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Active ingredient: Levallorphan - Brands, Medical Use, Clinical Data

Brands, Medical Use, Clinical Data

Drug Category

  • Analgesic Antagonists
  • Morphine Antidotes
  • Antinarcotic Agents
  • Narcotic Antagonists

Dosage Forms

  • Solution for injection (intramuscular, subcutaneous or intravenous)

Brands / Synonyms

Levallofano [Dcit]; Levallorphane [Inn-French]; Levallorphanum [Inn-Latin]; Levalorfano [Inn-Spanish]; Lorfan; Naloxiphan

Indications

For the complete or partial reversal of narcotic depression, including respiratory depression, induced by opioids.

Pharmacology

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.

Absorption

Rapidly absorbed.

Toxicity

Oral, rat LD50: 109±4 mg/kg

Biotrnasformation / Drug Metabolism

Hepatic.

Contraindications

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

Drug Interactions

Not Available

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