Norlevorphanol

Norlevorphanol is a morphinan derivative that is used as an analgesic. It is most commonly used in the treatment of moderate to severe pain. Norlevorphanol is a potent opioid analgesic that is approximately five to ten times more potent than morphine.

Pharmacology

Norlevorphanol acts primarily on the mu-opioid receptor, but also has effects on the kappa-opioid receptor and the delta-opioid receptor. It is a full agonist at the mu-opioid receptor, and this is thought to be the primary mechanism of its analgesic effect. The drug also has a high affinity for the kappa-opioid receptor, and this may contribute to its analgesic effect as well as its side effects.

Clinical Use

Norlevorphanol is used clinically for the management of moderate to severe pain. It is typically used in situations where other, less potent opioids have failed to provide adequate pain relief. The drug is usually administered orally, but can also be given by intravenous injection.

Side Effects

The most common side effects of Norlevorphanol are similar to those of other opioids and include nausea, vomiting, constipation, and drowsiness. More serious side effects can include respiratory depression, hypotension, and dependence.

History

Norlevorphanol was first synthesized in the 1940s as part of a series of morphinan derivatives. It was initially marketed as an analgesic under the brand name Levo-Dromoran.

See Also

• Opioid
• Morphinan
• Analgesic