Oxycontin

— THERAPEUTIC CATEGORIES —
  • Narcotic analgesics

Oxycontin Generic Name & Formulations

General Description

Oxycodone HCl 10mg, 15mg, 20mg, 30mg, 40mg, 60mg, 80mg; ext-rel tabs.

Pharmacological Class

Opioid agonist.

How Supplied

Tabs—100

Manufacturer

Generic Availability

NO

Mechanism of Action

Oxycodone is a full opioid agonist and is relatively selective for the mu receptor, although it can bind to other opioid receptors at higher doses. The principal therapeutic action of oxycodone is analgesia. Although the precise mechanism of the analgesic action is unknown, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.

Oxycontin Indications

Indications

Management of severe and persistent pain that requires an extended treatment period with a daily opioid analgesic and for which alternative opioid therapies inadequate in adults and opioid-tolerant (already on ≥20mg/day oral oxycodone or its equivalent) children.

Limitations of Use

Due to risks of addiction, abuse, and misuse with opioids (can occur at any dosage or duration); increased risks of overdose and death with extended-release/long-acting opioid formulations, reserve for use in patients for whom alternative treatment options (eg, non-opioid analgesics, immediate-release opioids) are ineffective, not tolerated, or inadequate to provide sufficient management of pain. Not indicated as an as-needed (prn) analgesic.

Oxycontin Dosage and Administration

Adult

Swallow whole. Individualize. Usually given on a 12hr schedule. ≥18yrs: Opioid-naive, opioid non-tolerant: initially 10mg every 12hrs. May increase total daily dose by 25–50%; adjust at 1–2 day intervals. Conversion from other opioids or combinations: see full labeling. Elderly (debilitated and opioid non-tolerant), hepatic dysfunction or concomitant CNS depressants: initiate at ⅓ to ½ the usual starting dose and titrate slowly. 60mg and 80mg tabs, a single dose >40mg, or a total daily dose >80mg: for use in opioid-tolerant patients only. Withdraw gradually (esp. if opioid-dependent), taper by ≤10–25% every 2–4 weeks. See full labeling.

Children

Swallow whole. Usually given on a 12hr schedule. ≥11yrs: Opioid-tolerant: daily dose of Oxycontin (mg) = mg/day of prior opioid x conversion factor (see full labeling). Do not initiate if total daily dose <20mg. May increase total daily dose by 25%. See full labeling.

Administration

Swallow whole with water. Do not crush, chew or dissolve. Do not pre-soak, lick or wet the tablet prior to placing in the mouth.

Nursing Considerations

Swallow whole with water. Do not crush, chew or dissolve. Do not pre-soak, lick or wet the tablet prior to placing in the mouth.

Oxycontin Contraindications

Contraindications

Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected paralytic ileus or GI obstruction.

Oxycontin Boxed Warnings

Boxed Warning

Serious and life-threatening risks from use of Oxycontin: Addiction, abuse, and misuse; Life-threatening respiratory depression; Accidental ingestion; Risks from concomitant use with benzodiazepines or other CNS depressants; Neonatal opioid withdrawal syndrome; Opioid analgesic risk evaluation and mitigation strategy (REMS); Cytochrome P450 3A4 interaction.

Oxycontin Warnings/Precautions

Warnings/Precautions

Assess the potential need for access to naloxone when initiating and renewing therapy. Consider prescribing naloxone based on risk factors for overdose (eg, history of opioid use disorder, prior opioid overdose, household members or other close contacts at risk for accidental ingestion or overdose). Abuse potential (monitor). Life-threatening respiratory depression esp. during initiation or following dose increases. Accidental exposure may cause fatal overdose (esp. in children). Sleep-related breathing disorders (including central sleep apnea (CSA), sleep-related hypoxemia); consider dose reduction if CSA develops. Opioid-induced hyperalgesia (OIH) and allodynia; consider decreasing dose of current opioid or opioid rotation if OIH is suspected. COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Adrenal insufficiency. Monitor for signs of hypotension when initiating or titrating dose. Head injury. Impaired consciousness, coma, shock; avoid. Increased intracranial pressure, brain tumors; monitor. Convulsive disorders. Difficulty swallowing. Underlying GI disorders (eg, esophageal or colon cancer with a small GI lumen). Biliary tract disease. Acute pancreatitis. Acute alcoholism. Drug abusers. Avoid abrupt cessation. Reevaluate periodically. Impaired renal or hepatic function. Elderly. Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.

REMS

YES

Oxycontin Pharmacokinetics

Absorption

Approximately 60–87% of an oral dose reaches the systemic circulation compared with a parenteral dose.

Distribution

Volume of distribution: 2.6 L/kg (after IV admin). Plasma protein bound: ~45%.

Metabolism

Hepatic (CYP3A4, CYP2D6).

Elimination

Renal. Total plasma clearance: ~1.4 L/min.

Oxycontin Interactions

Interactions

Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor closely; consider prescribing naloxone if concomitant use is warranted. During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5HT3 receptor antagonists, mirtazapine, trazodone, tramadol, cyclobenzaprine, metaxalone, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and/or precipitate withdrawal symptoms. May be potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors). May be antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics. Paralytic ileus may occur with anticholinergics. May increase serum amylase.

Oxycontin Adverse Reactions

Adverse Reactions

Constipation, nausea, somnolence, dizziness, vomiting, pruritus, headache, dry mouth, asthenia, sweating; orthostatic hypotension, syncope, respiratory/CNS depression, seizures, adrenal insufficiency, OIH and allodynia.

Oxycontin Clinical Trials

See Literature

Oxycontin Note

Not Applicable

Oxycontin Patient Counseling

See Literature

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