NICARDIPINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C26H29N3O6
Molecular Weight	479.526
Optical Activity	( + / - )
Defined Stereocenters	0 / 1
E/Z Centers	0
Charge	0

SHOW SMILES / InChI

Structure Search

SMILES

CC1=C(C(c2cccc(c2)N(=O)=O)C(=C(C)N1)C(=O)OCCN(C)Cc3ccccc3)C(=O)OC

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

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 41 Target ID: CHEMBL1940 Sources: https://www.ncbi.nlm.nih.gov/pubmed/22761000	Blocker 511		0.25 µM [IC50]
Voltage-gated L-type calcium channel 90 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2552119	Blocker 511		2.66 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 515 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf	Primary		Approved 8043	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 8043	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 1601 inhibitor 1467	inhibitor 1604 substrate 936	substrate 1118 inhibitor 1702	inhibitor 1475

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A 69 CYP2A6 627 CYP2C8 818 CYP2C19 1325 BCRP 643 MRP1 103	CYP2C8 634 CYP1A1 325 CYP1A2 972 CYP2B6 616 CYP2A6 485 CYP2C19 910 CYP2E1 606 UGT 173 P-gp 1400

Drug as perpetrator

Target	Modality	Activity
BCRP 713	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/16846237/ Page: -	yes [IC50 1 uM]
CYP2C19 1392	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.1 uM]
CYP3A4 1772	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.6 uM]
CYP2C9 1648	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 17.3 uM]
CYP2D6 1738	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 2.9 uM]
CYP1A 110	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 27 uM]
CYP2A6 659	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 29.4 uM]
CYP2C8 865	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 7.1 uM]
MRP1 166	inhibitor 3045 Sources: https://pubmed.ncbi.nlm.nih.gov/23470221/ Page: -	yes

Drug as victim

Target	Modality	Activity
CYP1A2 972	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2A6 485	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2E1 606	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP1A1 325	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2B6 616	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C19 910	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C9 936	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C8 634	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP2D6 1118	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP3A4 1601	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
P-gp 1400	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/9657975/ Page: -	yes
UGT 173	substrate 3113 Sources: https://pubmed.ncbi.nlm.nih.gov/3716455/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1507	inhibitor 1489 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
The calcium antagonist, nicardipine, inhibits antigen-stimulated and anti-IgE-induced histamine release from basophilic leucocytes of atopic asthmatics.	1985 Aug	2413722
Inhibition of histamine release from dispersed human lung and tonsillar mast cells by nicardipine and nifedipine.	1985 May	2408645
Haemodynamic analysis of the effects of nicardipine and metoprolol alone and in combination in coronary artery disease.	1985 Nov	4076202
Effects of nicardipine on left ventricular function and energetics in man.	1986 Mar	3957469
Efficacy and safety of nicardipine for chronic, stable angina pectoris: a multicenter randomized trial.	1986 Oct 1	3094355
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
Effects of calcium entry blockers on blood pressure and heart rate in neurogenic hypertensive dogs.	1987	3500100
Nicardipine in the treatment of essential hypertension controlled 6-month-study comparing nicardipine with propranolol at rest and during exercise.	1987	3319637
Comparative effects of prolonged therapy with four calcium ion antagonists (diltiazem, nicardipine, tiapamil and verapamil) in patients with chronic stable angina pectoris.	1987	3154312
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
Nicardipine and urinary retention.	1987 Dec 18	3682133
Metabolic and hemodynamic effects of nicardipine during pacing-induced angina pectoris.	1987 Feb 1	3812268
Nicardipine for systemic hypertension: effects on blood pressure and target organ function.	1987 Jun 30	3300238
The potential beneficial effect of nicardipine in a rat model of transient forebrain ischemia.	1987 May	3574682
Nicardipine causes sympathetic activation that does not involve baroreceptor reflex tachycardia in conscious sinoaortic-denervated dogs.	1987 Oct 6	3691633
Hemodynamic and cardiac metabolic changes during nicardipine-induced myocardial ischemia.	1988	3349516
Serum lipid changes in patients with mild to moderate essential hypertension taking nicardipine and propranolol.	1988 Dec	3076787
Endogenous opiate system and dihydropyridine-induced central regulation of sympathetic tone in rats.	1988 Dec 6	2851455
Calcium channel inhibitors prevent apomorphine- and oxytocin-induced penile erection and yawning in male rats.	1989 Aug 3	2806374
Intravenous nicardipine for the treatment of severe hypertension. A double-blind, placebo-controlled multicenter trial.	1989 Dec	2688586
[Antihypertensive effect and tolerability of slow-release nicardipine].	1989 Feb	2660993
[Calcium intestinal absorption in normotensive and essential hypertensive subjects before and after nicardipine].	1989 Jul	2510663
Erythromelalgia induced by nicardipine.	1989 Jul 29	2504422
Erythromelalgia induced by nicardipine.	1989 Jun 10	2503135
Haemodynamic responses to nicardipine in humans anaesthetised with halothane.	1989 May	2742097
Erythromelalgia induced by nicardipine (inverse Raynaud's phenomenon?).	1989 May 6	2502240
Nicardipine decreases blood pressure and heart rate at nucleus tractus solitarii of spontaneously hypertensive rats.	1989 Nov	2481182
Inotropic effect of nicardipine in patients with heart failure: assessment by left ventricular end-systolic pressure-volume analysis.	1989 Nov 1	2808990
Twenty-four hour ambulatory blood pressure profile of a new, sustained-release preparation of nicardipine.	1990 Apr	2285627
[Blood pressure monitoring in aged hypertensive patients treated with sustained-release nicardipine or nifedipine].	1990 Dec 8	2263931
Randomized double-blind comparison of side effects of nicardipine and nifedipine in angina pectoris. The Nicardipine Investigators Group.	1990 Feb	2405616
Acute antianginal hemodynamic effects of nicardipine in coronary artery disease.	1990 Feb	2301244
Oxytocin-induced penile erection and yawning: role of calcium and prostaglandins.	1990 Mar	2339153
Nicardipine reduces the cardio-respiratory toxicity of intravenously administered bupivacaine in rats.	1990 Nov	2253300
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
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011 Jul 14	21599003
Angioedema associated with dihydropyridine calcium-channel blockers in a child with Burkitt lymphoma.	2011 Mar 1	21330681
Deltamethrin, a type II pyrethroid insecticide, has neurotrophic effects on neurons with continuous activation of the Bdnf promoter.	2012 Feb	22079160
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).	2013 Dec	24014644
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.

Name

Type

Language

NICARDIPINE

Official Name

English

NICARDIPINE [WHO-DD]

Common Name

English

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

Systematic 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