lacidipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | BioActivity |

Stem definitionDrug idCAS RN
calcium channel blockers, nifedipine derivatives 1532 103890-78-4

Description:

MoleculeDescription

Molfile Inchi Smiles

Synonyms:

  • lacidipine
  • lacipil
  • lacirex
  • GR-43659X
  • motens
  • Molecular weight: 455.55
  • Formula: C26H33NO6
  • CLOGP: 5.93
  • LIPINSKI: 1
  • HAC: 7
  • HDO: 1
  • TPSA: 90.93
  • ALOGS: -5.31
  • ROTB: 11

Drug dosage:

DoseUnitRoute
4 mg O

ADMET properties:

PropertyValueReference
BA (Bioavailability) 18 % Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H

Approvals:

None

FDA Adverse Event Reporting System (Female)

None

FDA Adverse Event Reporting System (Male)

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
Procalcitonin abnormal 58.72 41.45 10 978 302 29573237
Encephalomalacia 49.93 41.45 10 978 743 29572796
Acquired macroglossia 47.54 41.45 6 982 18 29573521
PO2 decreased 43.34 41.45 10 978 1449 29572090

FDA Adverse Event Reporting System (Geriatric)

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
Procalcitonin abnormal 61.58 31.35 10 1590 305 64496827
Encephalomalacia 49.18 31.35 10 1590 1081 64496051
Drug interaction 48.88 31.35 52 1548 362031 64135101
International normalised ratio increased 40.73 31.35 25 1575 79142 64417990
PO2 decreased 40.11 31.35 10 1590 2703 64494429
Lymphocyte count increased 38.55 31.35 11 1589 4964 64492168
Scrotal oedema 36.75 31.35 8 1592 1199 64495933
Acquired macroglossia 36.23 31.35 6 1594 207 64496925
PCO2 decreased 34.55 31.35 9 1591 2893 64494239
Device related sepsis 33.75 31.35 10 1590 5145 64491987

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

SourceCodeDescription
ATC C08CA09 CARDIOVASCULAR SYSTEM
CALCIUM CHANNEL BLOCKERS
SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS
Dihydropyridine derivatives
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

Drug Use | Suggest Off label Use Form| |View source of the data|

None




🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

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-gated L-type calcium channel Ion channel BLOCKER SCIENTIFIC LITERATURE SCIENTIFIC LITERATURE
Cytochrome P450 3A4 Enzyme IC50 6.05 DRUG MATRIX
Sodium-dependent noradrenaline transporter Transporter Ki 5.25 DRUG MATRIX
D(3) dopamine receptor GPCR Ki 5.68 DRUG MATRIX
Adenosine receptor A3 GPCR Ki 5.64 DRUG MATRIX
Cytochrome P450 2C19 Enzyme IC50 5.70 DRUG MATRIX
Thromboxane-A synthase Enzyme IC50 5.77 DRUG MATRIX
Cytochrome P450 2C9 Enzyme IC50 5.70 DRUG MATRIX
Androgen receptor Transcription factor Ki 5.58 DRUG MATRIX

External reference:

IDSource
4025250 VUID
N0000179165 NUI
D04657 KEGG_DRUG
4025250 VANDF
C0064568 UMLSCUI
CHEBI:135737 CHEBI
CHEMBL460291 ChEMBL_ID
DB09236 DRUGBANK_ID
C060285 MESH_SUPPLEMENTAL_RECORD_UI
11740 IUPHAR_LIGAND_ID
6093 INN_ID
260080034N UNII
5311217 PUBCHEM_CID
28382 RXNORM
004453 NDDF
319299000 SNOMEDCT_US
395764001 SNOMEDCT_US

Pharmaceutical products:

None