Levorphanol: the forgotten opioid
@article{Prommer2006LevorphanolTF, title={Levorphanol: the forgotten opioid}, author={Eric Prommer}, journal={Supportive Care in Cancer}, year={2006}, volume={15}, pages={259-264} }
BackgroundLevorphanol (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…
36 Citations
Levorphanol: Revisiting an Underutilized Analgesic
- Medicine, BiologyPalliative care
- 2014
The pharmacodynamics, pharmacology, and clinical efficacy of this often overlooked step 3 opioid are provided, which makes it potentially useful for neuropathic pain.
Levorphanol use: past, present and future
- Medicine, BiologyPostgraduate medicine
- 2016
The purpose of this review is to inform practitioners about the attributes of this opioid and reintroduce it to clinicians as an option for treating moderate to severe pain when alternative treatment options are inadequate, not indicated or contraindicated.
Is levorphanol a better option than methadone?
- MedicinePain medicine
- 2015
Unlike methadone, levorphanol is a more potent NMDA antagonist, possesses a higher affinity for DOR and KOR, has a shorter plasma half-life yet longer duration of action, has no CYP450 interactions or QTc prolongation risk, can be a viable option in the elderly, palliative care, and SCI patients, and has potentially a lower risk of drug-related Emergency Department visits compared to other opioids.
Pharmacological Characterization of Levorphanol, a G-Protein Biased Opioid Analgesic
- Biology, MedicineAnesthesia and analgesia
- 2019
Its G-protein signaling bias is consistent with its diminished respiratory depression, while its incomplete cross tolerance with morphine suggests it may prove valuable clinically with opioid rotation.
Commentary Is Levorphanol a Better Option than Methadone ?
- Medicine
- 2015
Background. Methadone has been a stalwart pharmacologic option for the management of opioid drug dependence for many years. It substitutes for opioid agonists and possesses certain pharmacokinetic…
Identifying Levorphanol Ingestion Using Urine Biomarkers in Health Care Patients.
- MedicinePain physician
- 2018
This article is the first to report urine concentrations of levorphanol/dextrorphan and 3-hydroxymorphinan in human urine and assesses the need for an enantiomeric analysis to distinguish between dextromethorphan andlevorphanol ingestion.
Levorphanol versus methadone use: safety considerations.
- Psychology, MedicineAnnals of palliative medicine
- 2020
The objective of this article is to review and compare the safety considerations for methadone and levorphanol use and to highlight the need for greater awareness of the risks and benefits of this substance.
Synthesis and opioid activity of novel 6-ketolevorphanol derivatives.
- Chemistry, BiologyMedicinal chemistry (Shariqah (United Arab Emirates))
- 2013
Novel 6-ketolevorphanol analogs with diverse substitution patterns at ring C were synthesized and their binding affinities at the μ,δ and κ opioid receptors were investigated, showing no significant potency at any of the opioid receptor types.
Tapentadol, Buprenorphine, and Levorphanol for the Treatment of Neuropathic Pain: a Systematic Review
- MedicineCurrent Pain and Headache Reports
- 2021
The role of tapentadol, buprenorphine, and levorphanol for neuropathic pain conditions requires robust research including randomized controlled trials to evaluate their efficacy and safety.
A comprehensive review of partial opioid agonists for the treatment of chronic pain.
- Medicine, BiologyBest practice & research. Clinical anaesthesiology
- 2020
References
SHOWING 1-10 OF 26 REFERENCES
Unidirectional analgesic cross-tolerance between morphine and levorphanol in the rat
- Biology, MedicinePain
- 1988
Serotonin and norepinephrine uptake inhibiting activity of centrally acting analgesics: structural determinants and role in antinociception.
- Biology, ChemistryThe Journal of pharmacology and experimental therapeutics
- 1995
Investigation of a diverse group of opioids revealed that structurally identifiable subgroups inhibited the neuronal reuptake of these monoamines, suggesting a broader role for the combination of mu opioid affinity and 5-hydroxytryptamine uptake inhibition in the activity of other antinociceptive agents.
Levorphanol: pharmacokinetics and steady-state plasma concentrations in patients with pain.
- Medicine, BiologyResearch communications in chemical pathology and pharmacology
- 1983
Effective analgesic steady-state concentrations of levorphanol in patients receiving a wide range of chronic oral and i.m. and oral administration of therapeutic doses of the drug to patients with pain seems to be maintained within a narrow plasma concentration range for each subject.
Differential agonist regulation of the human kappa-opioid receptor.
- Biology, ChemistryJournal of neurochemistry
- 1997
It is demonstrated that the human kappa receptor is differentially regulated by selective and nonselective opioid agonists, with selective agonists able to desensitize the receptor.
Opioid analgesics: comparative features and prescribing guidelines.
- Medicine, BiologyDrugs
- 1996
The management of pain with opioid analgesics demands frequent patient assessment and a readiness to re-evaluate the therapeutic plan in the setting of either inadequate relief or adverse effects.
Sublingual absorption of selected opioid analgesics
- BiologyClinical pharmacology and therapeutics
- 1988
The results indicate that although the sublingual absorption and apparent sublingUAL bioavailability of morphine are poor, the sublingsual absorption of methadone, fentanyl, and buprenorphine under controlled conditions is relatively high.
Pharmacokinetic-pharmacodynamic modeling of opioids.
- BiologyJournal of pain and symptom management
- 2005
Oral opioid therapy for chronic peripheral and central neuropathic pain.
- Medicine, PsychologyThe New England journal of medicine
- 2003
The reduction in the intensity of neuropathic pain was significantly greater during treatment with higher doses of opioids than with lower doses, and higher doses produced more side effects without significant additional benefit in terms of other outcome measures.
Differential Agonist Regulation of the Human κ‐Opioid Receptor
- Biology, Chemistry
- 1997
It is demonstrated that the human κ receptor is differentially regulated by selective and nonselective opioid agonists, with selective agonists able to desensitize the receptor.