ISRADIPINE

First approved in 1990

Details

Stereochemistry	RACEMIC
Molecular Formula	C19H21N3O5
Molecular Weight	371.3871
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=CC3=NON=C23)C(=O)OC(C)C

InChI

InChIKey=HMJIYCCIJYRONP-UHFFFAOYSA-N

InChI=1S/C19H21N3O5/c1-9(2)26-19(24)15-11(4)20-10(3)14(18(23)25-5)16(15)12-7-6-8-13-17(12)22-27-21-13/h6-9,16,20H,1-5H3

HIDE SMILES / InChI

Molecular Formula	C19H21N3O5
Molecular Weight	371.3871
Charge	0
Count

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

Description
Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cd688799-036a-4429-88d7-da84d9762d4d

Isradipine (tradenames DynaCirc, Prescal) is a calcium channel blocker of the dihydropyridine class. It is usually prescribed for the treatment of high blood pressure in order to reduce the risk of stroke and heart attack. Except for diuretic activity, the mechanism of which is not clearly understood, the pharmacodynamics effects of isradipine observed in whole animals can also be explained by calcium channel blocking activity, especially dilating effects in arterioles, which reduce systemic resistance and lower blood pressure, with a small increase in resting heart rate. Isradipine binds to calcium channels with high affinity and specificity and inhibits calcium flux into cardiac and arterial smooth muscle cells. It exhibits greater selectivity towards arterial smooth muscle cells owing to alternative splicing of the alpha-1 subunit of the channel and increased prevalence of inactive channels in smooth muscle cells. Although like other dihydropyridine calcium channel blockers, isradipine has negative inotropic effects in vitro; studies conducted in intact anesthetized animals have shown that the vasodilating effect occurs at doses lower than those do which affect contractility. In patients with normal ventricular function, isradipine's afterload reducing properties lead to some increase in cardiac output. Effects in patients with impaired ventricular function have not been fully studied. Most adverse reactions were mild and related to the vasodilatory effects of isradipine (dizziness, edema, palpitations, flushing, tachycardia), and many were transient. About 5% of isradipine patients left studies prematurely because of adverse reactions (vs. 3% of placebo patients and 6% of active control patients), principally due to headache, edema, dizziness, palpitations, and gastrointestinal disturbances.

CNS Activity

Approval Year

Targets

Primary Target	Pharmacology	Condition	Potency
Voltage-gated L-type calcium channel 92 Target ID: CHEMBL2095229 Sources: https://www.ncbi.nlm.nih.gov/pubmed/10766758	Blocker 537

Conditions

Condition	Modality	Targets	Highest Phase	Product
Hypertension 567 Sources: https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=cd688799-036a-4429-88d7-da84d9762d4d	Primary		Approved 8429	ISRADIPINE Approved Use Isradipine capsules are indicated in the management of hypertension. It may be used alone or concurrently with thiazide-type diuretics. Launch Date 2015

C_max

Value	Dose	Analyte	Population
11.44 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
29.84 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
5.89 ng/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

AUC

Value	Dose	Analyte	Population
14.52 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
31.01 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
7.31 ng × h/mL EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

T_1/2

Value	Dose	Analyte	Population
2.85 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	5 mg single, oral dose: 5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.68 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	10 mg single, oral dose: 10 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED
2.93 h EXPERIMENT https://pubmed.ncbi.nlm.nih.gov/2965165/	2.5 mg single, oral dose: 2.5 mg route of administration: Oral experiment type: SINGLE co-administered:	ISRADIPINE plasma	Homo sapiens population: HEALTHY age: ADULT sex: MALE food status: FASTED

Doses

Dose	Population	Adverse events
30 mg single, oral Highest studied dose Dose: 30 mg Route: oral Route: single Dose: 30 mg Sources: https://pubmed.ncbi.nlm.nih.gov/15610940	healthy, 27 - 44 n = 8 Health Status: healthy Age Group: 27 - 44 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/15610940	Sources: https://pubmed.ncbi.nlm.nih.gov/15610940
0.015 mg/kg single, intravenous Highest studied dose Dose: 0.015 mg/kg Route: intravenous Route: single Dose: 0.015 mg/kg Sources: https://pubmed.ncbi.nlm.nih.gov/2966552 Page: p.1103	unhealthy, 58+/-8 n = 8 Health Status: unhealthy Condition: Chest pain\| stable angina Age Group: 58+/-8 Sex: M Population Size: 8 Sources: https://pubmed.ncbi.nlm.nih.gov/2966552 Page: p.1103	Sources: https://pubmed.ncbi.nlm.nih.gov/2966552 Page: p.1103
10 mg 1 times / day multiple, oral MTD Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827	unhealthy, 58.5 n = 26 Health Status: unhealthy Condition: Parkinson's disease Age Group: 58.5 Sex: M+F Population Size: 26 Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827	Disc. AE: Drop of blood pressure, Leg edema... AEs leading to discontinuation/dose reduction: Drop of blood pressure Leg edema Dizziness Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827
100 mg single, oral (max) Overdose Dose: 100 mg Route: oral Route: single Dose: 100 mg Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	Other AEs: Lethargy, Sinus tachycardia... Other AEs: Lethargy Sinus tachycardia Hypotension Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Co-administed with:: ethanol Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	Other AEs: Flushing, Tachycardia... Other AEs: Flushing Tachycardia Electrocardiogram ST segment depression Hypotension Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display

AEs

AE	Significance	Dose	Population
Dizziness	Disc. AE	10 mg 1 times / day multiple, oral MTD Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827	unhealthy, 58.5 n = 26 Health Status: unhealthy Condition: Parkinson's disease Age Group: 58.5 Sex: M+F Population Size: 26 Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827
Drop of blood pressure	Disc. AE	10 mg 1 times / day multiple, oral MTD Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827	unhealthy, 58.5 n = 26 Health Status: unhealthy Condition: Parkinson's disease Age Group: 58.5 Sex: M+F Population Size: 26 Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827
Leg edema	Disc. AE	10 mg 1 times / day multiple, oral MTD Dose: 10 mg, 1 times / day Route: oral Route: multiple Dose: 10 mg, 1 times / day Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827	unhealthy, 58.5 n = 26 Health Status: unhealthy Condition: Parkinson's disease Age Group: 58.5 Sex: M+F Population Size: 26 Sources: https://pubmed.ncbi.nlm.nih.gov/24123224 Page: p.1823, 1826, 1827
Hypotension		100 mg single, oral (max) Overdose Dose: 100 mg Route: oral Route: single Dose: 100 mg Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Lethargy		100 mg single, oral (max) Overdose Dose: 100 mg Route: oral Route: single Dose: 100 mg Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Sinus tachycardia		100 mg single, oral (max) Overdose Dose: 100 mg Route: oral Route: single Dose: 100 mg Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Electrocardiogram ST segment depression		200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Co-administed with:: ethanol Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Flushing		200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Co-administed with:: ethanol Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Hypotension		200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Co-administed with:: ethanol Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display
Tachycardia		200 mg single, oral Overdose Dose: 200 mg Route: oral Route: single Dose: 200 mg Co-administed with:: ethanol Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display	healthy Health Status: healthy Sources: https://dailymed.nlm.nih.gov/dailymed/fda/fdaDrugXsl.cfm?setid=bf3425e0-428d-4bdb-ac9a-3b9d483df83a&type=display

Overview

CYP3A4	CYP2C9	CYP2D6	hERG
			inhibitor 1612

OverviewOther

Other Inhibitor	Other Substrate	Other Inducer
Cav1.2 45		CYP2B6 547

Drug as perpetrator

Target	Modality	Activity	Metabolite	Clinical evidence
CYP2B6 1001	inducer 1573 Sources: https://pubmed.ncbi.nlm.nih.gov/11560876/ Page: -	yes
PXR 46	activator 214 Sources: https://pubmed.ncbi.nlm.nih.gov/11560876/ Page: -	yes

Tox targets

Target	Modality	Activity	Metabolite	Clinical evidence
Cav1.2 49	inhibitor 1626 Sources: https://pubmed.ncbi.nlm.nih.gov/11487504/ Page: -
hERG 1647	inhibitor 1626 Sources: https://pubmed.ncbi.nlm.nih.gov/12007180/ Page: 1.0

Sourcing

Vendor/Aggregator	ID	URL
001 Chemical	DY570475	https://www.001chemical.com/chem/75695-93-1
3B Scientific (Wuhan) Corp	3B2-0623	http://www.3bsc.com/index/pro_info.php?id=19979
AA Blocks	AA005AF5	https://www.aablocks.com/goods/Goods/detail?id=AA005AF5
AHH Chemical co.,ltd	API-1593	http://www.ahhchemical.com/product/API-1593.html
AK Scientific, Inc. (AKSCI)	K297	http://www.aksci.com/item_detail.php?cat=K297
Aaron Chemicals	AR005B6X	http://www.aaronchem.com/75695-93-1
AbMole Bioscience	M5717	http://www.abmole.com/products/isradipine.html
Achemtek	0104-014238	http://www.achemtek.com/75695-93-1
Alfa Chemistry	AP75695931	https://reagents.alfa-chemistry.com/product/isradipine-cas-75695-93-1-16078.html
Alfa Chemistry	88977-22-4	https://www.alfa-chemistry.com/cas_88977-22-4.htm
Alsachim	1851	http://www.alsachim.com/product-C2740-glo.bal-view.html
Ambeed	A782133	https://www.ambeed.com/products/75695-93-1.html
Angene	AGN-PC-00NXL2	http://www.angenechemical.com/productshow/AGN-PC-00NXL2.html
Ark Pharm	AK163124	http://www.arkpharminc.com/products/75695-93-1.html
Aurora Fine Chemicals LLC	A17.902.891	http://online.aurorafinechemicals.com/info?ID=A17.902.891
AvaChem Scientific	6444	https://www.avachem.com/productSearch.asp?6444
Avantor Inc	101095-278	https://us.vwr.com/store/catalog/product.jsp?catalog_number=101095-278
Avantor Inc	TCI0876-25MG	https://us.vwr.com/store/product/16812954/isradipine-98-0-by-hplc
BLD Pharm	BD135467	http://www.bldpharm.com/products/75695-93-1.html
BOC Sciences	1189959-59-8	https://www.bocsci.com/isradipine-d3-cas-1189959-59-8-item-473399.html
BioChemPartner	BCP06719	http://www.biochempartner.com/75695-93-1-BCP06719
BioCrick	BCC3797	http://www.biocrick.com/Isradipine-Dynacirc-BCC3797.html
BioSynth	J-513454	https://www.biosynth.com/en/products/all-products/products/J-513454.html
CSNpharm	CSN11235	https://www.csnpharm.com/products/isradipine.html
Chem Scene	CS-2201	http://www.chemscene.com/75695-93-1.html
ChemMol	30113833	http://www.chemmol.com/chemmol/30113833.html
ChemMol	49402358	http://www.chemmol.com/chemmol/49402358.html
ChemMol	97900499	http://www.chemmol.com/chemmol/97900499.html
Chemspace	CSSB00015190191	https://chem-space.com/CSSB00015190191
Clearsynth	CS-O-11671	https://www.clearsynth.com/en/CSO11671.html
DC Chemicals	DC8772	http://www.dcchemicals.com/product_show-Isradipine.html
Debye Scientific	DB-055981	http://www.debyesci.com/cas_75695-93-1.html
Finetech	FT-0627542	http://www.finetechnology-ind.com/prod/detail/pub/75695-93-1.html
Glentham Life Sciences	GP2233	http://www.glentham.com/products/product/GP2233/
Hairui	HR107688	http://www.hairuichem.com/en/product/75695-93-1.html
Hefei Hirisun Pharmatech Co., Ltd	HR010085	http://www.hirisunpharm.com/75695-93-1.html
Hello Bio	HB1223	https://www.hellobio.com/isradipine.html
LGC Standards	LGCFOR0466.00	https://www.lgcstandards.com/US/en/p/LGCFOR0466.00
LGC Standards	MM0466.00	https://www.lgcstandards.com/US/en/p/MM0466.00
Lab Network	LN01307033	https://labnetwork.com/frontend-app/p/#!/moleculedetails/LN01307033
Matrix Scientific	146736	https://www.matrixscientific.com/146736.html
MedChem Express	HY-B0233	https://www.medchemexpress.com/isradipine.html
Molcore	MC570475	https://www.molcore.com/product/75695-93-1
MuseChem	M111496	https://www.musechem.com/product/M111496.html
OChem	21165	http://www.ocheminc.com/index.php?act=psearch&pid=695I931
Parchem	29186	http://www.parchem.com/chemical-supplier-distributor/Isradipine-019186.aspx
Renno Tech	RL04885	http://www.rennotech.com/product_show.asp?id=5134
Sigma-Aldrich	Y0000366_SIAL	https://www.sigmaaldrich.com/catalog/product/sial/y0000366?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	I6658_SIGMA	https://www.sigmaaldrich.com/catalog/product/sigma/i6658?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Sigma-Aldrich	1354207_USP	https://www.sigmaaldrich.com/catalog/product/usp/1354207?utm_source=pubchem&utm_campaign=pubchem_2017&utm_medium=referral
Smolecule	S531002	http://www.smolecule.com/products/s531002
TCI (Tokyo Chemical Industry)	I0876	http://www.tcichemicals.com/eshop/en/us/commodity/I0876/index.html
THE BioTek	bt-270129	https://www.thebiotek.com/product/inhibitors/bt-270129
Tocris	2004	https://www.tocris.com/products/isradipine_2004
TripleBond	CI0041	http://www.triplebond-canada.com/prod/1395/
Vesino Industrial Co Ltd	VA11116	http://www.vsnchem.com/goto/product/22301/
abcr GmbH	AB349125	http://www.abcr.com/shop/en/AB349125
eNovation Chemicals	D624977	https://www.enovationchem.com/ProductDetails.asp?ProductID=D624977
iChemical	EBD33321	http://www.ichemical.com/chemicals/cas-75695-93-1

PubMed

Title	Date	PubMed
Evaluation of the safety and efficacy of isradipine in elderly patients with essential hypertension. The British Isradipine Hypertension Group.	1989 Apr 17	2523644
A comparison of antihypertensive drug effects on the progression of extracranial carotid atherosclerosis. The Multicenter Isradipine Diuretic Atherosclerosis Study (MIDAS).	1990	2150640
Antihypertensive effect of isradipine administered once or twice daily on ambulatory blood pressure.	1990 Feb 15	2137666
Antiischemic and hemodynamic effects of intravenous isradipine, a new calcium antagonist, in coronary heart disease: a comparative double-blind cross-over study with nifedipine.	1990 Nov	1703598
Effect of long-term isradipine treatment on the hypertension-dependent changes in coronary arteries in spontaneously hypertensive rats.	1991	1838976
The Multicenter Isradipine/Diuretic Atherosclerosis Study: a study of the antiatherogenic properties of isradipine in hypertensive patients. MIDAS Research Group.	1991	1720479
MIDAS, the Multicenter Isradipine/Diuretic Atherosclerosis Study. Design features and baseline data.	1991 Feb	1827000
MIDAS: hypertension and atherosclerosis. A trial of the effects of antihypertensive drug treatment on atherosclerosis. MIDAS Research Group.	1992	1376828
[Multicenter study of isradipine in the treatment of hypertension].	1992 Apr	1352927
Cloning and expression of a cardiac/brain beta subunit of the L-type calcium channel.	1992 Jan 25	1370480
Isradipine treatment for hypertension in general practice in Hong Kong.	1992 Jun	1451544
MIDAS: rationale, design and descriptive data of trial patients. The MIDAS Research Group.	1994	8205295
Calcium-channel entry blocker therapy for hypertensive patients with concomitant renal impairment: a focus on isradipine.	1994 Dec	7738211
A large, prospective, open-label study of isradipine in patients with essential hypertension. The Isradipine Investigators Group.	1994 Jul-Aug	7982252
Isradipine. An update of its pharmacodynamic and pharmacokinetic properties and therapeutic efficacy in the treatment of mild to moderate hypertension.	1995 Apr	7789292
The antiatherosclerotic effect of calcium antagonists in man--what did MIDAS actually show? Multicenter Isradipine Diuretic Atherosclerosis Study.	1995 May	7670645
Responding for rewarding brain stimulation: cocaine and isradipine plus naltrexone.	1998 Oct	9738534
An open trial comparing isradipine with hydralazine and methyl dopa in the treatment of patients with severe pre-eclampsia.	1999 May	15512286
[Effects of calcium antagonists on atherosclerosis progression and intima media thickness].	2000	11002857
Hypertension after liver transplantation: a predictive role for pretreatment hemodynamics and effects of isradipine on the systemic and renal circulations.	2000 Mar	10777026
Treatment advances for cocaine-induced ischemic stroke: focus on dihydropyridine-class calcium channel antagonists.	2001 Aug	11481148
alpha 1D (Cav1.3) subunits can form l-type Ca2+ channels activating at negative voltages.	2001 Jun 22	11285265
Life-threatening isradipine poisoning in a child.	2002 Jun	12066967
Phenytoin/isradipine interaction causing severe neurologic toxicity.	2002 Sep	12196060
Isradipine enhancement of cerebral blood flow in abstinent cocaine abusers with and without chronic perfusion deficits.	2002 Summer	12202012
Effects of naltrexone and isradipine, alone or in combination, on cocaine responses in humans.	2003 Jul	12957222
Cav1.4alpha1 subunits can form slowly inactivating dihydropyridine-sensitive L-type Ca2+ channels lacking Ca2+-dependent inactivation.	2003 Jul 9	12853422
Functional characterization of the L-type Ca2+ channel Cav1.4alpha1 from mouse retina.	2004 Feb	14744918
Comparison of blood pressure control with amlodipine and controlled-release isradipine: an open-label, drug substitution study.	2005 Apr	15858400
Isradipine decreases the hemodynamic response of cocaine and methamphetamine results from two human laboratory studies: results from two human laboratory studies.	2005 Jun	15925741
Effects of isradipine, a dihydropyridine-class calcium-channel antagonist, on d-methamphetamine's subjective and reinforcing effects.	2005 Jun	15850499
Calcium channel blocker-associated small bowel angioedema.	2009 Apr	19077729
Expression and 1,4-dihydropyridine-binding properties of brain L-type calcium channel isoforms.	2009 Feb	19029287
Antagonizing L-type Ca2+ channel reduces development of abnormal involuntary movement in the rat model of L-3,4-dihydroxyphenylalanine-induced dyskinesia.	2009 Mar 15	18947822
Blocking L-type calcium channels reduced the threshold of cAMP-induced steroidogenic acute regulatory gene expression in MA-10 mouse Leydig cells.	2010 Jan	19822634
Early identification of clinically relevant drug interactions with the human bile salt export pump (BSEP/ABCB11).	2013 Dec	24014644
Anti-addiction drug ibogaine inhibits voltage-gated ionic currents: a study to assess the drug's cardiac ion channel profile.	2013 Dec 1	23707769

Patents

Sample Use Guides

In Vivo Use Guide

The recommended initial dose of isradipine is 2.5 mg b.i.d. alone or in combination with a thiazide diuretic. An antihypertensive response usually occurs within 2-3 hours. Maximal response may require 2-4 weeks. If a satisfactory reduction in blood pressure does not occur after this period, the dose may be adjusted in increments of 5 mg/day at 2-4 week intervals up to a maximum of 20 mg/day. Most patients, however, show no additional response to doses above 10 mg/day, and adverse effects are increased in frequency above 10 mg/day.

Route of Administration: Oral

In Vitro Use Guide

Unknown

Substance Class	Chemical Created by `admin` on `Fri Dec 15 17:32:20 GMT 2023` Edited by `admin` on `Fri Dec 15 17:32:20 GMT 2023`
Record UNII	YO1UK1S598
Record Status	`Validated (UNII)`
Record Version

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Name

Type

Language

ISRADIPINE

Official Name

English

ISOPROPYL METHYL (±)-4-(4-BENZOFURAZANYL)-1,4-DIHYDRO-2,6-DIMETHYL-3,5-PYRIDINEDICARBOXYLATE

Systematic Name

English

ISRADIPINE [USP MONOGRAPH]

Common Name

English

ISRADIPINE [USP-RS]

Common Name

English

isradipine [INN]

Common Name

English

DYNACIRC

Brand Name

English

Isradipine [WHO-DD]

Common Name

English

ISRADIPINE [MI]

Common Name

English

ISRADIPINE [EP MONOGRAPH]

Common Name

English

PN-200-110

Code

English

ISRADIPINE [MART.]

Common Name

English

ISRADIPINE [VANDF]

Common Name

English

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

Common Name

English

ISRADIPINE [USAN]

Common Name

English

ISRADIPINE [ORANGE BOOK]

Common Name

English

NSC-759892

Code

English

PN 200-110

Code

English

Classification Tree Code System Code

NDF-RT

N0000007556