Drug Groups

approved

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. [PubChem]

Indication

For the treatment of Hypertension

Pharmacology

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.

Toxicity

LD₅₀=740mg/kg (orally in mice)

Affected Organisms

Biotransformation

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

Absorption

Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.

Half Life

3.0 - 4.5 hours

Protein Binding

70%-80%

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