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Propoxyphene

Name: Propoxyphene
Description: A narcotic analgesic structurally related to methadone. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect. (PubChem) Pharmacology: Propoxyphene, a synthetic opiate agonist, is structurally similar to methadone. The analgesic effect of propoxyphene is due to the d-isomer, dextropropoxyphene. It binds to the opiate receptors and leads to a decrease of the perception of pain stimuli. Mechanism of action: Propoxyphene acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS). Propoxyphene primarily affects OP3 receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as propoxyphene also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. Drug type: Approved. Illicit. Small Molecule. Drug category: Analgesics. Analgesics, Opioid. Antitussives. Narcotics
Synonym(s): D-Propoxyphene, Dextropropoxyphene, Dextropropoxyphene-M, Dextroproxifeno, Propoxyphene HCl, Algafan, Antalvic, Darvon, Darvon-N, Deprancol, Depromic, Dolene, Dolocap, Doloxen, Doloxene, Erantin, Femadol, Harmar, Kesso-Gesic, Propacet, Prophene 65, Propoxychel, Propoxyphene HCl 65, Proxagesic
Has role: Drug
Super-category: Molecular entity
URL: http://www.drugbank.ca/drugs/DB00647
Id: CHEBI: 8497
Related to: Delta-type opioid receptor, Kappa-type opioid receptor, Mu-type opioid receptor
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Bandrow, Ccdbuser, Nifbot2



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Commenttaken from DrugBank
CurationStatusuncurated  +
CuratorAb  +
DefiningCitationhttp://www.drugbank.ca/drugs/DB00647  +
DefinitionA narcotic analgesic structurally related A narcotic analgesic structurally related to methadone. Only the dextro-isomer has an analgesic effect; the levo-isomer appears to exert an antitussive effect. (PubChem) Pharmacology: Propoxyphene, a synthetic opiate agonist, is structurally similar to methadone. The analgesic effect of propoxyphene is due to the d-isomer, dextropropoxyphene. It binds to the opiate receptors and leads to a decrease of the perception of pain stimuli. Mechanism of action: Propoxyphene acts as a weak agonist at OP1, OP2, and OP3 opiate receptors within the central nervous system (CNS). Propoxyphene primarily affects OP3 receptors, which are coupled with G-protein receptors and function as modulators, both positive and negative, of synaptic transmission via G-proteins that activate effector proteins. Binding of the opiate stimulates the exchange of GTP for GDP on the G-protein complex. As the effector system is adenylate cyclase and cAMP located at the inner surface of the plasma membrane, opioids decrease intracellular cAMP by inhibiting adenylate cyclase. Subsequently, the release of nociceptive neurotransmitters such as substance P, GABA, dopamine, acetylcholine, and noradrenaline is inhibited. Opioids such as propoxyphene also inhibit the release of vasopressin, somatostatin, insulin, and glucagon. Opioids close N-type voltage-operated calcium channels (OP2-receptor agonist) and open calcium-dependent inwardly rectifying potassium channels (OP3 and OP1 receptor agonist). This results in hyperpolarization and reduced neuronal excitability. Drug type: Approved. Illicit. Small Molecule. Drug category: Analgesics. Analgesics, Opioid. Antitussives. Narcotics nalgesics, Opioid. Antitussives. Narcotics
Has roleDrug  +
IdCHEBI: 8497  +
LabelPropoxyphene  +
ModifiedDate14 April 2014  +
RelatedToDelta-type opioid receptor  +, Kappa-type opioid receptor  +, and Mu-type opioid receptor  +
SuperCategoryMolecular entity  +
SynonymD-Propoxyphene  +, Dextropropoxyphene  +, Dextropropoxyphene-M  +, Dextroproxifeno  +, Propoxyphene HCl  +, Algafan  +, Antalvic  +, Darvon  +, Darvon-N  +, Deprancol  +, Depromic  +, Dolene  +, Dolocap  +, Doloxen  +, Doloxene  +, Erantin  +, Femadol  +, Harmar  +, Kesso-Gesic  +, Propacet  +, Prophene 65  +, Propoxychel  +, Propoxyphene HCl 65  +, and Proxagesic  +