Source of information: Drugbank (External Link). Last updated on: 3rd July 18
*Trade Name used in the content below may not be the same as the HSA-registered product.
Active Ingredient / Synonyms
1,4:3,6-Dianhydrosorbitol 2,5-dinitrate | Carvasin | D-Isosorbide dinitrate | Dianhydrosorbitol 2,5-dinitrate | Dinitrate d'isosorbide | Dinitrato de isosorbida | Dinitroisosorbide | Dinitrosorbide | Flindix | ISDN | Isorbid | Isosorbide 2,5-dinitrate | Isosorbide dinitrate | Isosorbidi dinitras | Nitrosorbide | Sorbide nitrate | Sorbidilat | Sorbidnitrate | Isosorbide Dinitrate |
A vasodilator used in the treatment of angina pectoris. Its actions are similar to nitroglycerin but with a slower onset of action. [PubChem]
For the prevention of angina pectoris due to coronary artery disease.
Mechanism of Action
Similar to other nitrites and organic nitrates, isosorbide dinitrate is converted to nitric oxide (NO), an active intermediate compound which activates the enzyme guanylate cyclase (atrial natriuretic peptide receptor A). This stimulates the synthesis of cyclic guanosine 3',5'-monophosphate (cGMP) which then activates a series of protein kinase-dependent phosphorylations in the smooth muscle cells, eventually resulting in the dephosphorylation of the myosin light chain of the smooth muscle fiber. The subsequent release of calcium ions results in the relaxation of the smooth muscle cells and vasodilation.
Isosorbide Dinitrate 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.
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%.
* 2 to 4 L/kg
Symptoms of overdose include reduced cardiac output and hypotension.
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