Peringatan Keamanan

The oral LD50 is 2010 mg/kg in rats and 1771 mg/kg in mice.L11728

The symptoms of overdose from isosorbide mononitrate is associated with vasodilatation, venous pooling, reduced cardiac output, and hypotension. These symptoms can be accompanied by several manifestations, including increased intracranial pressure (possibly along with persistent throbbing headache, confusion, and moderate fever), vertigo, palpitations, visual disturbances, nausea and vomiting (possibly along with colic and bloody diarrhea), syncope (especially in the upright posture), air hunger and dyspnea (later followed by reduced ventilatory effort), diaphoresis (with flushed or cold and clammy skin), heart blocks and bradycardia, paralysis, coma, seizures, and death.L11698

There is limited clinical information on the management of isosorbide mononitrate overdose; it is advised that venodilatation and arterial hypovolemia from overdose are responded with therapy aimed to increase in central fluid volume. However, this method may be potentially hazardous in patients with renal disease or congestive heart failure: invasive monitoring may be required in these patients. The patient's legs should be passively elevated, and intravenous infusion of normal saline or similar fluid is recommended. Isosorbide mononitrate was shown to be significantly removed from the systemic circulation via hemodialysis. The use of epinephrine or other arterial vasoconstrictors is not recommended.L11698

Isosorbide mononitrate

DB01020

small molecule approved

Deskripsi

Isosorbide mononitrate is an organic nitrate with vasodilating properties. It is an anti-anginal agent that works by relaxing the smooth muscles of both arteries and veins, but but predominantly veins to reduce cardiac preload.L11698, L11743 Isosorbide mononitrate is an active metabolite of isosorbide dinitrate. Like other organic nitrates, isosorbide mononitrate acts as a prodrug for its active metabolite, nitric oxide, which mediates the therapeutic action of isosorbide mononitrate.L11743 Isosorbide mononitrate has a longer duration of action than nitroglycerin due to its slow onset of absorption and metabolism.T28

First approved by the FDA in 1991,L11743 isosorbide mononitrate is used for the prevention and management of angina pectoris caused by coronary artery disease; however, the onset of action of orally-administered isosorbide mononitrate is not rapid enough to offset an acute anginal episode.L11698 It is available in oral tablets generically and under the brand name ISMO and Monoket. The extended-release forms of the drug are also available generically and under the brand name Imdur.L11743

Struktur Molekul 2D

Berat 191.1388
Wujud solid

Peta Jejaring Molekuler
Legenda: Obat • Target • Gen • Enzim • (Panah → menunjukkan arah efek / relasi) • Transporter • Carrier

Profil Farmakokinetik

Waktu Paruh (Half-Life) The elimination half-life of isosorbide mononitrate is about 5 hours.[L11698] The elimination half-life of its metabolites, isosorbide and 2-glucuronide of mononitrate, are 8 hours and 6 hours, respectively.[A190738]
Volume Distribusi The volume of distribution is approximately 0.6 L/kg, which is approximately the volume of total body water.[A190738,L11698]
Klirens (Clearance) The total body clearance is 115-120 mL/min.[A190738]

Absorpsi

Upon oral administration, isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract. Isosorbide mononitrate has a dose-linear kinetics and the absolute bioavailability is nearly 100%. The Cmax is reached within 30 to 60 minutes following administration.L11698

Metabolisme

Isosorbide mononitrate is not subject to first pass metabolism in human liver.L11698 Detectable metabolites include isosorbide, sorbitol, and 2-glucuronide of mononitrate, which are pharmacologically inactive.A190738,L11698

Rute Eliminasi

In a human radio-labelled drug study, about 93% of the total dose was excreted in the urine within 48 hours.L11698 Following oral administration of 20 mg, only 2% of isosorbide mononitrate was excreted unchanged in the urine within 24 hours. A190738 Among the excreted dose, nearly half of the dose was found de-nitrated in urine as isosorbide and sorbitol: approximately 30% is excreted as isosorbide and about 17% is the 2-glucuronide of mononitrate.A190738 These metabolites were not vasoactive or pharmacologically active. Renal excretion was complete after 5 days, and fecal excretion accounted for only 1% of drug elimination.L11698

Interaksi Makanan

1 Data
  • 1. Take with or without food. The absorption is unaffected by food.

Interaksi Obat

1061 Data
Duloxetine The risk or severity of orthostatic hypotension and syncope can be increased when Isosorbide mononitrate is combined with Duloxetine.
Levodopa The risk or severity of hypotension and orthostatic hypotension can be increased when Isosorbide mononitrate is combined with Levodopa.
Risperidone Isosorbide mononitrate may increase the hypotensive activities of Risperidone.
Prilocaine The risk or severity of methemoglobinemia can be increased when Isosorbide mononitrate is combined with Prilocaine.
Dapoxetine Dapoxetine may increase the orthostatic hypotensive and hypotensive activities of Isosorbide mononitrate.
Riociguat Isosorbide mononitrate may increase the hypotensive activities of Riociguat.
Aripiprazole Aripiprazole may increase the hypotensive activities of Isosorbide mononitrate.
Aripiprazole lauroxil Aripiprazole lauroxil may increase the hypotensive activities of Isosorbide mononitrate.
Dapsone The risk or severity of methemoglobinemia can be increased when Dapsone is combined with Isosorbide mononitrate.
Ethanol Ethanol may increase the hypotensive and vasodilatory activities of Isosorbide mononitrate.
Linezolid Linezolid may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Furazolidone Furazolidone may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Tranylcypromine Tranylcypromine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Phenelzine Phenelzine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Minaprine Minaprine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Selegiline Selegiline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Procarbazine Procarbazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Moclobemide Moclobemide may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Isocarboxazid Isocarboxazid may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Rasagiline Rasagiline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Pargyline Pargyline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Clorgiline Clorgiline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Iproniazid Iproniazid may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Nialamide Nialamide may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Safinamide Safinamide may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline 7,8-Dichloro-1,2,3,4-tetrahydroisoquinoline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Methylene blue Methylene blue may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Hydracarbazine Hydracarbazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Pirlindole Pirlindole may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Toloxatone Toloxatone may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Benmoxin Benmoxin may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Mebanazine Mebanazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Octamoxin Octamoxin may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Pheniprazine Pheniprazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Phenoxypropazine Phenoxypropazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Pivhydrazine Pivhydrazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Safrazine Safrazine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Caroxazone Caroxazone may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Harmaline Harmaline may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Brofaromine Brofaromine may increase the orthostatic hypotensive activities of Isosorbide mononitrate.
Secobarbital Secobarbital may increase the hypotensive activities of Isosorbide mononitrate.
Methohexital Methohexital may increase the hypotensive activities of Isosorbide mononitrate.
Thiopental Thiopental may increase the hypotensive activities of Isosorbide mononitrate.
Methylphenobarbital Methylphenobarbital may increase the hypotensive activities of Isosorbide mononitrate.
Thiamylal Thiamylal may increase the hypotensive activities of Isosorbide mononitrate.
Amobarbital Amobarbital may increase the hypotensive activities of Isosorbide mononitrate.
Hexobarbital Hexobarbital may increase the hypotensive activities of Isosorbide mononitrate.
Barbital Barbital may increase the hypotensive activities of Isosorbide mononitrate.
Barbexaclone Barbexaclone may increase the hypotensive activities of Isosorbide mononitrate.
Butabarbital Butabarbital may increase the hypotensive activities of Isosorbide mononitrate.
Pentobarbital Pentobarbital may increase the hypotensive activities of Isosorbide mononitrate.
Primidone Primidone may increase the hypotensive activities of Isosorbide mononitrate.
Streptokinase The risk or severity of adverse effects can be increased when Streptokinase is combined with Isosorbide mononitrate.
Ropinirole The risk or severity of adverse effects can be increased when Ropinirole is combined with Isosorbide mononitrate.
Morphine The risk or severity of adverse effects can be increased when Morphine is combined with Isosorbide mononitrate.
Olanzapine The risk or severity of adverse effects can be increased when Olanzapine is combined with Isosorbide mononitrate.
Nabilone The risk or severity of adverse effects can be increased when Nabilone is combined with Isosorbide mononitrate.
Sotalol The risk or severity of adverse effects can be increased when Sotalol is combined with Isosorbide mononitrate.
Thioridazine The risk or severity of adverse effects can be increased when Thioridazine is combined with Isosorbide mononitrate.
Tizanidine The risk or severity of adverse effects can be increased when Tizanidine is combined with Isosorbide mononitrate.
Sufentanil The risk or severity of adverse effects can be increased when Sufentanil is combined with Isosorbide mononitrate.
Apomorphine The risk or severity of adverse effects can be increased when Apomorphine is combined with Isosorbide mononitrate.
Isoflurane The risk or severity of adverse effects can be increased when Isoflurane is combined with Isosorbide mononitrate.
Propofol The risk or severity of adverse effects can be increased when Propofol is combined with Isosorbide mononitrate.
Remifentanil The risk or severity of adverse effects can be increased when Remifentanil is combined with Isosorbide mononitrate.
Thalidomide The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Thalidomide.
Amifostine The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Amifostine.
Halothane The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Halothane.
Desflurane The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Desflurane.
Sevoflurane The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Sevoflurane.
Carbetocin The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Carbetocin.
Nesiritide The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Nesiritide.
Rotigotine The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Rotigotine.
Azilsartan medoxomil The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Azilsartan medoxomil.
Obinutuzumab The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Obinutuzumab.
Dinutuximab The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Dinutuximab.
Nitrous acid The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Nitrous acid.
Fimasartan The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Fimasartan.
Pipamperone The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Pipamperone.
Valsartan The risk or severity of adverse effects can be increased when Valsartan is combined with Isosorbide mononitrate.
Ramipril The risk or severity of adverse effects can be increased when Ramipril is combined with Isosorbide mononitrate.
Esmolol The risk or severity of adverse effects can be increased when Esmolol is combined with Isosorbide mononitrate.
Betaxolol The risk or severity of adverse effects can be increased when Betaxolol is combined with Isosorbide mononitrate.
Olmesartan The risk or severity of adverse effects can be increased when Olmesartan is combined with Isosorbide mononitrate.
Atenolol The risk or severity of adverse effects can be increased when Atenolol is combined with Isosorbide mononitrate.
Trandolapril The risk or severity of adverse effects can be increased when Trandolapril is combined with Isosorbide mononitrate.
Benazepril The risk or severity of adverse effects can be increased when Benazepril is combined with Isosorbide mononitrate.
Enalapril The risk or severity of adverse effects can be increased when Enalapril is combined with Isosorbide mononitrate.
Doxazosin The risk or severity of adverse effects can be increased when Doxazosin is combined with Isosorbide mononitrate.
Moexipril The risk or severity of adverse effects can be increased when Moexipril is combined with Isosorbide mononitrate.
Candesartan cilexetil The risk or severity of adverse effects can be increased when Candesartan cilexetil is combined with Isosorbide mononitrate.
Eprosartan The risk or severity of adverse effects can be increased when Eprosartan is combined with Isosorbide mononitrate.
Quinapril The risk or severity of adverse effects can be increased when Quinapril is combined with Isosorbide mononitrate.
Telmisartan The risk or severity of adverse effects can be increased when Telmisartan is combined with Isosorbide mononitrate.
Bretylium The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Bretylium.
Terazosin The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Terazosin.
Acebutolol The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Acebutolol.
Captopril The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Captopril.
Cilazapril The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Cilazapril.
Indoramin The risk or severity of adverse effects can be increased when Isosorbide mononitrate is combined with Indoramin.

Target Protein

Guanylate cyclase soluble subunit alpha-2 GUCY1A2

Referensi & Sumber

Artikel (PubMed)
  • PMID: 25446162
    Munzel T, Steven S, Daiber A: Organic nitrates: update on mechanisms underlying vasodilation, tolerance and endothelial dysfunction. Vascul Pharmacol. 2014 Dec;63(3):105-13. doi: 10.1016/j.vph.2014.09.002. Epub 2014 Oct 14.
  • PMID: 1449102
    Abshagen UW: Pharmacokinetics of isosorbide mononitrate. Am J Cardiol. 1992 Nov 27;70(17):61G-66G. doi: 10.1016/0002-9149(92)90028-w.
Textbook
  • ISBN: 978-0-7020-3471-8
    21. (2012). In Rang and Dale's Pharmacology (7th ed., pp. 260-261). Edinburgh: Elsevier/Churchill Livingstone.

Contoh Produk & Brand

Produk: 216 • International brands: 42
Produk
  • Apo-ismn
    Tablet, extended release • 60 mg • Oral • Canada • Generic • Approved
  • Dom-ismn
    Tablet, extended release • 60 mg • Oral • Canada • Generic • Approved
  • Imdur
    Tablet • 30 mg/1 • Oral • US • Approved
  • Imdur
    Tablet • 60 mg/1 • Oral • US • Approved
  • Imdur
    Tablet • 120 mg/1 • Oral • US • Approved
  • Imdur
    Tablet, extended release • 30 mg/1 • Oral • US • Generic • Approved
  • Imdur
    Tablet, extended release • 60 mg/1 • Oral • US • Generic • Approved
  • Imdur
    Tablet, extended release • 30 mg/1 • Oral • US • Generic • Approved
Menampilkan 8 dari 216 produk.
International Brands
  • Chemydur
  • Corangin
  • Dilatrate
  • Duride
  • Elantan
  • Etimonis
  • Imodur
  • Imtrate
  • Ismexin
  • Ismox

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