Contents

Search

oxycodone (Roxicodone, OxyContin, OxyIR, OxyFast, Oxecta, Xtampza ER)

Tradenames: Roxicodone, OxyContin (controlled release), OxyIR (immediate release). DEA-controlled substance: class 2. Indications: - moderate to severe acute pain-related syndromes - neuropathic pain - effective for treatment of osteoarthritis [12] Dosage: 1) 5-10 mg PO every 4-6 hours 2) no maximum dose 3) may be given every 1-2 hours for breakthrough pain 4) children: a) 6-12 years: 1.25 mg every 6 hours PRN b) > 12 years: 2.5 mg every 6 hours PRN Tabs: 5 mg. (OxyIR) Oxycontin. Tabs 10, 20, 40 & 80* mg OxyIR: 20 mg/mL (OxyFast) Syrup 5 mg/5 mL. Oxecta: immediate-release; resistant to abuse [10] * 80 mg tab to be used in opioid tolerant patients only for doses >= 160 mg * reformulated OxyContin is intended to prevent the tab from being cut, broken, chewed, crushed or dissolved to render fast-acting oxycodone [8] Pharmacokinetics: 1) well absorbed orally 2) onset of action 10-15 minutes 3) duration 4-6 hours; OxyContin is 12 hours - duration may be increased in the elderly [6] - Oxycontin fails to deliver 12 hours of pain relief in 85% of patients; withdrawal symptoms occur prior to 12 hours [11] 4) t1/2 of 3.2 hours (immediate release), 4.5 hours (sustained release) 4) metabolized by liver by cyt P450 2D6, excreted by kidney Adverse effects: 1) common (> 10%) - weakness, fatigue, nausea/vomiting, hypotension, drowsiness, dizziness 2) less common (1-10%) - ureteral spasms, pain at site of injection, nervousness, headache, restlessness, anorexia, malaise, epigastric cramps, dry mouth, constipation, biliary spasm, decreased urination, confusion, dyspnea* 3) uncommon (< 1%) - paralytic ileus, depression, histamine release, hallucinations, paradoxical CNS stimulation, rash, urticaria, increased intracranial pressure, physical & psychologic dependence * respiratory depression is dose & tolerance-related * refrain from driving or activities requiring heightened attention for 1 week after increasing oxyxocodone dose [14] Drug interactions: 1) alcohol, benzodiazepines, barbiturates in combination increase CNS side effects 2) naloxone is a direct opiate receptor antagonist 3) any pharmaceutical agent that inhibits cyt P450 2D6 or cyt P450 3A4 can increase oxycodone levels - initiating oxycodone in patients taking paroxetine or fluoxetine associated with increased risk of opioid overdose (RR=1.23) - effect attributed to CYP2D6 inhibition by paroxetine or fluoxetine [15] 4) new black box warning Laboratory: 1) specimen: a) serum, plasma b) stable for 6 months at -20 degrees C 2) methods: GLC, GC-MS, RIA, EIA, HPLC 3) high threshold (10 ug/mL) in urine opiate screen 4) rapidone oxycodone (VAMC) dipstick test detects 100 ng/mL in urine [7] 5) labs with Loincs - oxycodone in specimen - oxycodone in hair - oxycodone in gastric fluid - oxycodone in meconium - oxycodone free in stool - oxycodone in saliva - oxycodone in serum/plasma/blood - oxycodone in blood - oxycodone in serum/plasma - oxycodone in urine Mechanism of action: 1) alters perception of pain at the level of the spinal cord & higher levels of the CNS 2) alters emotional response to pain Notes: Abuse: [5] 1) tabs crushed for snorting or boiled for injection 2) these remove sustained-release coating 3) gives rush of euphoria similar to heroin Purdue Pharma & Abbott Laboratories pharmaceuticals aggressively marketed Oxycontin to make it a blockbuster drug [13]

Interactions

drug interactions drug adverse effects (more general classes)

Related

ibuprofen/oxycodone (Combunox) noroxycodone

General

opiate opioid receptor agonist (narcotic)

Properties

MISC-INFO: elimination route LIVER 1/2life 4-5 HOURS therapeutic-range 10-100 NG/ML toxic-range >200 NG/ML pregnancy-category B C D 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. Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
  3. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  4. Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
  5. Prescriber's Letter 8(2):11 2001
  6. Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
  7. Veterans Administration Medical Center (VAMC) Greater Los Angeles, clinical laboratory December, 2009
  8. FDA NEWS RELEASE Apr. 5, 2010 FDA Approves New Formulation for OxyContin
  9. Prescriber's Letter 17(6): 2010 Cytochrome P450 Drug Interactions Detail-Document#: 260623 (subscription needed) http://www.prescribersletter.com
  10. Prescriber's Letter 17(12): 2010 COMMENTARY: New OxyContin (Oxycodone Controlled-Release) Formulation Detail-Document#: 261201 (subscription needed) http://www.prescribersletter.com - Prescriber's Letter 18(10): 2011 COMMENTARY: New Formulation: Oxecta (Oxycodone) CHART: Fentanyl Products for Breakthrough Pain CHART: Drugs with REMS and Other Special Prescribing/ Dispensing Requirements Detail-Document#: 271021 (subscription needed) http://www.prescribersletter.com
  11. Young K. Sadoughi S, Sofair A OxyContin Fails to Deliver 12 Hours of Pain Relief in Many. Physician's First Watch, May 9, 2016 David G. Fairchild, MD, MPH, Editor-in-Chief Massachusetts Medical Society http://www.jwatch.org - Ryan H, Girion L, Glover S 'You want a description of hell?' OxyContin's 12-hour problem. Los Angeles Times. May 5, 2016 http://static.latimes.com/oxycontin-part1/#nt=oft07a-2gp1
  12. Geriatric Review Syllabus, 9th edition (GRS9) Medinal-Walpole A, Pacala JT, Porter JF (eds) American Geriatrics Society, 2016
  13. Armstrong D Secret trove reveals bold 'crusade' to make OxyContin a blockbuster. STAT. Sept 22,2016 https://www.statnews.com/2016/09/22/abbott-oxycontin-crusade/
  14. NEJM Knowledge+ Internal Medicine Board Review https://myknowledgeplus.nejm.org/flow/flowjs.html
  15. Yunusa I, Gagne JJ, Yoshida K et al Risk of Opioid Overdose Associated With Concomitant Use of Oxycodone and Selective Serotonin Reuptake Inhibitors. JAMA Netw Open. 2022;5(2):e220194 PMID: 3520131 https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2789401
  16. Oxycontin. HIGHLIGHTS OF PRESCRIBING INFORMATION. http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022272s027lbl.pdf

Component-of

acetaminophen/oxycodone (Percocet, Endocet, Tylox, Roxicet) aspirin/oxycodone (Percodan) benzenesulfonic acid/h2o2/lactic acid/oxycodone h2o2/lactic acid/oxycodone ibuprofen/oxycodone (Combunox) naloxone/oxycodone (Targiniq ER)