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

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1942 63675-72-9

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • BAY k-5552
  • nisoldipine
  • nisoldipin
  • zadipina
A dihydropyridine calcium channel antagonist that acts as a potent arterial vasodilator and antihypertensive agent. It is also effective in patients with cardiac failure and angina.
  • Molecular weight: 388.42
  • Formula: C20H24N2O6
  • CLOGP: 4.58
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 107.77
  • ALOGS: -4.83
  • ROTB: 8

Drug dosage:

DoseUnitRoute
20 mg O

Approvals:

DateAgencyCompanyOrphan
Feb. 2, 1995 FDA SHIONOGI INC

FDA Adverse Event Reporting System

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA07 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
FDA EPC N0000175421 Dihydropyridine Calcium Channel Blocker
FDA Chemical/Ingredient N0000007556 Dihydropyridines
FDA MoA N0000000069 Calcium Channel Antagonists
FDA PE N0000178477 Decreased Blood Pressure
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
CHEBI has role CHEBI:35674 antihypertensive agent
CHEBI has role CHEBI:35620 vasodilator agent
CHEBI has role CHEBI:50427 platelet aggregation inhibitor
CHEBI has role CHEBI:35554 cardiovascular drug
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

DiseaseRelationSNOMED_IDDOID
Hypertensive disorder indication 38341003 DOID:10763
Low blood pressure contraindication 45007003
Chronic heart failure contraindication 48447003
Coronary arteriosclerosis contraindication 53741008 DOID:3393
Hepatic failure contraindication 59927004

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation levelDissociation constantType (acidic/basic)
pKa1 2.37 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 BLOCKER UNKNOWN CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel GATING INHIBITOR IC50 7.10 IUPHAR CHEMBL
Adenosine receptor A2a GPCR Ki 5.64 DRUG MATRIX
Adenosine receptor A3 GPCR Ki 5.40 DRUG MATRIX
Cytochrome P450 1A2 Enzyme IC50 6 DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel Ki 5.34 WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.59 CHEMBL
Voltage-dependent P/Q-type calcium channel subunit alpha-1A Ion channel WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 4.64 WOMBAT-PK
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel GATING INHIBITOR IC50 8 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1D Ion channel GATING INHIBITOR IC50 7 IUPHAR

External reference:

IDSource
4020942 VUID
N0000148422 NUI
C0028116 UMLSCUI
D00618 KEGG_DRUG
4I8HAB65SZ UNII
4753 INN_ID
108524004 SNOMEDCT_US
4020942 VANDF
7435 RXNORM
386861009 SNOMEDCT_US
5178 MMSL
d03825 MMSL
147682 MMSL
004175 NDDF
DB00401 DRUGBANK_ID
CHEMBL1726 ChEMBL_ID
CHEBI:7577 CHEBI
D015737 MESH_DESCRIPTOR_UI
4499 PUBCHEM_CID
2524 IUPHAR_LIGAND_ID

Pharmaceutical products:

ProductCategoryIngredientsNDCFormQuantityRouteMarketingLabel
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2096 TABLET, FILM COATED, EXTENDED RELEASE 8.50 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2097 TABLET, FILM COATED, EXTENDED RELEASE 17 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2098 TABLET, FILM COATED, EXTENDED RELEASE 25.50 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2099 TABLET, FILM COATED, EXTENDED RELEASE 34 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2222 TABLET, FILM COATED, EXTENDED RELEASE 20 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2223 TABLET, FILM COATED, EXTENDED RELEASE 30 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0378-2224 TABLET, FILM COATED, EXTENDED RELEASE 40 mg ORAL ANDA 11 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0677-1978 TABLET, FILM COATED, EXTENDED RELEASE 8.50 mg ORAL NDA authorized generic 13 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0677-1979 TABLET, FILM COATED, EXTENDED RELEASE 17 mg ORAL NDA authorized generic 13 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0677-1980 TABLET, FILM COATED, EXTENDED RELEASE 25.50 mg ORAL NDA authorized generic 13 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 0677-1981 TABLET, FILM COATED, EXTENDED RELEASE 34 mg ORAL NDA authorized generic 13 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 54868-5931 TABLET, FILM COATED, EXTENDED RELEASE 40 mg ORAL ANDA 11 sections
SULAR HUMAN PRESCRIPTION DRUG LABEL 1 54868-5993 TABLET, FILM COATED, EXTENDED RELEASE 25.50 mg ORAL NDA 12 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 66993-472 TABLET, FILM COATED, EXTENDED RELEASE 8.50 mg ORAL NDA AUTHORIZED GENERIC 12 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 66993-473 TABLET, FILM COATED, EXTENDED RELEASE 17 mg ORAL NDA AUTHORIZED GENERIC 12 sections
Nisoldipine HUMAN PRESCRIPTION DRUG LABEL 1 66993-475 TABLET, FILM COATED, EXTENDED RELEASE 34 mg ORAL NDA AUTHORIZED GENERIC 12 sections
Sular HUMAN PRESCRIPTION DRUG LABEL 1 70515-500 TABLET, FILM COATED, EXTENDED RELEASE 8.50 mg ORAL NDA 11 sections
Sular HUMAN PRESCRIPTION DRUG LABEL 1 70515-501 TABLET, FILM COATED, EXTENDED RELEASE 17 mg ORAL NDA 11 sections
Sular HUMAN PRESCRIPTION DRUG LABEL 1 70515-503 TABLET, FILM COATED, EXTENDED RELEASE 34 mg ORAL NDA 11 sections