Jump to: navigation, search


Systematic (IUPAC) name
CAS number 42408-82-2
ATC code N02AX02 QR05DA90
PubChem CID 5361092
DrugBank APRD00835
ChemSpider 16735714
Chemical data
Formula Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox 
Mol. mass 327.473 g/mol
SMILES eMolecules & PubChem
Pharmacokinetic data
Bioavailability Nasal: 60-70%
Metabolism Hepatic hydroxylated & glucuronidated
Half-life 4-7 hours
Excretion Renal, 75%
Biliary, 11-14%
Fecal, 15%
Therapeutic considerations
Pregnancy cat. C/D (U.S.)
Legal status Schedule IV (US)
Routes IV, intranasal

Butorphanol(Stadol) (INN) is a morphinan-type synthetic opioid analgesic. Brand name Stadol was recently discontinued by the manufacturer. It is now only available in its generic formulations, manufactured by Novex, Mylan, Apotex and Roxane. Butorphanol is most closely structurally related to levorphanol. Butorphanol is available only as butorphanol tartrate in injectable and intranasal spray formulations.


Mechanism of action

Butorphanol exhibits partial agonist and antagonist activity at the μ opioid receptor and agonist activity at the κ opioid receptor.[1] Stimulation of these receptors on central nervous system neurons causes an intracellular inhibition of adenylate cyclase, closing of influx membrane calcium channels, and opening of membrane potassium channels. This leads to hyperpolarization of the cell membrane potential and suppression of action potential transmission of ascending pain pathways. Because of its κ-agonist activity, at analgesic doses butorphanol increases pulmonary arterial pressure and cardiac work. Additionally, κ-agonism can cause dysphoria at therapeutic or supertherapeutic doses; this gives butorphanol a lower potential for abuse than other opioid drugs.

Place in therapy

The most common indication for butorphanol is management of migraine using the intranasal spray formulation. It may also be used parenterally for management of moderate-to-severe pain, as a supplement for balanced general anesthesia, and management of pain during labor. Butorphanol is more effective in reducing pain in women than in men.[1]

In veterinary use, butorphanol ("Torbugesic") is widely used as a sedative and analgesic in dogs, cats and horses. For sedation, it may be combined with tranquilizers such as alpha-2 agonists (medetomidine (Domitor)), benzodiazepines, or phenothiazines (acepromazine) in dogs, cats and exotic animals. It is frequently combined with xylazine or detomidine (Domosedan etc) in horses[2].

Adverse effects

As with other opioid analgesics, central nervous system effects (such as sedation, confusion, and dizziness) are considerations with butorphanol. Nausea and vomiting are common. Less common are the gastrointestinal effects of other opioids (mostly constipation).

Proprietary preparations

Butorphanol is available in the U.S. as a generic drug; it is available in various nations under one of any number of trade names, including Moradol and Beforal (Brand name Stadol no longer available in the US); veterinary trade names include Butorphic, Dolorex, Morphasol, Torbugesic, and Torbutrol.

Use in horses

Butorphanol is a commonly used narcotic for pain relief in horses. It is administered either IM or IV, with its analgestic properties beginning to take effect about 15 minutes after injection and lasting 4 hours. It is also commonly paired with sedatives, such as xylazine and detomidine, to make the horse easier to handle during veterinary procedures.

Side effects, overdose, and precautions

Side effects specific to horses include sedation, CNS excitement (displayed by head pressing or tossing). Overdosing may result in seizures, falling, salivation, constipation, and muscle twitching. If an overdose occurs, a narcotic antagonist, such as naloxone, may be given. Caution should be used if Butorphanol is administered in addition to other narcotics, sedatives, depressants, or antihistamines as it will cause an additive effect.

Butorphanol can cross the placenta, and it will be present in the milk of lactating mares who are given the drug.

The drug is also prohibited for use in competition by most equestrian organizations, including the FEI, which considers it a class A drug.

In addition to horses, butorphanol with or without acepromazine is frequently used in veterinary settings for post-operative and accident-related pain in small mammals such as dogs, cats, ferrets, coatis, raccoons, mongooses, various marsupials, some rodents and perhaps some larger birds both in the operating suite and as a regular prescription medication for home use for management of moderate to severe pain. The efficacy of opioids (as well as other drugs that slow down the system like anaesthetics) in treating reptiles is a question about which there is currently not a lot of data.


  1. 1.0 1.1 Gear, RW; Miaskowski C, Gordon NC, Paul SM, Heller PH, Levine JD (November 1999). "The kappa opioid nalbuphine produces gender- and dose-dependent analgesia and antianalgesia in patients with postoperative pain". Pain 83 (2): 339–45. doi:10.1016/S0304-3959(99)00119-0. PMID 10534607. 
  2. NOAH Compendium of Data Sheets for Animal Medicines 2005


  • Katzung, Bertam G. (Ed.) (2001) Basic & Clinical Pharmacology (8th ed.). New York: McGraw-Hill. ISBN 0-8385-0598-8.
  • DiPiro, Joseph T. et al. (2005) Pharmacotherapy: A Pathophysiologic Approach (6th ed.). New York: McGraw-Hill. ISBN 0-07-141613-7.
  • Forney, Barbara C, MS, VMD. Equine Medications, Revised Edition.' Blood Horse Publications. Lexington, KY. Copyright 2007.
  • The Merck Manual of Veterinary Medicine, 2004 edition (English)
  • The Merck Manual, 2004 Edition (German)
  • Mosby's Drug Guide 2004


Premier Equine Classifieds


Subscribe to our newsletter and keep abreast of the latest news, articles and information delivered directly to your inbox.

Did You Know?

Modern horse breeds developed in response to a need for "form to function", the necessity to develop certain physical characteristics in order to perform a certain type of work... More...

The Gypsy Cob was originally bred to be a wagon horse and pulled wagons or caravans known as Vardos; a type of covered wagon that people lived in... More...

Archaeological evidence indicates that the Arabian horse bloodline dates back 4,500 years. Throughout history, Arabian horses spread around the world by both war and trade.... More...

That the term "Sporthorse" is a term used to describe a type of horse rather than any particular breed... More...