Dosing & Uses
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
Interactions
Interaction Checker
No Results
Contraindicated
Serious - Use Alternative
Significant - Monitor Closely
Minor
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.
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
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
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.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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