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Butorphanol

Name: Butorphanol
Description: A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain. (PubChem) Pharmacology: Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorphanol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord. Mechanism of action: Butorphanol is a mixed agonist-antagonist with low intrinsic activity at receptors of the -opioid type (morphine-like). It is also an agonist at -opioid receptors. Its interactions with these receptors in the central nervous system apparently mediate most of its pharmacologic effects, including analgesia. Drug type: Approved. Illicit. Small Molecule. Drug category: Analgesics, Opioid. Antitussive Agents. Narcotic Antagonists. Narcotics
Synonym(s): Butorfanol, Butorfanol (INN-Spanish), Butorphanol Tartrate, Butorphanolum (INN-Latin), Beforal, Moradol, Stadol, Stadol NS
Related to: Delta-type opioid receptor, Kappa-type opioid receptor, Mu-type opioid receptor
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00611
Id: DB00611
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Commenttaken from DrugBank
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00611  +
DefinitionA synthetic morphinan analgesic with narco A synthetic morphinan analgesic with narcotic antagonist action. It is used in the management of severe pain. (PubChem) Pharmacology: Butorphanol is a synthetic opioid agonist-antagonist analgesic with a pharmacological and therapeutic profile that has been well established since its launch as a parenteral formulation in 1978. The introduction of a transnasal formulation of butorphanol represents a new and noninvasive presentation of an analgesic for moderate to severe pain. This route of administration bypasses the gastrointestinal tract, and this is an advantage for a drug such as butorphanol that undergoes significant first-pass metabolism after oral administration. The onset of action and systemic bioavailability of butorphanol following transnasal delivery are similar to those after parenteral administration. Butorphanol blocks pain impulses at specific sites in the brain and spinal cord. Mechanism of action: Butorphanol is a mixed agonist-antagonist with low intrinsic activity at receptors of the -opioid type (morphine-like). It is also an agonist at -opioid receptors. Its interactions with these receptors in the central nervous system apparently mediate most of its pharmacologic effects, including analgesia. Drug type: Approved. Illicit. Small Molecule. Drug category: Analgesics, Opioid. Antitussive Agents. Narcotic Antagonists. Narcotics ve Agents. Narcotic Antagonists. Narcotics
Has roleDrug  +
IdDB00611  +
LabelButorphanol  +
ModifiedDate14 April 2014  +
RelatedToDelta-type opioid receptor  +, Kappa-type opioid receptor  +, and Mu-type opioid receptor  +
SuperCategoryMolecular entity  +
SynonymButorfanol  +, Butorfanol (INN-Spanish)  +, Butorphanol Tartrate  +, Butorphanolum (INN-Latin)  +, Beforal  +, Moradol  +, Stadol  +, and Stadol NS  +