/gum or cheek/gum q8hr (q5hr during waking hour), then increase to 2 mg q8hr, while awake

Renal Failure

CrCl: 10-50 mg/min: Administer q24-72hr

CrCl<10 mL/min: Administer q72-96hr

Not FDA approved

Angina Pectoris (Long-Term Prophylaxis)

Initially: 1 mg between lip/gum or cheek/gum q8hr (q5hr during waking hour), then increase to 2 mg q8hr, while awake

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Interactions

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    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            Common

            Headache

            Hypotension

            Tachycardia

            Dizziness

            Lightheadedness

            Blurred vision

            Flushing

            N/V

            Nervousness

            Xerostomia

            Serious

            Methemoglobinemia (rare)

            Syncope

            Prolonged bleeding time

            Exfoliative dermatitis

            Unstable angina

            Rebound hypertension

            Thrombocytopenia

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            Warnings

            Contraindications

            Hypersensitivity, acute MI, severe anemia

            Recent (last 24 hr) Sildenafil (Viagra) or other PDE5 inhibitor use: potential for dangerous hypotension

            Severe anemia

            Recent use (last 24 hr) sildenafil (Viagra), tadalafil (Cialis), or vardenafil (Levitra) or other phopsphodiesterase-5 inhibitor: potential for dangerous hypotension

            Narrow angle glaucoma (controversial: May not be clinically significant)

            Cautions

            MI or CHF, alcohol use, increased ICP (eg, head trauma, cerebral hemorrhage; potential contraindication), hyperthyroidism, hypertrophic cardiomyopathy, increased IOP, postural 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

            Controlled release product

            Use supportive treatment in overdose

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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

            Half-Life: 1-4 min

            Onset: 1-2 min

            Duration: upto 5 hr

            Bioavailability: 60-75%

            Protein Bound: 11-60%

            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

            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

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