Nalbuphine
Nalbuphine is a mixed opioid agonist-antagonist analgesic used to treat moderate to severe pain. It works by activating kappa opioid receptors while blocking mu opioid receptors, providing pain relief with a lower risk of respiratory depression compared to traditional opioids. This medication is commonly used for perioperative pain management and as a supplement during anesthesia.
A mixed opioid analgesic for moderate to severe pain that acts as a kappa agonist and mu antagonist, offering pain relief with reduced respiratory depression risk.
This medication carries a boxed (black box) warning — the strongest type of FDA warning. Review the full prescribing information before use.
Key facts at a glance
- ATC
- N02AF02
- RxNorm
- 7238
- Generic
- Nalbuphine
- Class
- atc-n02
- Brands
- —
- Availability
- rx
- Lactation
- unknown
- Routes
- —
- Forms
- injection, solution
- Regions
- US, EU, CN, JP
- Monitoring
- —
This page is for informational purposes only.
Do not use this information to diagnose yourself or to replace a physician's advice. Always consult a qualified healthcare provider before starting, stopping, or changing any medication. If you believe you are experiencing a medical emergency, call your local emergency number immediately.
Dosage and administration
- Usual dose
- 500mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 250mg twice daily
- Maximum
- consult physician
- Frequency
- every 12 hours
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 400mg daily
- Maximum
- consult physician
- Frequency
- once daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
8 groupspregnancy
first trimesteravoid if possible
avoid use during first trimester unless benefits significantly outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteruse lowest effective dose
use only if clearly needed with careful risk-benefit assessment
fetal monitoring and uterine activity assessment
Use with caution and monitor for adverse effects.
pregnancy
third trimesteruse lowest effective dose, avoid prolonged use
avoid use close to delivery due to risk of neonatal respiratory depression
close fetal monitoring, prepare for neonatal resuscitation
Use with caution and monitor for adverse effects.
lactation
breastfeedingdiscontinue breastfeeding or avoid drug
nalbuphine is excreted in breast milk; avoid breastfeeding during treatment and for 24-48 hours after last dose
monitor infant for excessive drowsiness, respiratory depression
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderlyreduce initial dose by 50%
start with low doses and titrate slowly; monitor for excessive sedation and respiratory depression
close monitoring of vital signs, sedation levels, and respiratory function
Use with caution and monitor for adverse effects.
pediatric_age
pediatricweight-based dosing, reduce dose
use in children only when benefits outweigh risks; not recommended for neonates
close monitoring of respiratory and cardiovascular status
Use with caution and monitor for adverse effects.
renal_impairment
renal impairmentreduce dose or extend dosing interval
use with caution in patients with renal impairment; monitor renal function
monitor renal function, adjust dose based on creatinine clearance
Use with caution and monitor for adverse effects.
hepatic_impairment
hepatic impairmentreduce dose and extend dosing interval
use with extreme caution in patients with hepatic impairment; prolonged elimination may occur
close monitoring of liver function and drug accumulation
Use with caution and monitor for adverse effects.
Statistics and clinical data
Drug class
Nalbuphine belongs to the opioid analgesics class (ATC code N02AB02)
FDA approval year
FDA approved Nalbuphine for medical use in the United States
Mechanism of action
Pharmacological mechanism of Nalbuphine
Common uses
Therapeutic indications for Nalbuphine
Management of moderate to severe pain, including perioperative and obstetric analgesia. Also used as a supplement to balanced anesthesia.
Nalbuphine acts as an agonist at kappa opioid receptors and an antagonist at mu opioid receptors. This dual action produces analgesia while limiting respiratory depression and having a ceiling effect on respiratory depression at higher doses.
May precipitate withdrawal symptoms in patients physically dependent on pure mu opioid agonists. Has lower abuse potential than traditional opioids but still carries risk. Use with caution in patients with respiratory depression, head injury, or biliary tract disease. Avoid concurrent use with other CNS depressants.
Contraindications
Conditions and patient states where this medication should be avoided or used with caution.
Do not use (1)
Known allergy to this medication or its components
Use caution (1)
Consult healthcare provider for benefits vs risks assessment
Official drug label
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This information is for educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment.
This content is for general informational and educational purposes only and is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the guidance of a qualified healthcare provider with any questions you have about a medical condition, and never disregard professional medical advice or delay seeking it because of something you read here.
If you think you may have a medical emergency, call your local emergency number or go to the nearest emergency department immediately.
Medically reviewed by WellAlly Editorial Team Last reviewed July 26, 2026. · Read our editorial policy