oxycodone hydrochloride
Endocodone, M-oxy, Oxycontin, Oxydose, OxyFAST, OxyIR, Percolone, Roxicodone, Roxicodone Intensol, Supeudol ◆

Pharmacologic classification: opioid
Therapeutic classification: analgesic
Pregnancy risk category C
Controlled substance schedule II

Available forms
Available by prescription only
Capsules: 5 mg
Oral solution: 5 mg/ml, 20 mg/ml
Suppository: 10 mg ◆, 20 mg ◆ (not available in U.S.)
Tablets: 5 mg, 15 mg, 30 mg
Tablets (sustained-release): 10 mg, 20 mg, 40 mg, 80 mg

Indications and dosages
 Moderate to severe pain. Adults: 5 mg P.O. q 6 hours. Or, 1 to 3 suppositories P.R. daily, as needed.For patients not currently receiving opiates, who need a continuous, around-the-clock analgesic for an extended period, give 10 mg (sustained- release tablet) P.O. q 12 hours. May increase dose q 1 to 2 days as needed. The 80-mg formulation is for opioid-tolerant patients only.
≡ Dosage adjustment. For patients with impaired hepatic function, begin sustained-release tablets at 33% to 50% of the usual dosage and adjust carefully.

Pharmacodynamics
Analgesic action: Oxycodone acts on opiate receptors, providing analgesia for moderate to moderately severe pain. Acute pain, rather than chronic pain, appears to be more responsive.

Pharmacokinetics
Absorption: Rapid and complete absorption.
Distribution: Rapidly distributed.
Metabolism: Metabolized in the liver.
Excretion: Excreted principally by the kidneys.

Route Onset Peak Duration
P.O., Regular 10-15 min 1 hr 3-12 hr
P.O., Sustained Unknown Unknown Unknown


Contraindications and precautions
Contraindicated in patients hypersensitive to drug. Use cautiously in elderly or debilitated patients and in those with head injury, increased intracranial pressure, seizures, asthma, COPD, prostatic hyperplasia, severe hepatic or renal disease, acute abdominal conditions, urethral stricture, hypothyroidism, Addison’s disease, or arrhythmias.

Interactions
Drug-drug. Anticholinergics: May cause paralytic ileus. Use together cautiously.
Anticoagulants: Oxycodone products that contain aspirin may increase anticoagulant effects. Monitor clotting times, and use together cautiously.
Cimetidine: May increase respiratory and CNS depression, causing confusion, disorientation, apnea, or seizures. Avoid use together.
CNS depressants, such as antihistamines, barbiturates, benzodiazepines, general anesthetics, muscle relaxants, narcotic analgesics, phenothiazines, sedative-hypnotics, and tricyclic antidepressants: Potentiates respiratory and CNS depression, sedation, and hypotensive effects of drug. Use together with extreme caution.
Digitoxin, phenytoin, rifampin: May cause drug accumulation and enhanced effects when with other drugs extensively metabolized in the liver. Monitor patient closely.
General anesthetics: Causes severe CV depression. Use together with extreme caution.
Opioid agonist-antagonist or a single dose of an antagonist: Patients who become physically dependent on oxycodone may experience acute withdrawal syndrome. Avoid use together in this situation.
Drug-herb. St. John’s wort: Increases narcotic-induced sleeptime. Discourage use together.
Drug-lifestyle. Alcohol use: Potentiates respiratory and CNS depression, sedation, and hypotensive effects of drug. Discourage alcohol use.

Adverse reactions
CNS: sedation, somnolence, clouded sensorium, euphoria, dizziness, light-headedness,seizures.
CV: hypotension,bradycardia.
GI: nausea, vomiting, constipation.
GU: urine retention.
Respiratory: respiratory depression.
Skin: diaphoresis, pruritus, rash.
Other: physical dependence.

Effects on lab test results
• May increase amylase, lipase, and liver enzyme levels.

Overdose and treatment
The most common signs and symptoms of a severe overdose are CNS depression, respiratory depression, and miosis. Other acute toxic effects include hypotension, bradycardia, hypothermia, shock, apnea, cardiopulmonary arrest, circulatory collapse, pulmonary edema, and seizures.
 To treat acute overdose, first establish adequate respiratory exchange via a patent airway and ventilation as needed; give a narcotic antagonist (naloxone) to reverse respiratory depression. Because the duration of action of oxycodone is longer than that of naloxone, repeated naloxone dosing is needed. Don’t give naloxone unless patient has clinically significant respiratory or CV depression. Monitor vital signs closely.
 If within 2 hours of ingestion of an oral overdose, empty the stomach immediately via induced emesis (ipecac syrup) or gastric lavage. Use caution to avoid risk of aspiration. Administer activated charcoal via nasogastric tube for further removal of drug. Provide symptomatic and supportive treatment, including continued respiratory support and correction of fluid or electrolyte imbalance. Monitor laboratory values, vital signs, and neurologic status closely. Dialysis may be helpful if aspirin-containing products are involved.

Special considerations
• Some commercial preparations contain sodium metabisulfite, which may cause an allergic reaction in susceptible people.
• Single-agent oxycodone solution or tablets are ideal for patients who can’t take aspirin or acetaminophen.
• The sustained-release preparation isn’t intended for preoperative or immediate postoperative pain in patients not already taking the drug. Drug is only indicated for postoperative use if patient was receiving it before surgery or if pain is expected to persist for a long time. It also isn’t intended for p.r.n. use.
• Oxycontin is potentially addictive and abused as much as morphine.
• Drug may obscure signs and symptoms of an acute abdominal condition and it may worsen gallbladder pain.
• Consider prescribing a stool softener for patients receiving long-term therapy.
• The 80-mg sustained-release tablets are for opioid-tolerant patients.
• Patients being transferred from 5- to 25-mg daily conventional dose should receive 10 to 20 mg q 12 hours of the sustained-release preparation. If conventional dose is 30 to 45 mg or 50 to 60 mg daily, the sustained-release dose is 20 to 30 mg q 12 hours or 30 to 40 mg q 12 hours, respectively.
• Chewing, crushing, snorting, or injecting the sustained-release preparation can lead to overdose and death.
Breast-feeding patients
• It isn’t known if drug appears in breast milk. Use cautiously in breast-feeding women.
Pediatric patients
• Dosage may be individualized for children; however, safety and effectiveness in children haven’t been established.
Geriatric patients
• Lower doses are usually indicated for elderly patients, who may be more sensitive to therapeutic and adverse effects of drug.

Patient education
• For full analgesic effect, teach patient to take drug before onset of intense pain.
• Warn patient about possibility of decreased alertness or visual changes.
• Advise patient to avoid alcohol use.
• Advise patient to avoid hazardous activities while taking this drug.

Reactions may be common, uncommon, life-threatening, or COMMON AND LIFE THREATENING.
◆ Canada only
◇ Unlabeled clinical use