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

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1947 39562-70-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • nitrendipine
  • nitrendipin
  • nitrepin
A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.
  • Molecular weight: 360.37
  • Formula: C18H20N2O6
  • CLOGP: 3.73
  • LIPINSKI: 0
  • HAC: 8
  • HDO: 1
  • TPSA: 107.77
  • ALOGS: -4.41
  • ROTB: 7

Drug dosage:

DoseUnitRoute
20 mg O

Approvals:

DateAgencyCompanyOrphan
Jan. 1, 1985 YEAR INTRODUCED

FDA Adverse Event Reporting System

MedDRA adverse event termLikelihood ratioLikelihood ratio thresholdPatients taking drug having adverse eventPatients taking drug not having adverse eventPatients not taking drug having adverse eventPatients not taking drug not having adverse event
Syncope 237.80 103.81 51 133 33344 4605464
Fall 155.77 103.81 43 141 78003 4560805

Pharmacologic Action:

SourceCodeDescription
ATC C08CA08 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
ATC C09BB06 CARDIOVASCULAR SYSTEM
AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM
ACE INHIBITORS, COMBINATIONS
ACE inhibitors and calcium channel blockers
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
MeSH PA D014665 Vasodilator Agents

Drug Use (View source of the data)

None

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 GATING INHIBITOR IC50 8.40 IUPHAR IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel BLOCKER UNKNOWN SCIENTIFIC LITERATURE
Cytochrome P450 2C9 Enzyme IC50 6.52 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 5.52 DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H Ion channel IC50 5.06 WOMBAT-PK
Transthyretin Secreted IC50 5.92 WOMBAT-PK
Sodium channel alpha subunits; brain (Types I, II, III) Ion channel IC50 4.44 CHEMBL
Potassium voltage-gated channel subfamily H member 2 Ion channel IC50 5 CHEMBL
Voltage-dependent calcium channel gamma-1 subunit Ion channel WOMBAT-PK
Adenosine receptor A3 GPCR Ki 5.08 WOMBAT-PK
Voltage-dependent L-type calcium channel subunit alpha-1F Ion channel GATING INHIBITOR IC50 6 IUPHAR
Intermediate conductance calcium-activated potassium channel protein 4 Ion channel BLOCKER IC50 7.60 IUPHAR
Platelet-activating factor receptor GPCR Ki 4.13 CHEMBL
Adenosine receptor A2a GPCR Ki 4.64 CHEMBL
Adenosine receptor A1 GPCR Ki 5.05 CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C Ion channel GATING INHIBITOR IC50 6 IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1S Ion channel GATING INHIBITOR IC50 6 IUPHAR

External reference:

IDSource
N0000167238 NUI
C0028127 UMLSCUI
D00629 KEGG_DRUG
7441 RXNORM
444757009 SNOMEDCT_US
005383 NDDF
9B627AW319 UNII
4739 INN_ID
DB01054 DRUGBANK_ID
CHEMBL475534 ChEMBL_ID
CHEBI:7582 CHEBI
D009568 MESH_DESCRIPTOR_UI
4507 PUBCHEM_CID
2334 IUPHAR_LIGAND_ID

Pharmaceutical products:

None