Darvon-N: profile and news

Public Citizen Petitions FDA to Ban Darvon Products Feb 28, 2006
488 subjects (17.7%) indicated that they had used Darvon or Darvon-N in their lifetimes, making propoxyphene the most frequently mentioned opiate drug. ... - PharmaLive.com (press release),

Accidental overdose caused teen's death Apr 3, 2005
Propoxyphene is available by prescription only, either in its generic form or under brand names that include Darvon-N and Darvon Puvules, according to Medline ... - Pittsburgh Tribune-Review,

Other information

Indication
For pain relief

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.

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.

Drug Category
Narcotics; Antitussives; Analgesics; ATC:N02AC04; ATC:N02AC54; ATC:N02AC74

Brand Names/Synonyms
Algafan; Antalvic; D-Propoxyphene; Darvocet; Darvon; Darvon-N; Deprancol; Depromic; Dextropropoxyphene; Dextropropoxyphene-M; Dextroproxifeno; Dolene; Dolocap; Doloxen; Doloxene; Erantin; Femadol; Harmar; Kesso-Gesic; Propacet; Prophene 65; Propoxychel; Propoxyphene; Propoxyphene Hcl; Propoxyphene Hcl 65; Proxagesic; SK 65

Dosage Forms
Tablets

Absorption
Not Available

Interactions
Interactions for Propoxyphene:

The CNS-depressant effect of propoxyphene is additive with that of other CNS depressants, including alcohol.

As is the case with many medicinal agents, propoxyphene may slow the metabolism of a concomitantly administered drug. Should this occur, the higher serum concentrations of that drug may result in increased pharmacologic or adverse effects of that drug. Such occurrences have been reported when propoxyphene was administered to patients on antidepressants, anticonvulsants, or warfarin-like drugs. Sever neurologic signs, including coma, have occurred with concurrent use of carbamazepine.

Chemical IUPAC Name
(4-dimethylamino-3-methyl-1,2-diphenyl-butan-2-yl) propanoate

Chemical Formula
C22H29NO2

Half Life
6-12 hours

Drug Type
Approved Drug

# Accession No
APRD00548

CAS Registry Number
469-62-5