Nitrates can be used to prevent chest pain (angina), limit the number of angina attacks that you have, relieve the pain of a current attack, or treat the symptoms of heart failure. Nitroglycerin is a type of nitrate. How does it work?Nitrates are vasodilators, which means they help widen (dilate) your blood vessels, making it easier for blood to flow through and let more oxygen-rich blood reach your heart. Better blood flow means your heart doesn't have to work as hard. Nitrates also relax the veins so less blood is returned to the heart, which can reduce the workload on your heart. How should I take it?There are several different forms of nitrates:
Always talk to your doctor or pharmacist about how and when to take your specific medication. What should I avoid while taking this medicine?You should avoid smoking while you are taking nitrates since it may make them less effective. You should also avoid alcohol, because it may increase the effect of the medicine. What if I am taking other medicines?Nitrates can interact with other medications, so be sure to tell your doctor about any other medications you may be taking including prescription, non-prescription, over-the-counter or natural health products (vitamins and minerals, herbal remedies, homeopathic medicines, traditional medicines such as traditional Chinese medicines, probiotics and other products such as amino acids and essential fatty acids). Some medications that may cause an interaction include:
Speak to your doctor or pharmacist about any other information you may need to know about your medications. What else should I tell my doctor?Always give your doctor your complete medical history, especially if you are over 60 years of age, have recently had a stroke or heart attack or have severe headaches, low iron (anemia) or glaucoma. You may also want to talk to your doctor about how effective nitrates are for managing your angina. Your doctor can adjust the amount of medicine or suggest other ways of managing your condition. What are some side effects?Some common side effects of nitrates include headaches, flushing, dizziness, fainting, low blood pressure (hypotension) and irregular heart rhythms (arrhythmia). Report any and all side effects to your doctor. Lifestyle changesEating a healthy diet that is lower in fat, especially saturated and trans fats, being smoke free, limiting alcohol use, being physically active and reducing stress are also important in lowering the risk of heart disease. Talk to your healthcare practitioner about how you can achieve these lifestyle changes. Related informationHealth Canada - Drugs and Health Products provides health and medical information to help Canadians maintain and improve their health. Learn more about Drug Product Database provides information about drugs approved for use in Canada. MedEffect Canada provides safety alerts, public health advisories, warnings and recalls. Your ministry of health also provides useful health resources in your province or territory. For example, Ontario’s MedsCheck program provides free pharmacist consultations on safety use of drugs. And British Columbia’s Senior Healthcare webpage provides information about important health programs. Drug coverage Summary Nitroglycerin is a nitrate vasodilator used to treat or prevent angina, heart failure, hypertension, and anal fissures. Brand NamesGonitro, Minitran, Mylan-nitro, Nitro-bid, Nitro-dur, Nitroject, Nitrolingual, Nitromist, Nitrostat, Rectiv, Trinipatch Generic NameNitroglycerinDrugBank Accession NumberDB00727BackgroundNitroglycerin, also known as glyceryl trinitrate,2 is an organic nitrate and a vasodilating agent 17 that was first discovered in 1847.9 Originally used to dynamite, its antianginal effects were identified in the late 1860s after it produced headaches in factory workers while workers with angina pectoris or heart failure experienced relief from chest pain.1,3 Its use as a treatment for angina dates back to 1879 and is still used to treat and prevent angina.10 Nitroglycerin causes vasodilation in both arteries and veins.3 Nitroglycerin is used in a variety of different conditions, including angina pectoris due to coronary artery disease,12,14,17,15 peri-operative hypertension, congestive heart failure,11 and chronic anal fissure.16 It is also used to induce intraoperative hypotension.11 TypeSmall MoleculeGroupsApproved, InvestigationalStructure Monoisotopic: 227.002578773 Chemical FormulaC3H5N3O9Synonyms
Sublingual nitroglycerin is indicated for the acute relief of an attack or acute prophylaxis of angina pectoris due to coronary artery disease.12,17,15 Transdermal nitroglycerin is indicated for the prevention of angina pectoris due to coronary artery disease.14 Intravenous nitroglycerin is indicated for the treatment of peri-operative hypertension; for control of congestive heart failure in the setting of acute myocardial infarction; for treatment of angina pectoris in patients who have not responded to sublingual nitroglycerin and beta (β)-blockers; and for induction of intraoperative hypotension.11 Topical nitroglycerin ointment is used to treat moderate to severe pain associated with chronic anal fissure.16 Reduce drug development failure rates Build, train, & validate machine-learning models Build, train, & validate predictive machine-learning models with structured datasets. Associated ConditionsContraindications & Blackbox WarningsAvoid life-threatening adverse drug events Improve clinical decision support with information on contraindications & blackbox warnings, population restrictions, harmful risks, & more. Avoid life-threatening adverse drug events & improve clinical decision support. PharmacodynamicsNitroglycerin causes the relaxation of vascular smooth muscles, causing arteriolar and venous dilatation.17 It increases blood flow to the myocardium and reduces cardiac preload and afterload, decreasing myocardial wall stress and ameliorating anginal symptoms.3,10,12 Nitroglycerin also reduces coronary artery spasm, decreasing systemic vascular resistance as well as systolic and diastolic blood pressure.17 Like other organic nitrates, repeated and prolonged administration of nitroglycerin can lead to the development of tolerance or desensitization of vascular smooth muscle to further nitroglycerin-induced vasorelaxation. This loss of efficacy may be associated with the inhibition of mitochondrial aldehyde dehydrogenase, which is an important enzyme involved in the bioactivation of nitroglycerin.1,2,3 Nitroglycerin tolerance may be accompanied by pro-oxidant effects, endothelial dysfunction, and increased sensitivity to vasoconstrictors.3 Mechanism of actionNitroglycerin is converted by mitochondrial aldehyde dehydrogenase in smooth muscle cells to nitric oxide (NO), a potent vasodilator. NO activates the enzyme guanylate cyclase, which converts guanosine triphosphate (GTP) to cyclic guanosine 3',5'-monophosphate (cGMP) in vascular smooth muscle and other tissues.1,2,10 cGMP is an endogenous vasodilator of vascular smooth muscle:3 it causes protein kinase-dependent phosphorylation and activates downstream cascades that promote relaxation and increased blood flow in veins, arteries and cardiac tissue.3,10 An in vitro study using mouse aorta suggests that nitric oxide, an active metabolite of nitroglycerin, targets the natriuretic peptide receptors.7
Nitroglycerin is rapidly absorbed and is often used in emergency situations for this reason.10 After a sublingual dose of 0.5 mg of nitroglycerin in patients with ischemic heart disease, the peak concentration (Cmax) was 2.56 ng/mL and the mean Tmax was 4.4 minutes.4 The Cmax following a 0.6mg dose of sublingual nitroglycerin was 2.1 ng/mL and the Tmax was 7.2 minutes.17 The absolute bioavailability following sublingual administration was about 40%. The bioavailability of nitroglycerin depends on several factors, such as mucosal metabolism and hydration status, which both affect the absorption of sublingual drugs.17 Volume of distributionThe volume of distribution of nitroglycerin is 3 L/kg.11 Protein bindingAfter a sublingual dose of nitroglycerin, at concentrations in the plasma ranging from 50 to 500 ng/mL, plasma protein binding of nitroglycerin is about 60%. The plasma protein binding of the metabolites 1,2-dinitroglycerin is 60% and that of 1,3-dinitroglycerin is 30%.17 Mitochondrial aldehyde dehydrogenase 2 (ALDH2) promotes the bioactivation of nitroglycerin. Nitroglycerin is metabolized to nitrite; 1,2-glyceryl dinitrate; and 1,3 glyceryl dinitrate.1,8,11 Nitrite is further metabolized to nitric oxide. 1,2- and 1,3-dinitroglycerols are less biologically active than nitroglycerin but they have longer half-lives, which explains some prolonged effects of nitrates. Both dinitrates are finally metabolized to glycerol, carbon dioxide, and mononitrates that do not have vasodilatory actions.6,11 Nitroglycerin can also chemically react with a thiol to generate an intermediate S-nitrosothiol, which resulted in further production of nitric oxide.1,3,8 Hover over products below to view reaction partners Route of eliminationMetabolism is the main route by which nitroglycerin is eliminated from the body.17 Half-lifeFollowing intravenous administration, the plasma half-life is about three minutes.5,11 The estimated plasma half-life following sublingual administration is approximately six minutes.4 The elimination half-lives of metabolites 1,2-dinitroglycerin and 1,3-dinitroglycerin range between 32 to 26 minutes.17 The estimated clearance following intravenous administration is 1 L/kg/min.11 The apparent clearance after a sublingual dose was 21.9 L/min in a pharmacokinetic study of patients with ischemic heart disease and angina.4 Adverse EffectsImprove decision support & research outcomes With structured adverse effects data, including: blackbox warnings, adverse reactions, warning & precautions, & incidence rates. Improve decision support & research outcomes with our structured adverse effects data. ToxicityThe oral LD50 of nitroglycerin in rats is 105 mg/kg and the LD50 of the intravenous form in rats is 23.2 mg/kg.13 Nitrate overdosage can result in following conditions: 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.17 Methemoglobinemia can rarely occur at conventional doses of organic nitrates. This condition is dose-related and it can be even more pronounced in patients with genetic abnormalities of hemoglobin that favor methemoglobin formation. Methemoglobinemia can be managed with the administration of methylene blue unless the patient has a known G-6-PD deficiency.17 There are no known antidotes to an overdose of nitroglycerin, and it is not known whether its metabolites can be removed from the circulation.17,11 Hypotension associated with nitroglycerin overdose can be managed with different symptomatic and supportive measures, including the elevation of the lower limbs, administration of intravenous saline or other fluids to maintain central fluid volume, and administration of oxygen and artificial ventilation. Gastric lavage may be used in case of ingestion of excess nitroglycerin.17 PathwaysNot AvailablePharmacogenomic Effects/ADRs Not AvailableDrug InteractionsThis information should not be interpreted without the help of a healthcare provider. If you believe you are experiencing an interaction, contact a healthcare provider immediately. The absence of an interaction does not necessarily mean no interactions exist.
InChI=1S/C3H5N3O9/c7-4(8)13-1-3(15-6(11)12)2-14-5(9)10/h3H,1-2H2 IUPAC Name1,3-bis(nitrooxy)propan-2-yl nitrate [O-][N+](=O)OCC(CO[N+]([O-])=O)O[N+]([O-])=O Manufacturers
DrugBank does not sell nor buy drugs. Pricing information is supplied for informational purposes only. PatentsKindProteinOrganismHumansPharmacological action No ActionsSubstrate General FunctionElectron carrier activitySpecific FunctionNot AvailableGene NameALDH2Uniprot IDP05091Uniprot NameAldehyde dehydrogenase, mitochondrialMolecular Weight56380.93 Da
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What is the medication nitroglycerin used for?
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