Levorphanol: the forgotten opioid.

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Prommer E

Levorphanol: the forgotten opioid.

Support Care Cancer. 2007 Mar;15(3):259-64. Epub 2006 Oct 13.

PubMed ID

17039381 [ View in PubMed

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Abstract

BACKGROUND: Levorphanol (levo-3-hydroxy-N-methylmorphinan) is a strong opioid that is the only available opioid agonist of the morphinan series. Levorphanol was originally synthesized as a pharmacological alternative to morphine more than 40 years ago. It is considered a step-3 opioid by the World Health Organization (WHO) and has a greater potency than morphine. Analgesia produced by levorphanol is mediated via its interactions with mu, delta, and kappa opioid receptors. Levorphanol is also an N-methyl-D-aspartate (NMDA) receptor antagonist. There is evidence that levorphanol may inhibit uptake of norepinephrine and serotonin. Similar to morphine, levorphanol undergoes glucuronidation in the liver, and the glucuronidated products are excreted in the kidney. Levorphanol can be given orally, intravenously, and subcutaneously. OBJECTIVE: This article reviews the pharmacodynamics, pharmacology, and clinical efficacy for this often overlooked step-3 opioid. CONCLUSION: The long half-life of the drug increases the potential for drug accumulation. Levorphanol has clinical efficacy in neuropathic pain.

DrugBank Data that Cites this Article

Drug Targets

Drug	Target	Kind	Organism	Pharmacological Action	Actions
Levorphanol	Delta-type opioid receptor	Protein	Humans	Unknown	Agonist	Details
Levorphanol	Kappa-type opioid receptor	Protein	Humans	Unknown	Agonist	Details
Levorphanol	Mu-type opioid receptor	Protein	Humans	Yes	Agonist	Details