Tuesday, February 20, 2018

ISOSORBID DINITRATE - ANTIANGINAL DRUG and its pharmacology

DESCRIPTION


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 Mononitrate 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.


SIDE EFFECTS-

Dizziness; flushing of the face and neck; headache; light-headedness, Severe allergic reactions (rash; hives; itching; difficulty breathing; tightness in the chest; swelling of the mouth, face, lips, or tongue); fainting; fast or slow heartbeat; nausea; new or worsening chest pain; vomiting.


DRUG DRUG INTERACTION-

The risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Acebutolol.
The risk or severity of adverse effects can be increased when Acetazolamide is combined with Isosorbide Dinitrate.
The risk or severity of adverse effects can be increased when Aldesleukin is combined with Isosorbide Dinitrate.
The risk or severity of adverse effects can be increased when Isosorbide Dinitrate is combined with Aliskiren.
The risk or severity of adverse effects can be increased when Amiloride is combined with Isosorbide Dinitrate.
The metabolism of Isosorbide Dinitrate can be decreased when combined with Amiodarone.
The risk or severity of adverse effects can be increased when Amlodipine is combined with Isosorbide Dinitrate.
Amobarbital may increase the hypotensive activities of Isosorbide Dinitrate.


USES-

It is used for angina, in addition to other medications for congestive heart failure, and for esophageal spasms.

REFERENCE:


Tripathi K.D,"Essentials of medical pharmacology",7th edition,page no.543

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