Chemical: Drug
nicardipine

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PharmGKB contains no Clinical Variants that meet the highest level of criteria.

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Overview

Generic Names
  • Nicardipine HCl
  • Nicardipino [INN-Spanish]
  • Nicardipinum [INN-Latin]
Trade Names
  • Cardene
  • Cardene IV
  • Cardene SR
Brand Mixture Names

PharmGKB Accession Id

PA450620

Type(s):

Drug

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.

Source: Drug Bank

Indication

Used for the management of patients with chronic stable angina and for the treatment of hypertension.

Source: Drug Bank

Other Vocabularies

Information pulled from DrugBank has not been reviewed by PharmGKB.

Pharmacology, Interactions, and Contraindications

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 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.

Source: Drug Bank

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 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.

Source: Drug Bank

Food Interaction

Grapefruit and grapefruit juice should be avoided throughout treatment. Grapefruit can increase serum levels of this product.|Take without regard to meals.

Source: Drug Bank

Absorption, Distribution, Metabolism, Elimination & Toxicity

Biotransformation

Nicardipine HCl is metabolized extensively by the liver.

Source: Drug Bank

Protein Binding

>95%

Source: Drug Bank

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.

Source: Drug Bank

Half-Life

8.6 hours

Source: Drug Bank

Toxicity

Oral LD 50 Rat = 184 mg/kg, Oral LD 50 Mouse = 322 mg/kg

Source: Drug Bank

Clearance

Source: Drug Bank

Route of Elimination

Nicardipine has been shown to be rapidly and extensively metabolized by the liver.

Source: Drug Bank

Volume of Distribution

  • 8.3 L/kg

Source: Drug Bank

Chemical Properties

Chemical Formula

C26H29N3O6

Source: Drug Bank

Isomeric SMILES

CC1=C([C@H](C(=C(N1)C)C(=O)OCCN(C)CC2=CC=CC=C2)C3=CC(=CC=C3)[N+](=O)[O-])C(=O)OC

Source: Drug Bank

COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1

Source: Drug Bank

Canonical SMILES

COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-]

Source: Drug Bank

Average Molecular Weight

479.525

Source: Drug Bank

Monoisotopic Molecular Weight

479.205635675

Source: Drug Bank

SMILES

COC(=O)C1=C(C)NC(C)=C(C1C1=CC(=CC=C1)[N+]([O-])=O)C(=O)OCCN(C)CC1=CC=CC=C1

Source: Drug Bank

InChI String

InChI=1S/C26H29N3O6/c1-17-22(25(30)34-4)24(20-11-8-12-21(15-20)29(32)33)23(18(2)27-17)26(31)35-14-13-28(3)16-19-9-6-5-7-10-19/h5-12,15,24,27H,13-14,16H2,1-4H3

Source: Drug Bank

Genes that are associated with this drug in PharmGKB's database based on (1) variant annotations, (2) literature review, (3) pathways or (4) information automatically retrieved from DrugBank, depending on the "evidence" and "source" listed below.

Curated Information ?

Drug Targets

Gene Description
ABCB1 (source: Drug Bank)
ABCG2 (source: Drug Bank)
ADRA1A (source: Drug Bank)
ADRA1B (source: Drug Bank)
ADRA1D (source: Drug Bank)
CACNA1C (source: Drug Bank)
CACNA1D (source: Drug Bank)
CACNA2D1 (source: Drug Bank)
CACNB2 (source: Drug Bank)
CALM3 (source: Drug Bank)
CHRM1 (source: Drug Bank)
CHRM2 (source: Drug Bank)
CHRM3 (source: Drug Bank)
CHRM4 (source: Drug Bank)
CHRM5 (source: Drug Bank)
PDE1A (source: Drug Bank)
PDE1B (source: Drug Bank)

Drug Interactions

Interaction Description
bromazepam - nicardipine 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. (source: Drug Bank)
cyclosporine - nicardipine Nicardipine increases the effect and toxicity of cyclosporine (source: Drug Bank)
cyclosporine - nicardipine Nicardipine increases the effect and toxicity of cyclosporine (source: Drug Bank)
dantrolene - nicardipine 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. (source: Drug Bank)
nicardipine - cyclosporine Nicardipine increases the effect and toxicity of cyclosporine (source: Drug Bank)
nicardipine - cyclosporine Nicardipine increases the effect and toxicity of cyclosporine (source: Drug Bank)
nicardipine - quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
nicardipine - quinupristin This combination presents an increased risk of toxicity (source: Drug Bank)
nicardipine - terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
nicardipine - terfenadine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
quinupristin - nicardipine This combination presents an increased risk of toxicity (source: Drug Bank)
tadalafil - nicardipine Nicardipine may reduce the metabolism of Tadalafil. Concomitant therapy should be avoided if possible due to high risk of Tadalafil toxicity. (source: Drug Bank)
tamoxifen - nicardipine 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. (source: Drug Bank)
tamoxifen - nicardipine 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. (source: Drug Bank)
tamsulosin - nicardipine 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. (source: Drug Bank)
tamsulosin - nicardipine 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. (source: Drug Bank)
telithromycin - nicardipine 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. (source: Drug Bank)
teniposide - nicardipine 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. (source: Drug Bank)
terfenadine - nicardipine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
terfenadine - nicardipine Increased risk of cardiotoxicity and arrhythmias (source: Drug Bank)
thiopental - nicardipine 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. (source: Drug Bank)
thiopental - nicardipine 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. (source: Drug Bank)
tiagabine - nicardipine 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. (source: Drug Bank)
tipranavir - nicardipine Tipranavir, co-administered with Ritonavir, may alter the concentration of Nicardipine. Monitor for efficacy and adverse/toxic effects of Nicardipine. (source: Drug Bank)
tolbutamide - nicardipine 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. (source: Drug Bank)
tolbutamide - nicardipine 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. (source: Drug Bank)
tolterodine - nicardipine Nicardipine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
tolterodine - nicardipine Nicardipine may decrease the metabolism and clearance of Tolterodine. Adjust Tolterodine dose and monitor for efficacy and toxicity. (source: Drug Bank)
topotecan - nicardipine 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. (source: Drug Bank)
torasemide - nicardipine 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. (source: Drug Bank)
tramadol - nicardipine Nicardipine may increase Tramadol toxicity by decreasing Tramadol metabolism and clearance. Nicardipine may decrease the effect of Tramadol by decreasing active metabolite production. (source: Drug Bank)
trazodone - nicardipine 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. (source: Drug Bank)
trazodone - nicardipine 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. (source: Drug Bank)
treprostinil - nicardipine Additive hypotensive effect. Monitor antihypertensive therapy during concomitant use. (source: Drug Bank)
trimethoprim - nicardipine 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. (source: Drug Bank)
trimipramine - nicardipine 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. (source: Drug Bank)
vardenafil - nicardipine 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. (source: Drug Bank)
venlafaxine - nicardipine 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. (source: Drug Bank)
verapamil - nicardipine 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. (source: Drug Bank)
vincristine - nicardipine 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. (source: Drug Bank)
vinorelbine - nicardipine 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. (source: Drug Bank)
voriconazole - nicardipine 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. (source: Drug Bank)
warfarin - nicardipine 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. (source: Drug Bank)
zafirlukast - nicardipine 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. (source: Drug Bank)
zolpidem - nicardipine 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. (source: Drug Bank)
zonisamide - nicardipine 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. (source: Drug Bank)
zopiclone - nicardipine 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. (source: Drug Bank)

Curated Information ?

Relationships from National Drug File - Reference Terminology (NDF-RT)

May Treat
Contraindicated With

Publications related to nicardipine: 8

No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
The genetics of pro-arrhythmic adverse drug reactions. British journal of clinical pharmacology. 2014. Petropoulou Evmorfia, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available VIP No VIP available
Very important pharmacogene summary: ABCB1 (MDR1, P-glycoprotein). Pharmacogenetics and genomics. 2011. Hodges Laura M, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Coprescription of tamoxifen and medications that inhibit CYP2D6. Journal of clinical oncology : official journal of the American Society of Clinical Oncology. 2010. Sideras Kostandinos, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Dihydropyridines: evaluation of their current and future pharmacological applications. Drug discovery today. 2009. Edraki Najmeh, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Machine learning methods and docking for predicting human pregnane X receptor activation. Chemical research in toxicology. 2008. Khandelwal Akash, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Structure, function and regulation of P-glycoprotein and its clinical relevance in drug disposition. Xenobiotica; the fate of foreign compounds in biological systems. 2008. Zhou S-F. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Relative activation of human pregnane X receptor versus constitutive androstane receptor defines distinct classes of CYP2B6 and CYP3A4 inducers. The Journal of pharmacology and experimental therapeutics. 2007. Faucette Stephanie R, et al. PubMed
No Dosing Guideline available No Drug Label available No Clinical Annotation available No Variant Annotation available No VIP available No VIP available
Calcium channel modulators of the dihydropyridine family are human pregnane X receptor activators and inducers of CYP3A, CYP2B, and CYP2C in human hepatocytes. Drug metabolism and disposition: the biological fate of chemicals. 2001. Drocourt L, et al. PubMed

LinkOuts

Web Resource:
Wikipedia
National Drug Code Directory:
0703-8315-03
DrugBank:
DB00622
KEGG Compound:
C07264
PubChem Compound:
4474
PubChem Substance:
182381
46504482
IUPHAR Ligand:
2559
Drugs Product Database (DPD):
2162733
BindingDB:
50017085
ChemSpider:
4319
Therapeutic Targets Database:
DAP000486

Clinical Trials

These are trials that mention nicardipine and are related to either pharmacogenetics or pharmacogenomics.

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NURSA Datasets

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No NURSA datasets available.

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Sources for PharmGKB drug information: DrugBank, PubChem.