化合物信息

Drug Groups

approved

Description

A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection. [PubChem]

Indication

For the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate

Pharmacology

Levorphanol is a potent synthetic opioid analgesic indicated for the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate. Levorphanol is similar to morphine in its actions, however it is up to 8 times more potent than morphine. Levorphanol produces a degree of respiratory depression similar to that produced by morphine at equianalgesic doses, and like many mu-opioid drugs, levorphanol produces euphoria or has a positive effect on mood in many individuals.

Toxicity

LD₅₀=150 mg/kg (orally in rats). Signs of overdose include nausea, emesis, dizziness, respiratory depression, hypotension, urinary retention, cardiac arrhythmias, allergic reactions, skin rash, and uticaria.

Affected Organisms

Biotransformation

Levorphanol is extensively metabolized in the liver and is eliminated as the glucuronide metabolite.

Absorption

Levorphanol is well absorbed after PO administration with peak plasma concentrations occurring approximately 1 hour after dosing.

Half Life

11-16 hours

Protein Binding

40%

Distribution

* 10 to 13 L/kg

Clearance

* 0.78 to 1.1 L/kg/hr

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