Trade Names:M-oxy- Tablets 5 mg
Trade Names:Endocodone- Tablets 5 mg
Trade Names:OxyIR- Capsules, immediate-release 5 mg
Trade Names:OxyContin- Tablets, controlled-release 10 mg- Tablets, controlled-release 20 mg- Tablets, controlled-release 40 mg- Tablets, controlled-release 80 mg- Tablets, controlled-release 160 mg
Trade Names:Oxydose- Solution, concentrate 20 mg/mL
Trade Names:OxyFAST- Solution, concentrate 20 mg/mL
Trade Names:Percolone- Tablets 5 mg
Trade Names:Roxicodone- Tablets 5 mg- Solution, oral 5 mg/5 mL
Trade Names:Roxicodone Intensol- Solution, concentrate 20 mg/mLSupeudol (Canada)
Relieves pain by stimulating opiate receptors in CNS; may cause respiratory depression, peripheral vasodilation, inhibition of intestinal peristalsis, sphincter of Oddi spasm, stimulation of chemoreceptors that cause vomiting and increased bladder tone.
High oral availability due to low presystemic or first-pass metabolism. Exhibits a biphasic absorption pattern. The immediate-release oral bioavailability is 100%. The oral bioavailability is 60% to 87%. Peak plasma concentration increased by 25% with a high fat meal. Once absorbed it is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain.
The Vd is 2.6 L/kg (IV). It is found in breast milk.
Extensively metabolized in the liver to noroxycodone (a major metabolite), oxymorphone, and their glucuronides.
Excreted through the urine, with less than 19% as free oxycodone, less than 50% as conjugated oxycodone, and less than 14% as conjugated oxymorphone. The t ½ for immediate release is 0.4 h. Cl is 0.8 L/min. Elimination on t 1/2 is 3.2 h (immediate release).
15 to 30 min.
4 to 6 h.
For less than 60 mL/min, higher peak plasma oxycodone (50%), and noroxycodone (20%), higher AUC for oxycodone (60%), noroxycodone (50%), oxymorphone (40%). There is an increased t ½ of oxycodone elimination of only 1 h.Mild to Moderate Hepatic Function Impairment
Peak plasma oxycodone and noroxycodone concentrations 50% and 20% higher; AUC values are 95% and 65% higher, respectively. Oxymorphone peak plasma concentration and AUC values are lower by 30% and 40%. The t ½ elimination for oxycodone is increased by 2.3 h.
Relief of moderate to moderately severe pain.
Hypersensitivity to opiates; upper airway obstruction; acute asthma; diarrhea due to poisoning or toxins.
Individualize dosing regimen for each patient.Immediate-ReleaseAdults
PO 10 to 30 mg every 4 h (5 mg every 6 h for OxyIR , oxycodone immediate-release capsules, Oxydose , and OxyFAST ) as needed.Controlled-ReleaseAdults
PO 10 to 160 mg twice daily (80 and 160 mg controlled-release tablets are for use in opioid-tolerant patients only).
Store at room temperature in tightly closed container; protect from light.
Additive CNS depression.
Increased amylase and lipase may occur up to 24 h after administration.
Hypotension; orthostatic hypotension; bradycardia; tachycardia.
Lightheadedness; dizziness; sedation; disorientation; incoordination.
Sweating; pruritus; urticaria.
Nausea; vomiting; constipation; abdominal pain.
Urinary retention or hesitancy.
Respiratory depression; laryngospasm; depression of cough reflex.
Tolerance; psychological and physical dependence with chronic use.
Controlled release is for management of moderate to severe pain with around-the-clock dosing. Not intended for as-needed use. Use 80 and 160 mg tablets in opioid tolerant patients only. Respiratory depression reported when used in opioid-naive patients. Swallow tablets whole. Do not crush, chew, or break; may result in potential fatal dose of oxycodone.
Category C .
Excreted in breast milk.
Not recommended for children.
Dosage reduction may be necessary.
Dosage reduction may be necessary.
Use with caution in elderly and debilitated patients and patients with myxedema, acute alcoholism, acute abdominal conditions, ulcerative colitis, decreased respiratory reserve, head injury or increased intracranial pressure, hypoxia, supraventricular tachycardia, depleted blood volume, or circulatory shock.
Has abuse potential.
Miosis, respiratory depression, CNS depression (somnolence progressing to stupor or coma), circulatory collapse, seizures, cardiopulmonary arrest, death.
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