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propoxyphene (Darvon, Dolene, Proxagesic, Novopropoxyn)

(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 [5] Withdrawn from US market Nov 2010.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: 1) extensive 1st pass metabolism in liver 2) N-demethylation to active metabolite norpropoxyphene (t1/2 of 18-29 hours) Adverse effects: 1) CNS depressant 2) potential for abuse 3) nephrogenic diabetes insipidus 4) acute overdose a) respiratory depression b) pulmonary edema c) convulsions d) coma 5) accumulation of norpropoxyphene [4] a) pulmonary edema b) apnea c) cardiac arrest 6) toxicity not easily reversed with naloxone 7) arrhythmogenic effects a) prolonged PR interval b) widened QRS complex c) prolonged QT interval [9] Drug interactions: -> smoking may increase hepatic metabolism Laboratory: 1) specimen: serum, urine (drug screen) 2) methods: GLC, EIA, HPLC 3) labs with Loincs - propoxyphene in specimen - propoxyphene in hair - propoxyphene in gastric fluid - propoxyphene in saliva - propoxyphene in blood - propoxyphene in serum/plasma - propoxyphene in stool - propoxyphene in meconium - propoxyphene in urine - propoxyphene in vitreous fluid Mechanism of action: 1) D-isomer binds primarily to mu opioid receptors 2) L-isomer is an antitussive agent

Interactions

drug interactions drug adverse effects (more general classes)

General

amine ester opiate opioid receptor agonist (narcotic)

Properties

MISC-INFO: 1/2life 8-24 HOURS 18-29 HOURS therapeutic-range 0.1-0.4 UG/ML toxic-range >5 UG/ML protein-binding 76% elimination by hemodialysis - peritoneal dialysis - pregnancy-category C safety in lactation ?

Database Correlations

PUBCHEM correlations

References

  1. The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
  2. The Pharmacological Basis of Therapeutics, 8th ed. Gilman et al, eds. Permagon Press/McGraw Hill
  3. Clinical Guide to Laboratory Tests, NW Tietz (ed) 3rd ed, WB Saunders, Philadelpha 1995
  4. Geriatrics Review Syllabus, American Geriatrics Society, 5th edition, 2002-2004
  5. 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
  6. Darvon Label http://www.xanodyne.com/pdf/Darvon.pdf
  7. Prescriber's Letter 16(3): 2009 Propoxyphene: Safety and Efficacy Detail-Document#: 250301 (subscription needed) http://www.prescribersletter.com
  8. Propoxyphene-containing Products FDA MedWatch http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm170763.htm
  9. FDA MmedWatch, 11/19/2010 Propoxyphene: Withdrawal - Risk of Cardiac Toxicity http://www.fda.gov/Safety/MedWatch/SafetyInformation/SafetyAlertsforHumanMedicalProducts/ucm234389.htm
  10. Prescriber's Letter 17(12): 2010 COMMENTARY: Propoxyphene Withdrawal from the Market Detail-Document#: 261228 (subscription needed) http://www.prescribersletter.com

Component-of

acetaminophen/propoxyphene (Darvocet, Wygesic) aspirin/caffeine/propoxyphene (Darvon Compound)