Butorphanol
Butorphanol is a mixed opioid agonist-antagonist analgesic used to manage moderate to severe pain. It works by binding to kappa receptors as a full agonist and mu receptors as a partial agonist/antagonist, providing pain relief while producing less respiratory depression than pure opioid agonists.
Butorphanol is an opioid analgesic used for moderate to severe pain that works as a mixed agonist-antagonist at opioid receptors.
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
- N02AF01
- RxNorm
- 1841
- Generic
- Butorphanol
- Class
- atc-n02
- Brands
- Butorphic, Torbugesic, Torphadine, Vetorphic, Dolorex Solution
- Availability
- rx
- Lactation
- unknown
- Routes
- nasal
- Forms
- injection, solution, spray
- 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
- 1mg (1 spray per nostril)
- Maximum
- consult physician
- Frequency
- every 3-4 hours as needed
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 0.5mg/kg
- Maximum
- consult physician
- Frequency
- every 3-4 hours as needed
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 0.5mg
- Maximum
- consult physician
- Frequency
- every 4-6 hours as needed
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
7 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks; use only if clearly needed
regular fetal monitoring
Use with caution and monitor for adverse effects.
pregnancy
third trimesteravoid near term
avoid use close to delivery due to risk of respiratory depression in newborn
fetal monitoring and assessment of newborn for respiratory depression
Use with caution and monitor for adverse effects.
lactation
breastfeedingavoid
discontinue breastfeeding or avoid butorphanol use during lactation
monitor infant for sedation, respiratory depression, and feeding difficulties
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
elderlyreduce initial dose by 50%
start with lowest effective dose; increased sensitivity to CNS effects
monitor for excessive sedation, respiratory depression, and fall risk
Use with caution and monitor for adverse effects.
pediatric_age
children 2 17 yearsweight-based dosing required
use lowest effective dose; not recommended for children under 2 years
close monitoring of respiratory rate and sedation
Use with caution and monitor for adverse effects.
renal_impairment
moderate to severereduce dose by 50%
use with caution; monitor renal function and adjust dose accordingly
monitor renal function and for signs of accumulation
Use with caution and monitor for adverse effects.
hepatic_impairment
moderate to severereduce dose by 50%
use with caution; butorphanol undergoes hepatic metabolism
monitor liver function and for signs of accumulation
Use with caution and monitor for adverse effects.
Statistics and clinical data
FDA Approval Year
FDA approval for human use
Drug class
Pharmacological classification
Common uses
Therapeutic applications
Route of administration
Administration methods
Management of moderate to severe pain, including preoperative medication, obstetric analgesia during labor, and as a component of balanced anesthesia.
Acts as a kappa receptor agonist and partial mu receptor agonist/antagonist, modulating pain transmission in the central nervous system.
May cause dependence and withdrawal symptoms in opioid-dependent patients. Use with caution in patients with respiratory depression, head injuries, or biliary tract disease. Avoid combining with other CNS depressants. Has a ceiling effect for respiratory depression but not for analgesia.
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 August 24, 2026. · Read our editorial policy