TY - JOUR
T1 - Levorphanol
T2 - The forgotten opioid
AU - Prommer, Eric
PY - 2007/3
Y1 - 2007/3
N2 - 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 μ, δ, and κ 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.
AB - 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 μ, δ, and κ 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.
KW - Glucuronidation
KW - Levorphanol
KW - NMDA
KW - Opioids
KW - Pain
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U2 - 10.1007/s00520-006-0146-2
DO - 10.1007/s00520-006-0146-2
M3 - Review article
C2 - 17039381
AN - SCOPUS:33847139761
SN - 0941-4355
VL - 15
SP - 259
EP - 264
JO - Supportive Care in Cancer
JF - Supportive Care in Cancer
IS - 3
ER -