Sorbitrate: profile and news

Other information

Indication
For the prevention of angina pectoris due to coronary artery disease

Pharmacology
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.

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.

Drug Category
Vasodilator Agents; Nitrates and Nitrites; ATC:C01DA08; ATC:D03AX08

Brand Names/Synonyms
Dilatrate; Isochron; Isordil; Titradose; Sorbitrate; Dinitrosorbide; Corosorbide; Carvanil; Carvasin; Cedocard; Claodical; Cornilat; Difutrat; Coronex; Flindix; 1,4:3, 6-Dianhydro-D-glucitol dinitrate; 1,4:3,6-Dianhydrosorbitol 2, 5-dinitrate; 87-33-2; AIDS-125686; AIDS125686; Cardio 10; Cardis; Carvanil; Carvasin; D-Glucitol, 1,4:3,6-dianhydro-, dinitrate; Dianhydrosorbitol 2,5-dinitrate; Dilatrate-SR; Dinitrosorbide; Emoper; Flindix; Glucitol, 1,4:3, 6-dianhydro-, dinitrate, D-; Harrical; IBD 20; ISD; ISDN; Ismotic; Iso-Bid; Isoket; Isorbid;; Isordil Tembids; Isosorbide Dinitrate; Isosorbide dinitrate(USAN); Isostat; Isotrate; Korodil; Lomilan; Maycor; Myorexon; Nitrosorbid; Nitrosorbide; Nitrosorbon; Nosim; Resoidan; Rifloc Retard; Rigedal; Sorbangil; Sorbide T.D.; Sorbide nitrate; Sorbide, dinitrate; Sorbidilat; Sorbidnitrate; Sorbislo; Sorbonit; Sorquad; Tinidil; Vascardin; Vasodilat; Vasorbate; Xanyl

Dosage Forms
Oral tablet

Absorption
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%

Interactions
DRUG INTERACTIONS The vasodilating effects of isosorbide dinitrate may be additive with those of other vasodilators. Alcohol, in particular, has been found to exhibit additive effects of this variety.

Chemical IUPAC Name
4,8-dinitrooxy-2,6-dioxabicyclo[3.3.0]octane

Chemical Formula
C6H8N2O8

Half Life
1 hour

Drug Type
Approved Drug

# Accession No
APRD00455

CAS Registry Number
87-33-2