Drug intelligence / Profile preview

propoxyphene

Development stage
Discontinued
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral, Intravenous, Rectal
01

Overview

Propoxyphene is a synthetic opioid analgesic that was historically used for the relief of mild to moderate pain. It was first approved by the FDA in 1957. The drug's primary mechanism of action involves acting as a weak agonist at opioid receptors in the central nervous system, particularly the OP3 receptor, to reduce the perception of pain. It also exhibits local anesthetic effects through the inhibition of sodium channels. Propoxyphene was withdrawn from the U.S. market in 2010 and the European Union in 2009 due to concerns over serious and potentially fatal cardiac rhythm abnormalities, even at therapeutic doses. It is classified as a Schedule IV narcotic due to its potential for abuse and dependence.

Brand names
DarvonDarvon-NDoleneDarvocetCapadexDi-GesicParadexLentogesicDi-AntalvicBalacet
Other names
dextropropoxypheneD-propoxypheneDextropropoxyphene-MDextroproxifenopropoxyphene HClpropoxyphene napsylateAlpha-d-4-dimethylamino-3-methyl-1,2-diphenyl-2-butanol propionate[(2S,3R)-4-(Dimethylamino)-3- methyl-1,2-diphenylbutan-2-yl] propanoate(+)-1,2-Diphenyl-2-propionoxy- 3-methyl-4-di-methylaminobutaneDesoxypropiophen
02

Targets

MOR (Mu opioid receptor)KOR (Kappa opioid receptor)DOR (Opioid Receptor Delta 1)

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