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

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	1532	103890-78-4

Description:

Molecule

Description

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:

Dose	Unit	Route
4	mg	O

ADMET properties:

Property	Value	Reference
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 term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Procalcitonin abnormal	64.18	39.47	11	1079	371	34955470
Encephalomalacia	55.29	39.47	11	1079	847	34954994
PO2 decreased	48.59	39.47	11	1079	1570	34954271
Acquired macroglossia	47.95	39.47	6	1084	18	34955823
PCO2 decreased	47.32	39.47	11	1079	1765	34954076
Device related sepsis	41.26	39.47	11	1079	3082	34952759
Lymphocyte count increased	40.34	39.47	11	1079	3354	34952487

FDA Adverse Event Reporting System (Geriatric)

MedDRA adverse event term	Likelihood ratio	Likelihood ratio threshold	Patients taking drug having adverse event	Patients taking drug not having adverse event	Patients not taking drug having adverse event	Patients not taking drug not having adverse event
Procalcitonin abnormal	67.53	32.46	11	1780	379	79742218
Encephalomalacia	54.82	32.46	11	1780	1230	79741367
Drug interaction	47.21	32.46	52	1739	415131	79327466
PO2 decreased	45.29	32.46	11	1780	2952	79739645
PCO2 decreased	44.60	32.46	11	1780	3143	79739454
International normalised ratio increased	44.05	32.46	26	1765	84695	79657902
Lymphocyte count increased	42.18	32.46	12	1779	5920	79736677
Device related sepsis	37.17	32.46	11	1780	6229	79736368
Acquired macroglossia	36.49	32.46	6	1785	219	79742378
Scrotal oedema	35.37	32.46	8	1783	1577	79741020

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
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 level	Dissociation constant	Type (acidic/basic)
pKa1	2.23	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Mechanism action	Bioact source	MoA source
Voltage-gated L-type calcium channel	Ion channel	Q01668 Q13936	CAC1D_HUMAN CAC1C_HUMAN	BLOCKER				SCIENTIFIC LITERATURE	SCIENTIFIC LITERATURE
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN		Ki	5.25		DRUG MATRIX
D(3) dopamine receptor	GPCR	P35462	DRD3_HUMAN		Ki	5.68		DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.64		DRUG MATRIX
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	6.05		DRUG MATRIX
Cytochrome P450 2C19	Enzyme	P33261	CP2CJ_HUMAN		IC50	5.70		DRUG MATRIX
Thromboxane-A synthase	Enzyme	P24557	THAS_HUMAN		IC50	5.77		DRUG MATRIX
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	5.70		DRUG MATRIX
Androgen receptor	Transcription factor		ANDR_RAT		Ki	5.58		DRUG MATRIX

External reference:

ID	Source
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