Adult: In patients with cancer, post-operative pain, or in severe cases that require strong opioid: As IV bolus inj: Initially, 1-10 mg over 1-2 minutes, then repeat as necessary at intervals not frequent than 4 hourly. As IV infusion: Initially, 2 mg/hour. As IV patient-controlled analgesia (PCA): 0.03 mg/kg bolus doses with a minimum lock-out time of 5 minutes. Dosage adjustment must be based on severity of pain, patient's condition or tolerability, and with previous or concomitant medication. Use the lowest effective dose for the shortest possible duration consistent with treatment goals. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines). Elderly: Initiate at the lower end of the dosing range; carefully titrate according to pain control.
Oral Moderate to severe pain
Adult: For the management of cases in which alternative treatments are inadequate: As conventional cap or tab, orodispersible tab, and oral solution: Usual initial dose: 5 mg 4-6 hourly. Alternatively, 5-15 mg 4-6 hourly as needed. As modified-release tab: Initially, 10 mg 12 hourly. Individualise dosing according to severity of pain, patient response, opioid tolerance, and prior analgesic experience. Use the lowest effective dose for the shortest possible duration consistent with treatment goals. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines). Elderly: Initiate at the lower end of the dosing range; carefully titrate according to pain control. Child: >12 years As modified-release tab: Same as adult dose. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines).
Subcutaneous Moderate to severe pain
Adult: In patients with cancer, post-operative pain, or in severe cases that require strong opioid: As SC bolus inj: Initially, 5 mg; may repeat 4 hourly as necessary. As SC infusion: Initially, 7.5 mg daily in opioid-naive patients. Dosage adjustment must be based on severity of pain, patient's condition or tolerability, and with previous or concomitant medication. Use the lowest effective dose for the shortest possible duration consistent with treatment goals. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines). Elderly: Initiate at the lower end of the dosing range; carefully titrate according to pain control.
What are the brands available for Oxycodone in Malaysia?
OxyContin
OxyNorm
Special Patient Group
Debilitated patients: Dose reduction may be required.
Renal Impairment
Reduce the initial dose by 50%, then carefully titrate to achieve adequate pain control according to patient's condition. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines).
Hepatic Impairment
Mild: Reduce the initial dose by 50%, then carefully titrate to achieve adequate pain control according to patient's condition. Moderate to severe: Contraindicated. Recommendations may vary among countries and between individual products (refer to specific product information or local guidelines).
Administration
Oxycodone May be taken with or without food. Recommendations on taking w/ or w/o food, opening cap, & crushing/chewing are product-specific. Consult product literature for specific instructions.
Reconstitution
IV bolus inj, infusion or PCA, and SC infusion: Dilute the dose using NaCl 0.9% inj, dextrose 5% in water, or water for inj to make a final concentration of 1 mg/mL.
Incompatibility
Incompatible with prochlorperazine; cyclizine in concentrations >3 mg/mL or when diluted in NaCl 0.9% solution.
Contraindications
Significant respiratory depression, acute or severe bronchial asthma (in an unmonitored setting or in the absence of resuscitative equipment), severe chronic obstructive lung disease, cor pulmonale, hypercapnia; cardiac arrhythmias; suspected or known gastrointestinal obstruction (including paralytic ileus), chronic constipation, delayed gastric emptying. Moderate to severe hepatic impairment. Concomitant or within 14 days after MAOI therapy. Contraindications may vary among countries and between individual products (refer to specific product information or local guidelines).
Special Precautions
Patient with hypersensitivity to other phenanthrene-derivative opioid agonists (e.g. codeine, hydrocodone, hydromorphone, levorphanol, oxymorphone); impaired respiratory function; CV disease (including acute MI), hypotension, hypovolaemia; inflammatory bowel disorders, biliary tract dysfunction (including acute pancreatitis); thyroid dysfunction (e.g. hypothyroidism or myxoedema), adrenocortical insufficiency (including Addison's disease); head injury, intracranial lesions, increased intracranial pressure, impaired or reduced level of consciousness; history of seizure disorders; delirium tremens, toxic psychosis, mental health conditions (e.g. anxiety disorders, depression, PTSD); current or history of substance (e.g. drug or alcohol) abuse disorder; sleep-related disorders (including sleep apnoea); prostatic hypertrophy or hyperplasia, urinary stricture. Use in the preoperative or perioperative setting, and within the 1st 12-24 hours after the operation. Avoid abrupt withdrawal. Concomitant use with sedative medicines or other CNS depressants (e.g. benzodiazepines). Morbidly obese or debilitated patients. Renal and mild hepatic impairment. Children and elderly. Pregnancy and lactation.
Adverse Reactions
Significant: CNS depression; neurotoxicity (e.g. seizures, tremors, delirium, hallucinations), opioid-induced hyperalgesia, constipation; severe hypotension, including orthostatic hypotension and syncope; central sleep apnoea and sleep-related hypoxaemia; may cause constriction of the sphincter of Oddi; exaggerated intracranial pressure elevation; secondary hypogonadism that may lead to mood disorders and osteoporosis (long-term use); withdrawal syndrome (characterised by mydriasis, restlessness, palpitations, insomnia, anorexia). Eye disorders: Blurred vision. Gastrointestinal disorders: Nausea, vomiting, abdominal pain, diarrhoea, dry mouth, dyspepsia, hiccup, gastritis. General disorders and administration site conditions: Asthenia, fatigue, chills, fever. Metabolism and nutrition disorders: Decreased appetite. Musculoskeletal and connective tissue disorders: Arthralgia, myalgia. Nervous system disorders: Dizziness, headache. Psychiatric disorders: Anxiety, confusion, depression, agitation, nervousness, abnormal thinking, abnormal dreams. Renal and urinary disorders: Urinary retention, dysuria. Respiratory, thoracic and mediastinal disorders: Dyspnoea, bronchospasm, pharyngitis. Skin and subcutaneous tissue disorders: Pruritus, rash, hyperhidrosis. Potentially Fatal: Respiratory depression; opioid addiction, abuse, and misuse; neonatal opioid withdrawal syndrome (prolonged use during pregnancy).
Patient Counseling Information
This drug may cause impaired physical or mental abilities, if affected, do not drive or operate machinery.
Monitoring Parameters
Evaluate risk factors for substance misuse, abuse or addiction prior to treatment initiation. Monitor pain relief, blood pressure, bowel function, and respiratory or mental status. Assess for signs and symptoms of substance abuse, misuse, or substance use disorder; hypogonadism or hypoadrenalism.
Overdosage
Symptoms: Nausea, vomiting, cold and/or clammy skin, miosis, hypotension, hypotonia, bradycardia, hallucinations, toxic leucoencephalopathy, somnolence progressing to stupor or deepening coma, apnoea, pulmonary oedema, respiratory depression, and circulatory failure; non-cardiac pulmonary oedema and rhabdomyolysis (particularly when given via IV inj). Management: Supportive treatment. Re-establish a patent airway with controlled ventilation. Administration of activated charcoal may be considered if a substantial amount is ingested within 1 hour. IV fluids and vasopressors may be given as indicated in the management of circulatory shock. Arrhythmias or cardiac arrest will require advanced life support techniques. May cautiously administer naloxone as an antidote in the presence of clinically significant respiratory or circulatory depression. Closely monitor until with re-established spontaneous respiration.
Drug Interactions
Increased plasma concentration resulting in enhanced or prolonged opioid effects with CYP3A4 inhibitors (e.g. clarithromycin, erythromycin, ketoconazole, voriconazole, ritonavir, saquinavir) and CYP2D6 inhibitors. Decreased plasma concentration and efficacy with CYP3A4 inducers (e.g. carbamazepine, phenytoin, rifampicin). Potential reduction of analgesic effects and induction of withdrawal symptoms with partial agonists or mixed agonist/antagonists opioid analgesics (e.g. nalbuphine, pentazocine, buprenorphine). Increased risk of urinary retention and severe constipation with anticholinergics. May reduce the therapeutic effect of diuretics. Potentially Fatal: Concomitant administration with MAOIs may cause severe CNS excitation or depression associated with hypotensive or hypertensive crisis. Increased risk of sedation, respiratory depression, and coma with sedative agents including benzodiazepines or other CNS depressants (e.g. non-benzodiazepine sedatives or hypnotics, antipsychotics, anxiolytics, antidepressants, general anaesthetics, muscle relaxants, tranquillisers, other opioids). May increase the risk of serotonin syndrome with SSRIs, SNRIs, TCAs, triptans, 5-HT3 receptor antagonists, certain muscle relaxants (e.g. metaxalone, cyclobenzaprine), and drugs that affect serotonergic neurotransmitter system (e.g. mirtazapine).
Food Interaction
Enhanced risk of sedation, respiratory depression, and coma with alcohol. Decreased plasma concentration and efficacy with St. John's wort. Increased plasma concentration with grapefruit juice.
Action
Description: Mechanism of Action: Oxycodone is a phenanthrene derivative opiate agonist that has analgesic, sedative and anxiolytic effects. It binds to CNS opioid receptors, thereby inhibiting the ascending pain pathways, changing the perception and response to pain, and inducing generalised CNS depression. Onset: Analgesia: 10-15 minutes (conventional form); within 1 hour (extended-release). Duration: 3-6 hours (conventional form); ≤12 hours (extended-release). Pharmacokinetics: Absorption: Absorbed from the gastrointestinal tract. Bioavailability: Approx 60-87%. Time to peak plasma concentration: 1.2-1.9 hours (conventional form); 4-5 hours (extended-release). Distribution: Distributed into the body, including the skeletal muscle, lungs, liver, intestinal tract, spleen, and brain. Crosses the placenta and enters breast milk. Plasma protein binding: 38-45%. Metabolism: Extensively metabolised in the liver by CYP3A4 into noroxycodone, noroxymorphone, α- and β-noroxycodol, and by CYP2D6 into oxymorphone, α- and β-oxymorphol. Excretion: Mainly via urine; faeces. Elimination half-life: 3-5 hours.
Chemical Structure
Oxycodone Source: National Center for Biotechnology Information. PubChem Database. Oxycodone, CID=5284603, https://pubchem.ncbi.nlm.nih.gov/compound/Oxycodone (accessed on Jan. 22, 2020)
Storage
Conventional cap or tab/Orodispersible tab/Oral solution/Modified-release tab: Store between 15-30°C. Protect from light and moisture. Solution for IV/SC inj or infusion: Store the intact vial below 30°C. Protect from light. Once opened, the undiluted or diluted solutions may be stored below 25°C for up to 24 hours. Storage recommendations may vary among countries and between individual products (refer to specific product guidelines).
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