nitroglycerin rectal (Rx)

Brand and Other Names:Rectiv
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Dosing & Uses

AdultPediatricGeriatric

Dosage Forms & Strengths

ointment, intra-anal

  • 0.4% (4mg nitroglycerin/1g of ointment)

Chronic Rectal Fissure Pain

Indicated for treatment of moderate-to-severe pain associated with chronic anal fissures; consider use if conservative treatment for acute symptoms of anal fissure fails

Cover finger with plastic-wrap, disposable surgical glove or a finger cot and measure 1-inch (375 mg of ointment equivalent to 1.5 mg of nitroglycerin) length of ointment using dosing line provided with packaging

The covered finger is then gently inserted into the anal canal no further than to the first finger joint and applied circumferentially to the anal canal

If this cannot be achieved due to pain, application of the ointment should be made directly to the outside of the anus

May be applied intra-anally q12h until pain abates, not to exceed treatment duration of 3 weeks

Storage

Do not store above 25°C

Do not freeze

Keep the tube tightly closed

Safety and efficacy not established

Clinical studies did not include sufficient numbers of individuals aged 65 yr or older to determine whether they respond differently from younger individuals

Clinical data from the published literature indicate that the elderly demonstrate increased sensitivity to nitrates, which may be therapeutic but also manifest by more frequent or severe hypotension and related dizziness or fainting

Increased sensitivity may reflect the greater frequency of decreased hepatic, renal, or cardiac function, and of concomitant disease or other drug therapy common in elderly individuals

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Interactions

Interaction Checker

and nitroglycerin rectal

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            Contraindicated (4)

            • avanafil

              avanafil increases effects of nitroglycerin rectal by additive vasodilation. Contraindicated. Use of nitroglycerin within a few days of PDE5 inhibitors is contraindicated. PDE5 inhibitors have been shown to potentiate the hypotensive effects of organic nitrates.

            • sildenafil

              sildenafil increases effects of nitroglycerin rectal by additive vasodilation. Contraindicated. Use of nitroglycerin within a few days of PDE5 inhibitors is contraindicated. PDE5 inhibitors have been shown to potentiate the hypotensive effects of organic nitrates.

            • tadalafil

              tadalafil increases effects of nitroglycerin rectal by additive vasodilation. Contraindicated. Use of nitroglycerin within a few days of PDE5 inhibitors is contraindicated. PDE5 inhibitors have been shown to potentiate the hypotensive effects of organic nitrates.

            • vardenafil

              vardenafil increases effects of nitroglycerin rectal by additive vasodilation. Contraindicated. Use of nitroglycerin within a few days of PDE5 inhibitors is contraindicated. PDE5 inhibitors have been shown to potentiate the hypotensive effects of organic nitrates.

            Serious - Use Alternative (0)

              Monitor Closely (87)

              • acebutolol

                nitroglycerin rectal, acebutolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • acetazolamide

                nitroglycerin rectal, acetazolamide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • aldesleukin

                nitroglycerin rectal, aldesleukin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • alfuzosin

                nitroglycerin rectal, alfuzosin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • aliskiren

                nitroglycerin rectal, aliskiren. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • alteplase

                nitroglycerin rectal decreases effects of alteplase by Other (see comment). Use Caution/Monitor. Comment: Caution should be observed in patients receiving nitroglycerin during t-PA therapy. IV administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. .

              • amiloride

                nitroglycerin rectal, amiloride. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • amlodipine

                nitroglycerin rectal, amlodipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • amyl nitrite

                nitroglycerin rectal, amyl nitrite. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • aspirin

                aspirin will increase the level or effect of nitroglycerin rectal by Other (see comment). Use Caution/Monitor. The pharmacological effects of nitroglycerin may be enhanced by concomitant administration of aspirin.

              • aspirin/citric acid/sodium bicarbonate

                aspirin/citric acid/sodium bicarbonate will increase the level or effect of nitroglycerin rectal by Other (see comment). Use Caution/Monitor. The pharmacological effects of nitroglycerin may be enhanced by concomitant administration of aspirin.

              • atenolol

                nitroglycerin rectal, atenolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • azilsartan

                nitroglycerin rectal, azilsartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • benazepril

                nitroglycerin rectal, benazepril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • betaxolol

                nitroglycerin rectal, betaxolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • bisoprolol

                nitroglycerin rectal, bisoprolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • brimonidine

                nitroglycerin rectal, brimonidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • bumetanide

                nitroglycerin rectal, bumetanide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • candesartan

                nitroglycerin rectal, candesartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • captopril

                nitroglycerin rectal, captopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • carvedilol

                nitroglycerin rectal, carvedilol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • chlorothiazide

                nitroglycerin rectal, chlorothiazide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • chlorthalidone

                nitroglycerin rectal, chlorthalidone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • clevidipine

                nitroglycerin rectal, clevidipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • clonidine

                nitroglycerin rectal, clonidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • dapsone topical

                nitroglycerin rectal increases toxicity of dapsone topical by altering metabolism. Modify Therapy/Monitor Closely. May induce methemoglobinemia.

              • dihydroergotamine

                nitroglycerin rectal will increase the level or effect of dihydroergotamine by Other (see comment). Use Caution/Monitor. Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and consequently increases its oral bioavailability. Ergotamine is known to precipitate angina pectoris. Therefore the possibility of ergotism in patients receiving nitroglycerin should be considered.

              • dihydroergotamine intranasal

                nitroglycerin rectal will increase the level or effect of dihydroergotamine intranasal by Other (see comment). Use Caution/Monitor. Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and consequently increases its oral bioavailability. Ergotamine is known to precipitate angina pectoris. Therefore the possibility of ergotism in patients receiving nitroglycerin should be considered.

              • diltiazem

                nitroglycerin rectal, diltiazem. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • doxazosin

                nitroglycerin rectal, doxazosin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • enalapril

                nitroglycerin rectal, enalapril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • eplerenone

                nitroglycerin rectal, eplerenone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • eprosartan

                nitroglycerin rectal, eprosartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • ergotamine

                nitroglycerin rectal will increase the level or effect of ergotamine by Other (see comment). Use Caution/Monitor. Oral administration of nitroglycerin markedly decreases the first-pass metabolism of dihydroergotamine and consequently increases its oral bioavailability. Ergotamine is known to precipitate angina pectoris. Therefore the possibility of ergotism in patients receiving nitroglycerin should be considered.

              • esmolol

                nitroglycerin rectal, esmolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • ethacrynic acid

                nitroglycerin rectal, ethacrynic acid. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • ethanol

                ethanol increases effects of nitroglycerin rectal by Other (see comment). Use Caution/Monitor. Comment: Vasodilating effects of nitroglycerin have been shown to be additive to the effects observed with alcohol. Avoid alcohol assumption.

              • felodipine

                nitroglycerin rectal, felodipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • fosinopril

                nitroglycerin rectal, fosinopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • furosemide

                nitroglycerin rectal, furosemide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • guanfacine

                nitroglycerin rectal, guanfacine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • heparin

                nitroglycerin rectal decreases effects of heparin by Other (see comment). Use Caution/Monitor. Comment: Although an interaction has been reported between IV heparin and nitroglycerin (resulting in a decrease in anticoagulant effect of heparin), the data are not consistent. If patients are to receive IV heparin and nitroglycerin concurrently, the anticoagulation status of the patient must be checked.

              • hydralazine

                nitroglycerin rectal, hydralazine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • hydrochlorothiazide

                nitroglycerin rectal, hydrochlorothiazide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • indapamide

                nitroglycerin rectal, indapamide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • irbesartan

                nitroglycerin rectal, irbesartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • isosorbide dinitrate

                nitroglycerin rectal, isosorbide dinitrate. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • isosorbide mononitrate

                nitroglycerin rectal, isosorbide mononitrate. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • isradipine

                nitroglycerin rectal, isradipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • labetalol

                nitroglycerin rectal, labetalol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • lisinopril

                nitroglycerin rectal, lisinopril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • losartan

                nitroglycerin rectal, losartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • mannitol

                nitroglycerin rectal, mannitol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • metolazone

                nitroglycerin rectal, metolazone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • metoprolol

                nitroglycerin rectal, metoprolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • minoxidil

                nitroglycerin rectal, minoxidil. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • moexipril

                nitroglycerin rectal, moexipril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • nadolol

                nitroglycerin rectal, nadolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • nebivolol

                nitroglycerin rectal, nebivolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • nicardipine

                nitroglycerin rectal, nicardipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • nifedipine

                nitroglycerin rectal, nifedipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • nimodipine

                nitroglycerin rectal, nimodipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • nisoldipine

                nitroglycerin rectal, nisoldipine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              • nitroprusside sodium

                nitroglycerin rectal, nitroprusside sodium. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • olmesartan

                nitroglycerin rectal, olmesartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • papaverine

                nitroglycerin rectal, papaverine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • penbutolol

                nitroglycerin rectal, penbutolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • pindolol

                nitroglycerin rectal, pindolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • prazosin

                nitroglycerin rectal, prazosin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • propranolol

                nitroglycerin rectal, propranolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • quinapril

                nitroglycerin rectal, quinapril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • ramipril

                nitroglycerin rectal, ramipril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • reteplase

                nitroglycerin rectal decreases effects of reteplase by Other (see comment). Use Caution/Monitor. Comment: Caution should be observed in patients receiving nitroglycerin during t-PA therapy. IV administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. .

              • sacubitril/valsartan

                nitroglycerin rectal, sacubitril/valsartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • silodosin

                nitroglycerin rectal, silodosin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • sotalol

                nitroglycerin rectal, sotalol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • spironolactone

                nitroglycerin rectal, spironolactone. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • telmisartan

                nitroglycerin rectal, telmisartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • tenecteplase

                nitroglycerin rectal decreases effects of tenecteplase by Other (see comment). Use Caution/Monitor. Comment: Caution should be observed in patients receiving nitroglycerin during t-PA therapy. IV administration of nitroglycerin decreases the thrombolytic effect of tissue-type plasminogen activator (t-PA). Plasma levels of t-PA are reduced when coadministered with nitroglycerin. .

              • terazosin

                nitroglycerin rectal, terazosin. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • timolol

                nitroglycerin rectal, timolol. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects. If beta-blockers are used with nitroglycerin in patients with angina pectoris, additional hypotensive effects may occur.

              • tizanidine

                nitroglycerin rectal, tizanidine. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • torsemide

                nitroglycerin rectal, torsemide. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • trandolapril

                nitroglycerin rectal, trandolapril. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • triamterene

                nitroglycerin rectal, triamterene. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • valsartan

                nitroglycerin rectal, valsartan. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Observe for possible additive hypotensive effects during concomitant use. .

              • verapamil

                nitroglycerin rectal, verapamil. Either increases effects of the other by pharmacodynamic synergism. Use Caution/Monitor. Marked orthostatic hypotension has been reported when calcium channel blockers and organic nitrates were used concomitantly. Observe for possible additive hypotensive effects during concomitant use. .

              Minor (2)

              • acetylcysteine

                acetylcysteine increases effects of nitroglycerin rectal by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

              • acetylcysteine (Antidote)

                acetylcysteine (Antidote) increases effects of nitroglycerin rectal by Other (see comment). Minor/Significance Unknown. Comment: Acetylcysteine may enhance vasodilatory effects of nitroglycerin.

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              Adverse Effects

              Frequency Not Defined

              Headache

              Dizziness

              Lightheadedness

              Nausea

              Vomiting

              Hypotension, including orthostatic hypotension

              Allergic reactions, flushing, and application site reactions (including drug rash and exfoliative dermatitis)

              Methemoglobinemia may occur with organic nitrates, particularly in the setting of overdose

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              Warnings

              Contraindications

              Hypersensitivity to nitroglycerin or to any of the excipients or idiosyncratic reactions to other organic nitrates

              Patients using a selective inhibitor of cyclicguanosine monophosphate (cGMP)-specific phosphodiesterase type 5 (PDE5), such as sildenafil,vardenafil, and tadalafil

              Increased intracranial pressure (eg, head trauma, cerebral hemorrhage) or inadequate cerebral circulation

              Severe anemia

              Cautions

              Use within a few days of selective PDE-5 inhibitors (eg, sildenafil, tadalafil, vardenafil) contraindicated; may potentiate hypotensive effects of organic nitrates; the time course of the interaction appears to be related to the PDE-5 inhibitor half-life

              Caution with existing cardiovascular disorders; venous and arterial dilatation may occur and decrease venous blood return to the heart and reduce arterial vascular resistance and systolic pressure

              Caution with blood volume depletion, existing hypotension, cardiomyopathies, CHF, acute MI, or poor cardiac function for other reasons

              Nitroglycerin produces dose-related headaches which may be severe; tolerance to headaches occurs

              Additive hypotensive effects may occur when coadministration with nitric oxide (NO) donors (eg, long-acting nitroglycerin, isosorbide dinitrate, isosorbide mononitrate, amyl nitrite, butyl nitrite), antihypertensive drugs, beta-adrenergic blockers, and calcium channel blockers

              Beta-blockers blunt the reflex tachycardia produced by nitroglycerin without preventing its hypotensive effects

              Coadministration with aspirin may increase nitroglycerin maximum serum concentration and AUC

              Alcohol may enhance nitroglycerin’s vasodilating effects

              Avoid use in patients with hypertrophic cardiomyopathy

              Caution when coadministration with t-PA, heparin, and ergotamine

              May precipidate or aggravate intracranial pressure

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              Pregnancy & Lactation

              Pregnancy Category: C

              Lactation: Unknown whether distributed in 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; nitric oxide released from nitroglycerin elicits internal anal sphincter relaxation; reduces sphincter tone and resting intra-anal pressure

              The smooth muscle relaxation is a result of guanylate cyclase activation and resulting increased cyclic GMP in smooth muscle and other tissues causing myosin dephosphorylation; this ultimately results in vasodilatation

              Hypertonicity of the internal but not the external anal sphincter is a predisposing factor in the formation of anal fissures and associated spasm; hypertonicity of the IAS may thereby decrease blood flow and cause ischemia to this region

              Absorption

              Bioavailability: 50% (with application of 0.75 mg dose of 0.2% ointment)

              Distribution

              Protein Bound: 60% (IV)

              Vd: 3 L/kg (IV)

              Metabolism

              Metabolized by liver reductase enzyme to glycerol di- and mononitrate metabolites and ultimately to glycerol and organic nitrate; extrahepatic metabolism include red blood cells and vascular walls

              Enzyme substrate, inhibitor, inducer Metabolites: Inorganic nitrate and 1,2 and 1,3-dinitroglycerols (partially active); the dinitrates are further metabolized to nonvasoactive mononitrates and ultimately to glycerol and carbon dioxide

              Elimination

              Half-life (mean): 2-3 minutes

              Total body clearance: 13.6 L;/min

              Metabolism is primary route of drug elimination

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              Patient Handout

              A Patient Handout is not currently available for this monograph.
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              Formulary

              FormularyPatient Discounts

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              The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

              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.
              ST Step Therapy
              Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
              OR Other Restrictions
              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.