Butorphanol

Mechanism-of-action classes: Competitive Opioid Antagonists; Opioid Agonists; Opioid Antagonists; Partial Opioid Agonists.

• Butorphanol tartrate nasal spray is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Limitations of Use : Because of the risks of addiction, abuse, and misuse, with opioids, which can occur at any dosage or duration [see WARNINGS ] reserve butorphanol tartrate nasal spray for use in patients for whom alternative treatment options (e.g., non-opioid analgesics): Have not been tolerated, or are not expected to be tolerated, Have not provided adequate analgesia, or are not expected to provide adequate analgesia Butorphanol tartrate nasal spray should not be used for an extended period of time unless the pain remains severe enough to require an opioid analgesic and for which alternative treatment options continue to be inadequate.

• Butorphanol tartrate nasal spray is contraindicated in: Patients with significant respiratory depression [see WARNINGS ] Patients with acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS ] Patients with known or suspected gastrointestinal obstruction, including paralytic ileus [see WARNINGS ] Patients with hypersensitivity to butorphanol tartrate, the preservative benzethonium chloride, or any of the formulation excipients (e.g., anaphylaxis) [see WARNINGS ])contraindicated

Important Dosage and Administration Instructions Butorphanol tartrate nasal spray should be prescribed only by healthcare professionals who are knowledgeable about the use of opioids and how to mitigate the associated risks. Use the lowest effective dosage for the shortest duration of time consistent with individual patient treatment goals [see WARNINGS ]. Because the risk of overdose increases as opioid doses increase, reserve titration to higher doses of butorphanol tartrate nasal spray for patients in whom lower doses are insufficiently effective and in whom the expected benefits of using a higher dose opioid clearly outweigh the substantial risks. Many acute pain conditions (e.g., the pain that occurs with a number of surgical procedures or acute musculoskeletal injuries) require no more than a few days of an opioid analgesic. Clinical guidelines on opioid prescribing for some acute pain conditions are available. There is variability in the opioid analgesic dose and duration needed to adequately manage pain due both to the cause of pain and to individual patient factors. Initiate the dosing regimen for each patient individually, taking into account the patient’s underlying cause and severity of pain, prior analgesic treatment and response, and risk factors for addiction, abuse, and misuse [see WARNINGS ]. Respiratory depression can occur at any time during opioid therapy, especially when initiating and following dosage increases with butorphanol tartrate nasal spray. Consider this risk when selecting an initial dose and when making dose adjustments [see WARNINGS ].

Addiction, Abuse, and Misuse Butorphanol tartrate nasal spray contains butorphanol, a Schedule IV controlled substance. As an opioid, butorphanol tartrate nasal spray exposes users to the risks of addiction, abuse, and misuse [see DRUG ABUSE AND DEPENDENCE ]. Although the risk of addiction in any individual is unknown, it can occur in patients appropriately prescribed butorphanol tartrate nasal spray. Addiction can occur at recommended dosages and if the drug is misused or abused. Assess each patient’s risk for opioid addiction, abuse, or misuse prior to prescribing butorphanol tartrate nasal spray, and reassess all patients receiving butorphanol tartrate nasal spray for the development of these behaviors and conditions. Risks are increased in patients with a personal or family history of substance abuse (including drug or alcohol abuse or addiction) or mental illness (e.g., major depression). The potential for these risks should not, however, prevent the proper management of pain in any given patient. Patients at increased risk may be prescribed opioids such as butorphanol tartrate nasal spray, but use in such patients necessitates intensive counseling about the risks and proper use of butorphanol tartrate nasal spray along with frequent reevaluation for signs of addiction, abuse, and misuse. Consider prescribing naloxone for the emergency treatment of opioid overdose (see WARNINGS , Life-Threatening Respiratory Depression ; DOSAGE AND ADMINISTRATION , Patient Access to Naloxone for the Emergency Treatment of Opioid Overdose ).

Clinical Trial Experience A total of 788 patients were studied in premarketing clinical trials of butorphanol tartrate nasal spray. In nearly all cases the type and incidence of side effects with butorphanol were those commonly observed with opioid analgesics. The adverse experiences described below are based on data from short-term and long-term clinical trials in patients receiving intranasal butorphanol, except acute studies in normal subjects. There has been no attempt to correct for placebo effect or to subtract the frequencies reported by placebo-treated patients in controlled trials. The most frequently reported adverse experiences across all clinical trials with Butorphanol Tartrate Nasal Spray were somnolence (49%), dizziness (23%), nausea and/or vomiting (8%). In long-term trials with butorphanol tartrate nasal spray only, nasal congestion (13%) and insomnia (11%) were frequently reported. The following adverse experiences were reported at a frequency of 1% or greater in clinical trials and were considered to be probably related to the use of butorphanol. Body as a Whole: Asthenia/lethargy, headache, sensation of heat, pain. Cardiovascular: Hypertension, hypotension Digestive: Anorexia, constipation, dry mouth, nausea and/or vomiting, diarrhea. Nervous: Anxiety, confusion, dizziness, euphoria, floating feeling, insomnia, nervousness, paresthesia, somnolence, tremor Respiratory: Epistaxis, nasal congestion, nasal irritation, rhinitis, sinus congestion, sinusitis, nose pain.

Clinical Presentation Acute overdose with butorphanol tartrate nasal spray can be manifested by respiratory depression, somnolence progressing to stupor or coma, skeletal muscle flaccidity, cold and clammy skin, constricted pupils, and, in some cases, pulmonary edema, bradycardia, hypotension, partial or complete airway obstruction, atypical snoring, and death. Marked mydriasis rather than miosis may be seen with hypoxia in overdose situations. Treatment of Overdose In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed. Employ other supportive measures (including oxygen and vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life-support techniques. Opioid antagonist, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose. For clinically significant respiratory or circulatory depression secondary to butorphanol tartrate overdose, administer an opioid antagonist.

• Jan 23, 1997ANDAANDA074626Hospira
• Mar 12, 2002ANDAANDA075824Hikma
• Dec 4, 2002ANDAANDA075499Apotex
• May 1, 2009ANDAANDA078400Hikma Farmaceutica

1. 1Drug Hypersensitivity4815%
2. 2Drug Ineffective4514%
3. 3Product Dose Omission Issue3712%
4. 4Nausea257.8%
5. 5Headache165.0%
6. 6Pain165.0%
7. 7Pruritus165.0%
8. 8Vomiting154.7%
9. 9Anxiety144.4%
10. 10Dyspnoea144.4%
11. 11Migraine134.1%
12. 12Product Quality Issue134.1%
13. 13Dizziness123.8%
14. 14Product Packaging Quantity Issue113.4%
15. 15Depression103.1%

Recent PubMed references pinned to Butorphanol as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.

• Impact of butorphanol combined with propofol general anesthesia on laboratory indicators and reproductive outcomes in elderly patients undergoing oocyte retrieval.
  Medicine · 2026 · Rao J, Wang J, Liu L, et al.
  PMID 42071792DOI 10.1097/MD.0000000000048487
• Effects of vatinoxan in horses sedated with detomidine and butorphanol for gastroscopy: A randomized clinical study.
  Veterinary journal (London, England : 1997) · 2026 · Jantunen N, Raekallio M, Karikoski N, et al.
  PMID 42025909DOI 10.1016/j.tvjl.2026.106680
• Effect of a Standardized Sedation Protocol on Portal Vein Velocity Measurements in Hospitalized Dogs Using Triplex-Doppler Ultrasonography.
  Veterinary radiology & ultrasound : the official journal of the American College of Veterinary Radiology and the International Veterinary Radiology Association · 2026 · Jamont W, Peschard AL, Augusto M, et al.
  PMID 42007642DOI 10.1111/vru.70175
• EVALUATION OF A BUTORPHANOL-MEDETOMIDINE REVERSIBLE ANESTHETIC PROTOCOL FOR MANED WOLVES (CHRYSOCYON BRACHYURUS ) UNDER MANAGED CARE.
  Journal of zoo and wildlife medicine : official publication of the American Association of Zoo Veterinarians · 2026 · Palmer AG, Delaski KM, Hayek LC, et al.
  PMID 41926260DOI 10.1638/2025-0026
• Dynamics of blood glucose changes and hormonal sensitivity under anesthesia with medetomidine-midazolam-butorphanol anesthesia in rats.
  Research in veterinary science · 2026 · Horii Y, Naitou K, Shiina T, et al.
  PMID 41903437DOI 10.1016/j.rvsc.2026.106159
• Evaluation of the efficacy and safety of a modified anesthetic protocol using dexmedetomidine, midazolam, and butorphanol in mice.
  The Journal of veterinary medical science · 2026 · Kida N, Takeda H, Sakamoto K, et al.
  PMID 41850854DOI 10.1292/jvms.25-0568
• Compatibility and Stability Study of Butorphanol, Nicardipine, Urapidil, and Tirofiban During Multidrug Simultaneous Infusion.
  Drug design, development and therapy · 2026 · Zhao X, Zhang L, Yu S, et al.
  PMID 41804455DOI 10.2147/DDDT.S578559
• Sedative and physiological effects of intramuscular alfaxalone 4% with butorphanol or dexmedetomidine in dogs - a randomized crossover study.
  Veterinary anaesthesia and analgesia · 2026 · Hoon TMAY, Pasloske K, Farry T, et al.
  PMID 41793846DOI 10.1016/j.vaa.2025.101174

The 10 most recently updated of 24 ClinicalTrials.gov registrations naming Butorphanol as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.

• EOIB for Pain After Laparoscopic Cholecystectomy
  Recruiting · Interventional · 56 enrolled · Shiyou Wei
  NCT07332546updated 2026-06-09
• Effects of Transversus Abdominis Plane Block on Recovery Quality and Maternal-Neonatal Outcomes After Cesarean Delivery
  Completed · Interventional · 83 enrolled · Qing Yuan
  NCT07478692updated 2026-03-17
• Butorphanol for Pain Relief After Cesarean Section: A Retrospective Study
  Not yet recruiting · Observational · 2,500 enrolled · Sichuan Provincial People's Hospital
  NCT07175363updated 2025-09-16
• Study on Gynecological Laparoscopy Under Total Intravenous Anesthesia
  Completed · Interventional · 59 enrolled · Wuhan Children's Hospital
  NCT06524596updated 2024-07-29
• Esketamine and Butorphanol for Post-Lobectomy Pain
  Completed · Phase 4 · Interventional · 223 enrolled · Second People's Hospital of Hefei City
  NCT06398834updated 2024-05-06
• Butorphanol in Pain Following Ablation for Hepatic Tumor
  Completed · Interventional · 300 enrolled · Bibo Wang
  NCT06031129updated 2023-09-11
• Effect of Butorphanol on Colonoscopy for Patients With Postoperative Visceral Pain
  Completed · Phase 4 · Interventional · 203 enrolled · Beijing Tiantan Hospital
  NCT04477733updated 2022-02-21
• Efficacy and Safety of Butorphanol Tartrate Injection for the Patients With Mechanical Ventilation
  Unknown · Interventional · 40 enrolled · Shanghai Zhongshan Hospital
  NCT05201560updated 2022-01-21
• Hydromorphone for ICU-analgesia in Patients With Non-mechanical Ventilation
  Unknown · Phase 4 · Interventional · 530 enrolled · Nanfang Hospital, Southern Medical University
  NCT04436224updated 2022-01-20
• Effect of Different Sedation and Analgesia Strategies on Patients With Mechanical Ventilation
  Unknown · Phase 4 · Interventional · 300 enrolled · The Affiliated Hospital of Qingdao University
  NCT05024799updated 2021-08-27

Frequently asked questions

How does Butorphanol work?

Mechanism-of-action classes: Competitive Opioid Antagonists; Opioid Agonists; Opioid Antagonists; Partial Opioid Agonists.

What is Butorphanol used for?

According to FDA labeling, Butorphanol carries indications including: Butorphanol tartrate nasal spray is indicated for the management of pain severe enough to require an opioid analgesic and for which alternative treatments are inadequate. Limitations of Use : Because of the risks of addiction, abuse, and misuse, with opioids, which can occur at any dosage or duration [see WARNINGS ] reserve butorphanol tartrate nasal spray for use in patients for whom alternative treatment options (e.g., non-opioid analgesics): Have not been tolerated, or are not expected to be tolerated, Have not provided adequate analgesia, or are not expected to provide adequate analgesia Butorphanol tartrate nasal spray should not be used for an extended period of time unless the pain remains severe enough to require an opioid analgesic and for which alternative treatment options continue to be inadequate.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.

What class of drug is Butorphanol?

Butorphanol is classified as Morphinan derivatives, Opioid Agonist/Antagonist, Competitive Opioid Antagonists, Opioid Agonists, Opioid Antagonists, Partial Opioid Agonists, Decreased Organized Electrical Activity.

What are the brand names for Butorphanol?

Butorphanol is marketed under brand names including Butorphic, Dolorex Solution, Torbugesic, Torphadine, Vetorphic.

What are the contraindications for Butorphanol?

Butorphanol labeling lists contraindications including: Butorphanol tartrate nasal spray is contraindicated in: Patients with significant respiratory depression [see WARNINGS ] Patients with acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment [see WARNINGS ] Patients with known or suspected gastrointestinal obstruction, including paralytic ileus [see WARNINGS ] Patients with hypersensitivity to butorphanol tartrate, the preservative benzethonium chloride, or any of the formulation excipients (e.g., anaphylaxis) [see WARNINGS ]). Always consult the full prescribing information and a clinician.