Butorphan

Butorphanol is a morphinan-type synthetic agonist–antagonist opioid characterized by a kappa-opioid receptor (KOR) agonist and mu-opioid receptor (MOR) antagonist activity. It is structurally most similar to levorphanol. Butorphanol is available in intranasal form and injectable form.

Pharmacology

Butorphanol exhibits partial agonist and antagonist activity at the mu opioid receptor, and antagonist activity at the kappa opioid receptor. The agonist or antagonist activity of butorphanol at the kappa opioid receptor may be dependent upon the degree of endogenous activity at the receptor.

Medical uses

Butorphanol is used for the relief of moderate to severe pain. It can also be used as a preoperative or preanesthetic medication to alleviate anxiety and induce sedation. It is also used for the treatment of severe, chronic pain in certain patients.

Side effects

Common side effects of butorphanol include sedation, dizziness, nausea, vomiting, and sweating. Less common side effects can include confusion, hallucinations, and severe respiratory depression.

Contraindications

Butorphanol is contraindicated in patients with a known hypersensitivity to the drug, and in patients with severe respiratory depression.

See also

• Opioid
• Morphinan
• Kappa-opioid receptor
• Mu-opioid receptor

Butorphan Resources
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