nitroglycerin sublingual (Rx)

Brand and Other Names:Nitrostat, Nitrolingual Pumpspray, more...GoNitro, NitroQuick, glyceryl trinitrate sublingual, Sublingual Nitroglycerin
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

tablet, SL

  • 0.3mg
  • 0.4mg
  • 0.6mg

powder, SL (GoNitro)

  • 0.4mg

Angina Pectoris (Acute Relief)

0.3-0.6 mg SL q5min up to 3 times; use at first sign of angina

Prompt medical attention needed if no relief

Dissolve under tongue or in buccal pouch; do not rinse mouth or spit for 5 minutes after administration

Angina Pectoris (Prophylaxis)

1 tablet SL 5-10 minutes before activities likely to provoke angina attacks

Renal Failure

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

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

Not FDA approved

Angina Pectoris (Acute Relief)

0.3-0.6 mg SL q5min up to 3 times; use at first sign of angina

Prompt medical attention needed if no relief

Dissolve under tongue or in buccal pouch; do not rinse mouth or spit for 5 minutes after adminstration

Angina Pectoris (Prevention)

1 tablet SL 5-10 minutes before activities likely to provoke angina attacks

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Interactions

Interaction Checker

and nitroglycerin sublingual

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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

            Early myocardial infarction, severe anemia, increased intracranial pressure, and known hypersensitivity to nitroglycerin

            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)

            Acute circulatory failure or shock

            Cautions

            Caution in 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

            Severe hypotension, particularly with upright posture, may occur with small doses of nitroglycerin particularly in patients with constrictive pericarditis, aortic or mitral stenosis, patients who may be volume- depleted; symptoms of severe hypotension (nausea, vomiting, weakness, pallor, perspiration and collapse/syncope) may occur even with therapeutic doses

            Inability to relieve chest pain after 3 doses indicates acute MI-rush to ER if possible

            Lack of burning/tingling does not indicate loss of potency

            Store in original container at room temp; protect from moisture

            Discard unused tabs 6 months after bottle opened

            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

            Benefits of sublingual nitroglycerin in patients with acute myocardial infarction or congestive heart failure not established; if one elects to use nitroglycerin in these conditions, careful clinical or hemodynamic monitoring must be used because of possibility of hypotension and tachycardia

            Use smallest dose required for effective relief acute anginal attack; excessive use may lead to development of tolerance

            Sublingual tablets should not be swallowed

            Hypotension induced by nitroglycerin may be accompanied by paradoxical bradycardia and increased angina pectoris

            May aggravate angina caused by hypertrophic cardiomyopathy

            Industrial workers who have had long-term exposure to unknown (presumably high) doses of organic nitrates, tolerance rarely occurs; chest pain, acute myocardial infarction, and even sudden death have occurred during temporary withdrawal of nitrates from these workers, demonstrating existence of true physical dependence

            Discontinue drug if blurring of vision or drying of mouth occurs; excessive dosage of nitroglycerin may produce severe headaches

            Nitroglycerin produces dose-related headaches, especially at start of nitroglycerin therapy, which may be severe and persist but usually subside with continued use

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            Pregnancy & Lactation

            Pregnancy

            Limited published data on use of nitroglycerin are insufficient to determine drug associated risk of major birth defects or miscarriage; in animal reproduction studies, there were no adverse developmental effects when nitroglycerin was administered intravenously to rabbits or intraperitoneally to rats during organogenesis at doses greater than 64-times the human dose

            Lactation

            Sublingual nitroglycerin has not been studied in lactating women; not known if nitroglycerin is present in human milk or if nitroglycerin has effects on milk production

            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: 1-4 min

            Onset: 1-3 min (antianginal and hemodynamic effects)

            Duration of antianginal effects: Up to 30 min

            Duration of hemodynamic effects: Up to 30 min

            Bioavailability: 38.5%

            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, & glyceryl mononitrate (inactive)

            Clearance: 5.5-11 L/min

            Excretion: Urine

            Dialyzable No

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            Images

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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.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
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            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
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            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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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.