A-Z Drug Facts > Nitroglycerin

Nitroglycerin

Pronouncation: (nye-troe-GLIH-suh-rin)
Class: Vasodilator, Nitrate

Trade Names:
Minitran
- Transdermal systems 9 mg
- Transdermal systems 18 mg
- Transdermal systems 36 mg
- Transdermal systems 54 mg

Trade Names:
Nitrek
- Transdermal systems 22.4 mg
- Transdermal systems 44.8 mg
- Transdermal systems 67.2 mg

Trade Names:
Nitro-Bid
- Ointment, topical 2% in a lanolin-petrolatum base

Trade Names:
Nitro-Dur
- Transdermal systems 20 mg
- Transdermal systems 40 mg
- Transdermal systems 60 mg
- Transdermal systems 80 mg
- Transdermal systems 100 mg
- Transdermal systems 120 mg
- Transdermal systems 160 mg

Trade Names:
Nitro-Time
- Capsules, sustained-release 2.5 mg
- Capsules, sustained-release 9 mg

Trade Names:
Nitroglycerin
- IV Injection 5 mg/mL
- Capsules, sustained-release 6.5 mg

Trade Names:
Nitroglycerin in 5% Dextrose
- Injection 100 mcg/mL
- Injection 200 mcg/mL
- Injection 400 mcg/mL

Trade Names:
Nitrolingual
- Aerosol spray, translingual 0.4 mg/metered dose

Trade Names:
NitroQuick
- Tablets, sublingual 0.3 mg
- Tablets, sublingual 0.4 mg
- Tablets, sublingual 0.6 mg

Trade Names:
Nitrostat
- Tablets, sublingual 0.3 mg
- Tablets, sublingual 0.4 mg
- Tablets, sublingual 0.6 mg

Gen-Nitro (Canada)
Nitrolingual Pumpspray (Canada)

Pharmacology

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Relaxation of vascular smooth muscle and dilation of peripheral arteries and veins.

Pharmacokinetics

Absorption

Rapid.

Distribution

Vd is 3 L/kg. Protein binding is approximately 60% (parent); 1,2 dinitroglycerin, 60%; 1,3 dinitroglycerin, 30%.

Metabolism

Primarily metabolized in the liver by nitrate reductase; known sites of extrahepatic metabolism include red blood cells and vascular walls. Metabolized to inorganic nitrate and the active 1,2 and 1,3 dinitroglycerols.

Elimination

Serum t _½ is 3 min and 1 to 8 min (sublingual). Cl is 1 L/kg/min.

Onset

1 to 2 min (IV), 1 to 3 min (sublingual), 1 h (extended-release).

Peak

1 to 4 h (immediate-release tablet), 6 to 7 min (sublingual), 2 h (transdermal).

Duration

3 to 5 min (IV), 30 to 60 min (sublingual), 5 h (extended-release), up to 12 h (topical ointment).

Indications and Usage

Extended-release capsules, ointment, transdermal patch Prevention of angina pectoris caused by coronary artery disease (CAD). IV Treatment of perioperative hypertension; control of CHF in the setting of acute MI; treatment of angina pectoris in patients not responding to sublingual nitroglycerin and beta-blockers; induction of intraoperative hypotension. Lingual spray, sublingual tablets Acute relief of an attack or prophylaxis of angina pectoris caused by CAD.

Unlabeled Uses

IV Management of acute MI; treatment of hypertensive emergencies; in combination with vasopressin to treat variceal bleeding, cocaine-induced acute coronary syndrome; management of Prinzmetal angina occurring in patients without coronary heart disease. Sublingual Management of acute MI; management of Prinzmetal angina occurring in patients without coronary heart disease. Topical Management of acute MI; treatment of Prinzmetal angina occurring in patients without coronary heart disease; treatment of chronic anal fissure pain; erectile dysfunction; Raynaud disease.

Contraindications

IV, lingual spray, sublingual, transdermal Allergy to organic nitrates; patient using phosphodiesterase type 5 inhibitors (eg, sildenafil, tadalafil, vardenafil). IV Pericardia tamponade; restrictive cardiomyopathy, constrictive pericarditis; solutions containing dextrose in patients with known allergy to corn or corn products. Ointment, extended-release Allergy to organic nitrates. Sublingual Early MI; severe anemia; increased intracranial pressure. Transdermal Allergy to adhesives used in transdermal patches.

Dosage and Administration

Angina
Adults

PO 2.5 mg to 6.5 mg (extended-release capsules) 3 to 4 times daily initially, titrate to response. Ensure daily nitroglycerin-free interval of 10 to 12 h. Sublingual 0.3 to 0.6 mg dissolved under the tongue or in buccal pouch at first sign of acute angina attack; repeat every 5 min (do not exceed 3 tablets in 15 min). Also may be used as a single dose 5 to 10 min before activity that might precipitate an anginal attack. Topical Initially, ½-inch dose applied twice daily (upon arising in the morning and 6 h later). May titrate dose up to 2 inches applied twice daily (6 h apart). Transdermal Initially, 0.2 to 0.4 mg/h patch applied once daily; titrate dose to response. Remove patch after 12 to 14 h to provide nitroglycein-free interval. Translingual 1 or 2 sprays onto or under tongue at first sign of acute angina attack; repeat every 5 min (do not exceed 3 sprays in 15 min). Also may be used 5 to 10 min before activity that might precipitate an anginal attack.

Perioperative Hypertension, Induction of Intraoperative Hypotension, Refractory angina, CHF secondary to acute MI
Adults

IV 5 mcg/min initially using non-absorbing infusion set or 25 mcg/min using a polyvinyl chloride (PVC) administration set; titrate to response.

General Advice

• To minimize development of tolerance, ensure daily nitroglycerin-free interval of 10 to 12 h is provided.
• Caution patient not to chew, crush, or open extended-release capsules.
• Caution patient not to crush, chew, or swallow sublingual tablets.
• During administration of sublingual tablets and translingual spray, patient should rest, preferably in the sitting position.

• Translingual spray
• Do not shake container before administering dose.
• Prime aerosol unit initially with 1 spray. Reprime with 1 spray if unit has not been used for 6 or more weeks.
• Hold container upright as close to open mouth as possible; press button firmly to release spray onto or under the tongue; caution patient not to inhale spray. Have patient avoid swallowing immediately after administering spray; do not expectorate or rinse mouth for 5 to 10 min following administration.
• Contains alcohol. Do not spray toward flames.

• Topical ointment
• Measure prescribed dose of ointment using measuring applicator supplied with tube. Squeeze necessary amount of ointment onto applicator and place applicator (ointment side down) on desired area of skin. Spread ointment using dose measuring applicator then tape applicator into place. Do not rub ointment into skin.
• Keep ointment tube tightly wrapped; cover dose measuring applicator with plastic kitchen wrap to prevent staining of clothing by ointment.

• Transdermal systems
• Remove patch from foil pouch immediately prior to application.
• Remove protective liner from patch and apply to any area of the body except the extremities below the knee or elbow; the chest is preferred site. Press the patch on the skin and smooth down.
• Apply only to area that is clean, dry, and hairless. If hair is likely to interfere with patch adherence, clip, do not shave, the area before application.
• Do not apply patch to skin areas with cuts or irritation or immediately after showering or bathing.
• If the patch becomes dislodged, discard it and put a new one on at a different skin site.
• Do not discharge cardioverter/defribrillator through paddle electrode that overlies a transdermal patch. May cause current arching that can damage the paddles and burn the patient.

• Injection
• For IV infusion only. Not for intradermal, subcutaneous, IM, IV bolus, intra-arterial, or intracoronary administration.
• Several preparations of nitroglycerin injection are available. They differ in concentration and/or volume per container. When switching from one product to another, pay attention to the dilution and dosage and administration instructions.
• Nitroglycerin solution for injection is concentrated and must be diluted prior to administration. Transfer contents of 1 vial (25 or 50 mg) into 500 mL glass bottle of dextrose 5% or sodium chloride 0.9% to provide final concentration of 50 mcg/mL or 100 mg/mL. After initial titration, concentration of solution may be increased, if necessary, to a max concentration of 400 mcg/mL to limit fluids given to patient.
• Nitroglycerin in 5% dextrose is premixed and requires no further dilution.
• Use only with glass bottles and non-polyvinyl chloride (PVC) infusions sets provided by manufacturer, or use non-PVC infusion sets.
• Administer only via infusion pump that can maintain constant infusion rate.
• Do not administer if container has lost vacuum or if solution is discolored, cloudy, or contains particulate matter.
• Usual starting dose when using PVC administrations sets is 25 mcg/min. Usual starting dose when using nonabsorptive infusion (non-PVC) set is 5 mcg/min.
• Initial dose (non-PVC set) titration should be in 5 mcg/min increments every 3 to 5 min until some response is observed. If no response occurs at 20 mcg/min, increments of 10 to 20 mcg/min can be used. Once a partial BP response is observed, reduce dose and lengthen interval between dose increases.
• Avoid use of in-line filters that absorb nitroglycerin.
• When changing concentrations, disconnect tubing from patient and flush with new solution before continuing therapy.
• Do not mix nitroglycerin infusions through the same infusion set as blood to avoid pseudoagglutination and hemodialysis.
• Do not mix nitroglycerin solutions with any other medication.

Storage/Stability

Store nitroglycerin for injection at controlled room temperature (59° to 86°F). Protect from freezing and light. Discard any unused solution. Store premixed nitroglycerin with dextrose at room temperature of 77°F (brief exposure up to 104°F does not affect product). Protect from freezing. Avid excessive heat. Store extended-release capsules, translingual spray, topical ointment, and transdermal systems at controlled room temperature (59° to 86°F). Store sublingual tablets at controlled room temperature (68° to 77°F). Protect sublingual tablets from moisture.

Drug Interactions

Alcohol

Severe hypotension and CV collapse may occur.

Alteplase

Concurrent administration decreases thrombolytic effects of alteplase.

Aspirin

Vasodilatory and hemodynamic effects of nitroglycerin may be enhanced.

Calcium channel blockers

Symptomatic orthostatic hypotension may occur.

Dihydroergotamine

May increase systolic BP and decrease antianginal effects.

Heparin

May decrease anticoagulation effect when used in conjunction with IV nitroglycerin.

Phosphodiesterase type 5 inhibitors (eg, sildenafil, tadalafil, vardenafil)

Because the hypotensive effects of nitrates may be potentiated, concomitant use of any form of organic nitrates is contraindicated in patients receiving phosphodiesterase type 5 inhibitors.

Laboratory Test Interactions

May cause false report of reduced serum cholesterol with Zlatkis-Zak color reaction. May cause falsely elevated results of serum triglyceride assays (IV).

Adverse Reactions

Cardiovascular

Crescendo angina, hypotension, palpitations, rebound hypertension, syncope, vasodilation.

CNS

Asthenia, dizziness, headache, light-headedness, paresthesia, restlessness, vertigo, weakness.

Dermatologic

Allergic reactions including contact dermatitis or fixed drug eruptions (ointment or patches), drug rash, exfoliative dermatitis, flushing, perspiration.

EENT

Pharyngitis.

GI

Abdominal pain, burning or tingling in the oral cavity (sublingual), nausea, vomiting.

Hematologic-Lymphatic

Methemoglobinemia.

Local

Application-site irritation (transdermal).

Respiratory

Dyspnea.

Miscellaneous

Collapse, pallor, peripheral edema.

Precautions

Monitor Continuously monitor BP and heart rate while administering IV nitroglycerin; monitor pulmonary capillary wedge pressure when indicated.

Pregnancy

Category C .

Lactation

Undetermined.

Children

Safety and efficacy not established.

Elderly

Make dose selection with caution, usually starting at the lower end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and comorbidity.

Acute MI/Heart failure

Benefits of oral and topical nitroglycerin not established; use with caution and with close clinical and hemodynamic monitoring in these settings to avoid hypotension and tachycardia. Use of extended-release nitroglycerin in these settings is not recommended because effects of nitroglycerin are difficult to terminate rapidly.

Angina

May aggravate angina caused by hypertrophic cardiomyopathy.

Diabetes mellitus

Use nitroglycerin solutions containing dextrose with caution.

Methemoglobinemia

High doses may produce methemoglobinemia, especially in patients with methemoglobin reductase deficiency.

Severe hypotension

Severe hypotension and shock may occur even with small doses, particularly with an upright posture; use with caution in patients who are hypotensive or volume depleted; alcohol accentuates this reaction.

Tolerance

May develop with repeated use for prolonged periods of time; minimize tolerance by ensuring daily nitroglycerin-free intervals of 10 to 12 h are provided.

Overdosage

Symptoms

Air hunger, bloody diarrhea, coma, confusion, death, diaphoresis with either flushed or cold and clammy skin, dyspnea followed later by reduced ventilatory effort, heart block and bradycardia, increased intracranial pressure, methemoglobinemia, moderate fever, nausea, palpitations, paralysis, seizures, syncope, throbbing headache, vertigo, visual disturbances, vomiting.

Patient Information

• Advise patient to carefully review the patient information leaflets and booklets supplied with each product before starting therapy, and to read and check for new information each time the medication is refilled.
• Review with patient and family the signs and symptoms of angina (eg, acute onset of pressure-like chest pain that may radiate down the left arm and/or into the neck or jaw, often associated with sweating and shortness of breath or difficulty breathing).
• Ensure patient using extended-release capsules, topical ointment, or transdermal nitroglycerin to prevent angina attacks has sublingual nitroglycerin tablets or translingual spray available at all times. Ensure patient knows when and how to use sublingual nitroglycerin or translingual spray and what to do if angina pain worsens or fails to respond to sublingual nitroglycerin.
• Caution patient that antianginal effectiveness of nitroglycerin is strongly related to the dosing regimen and not to stop taking or change the dose or frequency of administration unless advised by health care provider.
• Advise patient that headaches are a common adverse reaction of therapy and are also a marker of antianginal effectiveness. Advise patient that acetaminophen can be used to relieve headache without reducing the medications antianginal effectiveness. Caution patient not to reduce the dose or change the frequency of administration of isosorbide to avoid medication-induced headache.
• Advise patient to notify health care provider if angina symptoms increase in frequency or severity, or if there is a sudden increase in the frequency of use of sublingual nitroglycerin or translingual spray.
• Caution patient that medication may cause dizziness, light-headedness, or fainting, especially while standing or following consumption of alcohol.
• Caution patient to avoid sudden position changes to prevent orthostatic hypotension.
• Instruct patient to notify health care provider if any of the following occur: frequent episodes of dizziness or lightheadedness; fainting; intolerable headache; episodes or sweating, nausea and/or vomiting; any unusual or unexplained feeling or sensation.

• Sublingual tablets
• Instruct patient to carry the tablets with them at all times and to keep the tablets in the original glass container and tightly capped.
• Instruct patient to sit down and dissolve 1 tablet under the tongue or between the cheek and gum at the first sign of an anginal attack. If pain remains, dose may be repeated every 5 min until 3 tablets are taken. Instruct patient to call 911 if pain becomes more intense or persists after a total of 3 tablets.
• Caution patient not to crush, chew, or swallow sublingual tablets.
• Instruct patient to lie down if dizziness or lightheadedness occurs.
• Advise patient that tablets may produce a burning or tingling sensation but that the ability to cause burning or tingling is not considered a reliable method for determining potency of the tablets.
• Advise patient to discontinue nitroglycerin and notify health care provider if vision blurring or dry mouth occurs.

• Translingual spray
• Ensure patient knows when and how to use translingual spray: Sit down before using spray. Do not shake container before administering dose. Prime aerosol unit initially with 1 spray. Reprime with 1 spray if unit has not been used for 6 or more weeks. Hold container upright as close to open mouth as possible; press button firmly to release spray onto or under the tongue. Caution patient not to inhale spray. Have patient avoid swallowing immediately after administering spray or expectorating or rinsing the mouth for 5 to 10 min following administration. If pain remains, dose may be repeated every 5 min until 3 sprays are taken. Instruct patient to call 911 if pain becomes more intense or persists after a total of 3 sprays.
• Caution patient that aerosol spray contains alcohol and not to spray toward flames or forcefully open or burn container after use.
• Advise patient to discard aerosol and replace with new unit when end of pump is no longer covered by fluid.

• Transdermal systems
• Ensure patient knows how to use transdermal system: remove patch from foil pouch immediately prior to application and remove protective liner from patch and apply to any area of the body except the extremities below the knee or elbow. Advise patient that the chest is preferred site. Press the patch on the skin and smooth down.
• Advise patient to apply only to area that is clean, dry, and hairless. If hair is likely to interfere with patch adherence, instruct patient to clip, not shave, the area before application.
• Caution patient not to apply patch to skin areas with cuts or irritation, or immediately after showering or bathing.
• Advise patient that if the patch becomes dislodged, discard it and put a new one on at a different skin site.
• Caution patient to remove and discard patch after 12 to 14 h, as instructed by health care provider, to provide nitroglycerin-free interval.

• Topical ointment
• Ensure patient knows how to use topical ointment: measure prescribed dose of ointment using measuring applicator supplied with tube by squeezing necessary amount of ointment onto applicator and placing applicator (ointment side down) on desired area of skin. Spread ointment using dose measuring applicator then tape applicator into place. Caution patient not to rub ointment into skin.
• Advise patient to cover dose-measuring applicator with plastic kitchen wrap to prevent staining of clothing by ointment.
• Instruct patient to remove first applicator 6 h after application and apply a second applicator. Instruct patient to remove second applicator after 6 h to provide nitrate-free dosing interval.

• Extended-release capsules
• Instruct patient using extended-release capsules to swallow whole and not to crush, chew, or open capsules.

• Injection
• Advise patient, family, or caregiver that medication will be prepared and administered by a health care professional in the intensive care center with close monitoring.

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