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

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	3880	105979-17-7

Description:

Molecule

Description

Molfile Inchi Smiles

Synonyms:

benidipine
benidipine hydrochloride
coniel
benidipine HCl

Molecular weight: 505.57
Formula: C28H31N3O6
CLOGP: 5.71
LIPINSKI: 2
HAC: 9
HDO: 1
TPSA: 111.01
ALOGS: -5.32
ROTB: 9

Drug dosage:

None

ADMET properties:

Property	Value	Reference
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	1.90 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	1 %	Benet LZ, Broccatelli F, Oprea TI
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.23 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD

Predicted pharmacokinetic/toxicological properties (PK-AZ):

Property	Description	Value	Unit	Confidence	Similarity
kinase-safety-class	ACVR2B,AKT2,AKT3,AURKA,AXL,BRAF,BTK,CAMK2B,CAMK2D,CDK5,CDK9,DYRK1B,EIF2AK3,EPHB4,ERBB2,GRK2,GSK3B,ITK,JAK2,JAK3,MAP3K7,MAPK10,MAPK7,MAPK9,MAPKAPK2,MET,NTRK2,PDK1,PDK4,PDPK1,PIK3CA,PIK3CB,PIK3CD,PIM2,PRKDC,STK33,TEK,TTK,ZAP70	39
kinase-selectivity-class	AXL,BRAF,CDK9,GRK2,STK33,TEK	6
pfas-class	PFAS structural alert (1 = True, 0 = False)	0

Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1991	YEAR INTRODUCED

FDA Adverse Event Reporting System (Female)

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
Cerebral infarction	77.43	33.48	25	1427	26571	90600424
Inappropriate antidiuretic hormone secretion	72.07	33.48	22	1430	19483	90607512
Renal impairment	52.56	33.48	28	1424	105393	90521602
Altered state of consciousness	46.93	33.48	18	1434	31514	90595481
Hepatic function abnormal	46.76	33.48	20	1432	46268	90580727
Blood pressure decreased	43.34	33.48	22	1430	74873	90552122
Hyponatraemia	33.91	33.48	23	1429	133515	90493480

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
Interstitial lung disease	58.87	26.39	37	1614	78425	42541259
Cerebral infarction	52.14	26.39	25	1626	31144	42588540
Prinzmetal angina	42.57	26.39	10	1641	1347	42618337
Renal impairment	34.94	26.39	31	1620	110197	42509487
Cardiac failure	31.79	26.39	29	1622	106827	42512857

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
Cerebral infarction	120.45	24.86	49	3375	51789	110534086
Interstitial lung disease	79.60	24.86	51	3373	139283	110446592
Renal impairment	79.14	24.86	57	3367	188388	110397487
Altered state of consciousness	59.42	24.86	31	3393	57595	110528280
Hepatic function abnormal	59.32	24.86	36	3388	89259	110496616
Cardiac failure	57.32	24.86	47	3377	187579	110398296
Inappropriate antidiuretic hormone secretion	55.43	24.86	25	3399	33826	110552049
Prinzmetal angina	54.96	24.86	13	3411	2256	110583619
Blood pressure decreased	44.14	24.86	33	3391	115058	110470817
Platelet count decreased	43.38	24.86	44	3380	230399	110355476
Drug interaction	27.90	24.86	53	3371	500130	110085745
Erythema multiforme	26.56	24.86	13	3411	21084	110564791
Colon cancer	26.45	24.86	12	3412	16431	110569444

FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

Source	Code	Description
ATC	C08CA15	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	D002121	Calcium Channel Blockers
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D014665	Vasodilator Agents
MeSH PA	D049990	Membrane Transport Modulators
CHEBI has role	CHEBI:35554	cardiovascular drug

Related Drugs by ATC class:

C08CA Dihydropyridine derivatives 17 drugs

amlodipine barnidipine celecoxib cilnidipine clevidipine felodipine isradipine lacidipine lercanidipine levamlodipine manidipine nicardipine show all 17 →

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	7.05	Basic
pKa2	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	IC50	5.31		IUPHAR	SCIENTIFIC LITERATURE
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN	BLOCKER	IC50	6.84		SCIENTIFIC LITERATURE

External reference:

ID	Source
D02045	KEGG_DRUG
C0053108	UMLSCUI
CHEBI:135806	CHEBI
CHEMBL2074972	ChEMBL_ID
DB09231	DRUGBANK_ID
C061004	MESH_SUPPLEMENTAL_RECORD_UI
10159	IUPHAR_LIGAND_ID
6137	INN_ID
91599-74-5	SECONDARY_CAS_RN
4G9T91JS7E	UNII
656668	PUBCHEM_CID
008170	NDDF
008171	NDDF
1303527004	SNOMEDCT_US
1303528009	SNOMEDCT_US
C050883	MESH_SUPPLEMENTAL_RECORD_UI
4G9T91JS7E	INXIGHT DRUGS

Pharmaceutical products:

None