QuickView for Nicardipine (compound)

Summary
General Info

PubChem

PubChem Compound 197067

Name:	Nicardipine
PubChem Compound ID:	197067
Description:	A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Molecular formula:	C₂₁H₂₇ClN₂O₃
Molecular weight:	390.903 g/mol
Synonyms:	EINECS 228-279-6; NSC 407307; 20alpha-Yohimban-16beta-carboxylic acid, 17alpha-hydroxy-, methyl ester, monohydrochloride (8CI); Rauwolscine hydrochloride; alpha-Yohimbine hydrochloride; alpha-Yohimbin hydrochloride; Methyl (16beta,17alpha,20alpha)-17-hydroxyyohimban-16-carboxylate hydrochloride; EU-0101093; Yohimban-16-carboxylic acid, 17-hydroxy-, methyl ester, monohydrochloride, (16beta,17alpha,20alpha)- (9CI); 20-alpha-Yohimban-16-beta-carboxylic acid, 17-alpha-hydroxy-, methyl ester, hydrochloride. show more » EINECS 228-279-6; NSC 407307; 20alpha-Yohimban-16beta-carboxylic acid, 17alpha-hydroxy-, methyl ester, monohydrochloride (8CI); Rauwolscine hydrochloride; alpha-Yohimbine hydrochloride; alpha-Yohimbin hydrochloride; Methyl (16beta,17alpha,20alpha)-17-hydroxyyohimban-16-carboxylate hydrochloride; EU-0101093; Yohimban-16-carboxylic acid, 17-hydroxy-, methyl ester, monohydrochloride, (16beta,17alpha,20alpha)- (9CI); 20-alpha-Yohimban-16-beta-carboxylic acid, 17-alpha-hydroxy-, methyl ester, hydrochloride; 6211-32-1; Fauwolscine, hydrochloride show less «

DrugBank

Identification

Name:	Nicardipine
Name (isomeric):	DB00622
Drug Type:	small molecule
Description:	A potent calcium channel blockader with marked vasodilator action. It has antihypertensive properties and is effective in the treatment of angina and coronary spasms without showing cardiodepressant effects. It has also been used in the treatment of asthma and enhances the action of specific antineoplastic agents.
Synonyms:	Nicardipine HCl; Nicardipinum [INN-Latin]; Nicardipino [INN-Spanish]
Brand:	Cardene SR, Cardene, Cardene IV
Category:	Vasodilator Agents, Antiarrhythmic Agents, Calcium Channel Blockers, Antihypertensive Agents, Dihydropyridines
CAS number:	55985-32-5

Pharmacology

Indication:	Used for the management of patients with chronic stable angina and for the treatment of hypertension.
Pharmacology:	Nicardipine, a dihydropyridine 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. Nicardipine is similar to other peripheral vasodilators. Nicardipine inhibits the influx of extra cellular calcium across the myocardial and... show more » Nicardipine, a dihydropyridine 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. Nicardipine is similar to other peripheral vasodilators. Nicardipine 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:	By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes The decrease in intracellular calcium inhibits the contractile processes of the m... show more » By deforming the channel, inhibiting ion-control gating mechanisms, and/or interfering with the release of calcium from the sarcoplasmic reticulum, nicardipine inhibits the influx of extracellular calcium across the myocardial and vascular smooth muscle cell membranes 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 «
Absorption:	While nicardipine is completely absorbed, it is subject to saturable first pass metabolism and the systemic bioavailability is about 35% following a 30 mg oral dose at steady state.
Protein binding:	>95%
Biotransformation:	Nicardipine HCl is metabolized extensively by the liver.
Route of elimination:	Nicardipine has been shown to be rapidly and extensively metabolized by the liver.
Half Life:	8.6 hours
Clearance:	0.4 L/hr∙kg [Following infusion]
Toxicity:	Oral LD₅₀ Rat = 184 mg/kg, Oral LD₅₀ Mouse = 322 mg/kg
Affected organisms:	Humans and other mammals

Interactions

Food interaction:

Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.

Take without regard to meals.

Drug interaction:

Zafirlukast	Nicardipine, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of zafirlukast. Consider alternate therapy or monitor for changes in zafirlukast therapeutic and adverse effects if nicardipine is initiated, discontinued or dose changed.
Vinorelbine	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of Vinorelbine by decreasing its metabolism. Consider alternate therapy to avoid Vinorelbine toxicity. Monitor for changes in the therapeutic and adverse effects of Vinorelbine if Nicardipine is initiated, discontinued or dose changed.
Tipranavir	Tipranavir, co-administered with Ritonavir, may alter the concentration of Nicardipine. Monitor for efficacy and adverse/toxic effects of Nicardipine.
Vardenafil	Nicardipine, a strong CYP3A4 inhibitor, may reduce the metabolism and clearance of Vardenafil. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Vardenafil.
Teniposide	The strong CYP3A4 inhibitor, Nicardipine, may decrease the metabolism and clearance of Teniposide, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Teniposide if Nicardipine is initiated, discontinued or dose changed.

Zafirlukast	Nicardipine, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of zafirlukast. Consider alternate therapy or monitor for changes in zafirlukast therapeutic and adverse effects if nicardipine is initiated, discontinued or dose changed.
Vinorelbine	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of Vinorelbine by decreasing its metabolism. Consider alternate therapy to avoid Vinorelbine toxicity. Monitor for changes in the therapeutic and adverse effects of Vinorelbine if Nicardipine is initiated, discontinued or dose changed.
Tipranavir	Tipranavir, co-administered with Ritonavir, may alter the concentration of Nicardipine. Monitor for efficacy and adverse/toxic effects of Nicardipine.
Vardenafil	Nicardipine, a strong CYP3A4 inhibitor, may reduce the metabolism and clearance of Vardenafil. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Vardenafil.
Teniposide	The strong CYP3A4 inhibitor, Nicardipine, may decrease the metabolism and clearance of Teniposide, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Teniposide if Nicardipine is initiated, discontinued or dose changed.
Tramadol	Nicardipine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Nicardipine may decrease the effect of Tramadol by decreasing active metabolite production.
Verapamil	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of Veramapil, a CYP3A4 substrate, by decreasing its metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Verapamil if Nicardipine is initiated, discontinued or dose changed.
Cyclosporine	Nicardipine increases the effect and toxicity of cyclosporine
Temsirolimus	Nicardipine may inhibit the metabolism and clearance of Temsirolimus. Concomitant therapy should be avoided.
Zopiclone	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of zopiclone by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zopiclone if nicardipine is initiated, discontinued or dose changed.
Torasemide	Nicardipine, a strong CYP2C9 inhibitor, may increase the serum concentration of Torasemide, a CYP2C9 substrate, by decreasing Torasemide metabolism and clearance. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of Torasemide if Nicardipine is initiated, discontinued or dose changed.
Tadalafil	Nicardipine may reduce the metabolism of Tadalafil. Concomitant therapy should be avoided if possible due to high risk of Tadalafil toxicity.
Dantrolene	Nicardipine may increase the serum concentration of dantrolene by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of dantrolene if nicardipine is initiated, discontinued or dose changed.
Tamsulosin	Nicardipine, a CYP3A4/2D6 inhibitor, may decrease the metabolism and clearance of Tamsulosin, a CYP3A4/2D6 substrate. Monitor for changes in therapeutic/adverse effects of Tamsulosin if Nicardipine is initiated, discontinued, or dose changed.
Topotecan	The p-glycoprotein inhibitor, Nicardipine, may increase the bioavailability of oral Topotecan. A clinically significant effect is also expected with IV Topotecan. Concomitant therapy should be avoided.
Tolterodine	Nicardipine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity.
Telithromycin	Co-administration may result in altered plasma concentrations of Nicardipine and/or Telithromycin. Consider alternate therapy or monitor the therapeutic/adverse effects of both agents.
Tacrolimus	The calcium channel blocker, Nicardipine, may increase the blood concentration of Tacrolimus. Monitor for changes in the therapeutic/toxic effects of Tacrolimus if Nicardipine therapy is initiated, discontinued or altered.
Vincristine	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of Vincristine by decreasing its metabolism. Consider alternate therapy to avoid Vincristine toxicity. Monitor for changes in the therapeutic and adverse effects of Vincristine if Nicardipine is initiated, discontinued or dose changed.
Vinblastine	Nicardipine, a strong CYP3A4 inhibitor, may decrease the metabolism of Vinblastine. Consider alternate therapy to avoid Vinblastine toxicity. Monitor for changes in the therapeutic/adverse effects of Vinblastine if Nicardipine is initiated, discontinued or dose changed.
Treprostinil	Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use.
Trazodone	The CYP3A4 inhibitor, Nicardipine, may increase Trazodone efficacy/toxicity by decreasing Trazodone metabolism and clearance. Consider alternate therapy or monitor for changes in Trazodone efficacy/toxicity if Nicardipine is initiated, discontinued or dose changed.
Voriconazole	Nicardipine, a strong CYP2C9 inhibitor, may increase the serum concentration of voriconazole by decreasing its metabolism. Voriconazole, a strong CYP3A4 inhibitor, may increase the serum concentration of nicardipine by decreasing its metabolism. Monitor for changes in the therapeutic and adverse effects of voriconazole and nicardipine if concomitant therapy is initiated, discontinued or doses are changed.
Tiagabine	The strong CYP3A4 inhibitor, Nicardipine, may decrease the metabolism and clearance of Tiagabine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in the therapeutic/adverse effects of Tiagabine if Nicardipine is initiated, discontinued or dose changed.
Warfarin	Nicardipine, a strong CYP2C9 inhibitor, may decrease the metabolism of warfarin. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of warfarin if nicardipine is initiated, discontinued or dose changed.
Thiopental	The CYP3A4 inducer, Thiopental, may increase the metabolism and clearance of Nicardipine, a CYP3A4 substrate. Monitor for changes in the therapeutic/adverse effects of Nicardipine if Thiopental is initiated, discontinued or dose changed.
Bromazepam	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of bromazepam by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of bromazepam if nicardipine is initiated, discontinued or dose changed. Dosage adjustments may be required.
Terfenadine	Increased risk of cardiotoxicity and arrhythmias
Trimethoprim	The strong CYP2C9 inhibitor, Nicardipine, may decrease the metabolism and clearance of Trimethoprim, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimethoprim if Nicardipine is initiated, discontinued or dose changed.
Quinupristin	This combination presents an increased risk of toxicity
Tolbutamide	Nicardipine, a strong CYP2C9 inhibitor, may decrease the metabolism and clearance of Tolbutamide, a CYP2C9 substrate. Consider alternate therapy or monitor for changes in Tolbutamide therapeutic and adverse effects if Nicardipine is initiated, discontinued or dose changed.
Tamoxifen	Nicardipine may increase the serum concentration of Tamoxifen by decreasing its metabolism and clearance. Nicardipine may also decrease the therapeutic effect of Tamoxifen by decreasing active metabolite production. Monitor for changes in the therapeutic/adverse effects of Tamoxifen if Nicardipine is initiated, discontinued or dose changed.
Venlafaxine	Nicardipine, a CYP3A4 inhibitor, may decrease the metabolism and clearance of Venlafaxine, a CYP3A4 substrate. Monitor for changes in therapeutic/adverse effects of Venlafaxine if Nicardipine is initiated, discontinued, or dose changed.
Zolpidem	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of zolpidem by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zolpidem if nicardipine is initiated, discontinued or dose changed.
Zonisamide	Nicardipine, a strong CYP3A4 inhibitor, may increase the serum concentration of zonisamide by decreasing its metabolism. Consider alternate therapy or monitor for changes in the therapeutic and adverse effects of zonisamide if nicardipine is initiated, discontinued or dose changed.
Trimipramine	The strong CYP3A4 inhibitor, Nicardipine, may decrease the metabolism and clearance of Trimipramine, a CYP3A4 substrate. Consider alternate therapy or monitor for changes in therapeutic and adverse effects of Trimipramine if Nicardipine is initiated, discontinued or dose changed.