Oxycodone Hydrochloride

Pronunciation

Pronunciation: OX-ee-KOE-dohn HIGH-droe-KLOR-ide
Class: Opioid analgesic

Trade Names

Oxecta
- Tablets 5 mg
- Tablets 7.5 mg

Oxycodone
- Tablets 10 mg
- Tablets 20 mg
- Capsules 5 mg
- Solution, oral 5 mg/5 mL
- Solution, concentrate, oral 20 mg/mL

OxyContin
- Tablets, controlled-release 10 mg
- Tablets, controlled-release 15 mg
- Tablets, controlled-release 20 mg
- Tablets, controlled-release 30 mg
- Tablets, controlled-release 40 mg
- Tablets, controlled-release 60 mg
- Tablets, controlled-release 80 mg

Roxicodone
- Tablets 5 mg
- Tablets 15 mg
- Tablets 30 mg

Supeudol (Canada)

Pharmacology

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.

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Pharmacokinetics

Absorption

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.

Distribution

The Vd is 2.6 L/kg (IV). It is found in breast milk.

Metabolism

Extensively metabolized in the liver to noroxycodone (a major metabolite), oxymorphone, and their glucuronides.

Elimination

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).

Onset

15 to 30 min.

Peak

1 h.

Duration

4 to 6 h.

Special Populations

Severe Renal Function Impairment

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.

Indications and Usage

Relief of moderate to moderately severe pain.

Contraindications

Hypersensitivity to opiates; upper airway obstruction; acute asthma; diarrhea due to poisoning or toxins.

Dosage and Administration

Individualize dosing regimen for each patient.

Immediate-Release
Adults

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-Release
Adults

PO 10 to 160 mg twice daily (80 and 160 mg controlled-release tablets are for use in opioid-tolerant patients only).

Storage/Stability

Store at room temperature in tightly closed container; protect from light.

Drug Interactions

CNS depressants (eg, alcohol, barbiturate anesthetics, phenothiazines, sedatives, tricyclic antidepressants, other narcotics)

Additive CNS depression.

Laboratory Test Interactions

Increased amylase and lipase may occur up to 24 h after administration.

Adverse Reactions

Cardiovascular

Hypotension; orthostatic hypotension; bradycardia; tachycardia.

CNS

Lightheadedness; dizziness; sedation; disorientation; incoordination.

Dermatologic

Sweating; pruritus; urticaria.

GI

Nausea; vomiting; constipation; abdominal pain.

Genitourinary

Urinary retention or hesitancy.

Respiratory

Respiratory depression; laryngospasm; depression of cough reflex.

Miscellaneous

Tolerance; psychological and physical dependence with chronic use.

Precautions

Warnings

Controlled release

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.


Pregnancy

Category C .

Lactation

Excreted in breast milk.

Children

Not recommended for children.

Renal Function

Dosage reduction may be necessary.

Hepatic Function

Dosage reduction may be necessary.

Special Risk Patients

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.

Drug dependence

Has abuse potential.

Overdosage

Symptoms

Miosis, respiratory depression, CNS depression (somnolence progressing to stupor or coma), circulatory collapse, seizures, cardiopulmonary arrest, death.

Patient Information

  • Instruct patient to take medication before pain becomes severe for greatest effectiveness.
  • Instruct patient on methods of preventing constipation.
  • Instruct patient to make position changes slowly if lightheadedness or sedation occur.
  • Advise patient to avoid intake of alcoholic beverages or products containing alcohol while using this medication.
  • Advise patient that drug may cause drowsiness, and to use caution while driving or performing other tasks requiring mental alertness.
  • Explain that physical dependency may occur and that withdrawal symptoms may be noted on discontinuation after long-term therapy.
  • Instruct and alert patient to swallow the controlled-release tablets whole and not to break, chew, or crush them before ingestion.

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