Isosorbide Dinitrate information from DrugsUpdate
P - Caution when used during pregnancy
L - Caution when used during lactation
LI - Lab *
Isosorbide dinitrate (ISDN) (also known as Dilatrate) is a nitrate used pharmacologically as a vasodilator, e.g. in angina pectoris but also for anal fissure, a condition which is known to involve decreased blood supply leading to poor healing. It is also used as a direct vasodilator to treat congestive heart failure.
Isosorbide dinitrate is sold under the brand names Isordil by Biovail, Cedocard and Sorbitrate. In UK and Hong Kong, a trade name of it is Isoket. It is also a component of BiDil.
Pharmacodynamics
Pharmacokinetics
Isosorbide dinitrate relaxes vascular smooth muscles by stimulating cyclic-GMP. It decreases left ventricular pressure (preload) and arterial resistance (afterload).
Onset
2-5 minutes (sublingual); <1 hour (oral as conventional tab).
Duration
2 hours (sublingual); 4-6 hours (oral as conventional tab).
Absorption
Readily absorbed from the oral mucosa (sublingual) and from the GIT (oral); absorbed from the skin (topical).
Distribution
Widely distributed: Smooth muscle cells of the blood vessels.
Metabolism
Extensive hepatic first-pass metabolism; converted to isosorbide-2-mononitrate and isosorbide-5-mononitrate.
Excretion
Elimination half-life: 45-60 minutes (sublingual); 20 minutes -4 hours (IV, oral).
Isosorbide Dinitrate Indications / Isosorbide Dinitrate Uses
Information Not Available
Isosorbide Dinitrate Adverse Reactions / Isosorbide Dinitrate Side Effects
Hypotension, tachycardia, flushing, headache, dizziness, palpitation, syncope, confusion. Nausea, vomiting, abdominal pain. Apprehension, restlessness, weakness and vertigo.
Potentially Fatal: Severe hypotension, circulatory collapse.
Precautions
Information Not Available
Special Precautions
Raised intracranial pressure, hypotension, hypovolaemia. Mitral valve prolapse, arterial hypoxaemia, glaucoma, elderly, hypothyroidism, malnutrition, pregnancy, lactation.
Other Drug Interactions
Increased hypotensive effects with alcohol or vasodilators. Marked orthostatic hypotension may occur when used with calcium channel blockers. Vasodilatory effect may be reduced with dihydroergotamine. Ergotamine effects may be enhanced. Reduced effectiveness of sublingual form with disopyramide.
Potentially Fatal: Significant hypotension may occur with phosphodiesterase-5 inhibitors.
Other Interactions
Information Not Available
Dosage
Sublingual
Heart failure
Adult: 5-15 mg every 2-3 hours
Sublingual
Acute angina
Adult: As tablet: 2.5-10 mg placed under the tongue. As spray: 1-3 sprays (1.25 mg/spray) directed under the tongue.
Oral
Management of angina
Adult: 20-120 mg daily in divided doses. Gradually increase according to patient's response. Max dose: 240 mg daily.
Oral
Heart failure
Adult: 30-160 mg daily in divided doses. Max dose: 240 mg daily.
Intravenous
Unstable angina
Adult: 2-12 mg/hr titrated according to patient's response. Max dose: 20 mg/hour.
Intravenous
Heart failure
Adult: 2-12 mg/hr titrated according to patient's response. Max dose: 20 mg/hour.
Intracoronary
Percutaneous transluminal coronary angioplasty
Adult: 1 mg as a bolus before balloon inflation. Max dose within a 30-min period: 5 mg.
Food(before/after)
Should be taken on an empty stomach. (Take on an empty stomach ½ hr before meals.)
List of Contraindications
Isosorbide Dinitrate and Pregnancy
Caution when used during pregnancy
Category C: Either studies in animals have revealed adverse effects on the foetus (teratogenic or embryocidal or other) and there are no controlled studies in women or studies in women and animals are not available. Drugs should be given only if the potential benefit justifies the potential risk to the foetus.
Isosorbide Dinitrate and Lactation
Caution when used during lactation
Isosorbide Dinitrate and Children
Safety and efficacy not established
Isosorbide Dinitrate and Geriatic
Dose selection should be cautious, usually starting at the lower end of the dosing range, reflecting the greater frequency of decreased hepatic, renal, or cardiac function, and comorbidity.
Isosorbide Dinitrate and Other Contraindications
Severe hypotension or anaemia, hypovolaemia, heart failure due to obstruction, or raised intracranial pressure due to head trauma or cerebral haemorrhage.
Storage
Oral
Store at room temperature (25°C)
Sublingual
Store at room temperature (25°C)
Lab interference
Oral
Store at room temperature (25°C)
Sublingual
Store at room temperature (25°C)
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