NISOLDIPINE

Details

Stereochemistry	RACEMIC
Molecular Formula	C20H24N2O6
Molecular Weight	388.4144
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=C(C=CC=C2)[N+]([O-])=O)C(=O)OCC(C)C

InChI

InChIKey=VKQFCGNPDRICFG-UHFFFAOYSA-N

InChI=1S/C20H24N2O6/c1-11(2)10-28-20(24)17-13(4)21-12(3)16(19(23)27-5)18(17)14-8-6-7-9-15(14)22(25)26/h6-9,11,18,21H,10H2,1-5H3

HIDE SMILES / InChI

Molecular Formula	C20H24N2O6
Molecular Weight	388.4144
Charge	0
Count

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

Description
Sources: S. Kazda, J.-P. Stasch, C. Hirth. Experimental Pharmacology of Nisoldipine: Perspectives from Long-Term Studies pp 3-12/ Nisoldipine 1987 Editors: P.G. Hugenholtz, J. Meyer ISBN: 978-3-540-18394-5 (Print) 978-3-642-73010-8 (Online) Springer Berlin Heidelberg | http://link.springer.com/chapter/10.1007/978-3-642-73010-8_1
Curator's Comment: Description was created based on several sources, including: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bcdeafac-f4ef-4dda-bdb7-1f819c33bb76 Pharmaceutical Innovation: Revolutionizing Human Health/ Editors. R. Landau, B. Achilladelis, A. Scriabine Chemical Heritage Foundation, 1999 -P. 408 ISBN 0-941901-21-1

Nisoldipine is a 1,4-dihydropyridine derivative with an outstanding vascular selectivity. As a specific calcium antagonist, it shortens the action potential and causes electromechanical uncoupling in ventricular myocardium. However, this effect, resulting in a negative inotropic action, appears at 100–1000 times higher concentrations of nisoldipine in comparison with its inhibition of calcium-dependent vascular contractions. Detailed analyses of pharmacological effects revealed additional properties such as enhancement of sodium excretion, an interaction with the reninangiotensin-aldosterone system and a protective effect against acute renal ischaemia, that may contribute to its therapeutic efficacy. Nisoldipine was developed at Bayer then licensed to Zeneca and marketed in the United States as SULAR. SULAR is indicated for the treatment of hypertension. It may be used alone or in combination with other antihypertensive agents. The mechanism of the therapeutic effect of nisoldipine is complex. It involves a decrease of the total peripheral vascular resistance (reduction of afterload) and an increase in coronary blood flow. Moreover, nisoldipine obviously normalises the impaired volume homoeostasis by improving renal function and thus reduces the need for activation of the ANP system. In the advanced stages of hypertension, nisoldipine prevents deleterious calcium overload and the resulting tissue damage.

CNS Activity

Originator

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-gated L-type calcium channel 91 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/3154674	Antagonist 2760		0.04 nM [Kd]

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 549 Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=bcdeafac-f4ef-4dda-bdb7-1f819c33bb76	Primary		Approved 8360	SULAR Approved Use Nisoldipine extended-release tablets are indicated for the treatment of hypertension. They may be used alone or in combination with other antihypertensive agents. Launch Date 7.916832E11

C_max

Value	Dose	Analyte	Population
1.44 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1634646/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
2.26 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1634646/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
3.4 ng/mL EXPERIMENT https://link.springer.com/chapter/10.1007/978-3-642-73010-8_6	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

AUC

Value	Dose	Analyte	Population
19.06 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1634646/	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
29.42 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1634646/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
54 mg × h/mL/(mg dose/kg) EXPERIMENT https://link.springer.com/chapter/10.1007/978-3-642-73010-8_6	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:	NISOLDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

T_1/2

Value	Dose	Co-administered	Analyte	Population
12.61 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/1634646/	20 mg 1 times / day multiple, oral dose: 20 mg route of administration: Oral experiment type: MULTIPLE co-administered:		NISOLDIPINE plasma	Homo sapiens population: UNHEALTHY age: ADULT sex: FEMALE / MALE food status: FASTED
9.7 h EXPERIMENT https://link.springer.com/chapter/10.1007/978-3-642-73010-8_6	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		NISOLDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

F_unbound

Value	Dose	Co-administered	Analyte	Population
0.27% EXPERIMENT https://link.springer.com/chapter/10.1007/978-3-642-73010-8_6	20 mg single, oral dose: 20 mg route of administration: Oral experiment type: SINGLE co-administered:		NISOLDIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: UNKNOWN

Doses

Dose	Population	Adverse events
40 mg 1 times / day multiple, oral (max) Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Co-administed with:: atenolol(50 mg four times daily) Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/	unhealthy, adult n = 503 Health Status: unhealthy Condition: hypertension Age Group: adult Sex: M+F Population Size: 503 Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/	Disc. AE: Ischemia, Myocardial infarction... AEs leading to discontinuation/dose reduction: Ischemia (13.6%) Myocardial infarction (grade 5, 2 patients) Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/

AEs

AE	Significance	Dose	Population
Ischemia	13.6% Disc. AE	40 mg 1 times / day multiple, oral (max) Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Co-administed with:: atenolol(50 mg four times daily) Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/	unhealthy, adult n = 503 Health Status: unhealthy Condition: hypertension Age Group: adult Sex: M+F Population Size: 503 Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/
Myocardial infarction	grade 5, 2 patients Disc. AE	40 mg 1 times / day multiple, oral (max) Recommended Dose: 40 mg, 1 times / day Route: oral Route: multiple Dose: 40 mg, 1 times / day Co-administed with:: atenolol(50 mg four times daily) Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/	unhealthy, adult n = 503 Health Status: unhealthy Condition: hypertension Age Group: adult Sex: M+F Population Size: 503 Sources: https://pubmed.ncbi.nlm.nih.gov/7726128/

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
substrate 1709	substrate 1010	substrate 1193	inhibitor 1599

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
CYP1A2 1509 ASBT 5 OCTN2 66	CYP1A2 1032 CYP2C19 985 CYP2E1 648	CYP1A2 689 CYP2C11 14 CYP2D1 2 CYP3A1 4

Drug as perpetrator

Target	Modality	Activity
CYP1A2 1673	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/10805063/ Page: -	yes [Ki 1.97 uM]
ASBT 6	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/20599790/ Page: -	yes
CYP1A2 1673	inducer 1542 Sources: https://pubmed.ncbi.nlm.nih.gov/28756727/ Page: -	yes
CYP2C11 15	inducer 1542 Sources: https://pubmed.ncbi.nlm.nih.gov/28756727/ Page: -	yes
CYP2D1 8	inducer 1542 Sources: https://pubmed.ncbi.nlm.nih.gov/28756727/ Page: -	yes
CYP3A1 5	inducer 1542 Sources: https://pubmed.ncbi.nlm.nih.gov/28756727/ Page: -	yes
OCTN2 71	inhibitor 3240 Sources: https://pubmed.ncbi.nlm.nih.gov/20599790/ Page: -	yes

Drug as victim

Target	Modality	Activity	Metabolite
CYP1A2 1032	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP1A2 1032	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M7 1
CYP1A2 1032	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M9 2
CYP2C19 985	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP2C19 985	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M7 1
CYP2C19 985	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M9 2
CYP2C9 1010	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP2D6 1193	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP2D6 1193	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M7 1
CYP2D6 1193	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M9 2
CYP2E1 648	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP3A4 1709	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes
CYP3A4 1709	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M7 1
CYP3A4 1709	substrate 3326 Sources: https://pubmed.ncbi.nlm.nih.gov/24816159/ Page: -	yes	M9 2

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
hERG 1632	inhibitor 1613 Sources: https://pubmed.ncbi.nlm.nih.gov/19399628/ Page: -

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY564824	https://www.001chemical.com/chem/63675-72-9
3B Scientific (Wuhan) Corp	3B2-0601	http://www.3bsc.com/index/pro_info.php?id=19957
3B Scientific (Wuhan) Corp	3B1-00313	http://www.3bsc.com/index/pro_info.php?id=20525
AA Blocks	AA003T1M	https://www.aablocks.com/goods/Goods/detail?id=AA003T1M
AHH Chemical co.,ltd	API-1571	http://www.ahhchemical.com/product/API-1571.html
AHH Chemical co.,ltd	MT-00026	http://www.ahhchemical.com/product/MT-00026.html
AK Scientific, Inc. (AKSCI)	J10291	http://www.aksci.com/item_detail.php?cat=J10291
Aaron Chemicals	AR003TTE	http://www.aaronchem.com/63675-72-9
AbMole Bioscience	M3462	http://www.abmole.com/products/nisoldipine.html
Achemtek	0104-002010	http://www.achemtek.com/63675-72-9
Acorn PharmaTech	ACN-034408	http://www.acornpharmatech.com/
Alfa Chemistry	AP63675729	https://reagents.alfa-chemistry.com/product/nisoldipine-cas-63675-72-9-14426.html
Ambeed	A127509	https://www.ambeed.com/products/63675-72-9.html
Angel Pharmatech	AG131533	http://www.angelpharmatech.com/63675-72-9.html
Angene	AGN-PC-0511LH	http://www.angenechemical.com/productshow/AGN-PC-0511LH.html
Ark Pharm	AK143131	http://www.arkpharminc.com/products/63675-72-9.html
Aurora Fine Chemicals LLC	A13.140.992	http://online.aurorafinechemicals.com/info?ID=A13.140.992
Aurum Pharmatech LLC	KM0774	http://www.Aurumpharmatech.com/Product/ProductDetails/KM0774
AvaChem Scientific	1636	http://www.avachem.com/productSearch.asp?1636
Avantor Inc	100571-150	https://us.vwr.com/store/catalog/product.jsp?catalog_number=100571-150
BLD Pharm	BD54662	http://www.bldpharm.com/products/63675-72-9.html
BOC Sciences	1219795-47-7	https://www.bocsci.com/nisoldipine-d4-2-nitrophenyl-d4-cas-1219795-47-7-item-307396.html
BioChemPartner	BCP22696	http://www.biochempartner.com/63675-72-9-BCP22696
BioCrick	BCC4809	http://www.biocrick.com/Nisoldipine-BCC4809.html
Boerchem	BC204167	http://www.boerchem.com/?product_34328.html
CSNpharm	CSN17095	https://www.csnpharm.com/products/nisoldipine.html
Chem Scene	CS-1131	http://www.chemscene.com/63675-72-9.html
ChemMol	30101985	http://www.chemmol.com/chemmol/30101985.html
ChemMol	44001727	http://www.chemmol.com/chemmol/44001727.html
ChemMol	49401456	http://www.chemmol.com/chemmol/49401456.html
ChemMol	99122901	http://www.chemmol.com/chemmol/99122901.html
Chemenu	CM110416	http://www.chemenu.com/products/CM110416
Chemspace	CSSB00000693939	https://chem-space.com/CSSB00000693939
Clearsynth	CS-O-30680	https://www.clearsynth.com/en/CSO30680.html
Combi-Blocks	QA-7818	http://www.combi-blocks.com/cgi-bin/find.cgi?QA-7818
DAOGE BIOPHARMA	DG21-14144	https://www.daogechem.com/product/63675-72-9.html
DC Chemicals	DC9108	http://www.dcchemicals.com/product_show-Nisoldipine.html
Finetech	FT-0601599	http://www.finetechnology-ind.com/prod/detail/pub/63675-72-9.html
Glentham Life Sciences	GP4494	http://www.glentham.com/products/product/GP4494/
Hairui	HR138684	http://www.hairuichem.com/en/product/63675-72-9.html
Hefei Hirisun Pharmatech Co., Ltd	HR011300	http://www.hirisunpharm.com/63675-72-9.html
LGC Standards	DRE-A15530500ME-100	https://www.lgcstandards.com/US/en/p/DRE-A15530500ME-100
LGC Standards	DRE-C15530500	https://www.lgcstandards.com/US/en/p/DRE-C15530500
Lab Network	LN00847886	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN00847886
MedChem Express	HY-17402	https://www.medchemexpress.com/Nisoldipine.html
Molcore	MC564824	https://www.molcore.com/product/63675-72-9
MuseChem	I004404	https://www.musechem.com/product/I004404.html
OChem	4379	http://www.ocheminc.com/index.php?act=psearch&pid=675N729
Sigma-Aldrich	N0165_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/n0165?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	N0641_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/n0641?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S537263	http://www.smolecule.com/products/s537263
TCI (Tokyo Chemical Industry)	N0900	http://www.tcichemicals.com/eshop/en/us/commodity/N0900/index.html
THE BioTek	bt-277162	https://www.thebiotek.com/product/inhibitors/bt-277162
Yuhao Chemical	JZ0205	http://www.chemyuhao.com/63675-72-9.html
abcr GmbH	AB505779	http://www.abcr.com/shop/en/AB505779
eNovation Chemicals	D491518	https://www.enovationchem.com/ProductDetails.asp?ProductID=D491518
mcule	MCULE-5009799152	https://mcule.com/MCULE-5009799152/

PubMed

Title	Date	PubMed
The hypotensive effect of nisoldipine in renovascular hypertensive rats.	1986 Dec	3471895
Alteration of left ventricular diastolic filling in hypertensive patients: effects of nitrendipine and atenolol.	1986 Sep	3769959
Renal effects of 1,4-dihydropyridines in animal models of hypertension and renal failure.	1987	2441191
Comparative antianginal effects of nisoldipine and nifedipine in patients with chronic stable angina.	1987 Feb	3544754
Effects of nisoldipine on left ventricular function during exercise or cold pressor stress.	1987 Nov	3450520
Differential effects of 1,4-dihydropyridine calcium channel blockers: therapeutic implications.	1987 Nov	3323259
Monotherapy with the calcium channel antagonist nisoldipine for systemic hypertension and comparison with diuretic drugs.	1987 Sep 15	3661439
The acute effects of intravenous nisoldipine on left ventricular function 24 to 72 hours after uncomplicated acute myocardial infarction.	1988 Dec	3154643
Nisoldipine. A preliminary review of its pharmacodynamic and pharmacokinetic properties, and therapeutic efficacy in the treatment of angina pectoris, hypertension and related cardiovascular disorders.	1988 Dec	3065058
The initial hemodynamic response to newer antihypertensive agents at rest and during exercise: review of visacor, doxazosin, nisoldipine, tiapamil, perindoprilat, pinacidil, dilevalol, and carvedilol.	1990 Aug	1964580
Effects of nisoldipine on stress-induced changes in haemodynamics and plasma catecholamines in normotensives and hypertensives.	1990 Dec	2096212
[Responses of plasma eicosanoids and hemodynamics to myocardial ischemia and the salutary effect of calcium entry blocker].	1990 Feb	2329180
Hemodynamic mechanisms of antianginal action of calcium channel blocker nisoldipine in dynamic exercise-induced angina.	1990 Jun	2344682
Usefulness of oral nisoldipine for stable angina pectoris. The Nisoldipine Multicenter Angina Study Group.	1991 Oct 15	1927911
The acute effects of intravenous nisoldipine on left ventricular function within 24 h after acute myocardial infarction.	1992 Dec	1289100
Improved diastolic function with the calcium antagonist nisoldipine (coat-core) in patients post myocardial infarction: results of the DEFIANT study. Doppler Flow and Echocardiography in Functional cardiac Insufficiency: Assessment of Nisoldipine Therapy.	1992 Nov	1464339
Cardiovascular effects of nisoldipine in essential hypertension.	1994 Feb	8150600
Acute effects of intravenous nisoldipine on left ventricular function after acute myocardial infarction.	1994 May	7947377
The effects of nisoldipine on carotid artery stiffness and left ventricular functions.	1995 Sep	8558767
Nisoldipine improves ventricular function in rats with ischemic heart failure.	1995 Sep	8523445
Plasma endothelin-1 concentrations in patients with coronary artery disease during stress test before and after nisoldipine administration.	1996	8742913
Nisoldipine CC: clinical experience in hypertension.	1997	9118169
Effects of nisoldipine on cytosolic calcium, platelet aggregation, and coagulation/fibrinolysis in patients with coronary artery disease.	1997 Jun	9194537
Effects of nisoldipine and/or enalapril on left ventricular function and exercise capacity in patients with recent anterior myocardial infarction and mild cardiac dysfunction.	1997 Mar	9060793
Efficacy and tolerability of nisoldipine coat-core formulation in the treatment of essential hypertension: The South African Multicenter ANCHOR Study. Ambulatory Nisoldipine Coat-Core Hypertension Outpatient Response (ANCHOR) Investigators.	1997 Mar	9056681
Nisoldipine CC and lisinopril alone or in combination for treatment of mild to moderate systemic hypertension. Canadian Nisoldipine CC Hypertension Trial Group.	1997 Sep	9358963
New evidence on the prevention of cardiovascular events in hypertensive patients with type 2 diabetes.	1998	9736437
Protective effect of nisoldipine on dipyridamole-induced myocardial ischemia: correlation with exercise electrocardiography.	1998	9649927
Nisoldipine selectively induces coronary vasodilation and improves mild myocardial ischemia in dogs: a potential role of cellular acidosis.	1998 Dec	10410823
A comparison of nisoldipine coat-core and felodipine in the treatment of mild-to-moderate hypertension.	1998 Jun	9744143
Differential effects of morning and evening dosing of nisoldipine ER on circadian blood pressure and heart rate.	1999 Aug	10480474
Rapid-release and coat-core formulations of nisoldipine in treatment of hypertension, angina, and heart failure.	1999 Nov-Dec	11720635
Functional embryonic cardiomyocytes after disruption of the L-type alpha1C (Cav1.2) calcium channel gene in the mouse.	2000 Dec 15	10973973
Inhibition of human cytochrome P450 enzymes by 1,4-dihydropyridine calcium antagonists: prediction of in vivo drug-drug interactions.	2000 Feb-Mar	10805063
Interaction of digoxin with antihypertensive drugs via MDR1.	2002 Feb 15	11895100
Intensive blood pressure control reduces the risk of cardiovascular events in patients with peripheral arterial disease and type 2 diabetes.	2003 Feb 11	12578880
Block of cardiac delayed-rectifier and inward-rectifier K+ currents by nisoldipine.	2003 Nov	14530219
Enhanced expression of L-type Cav1.3 calcium channels in murine embryonic hearts from Cav1.2-deficient mice.	2003 Oct 17	12900400
Comparative efficacy and safety of nisoldipine extended-release (ER) and amlodipine (CESNA-III study) in African American patients with hypertension.	2003 Sep	12944032
Ca(V)1.2 calcium channel dysfunction causes a multisystem disorder including arrhythmia and autism.	2004 Oct 1	15454078
The effect of beta-carotene on the photostability of nisoldipine.	2005 Apr	15834448
Prediction of genotoxicity of chemical compounds by statistical learning methods.	2005 Jun	15962942
Pharmacokinetics of oral doses of telmisartan and nisoldipine, given alone and in combination, in patients with essential hypertension.	2007 Mar	17322141
Calcium channel blocker-associated small bowel angioedema.	2009 Apr	19077729
FDA-approved drugs and other compounds tested as inhibitors of human glutathione transferase P1-1.	2013 Sep 5	23769903

Patents

Sample Use Guides

In Vivo Use Guide

The dosage of SULAR (nisoldipine tablet, film coated, extended release) must be adjusted to each patient's needs. Therapy usually should be initiated with 17 mg orally once daily, then increased by 8.5 mg per week or longer intervals, to attain adequate control of blood pressure. Usual maintenance dosage is 17 to 34 mg once daily. Blood pressure response increases over the 8.5 - 34 mg daily dose range but adverse event rates also increase. Doses beyond 34 mg once daily are not recommended. SULAR has been used safely with diuretics, ACE inhibitors, and beta-blocking agents. Patients over age 65, or patients with impaired liver function are expected to develop higher plasma concentrations of nisoldipine. Their blood pressure should be monitored closely during any dosage adjustment. A starting dose not exceeding 8.5 mg daily is recommended in these patient groups. SULAR tablets should be administered orally once daily. SULAR should be taken on an empty stomach (1 hour before or 2 hours after a meal). Grapefruit products should be avoided before and after dosing. SULAR is an extended release dosage form and tablets should be swallowed whole, not bitten, divided or crushed.

Route of Administration: Oral

In Vitro Use Guide

Nisoldipine depressed in a dose dependent manner the spontaneous rhythmic contractions displayed by the human coronary artery preparations and at 1 nM abolished these contractions. Nisoldipine was twenty times more potent than nifedipine as an inhibitor of increase in tone induced by depolarization (100 mM K+). The rhythmic activity induced by serotonin (10μM) was more sensitive to nisoldipine than to nifedipine.

Substance Class	Chemical Created by `admin` on `Thu Jul 06 23:11:25 UTC 2023` Edited by `admin` on `Thu Jul 06 23:11:25 UTC 2023`
Record UNII	4I8HAB65SZ
Record Status	`Validated (UNII)`
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Name

Type

Language

NISOLDIPINE

Official Name

English

NISOLDIPINE [MART.]

Common Name

English

3,5-PYRIDINEDICARBOXYLIC ACID, 1,4-DIHYDRO-2,6-DIMETHYL-4-(2-NITROPHENYL)-, METHYL 2-METHYLPROPYL ESTER, (±)-

Common Name

English

NISOLDIPINE [ORANGE BOOK]

Common Name

English

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

Systematic Name

English

NISOLDIPIN

Brand Name

English

BAYMYCARD

Brand Name

English

SULAR

Brand Name

English

NISOCOR

Brand Name

English

(±)-NISOLDIPINE

Common Name

English

NISOLDIPINE [JAN]

Common Name

English

nisoldipine [INN]

Common Name

English

NISOLDIPINE [USAN]

Common Name

English

METHYL 2-METHYLPROPYL-1,4-DIHYDRO-2,6-DIMETHYL-4-(2-NITROPHENYL)-3,5-PYRIDINEDICARBOXYLATE, DL-

Common Name

English

(±)-BAY-K-5552

Common Name

English

NISOLDIPINE [VANDF]

Common Name

English

NSC-759106

Code

English

NISOLDIPINE (STN)

Brand Name

English

NISOLDIPINE [USP-RS]

Common Name

English

Nisoldipine [WHO-DD]

Common Name

English

NISOLDIPINE [MI]

Common Name

English

BAY-K-5552

Code

English

GEOMATRIX 16E

Brand Name

English

BAY K 5552

Code

English

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

Common Name

English

Classification Tree Code System Code

WHO-VATC

QC08CA07