NICARDIPINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C26H29N3O6
Molecular Weight	479.525
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

COC(=O)C1=C(C)NC(C)=C(C1C2=CC(=CC=C2)[N+]([O-])=O)C(=O)OCCN(C)CC3=CC=CC=C3

InChI

InChIKey=ZBBHBTPTTSWHBA-UHFFFAOYSA-N

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

HIDE SMILES / InChI

Molecular Formula	C26H29N3O6
Molecular Weight	479.525
Charge	0
Count

Stereochemistry	RACEMIC
Additional Stereochemistry	No
Defined Stereocenters	0 / 1
E/Z Centers	0
Optical Activity	( + / - )

Description
Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf
Curator's Comment: description was created based on several sources, including https://www.drugbank.ca/drugs/DB00622 | https://www.drugs.com/cdi/nicardipine.html | https://www.ncbi.nlm.nih.gov/pubmed/2772808 | http://reference.medscape.com/drug/cardene-iv-nicardipine-342377

Nicardipine is a potent calcium channel blockader with marked vasodilator action used to treat high blood pressure and angina. 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.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-gated L-type calcium channel alpha-1C subunit 44 Target ID: CHEMBL1940 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22761000	Blocker 534		0.25 µM [IC50]
Voltage-gated L-type calcium channel 91 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2552119	Blocker 534		2.66 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 549 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf	Primary		Approved 8360	CARDENE Approved Use I. Stable Angina Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina). They may be used alone or in combination with beta-blockers. II. Hypertension Nicardipine hydrochloride capsules are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive drugs. In administering nicardipine hydrochloride it is important to be aware of the relatively large peak to trough differences in blood pressure effect. (See .) DOSAGE AND ADMINISTRATION Launch Date 5.9866559E11
Chronic stable angina 10 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf	Primary		Approved 8360	CARDENE Approved Use I. Stable Angina Nicardipine hydrochloride capsules are indicated for the management of patients with chronic stable angina (effort-associated angina). They may be used alone or in combination with beta-blockers. II. Hypertension Nicardipine hydrochloride capsules are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive drugs. In administering nicardipine hydrochloride it is important to be aware of the relatively large peak to trough differences in blood pressure effect. (See .) DOSAGE AND ADMINISTRATION Launch Date 5.9866559E11

C_max

Value	Dose	Analyte	Population
35.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	1 mg/h steady-state, intravenous dose: 1 mg/h route of administration: Intravenous experiment type: STEADY-STATE co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
64.1 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	2 mg/h other, intravenous dose: 2 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
183.9 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	4 mg/h other, intravenous dose: 4 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
18.8 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	0.5 mg/h other, intravenous dose: 0.5 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
1426.2 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	1 mg/h steady-state, intravenous dose: 1 mg/h route of administration: Intravenous experiment type: STEADY-STATE co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
2996.1 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	2 mg/h other, intravenous dose: 2 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
7510.7 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	4 mg/h other, intravenous dose: 4 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
846.3 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	0.5 mg/h other, intravenous dose: 0.5 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

T_1/2

Value	Dose	Analyte	Population
11.3 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	1 mg/h steady-state, intravenous dose: 1 mg/h route of administration: Intravenous experiment type: STEADY-STATE co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
14 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	2 mg/h other, intravenous dose: 2 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
17.9 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	4 mg/h other, intravenous dose: 4 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN
20.6 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2357865	0.5 mg/h other, intravenous dose: 0.5 mg/h route of administration: Intravenous experiment type: OTHER co-administered:	NICARDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
5% DRUG LABEL https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf			NICARDIPINE plasma	Homo sapiens population: UNKNOWN age: UNKNOWN sex: UNKNOWN food status: UNKNOWN

Doses

Dose	Population	Adverse events
2160 mg single, oral Overdose Dose: 2160 mg Route: oral Route: single Dose: 2160 mg Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21	unhealthy n = 1 Health Status: unhealthy Condition: Hypertension Population Size: 1 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21	Other AEs: Slurred speech, Hypotension... Other AEs: Slurred speech Hypotension (marked) Bradycardia Palpitations Flushing Drowsiness Confusion Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21
100 mg 2 times / day multiple, oral Recommended Dose: 100 mg, 2 times / day Route: oral Route: multiple Dose: 100 mg, 2 times / day Sources: https://www.medicines.org.uk/emc/product/3322/smpc#gref	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.medicines.org.uk/emc/product/3322/smpc#gref	Sources: https://www.medicines.org.uk/emc/product/3322/smpc#gref
15 mg/h single, intravenous (max) Recommended Dose: 15 mg/h Route: intravenous Route: single Dose: 15 mg/h Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21	unhealthy n = 144 Health Status: unhealthy Condition: Hypertension Population Size: 144 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21	Disc. AE: Hypotension, Headache... AEs leading to discontinuation/dose reduction: Hypotension Headache Tachycardia Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf Page: p.21
60 mg 2 times / day multiple, oral (max) Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.10	unhealthy n = 322 Health Status: unhealthy Condition: Hypertension Population Size: 322 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.10	Disc. AE: Rash, Diarrhea... AEs leading to discontinuation/dose reduction: Rash (0.9%) Diarrhea (0.9%) Tachycardia (0.9%) Blurred vision (0.6%) Chest pain (0.6%) Face edema (0.6%) Myocardial infarct (0.6%) Vasodilatation (0.6%) Vomiting (0.6%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.10
60 mg 2 times / day multiple, oral (max) Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.9	unhealthy n = 322 Health Status: unhealthy Condition: Hypertension Population Size: 322 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.9	Disc. AE: Headache, Palpitation... AEs leading to discontinuation/dose reduction: Headache (2.5%) Palpitation (2.2%) Dizziness (1.9%) Asthenia (1.9%) Pedal edema (1.2%) Nausea (1.2%) Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.9
60 mg 2 times / day multiple, oral (max) Studied dose Dose: 60 mg, 2 times / day Route: oral Route: multiple Dose: 60 mg, 2 times / day Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.5	unhealthy Health Status: unhealthy Condition: Hypertension Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.5	Disc. AE: Angina... AEs leading to discontinuation/dose reduction: Angina Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf Page: p.5

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709 inhibitor 1579	inhibitor 1752 substrate 1010	substrate 1193 inhibitor 1837	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A 72 CYP2A6 704 CYP2C8 901 CYP2C19 1463 BCRP 691 MRP1 106	CYP2C8 688 CYP1A1 348 CYP1A2 1032 CYP2B6 660 CYP2A6 523 CYP2C19 985 CYP2E1 648 UGT 187 P-gp 1527

Drug as perpetrator

Target	Modality	Activity
BCRP 765	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/16846237/ Page: -	yes [IC50 1 uM]
CYP2C19 1537	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.1 uM]
CYP3A4 1909	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.6 uM]
CYP2C9 1803	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 17.3 uM]
CYP2D6 1875	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 2.9 uM]
CYP1A 121	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 27 uM]
CYP2A6 736	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 29.4 uM]
CYP2C8 955	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 7.1 uM]
MRP1 172	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/23470221/ Page: -	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1032	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2A6 523	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2E1 648	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP1A1 348	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2B6 660	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C19 985	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C9 1010	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C8 688	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP2D6 1193	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP3A4 1709	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
P-gp 1527	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/9657975/ Page: -	yes
UGT 187	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/3716455/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://www.koreascience.or.kr/article/JAKO201032755114842.page Page: -

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY560485	https://www.001chemical.com/chem/55985-32-5
3B Scientific (Wuhan) Corp	3B2-0617	http://www.3bsc.com/index/pro_info.php?id=19973
AHH Chemical co.,ltd	API-1587	http://www.ahhchemical.com/product/API-1587.html
AK Scientific, Inc. (AKSCI)	V1328	http://www.aksci.com/item_detail.php?cat=V1328
Ambeed	A407345	https://www.ambeed.com/products/55985-32-5.html
Aurora Fine Chemicals LLC	K02.796.495	http://online.aurorafinechemicals.com/info?ID=K02.796.495
Axon MedChem	3254	https://www.axonmedchem.com/product/3254
BioChemPartner	BCP21397	http://www.biochempartner.com/55985-32-5-BCP21397
Boerchem	BC215912	http://www.boerchem.com/?product_36607.html
CSNpharm	CSN11400	https://www.csnpharm.com/products/nicardipine.html
Chem Scene	CS-3685	http://www.chemscene.com/55985-32-5.html
ChemMol	30107614	http://www.chemmol.com/chemmol/30107614.html
ChemMol	44005421	http://www.chemmol.com/chemmol/44005421.html
ChemMol	49425013	http://www.chemmol.com/chemmol/49425013.html
ChemMol	99106622	http://www.chemmol.com/chemmol/99106622.html
ChemShuttle	187919	https://www.chemshuttle.com/catalogsearch/result/?q=55985-32-5&cat=
Chemspace	CSSB00000053284	https://chem-space.com/CSSB00000053284
Clearsynth	CS-O-01985	http://www.clearsynth.com/en/CSO01985.html
DC Chemicals	DC25090	http://www.dcchemicals.com/product_show-DC23090.html
Debye Scientific	DB-052833	http://www.debyesci.com/cas_55985-32-5.html
Excenen	EX-A4680	https://www.excenen.com/searchresultlist.php?id=EX-A4680
Finetech	FT-0630688	http://www.finetechnology-ind.com/prod/detail/pub/55985-32-5.html
Glentham Life Sciences	GP0799	http://www.glentham.com/products/product/GP0799/
Hairui	HR109252	http://www.hairuichem.com/en/product/55985-32-5.html
Hefei Hirisun Pharmatech Co., Ltd	HR010675	http://www.hirisunpharm.com/55985-32-5.html
Lab Network	LN01342879	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01342879
MedChem Express	HY-12515	https://www.medchemexpress.com/Nicardipine.html
Molcore	MC560485	https://www.molcore.com/product/55985-32-5
MuseChem	I004092	https://www.musechem.com/product/I004092.html
OChem	5154	http://www.ocheminc.com/index.php?act=psearch&pid=985N325
Smolecule	S537152	http://www.smolecule.com/products/s537152
THE BioTek	bt-277061	https://www.thebiotek.com/product/inhibitors/bt-277061
Yuhao Chemical	LQ5354	http://www.chemyuhao.com/55985-32-5.html
eNovation Chemicals	D590715	https://www.enovationchem.com/ProductDetails.asp?ProductID=D590715
eNovation Chemicals	D674858	https://www.enovationchem.com/ProductDetails.asp?ProductID=D674858
iChemical	EBD6545	http://www.ichemical.com/chemicals/cas-55985-32-5

PubMed

Title	Date	PubMed
Antihypertensive and renal effects of nicardipine.	1984 Jul	6743490
[Treatment of arterial hypertension in the aged with a calcium antagonist: nicardipine].	1984 Oct	6441544
Inhibition of histamine release from dispersed human lung and tonsillar mast cells by nicardipine and nifedipine.	1985 May	2408645
A comparison of nine calcium ion antagonists and propranolol: exercise tolerance, heart rate and ST-segment changes in patients with chronic stable angina pectoris.	1987	3653222
Nicardipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in the treatment of angina pectoris, hypertension and related cardiovascular disorders.	1987 Apr	3297616
An evaluation of the pharmacodynamics and pharmacokinetics of nicardipine combined with enalapril in essential hypertension.	1987 Dec	2450244
Central interactions between dihydropyridines and cholinergic systems in the control of blood pressure in rat.	1987 Dec 1	2448012
Hemodynamic and cardiac metabolic changes during nicardipine-induced myocardial ischemia.	1988	3349516
Erythromelalgia induced by nicardipine.	1989 Jul 29	2504422
The influence of nicardipine on left ventricular hemodynamics and compliance in patients with coronary heart disease.	1990	1369704
Inhibitory effects of diltiazem, verapamil, nifedipine, and nicardipine on sympathetic tachycardia in decentralized hearts of anesthetized dogs.	1990 Oct	1706810
Heterogeneous interference of nicardipine, verapamil, and diltiazem with forearm arteriolar responsiveness to adrenergic stimulation in hypertensive patients.	1991 Jul	2053555
Combined treatment with MK-801 and nicardipine reduces global ischemic damage in the gerbil.	1992 Jan	1731424
Nicardipine in the prevention of spasm-induced neurological deficits after subarachnoid hemorrhage: a dose-ranging study.	1992 Jul	1615378
Hemodynamic effects of nicardipine-induced hypotension during enflurane/nitrous oxide anesthesia in man.	1992 Oct	15278512
Profile of capsaicin-induced mouse ear oedema as neurogenic inflammatory model: comparison with arachidonic acid-induced ear oedema.	1993 Dec	7508328
Intravenous nicardipine in hypertensive children.	1993 Sep	8223797
Nifedipine and nicardipine potentiate glucagon-stimulated glycogenolysis in primary cultures of rat hepatocytes.	1993 Sep	7505685
Effects of a novel dihydropyridine calcium antagonist on venous capacitance in Wistar-Kyoto rats.	1994	7924898
Protective effect of nicardipine treatment on renal microanatomical changes in spontaneously hypertensive rats.	1994 Jul	7920453
Coronary vasomotion during dynamic exercise: influence of intravenous and intracoronary nicardipine.	1995 Sep	7642851
Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions.	2000 Feb-Mar	10805063
Calmodulin kinases II and IV and calcineurin are involved in leukemia inhibitory factor-induced cardiac hypertrophy in rats.	2000 Nov 10	11073891
Profound sinus bradycardia after intravenous nicardipine.	2002 Jul	12088942
Inactivation of aconitase during the apoptosis of mouse cerebellar granule neurons induced by a deprivation of membrane depolarization.	2003 Feb 15	12548706
Dihydropyridine Ca2+ channel antagonists and agonists block Kv4.2, Kv4.3 and Kv1.4 K+ channels expressed in HEK293 cells.	2003 Jun	12788813
Ameliorative effect of NC-1900, a new AVP4-9 analog, through vasopressin V1A receptor on scopolamine-induced impairments of spatial memory in the eight-arm radial maze.	2003 Mar	12646291
Inhibitory effects of carvedilol on calcium channels in vascular smooth muscle cells.	2003 Nov	14711191
Automated screening with confirmation of mechanism-based inactivation of CYP3A4, CYP2C9, CYP2C19, CYP2D6, and CYP1A2 in pooled human liver microsomes.	2005 Aug	15860655
Prediction of genotoxicity of chemical compounds by statistical learning methods.	2005 Jun	15962942
Inhibitory effects of nicardipine to cytochrome P450 (CYP) in human liver microsomes.	2005 May	15863898
The cGMP/protein kinase G pathway contributes to dihydropyridine-sensitive calcium response and cytokine production in TH2 lymphocytes.	2006 May 5	16533816
Effects of nicardipine-induced hypotension on cerebrovascular carbon dioxide reactivity in patients with diabetes mellitus under sevoflurane anesthesia.	2007	17458638
Treatment of cerebral vasospasm with biocompatible controlled-release systems for intracranial drug delivery.	2008 Dec	19057314
Comparison between atosiban and nicardipine in inducing hypotension during in-utero transfers for threatening premature delivery.	2010 Jun	19696681
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011 Jul 14	21599003
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.	2013 Nov	23956101
Screening of a chemical library reveals novel PXR-activating pharmacologic compounds.	2015 Jan 5	25455453

Patents

Sample Use Guides

In Vivo Use Guide

Hypertension. PO: 20-40 mg (conventional) q8hr or 30-60 mg (extended release) q12hr; IV: 5 mg/hr by slow infusion (50 mL/hr) initially; may be increased by 2.5 mg/hr every 15 minutes; not to exceed 15 mg/hr Chronic Stable Angina. 20-40 mg (conventional) PO q8h

Route of Administration: Other

In Vitro Use Guide

The growth effects of EGF and nicardipine on U251MG cultured in serum-free and serum-supplemented (10% fetal bovine serum, FBS) medium respectively were observed by MTT colorimeritric analysis. EGF significantly enhanced the growth of U251MG cells in a dose-dependent manner in serum-free medium. The maximal effect was seen at 20 ng/ml. The effects of EGF approximated those obtained in 10% FBS. Nicardipine decreased U251MG cell proliferation, especially in serum-supplemented medium, and completely blocked the growth-stimulated effects of EGF. The combined effects of EGF (10 ng/ml) and nicardipine equaled those of nicardipine alone.

Substance Class	Chemical Created by `admin` on `Wed Jul 05 23:14:24 UTC 2023` Edited by `admin` on `Wed Jul 05 23:14:24 UTC 2023`
Record UNII	CZ5312222S
Record Status	`Validated (UNII)`
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Name

Type

Language

NICARDIPINE

Official Name

English

2-(BENZYLMETHYLAMINO)ETHYL METHYL 1,4-DIHYDRO-2,6-DIMETHYL-4-(M-NITROPHENYL)-3,5-PYRIDINEDICARBOXYLATE

Systematic Name

English

Nicardipine [WHO-DD]

Common Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, 3-METHYL 5-(2-(METHYL(PHENYLMETHYL)AMINO)ETHYL) ESTER

Systematic Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(3-NITROPHENYL)-, METHYL 2-(METHYL(PHENYLMETHYL)AMINO)ETHYL ESTER

Common Name

English

NICARDIPINE [VANDF]

Common Name

English

NICARDIPINE [MI]

Common Name

English

(±)-NICARDIPINE

Common Name

English

nicardipine [INN]

Common Name

English

PERPIDINE

Brand Name

English

NICARDIPINE (STN)

Common Name

English

Classification Tree Code System Code

WHO-ATC

C08CA04