Levorphanol drug data and news

Levorphanol drug data, resources, and news articles (when available). Onconews.org provides news on cancer research. This section, which includes profiles on medicines that may or not be cancer-related is in beta form. If things run smoothly we will be releasing a new format late in the summer of 2006.

Generic name Levorphanol
Brand Names/Synonyms Antalgin; Aromarone; Cetarin; Dea No. 9220; Dea No. 9733; Dromoran; HSDB 3349; LEVORPHANOL; Lemoran; Levo-Dromoran; Levorfanol [Inn-Spanish]; Levorfanolo [Dcit]; Levorphan; Levorphanal; Levorphanol; Levorphanol Dl-Form; Levorphanol Tartrate; Levorphanolum [Inn-Latin]; Methorfinan [Czech]; Methorphinan; NU 2206; Orphan; Racemethorphanum; Racemic Dromoran; Racemorfano [Inn-Spanish]; Racemorphan; Racemorphan [Ban:Inn]; Racemorphane [Inn-French]; Racemorphanum [Inn-Latin]
Indication For the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate
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Description Not Available
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.
Mechanism Of Action Like other mu-agonist opioids it is believed to act at receptors in the periventricular and periaqueductal gray matter in both the brain and spinal cord to alter the transmission and perception of pain.
Levorphanol News
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Dosage Forms TABLET
Drug_Category Narcotics; Analgesics, Opioid
Absorption Levorphanol is well absorbed after PO administration with peak plasma concentrations occurring approximately 1 hour after dosing.
Interactions Interactions for Levorphanol:
Interactions with Other CNS Agents: Concurrent use of Levo-Dromoran with all central nervous system depressants (eg, alcohol, sedatives, hypnotics, other opioids, general anesthetics, barbiturates, tricyclic antidepressants, phenothiazines, tranquilizers, skeletal muscle relaxants and antihistamines) may result in additive central nervous system depressant effects. Respiratory depression, hypotension, and profound sedation or coma may occur. When such combined therapy is contemplated, the dose of one or both agents should be reduced. Although no interaction between MAO inhibitors and Levo-Dromoran has been observed, it is not recommended for use with MAO inhibitors.

Most cases of serious or fatal adverse events involving Levo-Dromoran reported to the manufacturer or the FDA have involved either the administration of large initial doses or too frequent doses of the drug to nonopioid tolerant patients, or the simultaneous administration of levorphanol with other drugs affecting respiration. The initial dose of levorphanol should be reduced by approximately 50% or more when it is given to patients along with another drug affecting respiration.

Interactions with Mixed Agonist/Antagonist Opioid Analgesics:   Agonist/antagonist analgesics (eg, pentazocine, nalbuphine, butorphanol, dezocine and buprenorphine) should NOT be administered to a patient who has received or is receiving a course of therapy with a pure agonist opioid analgesic such as Levo-Dromoran. In opioid-dependent patients, mixed agonist/antagonist analgesics may precipitate withdrawal symptoms.

Toxicity Oral, rat LD50: 150 mg/kg. Signs of overdose include nausea, emesis, dizziness, respiratory depression, hypotension, urinary retention, cardiac arrhythmias, allergic reactions, skin rash, and uticaria.
Organisms Affected Humans and other mammals
Chemical IUPAC Name Not Available
Chemical Formula C17H23NO
Molecular Weight 257.371 g/mol
Smiles String CN1CCC23CCCCC2C1CC4=C3C=C(C=C4)O
Melting Point 198-199 °C
Water Solubility 1840 mg/L
State Solid
LogP/Hphobicity 3.986
Isoelectric Point 9.58
Biotransformation Levorphanol is extensively metabolized in the liver and is eliminated as the glucuronide metabolite.
Half Life 11-16 hours
Protein Binding [%] 40%
RxList Link RXlist
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Drug Reference http://www.drugs.com/cons/Levorphanol.html
http://www.rxlist.com/cgi/generic2/levorphanol.htm
Drug Type Approved Drug
Accession No APRD00764
CAS Registry Number 77-07-6
KEGG Compound ID C08014
PubChem ID SID:10214
PharmGKB ID PA450219
SwissProt ID Not Available
GenBank ID Not Available
Drug ID Number [DIN] Not Available

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