Peringatan Keamanan

The oral LD50 of nitroglycerin in rats is 105 mg/kg and the LD50 of the intravenous form in rats is 23.2 mg/kg.L7105

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.L38369

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.L38369

There are no known antidotes to an overdose of nitroglycerin, and it is not known whether its metabolites can be removed from the circulation.L38369,L7099 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.L38369

Nitroglycerin

DB00727

small molecule approved investigational

Deskripsi

Nitroglycerin, also known as glyceryl trinitrate,A180169 is an organic nitrate and a vasodilating agent L38369 that was first discovered in 1847.A249965 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.A180166,A180172 Its use as a treatment for angina dates back to 1879 and is still used to treat and prevent angina.A249970 Nitroglycerin causes vasodilation in both arteries and veins.A180172

Nitroglycerin is used in a variety of different conditions, including angina pectoris due to coronary artery disease,L7102,L7141,L38369,L42320 peri-operative hypertension, congestive heart failure,L7099 and chronic anal fissure.L42445 It is also used to induce intraoperative hypotension.L7099

Struktur Molekul 2D

Berat 227.0865
Wujud liquid

Peta Jejaring Molekuler
Legenda: ObatTargetGenEnzim(Panah → menunjukkan arah efek / relasi)TransporterCarrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) Following intravenous administration, the plasma half-life is about three minutes.[A180178,L7099] The estimated plasma half-life following sublingual administration is approximately six minutes.[A180175] The elimination half-lives of metabolites 1,2-dinitroglycerin and 1,3-dinitroglycerin range between 32 to 26 minutes.[L38369]
Volume Distribusi The volume of distribution of nitroglycerin is 3 L/kg.[L7099]
Klirens (Clearance) The estimated clearance following intravenous administration is 1 L/kg/min.[L7099] The apparent clearance after a sublingual dose was 21.9 L/min in a pharmacokinetic study of patients with ischemic heart disease and angina.[A180175]

Absorpsi

Nitroglycerin is rapidly absorbed and is often used in emergency situations for this reason.A249970 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.A180175 The Cmax following a 0.6mg dose of sublingual nitroglycerin was 2.1 ng/mL and the Tmax was 7.2 minutes.L38369 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.L38369

Metabolisme

Mitochondrial aldehyde dehydrogenase 2 (ALDH2) promotes the bioactivation of nitroglycerin. Nitroglycerin is metabolized to nitrite; 1,2-glyceryl dinitrate; and 1,3 glyceryl dinitrate.A180166,A180265,L7099 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.A180184,L7099 Nitroglycerin can also chemically react with a thiol to generate an intermediate S-nitrosothiol, which resulted in further production of nitric oxide.A180166,A180172,A180265

Rute Eliminasi

Metabolism is the main route by which nitroglycerin is eliminated from the body.L38369

Interaksi Makanan

1 Data
  • 1. Avoid alcohol. Alcohol can increase the risk of hypotension.

Interaksi Obat

716 Data
Alteplase The serum concentration of Alteplase can be decreased when it is combined with Nitroglycerin.
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Nitroglycerin is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Nitroglycerin is combined with Levodopa.
Risperidone Nitroglycerin may increase the hypotensive activities of Risperidone.
Alfuzosin Alfuzosin may increase the hypotensive activities of Nitroglycerin.
Amifostine Nitroglycerin may increase the hypotensive activities of Amifostine.
Diazoxide Diazoxide may increase the hypotensive activities of Nitroglycerin.
Methylphenidate Methylphenidate may decrease the antihypertensive activities of Nitroglycerin.
Dexmethylphenidate Dexmethylphenidate may decrease the antihypertensive activities of Nitroglycerin.
Obinutuzumab Nitroglycerin may increase the hypotensive activities of Obinutuzumab.
Pentoxifylline Pentoxifylline may increase the hypotensive activities of Nitroglycerin.
Rituximab Nitroglycerin may increase the hypotensive activities of Rituximab.
Desmopressin Desmopressin may decrease the antihypertensive activities of Nitroglycerin.
Cyclosporine Cyclosporine may decrease the antihypertensive activities of Nitroglycerin.
Phentermine Phentermine may decrease the antihypertensive activities of Nitroglycerin.
Midodrine Midodrine may decrease the antihypertensive activities of Nitroglycerin.
Eletriptan Eletriptan may decrease the antihypertensive activities of Nitroglycerin.
Isoetharine Isoetharine may decrease the antihypertensive activities of Nitroglycerin.
Atomoxetine Atomoxetine may decrease the antihypertensive activities of Nitroglycerin.
Etomidate Etomidate may decrease the antihypertensive activities of Nitroglycerin.
Zolmitriptan Zolmitriptan may decrease the antihypertensive activities of Nitroglycerin.
Amitriptyline Amitriptyline may decrease the antihypertensive activities of Nitroglycerin.
Protriptyline Protriptyline may decrease the antihypertensive activities of Nitroglycerin.
Norepinephrine Norepinephrine may decrease the antihypertensive activities of Nitroglycerin.
Mirtazapine Mirtazapine may decrease the antihypertensive activities of Nitroglycerin.
Phenylephrine Phenylephrine may decrease the antihypertensive activities of Nitroglycerin.
Phenylpropanolamine Phenylpropanolamine may decrease the antihypertensive activities of Nitroglycerin.
Promazine Promazine may decrease the antihypertensive activities of Nitroglycerin.
Droperidol Droperidol may decrease the antihypertensive activities of Nitroglycerin.
Buspirone Buspirone may decrease the antihypertensive activities of Nitroglycerin.
Nortriptyline Nortriptyline may decrease the antihypertensive activities of Nitroglycerin.
Amoxapine Amoxapine may decrease the antihypertensive activities of Nitroglycerin.
Doxapram Doxapram may decrease the antihypertensive activities of Nitroglycerin.
Atropine Atropine may decrease the antihypertensive activities of Nitroglycerin.
Metaraminol Metaraminol may decrease the antihypertensive activities of Nitroglycerin.
Trazodone Trazodone may decrease the antihypertensive activities of Nitroglycerin.
Epinephrine Epinephrine may decrease the antihypertensive activities of Nitroglycerin.
Sumatriptan Sumatriptan may decrease the antihypertensive activities of Nitroglycerin.
Methoxamine Methoxamine may decrease the antihypertensive activities of Nitroglycerin.
Trimipramine Trimipramine may decrease the antihypertensive activities of Nitroglycerin.
Propiomazine Propiomazine may decrease the antihypertensive activities of Nitroglycerin.
Alfentanil Alfentanil may decrease the antihypertensive activities of Nitroglycerin.
Fentanyl Fentanyl may decrease the antihypertensive activities of Nitroglycerin.
Orciprenaline Orciprenaline may decrease the antihypertensive activities of Nitroglycerin.
Phenmetrazine Phenmetrazine may decrease the antihypertensive activities of Nitroglycerin.
Trifluoperazine Trifluoperazine may decrease the antihypertensive activities of Nitroglycerin.
Dobutamine Dobutamine may decrease the antihypertensive activities of Nitroglycerin.
Pseudoephedrine Pseudoephedrine may decrease the antihypertensive activities of Nitroglycerin.
Benzphetamine Benzphetamine may decrease the antihypertensive activities of Nitroglycerin.
Ritodrine Ritodrine may decrease the antihypertensive activities of Nitroglycerin.
Terbutaline Terbutaline may decrease the antihypertensive activities of Nitroglycerin.
Flupentixol Flupentixol may decrease the antihypertensive activities of Nitroglycerin.
Bitolterol Bitolterol may decrease the antihypertensive activities of Nitroglycerin.
Quinidine Quinidine may decrease the antihypertensive activities of Nitroglycerin.
Almotriptan Almotriptan may decrease the antihypertensive activities of Nitroglycerin.
Diethylpropion Diethylpropion may decrease the antihypertensive activities of Nitroglycerin.
Salmeterol Salmeterol may decrease the antihypertensive activities of Nitroglycerin.
Naratriptan Naratriptan may decrease the antihypertensive activities of Nitroglycerin.
Rizatriptan Rizatriptan may decrease the antihypertensive activities of Nitroglycerin.
Formoterol Formoterol may decrease the antihypertensive activities of Nitroglycerin.
Dopamine Dopamine may decrease the antihypertensive activities of Nitroglycerin.
Frovatriptan Frovatriptan may decrease the antihypertensive activities of Nitroglycerin.
Albuterol Salbutamol may decrease the antihypertensive activities of Nitroglycerin.
Methoxyflurane Methoxyflurane may decrease the antihypertensive activities of Nitroglycerin.
Isoprenaline Isoprenaline may decrease the antihypertensive activities of Nitroglycerin.
Arbutamine Arbutamine may decrease the antihypertensive activities of Nitroglycerin.
Dutasteride Dutasteride may decrease the antihypertensive activities of Nitroglycerin.
Doxepin Doxepin may decrease the antihypertensive activities of Nitroglycerin.
Nefazodone Nefazodone may decrease the antihypertensive activities of Nitroglycerin.
Desipramine Desipramine may decrease the antihypertensive activities of Nitroglycerin.
Propafenone Propafenone may decrease the antihypertensive activities of Nitroglycerin.
Finasteride Finasteride may decrease the antihypertensive activities of Nitroglycerin.
Lisdexamfetamine Lisdexamfetamine may decrease the antihypertensive activities of Nitroglycerin.
Paliperidone Paliperidone may decrease the antihypertensive activities of Nitroglycerin.
Arformoterol Arformoterol may decrease the antihypertensive activities of Nitroglycerin.
Fenoterol Fenoterol may decrease the antihypertensive activities of Nitroglycerin.
Pirbuterol Pirbuterol may decrease the antihypertensive activities of Nitroglycerin.
Ephedra sinica root Ephedra sinica root may decrease the antihypertensive activities of Nitroglycerin.
Ephedrine Ephedrine may decrease the antihypertensive activities of Nitroglycerin.
Mephentermine Mephentermine may decrease the antihypertensive activities of Nitroglycerin.
Procaterol Procaterol may decrease the antihypertensive activities of Nitroglycerin.
Yohimbine Yohimbine may decrease the antihypertensive activities of Nitroglycerin.
Methotrimeprazine Methotrimeprazine may decrease the antihypertensive activities of Nitroglycerin.
Clenbuterol Clenbuterol may decrease the antihypertensive activities of Nitroglycerin.
Bambuterol Bambuterol may decrease the antihypertensive activities of Nitroglycerin.
MMDA MMDA may decrease the antihypertensive activities of Nitroglycerin.
Midomafetamine Midomafetamine may decrease the antihypertensive activities of Nitroglycerin.
2,5-Dimethoxy-4-ethylamphetamine 2,5-Dimethoxy-4-ethylamphetamine may decrease the antihypertensive activities of Nitroglycerin.
4-Methoxyamphetamine 4-Methoxyamphetamine may decrease the antihypertensive activities of Nitroglycerin.
4-Bromo-2,5-dimethoxyamphetamine 4-Bromo-2,5-dimethoxyamphetamine may decrease the antihypertensive activities of Nitroglycerin.
Tenamfetamine Tenamfetamine may decrease the antihypertensive activities of Nitroglycerin.
Chlorphentermine Chlorphentermine may decrease the antihypertensive activities of Nitroglycerin.
Dextroamphetamine Dextroamphetamine may decrease the antihypertensive activities of Nitroglycerin.
Metamfetamine Metamfetamine may decrease the antihypertensive activities of Nitroglycerin.
Phendimetrazine Phendimetrazine may decrease the antihypertensive activities of Nitroglycerin.
Solifenacin Solifenacin may decrease the antihypertensive activities of Nitroglycerin.
Periciazine Periciazine may decrease the antihypertensive activities of Nitroglycerin.
Acepromazine Acepromazine may decrease the antihypertensive activities of Nitroglycerin.
Thioproperazine Thioproperazine may decrease the antihypertensive activities of Nitroglycerin.
Zuclopenthixol Zuclopenthixol may decrease the antihypertensive activities of Nitroglycerin.

Target Protein

Epidermal growth factor receptor EGFR
Guanylate cyclase soluble subunit alpha-1 GUCY1A1
Guanylate cyclase soluble subunit beta-1 GUCY1B1
Atrial natriuretic peptide receptor 1 NPR1

Referensi & Sumber

Synthesis reference: Izhak Blank, "Nitroglycerin preparations." U.S. Patent US4482534, issued December, 1979.
Artikel (PubMed)
  • PMID: 12060725
    Ignarro LJ: After 130 years, the molecular mechanism of action of nitroglycerin is revealed. Proc Natl Acad Sci U S A. 2002 Jun 11;99(12):7816-7. doi: 10.1073/pnas.132271799.
  • PMID: 12048254
    Chen Z, Zhang J, Stamler JS: Identification of the enzymatic mechanism of nitroglycerin bioactivation. Proc Natl Acad Sci U S A. 2002 Jun 11;99(12):8306-11. doi: 10.1073/pnas.122225199. Epub 2002 Jun 4.
  • PMID: 22040938
    Ferreira JC, Mochly-Rosen D: Nitroglycerin use in myocardial infarction patients. Circ J. 2012;76(1):15-21. Epub 2011 Nov 1.
  • PMID: 3125063
    Blagodatskikh SV, Piotrovskii VK, Metelits VI, Riabokon' OS, Martsevich SIu: Pharmacokinetics of glycerin trinitrate (nitroglycerin) after sublingual administration in patients with chronic ischemic heart disease. Farmakol Toksikol. 1987 Nov-Dec;50(6):59-63.
  • PMID: 6101155
    McNiff EF, Yacobi A, Young-Chang FM, Golden LH, Goldfarb A, Fung HL: Nitroglycerin pharmacokinetics after intravenous infusion in normal subjects. J Pharm Sci. 1981 Sep;70(9):1054-8.
  • PMID: 3086541
    Cossum PA, Roberts MS, Yong AC, Kilpatrick D: Distribution and metabolism of nitroglycerin and its metabolites in vascular beds of sheep. J Pharmacol Exp Ther. 1986 Jun;237(3):959-66.
  • PMID: 12890708
    Madhani M, Scotland RS, MacAllister RJ, Hobbs AJ: Vascular natriuretic peptide receptor-linked particulate guanylate cyclases are modulated by nitric oxide-cyclic GMP signalling. Br J Pharmacol. 2003 Aug;139(7):1289-96.
  • PMID: 17055381
    Chen Z, Stamler JS: Bioactivation of nitroglycerin by the mitochondrial aldehyde dehydrogenase. Trends Cardiovasc Med. 2006 Nov;16(8):259-65. doi: 10.1016/j.tcm.2006.05.001.
Menampilkan 8 dari 10 artikel.

Contoh Produk & Brand

Produk: 284 • International brands: 28
Produk
  • Apo-nitroglycerin
    Spray, metered • 0.4 mg / act • Sublingual • Canada • Generic • Approved
  • Basic Dental Emergency Kit
    Aerosol, metered; Injection; Kit; Tablet; Tablet, chewable • - • Intramuscular; Intravenous; Oral; Respiratory (inhalation); Subcutaneous; Sublingual • US
  • Deluxe Dental Emergency Kit
    Aerosol, metered; Injection; Kit; Solution; Tablet; Tablet, chewable • - • Intramuscular; Intravenous; Oral; Respiratory (inhalation); Subcutaneous; Sublingual • US
  • Gonitro
    Powder • 400 ug/1 • Sublingual • US • Approved
  • Gonitro
    Powder • 400 ug/1 • Sublingual • US • Approved
  • Minitran
    Patch • 2.5 mg/1d • Transdermal • US • Generic • Approved
  • Minitran
    Patch • 5 mg/1d • Transdermal • US • Generic • Approved
  • Minitran
    Patch • 10 mg/1d • Transdermal • US • Generic • Approved
Menampilkan 8 dari 284 produk.
International Brands
  • Deponit — UCB Pharma
  • Dermatrans — Bayer
  • Gen-Nitro — Genpharm ULC
  • Glytrin — Sanofi-Aventis
  • Glytrin Spray — Sanofi-Aventis
  • Natispray — Teofarma
  • Nitrocap — Orion
  • Nitroderm TTS — Novartis
  • Nitrolingual Pump Spray — Arbor Pharmaceuticals
  • Rectogesic — ProStrakan

Sekuens Gen/Protein (FASTA)

Sekuens dimuat saat dibutuhkan agar halaman tetap ringan.
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