Company InfoNewsInvestor InformationResearchDevelopmentCareersBusiness DevelopmentResourcesDrugs databaseBack to the home pageSearch  
Drugs database
Drugs A-Z

Brands A-Z

Drugs by categories

Drugs by manufacturer

Drugs by packager

Antibiotics for sale

Online Viagra bestellen in Nederland

Home / Drugs / Starting with P / Propoxyphene

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]
Prophene 65
Propoxyphene HCl 65
Analgesics, Opioid
ManufacturersXanodyne pharmaceutics inc
Heritage pharmaceuticals inc
Mk laboratories inc
Halsey drug co inc
Alra laboratories inc
Impax laboratories inc
Ivax pharmaceuticals inc sub teva pharmaceuticals usa
Mutual pharmaceutical co inc
Mylan pharmaceuticals inc
Nexgen pharma inc
Par pharmaceutical inc
Purepac pharmaceutical co
Private formulations inc
Roxane laboratories inc
Sandoz inc
Teva pharmaceuticals usa inc
Valeant pharmaceuticals international
Vintage pharmaceuticals inc
Watson laboratories inc
West ward pharmaceutical corp
Whiteworth towne paulsen inc
Warner chilcott div warner lambert co
Aaipharma llc
PackagersAAIPharma Inc.
Aidarex Pharmacuticals LLC
Altura Pharmaceuticals Inc.
Amerisource Health Services Corp.
Apotheca Inc.
Aristos Pharmaceuticals
A-S Medication Solutions LLC
Blenheim Pharmacal
Bryant Ranch Prepack
Cardinal Health
Caremark LLC
Comprehensive Consultant Services Inc.
Corepharma LLC
Cornerstone Pharmacy
D.M. Graham Laboratories Inc.
Direct Dispensing Inc.
Dispensing Solutions
Diversified Healthcare Services Inc.
DSM Corp.
Golden State Medical Supply Inc.
H and H Laboratories
H.J. Harkins Co. Inc.
Heartland Repack Services LLC
Innoviant Pharmacy Inc.
Ivax Pharmaceuticals
Kaiser Foundation Hospital
Keltman Pharmaceuticals Inc.
Lake Erie Medical and Surgical Supply
Liberty Pharmaceuticals
Lilly Del Caribe Inc.
Major Pharmaceuticals
Mallinckrodt Inc.
Mckesson Corp.
Medvantx Inc.
Mikart Inc.
Murfreesboro Pharmaceutical Nursing Supply
Nexgen Pharma Inc.
Nucare Pharmaceuticals Inc.
Palmetto Pharmaceuticals Inc.
Par Pharmaceuticals
PD-Rx Pharmaceuticals Inc.
Physicians Total Care Inc.
Pliva Inc.
Preferred Pharmaceuticals Inc.
Prepackage Specialists
Prepak Systems Inc.
Ranbaxy Laboratories
Rebel Distributors Corp.
Redpharm Drug
Remedy Repack
Resource Optimization and Innovation LLC
Sandhills Packaging Inc.
Smartscience Laboratories Inc.
Southwood Pharmaceuticals
St Mary's Medical Park Pharmacy
Stat Rx Usa
Talbert Medical Management Corp.
Teva Pharmaceutical Industries Ltd.
UDL Laboratories
Va Cmop Dallas
Veratex Corp.
Vintage Pharmaceuticals Inc.
Watson Pharmaceuticals
West-Ward Pharmaceuticals
Wockhardt Ltd.
Xanodyne Pharmaceuticals Inc.
Propoxyphene HCl


For the relief of mild to moderate pain


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 little to no antitussive activity and no antipyretic action.

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.


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)



half life

6-12 hours

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.

drug interactions

Acenocoumarol: Propoxyphene may increase the anticoagulant effect of acenocoumarol.

Anisindione: Propoxyphene may increase the anticoagulant effect of anisindione.

Atomoxetine: The CYP2D6 inhibitor could increase the effect and toxicity of atomoxetine

Carbamazepine: Propoxyphene increases the effect of carbamazepine

Cimetidine: Cimetidine, a moderate CYP3A4 inhibitor, may decrease the metabolism of propoxyphene. Monitor for changes in the therapeutic and adverse effects of propoxyphene if cimetidine is intitiated, discontinued or dose changed.

Dicumarol: Propoxyphene may increase the anticoagulant effect of dicumarol.

Ritonavir: Ritonavir increases the levels of analgesic

Tranylcypromine: Increased risk of serotonin syndrome. Concomitant use should be avoided.

Triprolidine: The CNS depressants, Triprolidine and Propoxyphene, may increase adverse/toxic effects due to additivity. Monitor for increased CNS depressant effects during concomitant therapy.

Warfarin: Propoxyphene may increase the anticoagulant effect of warfarin.