General
Preferred name
nalbuphine
Synonyms
NALBUPHINE HYDROCHLORIDE ()
PHN-131 ()
Nalbuphine HCl ()
Nalbufine hydrochloride ()
EN-2234A ()
NSC-757829 ()
Nubain ()
Intapan ()
P&D ID
PD009692
CAS
23277-43-2
20594-83-6
Tags
natural product
biased GPCR ligand
drug
available
Approved by
FDA
First approval
1979
Drug indication
Antagonist (to narcotics)
Analgesic
Prurigo nodularis
Pain
Uremic pruritus
Drug Status
approved
Max Phase
4.0
Probe control
Probe control not defined
Orthogonal probes
0
No orthogonal probes found
Similar probes
0
No structurally similar probes found
Structure
P&D probe-likeness score
Structure formats
[[ format ]]
[[ compound[format === 'MOL' ? 'molblock' : format.toLowerCase()] ]]
Description
(extracted from source data)
HALF-LIFE
The plasma half-life of nalbuphine is about 5 hours.
PHARMACODYNAMICS
Nalbuphine is a synthetic opioid agonist-antagonist analgesic of the phenanthrene series. Nalbuphine's analgesic potency is essentially equivalent to that of [morphine] on a milligram basis. The opoioid antagonist activity of nalbuphine is about one-fourth to that of [nalorphine] and 10 times to that of [pentazocine]. Nalbuphine by itself has potent opioid antagonist activity at doses equal to or lower than its analgesic dose. When administered following or concurrent with mu agonist opioid analgesics (e.g., morphine, oxymorphone, fentanyl), nalbuphine may partially reverse or block opioid-induced respiratory depression from the mu agonist analgesic. Nalbuphine may precipitate withdrawal in patients dependent on opioid drugs. Nalbuphine should be used with caution in patients who have been receiving mu opioid analgesics on a regular basis.
ABSORPTION
The mean absolute bioavailability was 81% and 83% for the 10 and 20 mg intramuscular doses, respectively, and 79% and 76% following 10 and 20 mg of subcutaneous nalbuphine. Clinical studies show that the duration of analgesic activity of the drug can range from 3 to 6 hours.
DESCRIPTION
Nalbuphine is a semi-synthetic opioid drug that acts as a full agonist at the κ opioid receptor and a partial agonist at μ and δ opioid receptors. It is chemically related to the opioid antagonists, and , and the potent opioid analgesic, .
(GtoPdb)
[[ p.pathway_name ]]
[[ compound.targets[tid].gene_name ]]
Cell lines
0
Organisms
1
Compound Sets
18
Axon Medchem Screening Library
BiasDB
ChEMBL Approved Drugs
ChEMBL Drugs
Drug Repurposing Hub
DrugBank
DrugBank Approved Drugs
DrugCentral
DrugCentral Approved Drugs
DrugMAP Approved Drugs
Guide to Pharmacology
LSP-MoA library (Laboratory of Systems Pharmacology)
NCATS Inxight Approved Drugs
Novartis Chemogenetic Library (NIBR MoA Box)
NPC Screening Collection
Prestwick Chemical Library
ReFrame library
[[ a.name ]]
[[ ligand_id ]]
free of charge
External IDs
50
Molecular Weight
357.19
Hydrogen Bond Acceptors
5
Hydrogen Bond Donors
3
Rotatable Bonds
2
Ring Count
6
Aromatic Ring Count
1
cLogP
1.71
TPSA
73.16
Fraction CSP3
0.71
Chiral centers
5.0
Largest ring
6.0
QED
0.75
Structural alerts
0
No structural alerts detected
Related compounds
Custom attributes
(extracted from source data)
Member status
virtual
MOA
Opioid receptor mu antagonist
Opioid receptor kappa agonist
opioid receptor agonist, opioid receptor antagonist
Target
OPRD1, OPRK1, OPRM1
Opioid agonist
Indication
pain relief
Therapeutic Class
Analgesics
Source data
