Sorbidilat
Sorbidilat 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).
Sorbidilat 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.
Trade Name | Sorbidilat |
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 | |
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.
Sorbidilat is also used to associated treatment for these conditions: Angina Pectoris, Coronary Artery Disease (CAD), Heart Failure, High Blood Pressure (Hypertension)
How Sorbidilat 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
Sorbidilat dosage
The usual starting dose of Sorbidilat 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.
Storage Condition
Store at room temperature (25° C).
Innovators Monograph
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