Antalgin - General Information
A narcotic analgesic that may be habit-forming. It is nearly as effective orally as by injection.
Pharmacology of Antalgin
Antalgin 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. Antalgin is similar to morphine in its actions, however it is up to 8 times more potent than morphine. Antalgin 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.
Antalgin for patients
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.
Levo-Dromoran is contraindicated in patients hypersensitive to levorphanol tartrate.
Additional information about Antalgin
Antalgin Indication: For the management of moderate to severe pain or as a preoperative medication where an opioid analgesic is appropriate
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.
Drug Interactions: Cimetidine Cimetidine increases the effect of the narcotic
Naltrexone Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individual
Food Interactions: Take without regard to meals. Avoid alcohol.
Generic Name: Levorphanol
Synonyms: Dea No. 9220; Dea No. 9733; Levorfanol [Inn-Spanish]; Levorfanolo [Dcit]; Levorphanol Dl-Form; Levorphanol Tartrate; Levorphanolum [Inn-Latin]; Methorfinan [Czech]; Methorphinan; Racemethorphanum; Racemorfano [Inn-Spanish]; Levorphanal; Levorphan
Drug Category: Narcotics; Analgesics, Opioid
Drug Type: Small Molecule; Approved
Other Brand Names containing Levorphanol: Antalgin; Aromarone; Cetarin; Dromoran; Lemoran; Levo-Dromoran; Racemic Dromoran;
Absorption: Levorphanol is well absorbed after PO administration with peak plasma concentrations occurring approximately 1 hour after dosing.
Toxicity (Overdose): 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.
Protein Binding: 40%
Biotransformation: Levorphanol is extensively metabolized in the liver and is eliminated as the glucuronide metabolite.
Half Life: 11-16 hours
Dosage Forms of Antalgin: Injection, solution Subcutaneous
Injection, solution Intravenous
Injection, solution Intramuscular
Chemical IUPAC Name: Not Available
Chemical Formula: C17H23NO
Levorphanol on Wikipedia: http://en.wikipedia.org/wiki/Levorphanol
Organisms Affected: Humans and other mammals