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Naloxiphan

Naloxiphan - General Information

An opioid antagonist with properties similar to those of naloxone; in addition it also possesses some agonist properties. It should be used cautiously; levallorphan reverses severe opioid-induced respiratory depression but may exacerbate respiratory depression such as that induced by alcohol or other non-opioid central depressants. (From Martindale, The Extra Pharmacopoeia, 30th ed, p683)

 

Pharmacology of Naloxiphan

Naloxiphan, an opioid antagonist similar to naloxone, is used to treat drug overdoses. Naloxiphan 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. Naloxiphan 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.

 

Naloxiphan for patients

 

Naloxiphan Interactions

 

Naloxiphan Contraindications

Levallorphan is contraindicated in patients known to be hypersensitive to it.

 

Additional information about Naloxiphan

Naloxiphan Indication: For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.
Mechanism Of Action: Naloxiphan antagonizes opioid effects by competing for the same receptor sites. It binds to the opioid mu receptor and the nicotinic acetylcholine receptor alpha2/alpha3.
Drug Interactions: Not Available
Food Interactions: Not Available
Generic Name: Levallorphan
Synonyms: Not Available
Drug Category: Analgesic Antagonists; Morphine Antidotes; Antinarcotic Agents; Narcotic Antagonists
Drug Type: Small Molecule; Approved

Other Brand Names containing Levallorphan: Levallofano [Dcit]; Levallorphane [Inn-French]; Levallorphanum [Inn-Latin]; Levalorfano [Inn-Spanish]; Lorfan; Naloxiphan;
Absorption: Rapidly absorbed.
Toxicity (Overdose): Oral, rat LD50: 109±4 mg/kg
Protein Binding: Not Available
Biotransformation: Hepatic.
Half Life: 1 hour
Dosage Forms of Naloxiphan: Not Available
Chemical IUPAC Name: adamantan-1-amine
Chemical Formula: C19H25NO
Levallorphan on Wikipedia: Not Available
Organisms Affected: Humans and other mammals