Isopit

Isopit Uses, Dosage, Side Effects, Food Interaction and all others data.

Isosorbide dinitrate relaxes vascular smooth muscles by stimulating cyclic-GMP. It decreases left ventricular pressure (preload) and arterial resistance (afterload).

Isopit is a moderate to long acting oral organic nitrate used for the relief and prophylactic management of angina pectoris. It relaxes the vascular smooth muscle and consequent dilatation of peripheral arteries and veins, especially the latter. Dilatation of the veins promotes peripheral pooling of blood and decreases venous return to the heart, thereby reducing left ventricular end- diastolic pressure and pulmonary capillary wedge pressure (preload). Arteriolar relaxation reduces systemic vascular resistance, systolic arterial pressure, and mean arterial pressure.

Isopit
Uses
Dosage
Side Effect
Precautions
Interactions
Uses during Pregnancy
Uses during Breastfeeding
Accute Overdose
Food Interaction
Half Life
Volume of Distribution
Clearance
Interaction With other Medicine
Contradiction
Storage

Trade Name	Isopit
Generic	Isosorbide Dinitrate
Isosorbide Dinitrate Other Names	Dinitrate d'isosorbide, Dinitrato de isosorbida, Dinitroisosorbide, Dinitrosorbide, ISDN, Isosorbide dinitrate, Isosorbidi dinitras, Sorbide nitrate, Sorbidnitrate
Type
Formula	C₆H₈N₂O₈
Weight	Average: 236.1363 Monoisotopic: 236.028065242
Protein binding	Very low
Groups	Approved, Investigational
Therapeutic Class	Nitrates: Coronary vasodilators
Manufacturer
Available Country	Japan
Last Updated:	September 19, 2023 at 7:00 am

Uses

Isosorbide dinitrate tablets are used for the prevention of angina pectoris due to coronary artery disease. The onset of action of immediate-release oral isosorbide dinitrate is not sufficiently rapid for this product to be useful in aborting an acute anginal episode.

Isopit is also used to associated treatment for these conditions: Angina Pectoris, Coronary Artery Disease (CAD), Heart Failure, High Blood Pressure (Hypertension)

How Isopit works

Isosorbide dinitrate is converted to the active nitric oxide to activate guanylate cyclase. This activation increases levels of cyclic guanosine 3',5'-monophosphate (cGMP). cGMP activates protein kinases and causes a series of phosphorylation reactions which leads to dephosphorylation of myosin light chains of smooth muscle fibres. Finally there is a release of calcium ions which causes smooth muscle relaxation and vasodilation.

Dosage

Isopit dosage

The usual starting dose of Isopit is 5 mg to 20 mg, two or three times daily. Formaintenance therapy, 10 mg to 40 mg, two or three times daily is recommended. Some patients may require higher doses. A daily dose-free interval of at least 14 hours is advisable to minimize tolerance. The optimal interval will vary with the individual patient, dose and regimen.

Should be taken on an empty stomach. Take ½ hr before meals

Side Effects

Rebound hypertension (uncommon), syncope, unstable angina flushing, hypotension/orthostatic hypotension, lightheadedness, palpitations, tachyarrhythmia, Dizziness, headache, restlessness, weakness, Nausea, Methemoglobinemia (infrequent)

Toxicity

Symptoms of overdose include reduced cardiac output and hypotension.

Precaution

Raised intracranial pressure, hypotension, hypovolaemia. Mitral valve prolapse, arterial hypoxaemia, glaucoma, elderly, hypothyroidism, malnutrition, pregnancy, lactation

Interaction

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.

Food Interaction

Take with or without food. Food decreases drug absorption.

Volume of Distribution

2 to 4 L/kg

Elimination Route

Absorption of isosorbide dinitrate after oral dosing is nearly complete, but bioavailability is highly variable (10% to 90%), with extensive first-pass metabolism in the liver. The average bioavailability of isosorbide dinitrate is about 25%.

Half Life

1 hour

Pregnancy & Breastfeeding use

Pregnancy Category-C. Animal reproduction studies have shown an adverse effect on the fetus and there are no adequate and well-controlled studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks

Lactation: Unknown whether drug is distributed into breast milk

Contraindication

Severe hypotension or anaemia, hypovolaemia, heart failure due to obstruction, or raised intracranial pressure due to head trauma or cerebral haemorrhage.

Acute Overdose

Symptoms: Increased intracranial pressure, throbbing headache, confusion, moderate fever; vertigo; palpitations; visual disturbances; nausea and vomiting; syncope; air hunger and dyspnoea; diaphoresis; heart block and bradycardia; paralysis; coma; seizures; and death. Methaemoglobinaemia.