DEA No. 9720

• Analgesics, Opioid
• Antitussive Agents
• Narcotic Antagonists
• Narcotics
• ATC:N02AF01

• Butorfanol
• Butorfanol [INN-Spanish]
• Butorphanol
• Butorphanol Tartrate Preservative Free
• Butorphanol [USAN:BAN:INN]
• Butorphanolum [INN-Latin]
• DEA No. 9720
• Stadol
• Stadol Preservative Free

• No information avaliable

C₂₁H₂₉NO₂

http://www.rxlist.com/cgi/generic2/butor.htm

DEA_No._9720 FDA

DEA_No._9720 MSDS

No information avaliable

327.461 g/mol

No information avaliable

Moderate

Solid

4.176

Drops; Drug premix; Gel; Globules; Liquid; Powder for solution; Solution; Spray; Tablet

For the management of pain when the use of an opioid analgesic is appropriate. Also indicated as a preoperative or preanesthetic medication, as a supplement to balanced anesthesia, and for the relief of pain during labor.

Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorphanol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord.

Rapidly absorbed after intramuscular injection and peak plasma levels are reached in 20-40 minutes. The absolute bioavailability is 60-70% and is unchanged in patients with allergic rhinitis. In patients using a nasal vasoconstrictor (oxymetazoline) the fraction of the dose absorbed was unchanged, but the rate of absorption was slowed. Oral bioavailability is only 5-17% because of extensive first-pass metabolism.

The clinical manifestations of butorphanol overdose are those of opioid drugs in general. The most serious symptoms are hypoventilation, cardiovascular insufficiency, coma, and death.

Humans and other mammals