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

Stem definition	Drug id	CAS RN
opioid receptor antagonists/agonists related to normorphine	1874	20594-83-6

Description:

Molecule	Description
Molfile Inchi Smiles Synonyms: nalbuphine N-Cyclobutylmethyl-14-hydroxydihydronormorphine nalbuphine hydrochloride nalbuphine HCl	A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS. Molecular weight: 357.45 Formula: C21H27NO4 CLOGP: 1.05 LIPINSKI: 0 HAC: 5 HDO: 3 TPSA: 73.16 ALOGS: -2.23 ROTB: 2 Status: OFP Legend: OFP - off patent OFM - off market ONP - on patent

Molecule

Description

Molfile Inchi Smiles

Synonyms:

nalbuphine
N-Cyclobutylmethyl-14-hydroxydihydronormorphine
nalbuphine hydrochloride
nalbuphine HCl

A narcotic used as a pain medication. It appears to be an agonist at KAPPA RECEPTORS and an antagonist or partial agonist at MU RECEPTORS.

Molecular weight: 357.45
Formula: C21H27NO4
CLOGP: 1.05
LIPINSKI: 0
HAC: 5
HDO: 3
TPSA: 73.16
ALOGS: -2.23
ROTB: 2

Status: OFP

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

Drug dosage:

Dose	Unit	Route
80	mg	P

ADMET properties:

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Property	Value	Reference
Vd (Volume of distribution)	4.60 L/kg	Lombardo F, Berellini G, Obach RS
EoM (Fraction excreted unchanged in urine)	4 %	Benet LZ, Broccatelli F, Oprea TI
S (Water solubility)	35.50 mg/mL	Benet LZ, Broccatelli F, Oprea TI
t_half (Half-life)	3.70 hours	Lombardo F, Berellini G, Obach RS
CL (Clearance)	22 mL/min/kg	Lombardo F, Berellini G, Obach RS
MRTD (Maximum Recommended Therapeutic Daily Dose)	2.80 µM/kg/day	Contrera JF, Matthews EJ, Kruhlak NL, Benz RD
BA (Bioavailability)	16 %	Kim MT, Sedykh A, Chakravarti SK, Saiakhov RD, Zhu H
BDDCS (Biopharmaceutical Drug Disposition Classification System)	1	Benet LZ, Broccatelli F, Oprea TI
fu (Fraction unbound in plasma)	0.50 %	Lombardo F, Berellini G, Obach RS

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Approvals:

Date	Agency	Company	Orphan
May 15, 1979	FDA

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
Drug hypersensitivity	256.96	44.76	93	405	310594	63177930
Antithrombin III	88.52	44.76	11	487	156	63488368
Hypoalbuminaemia	46.61	44.76	12	486	11793	63476731

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FDA Adverse Event Reporting System (Male)

None

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
Drug hypersensitivity	173.76	36.01	76	749	298840	79444723
Febrile bone marrow aplasia	46.64	36.01	13	812	13007	79730556
Antithrombin III	46.45	36.01	6	819	87	79743476
Transverse sinus thrombosis	41.51	36.01	7	818	658	79742905
Superior sagittal sinus thrombosis	38.23	36.01	7	818	1056	79742507

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FDA Adverse Event Reporting System (Pediatric)

None

Pharmacologic Action:

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Source	Code	Description
ATC	N02AF02	NERVOUS SYSTEM ANALGESICS OPIOIDS Morphinan derivatives
CHEBI has role	CHEBI:35482	narcotic analgesic
CHEBI has role	CHEBI:50137	mu-opioid receptor antagonists
FDA EPC	N0000175692	Opioid Agonist/Antagonist
FDA MoA	N0000175685	Partial Opioid Agonists
FDA MoA	N0000175686	Competitive Opioid Antagonists
MeSH PA	D000700	Analgesics
MeSH PA	D000701	Analgesics, Opioid
MeSH PA	D002491	Central Nervous System Agents
MeSH PA	D002492	Central Nervous System Depressants

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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
Pain	indication	22253000
General anesthesia	indication	50697003
Labor pain	indication	247412007
Local anesthesia	indication	386761002
Suicidal thoughts	contraindication	6471006
Dependent drug abuse	contraindication	6525002
Alcohol withdrawal delirium	contraindication	8635005
Asthenia	contraindication	13791008
Constipation	contraindication	14760008	DOID:2089
Mood swings	contraindication	18963009

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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	9.93	acidic
pKa2	8.23	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
Mu-type opioid receptor	GPCR	P35372	OPRM_HUMAN	AGONIST	Ki	8.80	WOMBAT-PK	CHEMBL
Kappa-type opioid receptor	GPCR	P41145	OPRK_HUMAN	AGONIST	Ki	8	WOMBAT-PK	CHEMBL
Delta-type opioid receptor	GPCR	P41143	OPRD_HUMAN	AGONIST	Ki	6	WOMBAT-PK	CHEMBL
Kappa-type opioid receptor	GPCR		OPRK_MOUSE	AGONIST	IC50	7.40	IUPHAR

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External reference:

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ID	Source
001565	NDDF
004627	NDDF
111123003	SNOMEDCT_US
154985	RXNORM
1663	IUPHAR_LIGAND_ID
2038	MMSL
23277-43-2	SECONDARY_CAS_RN
2623	INN_ID
373539006	SNOMEDCT_US
4019046	VANDF

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Pharmaceutical products:

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Product	Category	Ingredients	NDC	Form	Quantity	Route	Marketing	Label
NALBUPHINE HCI	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1418	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	14 sections
NALBUPHINE HCI	HUMAN PRESCRIPTION DRUG LABEL	1	51662-1420	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	14 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9917	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	14 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9917	INJECTION, SOLUTION	20 mg	INTRAMUSCULAR	ANDA	14 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9918	INJECTION, SOLUTION	10 mg	INTRAMUSCULAR	ANDA	13 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9918	INJECTION, SOLUTION	10 mg	INTRAMUSCULAR	ANDA	13 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9919	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	13 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0404-9919	INJECTION, SOLUTION	10 mg	INTRAVENOUS	ANDA	13 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1463	INJECTION, SOLUTION	10 mg	INTRAMUSCULAR	ANDA	28 sections
Nalbuphine Hydrochloride	HUMAN PRESCRIPTION DRUG LABEL	1	0409-1463	INJECTION, SOLUTION	10 mg	INTRAMUSCULAR	ANDA	28 sections

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