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

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	1922	21829-25-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: BAY A1040 nifedipine nedipin fedipin	A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure. Molecular weight: 346.34 Formula: C17H18N2O6 CLOGP: 3.12 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 110.45 ALOGS: -4.29 ROTB: 6 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

BAY A1040
nifedipine
nedipin
fedipin

A potent vasodilator agent with calcium antagonistic action. It is a useful anti-anginal agent that also lowers blood pressure.

Molecular weight: 346.34
Formula: C17H18N2O6
CLOGP: 3.12
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 110.45
ALOGS: -4.29
ROTB: 6

Status: OFP

Legend:
OFP - off patent
OFM - off market
ONP - on patent

Drug dosage:

Dose	Unit	Route
30	mg	O
30	mg	P

ADMET properties:

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Property	Value	Reference
CL (Clearance)	7.30 mL/min/kg	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	3.71 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	1.90 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	0.79 L/kg	Lombardo F, Berellini G, Obach RS
fu (Fraction unbound in plasma)	0.04 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.01 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	0.01 %	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Dec. 31, 1981	FDA	PFIZER

FDA Adverse Event Reporting System (Female)

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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
Premature delivery	674.67	10.09	404	62990	29877	63395751
Exposure during pregnancy	318.68	10.09	563	62831	154984	63270644
Premature baby	299.83	10.09	211	63183	20524	63405104
Low birth weight baby	206.62	10.09	113	63281	7016	63418612
Pre-eclampsia	178.11	10.09	112	63282	9021	63416607
Pemphigus	147.56	10.09	9	63385	183717	63241911
Foetal exposure during pregnancy	143.09	10.09	168	63226	31794	63393834
Alopecia	136.83	10.09	84	63310	337452	63088176
Glossodynia	124.22	10.09	16	63378	178860	63246768
Maternal exposure during pregnancy	116.90	10.09	482	62912	219580	63206048

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FDA Adverse Event Reporting System (Male)

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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
Premature baby	234.26	10.73	194	42916	19439	34894382
Low birth weight baby	154.42	10.73	105	43005	7800	34906021
Foetal exposure during pregnancy	126.91	10.73	193	42917	37908	34875913
Photodermatosis	99.01	10.73	34	43076	529	34913292
Solar lentigo	92.07	10.73	32	43078	517	34913304
Dysplastic naevus	91.31	10.73	31	43079	465	34913356
Off label use	77.18	10.73	263	42847	419261	34494560
Polydactyly	70.60	10.73	33	43077	1180	34912641
Foetal growth restriction	69.46	10.73	50	43060	4067	34909754
Gingival hypertrophy	66.14	10.73	36	43074	1785	34912036

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FDA Adverse Event Reporting System (Geriatric)

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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
Premature delivery	504.76	9.64	322	91074	23145	79629847
Exposure during pregnancy	260.76	9.64	438	90958	100694	79552298
Pre-eclampsia	142.45	9.64	93	91303	6948	79646044
Renal impairment	137.84	9.64	446	90950	157337	79495655
Maternal exposure during pregnancy	116.58	9.64	383	91013	136155	79516837
Cerebral infarction	112.58	9.64	194	91202	45482	79607510
Bradycardia	102.36	9.64	365	91031	135192	79517800
Cardiac failure congestive	99.58	9.64	374	91022	142028	79510964
Hypotension	99.52	9.64	852	90544	439465	79213527
Alopecia	93.14	9.64	77	91319	231278	79421714

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	C07FB03	CARDIOVASCULAR SYSTEM BETA BLOCKING AGENTS BETA BLOCKING AGENTS, OTHER COMBINATIONS Beta blocking agents and calcium channel blockers
ATC	C08CA05	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
ATC	C08CA55	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
ATC	C08GA01	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS CALCIUM CHANNEL BLOCKERS AND DIURETICS Calcium channel blockers and diuretics
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:38215	calcium channel blockers
CHEBI has role	CHEBI:66993	tocolytic drugs
CHEBI has role	CHEBI:77746	Homo sapiens metabolite
FDA CS	M0006414	Dihydropyridines
FDA EPC	N0000175421	Dihydropyridine Calcium Channel Blocker

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

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Disease	Relation	SNOMED_ID	DOID
Hypertensive disorder	indication	38341003	DOID:10763
Prinzmetal angina	indication	87343002
Angina pectoris	indication	194828000
Premature labor	off-label use	6383007
Raynaud's phenomenon	off-label use	266261006
Cirrhosis of liver	contraindication	19943007	DOID:5082
Myocardial infarction	contraindication	22298006	DOID:5844
Stenosis of intestine	contraindication	23065003
Low blood pressure	contraindication	45007003
Chronic heart failure	contraindication	48447003

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🐶 Veterinary Drug Use

None

🐶 Veterinary products

None

Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	2.5	Basic

Orange Book patent data (new drug applications)

None

Orange Book exclusivity data (new drug applications)

None

Bioactivity Summary:

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Target	Class	Pharos	UniProt	Action	Type	Activity value (-log[M])	Bioact source	MoA source
Voltage-dependent L-type calcium channel subunit alpha-1D	Ion channel	Q01668	CAC1D_HUMAN	GATING INHIBITOR	IC50	7.70	IUPHAR	CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel	Q13936	CAC1C_HUMAN	BLOCKER	Kd	9.40	CHEMBL	SCIENTIFIC LITERATURE
Sodium/nucleoside cotransporter 1	Transporter	O00337	S28A1_HUMAN		Ki	5.09	DRUG MATRIX
Adenosine receptor A2a	GPCR	P29274	AA2AR_HUMAN		Ki	4.65	CHEMBL
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	4.30	WOMBAT-PK
Cytochrome P450 3A4	Enzyme	P08684	CP3A4_HUMAN		IC50	5.26	WOMBAT-PK
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN		Ki	6.50	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN		Ki	5.02	DRUG MATRIX
Adenosine receptor A1	GPCR	P30542	AA1R_HUMAN		Ki	5.35	DRUG MATRIX
Adenosine receptor A3	GPCR	P0DMS8	AA3R_HUMAN		Ki	5.08	CHEMBL

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External reference:

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ID	Source
000710	NDDF
017700	NDDF
2302	MMSL
2514	IUPHAR_LIGAND_ID
3222	INN_ID
387490003	SNOMEDCT_US
4018390	VUID
4018390	VANDF
4485	PUBCHEM_CID
5175	MMSL

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2497	CAPSULE, LIQUID FILLED	10 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0228-2530	CAPSULE, LIQUID FILLED	20 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7080	TABLET, EXTENDED RELEASE	30 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7080	TABLET, EXTENDED RELEASE	30 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7081	TABLET, EXTENDED RELEASE	60 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7081	TABLET, EXTENDED RELEASE	60 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7082	TABLET, EXTENDED RELEASE	90 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7082	TABLET, EXTENDED RELEASE	90 mg	ORAL	ANDA	19 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7208	TABLET, EXTENDED RELEASE	30 mg	ORAL	ANDA	12 sections
Nifedipine	HUMAN PRESCRIPTION DRUG LABEL	1	0904-7229	CAPSULE	10 mg	ORAL	ANDA	19 sections

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