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QuickView for Diltiazem (compound)

Name: Diltiazem
PubChem Compound ID: 168918
Description: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
Molecular formula: C26H32N2O9S
Molecular weight: 548.606 g/mol
Name: Diltiazem
Name (isomeric): DB00343
Drug Type: small molecule
Description: A benzothiazepine derivative with vasodilating action due to its antagonism of the actions of CALCIUM ion on membrane functions.
Brand: Calcicard, Syn-Diltiazem, Cormax, Anoheal, Endrydil, Diladel, Dilt-cd, Herbesser, Cartia XT, Dilacor-XR, Dilpral, Dilticard, Tiazac Tildiem, Cardizem, Deltazen, Nu-Diltiaz, Novo-Diltazem, Dilta-Hexal, Incoril AP, Bruzem, Altiazem, Dilcontin, Masdil, Dilrene, Cardizem SR, Citizem, Viazem, Anginyl, Tiazac, Britiazim, Cardizem CD, Tiamate, Tiazac XC, Diltia, Apo-Diltiaz, Acalix, Dilzen, Adizem, Angizem, Dilacor, Dilzem, Cardizen LA
Category: Vasodilator Agents, Calcium Channel Blockers, Cardiovascular Agents, Antihypertensive Agents
CAS number: 42399-41-7
Indication: For the treatment of Hypertension
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 perip...
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Mechanism of Action:
Possibly by deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, diltiazem, like verapamil, inhibits the influx of extracellular calcium across both the myocardial and vascular smooth muscle cell membranes. The resultant inhibition of the contractile process...
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Absorption: Diltiazem is well absorbed from the gastrointestinal tract but undergoes substantial hepatic first-pass effect.
Protein binding: 70%-80%
Biotransformation: 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)
Affected organisms: Humans and other mammals
Food interaction:
Take this medication 30 minutes before meals.
Avoid natural licorice.
Drug interaction:
CilostazolDiltiazem, a moderate CYP3A4 inhibitor, may increase the serum concentration of cilostazol by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cilostazol if diltiazem is initiated, discontinued or dose changed.
PropranololIncreased risk of bradycardia
TriazolamThe calcium channel blocker, diltiazem, may increase the effect and toxicity of the benzodiazepine, triazolam.
CyclosporineDiltiazem may increase the effect and toxicity of cyclosporine.
TamsulosinDiltiazem, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Diltiazem is initiated, discontinued, or dose changed.
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