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

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
Inappropriate antidiuretic hormone secretion	61.41	33.43	19	1140	15443	63472420
Cerebral infarction	45.83	33.43	17	1142	23876	63463987
Hepatic function abnormal	45.15	33.43	19	1140	37123	63450740
Altered state of consciousness	37.80	33.43	15	1144	25215	63462648
Renal impairment	34.67	33.43	21	1138	88334	63399529

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	52.29	27.49	32	1312	65250	34890337
Cerebral infarction	37.09	27.49	19	1325	27436	34928151
Renal impairment	35.11	27.49	29	1315	94484	34861103
Cardiac failure	31.82	27.49	27	1317	91221	34864366

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	74.72	24.93	35	2764	45641	79695948
Renal impairment	61.52	24.93	48	2751	157735	79583854
Interstitial lung disease	61.48	24.93	42	2757	112558	79629031
Hepatic function abnormal	56.60	24.93	34	2765	73073	79668516
Cardiac failure	47.51	24.93	41	2758	154801	79586788
Altered state of consciousness	46.34	24.93	25	2774	43797	79697792
Inappropriate antidiuretic hormone secretion	45.60	24.93	21	2778	26292	79715297
Platelet count decreased	41.33	24.93	42	2757	194622	79546967
Erythema multiforme	27.22	24.93	13	2786	17638	79723951
Colon cancer	26.44	24.93	12	2787	14511	79727078
Prinzmetal angina	26.34	24.93	7	2792	1713	79739876
Hyperuricaemia	25.51	24.93	11	2788	11788	79729801

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	D002121	Calcium Channel Blockers
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D002317	Cardiovascular Agents
MeSH PA	D049990	Membrane Transport Modulators
MeSH PA	D014665	Vasodilator Agents

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
CHEMBL2105555	ChEMBL_ID
CHEMBL2218858	ChEMBL_ID
DB09231	DRUGBANK_ID
C061004	MESH_SUPPLEMENTAL_RECORD_UI
10159	IUPHAR_LIGAND_ID
C050883	MESH_SUPPLEMENTAL_RECORD_UI
6137	INN_ID
91599-74-5	SECONDARY_CAS_RN
4G9T91JS7E	UNII
656668	PUBCHEM_CID
008170	NDDF
008171	NDDF

Pharmaceutical products:

None