Brands, Medical Use, Clinical Data
- Analgesic Antagonists
- Morphine Antidotes
- Antinarcotic Agents
- Narcotic Antagonists
- Solution for injection (intramuscular, subcutaneous or intravenous)
Brands / Synonyms
Levallofano [Dcit]; Levallorphane [Inn-French]; Levallorphanum [Inn-Latin]; Levalorfano [Inn-Spanish]; Lorfan; Naloxiphan
For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.
Levallorphan, an opioid antagonist similar to naloxone, is used to treat drug overdoses. Levallorphan differs from naloxone in that it also possesses some agonist properties. It is an analogue of levelorphanol that counteracts the actions of narcotic analgesics such as morphine. It is used especially in the treatment of respiratory depression due to narcotic overdoses. Levallorphan prevents or reverses the effects of opioids including respiratory depression, sedation and hypotension. Also, it can reverse the psychotomimetic and dysphoric effects of agonist-antagonists such as pentazocine.
Mechanism of Action
Levallorphan antagonizes opioid effects by competing for the same receptor sites. It binds to the opioid mu receptor and the nicotinic acetylcholine receptor alpha2/alpha3.
Oral, rat LD50: 109±4 mg/kg
Biotrnasformation / Drug Metabolism
Levallorphan is contraindicated in patients known to be hypersensitive to