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Levorphanol

LEVO-DROMORAN

Pronunciation: lee-VOR-fa-noel

Levorphanol ballicule: receptor binding, kinetics and half-life diagram
Mechanism of action: Levorphanol ballicule

What it isFull mu-opioid agonist; severe pain.

Why this oneIts unusually long and variable persistence can sustain analgesia but makes titration harder than with morphine.

What limits itAccumulation can cause delayed sedation and respiratory depression; addiction and benzodiazepine warnings apply.

Levorphanol molecular structure (skeletal formula)
Molecular structure: Levorphanol

FDA-approved for

FDA label

BOXED WARNING Addiction, abuse, misuse; life-threatening respiratory depression; accidental ingestion can be fatal (esp. children); fatal risk with benzodiazepines/CNS depressants/alcohol; neonatal opioid withdrawal syndrome; opioid REMS.
FDA dosingPopulationStartTargetMax
Pain (opioid analgesic, opioid-naive)Adults1–2 mg q6–8h PRNTitrate to response3 mg q6–8h (higher if opioid-tolerant)

Titration Allow ~72h after each dose change to reach steady state before further adjustment (long half-life).

Renal Undefined

Hepatic Undefined

Instructions

Available strengths

Contraindications

Cautions

Adverse reactions

Pregnancy Insufficient human data; prolonged use can cause neonatal opioid withdrawal syndrome; animal malformations and ~50% embryolethality.

Lactation Undefined

Cost

Levorphanol (LEVO-DROMORAN)
What pharmacies pay · NADAC 9/30/26
Strength#/mogeneric $/unitCostPlus
1 mgtabper unitnot offered
2 mgtabper unit$10.65/eanot offered
3 mgtabper unitnot offered

Generic entry2000

⚠ BOXED WARNINGS

Classes and tags

Clinical profile

Therapeutic safety burden3 / 4
Overdose danger4 / 4
Weight-gain liability0 / 4
Sedation liability2 / 4
QT / Torsades0 / 4
Direct muscarinic antagonism0 / 4
Embryofetal risk2 / 4

Legacy pregnancy categoryC

Defining liabilityRespiratory depression, dependence and overdose; risk rises sharply with sedatives or impaired clearance.

Serotonin and MAOI

Provisional washout figures

SRI significance2 / 4
MAO-A inhibition0 / 4
Serotonin release0 / 4

Elevating mechanismSRI

Non-elevating actionNone recorded

Exposure dependenceNo serotonin-elevating mechanism identified

Evidence confidenceHigh

InterpretationRat synaptosome 5-HT uptake IC50 ~0.88 uM — second only to methadone (~0.25 uM) among narcotics tested and far above morphine (>1e-3 M). Multimodal opioid with SNRI-like action; proposed to contribute to neuropathic-pain efficacy. Replaces a stale opioid-template note.

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