Drug/Small Molecule:
isosorbide mononitrate

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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The annotations do not account for individual variations among patients, and cannot be considered inclusive of all proper methods of care or exclusive of other treatments. It remains the responsibility of the health-care provider to determine the best course of treatment for a patient. Adherence to any guideline is voluntary, with the ultimate determination regarding its application to be made solely by the clinician and the patient. PharmGKB assumes no responsibility for any injury or damage to persons or property arising out of or related to any use of the PharmGKB clinical annotations, or for any errors or omissions.

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This is a non-comprehensive list of genetic tests with pharmacogenetics relevance, typically submitted by the manufacturer and manually curated by PharmGKB. The information listed is provided for educational purposes only and does not constitute an endorsement of any listed test or manufacturer.

A more complete listing of genetic tests is found at the Genetic Testing Registry (GTR).

PGx Test Variants Assayed Gene?
2D structure from PubChem
provided by PubChem

Overview

Generic Names
  • IHD
  • ISMN
  • Isosorbidi Mononitras [Latin]
  • Mononitrate d'Isosorbide [French]
  • Mononitrato de Isosorbida [Spanish]
  • Monosorbitrate
Trade Names
  • Conpin
  • Conpin Retardkaps
  • Corangin
  • Corangin Sr
  • Duride
  • Edistol
  • Elantan
  • Elantan Long
  • Elantan Retard
  • Epicordin
  • Etimonis
  • Fem-Mono
  • IS 5MN
  • ISMN AL
  • Imazin
  • Imdur
  • Imdur 60
  • Imdur Durules
  • Imodur
  • Imtrate
  • Ismexin
  • Ismn Abz
  • Ismn Apogepha
  • Ismn Atid
  • Ismn Basics
  • Ismn Heumann
  • Ismn Hexal
  • Ismn Lannacher
  • Ismn Stada
  • Ismo
  • Ismo-20
  • Ismox
  • Isomon
  • Isomonat
  • Isomonit
  • Isopen-20
  • Iturol
  • Medocor
  • Monicor
  • Monis
  • Monisid
  • Monit
  • Monit 20
  • Monizid
  • Mono Corax
  • Mono Corax Retard
  • Mono Mack
  • Mono-Mack
  • Mono-Sanorania
  • Monocedocard
  • Monoclair
  • Monocord 20
  • Monocord 40
  • Monocord 50 Sr
  • Monodur Durules
  • Monoket
  • Monoket Od
  • Monoket Retard
  • Monolong
  • Monolong 40
  • Monolong 60
  • Mononit
  • Mononit 20
  • Mononit 40
  • Mononit Retard 50
  • Monopront
  • Monosigma
  • Monosorb
  • Monosordil
  • Monotrate
  • Multitab
  • Nitex
  • Nitramin
  • Olicard
  • Olicardin
  • Orasorbil
  • Pentacard
  • Pentacard 20
  • Percorina
  • Pertil
  • Plodin
  • Promocard
  • Sigacora
  • Sorbimon
  • Titarane
  • Turimonit
  • Uniket
  • Vasdilat
  • Vasotrate
Brand Mixture Names

PharmGKB Accession Id:
PA450126

Description

Isosorbide mononitrate is a drug used principally in the treatment of angina pectoris[1] and acts by dilating the blood vessels so as to reduce the blood pressure. It is sold by AstraZeneca under the trade name Imdur.

Isosorbide mononitrate is used to for the the prophylactic treatment of angina pectoris; that is, it is taken in order to prevent or at least reduce the occurrence of angina. Research on Isosorbide mononitrate as a cervical ripener to reduce time at hospital to birth is supportive.

Isosorbide mononitrate is an active metabolite of isosorbide dinitrate and exerts qualitatively similar effects. Isosorbide mononitrate reduces the workload of the heart by producing venous and arterial dilation. By reducing the end diastolic pressure and volume, isosorbide mononitrate lowers intramural pressure, hence leading to an improvement in the subendocardial blood flow. The net effect when administering isosorbide mononitrate is therefore a reduced workload for the heart and an improvement in the oxygen supply/demand balance of the myocardium.

The adverse reactions which follow have been reported in studies with isosorbide mononitrate:
Very common. Headache predominates (up to 30%) necessitating withdrawal of 2 to 3 % of patients, but the incidence reduces rapidly as treatment continues .
Common. Tiredness, sleep disturbances (6%) and gastrointestinal disturbances (6%) have been reported during clinical trials with isosorbide mononitrate modified release tablets, but at a frequency no greater than for placebo. Hypotension (4 to 5%), poor appetite (2.5%), nausea (1%).
Adverse effects associated with the clinical use of the drug are as expected with all nitrate preparations. They occur mainly in the early stages of treatment.
Hypotension (4%) with symptoms such as dizziness and nausea (1%) have been reported. These symptoms generally disappear during long-term treatment.
Other reactions that have been reported with isosorbide mononitrate modified release tablets include tachycardia, vomiting, diarrhoea, vertigo and heartburn

Source: Drug Bank

Indication

For the prevention of angina pectoris due to coronary artery disease and the treatment of acute and chronic angina pectoris, hypertension, and myocardial infarction.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

Mechanism of Action

Similar to other nitrites and organic nitrates, Isosorbide Mononitrate is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (Atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.

Source: Drug Bank

Pharmacology

Isosorbide-5-mononitrate, the long-acting metabolite of isosorbide dinitrate, is used as a vasodilatory agent in the management of angina pectoris. By dilating the vessels, it lowers the blood pressure and reduces the left ventricular preload and afterload, therefore, leads to a reduction of myocardial oxygen requirement.

Source: Drug Bank

Food Interaction

Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Hepatic

Source: Drug Bank

Protein Binding

5%

Source: Drug Bank

Absorption

100%

Source: Drug Bank

Half-Life

5 hours

Source: Drug Bank

Toxicity

Symptoms of overdose include vasodilatation, venous pooling, reduced cardiac output, and hypotension. There are no data suggesting what dose of isosorbide mononitrate is likely to be life-threatening in humans. In rats and mice, there is significant lethality at doses of 2000 mg/kg and 3000 mg/kg, respectively.

Source: Drug Bank

Route of Elimination

Isosorbide mononitrate is primarily metabolized by the liver, but unlike oral isosorbide dinitrate, it is not subject to first-pass metabolism.
Isosorbide mononitrate is cleared by denitration to isosorbide and glucuronidation as the mononitrate, with 96% of the administered dose excreted in the urine within 5 days and only about 1% eliminated in the feces. At least six different compounds have been detected in urine, with about 2% of the dose excreted as the unchanged drug and at least five metabolites.

Source: Drug Bank

Volume of Distribution

  • 0.6 to 0.7 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C6H9NO6

Source: Drug Bank

Isomeric SMILES

C1[C@@H]([C@@H]2[C@H](O1)[C@@H](CO2)O[N+](=O)[O-])O

Source: Drug Bank

[H][C@]12OC[C@@H](O[N+]([O-])=O)[C@@]1([H])OC[C@@H]2O

Source: Drug Bank

Canonical SMILES

O[C@H]1CO[C@@H]

Source: Drug Bank

Average Molecular Weight

191.1388

Source: Drug Bank

Monoisotopic Molecular Weight

191.042987025

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Drug Targets

Gene Description
GUCY1A2 (source: Drug Bank)
NPR1 (source: Drug Bank)

Drug Interactions

Drug Description
dihydroergotamine Possible antagonism of action (source: Drug Bank)
dihydroergotoxine Possible antagonism of action (source: Drug Bank)
ergonovine Possible antagonism of action (source: Drug Bank)
ergonovine Possible antagonism of action (source: Drug Bank)
ergotamine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methylergonovine Possible antagonism of action (source: Drug Bank)
methysergide Possible antagonism of action (source: Drug Bank)
sildenafil Possible significant hypotension with this combination (source: Drug Bank)
sildenafil Possible significant hypotension with this combination (source: Drug Bank)
tadalafil Possible significant hypotension with this combination (source: Drug Bank)
tadalafil Possible significant hypotension with this combination (source: Drug Bank)
vardenafil Possible significant hypotension with this combination (source: Drug Bank)
vardenafil Possible significant hypotension with this combination (source: Drug Bank)
No related diseases are available

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0085-3306-03
DrugBank:
DB01020
ChEBI:
6062
KEGG Compound:
C07714
KEGG Drug:
D00630
PubChem Compound:
27661
PubChem Substance:
46506594
9916
Drugs Product Database (DPD):
2126559
ChemSpider:
25736
Therapeutic Targets Database:
DAP001058

Clinical Trials

These are trials that mention isosorbide mononitrate and are related to either pharmacogenetics or pharmacogenomics.

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Sources for PharmGKB drug information: DrugBank, Open Eye Scientific Software.