pharmacopeia
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/api/v1/drug/nitroglycerin

Mechanism of action

Sourced from openFDA

Nitroglycerin forms free radical nitric oxide (NO) which activates guanylate cyclase, resulting in an increase of guanosine 3'5' monophosphate (cyclic GMP) in smooth muscle and other tissues. These events lead to dephosphorylation of myosin light chains, which regulate the contractile state in smooth muscle, and result in vasodilatation.

Guanylate CyclasePhosphodiesterase 5

Indications

Sourced from openFDA
  • Nitroglycerin sublingual tablets are indicated for the acute relief of an attack or acute prophylaxis of angina pectoris due to coronary artery disease. Nitroglycerin sublingual tablets are a nitrate vasodilator indicated for relief of an attack or prophylaxis of angina pectoris due to coronary artery disease.ICD-10: I20.9

Contraindications

Sourced from openFDA
  • • Use of phosphodiesterase type 5 (PDE-5) inhibitors, such as avanafil, sildenafil, tadalafil, or vardenafil, or soluble guanylate cyclase (sGC) stimulators. ( 4.1 , 7.1 ) • Severe anemia ( 4.2 ) • Increased intracranial pressure ( 4.3 ) • Hypersensitivity to nitroglycerin or to other nitrates or nitrites or any excipient ( 4.4 ) • Circulatory failure and shock ( 4.5 ) 4.1 PDE-5-Inhibitors and sGC-Stimulators Do not use nitroglycerin sublingual tablets in patients who are taking PDE-5 Inhibitors, such as avanafil, sildenafil, tadalafil, vardenafil hydrochloride.contraindicated

Dosage & administration

Sourced from openFDA

Administer one tablet under the tongue or in the buccal pouch at the first sign of an acute anginal attack. Allow tablet to dissolve without swallowing. One additional tablet may be administered every 5 minutes until relief is obtained. No more than three tablets are recommended within a 15-minute period. If the pain persists after a total of 3 tablets in a 15-minute period, or if the pain is different than is typically experienced, seek prompt medical attention. Nitroglycerin sublingual tablets may be used prophylactically 5 to 10 minutes prior to engaging in activities that might precipitate an acute attack. For patients with xerostomia, a small sip of water prior to placing the tablet under the tongue may help maintain mucosal hydration and aid dissolution of the tablet. Administer nitroglycerin sublingual tablets at rest, preferably in the sitting position. • At the onset of an attack, administer one tablet under the tongue or buccal pouch. One additional tablet may be administered every 5 minutes as needed. No more than 3 total tablets are recommended within a 15 minute period. ( 2 ) • If chest pain persists after three tablets, seek prompt medical attention. ( 2 ) • May be used prophylactically 5 to 10 minutes prior to engaging in activities that might precipitate an acute attack. ( 2 )

Warnings & precautions

Sourced from openFDA

• Tolerance: Excessive use may lead to tolerance. ( 5.1 ) • Hypotension: Severe hypotension may occur. ( 5.2 ) 5.1 Tolerance Excessive use may lead to the development of tolerance. Only the smallest dose required for effective relief of the acute angina attack should be used. A decrease in therapeutic effect of sublingual nitroglycerin may result from use of long-acting nitrates. 5.2 Hypotension 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, or are already hypotensive. Hypotension induced by nitroglycerin may be accompanied by paradoxical bradycardia and increased angina pectoris. Symptoms of severe hypotension (nausea, vomiting, weakness, pallor, perspiration and collapse/syncope) may occur even with therapeutic doses. 5.3 Hypertrophic Obstructive Cardiomyopathy Nitrate therapy may aggravate the angina caused by hypertrophic cardiomyopathy. 5.4 Headache Nitroglycerin produces dose-related headaches, especially at the start of nitroglycerin therapy, which may be severe and persist but usually subside with continued use.

Adverse reactions

Sourced from openFDA

The following adverse reactions are discussed in more detail elsewhere in the label: • Hypotension [see Warnings and Precautions (5.2) ] • Headache [see Warnings and Precautions (5.4) ] • Hypersensitivity [see Contraindications (4.4) ] Vertigo, dizziness, weakness, palpitation, and other manifestations of postural hypotension may develop occasionally, particularly in erect, immobile patients. Marked sensitivity to the hypotensive effects of nitrates (manifested by nausea, vomiting, weakness, diaphoresis, pallor, and collapse) may occur at therapeutic doses. Syncope due to nitrate vasodilatation has been reported. Flushing, drug rash, and exfoliative dermatitis have been reported in patients receiving nitrate therapy. Most common adverse reactions occurring at a frequency greater than 2% are headache, dizziness and paresthesia. ( 6 ) To report SUSPECTED ADVERSE REACTIONS, contact Viatris at 1-877-446-3679 (1-877-4-INFO-RX) or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.

Use in specific populations

Sourced from openFDA

8.1 Pregnancy Risk Summary Limited published data on the use of nitroglycerin are insufficient to determine a 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 [see Data ] . The estimated background risk of major birth defects and miscarriage for the indicated population is unknown. In the U.S. general population, the estimated background risk of major birth defects and miscarriage in clinically recognized pregnancies is 2-4% and 15-20%, respectively. Data Animal Data No embryotoxic or postnatal development effects were observed with transdermal application in pregnant rabbits and rats at doses up to 80 and 240 mg/kg/day, respectively, at intraperitoneal doses in pregnant rats up to 20 mg/kg/day from gestation day 7-17, and at intravenous doses in pregnant rabbits up to 4 mg/kg/day from gestation day 6-18. 8.2 Lactation Risk Summary Sublingual nitroglycerin has not been studied in lactating women. It is not known if nitroglycerin is present in human milk or if nitroglycerin has effects on milk production. 8.4 Pediatric Use The safety and effectiveness of nitroglycerin in pediatric patients have not been established.

Pharmacokinetics

Sourced from openFDA
Metabolism
Absorption Nitroglycerin is rapidly absorbed following sublingual administration of nitroglycerin sublingual tablets. Mean peak nitroglycerin plasma concentrations occur at a mean time of approximately 6 to 7 minutes postdose (Table 1).

Overdosage

Sourced from openFDA

10.1 Signs and Symptoms, Methemoglobinemia Nitrate overdosage may result in: severe hypotension, persistent throbbing headache, vertigo, palpitation, visual disturbance, flushing and perspiring skin (later becoming cold and cyanotic), nausea and vomiting (possibly with colic and even bloody diarrhea), syncope (especially in the upright posture), methemoglobinemia with cyanosis and anorexia, initial hyperpnea, dyspnea and slow breathing, slow pulse (dicrotic and intermittent), heart block, increased intracranial pressure with cerebral symptoms of confusion and moderate fever, paralysis and coma followed by clonic convulsions, and possibly death due to circulatory collapse. Case reports of clinically significant methemoglobinemia are rare at conventional doses of organic nitrates. The formation of methemoglobin is dose-related and in the case of genetic abnormalities of hemoglobin that favor methemoglobin formation, even conventional doses of organic nitrates could produce harmful concentrations of methemoglobin.

Approval history

Sourced from openFDA
  • May 28, 1981ANDAANDA087355Fougera Pharms Inc
  • Oct 31, 1985NDANDA018705Pohl Boskamp
  • Dec 10, 1985NDANDA020145Uspharma
  • May 24, 1988ANDAANDA072034Am Regent
  • Dec 29, 1989NDANDA019970Baxter Hlthcare
  • Aug 30, 1996ANDAANDA074559Mylan Technologies
  • May 1, 2000NDANDA021134Viatris
  • Jun 21, 2011NDANDA021359Abbvie

FDA shortages

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Reference statistics from the openFDA drug-shortage dataset. For a live view, consult the FDA database directly. Not clinical guidance.

  • Nitroglycerin in Dextrose 5%, Injection, 10 mg/100 mL (NDC 0338-1047-02)Resolved
    Sponsor: Baxter Healthcare
    Updated
  • Nitroglycerin in Dextrose 5%, Injection, 20 mg/100 mL (NDC 0338-1049-02)Resolved
    Sponsor: Baxter Healthcare
    Updated
  • Nitroglycerin in Dextrose 5%, Injection, 40 mg/100 mL (NDC 0338-1051-02)Resolved
    Sponsor: Baxter Healthcare
    Updated
  • Nitroglycerin, Injection, 5 mg/1 mL (NDC 0517-4810-25)Resolved
    Sponsor: American Regent, Inc.
    Updated
  • Rectiv, Ointment, 0.4% (NDC 58914-301-80)To be discontinued
    Sponsor: AbbVie Inc.
    Updated

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
53,035 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea4,2478.0%
  2. 2Pain3,6917.0%
  3. 3Fatigue3,5936.8%
  4. 4Myocardial Infarction3,4116.4%
  5. 5Nausea3,3396.3%
  6. 6Dizziness3,0025.7%
  7. 7Drug Ineffective2,9955.6%
  8. 8Chest Pain2,9775.6%
  9. 9Fall2,9465.6%
  10. 10Diarrhoea2,7475.2%
  11. 11Headache2,6575.0%
  12. 12Renal Failure2,5204.8%
  13. 13Asthenia2,4524.6%
  14. 14Death2,4424.6%
  15. 15Hypotension2,2804.3%

Literature

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Recent PubMed references pinned to Nitroglycerin as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 330 ClinicalTrials.gov registrations naming Nitroglycerin as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Nitroglycerin work?
Nitroglycerin forms free radical nitric oxide (NO) which activates guanylate cyclase, resulting in an increase of guanosine 3'5' monophosphate (cyclic GMP) in smooth muscle and other tissues. These events lead to dephosphorylation of myosin light chains, which regulate the contractile state in smooth muscle, and result in vasodilatation.
What is Nitroglycerin used for?
According to FDA labeling, Nitroglycerin carries indications including: Nitroglycerin sublingual tablets are indicated for the acute relief of an attack or acute prophylaxis of angina pectoris due to coronary artery disease. Nitroglycerin sublingual tablets are a nitrate vasodilator indicated for relief of an attack or prophylaxis of angina pectoris due to coronary artery disease.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Nitroglycerin?
Nitroglycerin is classified as Muscle relaxants, Organic nitrates, Nitrate Vasodilator, Guanylate Cyclase Activators, Nitric Oxide Donors, Phosphodiesterase 5 Inhibitors, Arterial Vasodilation, Decreased Blood Pressure, Decreased Vascular Smooth Muscle Tone, Increased Nitric Oxide Activity, Vasodilation, Venous Vasodilation.
What are the brand names for Nitroglycerin?
Nitroglycerin is marketed under brand names including Gonitro, Nitro-Bid, Nitro-Dur, NitroMist, Nitrolingual, Nitrostat, Rectiv.
What are the contraindications for Nitroglycerin?
Nitroglycerin labeling lists contraindications including: • Use of phosphodiesterase type 5 (PDE-5) inhibitors, such as avanafil, sildenafil, tadalafil, or vardenafil, or soluble guanylate cyclase (sGC) stimulators. ( 4.1 , 7.1 ) • Severe anemia ( 4.2 ) • Increased intracranial pressure ( 4.3 ) • Hypersensitivity to nitroglycerin or to other nitrates or nitrites or any excipient ( 4.4 ) • Circulatory failure and shock ( 4.5 ) 4.1 PDE-5-Inhibitors and sGC-Stimulators Do not use nitroglycerin sublingual tablets in patients who are taking PDE-5 Inhibitors, such as avanafil, sildenafil, tadalafil, vardenafil hydrochloride.. Always consult the full prescribing information and a clinician.
Note. Data for nitroglycerin is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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