DESCRIPTION

A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of the calcium ion in membrane functions. It is also teratogenic.

CATEGORIES

Calcium Antagonists

CHEMICAL FORMULA

C22H26N2O4S

COMPOSITION

Diltiazem 30 MG

INDICATION

For the treatment of Hypertension

PHARMACODYNAMICS

Diltiazem, a benzothiazepine calcium-channel blocker, is used alone or with an angiotensin-converting enzyme inhibitor, to treat hypertension, chronic stable angina pectoris, and Prinzmetal’s variant angina. Diltiazem is a non-dihydropyridine (DHP)member of the calcium channel blocker class, along with Verapamil. Diltiazem is similar to other peripheral vasodilators. Diltiazem inhibits the influx of extra cellular calcium across the myocardial and vascular smooth muscle cell membranes possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum. The decrease in intracellular calcium inhibits the contractile processes of the myocardial smooth muscle cells, causing dilation of the coronary and systemic arteries, increased oxygen delivery to the myocardial tissue, decreased total peripheral resistance, decreased systemic blood pressure, and decreased afterload.

MECHANISM

Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

METABOLISM

Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.

HALF LIFE

3.0 – 4.5 hours

TOXICITY

LD50=740mg/kg (orally in mice)

FOOD INTERACTIONS

Avoid natural licorice. Take this medication 30 minutes before meals.

SIDE EFFECTS

Feeling dizzy. Rise slowly over a few minutes when sitting or lying down. Be careful climbing. – Headache. – Upset stomach or throwing up. Many small meals, good mouth care, sucking hard, sugar-free candy, or chewing sugar-free gum may help. – Hard stools (constipation). Drinking more liquids, working out, or adding fiber to your diet may help. Talk with your doctor about a stool softener or laxative.