Overview
| Generic Names: | D-Propoxyphene; Dextropropoxyphene; Dextropropoxyphene-M; Dextroproxifeno; Propoxyphene HCl |
|---|---|
| Trade Names: | Algafan; Antalvic; Darvon; Darvon-N; Deprancol; Depromic; Dolene; Dolocap; Doloxen; Doloxene; Erantin; Femadol; Harmar; Kesso-Gesic; Propacet; Prophene 65; Propoxychel; Propoxyphene HCl 65; Proxagesic |
| PharmGKB Accession Id: | PA451142 |
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 (source: Drug Bank)
Indication
For the relief of mild to moderate pain (source: Drug Bank)
ATC Therapeutic Category
- N02AC:Diphenylpropylamine derivatives
Pharmacology, Interactions, and Contraindications
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. (source: Drug Bank)
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. (source: Drug Bank)
Food Interactions
Take without regard to meals. Avoid alcohol. (source: Drug Bank)
Absorption, Distribution, Metabolism, Elimination & Toxicity
Biotransformation
Hepatic (source: Drug Bank)
Toxicity
Coma, respiratory depression, circulatory collapse, and pulmonary edema. Seizures occur more frequently in patients with propoxyphene intoxication than in those with opiate intoxication. LD<sub>50</sub>=230mg/kg (orally in rat, Emerson) (source: Drug Bank)
Isomeric SMILES Code:
CCC(=O)OC(Cc1ccccc1)(c2ccccc2)C(C)CN(C)C (source: Drug Bank)
The following genes are in curated knowledge about this drug.
| Gene | Relationship | Evidence | |
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CYP2D6 |
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Publications |
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CYP3A |
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Publications |
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CYP3A4 |
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Publications |
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CYP3A5 |
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Publications |
A list of non-curated publications that mention this drug along with other genes is available.
Drug Targets
| Gene | Description | |
|---|---|---|
| OPRD1 |
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(source: Drug Bank) |
| OPRK1 |
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(source: Drug Bank) |
| OPRM1 |
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(source: Drug Bank) |
The following drugs are in curated knowledge about this drug.
| Drug | Relationship | Evidence | |
|---|---|---|---|
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warfarin |
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Publications |
A list of non-curated publications that mention this drug along with other drugs is available.
Drug Interactions
| Drug | Description | |
|---|---|---|
| acenocoumarol |
|
Propoxyphene increases the anticoagulant effect (source: Drug Bank) |
| atomoxetine |
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The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine (source: Drug Bank) |
| carbamazepine |
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Propoxyphene increases the effect of carbamazepine (source: Drug Bank) |
| cimetidine |
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Cimetidine increases the effect of the narcotic (source: Drug Bank) |
| dicumarol |
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Propoxyphene increases the anticoagulant effect (source: Drug Bank) |
| naltrexone |
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Naltrexone may precipitate a withdrawal syndrome in opioid-dependent individuals (source: Drug Bank) |
| ritonavir |
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Ritonavir increases the levels of analgesic (source: Drug Bank) |
| warfarin |
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Propoxyphene increases the anticoagulant effect (source: Drug Bank) |
Curated Information
The following diseases are in curated knowledge about this drug.
| Disease | Relationship | Evidence | |
|---|---|---|---|
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Bradycardia |
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Publications |
Non-Curated Information
A list of non-curated publications that mention this drug along with other diseases is available.
LinkOuts
Common Searches
Search PubMed
Search Medline Plus
Search PubChem
Search CTD
Non-Curated Publications
A list of non-curated publications that mention this drug is available.
