Drug intelligence / Profile preview

dextropropoxyphene

Development stage
Approved
Lead developer
Eli Lilly
Modality
Small Molecules
Administration
Oral
01

Overview

Dextropropoxyphene is a synthetic opioid analgesic used for the symptomatic treatment of mild to moderate pain. It is an optical isomer of levopropoxyphene, with only the dextro-isomer exhibiting significant analgesic activity. Dextropropoxyphene acts primarily as a mu-opioid receptor agonist in the central nervous system, inhibiting adenylate cyclase and decreasing intracellular cAMP levels. This leads to reduced release of nociceptive neurotransmitters and hyperpolarization of neurons, resulting in decreased pain transmission. Additionally, it acts as a potent noncompetitive antagonist at α3β4 neuronal nicotinic acetylcholine receptors and has weak serotonin reuptake inhibitory effects. The drug also displays antitussive and local anesthetic actions. Due to risks such as cardiac arrhythmias and fatal overdose—especially when combined with other depressants or alcohol—dextropropoxyphene has been withdrawn from markets in Europe and the United States[1][2][3][8].

Brand names
DarvonDarvocet-NDarvon-NPP-Cap
Other names
propoxyphene (refers to the general form, but only the dextro-isomer is analgesic)(+)-alpha-propoxyphene
02

Targets

MOR (Mu opioid receptor)

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