Pentazocine
Pentazocine is a mixed opioid agonist-antagonist used to treat moderate to severe pain. It works by binding to kappa opioid receptors as an agonist and to mu receptors as an antagonist, providing pain relief while producing fewer respiratory depression effects than pure opioid agonists. This medication is typically used when non-opioid analgesics are insufficient for pain control.
Pentazocine is an opioid pain medication 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
- N02AD01
- RxNorm
- 8001
- Generic
- Pentazocine
- Class
- atc-n02
- Brands
- —
- Availability
- rx
- Lactation
- unknown
- Routes
- oral, rectal
- Forms
- tablet, solution, capsule
- 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
- 50mg every 4-6 hours
- Maximum
- consult physician
- Frequency
- as needed, up to 600mg daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 25mg every 4-6 hours
- Maximum
- consult physician
- Frequency
- as needed, up to 300mg daily
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
- Usual dose
- 25mg every 4-6 hours
- Maximum
- consult physician
- Frequency
- as needed, lower maximum dose recommended
- Instructions
- Follow physician instructions
- Duration limits
- as prescribed
- Monitoring
- standard
Overdose information
Special Populations
10 groupspregnancy
first trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
second trimesteravoid if possible
avoid use during pregnancy unless benefits outweigh risks
regular fetal monitoring
Use of this medication in this population requires careful consideration of risks and benefits.
pregnancy
third trimesteravoid
avoid use near delivery due to risk of neonatal respiratory depression and withdrawal
close fetal monitoring and assessment of newborn for withdrawal symptoms
Use of this medication in this population requires careful consideration of risks and benefits.
pediatric_age
generalavoid
not recommended for use in children under 18 years due to risk of respiratory depression
close monitoring of respiratory status
Use of this medication in this population requires careful consideration of risks and benefits.
geriatric
generalreduce dose by 25-50%
use with caution in elderly, start with lowest effective dose and titrate slowly
monitor for sedation, confusion, respiratory depression, and falls
Use with caution and monitor for adverse effects.
renal_impairment
mild moderatedose adjustment may be needed
use with caution, may need dose reduction in moderate impairment
monitor renal function and for signs of metabolite accumulation
Use with caution and monitor for adverse effects.
renal_impairment
severeavoid or significantly reduce dose
avoid use in severe renal impairment due to risk of metabolite accumulation
monitor renal function closely
Use of this medication in this population requires careful consideration of risks and benefits.
hepatic_impairment
mild moderatedose adjustment may be needed
use with caution, may need dose reduction in moderate impairment
monitor liver function and for increased opioid effects
Use with caution and monitor for adverse effects.
hepatic_impairment
severeavoid or significantly reduce dose
avoid use in severe hepatic impairment due to impaired drug metabolism
monitor liver function closely
Use of this medication in this population requires careful consideration of risks and benefits.
lactation
generalavoid
not recommended during breastfeeding
monitor infant for sedation and respiratory depression
Use of this medication in this population requires careful consideration of risks and benefits.
Statistics and clinical data
FDA approval year
FDA approval year for Pentazocine
Drug class
ATC classification for Pentazocine
Common uses
Therapeutic indications
Controlled substance schedule
US controlled substance classification
Management of moderate to severe pain, including postoperative pain, labor pain, and pain associated with trauma or malignancy. May also be used for preoperative sedation and as an adjunct to anesthesia.
Pentazocine is a mixed opioid receptor agonist-antagonist. It acts as an agonist at kappa receptors and as an antagonist or partial agonist at mu receptors, producing analgesia while limiting some adverse effects associated with full opioid agonists.
May precipitate withdrawal symptoms in patients dependent on full opioid agonists. Has a ceiling effect for respiratory depression but not for analgesia or cardiovascular effects. Associated with risk of dependence, hallucinations, and should be used with caution in patients with head injuries, respiratory conditions, or hepatic/renal impairment. Not typically a controlled substance in many jurisdictions due to its mixed agonist-antagonist properties.
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