Isosorbide mononitrate


Concise Prescribing Info
Indications/Uses
Listed in Dosage.
Dosage/Direction for Use
Adult : PO Angina pectoris Dosage must be individualised according to clinical response. Prophylaxis and long-term treatment: As immediate-release tab: 20 mg 2 or 3 times/day. Dose may range from 20-120 mg/day in divided doses. Prophylaxis: As extended-release/prolonged-release tab or cap: Initial: 30-60 mg once daily in the morning. Doses may be increased to 120 mg once daily if necessary. Adjunct in congestive heart failure For cases not responding to cardiac glycosides and/or diuretics: As immediate-release tab: 20 mg 2 or 3 times/day depending on individual needs.
Dosage Details
Oral
Angina pectoris
Adult: Dosage must be individualised according to clinical response. Prophylaxis and long-term treatment: As immediate-release tab: 20 mg 2 or 3 times daily. Dose may range from 20-120 mg daily in divided doses. Prophylaxis: As extended-release/prolonged-release tab or cap: Initially, 30-60 mg once daily in the morning. Doses may be increased to 120 mg once daily if necessary. Use the lowest effective dose.

Oral
Congestive heart failure
Adult: Adjunctive therapy in cases not responding to cardiac glycosides and/or diuretics: As immediate-release tab: 20 mg 2 or 3 times daily depending on individual needs and continuous haemodynamic monitoring.
Administration
Should be taken on an empty stomach.
Contraindications
Severe hypotension, hypertrophic obstructive cardiomyopathy, constrictive pericarditis, cardiac tamponade, aortic or mitral valve stenosis, acute circulatory failure/shock, circulatory collapse, cardiogenic shock, acute MI with low left ventricular filling pressure, conditions associated with increased intracranial pressure (e.g. cerebral haemorrhage, head trauma), closed-angle glaucoma, marked anaemia, hypovolaemia. Concomitant use with phosphodiesterase-5 (PDE-5) inhibitors (e.g. sildenafil) or riociguat.
Special Precautions
Patient with recent history of MI, inferior wall MI and suspected right ventricular infarctions; hypothyroidism, hypoxaemia, malnutrition, hypothermia. Not indicated for the treatment of acute angina attacks. Avoid abrupt withdrawal. Severe renal and hepatic impairment. Elderly. Pregnancy and lactation.
Adverse Reactions
Significant: Severe hypotension accompanied by paradoxical bradycardia and increased angina pectoris; orthostatic hypotension, syncope; increased intracranial pressure; drug tolerance, CNS depression, headache.
Cardiac disorders: Tachycardia.
Ear and labyrinth disorders: Vertigo.
Gastrointestinal disorders: Nausea, vomiting, diarrhoea, gastrointestinal disturbance.
General disorders and administration site conditions: Asthenia, tiredness.
Nervous system disorders: Dizziness, restlessness.
Psychiatric disorders: Somnolence, sleep disturbance.
Skin and subcutaneous tissue disorders: Rash, pruritus, increased sweating.
Respiratory, thoracic and mediastinal disorders: Transient hypoxaemia.
Vascular disorders: Pallor, flushing.
Patient Counseling Information
This drug may cause dizziness, blurred vision, and postural hypotension; if affected, do not drive or operate machinery.
MonitoringParameters
Monitor blood pressure and heart rate.
Overdosage
Symptoms: Hypotension, headache, dizziness, nausea, vomiting, excitation, tachycardia, sweating, syncope, vertigo, restlessness, flushing, blurred vision, confusion, increased intracranial pressure, and neurological deficits. Rarely, methaemoglobinaemia in very high doses. Management: Symptomatic treatment. Administer activated charcoal within 1 hour of ingesting toxic doses; perform gastric lavage if necessary. To treat hypotension, place the patient in a supine position with the legs raised; administer normal saline IV infusion as necessary. For severe hypotension, may administer inotropes (e.g. dopamine, dobutamine). In case of methaemoglobinaemia, give 1-2 mg/kg IV methylene blue.
Drug Interactions
Increased risk of orthostatic hypotension with Ca channel blockers. Additive hypotensive effect with other vasodilators, β-blockers, angiotensin II receptor antagonists, ACE inhibitors, aldesleukin, alprostadil, and TCAs. May increase the plasma levels and hypertensive effects of dihydroergotamine.
Potentially Fatal: Severe hypotension may occur when used with PDE-5 inhibitors (e.g. sildenafil, tadalafil, vardenafil) or riociguat.
Food Interaction
Increased risk of hypotension with alcohol. May reduce the rate but not the extent of absorption with food.
Lab Interference
May cause falsely low serum cholesterol determination with Zlatkis-Zak colour reaction.
Action
Description: Isosorbide mononitrate is a vasodilator and the major active metabolite of isosorbide dinitrate. It serves as an exogenous source of nitric oxide which causes vascular smooth muscle relaxation and consequent dilation of peripheral arteries and veins. This effect decreases the left and right ventricular end-diastolic pressures and volume, thereby improving the subendocardial blood flow.
Onset: Within 20-45 minutes.
Duration: ≥6 hours (immediate-release); ≥12-24 hours (extended-release).
Pharmacokinetics:
Absorption: Readily and completely absorbed from the gastrointestinal tract. May reduce the rate but not the extent of absorption with food. Bioavailability: Approx 100%. Time to peak plasma concentration: 30-60 minutes.
Distribution: Distributed into the blood cells and saliva. Volume of distribution: Approx 0.6 L/kg. Plasma protein binding: <5%.
Metabolism: Metabolised in the liver into nitric oxide (active) and other inactive metabolites, such as isosorbide and isosorbide glucuronide.
Excretion: Mainly via urine (2% as unchanged drug); faeces (1%). Elimination half-life: Approx 5 hours.
Chemical Structure

Chemical Structure Image
Isosorbide mononitrate

Source: National Center for Biotechnology Information. PubChem Compound Summary for CID 27661, Isosorbide mononitrate. https://pubchem.ncbi.nlm.nih.gov/compound/Isosorbide-mononitrate. Accessed Aug. 24, 2020.

Storage
Store between 20-30°C. Protect from light and moisture.
MIMS Class
ATC Classification
C01DA14 - isosorbide mononitrate ; Belongs to the class of organic nitrate vasodilators. Used in the treatment of cardiac disease.
References
Anon. Isosorbide Mononitrate. Lexicomp Online. Hudson, Ohio. Wolters Kluwer Clinical Drug Information, Inc. https://online.lexi.com. Accessed 23/07/2020.

Anon. Isosorbide. AHFS Clinical Drug Information [online]. Bethesda, MD. American Society of Health-System Pharmacists, Inc. https://www.ahfscdi.com. Accessed 23/07/2020.

Buckingham R (ed). Isosorbide Mononitrate. Martindale: The Complete Drug Reference [online]. London. Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/07/2020.

Elantan LA Prolonged Release Capsules (Norgine Pharmaceuticals Limited). MHRA. https://products.mhra.gov.uk/. Accessed 04/08/2020.

Imdur (AstraZeneca Pharmaceutical Co. Ltd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 23/07/2020.

ISMN Stada Tablets (Stadpharm Sdn Bhd). National Pharmaceutical Regulatory Agency - Ministry of Health Malaysia. https://www.npra.gov.my/. Accessed 20/08/2020.

Isosorbide Mononitrate 10 mg Tablets (Teva UK Limited). MHRA. https://products.mhra.gov.uk/. Accessed 23/07/2020.

Isosorbide Mononitrate 20 mg Tablets (Pharmavit Ltd). MHRA. https://products.mhra.gov.uk/. Accessed 04/08/2020.

Isosorbide Mononitrate Tablet (Lannett Company, Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/07/2020.

Isosorbide Mononitrate Tablet, Extended Release (Avet Pharmaceuticals Inc.). DailyMed. Source: U.S. National Library of Medicine. https://dailymed.nlm.nih.gov/dailymed/. Accessed 23/07/2020.

Joint Formulary Committee. Isosorbide Mononitrate. British National Formulary [online]. London. BMJ Group and Pharmaceutical Press. https://www.medicinescomplete.com. Accessed 23/07/2020.

Disclaimer: This information is independently developed by MIMS based on Isosorbide mononitrate from various references and is provided for your reference only. Therapeutic uses, prescribing information and product availability may vary between countries. Please refer to MIMS Product Monographs for specific and locally approved prescribing information. Although great effort has been made to ensure content accuracy, MIMS shall not be held responsible or liable for any claims or damages arising from the use or misuse of the information contained herein, its contents or omissions, or otherwise. Copyright © 2020 MIMS. All rights reserved. Powered by MIMS.com
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