Drug intelligence / Profile preview

acetaminophen + propoxyphene napsylate

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

Overview

Acetaminophen + propoxyphene napsylate is an oral combination analgesic drug comprised of acetaminophen, a non-opioid analgesic and antipyretic, and propoxyphene napsylate, a mild opioid (narcotic) analgesic structurally related to methadone. Propoxyphene napsylate is the napsylate salt of dextropropoxyphene, introduced for oral dosage stability and lower water solubility. **Mechanism of action:** - Acetaminophen acts as an analgesic and antipyretic, exerting its antipyretic effect by inhibiting prostaglandin synthesis in the hypothalamic heat-regulating center. - Propoxyphene (dextropropoxyphene) is a centrally-acting opioid receptor agonist providing mild analgesic activity, with additional local anesthetic and antiarrhythmic (sodium channel-blocking) effects at higher doses or with metabolite (norpropoxyphene) accumulation. The combination provides greater analgesia than either agent alone. The product has been discontinued or withdrawn in the US and many other markets due to safety concerns, primarily cardiac toxicity and risk of fatal overdose[4][5][1][2].

Brand names
Darvocet-NDarvocet-N50Darvocet-N-50Darvocet-N 50Darvocet-N100Darvocet-N-100Darvocet-N 100Darvon with APAPDi-GesicCapadexDistalgesic
Other names
propoxyphene napsylate and acetaminophenco-proxamoldextropropoxyphene napsylate + acetaminophenparacetamol + dextropropoxyphene napsylate
02

Targets

MOR (Mu opioid receptor)PGHS-1 (Prostaglandin G/H Synthase 1)KOR (Kappa opioid receptor)

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