|
|
|
|
|
Propoxyphene
drug data and news
Propoxyphene 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 | Propoxyphene | ||
| Brand Names/Synonyms | Algafan; Antalvic; D-Propoxyphene; Darvocet; Darvon; Darvon-N; Deprancol; Depromic; Dextropropoxyphene; Dextropropoxyphene-M; Dextroproxifeno; Dolene; Dolocap; Doloxen; Doloxene; Erantin; Femadol; Harmar; Kesso-Gesic; Propacet; Prophene 65; Propoxychel; Propoxyphene; Propoxyphene Hcl; Propoxyphene Hcl 65; Proxagesic; SK 65 | ||
| Indication | For pain relief | ||
| Sponsored links | Description | Not Available | |
| 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. | ||
| Propoxyphene News (When available) |
WayPoint Biomedical Launches New Range of Clinical Drugs of Abuse ... 16 May 2006 Don’t ask, might not think to tell: Communication key to ... 16 May 2006 Baker sentenced to six years May 13, 2006 7.5 crore drug addicts in India: Survey May 3, 2006 Two face drug charges Apr 18, 2006 | ||
| Dosage Forms | Tablets | ||
| Drug_Category | Narcotics; Antitussives; Analgesics; ATC:N02AC04; ATC:N02AC54; ATC:N02AC74 | ||
| Absorption | Not Available | ||
| Interactions |
Interactions for Propoxyphene: The CNS-depressant effect of propoxyphene is additive with that of other CNS depressants, including alcohol. As is the case with many medicinal agents, propoxyphene may slow the metabolism of a concomitantly administered drug. Should this occur, the higher serum concentrations of that drug may result in increased pharmacologic or adverse effects of that drug. Such occurrences have been reported when propoxyphene was administered to patients on antidepressants, anticonvulsants, or warfarin-like drugs. Sever neurologic signs, including coma, have occurred with concurrent use of carbamazepine. | ||
| 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) | ||
| Organisms Affected | Humans and other mammals | ||
| Chemical IUPAC Name | (4-dimethylamino-3-methyl-1,2-diphenyl-butan-2-yl) propanoate | ||
| Chemical Formula | C22H29NO2 | ||
| Molecular Weight | 339.471 g/mol | ||
| Smiles String | CCC(=O)OC(CC1=CC=CC=C1)(C2=CC=CC=C2)C(C)CN(C)C | ||
| Melting Point | 75-76°C | ||
| Water Solubility | 19.6mg/L | ||
| State | odorless, white crystalline powder with a bitter taste | ||
| LogP/Hphobicity | 4.901 | ||
| Isoelectric Point | Not Available | ||
| Biotransformation | Hepatic | ||
| Half Life | 6-12 hours | ||
| Protein Binding [%] | Not Available | ||
| RxList Link | RXlist | ||
| Sponsored links | |||
| Drug Reference |
http://www.drugs.com/cons/Propoxyphene.html http://www.rxlist.com/cgi/generic/propox.htm | ||
| Drug Type | Approved Drug | ||
| Accession No | APRD00548 | ||
| CAS Registry Number | 469-62-5 | ||
| KEGG Compound ID | C07406 | ||
| PubChem ID | SID:270993 | ||
| PharmGKB ID | PA451142 | ||
| SwissProt ID | Not Available | ||
| GenBank ID | Not Available | ||
| Drug ID Number [DIN] | Not Available |
|
Home | About | Cancers | Treatment | Medications Copyright onconews.org 2005. All Rights Reserved. |