Butorphanol
STADOL
What it isKappa-opioid agonist and partial mu agonist; moderate-to-severe pain, including migraine.
Why this oneThe nasal spray gives rapid analgesia without injection, while partial mu activity limits but does not eliminate respiratory depression.
What limits itIt can precipitate withdrawal in opioid-dependent patients; kappa agonism causes dysphoria, and dependence still develops.
FDA-approved for
- pain (~1978)
FDA label
Read the full label on DailyMed ↗
| FDA dosing | Population | Start | Target | Max |
|---|---|---|---|---|
| Pain severe enough to require an opioid, alternatives inadequate | Adults | 1 mg (1 spray, one nostril); if inadequate relief in 60-90 min, may give additional 1 mg; sequence may repeat q3-4h PRN | 1-2 mg q3-4h PRN (lowest dose achieving analgesia) | 2 mg/dose (1 spray each nostril) only if patient can remain recumbent; no additional 2 mg dose for 3-4 h |
Renal Initial sequence limited to 1 mg, repeat 1 mg in 90-120 min if needed; subsequent doses generally no less than q6h
Hepatic Initial sequence limited to 1 mg, repeat 1 mg in 90-120 min if needed; subsequent doses generally no less than q6h
Elderly: same reduced sequence as renal/hepatic impairment (1 mg, repeat in 90-120 min; then generally no less than q6h)
Instructions
- Use lowest effective dose for shortest duration
- Do not abruptly discontinue in physically dependent patients - taper gradually (risk of withdrawal, uncontrolled pain, suicide)
- Discuss access to an opioid overdose reversal agent (naloxone/nalmefene)
- Conservative dosing when converting from other opioids (agonist-antagonist; underestimate 24-h dose)
- Not recommended in labor or for balanced anesthesia (not studied intranasally)
Contraindications
- Significant respiratory depression
- Acute or severe bronchial asthma in an unmonitored setting or without resuscitative equipment
- Known or suspected gastrointestinal obstruction, including paralytic ileus
Cautions
- Addiction, abuse, and misuse (Schedule IV) - assess risk before prescribing and reassess regularly
- Life-threatening respiratory depression - greatest at initiation and after dose increase
- Sleep-related breathing disorders incl. central sleep apnea (dose-dependent) - consider opioid taper
- Profound sedation/respiratory depression/coma/death with benzodiazepines, alcohol, or other CNS depressants - reserve for inadequate alternatives
- Neonatal opioid withdrawal syndrome with extended use in pregnancy (may be life-threatening)
- CYP3A4 inhibitors (or discontinuing inducers) may increase butorphanol levels - fatal respiratory depression possible; inducers may reduce efficacy/precipitate withdrawal
- Opioid-induced hyperalgesia and allodynia - consider dose decrease or opioid rotation
- Extra caution in elderly and hepatic or renal disease
Adverse reactions
- Somnolence (49%)
- Dizziness (23%)
- Nausea and/or vomiting (8%)
- Nasal congestion (13%, long-term use)
- Insomnia (11%, long-term use)
- Asthenia/lethargy
- Headache
- Sweating
- Nasal irritation/epistaxis
Pregnancy No adequate human studies; use only if benefit justifies fetal risk; extended use can cause neonatal opioid withdrawal syndrome (may be life-threatening); higher stillbirth/postimplantation loss in animals
Lactation Present in milk (est. 4 mcg/L with 2 mg IM QID - probably clinically insignificant); monitor breastfed infant for excess sedation and respiratory depression
⚠ BOXED WARNINGS
- Addiction, abuse and misuse
- Life-threatening respiratory depression
- Risk from concomitant use with benzodiazepines
Principal riskPrecipitated withdrawal; dysphoria from kappa agonism
Cost, est. cash$10–$300/month
Generic entry1997
Classes and tags
Clinical profile
Legacy pregnancy categoryC
Defining liabilityRespiratory depression, dependence and overdose; risk rises sharply with sedatives or impaired clearance.
Mechanism of action: Butorphanol ballicule
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