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 555		0.25 µM [IC50]
Voltage-gated L-type calcium channel 95 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/2552119	Blocker 555		2.66 nM [IC50]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 575 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf	Primary		Approved 8583	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 1988
Chronic stable angina 10 Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/019734s027lbl.pdf	Primary		Approved 8583	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 1988

C_max

Value	Dose	Analyte	Population
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
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

AUC

Value	Dose	Analyte	Population
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
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

T_1/2

Value	Dose	Analyte	Population
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
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

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	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf	Other AEs: Hypotension, Bradycardia... Other AEs: Hypotension (marked) Bradycardia Palpitations Flushing Drowsiness Confusion Slurred speech Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf
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 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 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	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2011/019734s017lbl.pdf	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
60 mg 2 times / day multiple, oral 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	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf	Disc. AE: Angina... AEs leading to discontinuation/dose reduction: Angina Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf
60 mg 2 times / day multiple, oral 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	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf	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
60 mg 2 times / day multiple, oral 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	unhealthy Health Status: unhealthy Sources: https://www.accessdata.fda.gov/drugsatfda_docs/label/2016/020005s014lbl.pdf	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

AEs

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1946 inhibitor 2252	inhibitor 2438 substrate 1193	substrate 1388 inhibitor 2507	inhibitor 2217

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A 70 CYP2A6 879 CYP2C8 1057 CYP2C19 2057 BCRP 910 MRP1 116	CYP2C8 810 CYP1A1 389 CYP1A2 1197 CYP2B6 776 CYP2A6 626 CYP2C19 1119 CYP2E1 729 UGT 219 P-gp 2052

Drug as perpetrator

Target	Modality	Activity
BCRP 985	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/16846237/ Page: -	yes [IC50 1 uM]
CYP2C19 2141	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.1 uM]
CYP3A4 2633	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 1.6 uM]
CYP2C9 2497	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 17.3 uM]
CYP2D6 2546	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 2.9 uM]
CYP1A 122	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 27 uM]
CYP2A6 911	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 29.4 uM]
CYP2C8 1117	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes [Ki 7.1 uM]
MRP1 232	inhibitor 4027 Sources: https://pubmed.ncbi.nlm.nih.gov/23470221/ Page: -	yes

Drug as victim

Target	Modality	Activity
CYP1A2 1197	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2A6 626	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP2E1 729	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	inconclusive
CYP1A1 389	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2B6 776	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C19 1119	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C9 1193	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	poor
CYP2C8 810	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP2D6 1388	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
CYP3A4 1946	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/15863898/ Page: -	yes
P-gp 2052	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/9657975/ Page: -	yes
UGT 219	substrate 4014 Sources: https://pubmed.ncbi.nlm.nih.gov/3716455/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 2263	inhibitor 2237 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
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
CSNpharm	CSN11400	https://www.csnpharm.com/products/nicardipine.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
eNovation Chemicals	D590715	https://www.enovationchem.com/ProductDetails.asp?ProductID=D590715
eNovation Chemicals	D674858	https://www.enovationchem.com/ProductDetails.asp?ProductID=D674858
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
iChemical	EBD6545	http://www.ichemical.com/chemicals/cas-55985-32-5
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

PubMed

Title	Date	PubMed
Screening of a chemical library reveals novel PXR-activating pharmacologic compounds.	2015-01-05	25455453
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).	2013-12	24014644
A multifactorial approach to hepatobiliary transporter assessment enables improved therapeutic compound development.	2013-11	23956101
Deltamethrin, a type II pyrethroid insecticide, has neurotrophic effects on neurons with continuous activation of the Bdnf promoter.	2012-02	22079160
Profiling of a prescription drug library for potential renal drug-drug interactions mediated by the organic cation transporter 2.	2011-07-14	21599003
Angioedema associated with dihydropyridine calcium-channel blockers in a child with Burkitt lymphoma.	2011-03-01	21330681
Coronary vasomotion during dynamic exercise: influence of intravenous and intracoronary nicardipine.	1995-09	7642851
Protective effect of nicardipine treatment on renal microanatomical changes in spontaneously hypertensive rats.	1994-07	7920453
Effects of a novel dihydropyridine calcium antagonist on venous capacitance in Wistar-Kyoto rats.	1994	7924898
Profile of capsaicin-induced mouse ear oedema as neurogenic inflammatory model: comparison with arachidonic acid-induced ear oedema.	1993-12	7508328
Intravenous nicardipine in hypertensive children.	1993-09	8223797
Nifedipine and nicardipine potentiate glucagon-stimulated glycogenolysis in primary cultures of rat hepatocytes.	1993-09	7505685
[Blood pressure monitoring in aged hypertensive patients treated with sustained-release nicardipine or nifedipine].	1990-12-08	2263931
Nicardipine reduces the cardio-respiratory toxicity of intravenously administered bupivacaine in rats.	1990-11	2253300
Twenty-four hour ambulatory blood pressure profile of a new, sustained-release preparation of nicardipine.	1990-04	2285627
Oxytocin-induced penile erection and yawning: role of calcium and prostaglandins.	1990-03	2339153
Randomized double-blind comparison of side effects of nicardipine and nifedipine in angina pectoris. The Nicardipine Investigators Group.	1990-02	2405616
Acute antianginal hemodynamic effects of nicardipine in coronary artery disease.	1990-02	2301244
Intravenous nicardipine for the treatment of severe hypertension. A double-blind, placebo-controlled multicenter trial.	1989-12	2688586
Inotropic effect of nicardipine in patients with heart failure: assessment by left ventricular end-systolic pressure-volume analysis.	1989-11-01	2808990
Nicardipine decreases blood pressure and heart rate at nucleus tractus solitarii of spontaneously hypertensive rats.	1989-11	2481182
Calcium channel inhibitors prevent apomorphine- and oxytocin-induced penile erection and yawning in male rats.	1989-08-03	2806374
Erythromelalgia induced by nicardipine.	1989-07-29	2504422
[Calcium intestinal absorption in normotensive and essential hypertensive subjects before and after nicardipine].	1989-07	2510663
Erythromelalgia induced by nicardipine.	1989-06-10	2503135
Erythromelalgia induced by nicardipine (inverse Raynaud's phenomenon?).	1989-05-06	2502240
Haemodynamic responses to nicardipine in humans anaesthetised with halothane.	1989-05	2742097
[Antihypertensive effect and tolerability of slow-release nicardipine].	1989-02	2660993
Endogenous opiate system and dihydropyridine-induced central regulation of sympathetic tone in rats.	1988-12-06	2851455
Serum lipid changes in patients with mild to moderate essential hypertension taking nicardipine and propranolol.	1988-12	3076787
Hemodynamic and cardiac metabolic changes during nicardipine-induced myocardial ischemia.	1988	3349516
Nicardipine and urinary retention.	1987-12-18	3682133
Central interactions between dihydropyridines and cholinergic systems in the control of blood pressure in rat.	1987-12-01	2448012
An evaluation of the pharmacodynamics and pharmacokinetics of nicardipine combined with enalapril in essential hypertension.	1987-12	2450244
Nicardipine causes sympathetic activation that does not involve baroreceptor reflex tachycardia in conscious sinoaortic-denervated dogs.	1987-10-06	3691633
Nicardipine for systemic hypertension: effects on blood pressure and target organ function.	1987-06-30	3300238
The potential beneficial effect of nicardipine in a rat model of transient forebrain ischemia.	1987-05	3574682
Nicardipine. A review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy, in the treatment of angina pectoris, hypertension and related cardiovascular disorders.	1987-04	3297616
Metabolic and hemodynamic effects of nicardipine during pacing-induced angina pectoris.	1987-02-01	3812268
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
Efficacy and safety of nicardipine for chronic, stable angina pectoris: a multicenter randomized trial.	1986-10-01	3094355
Effects of nicardipine on left ventricular function and energetics in man.	1986-03	3957469
Haemodynamic analysis of the effects of nicardipine and metoprolol alone and in combination in coronary artery disease.	1985-11	4076202
The calcium antagonist, nicardipine, inhibits antigen-stimulated and anti-IgE-induced histamine release from basophilic leucocytes of atopic asthmatics.	1985-08	2413722
Inhibition of histamine release from dispersed human lung and tonsillar mast cells by nicardipine and nifedipine.	1985-05	2408645
[Treatment of arterial hypertension in the aged with a calcium antagonist: nicardipine].	1984-10	6441544
Antihypertensive and renal effects of nicardipine.	1984-07	6743490

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 `Mon Mar 31 18:07:46 GMT 2025` Edited by `admin` on `Mon Mar 31 18:07:46 GMT 2025`
Record UNII	CZ5312222S
Record Status	`Validated (UNII)`
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Name

Type

Language

Nicardipine

Official Name

English

PERPIDINE

Preferred 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

Nicardipine (STN)

Common Name

English

Classification Tree Code System Code

WHO-ATC

C08CA04