While butorphanol can be made from thebaine, it is usually manufactured synthetically.
It was initially available in injectable formulations for human (Stadol®) and veterinary (Torbugesic® and Torbutrol®) use.
More recently, a nasal spray (Stadol NS®) became available, and significant diversion and abuse of this product led to the 1997 control of butorphanol in Schedule IV of the CSA. Butorphanol is a clear example of a drug gaining favor as a drug of abuse only after it became available in a form that facilitated its mode of administration (nasal spray v. injection).
Now only available in its generic formulations,the most common indication for butorphanol is management of migraine using the intranasal spray formulation. It may also be used for management of moderate-to-severe pain, and as a supplement for balanced general anesthesia.
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). Another side effect experienced by people taking the medication is increased perspiration.