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

Stem definition	Drug id	CAS RN
	1891	13669-70-0

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nefopam fenazoxine (+/-)-Nefopam nefopam hydrochloride nefopam HCl	Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26) Molecular weight: 253.35 Formula: C17H19NO CLOGP: 2.91 LIPINSKI: 0 HAC: 2 HDO: 0 TPSA: 12.47 ALOGS: -3.50 ROTB: 1

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nefopam
fenazoxine
(+/-)-Nefopam
nefopam hydrochloride
nefopam HCl

Non-narcotic analgesic chemically similar to ORPHENADRINE. Its mechanism of action is unclear. It is used for the relief of acute and chronic pain. (From Martindale, The Extra Pharmacopoeia, 30th ed, p26)

Molecular weight: 253.35
Formula: C17H19NO
CLOGP: 2.91
LIPINSKI: 0
HAC: 2
HDO: 0
TPSA: 12.47
ALOGS: -3.50
ROTB: 1

Drug dosage:

None

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	5.60 L/kg	Lombardo F, Berellini G, Obach RS
t_half (Half-life)	5 hours	Lombardo F, Berellini G, Obach RS
BA (Bioavailability)	36 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
S (Water solubility)	34 mg/mL	Benet LZ, Broccatelli F, Oprea TI
EoM (Fraction excreted unchanged in urine)	3 %	Benet LZ, Broccatelli F, Oprea TI
CL (Clearance)	12 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	1.04 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI

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Approvals:

Date	Agency	Company	Orphan
Jan. 1, 1978	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
Hepatocellular injury	371.17	25.81	124	5339	27257	63456302
Cholestasis	335.19	25.81	117	5346	29317	63454242
Hepatic cytolysis	136.70	25.81	51	5412	15356	63468203
Acute kidney injury	135.18	25.81	138	5325	263277	63220282
Acute generalised exanthematous pustulosis	125.65	25.81	44	5419	11055	63472504
Drug reaction with eosinophilia and systemic symptoms	95.28	25.81	50	5413	33786	63449773
Thrombocytopenia	88.05	25.81	85	5378	151072	63332487
Coma	72.45	25.81	53	5410	64311	63419248
Foetal megacystis	70.81	25.81	10	5453	26	63483533
Drug dependence	65.56	25.81	35	5428	24448	63459111

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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
Agranulocytosis	203.25	29.28	83	3958	23738	34929152
Drug reaction with eosinophilia and systemic symptoms	155.82	29.28	76	3965	32936	34919954
Cholestasis	154.66	29.28	71	3970	26877	34926013
Rash maculo-papular	150.98	29.28	71	3970	28380	34924510
Hepatocellular injury	135.24	29.28	61	3980	22150	34930740
Eosinophilia	131.63	29.28	63	3978	26159	34926731
Confusional state	91.33	29.28	97	3944	144063	34808827
Alveolar lung disease	84.11	29.28	17	4024	369	34952521
Pulmonary interstitial emphysema syndrome	78.93	29.28	17	4024	507	34952383
Toxic skin eruption	65.21	29.28	30	4011	11355	34941535

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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
Hepatocellular injury	465.37	22.55	185	9408	47408	79687387
Cholestasis	452.54	22.55	186	9407	51923	79682872
Drug reaction with eosinophilia and systemic symptoms	231.38	22.55	125	9468	64119	79670676
Agranulocytosis	206.27	22.55	103	9490	44927	79689868
Acute kidney injury	158.18	22.55	248	9345	519156	79215639
Eosinophilia	156.97	22.55	86	9507	45259	79689536
Hepatic cytolysis	148.04	22.55	70	9523	27081	79707714
Rash maculo-papular	142.54	22.55	87	9506	55991	79678804
Acute generalised exanthematous pustulosis	130.75	22.55	56	9537	17198	79717597
Thrombocytopenia	102.54	22.55	142	9451	265117	79469678

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02BG06	NERVOUS SYSTEM ANALGESICS OTHER ANALGESICS AND ANTIPYRETICS Other analgesics and antipyretics
CHEBI has role	CHEBI:35640	adrenergic uptake inhibitors
CHEBI has role	CHEBI:50949	SSRI
CHEBI has role	CHEBI:51039	dopamine reuptake inhibitor
MeSH PA	D000700	Analgesics
MeSH PA	D018712	Analgesics, Non-Narcotic
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D018373	Peripheral Nervous System Agents
MeSH PA	D018689	Sensory System 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	7.85	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	Type	Activity value (-log[M])	Bioact source
Sodium channel protein type 5 subunit alpha	Ion channel	Q14524	SCN5A_HUMAN			WOMBAT-PK
Sodium-dependent serotonin transporter	Transporter	P31645	SC6A4_HUMAN	Ki	7.54	PDSP
Sodium-dependent noradrenaline transporter	Transporter	P23975	SC6A2_HUMAN	Ki	7.48	PDSP
5-hydroxytryptamine receptor 2A	GPCR	P28223	5HT2A_HUMAN	Ki	5.77	PDSP
5-hydroxytryptamine receptor 2B	GPCR	P41595	5HT2B_HUMAN	Ki	6.48	PDSP
5-hydroxytryptamine receptor 2C	GPCR	P28335	5HT2C_HUMAN	Ki	7.25	PDSP
Sodium-dependent dopamine transporter	Transporter	Q01959	SC6A3_HUMAN	Ki	6.28	PDSP

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External reference:

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ID	Source
001582	NDDF
004636	NDDF
23327-57-3	SECONDARY_CAS_RN
3018	INN_ID
322300008	SNOMEDCT_US
350324006	SNOMEDCT_US
419768004	SNOMEDCT_US
4324	RXNORM
4450	PUBCHEM_CID
4UP8060B7J	UNII

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Pharmaceutical products:

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