• Moderate to severe pain.
• Pain severe enough to require daily, around-the-clock long-term opioid treatment and for which alternative treatment options are inadequate (extended-release) (children 11 yr should be tolerating a minimum opioid dose of 20 mg of oxycodone or equivalent for 5 days before initiating extended-release oxycodone therapy).

Contraindicated in:

• Hypersensitivity
• Some products contain alcohol or bisulfites and should be avoided in patients with known intolerance or hypersensitivity
• Significant respiratory depression
• Paralytic ileus
• Acute or severe bronchial asthma
• Acute, mild, intermittent, or postoperative pain (extended-release).

Use Cautiously in:

• Head trauma
• ↑intracranial pressure
• Severe renal or hepatic disease
• Hypothyroidism
• Adrenal insufficiency
• Alcoholism
• Seizure disorders
• Undiagnosed abdominal pain
• Prostatic hyperplasia
• Difficulty swallowing or GI disorders that may predispose patient to obstruction (↑ risk for GI obstruction)
• OB: Avoid chronic use; prolonged use of opioids during pregnancy can result in neonatal opioid withdrawal syndrome
• Lactation: Use while breastfeeding only if potential maternal benefit justifies potential risk to infant
• Pedi: Children <11 yr (safety and effectiveness of extended-release products not established)
• Geri: ↑risk of respiratory depression in older adults; initial dose ↓ recommended.

CV: orthostatic hypotension.

Derm: flushing, sweating.

EENT: blurred vision, diplopia, miosis.

Endo: adrenal insufficiency.

GI: constipation, choking, dry mouth, GI obstruction, nausea, vomiting.

GU: urinary retention.

Neuro: confusion, sedation, dizziness, dysphoria, euphoria, floating feeling, hallucinations, headache, unusual dreams.

Resp: RESPIRATORY DEPRESSION (INCLUDING CENTRAL SLEEP APNEA AND SLEEP-RELATED HYPOXEMIA).
Misc: physical dependence, psychological dependence, tolerance.

Drug-Drug:

• Use with caution in patients receiving MAO inhibitors (may result in unpredictable reactions — ↓ initial dose of oxycodone to 25% of usual dose).
• Additive CNS depression with alcohol, antihistamines, and sedative/hypnotics.
• Mixed agonist/antagonist analgesics, including nalbuphine or butorphanol and partial agonist analgesics, including buprenorphine, may ↓ oxycodone's analgesic effects and/or precipitate opioid withdrawal in physically dependent patients.
• Concurrent use of CYP3A4 inhibitors including ritonavir, ketoconazole, itraconazole, fluconazole, clarithromycin, erythromycin, nefazodone, diltiazem, verapamil, nelfinavir, and fosamprenavir↑ levels and risk of opioid toxicity; careful monitoring during initiation, dose changes, or discontinuation of the inhibitor is recommended.
• Concurrent use with CYP3A4 inducers including barbiturates, carbamazepine, efavirenz, corticosteroids, modafinil, nevirapine, oxcarbazepine, phenobarbital, phenytoin, rifabutin, or rifampin may ↓ fentanyl levels and analgesia; if inducers are discontinued or dosage ↓, patients should be monitored for signs of opioid toxicity and necessary dose adjustments should be made.
• CYP2D6 inhibitors may ↑ levels.
• Use with benzodiazepines or other CNS depressants including other opioids, non-benzodiazepine sedative/hypnotics, anxiolytics, general anesthetics, muscle relaxants, antipsychotics, and alcohol may cause profound sedation, respiratory depression, coma, and death; reserve concurrent use for when alternative treatment options are inadequate.
• Drugs that affect serotonergic neurotransmitter systems, including tricyclic antidepressants, SSRIs, SNRIs, MAO inhibitors, TCAs, tramadol, trazodone, mirtazapine, 5–HT₃ receptor antagonists, linezolid, methylene blue, and triptans, ↑ risk of serotonin syndrome.

(Generic available)

• Immediate-release capsules: 5 mg;
• Immediate-release tablets (Roxicodone): 5 mg; 10 mg; 15 mg; 20 mg; 30 mg;
• Immediate-release tablets (abuse-deterrent) (Oxaydo): 5 mg; 7.5 mg;
• Immediate-release tablets (abuse-deterrent) (Roxybond): 5 mg; 15 mg; 30 mg;
• Oral solution: 5 mg/5 mL; 100 mg/5 mL (concentrated);
• Extended-release capsules (abuse deterrent) (Xtampza ER): 9 mg; 13.5 mg; 18 mg; 27 mg; 36 mg;
• Extended-release tablets (abuse deterrent) (Oxycontin): 10 mg; 15 mg; 20 mg; 30 mg; 40 mg; 60 mg; 80 mg;
• Rectal suppositories: 10 mg; 20 mg;
• In combination with: aspirin (Endodan, Percodan), acetaminophen (Endocet, Magnacet, Oxycet, Percocet, Xartemis XR); see Appendix [not included in this PDA edition].

• PO (Adults 50 kg): Opioid-naive patients: 5–10 mg every 3–4 hr initially, as needed. Once optimal analgesia is obtained, patients with chronic pain may be converted to an equivalent 24-hr dose given in 2 divided doses as extended-release tablets every 12 hr.
• PO (Adults <50 kg): Opioid-naive patients: 0.2 mg/kg every 3–4 hr initially, as needed. Once optimal analgesia is obtained, patients with chronic pain may be converted to an equivalent 24-hr dose given in 2 divided doses as extended-release tablets every 12 hr.
• PO (Children 11 yr): 0.05–0.15 mg/kg every 4–6 hr as needed, as immediate-release product. Once optimal analgesia is obtained, patients with chronic pain may be converted to an equivalent 24-hr dose given in 2 divided doses as extended-release tablets every 12 hr.
• Rect (Adults): 10–40 mg 3–4 times daily initially, as needed.

Oxaydo, OxyCONTIN, Roxicodone, Roxybond, Xtampza ER

• Binds to opiate receptors in the CNS.
• Alters the perception of and response to painful stimuli, while producing generalized CNS depression.

• Decreased pain.

Therapeutic Classification: opioid analgesics

Pharmacologic Classification: opioid agonists, opioid agonists nonopioid analgesic combinations

Absorption: Well absorbed from the GI tract.

Distribution: Widely distributed. Crosses the placenta; enters breast milk.

Protein Binding: 38–45%.

Metabolism/Excretion: Mostly metabolized by the liver by the CYP3A4 isoenzyme, and to a lesser extent by the CYP2D6 isoenzyme.

Half-life: 2–3 hr.

Schedule II (C-II)

Oxy IR, OxyNEO, Supeudol

(analgesic effects)

†Extended-release.

• REMS: Instruct patient on how and when to ask for and take pain medication. Do not stop taking without discussing with health care professional; may cause withdrawal symptoms if discontinued abruptly after prolonged use. Do not increase doses without discussing with health care professional, may lead to overdose. Discuss safe use, risks, and proper storage and disposal of opioid analgesics with patients and caregivers with each Rx. The Patient Counseling Guide is available at www.fda.gov/OpioidAnalgesicREMSPCG.
• Advise patient that oxycodone is a drug with known abuse potential. Protect it from theft, and never give to anyone other than the individual for whom it was prescribed. Store out of sight and reach of children, and in a location not accessible by others.
• Educate patients and caregivers on how to recognize respiratory depression and emphasize the importance of calling 911 or getting emergency medical help right away in the event of a known or suspected overdose. Inform patients and caregivers about various ways to obtain naloxone as permitted by individual state naloxone dispensing and prescribing requirements or guidelines (by prescription, directly from a pharmacist, or as part of a community-based program).
• Advise patient to notify health care professional if pain control is not adequate or if severe or persistent side effects occur.
• Medication may cause drowsiness or dizziness. Advise patient to call for assistance when ambulating or smoking. Caution patient to avoid driving and other activities requiring alertness until response to medication is known.
• Advise patients taking Oxycontin tablets that empty matrix tablets may appear in stool.
• Advise patient to make position changes slowly to minimize orthostatic hypotension.
• Emphasize the importance of aggressive prevention of constipation with the use of oxycodone.
• Advise patient to avoid concurrent use of alcohol or other CNS depressants with this medication, may cause overdose.
• Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
• Encourage patient to turn, cough, and breathe deeply every 2 hr to prevent atelectasis.
• Advise patient that good oral hygiene, frequent mouth rinses, and sugarless gum or candy may decrease dry mouth.
• Advise patient to notify health care professional if pregnancy is planned or suspected, or if breastfeeding. Inform patient of potential for neonatal opioid withdrawal syndrome with prolonged use during pregnancy. Monitor neonate for signs and symptoms of withdrawal symptoms (irritability, hyperactivity and abnormal sleep pattern, high pitched cry, tremor, vomiting, diarrhea, and/or failure to gain weight); usually occur the first days after birth. Monitor infants exposed to oxycodone through breast milk for excess sedation and respiratory depression. Chronic use may reduce fertility in females and males.
• Emphasize the importance of aggressive prevention of constipation with the use of oxycodone.

ox-i-KOE-done