Name: | Dextropropoxyphene |
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PubChem Compound ID: | 10100 |
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. |
Molecular formula: | C22H29NO2 |
Molecular weight: | 339.471 g/mol |
Synonyms: |
alpha-D-4-Dimethylamino-3-methyl-1,2-diphenyl-2-butanol-propionat [German]; (S)-alpha-(2-(Dimethylamino)-1-methylethyl)-alpha-phenylbenzeneethanol propanoate; Antalvic; (+)-1,2-Diphenyl-2-propionoxy-3-methyl-4-dimethylaminobutane; HSDB 3175; Dextropropoxyphene; EINECS 207-420-5; Femadol; 2-Butanol, 4-(dimethylamino)-3-methyl-1,2-diphenyl-, propionate, (+)-; Algafan.
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Name: | Dextropropoxyphene |
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Name (isomeric): | DB00647 |
Drug Type: | small molecule |
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. |
Synonyms: |
Dextropropoxyphene; Propoxyphene HCl; D-Propoxyphene; Dextropropoxyphene-M; Dextroproxifeno
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Brand: | Kesso-Gesic, Darvon-N, Dolene, Darvon, Antalvic, Doloxen, Doloxene, Proxagesic, Propoxychel, Prophene 65, Dolocap, Propacet, Algafan, Erantin, Deprancol, Propoxyphene HCl 65, Femadol, Depromic, Harmar |
Category: | Narcotics, Analgesics, Antitussives, Analgesics, Opioid |
CAS number: | 469-62-5 |
Indication: | For the relief of mild to moderate pain |
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Pharmacology: |
Propoxyphene, a synthetic opiate agonist, is structurally similar to methadone. Its general pharmacologic properties are those of the opiates as a group. 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. Propoxyphene possesses ...
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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 op...
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Biotransformation: | Hepatic |
Route of elimination: | The major route of metabolism is cytochrome CYP3A4 mediated N-demethylation to norpropoxyphene, which is excreted by the kidneys. In 48 hours, approximately 20% to 25% of the administered dose of propoxyphene is excreted via the urine, most of which is free or conjugated norpropoxyphene. |
Half Life: | 6-12 hours |
Clearance: | 2.6 L/min |
Toxicity: | Coma, respiratory depression, circulatory collapse, and pulmonary edema. Seizures occur more frequently in patients with propoxyphene intoxication than in those with opiate intoxication. LD50=230mg/kg (orally in rat, Emerson) |
Affected organisms: | Humans and other mammals |
Food interaction: |
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