QuickView for Diltiazem (compound)

Summary
General Info

PubChem

PubChem Compound 168918

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

DrugBank

Identification

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.
Synonyms:	d-cis-Diltiazem
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

Pharmacology

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 perip... show more » 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. show less «
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... show more » 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 processes of the myocardial smooth muscle cells leads to dilation of the coronary and systemic arteries and improved oxygen delivery to the myocardial tissue. show less «
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

Interactions

Food interaction:

Take this medication 30 minutes before meals.

Avoid natural licorice.

Drug interaction:

Cilostazol	Diltiazem, 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.
Propranolol	Increased risk of bradycardia
Triazolam	The calcium channel blocker, diltiazem, may increase the effect and toxicity of the benzodiazepine, triazolam.
Cyclosporine	Diltiazem may increase the effect and toxicity of cyclosporine.
Tamsulosin	Diltiazem, 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.

Cilostazol	Diltiazem, 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.
Propranolol	Increased risk of bradycardia
Triazolam	The calcium channel blocker, diltiazem, may increase the effect and toxicity of the benzodiazepine, triazolam.
Cyclosporine	Diltiazem may increase the effect and toxicity of cyclosporine.
Tamsulosin	Diltiazem, 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.
Cerivastatin	Diltiazem may increase the serum concentration of cerivastatin. Cerivastatin may increase the serum concentration of diltiazem. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed.
Atenolol	Increased risk of bradycardia
Quinidine	Diltiazem may increase the serum concentration of quinidine. Monitor for changes in the therapeutic and adverse effects of quinidine if diltiazem is initiated, discontinued or dose changed.
Bromazepam	Diltiazem may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or a reductin in the bromazepam dose. Monitor for changes in the therapeutic and adverse effects of bromazepam if diltiazem is initiated, discontinued or dose changed.
Tacrolimus	Diltiazem may increase the serum concentration of tacrolimus by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of tacrolimus if diltiazem therapy is initiated, discontinued or dose changed.
Sirolimus	Increases the effect and toxicity of sirolimus
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Mesoridazine	Increased risk of cardiotoxicity and arrhythmias
Simvastatin	Diltiazem may increase the serum concentration of simvastatin. Simvastatin may increase the serum concentration of diltiazem. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed.
Ranolazine	Diltiazem may increase the serum concentration of ranolazine. Consider alternate therapy or limit ranolazine dose to 500 mg twice daily and monitor for changes in the therapeutic and adverse effects if diltiazem is initiated, discontinued or dose changed.
Tolterodine	Diltiazem may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Tipranavir	Tipranavir, co-administered with Ritonavir, may alter the concentration of Diltiazem. Monitor for efficacy and adverse/toxic effects of Diltiazem.
Ritonavir	Ritonavir increases diltiazem levels
Aprepitant	This CYP3A4 inhibitor increases the effect and toxicity of aprepitant
Trazodone	The CYP3A4 inhibitor, Diltizem, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Monitor for changes in Trazodone efficacy/toxicity if Diltiazem is initiated, discontinued or dose changed.
Voriconazole	Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of diltiazem by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of diltiazem if voriconazole is initiated, discontinued or dose changed.
Thioridazine	Increased risk of cardiotoxicity and arrhythmias
Quinidine barbiturate	Increases the effect and toxicity of quinidine
Timolol	Additive effects of decreased heart rate and contractility may occur. Increased risk of heart block.
Amlodipine	Diltiazem may increase the serum concentration of amlodipine. Concomitant therapy will result in additive hypotensive effects. Monitor for changes in the hypotensive effect of amlodipine if diltiazem is initiated, discontinued or dose changed.
Terfenadine	Increased risk of cardiotoxicity and arrhythmias
Buspirone	The calcium channel blocker, diltiazem, increases the effect and toxicity of buspirone.
Midazolam	The calcium channel blocker, diltiazem, may increase the effect and toxicity of the benzodiazepine, midazolam.
Tramadol	Diltiazem may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance.
Rifampin	Rifampin decreases levels of diltiazem
Quinupristin	This combination presents an increased risk of toxicity
Dihydroquinidine barbiturate	Increases the effect and toxicity of quinidine
Moricizine	Increased effect/toxicity of moricizine
Pindolol	Increased risk of bradycardia
Amiodarone	Increased risk of cardiotoxicity and arrhythmias
Carbamazepine	Carbamazepine may decrease the serum concentration of diltiazem by increasing its metabolism. Diltiazem may increase the serum concentration of carbamazepine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if dosages are changed.
Lovastatin	Diltiazem may increase the serum concentration of lovastatin. Lovastatin may increase the serum concentration of diltiazem. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed.
Telithromycin	Telithromycin may reduce clearance of Diltiazem. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Diltiazem if Telithromycin is initiated, discontinued or dose changed.
Atorvastatin	Diltiazem may increase the serum concentration of atorvastatin. Atorvastatin may increase the serum concentration of diltiazem. Monitor for changes in the therapeutic and adverse effects of both agents if concomitant therapy is initiated, discontinued or if doses are changed.
Thiopental	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Diltiazem, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Diltiazem if Thiopental is initiated, discontinued or dose changed.
Cisapride	Diltiazem, a moderate CYP3A4 inhibitor, may increase the serum concentration of cisapride by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of cisapride if diltiazem is initiated, discontinued or dose changed.
Atazanavir	Atazanavir may increase the therapeutic and adverse effects of diltiazem resulting in increased risk of AV block. Consider alternate therapy, a 50% dose reduction of diltiazem and monitor for changes in the therapeutic and adverse effects of diltiazem if atazanavir is initiated, discontinued or dose changed.
Metoprolol	Increased risk of bradycardia

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Targets

Voltage-dependent calcium channel gamma-1 subunit

Enzymes

Transporters

Multidrug resistance protein 1