propoxyphene (Darvon, Dolene, Proxagesic, Novopropoxyn)
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Introduction
(propoxyphene hydrochloride) Tradenames: Darvon, Dolene. DEA-controlled substance: class 4. Banned by FDA Feb 2009.[5] Withdrawn from US market Nov 2010.[9]
Indications
- relief of mild to moderate pain*
* Not appropriate for severe pain Never shown to be superior to aspirin or acetaminophen
Dosage
65 mg PO every 4 hours
Tabs: 32 & 65 mg.
100 mg of propoxyphene is equal in analgesia to 60 mg of codeine or 650 mg of aspirin
Pharmacokinetics
- extensive 1st pass metabolism in liver
- N-demethylation to active metabolite norpropoxyphene (t1/2 of 18-29 hours)
1/2life = 8-24 hours
1/2life = 18-29 hours norpropoxyphene
protein binding = 76 %
elimination by hemodialysis = -
elimination by peritoneal dialysis = -
Adverse effects
- CNS depressant
- potential for abuse
- nephrogenic diabetes insipidus
- acute overdose
- accumulation of norpropoxyphene[4]
- toxicity not easily reversed with naloxone
- arrhythmogenic effects
- drug adverse effects of opiates
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- smoking may increase hepatic metabolism
- drug interaction(s) of benzodiazepine with opiates
- drug interaction(s) of antidepressant with opiates
- drug interaction(s) of Z-drugs with opiates
- drug interaction(s) of alcoholic beverage with opiates
- drug interaction(s) of pregabalin with opiates
- drug interaction(s) of gabapentin with opiates
Laboratory
Mechanism of action
- D-isomer binds primarily to mu opioid receptors
- L-isomer is an antitussive agent
More general terms
Component of
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill
- ↑ Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
- ↑ 4.0 4.1 Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004
- ↑ 5.0 5.1 FDA panel recommends ban on the painkiller Darvon http://www.google.com/hostednews/ap/article/ALeqM5iimSGh-TXwePdZHMMlPq4MBSdKGgD961N61O0
FDA holds safety hearing on 50-year-old painkiller http://www.google.com/hostednews/ap/article/ALeqM5iimSGh-TXwePdZHMMlPq4MBSdKGgD961J3U00 - ↑ Darvon Label http://www.xanodyne.com/pdf/Darvon.pdf
- ↑ Prescriber's Letter 16(3): 2009 Propoxyphene: Safety and Efficacy Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=250301&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ Propoxyphene-containing Products FDA MedWatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm170763.htm
- ↑ 9.0 9.1 9.2 FDA MmedWatch, 11/19/2010 Propoxyphene: Withdrawal - Risk of Cardiac Toxicity http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm234389.htm
- ↑ Prescriber's Letter 17(12): 2010 COMMENTARY: Propoxyphene Withdrawal from the Market Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=261228&pb=PRL (subscription needed) http://www.prescribersletter.com
Patient information
propoxyphene patient information