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 Hydrocholoride 30mg Tab IP
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.
No Information
ABSORPTION
Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
METABOLISM
Diltiazem is metabolized by and acts as an inhibitor of the CYP3A4 enzyme.
ELIMINATION
Renal,Biliary,Lactic (in lactating females).
HALF LIFE
3–4.5 hours
TOXICITY
LD50=740mg/kg (orally in mice)
FOOD INTERACTIONS
avoid alcohol
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 laxativ