Short answer: Butorphanol is a prescription opioid that activates kappa opioid receptors and partly blocks mu receptors. It is a Schedule IV controlled substance, most often used as a nasal spray for acute pain. It can cause dependence and can trigger withdrawal in people who take other opioids.
Key takeaways
- What it is: Butorphanol is a mixed opioid agonist-antagonist and a Schedule IV controlled substance in the US.
- Main uses: Pain; migraine (nasal spray, off-label); labor.
- Timing: effects start in about 15 minutes (nasal) and last 3 to 5 hours.
- Most dangerous mix: Benzodiazepines (alprazolam, diazepam, clonazepam), which can cause profound sedation, slowed breathing, coma, death.
- Naloxone: it reverses an overdose.
- Dependence risk: Moderate.
- Legal route: only with a prescription from a DEA-registered clinician, filled by a licensed pharmacy.
What is butorphanol?
Butorphanol is approved for pain severe enough to require an opioid. The injection is used in labor and before surgery, and the nasal spray for acute pain, including, off-label, migraine attacks.
As a mixed agonist-antagonist, its effect on breathing levels off at higher doses, but it still causes sedation and can cause dangerous slowed breathing, especially with other depressants.
Quick facts
| Fact | Butorphanol |
|---|---|
| Generic name | Butorphanol tartrate |
| Brand names | Stadol NS (discontinued brand); generic nasal spray and injection |
| Drug class | Mixed opioid agonist-antagonist |
| US legal status | Schedule IV, prescription only (since 1997) |
| Approved uses | Pain severe enough to require an opioid; pain during labor and before surgery (injection) |
| Forms | Nasal spray (1 mg per spray), injection |
| Onset | About 15 minutes (nasal) |
| Half-life | About 5 to 6 hours |
| Reversal agent | Naloxone |
How long does butorphanol last?
- Starts working: About 15 minutes (nasal)
- Effects last: 3 to 5 hours
- Half-life: About 5 to 6 hours
Pain relief from the nasal spray usually lasts 3 to 5 hours.
Timing varies with the dose, the form, how it is taken, liver and kidney function, age, and other drugs taken at the same time.
What are the biggest risks of butorphanol?
The FDA requires boxed warnings, its strongest, on butorphanol products, including:
- Addiction, abuse, and misuse, which can lead to overdose and death.
- Life-threatening slowed breathing, especially when starting treatment or after a dose increase.
- Accidental ingestion, especially by children, can cause a fatal overdose.
- Use with benzodiazepines or other central nervous system depressants, including alcohol, can cause profound sedation, slowed breathing, coma, and death.
Common side effects include drowsiness, dizziness, nausea, nasal congestion, and unpleasant mood effects such as anxiety or feeling detached.
Rebound headache and dependence: frequent use for migraine can lead to more frequent headaches, dependence, and misuse.
Withdrawal in opioid users: because it partly blocks mu receptors, butorphanol can cause sudden withdrawal in people dependent on other opioids.
What should you never mix with butorphanol?
| Combined with | What happens | Label guidance |
|---|---|---|
| Benzodiazepines (alprazolam, diazepam, clonazepam) | Profound sedation, slowed breathing, coma, death | Boxed warning; avoid unless no alternative |
| Alcohol | Stronger sedation and slowed breathing | Avoid |
| Gabapentin, pregabalin, sleep medicines, muscle relaxants | Additive sedation and breathing problems | Use caution; lower doses |
| Full opioid agonists in dependent patients | Sudden withdrawal; reduced pain relief | Avoid |
| Nasal decongestant sprays (oxymetazoline) | Slower absorption of butorphanol | Be aware |
Check any combination with the DoseUses combination checker or ask a pharmacist.
What are the signs of a butorphanol overdose, and what should you do?
Butorphanol overdose causes extreme sleepiness, confusion, slow breathing, and low blood pressure, especially combined with alcohol or sedatives.
If someone may have overdosed
- Call 911 if the person is unresponsive, cannot be woken, has blue or gray lips, or is breathing slowly or not at all.
- Give naloxone (Narcan or a generic nasal spray, sold without a prescription) into one nostril. If there is no response after 2 to 3 minutes, give another dose.
- If you are trained, give rescue breaths. Otherwise place the person on their side so they do not choke.
- Stay with them. Naloxone can wear off before butorphanol does, so the overdose can return even after the person wakes up.
- Most states have Good Samaritan laws that protect people who call 911 for an overdose from some drug charges.
What is butorphanol withdrawal like, and how long does it last?
People who take butorphanol regularly for more than a few weeks become physically dependent, even when they take it exactly as prescribed. Dependence is not the same as addiction, but it means stopping suddenly causes withdrawal.
- 12 to 24 hoursEarly symptomsAnxiety, restlessness, yawning, sweating, runny nose, watery eyes, and muscle aches.
- Days 2 to 4Peak withdrawalDiarrhea, stomach cramps, nausea and vomiting, goosebumps, dilated pupils, fast heartbeat, and strong cravings. Rarely dangerous in healthy adults, but dehydration can be serious.
- 1 to 2 weeksLingering symptomsPoor sleep, low mood, low energy, and cravings can continue for weeks. Tolerance falls quickly, which raises the risk of overdose if use restarts.
See the withdrawal timelines and the full butorphanol withdrawal guide.
Is butorphanol legal?
In the United States, butorphanol is a Schedule IV controlled substance. The only legal way to get it is with a prescription from a clinician registered with the Drug Enforcement Administration (DEA), filled by a licensed pharmacy. Depending on state law, that can be a physician, nurse practitioner, or physician assistant.
- Refills: a Schedule IV prescription can be refilled up to five times within six months of the date it was written. After that, a new prescription is needed.
- Telehealth: federal flexibilities let DEA-registered clinicians prescribe Schedule II to V medicines after a telemedicine visit, without a prior in-person exam, through December 31, 2026. A permanent DEA rule was under final review in late 2026. State rules can be stricter.
- Monitoring: prescribers and pharmacists in most states check a prescription drug monitoring program, a database of controlled-substance prescriptions, before prescribing or dispensing.
Outside the United States
| Country | Status |
|---|---|
| International | Not under UN control; controlled nationally in some countries |
Frequently asked questions about butorphanol
Is butorphanol an opioid?
Yes. It is a mixed agonist-antagonist opioid and a Schedule IV controlled substance.
Is butorphanol good for migraine?
It can relieve migraine pain, but guidelines discourage opioids for migraine because of rebound headaches and dependence.
Can butorphanol be taken with oxycodone?
No. It can block other opioids and cause withdrawal.
Is butorphanol used in animals?
Yes. It is widely used as a sedative and pain reliever in veterinary medicine.
How long does butorphanol last?
Pain relief from the nasal spray usually lasts 3 to 5 hours.
Sources
- butorphanol prescribing information, DailyMed, US National Library of Medicine.
- FDA warns about serious risks and death when combining opioid pain or cough medicines with benzodiazepines, US Food and Drug Administration, 2016.
- Information about naloxone and nalmefene, US Food and Drug Administration.
- CDC Clinical Practice Guideline for Prescribing Opioids for Pain, 2022, Centers for Disease Control and Prevention, MMWR.
- Controlled Substance Schedules, DEA Diversion Control Division.
- 21 CFR 1306.22, Refilling of prescriptions (Schedules III and IV), Electronic Code of Federal Regulations.
- Prescribing controlled substances via telehealth, US Department of Health and Human Services.
- BeSafeRx: Your Source for Online Pharmacy Information, US Food and Drug Administration.
This guide summarizes the sourced DoseUses Butorphanol profile, written from FDA labels, DEA rules, and federal health agencies. It is educational and is not medical advice. Last updated October 5, 2026.
