oxycodone (Roxicodone, OxyContin, OxyIR, OxyFast, Oxecta, Xtampza ER)
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Introduction
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
- 5-10 mg PO every 4-6 hours
- no maximum dose
- may be given every 1-2 hours for breakthrough pain
- children:
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
- well absorbed orally
- onset of action 10-15 minutes
- 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]
- t1/2 of 3.2 hours (immediate release), 4.5 hours (sustained release)
- metabolized by liver by cyt P450 2D6, excreted by kidney
elimination via liver
1/2life = 4-5 hours
Adverse effects
- common (> 10%)
- 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*
- 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 adverse effects of opiates
- drug adverse effects of psychotropic agents
- drug adverse effects of sedatives
Drug interactions
- alcohol, benzodiazepines, barbiturates in combination increase CNS side effects
- naloxone is a direct opiate receptor antagonist
- 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]
- initiating oxycodone in patients taking paroxetine or fluoxetine associated with increased risk of opioid overdose (RR=1.23)
- new black box warning
- 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
- specimen:
- methods: GLC, GC-MS, RIA, EIA, HPLC
- high threshold (10 ug/mL) in urine opiate screen
- rapidone oxycodone (VAMC) dipstick test detects 100 ng/mL in urine[7]
- labs with Loincs
Mechanism of action
- alters perception of pain at the level of the spinal cord & higher levels of the CNS
- alters emotional response to pain
Notes
Abuse:[5]
- tabs crushed for snorting or boiled for injection
- these remove sustained-release coating
- gives rush of euphoria similar to heroin
Purdue Pharma & Abbott Laboratories pharmaceuticals aggressively marketed Oxycontin to make it a blockbuster drug[13]
More general terms
Additional terms
Component of
- naloxone/oxycodone (Targiniq ER)
- h2o2/lactic acid/oxycodone
- benzenesulfonic acid/h2o2/lactic acid/oxycodone
- acetaminophen/hydrocodone (Anexsia, Lorcet, Lortab, Vicodin, Norco)
- aspirin/oxycodone (Percodan)
- acetaminophen/oxycodone (Percocet, Endocet, Tylox, Roxicet)
- ibuprofen/oxycodone (Combunox)
References
- ↑ The Pharmacological Basis of Therapeutics, 9th ed. Gilman et al, eds. Permagon Press/McGraw Hill, 1996
- ↑ Drug Information & Medication Formulary, Veterans Affairs, Central California Health Care System, 1st ed., Ravnan et al eds, 1998
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Clinical Guide to Laboratory Tests, 3rd ed. Teitz ed., W.B. Saunders, 1995
- ↑ 5.0 5.1 Prescriber's Letter 8(2):11 2001
- ↑ 6.0 6.1 Geriatric Dosage Handbook, 6th edition, Selma et al eds, Lexi-Comp, Cleveland, 2001
- ↑ 7.0 7.1 Veterans Administration Medical Center (VAMC) Greater Los Angeles, clinical laboratory December, 2009
- ↑ 8.0 8.1 FDA NEWS RELEASE Apr. 5, 2010 FDA Approves New Formulation for OxyContin
- ↑ Prescriber's Letter 17(6): 2010 Cytochrome P450 Drug Interactions Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260623&pb=PRL (subscription needed) http://www.prescribersletter.com
- ↑ 10.0 10.1 Prescriber's Letter 17(12): 2010 COMMENTARY: New OxyContin (Oxycodone Controlled-Release) Formulation Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=261201&pb=PRL (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#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=271021&pb=PRL (subscription needed) http://www.prescribersletter.com - ↑ 11.0 11.1 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 - ↑ 12.0 12.1 Geriatric Review Syllabus, 9th edition (GRS9) Medinal-Walpole A, Pacala JT, Porter JF (eds) American Geriatrics Society, 2016
- ↑ 13.0 13.1 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/
- ↑ 14.0 14.1 NEJM Knowledge+ Internal Medicine Board Review https://myknowledgeplus.nejm.org/flow/flowjs.html
- ↑ 15.0 15.1 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: https://www.ncbi.nlm.nih.gov/pubmed/3520131 https://jamanetwork.com/journals/jamanetworkopen/fullarticle/2789401
- ↑ Oxycontin. HIGHLIGHTS OF PRESCRIBING INFORMATION. http://www.accessdata.fda.gov/drugsatfda_docs/label/2015/022272s027lbl.pdf