isradipine Indications/Contra | FAERs | Orange Book | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1511 75695-93-1

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • isradipine
  • dynacrine
  • isradipin
  • isrodipine
A potent antagonist of CALCIUM CHANNELS that is highly selective for VASCULAR SMOOTH MUSCLE. It is effective in the treatment of chronic stable angina pectoris, hypertension, and congestive cardiac failure.
  • Molecular weight: 371.39
  • Formula: C19H21N3O5
  • CLOGP: 3.92
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 103.55
  • ALOGS: -3.21
  • ROTB: 6

Drug dosage:

DoseUnitRoute
5 mg O
5 mg P

Approvals:

DateAgencyCompanyOrphan
Dec. 20, 1990 FDA SMITHKLINE BEECHAM

FDA Adverse Event Reporting System

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA03 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
FDA MoA N0000000069 Calcium Channel Antagonists
FDA EPC N0000175421 Dihydropyridine Calcium Channel Blocker
FDA Chemical/Ingredient N0000007556 Dihydropyridines
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Angina pectoris off-label use 194828000
Raynaud's phenomenon off-label use 266261006
Myocardial infarction contraindication 22298006 DOID:5844
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Disease of liver contraindication 235856003 DOID:409
Peripheral edema contraindication 271809000

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.23 Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

TargetClassPharosUniProtActionTypeActivity value
(-log[M])
Mechanism
action
Bioact sourceMoA source
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel GATING INHIBITOR IC50 9.30 IUPHAR CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER WOMBAT-PK CHEMBL
Nuclear receptor subfamily 1 group I member 2 Nuclear hormone receptor WOMBAT-PK
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 5.51 WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel WOMBAT-PK
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel IC50 6.97 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel IC50 6.66 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel GATING INHIBITOR IC50 7.50 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1F Unclassified GATING INHIBITOR IC50 6.70 IUPHAR

External reference:

IDSource
4019560 VUID
N0000147660 NUI
C0071304 UMLSCUI
D00349 KEGG_DRUG
108533002 SNOMEDCT_US
4019560 VANDF
73302 MMSL
33910 RXNORM
386862002 SNOMEDCT_US
4939 MMSL
d00270 MMSL
003570 NDDF
DB00270 DRUGBANK_ID
CHEMBL1648 ChEMBL_ID
CHEBI:6073 CHEBI
YO1UK1S598 UNII
5724 INN_ID
D017275 MESH_DESCRIPTOR_UI
3784 PUBCHEM_CID
4488 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 16252-539 CAPSULE 2.50 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 16252-540 CAPSULE 5 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 42806-263 CAPSULE 2.50 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 42806-264 CAPSULE 5 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 50268-454 CAPSULE 2.50 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 50268-455 CAPSULE 5 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 60429-385 CAPSULE 2.50 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 60429-386 CAPSULE 5 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 68151-1333 CAPSULE 5 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 68462-807 CAPSULE 2.50 mg ORAL ANDA 11 sections
Isradipine HUMAN PRESCRIPTION DRUG LABEL 1 68462-808 CAPSULE 5 mg ORAL ANDA 11 sections