lacidipine 🐶 Veterinary Use | Indications/Contra | FAERs-F | FAERs-M | Orange Bk | PK/Tox | Related Drugs | 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

Predicted pharmacokinetic/toxicological properties (PK-AZ):

PropertyDescriptionValueUnitConfidenceSimilarity
kinase-safety-class ACVR2A,ACVR2B,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DDR1,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K21,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK2,PDK4,PDPK1,PIK3CB,PIK3CD,PIM2,PRKDC,STK33,TEK,TTK,ZAP70 40
kinase-selectivity-class AXL,BRAF,GRK2,PDK4,PIK3CD,STK33 6
pfas-class PFAS structural alert (1 = True, 0 = False) 0

Approvals:

None

FDA Adverse Event Reporting System (Female)

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
Lower urinary tract symptoms 54.36 35.20 7 865 107 90627468

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 70.33 30.82 12 1353 383 42619587
Encephalomalacia 58.49 30.82 12 1353 1049 42618921
Lymphocyte count increased 56.42 30.82 15 1350 4049 42615921
PO2 decreased 53.28 30.82 12 1353 1629 42618341
PCO2 decreased 52.21 30.82 12 1353 1782 42618188
Acquired macroglossia 46.26 30.82 6 1359 25 42619945
Device related sepsis 43.00 30.82 12 1353 3875 42616095
Monocyte count increased 38.47 30.82 12 1353 5682 42614288
Drug interaction 35.44 30.82 43 1322 266956 42353014
Procedural haemorrhage 32.47 30.82 9 1356 2832 42617138

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 75.42 26.16 12 2220 397 110586670
Encephalomalacia 59.84 26.16 12 2220 1490 110585577
Lymphocyte count increased 59.42 26.16 16 2216 7187 110579880
PO2 decreased 50.99 26.16 12 2220 3136 110583931
PCO2 decreased 50.94 26.16 12 2220 3149 110583918
Drug interaction 48.79 26.16 55 2177 500128 110086939
International normalised ratio increased 48.75 26.16 27 2205 86745 110500322
Device related sepsis 40.43 26.16 12 2220 7635 110579432
Lower urinary tract symptoms 38.73 26.16 7 2225 499 110586568
Acquired macroglossia 36.08 26.16 6 2226 262 110586805
Scrotal oedema 35.75 26.16 8 2224 1673 110585394
Monocyte count increased 33.91 26.16 12 2220 13281 110573786
Procedural haemorrhage 30.81 26.16 9 2223 5418 110581649
Attention deficit hyperactivity disorder 27.95 26.16 8 2224 4483 110582584
Melaena 27.04 26.16 17 2215 68740 110518327
Splenomegaly 26.80 26.16 12 2220 24486 110562581

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 D000077264 Calcium-Regulating Hormones and Agents
MeSH PA D000959 Antihypertensive Agents
MeSH PA D002121 Calcium Channel Blockers
MeSH PA D002317 Cardiovascular Agents
MeSH PA D049990 Membrane Transport Modulators
CHEBI has role CHEBI:35554 cardiovascular drug
CHEBI has role CHEBI:35674 antihypertensive agent

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs

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
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 3A4 Enzyme IC50 6.05 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