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

Stem definition	Drug id	CAS RN
calcium channel blockers, nifedipine derivatives	1947	39562-70-4

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nitrendipine nitrendipin nitrepin	A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive. Molecular weight: 360.37 Formula: C18H20N2O6 CLOGP: 3.73 LIPINSKI: 0 HAC: 8 HDO: 1 TPSA: 107.77 ALOGS: -4.41 ROTB: 7

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nitrendipine
nitrendipin
nitrepin

A calcium channel blocker with marked vasodilator action. It is an effective antihypertensive agent and differs from other calcium channel blockers in that it does not reduce glomerular filtration rate and is mildly natriuretic, rather than sodium retentive.

Molecular weight: 360.37
Formula: C18H20N2O6
CLOGP: 3.73
LIPINSKI: 0
HAC: 8
HDO: 1
TPSA: 107.77
ALOGS: -4.41
ROTB: 7

Drug dosage:

Dose	Unit	Route
20	mg	O

ADMET properties:

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Property	Value	Reference
t_half (Half-life)	8.20 hours	Lombardo F, Berellini G, Obach RS
Vd (Volume of distribution)	6.10 L/kg	Lombardo F, Berellini G, Obach RS
CL (Clearance)	25 mL/min/kg	Lombardo F, Berellini G, Obach RS
BDDCS (Biopharmaceutical Drug Disposition Classification System)	2	Benet LZ, Broccatelli F, Oprea TI
BA (Bioavailability)	16.50 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
MRTD (Maximum Recommended Therapeutic Daily Dose)	0.92 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
EoM (Fraction excreted unchanged in urine)	0.50 %	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.02 %	Lombardo F, Berellini G, Obach RS
S (Water solubility)	0.00 mg/mL	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1985	YEAR INTRODUCED

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
General physical health deterioration	96.22	36.22	72	2404	201330	63285216
Fall	93.22	36.22	94	2382	392240	63094306
Antinuclear antibody negative	81.44	36.22	13	2463	221	63486325
Product prescribing error	79.33	36.22	32	2444	26257	63460289
Coombs positive haemolytic anaemia	75.46	36.22	13	2463	358	63486188
Herpes simplex reactivation	63.59	36.22	12	2464	556	63485990
Gastritis haemorrhagic	56.96	36.22	13	2463	1532	63485014
Antiphospholipid syndrome	55.05	36.22	13	2463	1777	63484769
Complex regional pain syndrome	51.50	36.22	13	2463	2344	63484202
Lymphopenia	47.42	36.22	20	2456	18307	63468239

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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
Rectal prolapse	112.68	35.83	22	3427	470	34953012
Renal cyst haemorrhage	106.94	35.83	22	3427	617	34952865
Intraductal papillary mucinous neoplasm	98.86	35.83	20	3429	515	34952967
SARS-CoV-2 antibody test positive	85.21	35.83	17	3432	407	34953075
Carotid arteriosclerosis	83.58	35.83	22	3427	1836	34951646
Abdominal wall haemorrhage	82.75	35.83	17	3432	473	34953009
Vena cava injury	82.75	35.83	16	3433	324	34953158
Delayed graft function	79.69	35.83	22	3427	2199	34951283
Vascular anastomotic haemorrhage	72.90	35.83	14	3435	273	34953209
Mean cell volume increased	71.96	35.83	22	3427	3147	34950335

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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
Product prescribing error	146.36	32.59	68	5374	44745	79694201
General physical health deterioration	137.53	32.59	128	5314	275110	79463836
Renal cyst haemorrhage	113.26	32.59	22	5420	670	79738276
Intraductal papillary mucinous neoplasm	98.21	32.59	20	5422	778	79738168
Dizziness	94.35	32.59	145	5297	526296	79212650
SARS-CoV-2 antibody test positive	90.86	32.59	17	5425	422	79738524
Syncope	88.54	32.59	83	5359	179366	79559580
Rectal prolapse	88.13	32.59	22	5420	2156	79736790
Vena cava injury	88.07	32.59	16	5426	336	79738610
Carotid arteriosclerosis	83.80	32.59	22	5420	2634	79736312

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FDA Adverse Event Reporting System (Pediatric)

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Pharmacologic Action:

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Source	Code	Description
ATC	C08CA08	CARDIOVASCULAR SYSTEM CALCIUM CHANNEL BLOCKERS SELECTIVE CALCIUM CHANNEL BLOCKERS WITH MAINLY VASCULAR EFFECTS Dihydropyridine derivatives
ATC	C09BB06	CARDIOVASCULAR SYSTEM AGENTS ACTING ON THE RENIN-ANGIOTENSIN SYSTEM ACE INHIBITORS, COMBINATIONS ACE inhibitors and calcium channel blockers
CHEBI has role	CHEBI:35620	vasodilator agents
CHEBI has role	CHEBI:35674	antihypertensive drugs
CHEBI has role	CHEBI:38215	calcium channel blockers
CHEBI has role	CHEBI:176497	geroprotectors
MeSH PA	D000959	Antihypertensive Agents
MeSH PA	D002121	Calcium Channel Blockers
MeSH PA	D000077264	Calcium-Regulating Hormones and Agents
MeSH PA	D002317	Cardiovascular Agents

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

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🐶 Veterinary Drug Use

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🐶 Veterinary products

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Acid dissociation constants calculated using MoKa v3.0.0

Dissociation level	Dissociation constant	Type (acidic/basic)
pKa1	2.37	Basic

Orange Book patent data (new drug applications)

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Orange Book exclusivity data (new drug applications)

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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	8.40	IUPHAR	IUPHAR
Voltage-dependent L-type calcium channel subunit alpha-1C	Ion channel	Q13936	CAC1C_HUMAN	BLOCKER	Ki	9.60	CHEMBL	SCIENTIFIC LITERATURE
Intermediate conductance calcium-activated potassium channel protein 4	Ion channel	O15554	KCNN4_HUMAN	BLOCKER	IC50	7.60	IUPHAR
Voltage-dependent calcium channel gamma-1 subunit	Ion channel	Q06432	CCG1_HUMAN				WOMBAT-PK
Transthyretin	Secreted	P02766	TTHY_HUMAN		IC50	5.92	WOMBAT-PK
ATP-binding cassette sub-family G member 2	Transporter	Q9UNQ0	ABCG2_HUMAN		IC50	4.68	CHEMBL
Cytochrome P450 2C9	Enzyme	P11712	CP2C9_HUMAN		IC50	6.52	DRUG MATRIX
Voltage-dependent T-type calcium channel subunit alpha-1H	Ion channel	O95180	CAC1H_HUMAN		IC50	5.06	WOMBAT-PK
Potassium voltage-gated channel subfamily H member 2	Ion channel	Q12809	KCNH2_HUMAN		IC50	5	CHEMBL
Voltage-dependent L-type calcium channel subunit alpha-1F	Ion channel	O60840	CAC1F_HUMAN	GATING INHIBITOR	IC50	6	IUPHAR

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External reference:

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ID	Source
005383	NDDF
2334	IUPHAR_LIGAND_ID
444757009	SNOMEDCT_US
4507	PUBCHEM_CID
4739	INN_ID
7441	RXNORM
9B627AW319	UNII
C0028127	UMLSCUI
CHEBI:7582	CHEBI
CHEMBL251230	ChEMBL_ID

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Pharmaceutical products:

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