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ALERT: U.S. Boxed Warning
The FDA-approved labeling includes a boxed warning. See Warnings/Precautions section for a concise summary of this information. For verbatim wording of the boxed warning, consult the product labeling or www.fda.gov.
Medication Safety Issues
Sound-alike/look-alike issues:
OxyCODONE may be confused with HYDROcodone, OxyContin®, oxymorphone
OxyContin® may be confused with MS Contin®, oxybutynin, oxycodone
OxyFast® may be confused with Roxanol™
Roxicodone® may be confused with Roxanol™
High alert medication: The Institute for Safe Medication Practices (ISMP) includes this medication among its list of drug classes which have a heightened risk of causing significant patient harm when used in error.
Pronunciation
(oks i KOE done)
U.S. Brand Names
Index Terms
Generic Available
Yes
Canadian Brand Names
Pharmacologic Category
Pharmacologic Category Synonyms
Use: Labeled Indications
Management of moderate-to-severe pain, normally used in combination with nonopioid analgesics
OxyContin® is indicated for around-the-clock management of moderate-to-severe pain when an analgesic is needed for an extended period of time.
Use: Dental
Treatment of postoperative pain
Restrictions
C-II
Pregnancy Risk Factor
B/D (prolonged use or high doses at term)
Pregnancy Considerations
Should be used in pregnancy only if clearly needed. Use of narcotics during pregnancy may produce physical dependence in the neonate; respiratory depression may occur in the newborn if narcotics are used prior to delivery (especially high doses).
Lactation
Enters breast milk/use caution
Contraindications
Hypersensitivity to oxycodone or any component of the formulation; significant respiratory depression; hypercarbia; acute or severe bronchial asthma; OxyContin® is also contraindicated in paralytic ileus (known or suspected); pregnancy (prolonged use or high doses at term)
Warnings/Precautions
Boxed warnings:
• Abuse/misuse/diversion: See “Other warnings/precautions” below.
• Controlled-release tablets: See “Dosage form specific issues” below.
Concerns related to adverse effects:
• CNS depression: May cause CNS depression, which may impair physical or mental abilities; patients must be cautioned about performing tasks which require mental alertness (eg, operating machinery or driving).
• Hypotension: May cause hypotension; use with caution in patients with hypovolemia, cardiovascular disease (including acute MI), or drugs which may exaggerate hypotensive effects (including phenothiazines or general anesthetics).
• Phenanthrene hypersensitivity: Use with caution in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (codeine, hydrocodone, hydromorphone, levorphanol, oxymorphone).
Disease-related concerns:
• Abdominal conditions: May obscure diagnosis or clinical course of patients with acute abdominal conditions.
• Adrenocortical insufficiency: Use with caution in patients with adrenocortical insufficiency, including Addison's disease.
• Biliary tract impairment: Use with caution in patients with biliary tract dysfunction; acute pancreatitis may cause constriction of sphincter of Oddi.
• CNS depression/coma: Use with caution in patients with CNS depression or coma.
• Drug abuse: Use with caution in patients with a history of drug abuse or acute alcoholism; potential for drug dependency exists. Tolerance, psychological and physical dependence may occur with prolonged use.
• Head trauma: Use with extreme caution in patients with head injury, intracranial lesions, or elevated intracranial pressure; exaggerated elevation of ICP may occur.
• Hepatic impairment: Use with caution in patients with severe hepatic dysfunction.
• Obesity: Use with caution in patients who are morbidly obese.
• Prostatic hyperplasia/urinary stricture: Use with caution in patients with prostatic hyperplasia and/or urinary stricture.
• Psychosis: Use with caution in patients with toxic psychosis.
• Renal impairment: Use with caution in patients with severe renal dysfunction.
• Respiratory disease: Use with caution in patients with pre-existing respiratory compromise (hypoxia and/or hypercapnia), COPD or other obstructive pulmonary disease, and kyphoscoliosis or other skeletal disorder which may alter respiratory function; critical respiratory depression may occur, even at therapeutic dosages.
• Seizures: Use with caution in patients with a history of seizure disorders.
• Thyroid dysfunction: Use with caution in patients with thyroid dysfunction.
Concurrent drug therapy issues:
• Sedatives: Effects may be potentiated when used with other sedative drugs or ethanol.
Special populations:
• Debilitated patients: Use with caution in debilitated patients; there is a greater potential for critical respiratory depression, even at therapeutic dosages.
• Elderly: Use with caution in the elderly; may be more sensitive to adverse effects. Decrease initial dose.
Dosage form specific issues:
• Controlled-release tablets: [U.S. Boxed Warning]: OxyContin® is not intended for use as an “as needed” analgesic or for immediately-postoperative pain management (should be used postoperatively only if the patient has received it prior to surgery or if severe, persistent pain is anticipated). [U.S. Boxed Warning]: Do NOT crush, break, or chew controlled-release tablets; 60 mg, 80 mg, and 160 mg strengths are for use only in opioid-tolerant patients.
• Latex sensitivity: Use the oral concentrate formulation with caution in patients with latex sensitivity; dropper dispenser contains dry, natural rubber.
Other warnings/precautions:
• Abuse/misuse/diversion: [U.S. Boxed Warning]: Healthcare provider should be alert to problems of abuse, misuse, and diversion.
• Withdrawal: Concurrent use of agonist/antagonist analgesics may precipitate withdrawal symptoms and/or reduced analgesic efficacy in patients following prolonged therapy with mu opioid agonists. Abrupt discontinuation following prolonged use may also lead to withdrawal symptoms.
Adverse Reactions
>10%:
Central nervous system: Somnolence (23% to 24%), dizziness (13% to 16%)
Dermatologic: Pruritus (12% to 13%)
Gastrointestinal: Nausea (23% to 27%), constipation (23% to 26%), vomiting (12% to 14%)
1% to 10%:
Cardiovascular: Postural hypotension (1% to 5%)
Central nervous system: Headache (7% to 8%), abnormal dreams (1% to 5%), anxiety (1% to 5%), chills (1% to 5%), confusion (1% to 5%), euphoria (1% to 5%), fever (1% to 5%), insomnia (1% to 5%), nervousness (1% to 5%), thought abnormalities (1% to 5%)
Dermatologic: Rash (1% to 5%)
Gastrointestinal: Xerostomia (6% to 7%), abdominal pain (1% to 5%), anorexia (1% to 5%), diarrhea (1% to 5%), dyspepsia (1% to 5%), gastritis (1% to 5%)
Neuromuscular & skeletal: Weakness (6% to 7%), twitching (1% to 5%)
Respiratory: Dyspnea (1% to 5%), hiccups (1% to 5%)
Miscellaneous: Diaphoresis (5% to 6%)
<1% (Limited to important or life-threatening): Agitation, amenorrhea, amnesia, anaphylaxis, anaphylactoid reaction, appetite increased, chest pain, cough, dehydration, depression, dysphagia, dysuria, edema, emotional lability, eructation, exfoliative dermatitis, facial edema, hallucinations, hematuria, histamine release, hyperkinesia, hypoesthesia, hyponatremia, hypotonia, ileus, impotence, intracranial pressure increased, libido decreased, malaise, migraine, paradoxical CNS stimulation, paralytic ileus, paresthesia, pharyngitis, physical dependence, polyuria, psychological dependence, seizure, SIADH, speech disorder, ST segment depression, stomatitis, stupor, syncope, tablet in stool (OxyCodone®), taste perversion, thirst, tinnitus, tremor, urinary retention, urticaria, vasodilation, vertigo, vision change, voice alteration, withdrawal syndrome
Metabolism/Transport Effects
Substrate (minor) of CYP2D6, 3A
Drug Interactions
Alcohol (Ethyl): CNS Depressants may enhance the CNS depressant effect of Alcohol (Ethyl). Risk C: Monitor therapy
Alvimopan: Analgesics (Opioid) may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Risk D: Consider therapy modification
Ammonium Chloride: May increase the excretion of Analgesics (Opioid). Risk C: Monitor therapy
Amphetamines: May enhance the analgesic effect of Analgesics (Opioid). Risk C: Monitor therapy
Antipsychotic Agents (Phenothiazines): May enhance the hypotensive effect of Analgesics (Opioid). Risk C: Monitor therapy
CNS Depressants: May enhance the adverse/toxic effect of other CNS Depressants. Risk C: Monitor therapy
Desmopressin: Analgesics (Opioid) may enhance the adverse/toxic effect of Desmopressin. Risk C: Monitor therapy
Pegvisomant: Analgesics (Opioid) may diminish the therapeutic effect of Pegvisomant. Risk C: Monitor therapy
Selective Serotonin Reuptake Inhibitors: Analgesics (Opioid) may enhance the serotonergic effect of Selective Serotonin Reuptake Inhibitors. This may cause serotonin syndrome. Risk C: Monitor therapy
Succinylcholine: May enhance the bradycardic effect of Analgesics (Opioid). Risk C: Monitor therapy
Thiazide Diuretics: Analgesics (Opioid) may enhance the orthostatic effect of Thiazide Diuretics. Risk C: Monitor therapy
Ethanol/Nutrition/Herb Interactions
Ethanol: Avoid ethanol (may increase CNS depression).
Food: When taken with a high-fat meal, peak concentration is 25% greater following a single OxyContin® 160 mg tablet as compared to two 80 mg tablets.
Herb/Nutraceutical: Avoid valerian, St John's wort, kava kava, gotu kola (may increase CNS depression).
Storage
Store at 15°C to 30°C (59°F to 86°F). Protect from light.
Mechanism of Action
Binds to opiate receptors in the CNS, causing inhibition of ascending pain pathways, altering the perception of and response to pain; produces generalized CNS depression
Pharmacodynamics/Kinetics
Onset of action: Pain relief: 10-15 minutes
Peak effect: 0.5-1 hour
Duration: Immediate release: 3-6 hours; Controlled release: ?12 hours
Distribution: Vd: 2.6 L/kg; distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, brain, and breast milk
Protein binding: ~45%
Metabolism: Hepatically via CYP3A4 to noroxycodone (has weak analgesic), noroxymorphone, and alpha- and beta-noroxycodol. CYP2D6 mediated metabolism produces oxymorphone (has analgesic activity; low plasma concentrations), alpha- and beta-oxymorphol.
Bioavailability: Controlled release, immediate release: 60% to 87%
Half-life elimination: Immediate release: 2-3 hours; controlled release: ~5 hours
Excretion: Urine (~19% as parent; >64% as metabolites)
Dosage
Oral:
Children: Immediate release:
6-12 years: 1.25 mg every 6 hours as needed
>12 years: 2.5 mg every 6 hours as needed
Adults:
Immediate release: 5 mg every 6 hours as needed
Controlled release:
Opioid naive: 10 mg every 12 hours
Concurrent CNS depressants: Reduce usual dose by 1/3 to 1/2
Conversion from transdermal fentanyl: For each 25 mcg/hour transdermal dose, substitute 10 mg controlled release oxycodone every 12 hours; should be initiated 18 hours after the removal of the transdermal fentanyl patch
Currently on opioids: Use standard conversion chart to convert daily dose to oxycodone equivalent. Divide daily dose in 2 (for twice-daily dosing, usually every 12 hours) and round down to nearest dosage form.
Note: 60 mg, 80 mg, or 160 mg tablets are for use only in opioid-tolerant patients. Special safety considerations must be addressed when converting to OxyContin® doses ?160 mg every 12 hours. Dietary caution must be taken when patients are initially titrated to 160 mg tablets. Using different strengths to obtain the same daily dose is equivalent (eg, four 40 mg tablets, two 80 mg tablets, one 160 mg tablet); all produce similar blood levels.
Multiplication factors for converting the daily dose of current oral opioid to the daily dose of oral oxycodone:
Current opioid mg/day dose x factor = Oxycodone mg/day dose
Codeine mg/day oral dose x 0.15 = Oxycodone mg/day dose
Hydrocodone mg/day oral dose x 0.9 = Oxycodone mg/day dose
Hydromorphone mg/day oral dose x 4 = Oxycodone mg/day dose
Levorphanol mg/day oral dose x 7.5 = Oxycodone mg/day dose
Meperidine mg/day oral dose x 0.1 = Oxycodone mg/day dose
Methadone mg/day oral dose x 1.5 = Oxycodone mg/day dose
Morphine mg/day oral dose x 0.5 = Oxycodone mg/day dose
Note: Divide the oxycodone mg/day dose into the appropriate dosing interval for the specific form being used.
Dosing adjustment in hepatic impairment: Reduce dosage in patients with severe liver disease
Dental Usual Dosing
Postoperative pain: Adults: Oral: 5 mg every 6 hours as needed
Administration: Oral
Do not crush, break, or chew controlled-release tablets; 60 mg, 80 mg, and 160 mg tablets are for use only in opioid-tolerant patients. Do not administer OxyContin® 160 mg tablet with a high-fat meal. Controlled release tablets are not indicated for rectal administration; increased risk of adverse events due to better rectal absorption.
Monitoring Parameters
Pain relief, respiratory and mental status, blood pressure
Reference Range
Blood level of 5 mg/L associated with fatality
Test Interactions
Some quinolones may produce a false-positive urine screening result for opiates using commercially-available immunoassay kits. This has been demonstrated most consistently for levofloxacin and ofloxacin, but other quinolones have shown cross-reactivity in certain assay kits. Confirmation of positive opiate screens by more specific methods should be considered.
Dietary Considerations
Instruct patient to avoid high-fat meals when taking OxyContin® 160 mg tablets.
Patient Education
If self-administered, use exactly as directed; do not increase dose or frequency. Drug may cause physical and/or psychological dependence. Do not crush or chew controlled-release tablets. While using this medication, do not use alcohol and other prescription or OTC medications (especially sedatives, tranquilizers, antihistamines, or pain medications) without consulting prescriber. Maintain adequate hydration unless instructed to restrict fluid intake. May cause hypotension, dizziness, drowsiness, impaired coordination, or blurred vision (use caution when driving, climbing stairs, or changing position - rising from sitting or lying to standing, or when engaging in tasks requiring alertness until response to drug is known); nausea, vomiting, or dry mouth (frequent mouth care, small frequent meals, chewing gum, or sucking lozenges may help); or constipation (increased exercise, fluids, fruit, or fiber may help; if unresolved, consult prescriber about use of stool softeners). The wax matrix from OxyContin® tablets may appear in stool. Report persistent dizziness or headache; excessive fatigue or sedation; changes in mental status; changes in urinary elimination or pain on urination; weakness or trembling; blurred vision; or shortness of breath. Pregnancy/breast-feeding precautions: Inform prescriber if you are or intend to become pregnant. If you are breast-feeding, take medication immediately after breast-feeding or 3-4 hours prior to next feeding.
Geriatric Considerations
The elderly may be particularly susceptible to the CNS depressant and constipating effects of narcotics. Prophylactic use of a laxative should be considered. Serum levels at a given dose may also be increased relative to concentrations in younger patients.
Additional Information
Prophylactic use of a laxative should be considered. OxyContin® 60 mg, 80 mg, and 160 mg tablets are for use in opioid-tolerant patients only.
Cardiovascular Considerations
Oxycodone may cause constipation which may be problematic in patients with unstable angina, and patients after myocardial infarction. The hemodynamic responses to valsalva-like maneuvers due to straining may have adverse cardiovascular consequences in patients with critical coronary artery disease.
Dental Health: Effects on Dental Treatment
Key adverse event(s) related to dental treatment: Xerostomia (normal salivary flow resumes upon discontinuation).
Dental Health: Vasoconstrictor/Local Anesthetic Precautions
No information available to require special precautions
Mental Health: Effects on Mental Status
Drowsiness and dizziness are common; may cause agitation, confusion, amnesia, depression, emotional lability, hallucinations, and malaise
Mental Health: Effects on Psychiatric Treatment
Concurrent use with psychotropics may cause additive sedation; use lower doses of both agents. Oxycodone may cause severe hypotension after concurrent administration with drugs which compromise vasomotor tone (eg, phenothiazines); monitor blood pressure.
Nursing: Physical Assessment/Monitoring
Assess other medications patient may be taking for additive or adverse interactions. Monitor for effectiveness of pain relief and monitor for signs of overdose. Monitor vital signs, CNS and respiratory status, and degree of sedation at beginning of therapy and at regular intervals with long-term use. May cause physical and/or psychological dependence. For inpatients, implement safety measures. Assess knowledge/teach patient appropriate use (if self-administered). Teach patient to monitor for adverse reactions, adverse reactions to report, and appropriate interventions to reduce side effects.
Dosage Forms
Excipient information presented when available (limited, particularly for generics); consult specific product labeling. [DSC] = Discontinued product
Capsule, immediate release, as hydrochloride: 5 mg
OxyIR®: 5 mg
Liquid, oral, as hydrochloride [concentrate]:
Roxicodone®: 20 mg/mL (30 mL) [contains sodium benzoate]
Solution, oral, as hydrochloride: 5 mg/5 mL (500 mL)
Roxicodone®: 5 mg/5 mL (5 mL, 500 mL) [contains ethanol]
Solution, oral, as hydrochloride [concentrate]: 20 mg/mL (30 mL)
ETH-Oxydose™: 20 mg/mL (1 mL, 30 mL) [contains sodium benzoate; berry flavor] [DSC]
Tablet, as hydrochloride: 5 mg, 10 mg, 15 mg, 20 mg, 30 mg
Roxicodone®: 5 mg, 15 mg, 30 mg
Tablet, controlled release, as hydrochloride:
OxyContin®: 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, 80 mg, 160 mg
Tablet, extended release, as hydrochloride: 10 mg, 20 mg, 40 mg, 80 mg [DSC]
Pricing: U.S. (www.drugstore.com)
Capsules (OxyCODONE HCl)
5 mg (20): $12.99
Capsules (OxyIR)
5 mg (20): $16.66
Concentrate (OxyCODONE HCl)
20 mg/mL (30): $33.99
Concentrate (Oxyfast)
20 mg/mL (30): $46.25
Solution (Roxicodone)
5 mg/5 mL (500): $53.00
Tablet, 12-hour (OxyCODONE HCl)
40 mg (20): $87.56
80 mg (20): $166.68
Tablet, 12-hour (OxyCONTIN)
10 mg (20): $45.47
20 mg (20): $76.67
40 mg (20): $137.91
60 mg (20): $189.98
80 mg (20): $257.93
Tablets (OxyCODONE HCl)
5 mg (20): $22.76
15 mg (20): $20.78
30 mg (20): $27.98
Tablets (Roxicodone)
15 mg (20): $31.99
References
“Drugs for Pain,” Med Lett Drugs Ther, 2000, 42(1085):73-8.
Kalso E and Vainio A, “Morphine and Oxycodone Hydrochloride in the Management of Cancer Pain,” Clin Pharmacol Ther, 1990, 47(5):639-46.
Mokhlesi B, Leikin JB, Murray P, et al, “Adult Toxicology in Critical Care: Part II: Specific Poisonings,” Chest, 2003, 123(3):897-922.
Turturro MA and O'Toole KS, “Oxycodone-Induced Pulmonary Edema,” Am J Emerg Med, 1991, 9(2):201-3.
Zacher JL and Givone DM, “False-Positive Urine Opiate Screening Associated With Fluoroquinolone Use,” Ann Pharmacother, 2004, 38:1525-28.
International Brand Names
Lexi-Comp.com
Last full review/revision July 2009
Content last modified July 2009
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