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Oxycodone


Pronunciation

 (oks i KOE done)


U.S. Brand Names

 OxyContin®; Oxydose™; OxyFast®; OxyIR®; Roxicodone™; Roxicodone™ Intensol™


Synonyms

 Dihydrohydroxycodeinone; Oxycodone Hydrochloride


Generic Available

 Yes


Canadian Brand Names

 OxyContin®; Oxy.IR®; Supeudol®


Use

 Management of moderate to severe pain, normally used in combination with non-narcotic 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. Note: 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).


Use - Dental

 Treatment of postoperative pain


Restrictions

 C-II


Pregnancy Risk Factor

 B/D (prolonged use or high doses at term)


Pregnancy Implications

 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

 Use with caution in patients with hypersensitivity reactions to other phenanthrene derivative opioid agonists (morphine, hydrocodone, hydromorphone, levorphanol, oxycodone, oxymorphone), respiratory diseases including asthma, emphysema, or COPD. Use with caution in pancreatitis or biliary tract disease, acute alcoholism (including delirium tremens), adrenocortical insufficiency, CNS depression/coma, kyphoscoliosis (or other skeletal disorder which may alter respiratory function), hypothyroidism (including myxedema), prostatic hyperplasia, urethral stricture, and toxic psychosis.

Use with caution in the elderly, debilitated, severe hepatic or renal function. Hemodynamic effects (hypotension, orthostasis) may be exaggerated in patients with hypovolemia, concurrent vasodilating drugs, or in patients with head injury. Respiratory depressant effects and capacity to elevate CSF pressure may be exaggerated in presence of head injury, other intracranial lesion, or pre-existing intracranial pressure. Tolerance or drug dependence may result from extended use. Healthcare provider should be alert to problems of abuse, misuse, and diversion. Do not crush controlled-release tablets. Some preparations contain sulfites which may cause allergic reactions. OxyContin® 80 mg and 160 mg strengths are for use only in opioid-tolerant patients requiring high daily dosages >160 mg (80 mg formulation) or >320 mg (160 mg formulation).


Adverse Reactions

>10%:

Central nervous system: Fatigue, drowsiness, dizziness, somnolence

Dermatologic: Pruritus

Gastrointestinal: Nausea, vomiting, constipation

Neuromuscular & skeletal: Weakness

1% to 10%:

Cardiovascular: Postural hypotension

Central nervous system: Nervousness, headache, restlessness, malaise, confusion, anxiety, abnormal dreams, euphoria, thought abnormalities

Dermatologic: Rash

Gastrointestinal: Anorexia, stomach cramps, xerostomia, biliary spasm, abdominal pain, dyspepsia, gastritis

Genitourinary: Ureteral spasms, decreased urination

Local: Pain at injection site

Respiratory: Dyspnea, hiccoughs

Miscellaneous: Diaphoresis

<1% (Limited to important or life-threatening): Anaphylaxis, anaphylactoid reaction, dysphagia, exfoliative dermatitis, hallucinations, histamine release, hyponatremia, ileus, intracranial pressure increased, mental depression, paradoxical CNS stimulation, paralytic ileus, physical and psychological dependence, SIADH, syncope, urinary retention, urticaria, vasodilation, withdrawal syndrome (may include seizure)

Note: Deaths due to overdose have been reported due to misuse/abuse after crushing the sustained release tablets.


Overdosage/Toxicology

 Symptoms of toxicity include CNS depression, respiratory depression, and miosis. Naloxone, 2 mg I.V. with repeat administration as necessary up to a total of 10 mg, can also be used to reverse toxic effects of the opiate.


Drug Interactions

 Substrate of CYP2D6 (major)

CNS depressants, MAO inhibitors, general anesthetics, and tricyclic antidepressants: May potentiate the effects of opiate agonists; dextroamphetamine may enhance the analgesic effect of opiate agonists

CYP2D6 inhibitors: May decrease the effects of oxycodone. Example inhibitors include chlorpromazine, delavirdine, fluoxetine, miconazole, paroxetine, pergolide, quinidine, quinine, ritonavir, and ropinirole.


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).


Stability

 Tablets should be stored at room temperature.


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: 3-6 hours; Controlled release: 12 hours

Metabolism: Hepatic

Half-life elimination: 2-3 hours

Excretion: Urine


Dosage

 Oral:

Immediate release:

Children:

6-12 years: 1.25 mg every 6 hours as needed

>12 years: 2.5 mg every 6 hours as needed

Adults: 5 mg every 6 hours as needed

Controlled release: Adults:

Opioid naive (not currently on opioid): 10 mg every 12 hours

Currently on opioid/ASA or acetaminophen or NSAID combination:

1-5 tablets: 10-20 mg every 12 hours

6-9 tablets: 20-30 mg every 12 hours

10-12 tablets: 30-40 mg every 12 hours

May continue the nonopioid as a separate drug.

Currently on opioids: Use standard conversion chart to convert daily dose to oxycodone equivalent. Divide daily dose in 2 (for every 12-hour dosing) and round down to nearest dosage form.

Note: 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.

Dosing adjustment in hepatic impairment: Reduce dosage in patients with severe liver disease


Administration

 Do not crush controlled-release tablets; 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.


Monitoring Parameters

 Pain relief, respiratory and mental status, blood pressure


Reference Range

 Blood level of 5 mg/L associated with fatality


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 (2-3 L/day of fluids) 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). 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.


Additional Information

 Prophylactic use of a laxative should be considered. OxyContin® 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.


Dosage Forms

Capsule, immediate release, as hydrochloride (OxyIR®): 5 mg

Solution, oral, as hydrochloride: 5 mg/5 mL (500 mL)

Roxicodone™: 5 mg/5 mL (5 mL, 500 mL) [contains alcohol]

Solution, oral concentrate, as hydrochloride: 20 mg/mL (30 mL)

Oxydose™: 20 mg/mL (30 mL) [contains sodium benzoate; berry flavor]

OxyFast®, Roxicodone™ Intensol™: 20 mg/mL (30 mL) [contains sodium benzoate]

Tablet, as hydrochloride: 5 mg

Roxicodone™: 5 mg, 15 mg, 30 mg

Tablet, controlled release, as hydrochloride (OxyContin®): 10 mg, 20 mg, 40 mg, 80 mg, 160 mg

Tablet, extended release, as hydrochloride: 80 mg


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.


International Brand Names

 Codix® (CO); Dinarkon® (CZ); Endone® (AU); Oxanest® (FI); Oxinovag® (AR); Oxycod Syrup® (IL); Oxycontin® (AR, AT, AU, BR); OxyContin® (CA); Oxycontin® (CH, CL, CO, CZ, DK, ES, FI, FR, GB, HU, IE, IL, MX, NO, NZ, SE, SI); Oxygesic® (DE); Oxy.IR® (CA); Oxynorm® (AU, CH, DK, FI, GB, IE, NO, NZ, SE); Proladone® (AU, NZ); Supeudol® (CA)


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