pharmacopeia
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Mechanism of action

Sourced from openFDA

Mechanism-of-action classes: Nitric Oxide Donors; Phosphodiesterase 5 Inhibitors.

Phosphodiesterase 5

Indications

Sourced from openFDA
  • Isosorbide Mononitrate Tablets USP are indicated for the prevention and treatment of angina pectoris due to coronary artery disease. The onset of action of oral isosorbide mononitrate is not sufficiently rapid for this product to be useful in aborting an acute anginal episode.ICD-10: I20.9

Contraindications

Sourced from openFDA
  • Isosorbide mononitrate is contraindicated in patients who are allergic to it. Do not use isosorbide mononitrate in patients who are taking certain drugs for erectile dysfunction (phosphodiesterase inhibitors), such as sildenafil, tadalafil, or vardenafil.contraindicated

Dosage & administration

Sourced from openFDA

The recommended regimen of isosorbide mononitrate tablets is 20 mg twice daily, with the doses seven hours apart. A starting dose of 5 mg (½ tablet of the 10 mg dosing strength) might be appropriate for persons of particularly small stature but should be increased to at least 10 mg by the second or third day of therapy. Dosage adjustments are not necessary for elderly patients or patients with altered hepatic or renal function. As noted above ( CLINICAL PHARMACOLOGY ), multiple studies of organic nitrates have shown that maintenance of continuous 24-hour plasma levels results in refractory tolerance. The asymmetric (2 doses, 7 hours apart) dosing regimen for isosorbide mononitrate tablets provides a daily nitrate-free interval to minimize the development of tolerance. As also noted under CLINICAL PHARMACOLOGY , well-controlled studies have shown that tolerance to isosorbide mononitrate tablets occurs to some extent when using the twice-daily regimen in which the two doses are given seven hours apart. This regimen has been shown to have antianginal efficacy beginning one hour after the first dose and lasting at least seven hours after the second dose. The duration (if any) of antianginal activity beyond fourteen hours has not been studied. In clinical trials, isosorbide mononitrate has been administered in a variety of regimens and doses. Doses above 20 mg twice a day (with the doses seven hours apart) have not been adequately studied.

Warnings & precautions

Sourced from openFDA

Amplification of the vasodilatory effects of isosorbide mononitrate by sildenafil can result in severe hypotension. The time course and dose dependence of this interaction have not been studied. Appropriate supportive care has not been studied, but it seems reasonable to treat this as a nitrate overdose, with elevation of the extremities and with central volume expansion. The benefits of isosorbide mononitrate in patients with acute myocardial infarction or congestive heart failure have not been established. Because the effects of isosorbide mononitrate are difficult to terminate rapidly, this drug is not recommended in these settings. If isosorbide mononitrate is used in these conditions, careful clinical or hemodynamic monitoring must be used to avoid the hazards of hypotension and tachycardia.

Adverse reactions

Sourced from openFDA

Headache is the most frequent side effect and was the cause of 2% of all dropouts from controlled-clinical trials. Headache decreased in incidence after the first few days of therapy. The following table shows the frequency of adverse reactions observed in 1% or more of subjects in 6 placebo-controlled trials, conducted in the United States and abroad. The same table shows the frequency of withdrawal for these adverse reactions. In many cases the adverse reactions were of uncertain relation to drug treatment. Frequency Of Adverse Reactions (Discontinuations)* 6 Placebo-Controlled Studies Dose Placebo 5 mg 10 mg 20 mg Patients 160 54 52 159 Headache 6% (0%) 17% (0%) 13% (0%) 35% (5%) Fatigue 2% (0%) 0% (0%) 4% (0%) 1% (0%) Upper Respiratory Infection <1% (0%) 0% (0%) 4% (0%) 1% (0%) Pain <1% (0%) 4% (0%) 0% (0%) <1% (0%) Dizziness 1% (0%) 0% (0%) 0% (0%) 4% (0%) Nausea <1% (0%) 0% (0%) 0% (0%) 3% (2%) Increased Cough <1% (0%) 0% (0%) 2% (0%) <1% (0%) Rash 0% (0%) 2% (2%) 0% (0%) <1% (0%) Abdominal Pain <1% (0%) 0% (0%) 2% (0%) 0% (0%) Allergic Reaction 0% (0%) 0% (0%) 2% (0%) 0% (0%) Cardiovascular Disorder 0% (0%) 2% (0%) 0% (0%) 0% (0%) Chest Pain <1% (0%) 0% (0%) 2% (0%) <1% (0%) Diarrhea 0% (0%) 0% (0%) 2% (0%) 0% (0%) Flushing 0% (0%) 0% (0%) 2% (0%) 0% (0%) Emotional Lability 0% (0%) 2% (0%) 0% (0%) 0% (0%) Pruritus 1% (0%) 2% (2%) 0% (0%) 0% (0%) *Some individuals discontinued for multiple reasons.

Use in specific populations

Sourced from openFDA

Pregnancy Teratogenic Effects Reproduction studies performed in rats and rabbits at doses of up to 540 and 810 mg/kg/day, respectively, have revealed no evidence of harm to the fetus due to isosorbide mononitrate. There are, however, no adequate and well-controlled studies in pregnant women. Because animal reproduction studies are not always predictive of human response, isosorbide mononitrate should be used during pregnancy only if clearly needed. Nonteratogenic Effects Birth weights, neonatal survival and development, and incidence of stillbirths were adversely affected when pregnant rats were administered oral doses of 540 (but not 270) mg isosorbide mononitrate/kg/day during late gestation and lactation. This dose was associated with decreased maternal body weight gain and decreased maternal motor activity. Species Daily dose (mg/kg) Multiple of MRHD* Based on: Body Weight Body Surface Rabbit 810 1013 375 Rat 900 540 500 360 270 1125 675 625 450 338 195 117 108 78 59 Calculations assume a human weight of 50 kg and human body surface area of 1.46 m 2 , a rabbit weight of 2 kg and rabbit body surface area of 0.163 m 2 , and a rat weight of 150 g and rat body surface area of 0.025 m 2 . *Maximum recommended human dose (MRHD) is 20 mg bid.

Pharmacokinetics

Sourced from openFDA
Metabolism
Isosorbide mononitrate is rapidly and completely absorbed from the gastrointestinal tract. In humans, isosorbide mononitrate is not subject to first pass metabolism in the liver.

Overdosage

Sourced from openFDA

Hemodynamic Effects The ill effects of isosorbide mononitrate overdose are generally the results of isosorbide mononitrate’s capacity to induce vasodilatation, venous pooling, reduced cardiac output, and hypotension. These hemodynamic changes may have protean manifestations, including increased intracranial pressure, with any or all of persistent throbbing headache, confusion, and moderate fever; vertigo; palpitations; visual disturbances; nausea and vomiting (possibly with colic and even bloody diarrhea); syncope (especially in the upright posture); air hunger and dyspnea, later followed by reduced ventilatory effort; diaphoresis, with the skin either flushed or cold and clammy; heart block and bradycardia; paralysis; coma; seizures and death. Laboratory determinations of serum levels of isosorbide mononitrate and its metabolites are not widely available, and such determinations have, in any event, no established role in the management of isosorbide mononitrate overdose. There are no data suggesting what dose of isosorbide mononitrate is likely to be life-threatening in humans.

Approval history

Sourced from openFDA
  • Nov 9, 1959NDANDA012093Bausch
  • Mar 12, 1987ANDAANDA086925Ph Health
  • Mar 12, 1987ANDAANDA086923Ph Health
  • Mar 12, 1987ANDAANDA087946Ph Health
  • Oct 2, 1987ANDAANDA087537Ph Health
  • Nov 2, 1987ANDAANDA088088Hikma Intl Pharms
  • Jun 30, 1993NDANDA020215Omnivium Pharms
  • Jun 23, 2005NDANDA020727Azurity

FAERS reports

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Reference statistics only. FAERS reports are voluntarily submitted and are not incidence rates, safety signals, or causal evidence. Counts reflect reporting volume — how often a reaction was reported, not how often it occurs. For decision-grade use, consult openFDA and the FAERS Public Dashboard directly.
39,191 total reports matchedLatest report Share = reports listing the reaction ÷ total matched reports. Rows can sum to >100% because a single report often lists multiple reactions.
  1. 1Dyspnoea2,8257.2%
  2. 2Dizziness2,3776.1%
  3. 3Nausea2,2615.8%
  4. 4Fatigue2,2585.8%
  5. 5Diarrhoea2,2025.6%
  6. 6Chest Pain1,9825.1%
  7. 7Myocardial Infarction1,8904.8%
  8. 8Headache1,7054.4%
  9. 9Vomiting1,6104.1%
  10. 10Pain1,5734.0%
  11. 11Hypotension1,5403.9%
  12. 12Acute Kidney Injury1,5173.9%
  13. 13Death1,4943.8%
  14. 14Fall1,4693.7%
  15. 15Asthenia1,4663.7%

Literature

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Recent PubMed references pinned to Isosorbide as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

Clinical trials

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The 10 most recently updated of 112 ClinicalTrials.gov registrations naming Isosorbide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

Frequently asked questions

How does Isosorbide work?
Mechanism-of-action classes: Nitric Oxide Donors; Phosphodiesterase 5 Inhibitors.
What is Isosorbide used for?
According to FDA labeling, Isosorbide carries indications including: Isosorbide Mononitrate Tablets USP are indicated for the prevention and treatment of angina pectoris due to coronary artery disease. The onset of action of oral isosorbide mononitrate is not sufficiently rapid for this product to be useful in aborting an acute anginal episode.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
What class of drug is Isosorbide?
Isosorbide is classified as Nitric Oxide Donors, Phosphodiesterase 5 Inhibitors, Arterial Vasodilation, Increased Nitric Oxide Activity, Venous Vasodilation.
What are the contraindications for Isosorbide?
Isosorbide labeling lists contraindications including: Isosorbide mononitrate is contraindicated in patients who are allergic to it. Do not use isosorbide mononitrate in patients who are taking certain drugs for erectile dysfunction (phosphodiesterase inhibitors), such as sildenafil, tadalafil, or vardenafil.. Always consult the full prescribing information and a clinician.
Note. Data for isosorbide is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.

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