Levallorphan

Levallorphan (also known as Levo-allyl-orphanol, Naloxiphan, and Ro 5-1550) is an opioid antagonist of the morphinan series that was introduced in 1954 for the treatment of opioid overdose and addiction. It is related to naloxone and naltrexone and is similar in effects, but has a longer duration of action. Levallorphan is not currently in common use.

Pharmacology

Levallorphan acts as an antagonist at the μ-opioid receptor (MOR), κ-opioid receptor (KOR), and, to a lesser extent, at the δ-opioid receptor (DOR). It has high affinity for the MOR and KOR, and lower affinity for the DOR. Levallorphan is also a κ-opioid receptor agonist, and its action at this receptor may contribute to its analgesic effects.

Medical uses

Levallorphan was originally used in the treatment of opioid overdose and addiction. It can reverse the effects of opioids, including respiratory depression, sedation, and hypotension. However, it is not currently in common use for these indications.

Side effects

Side effects of levallorphan can include nausea, vomiting, and sweating. It can also cause hallucinations and other psychological effects, particularly at high doses.

History

Levallorphan was introduced in 1954 for the treatment of opioid overdose and addiction. It was later found to have potential as a treatment for other conditions, including chronic pain and cough, but these uses have not been widely adopted.

See also

• Naloxone
• Naltrexone
• Opioid antagonist
• Opioid overdose

References

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