Oxycodone (Oxycontin) is a narcotic opioid analgesic medication that is used to treat moderate to severe pain.

Oxycodone Uses:

• Pain management:

  • Immediate-release formulations:

    • Administration of intense or persistent mild to acute pain with fitting symptom for the consumption of an opioid analgesic and inadequate replacement care.

  • Extended-release formulations:

    • Capsules:
      • Managing serious pain that involves regular, 24/7, prolonged-period opioid treatment and for which no other medication choices are sufficient.
    • Tablets:
      • Managing serious pain that involves regular, 24/7, prolonged-period opioid treatment and for which no other medication choices are sufficient, in grownups and opioid-tolerant kids ≥11 years of age who are previously getting and enduring least possible regular opioid prescription minimum of 20 mg oxycodone oral or equal to it.
  • Limitations of use:
    • Utilize oxycodone just for patients in whom substitute medication choices (eg, nonopioid analgesics, opioid combination products) are not helpful, endured, or insufficient in providing ample pain relief. Oxycodone ER is not suggested as an as-required analgesic.

Oxycodone (Oxycontin) Dose in Adults

Oxycodone (Oxycontin) Dose for Pain management: Oral:

Note: All dosages ought to be titrated till the desired result is attained.

• Immediate-release:

  • Oral:
    • Preliminary: 5 to 15 mg every 4 to 6 hours as required;
    • Dosing range: 5 to 20 mg per dosage.
    • For acute prolonged pain, manage in recurring gaps, every 4 to 6 hours, at the least possible amount that will attain sufficient analgesia.
  • Rectal [Canadian product]:
    • Initial: One suppository 3 to 4 times daily as necessary.

• Extended-release:

Note:

• Oxycodone ER capsules are not bioequivalent to ER tablets.
• The dosage of ER capsules is conveyed as oxycodone base as well as the dosage of ER tablets is expressed as oxycodone hydrochloride.
• Oxycodone ER 60 mg and 80 mg tablets are utilized in just opioid-tolerant patients. Single doses >40 mg (ER tablets) or >36 mg (ER capsules), or an overall dose of >80 mg daily (ER tablets) or >72 mg daily (ER capsules) are fixed for opioid-tolerant patients.

Opioid tolerance is defined as patients previously taking a minimum of morphine 60 mg orally every day, oxymorphone 25 mg orally every day, transdermal fentanyl 25 mcg per hour, oxycodone 30 mg orally daily, hydromorphone 8 mg orally daily, hydrocodone 60 mg orally daily, or an alike quantity of alternative opioid for at least 1 week.

• Opioid naive (use as the first opioid analgesic or consumption in patients who are not opioid-tolerant): Initial:
  • ER tablet: 10 mg two times daily
  • ER capsules: 9 mg two times daily

Conversion from other oral oxycodone formulations to oxycodone-ER:

• Begin oxycodone ER with 50%of the overall daily oral oxycodone daily dose (mg/day) administered two times daily.

Conversion from other opioids to oxycodone ER:

• Terminate all former 24/7 opioids when oxycodone ER is begun. Start with 10 mg (ER tablets) or 9 mg (ER capsules) two times every day.
• Considerable interpatient changeability happens due to patient individual factors, comparative effectiveness of dissimilar opioids, and dosage forms; thus, it is more appropriate to underestimate the inaugural 24-hour oral oxycodone obligations and handle saving medication (immediate-release opioid).

Conversion from transdermal fentanyl patch to oxycodone ER:

• Note:
  • Get Rid Of fentanyl patch at least 18 hours prior to initiating oxycodone ER. The manufacturer's recommendation is the use of careful transition factor of oxycodone ER tablets 10 mg or oxycodone ER capsules 9 mg every 12 hours for each fentanyl 25 mcg/hour transdermal patch;
  • Systematic evaluation of this proposed conversion has not been completed; tight monitoring required.

Conversion from methadone to oxycodone ER:

• Examine patients diligently when switching methadone to another opioid.
• The ratio between methadone and other opioid agonists significantly differs according to earlier dose exposure.
• Methadone has a long half-life and can accumulate in the plasma.

• Maintenance dose:

  • Dose modification (titration):
    • After starting oxycodone ER, adjust dosage in increments (25% to 50%) no more than every 1 to 2 days until needed pain control achieved.
    • The proposed maximum dose of ER capsules is 288 mg/day.
    • Patients might need rescuing doses of urgent-release analgesia for the duration of dose titration.
    • Monitor for markers and symptoms of opioid withdrawal or signs of oversedation/toxicity; if undesirable toxicity occurs, the following doses may be reduced.
    • Note:
      • Some clinicians have stated that in certain long-lasting pain patients, more recurrent dosing (i.e., every 8 hours) is needed for efficient pain management, though dosing more frequently than every 12 hours is not advocated by the manufacturer, and safety and efficiency have not been proven.

Dosage adjustment for concomitant therapy:

• Coexistent CNS depressants: Begin oxycodone ER with 33% to 50% of the calculated advised dose. Contemplate alternate analgesic if the reduced dose is less than the lowest accessible dosage form.

Discontinuation of therapy:

• When suspending persistent opioid treatment, the dosage should be steadily titrated down.
• A comprehensive decreasing schedule for all patients has not been recognized.
• Recommended schedules differ from gradual (eg, 10% reductions per week) to swift (eg, 25% to 50% reduction every few days).
• Decreasing schedules must be personalized for the least opioid withdrawal while keeping in mind patient-specific goals and worries as well as the pharmacokinetics of the opioid being tapered.
• A much slower reduction can be used in patients who have been getting opioids for a prolonged period of time(eg, years), specifically in the ultimate stage of decreasing, although more swift tapers may be suitable in patients suffering serious adverse events.
• Monitor intently for signs/symptoms of withdrawal. If the patient demonstrates withdrawal symptoms, consider reducing the taper schedule;  gaps between dose may be reduced, a lesser amount of daily dose reduction, pause tapering and start again when the patient is prepared, and/or administer an alpha-2 agonist (eg, clonidine) to blunted withdrawal symptoms along with it.
• Continue to propose nonopioid analgesics as needed for pain control for the duration of the taper; take into account nonopioid adjunctive treatments for withdrawal symptoms (eg, GI complaints, muscle spasms) as needed.

Dosage adjustment in debilitated patients (nonopioid tolerant):

• Immediate-release:
  • Initial: No specific dosage adjustments provided in the manufacturer's labeling; use with caution and with a smaller dose.
• Extended-release:
  • Initial: Start oxycodone ER with 33% to 50% of the calculated recommended dose.
  • Consider alternative analgesia if the reduced dose is less than the lowest available dosage form.

Oxycodone (Oxycontin) Dose in Children

Note:

• Dosages must be titrated to the needed effect.
• Numerous concentrations of oral solution accessible (20 mg/mL and 1 mg/mL); the highly concentrated formulation (20 mg/mL) must only be utilized in opioid-tolerant patients (taking ≥30 mg/day of oxycodone or equivalent for ≥1 week).
• Orders for oxycodone oral solutions (20 mg/mL or 1 mg/mL) must be visibly transcribed to involve the planned dose (in mg, not mL) and the intended product concentration to be distributed to prevent possible dosing inaccuracies:

Oxycodone (Oxycontin) Dose in the treatment of moderate to severe pain:

• Immediate release:

  • Infants ≤6 months: Limited data available:

    • Oral: Initial dose: 0.025 to 0.05 mg/kg/dose every 4 to 6 hours as required.

  • Infants >6 months, Children, and Adolescents: Oral:

    • Patient weight <50 kg:
      • Early dose: 0.1 to 0.2 mg/kg/dose every 4 to 6 hours as required; for acute pain, certain specialists have advised an early dose of 0.2 mg/kg; normal maximum dose range: 5 to 10 mg.
    • Patient weight ≥50 kg:
      • Initial dose: 5 to 10 mg every 4 to 6 hours as required; for intense pain an initial dose of 10 mg can be consumed; usual maximum dose: 20 mg/dose.

Oxycodone (Oxycontin) Dose in the treatment of severe pain requiring around-the-clock long-term opioid therapy:

• Extended-release tablets (eg, OxyContin):

Note:

• Use only in pediatric patients ≥11 years of age who are already receiving opioid therapy for at least 5 consecutive days, tolerating a minimum daily opioid dose of at least 20 mg of oxycodone orally or it's equivalent at least for the 2 days immediately before beginning extended-release oxycodone tablets, and for which alternative treatment options are inadequate.
• Prior to initiation, all other around-the-clock opioid therapy must be discontinued.

  • Initial dose: Children ≥11 years and Adolescents:

    • Oral: Initial dose based on current opioid regimen dose; use the following conversion factor table and equation to convert the current opioid(s) daily dose to the extended-release oxycodone tablet daily dose.
    • Note: Substantial interpatient variability exists due to patient-specific factors, the relative potency of different opioids, and dosage forms; therefore, it is preferable to underestimate the initial 24-hour oral oxycodone requirements and use rescue medication (immediate-release opioid):
  • Starting dose of extended-release oxycodone tablets administered every 12 hours = (mg/day of current opioid regimen X conversion factor)/2

Oxycodone Dose calculations or adjustments for specific clinical scenarios:

• If rounding is required, the numerical value should be rounded down to the nearest tablet strength. If the calculated daily dose is <20 mg, do not start extended-release oxycodone tablet as there is no safe tablet strength available.
• If more than one opioid in the regimen, calculate the approximate extended-release oxycodone tablet dose for each opioid and sum the totals for the approximate total daily extended-release oxycodone tablet dose, then divide by 2 for the 12-hour extended-release oxycodone dose.
• If the current opioid regimen includes a fixed-dose opioid/nonopioid dosage form (eg, hydrocodone/acetaminophen), only the mg of opioid should be used in the conversion calculations.
• If the patient receiving concomitant CNS depressants, reduce the extended-release oxycodone tablet initiating dose by one-third to one-half the calculated starting dose.
• If asymmetric dosing, the higher dose should be scheduled as the morning dose and the lower dose 12 hours later.

Note: The following conversion table should ONLY be used to convert opioid doses to extended-release oxycodone tablets (not from extended-release oxycodone tablets to other opioids; it is NOT a table of equianalgesic doses as it may overestimate initial dose).

Oxycodone Conversion Factor for Calculating Initial Extended-Release Oxycodone Tablet Dose in Pediatric Patients ≥11 years

Current opioid regimen to be converted to extended-release oxycodone tablet	Conversion Factor
	Oral	Parenteral*
Oxycodone	1	--
Hydrocodone	0.9	--
Hydromorphone	4	20
Morphine	0.5	3
Tramadol	0.17	0.2
* For patients receiving high-dose parenteral opioids, a more conservative conversion factor should be applied (ie, lower numerical conversion factor); for example, for high-dose parenteral morphine, conversion of 1.5 should be used for calculations instead of 3.

• Conversion from fentanyl patch to extended-release oxycodone tablet: Limited data available:

  • Children ≥11 years and Adolescents:
  • Note: Remove fentanyl patch at least 18 hours before beginning extended-release oxycodone.
  • Initial dose based on current opioid regimen dose; the manufacturer suggests using the conservative conversion factor of 10 mg every 12 hours of extended-release oxycodone tablet for each 25 mcg/hour fentanyl transdermal patch; systemic assessment of this suggested conversion has not been completed, monitor patients closely.

• Maintenance dose:

  • Dosage adjustment (titration):
    • After the beginning of the extended-release oxycodone tablet, adjust the dose in small increments (up to 25% of current total daily dosage) no more frequently than every 1 to 2 days until desired pain control; patients may need rescue doses of an immediate-release analgesic during dose titration.
    • Observe for signs and symptoms of opioid withdrawal or signs of oversedation and toxicity; if unacceptable adverse reactions occur, the subsequent dose may be reduced.

Oxycodone Pregnancy Risk Category: B

• [US Boxed Warning] Neonatal withdrawal syndrome can be caused by prolonged maternal opioid use during pregnancy. If not treated properly, it could prove fatal. Pregnant women who are on opioid therapy should be aware of the risks to their newborn.
• Oxycodone crosses into the placenta. The use of opioids by mothers may lead to birth defects, preterm delivery, low fetal growth, stillbirth, or other complications.
• Chronic opioid exposure during pregnancy can cause withdrawal symptoms in newborns.
• Symptoms of neonatal Abstinence Syndrome (NAS) may include autonomic symptoms (eg. fever, temperature instability), gastrointestinal symptoms (eg. diarrhea, vomiting), or neurologic (eg. high-pitched crying and hyperactivity, increased muscle tone/abnormal wakefulness/sleep pattern, increased wakefulness/abnormal sleeping pattern, irritability/seizure, tremors, yawning).
• Opioids can cause physical dependence in mothers who give birth to children who are also dependent. Opioids can cause respiratory depression and psycho-physiologic side effects in the neonate. Mothers who have received opioids during labor must be monitored.
• Other than oxycodone, agents are often used to treat pain associated with pregnancy and postpartum.

Oxycodone use during breastfeeding:

• Breast milk contains varying levels of oxycodone.
• One study found that oxycodone could be detected in breast milk for up to 37 hours after the last maternal dose.
• Additionally, therapeutic levels were detected in the serums of infants who were breastfeeding.
• Also, the urine of a breastfeeding infant was found to contain oxycodone (Sulton Villavasso 2012).
• Infants who were breastfed oxycodone have been known to experience constipation, CNS depression, reduced feeding, respiratory distress/irregular breath and decreased feeding.
• According to current guidelines, nonopioid painkillers are preferable for breastfeeding women suffering from postpartum discomfort.
• Some guidelines do not recommend breastfeeding mothers using oxycodone if an opiate needs to be taken.
• It may also be used to relieve pain in postpartum women. However, prolonged or frequent use can cause neonatal sedate.
• Doses greater than 30mg/day for mothers are not recommended.
• A woman who is an ultrarapid metabolizer should be cautious; oxycodone can be a substrate for CYP2D6 so their infants could be at greater risk of adverse effects.
• To limit the adverse effects on the infant and mother, it is important to use the lowest possible opioid dose when breastfeeding mothers are required.
• A single, occasional dose of opioid analgesics may be acceptable with breastfeeding.
• Breastfeeding mothers who use opioids to treat postpartum pain and chronic maternal pain should be vigilant for signs of drowsiness, sedation or feeding difficulties in infants.
• When breastfeeding is stopped or maternal use is cut off, withdrawal symptoms can occur.

Oxycodone (Oxycontin) Dose in Kidney Disease:

• CrCl ≥60 mL/minute:

  • There are no dosage adjustments provided in the manufacturer’s labeling.
  • Oxycodone clearance may decrease in patients with renal impairment; Start therapy at a low end of the dosing range.

• CrCl <60 mL/minute:

  • Serum concentrations are increased ~50%.
  • Start at the low end of the dosage range (use caution); adjust the dose as clinically indicated.
  • Alternatively, for both immediate and extended-release forms, doses of 33% to 50% of usual initial dosing have been recommended (Oxy IR Canadian product labeling; OxyNeo Canadian product labeling; Supeudol Canadian product labeling).
  • For ER tablets and capsules, if the reduced dose is less than the smallest available dosage form, consider an alternative analgesic.

Oxycodone (Oxycontin) Dose in Liver Disease:

• Immediate-release:

  • Start therapy at 33% to 50% of the usual dosage and titrate carefully.

• Extended-release tablets or Extended-release capsules:

  • Initial: Start oxycodone ER with 33% to 50% of the calculated recommended dose.
  • If the reduced dose is less than the smallest available dosage form, consider alternative analgesic.

---

As reported with adult patients, unless otherwise noted.

Common Side Effects of Oxycodone (Oxycontin):

• Central Nervous System:

  • Drowsiness
  • Headache
  • Dizziness

• Dermatologic:

  • Pruritus

• Gastrointestinal:

  • Nausea
  • Constipation
  • Vomiting

• Miscellaneous:

  • Fever

Less Common Side Effects Of Oxycodone (Oxycontin):

• Cardiovascular:

  • Flushing
  • Hypertension
  • Orthostatic Hypotension
  • Oxygen Saturation Decreased
  • Edema
  • Tachycardia
  • Cardiac Failure
  • Deep Vein Thrombosis
  • Hypotension
  • Palpitations
  • Peripheral Edema
  • Thrombophlebitis
  • Vasodilation

• Central Nervous System:

  • Abnormality In Thinking
  • Dysphoria
  • Insomnia
  • Irritability
  • Twitching
  • Abnormal Dreams
  • Anxiety
  • Chills
  • Confusion
  • Euphoria
  • Fatigue
  • Hypoesthesia
  • Migraine
  • Nervousness
  • Withdrawal Syndrome
  • Agitation
  • Pain
  • Depression
  • Lethargy
  • Paresthesia
  • Procedural Pain
  • Hypertonia
  • Neuralgia
  • Personality Disorder

• Dermatologic:

  • Excoriation
  • Diaphoresis
  • Hyperhidrosis
  • Skin Rash
  • Skin Photosensitivity
  • Urticaria

• Endocrine & Metabolic:

  • Hypochloremia
  • Hyponatremia
  • Weight Loss
  • Hyperglycemia
  • Gout

• Gastrointestinal:

  • Diarrhea
  • Xerostomia
  • Gastritis
  • Hiccups
  • Upper Abdominal Pain
  • Abdominal Pain
  • Anorexia
  • Decreased Appetite
  • Dyspepsia
  • Gastroesophageal Reflux Disease
  • Dysphagia
  • Gingivitis
  • Glossitis

• Genitourinary:

  • Dysuria
  • Urinary Retention
  • Urinary Tract Infection

• Hematologic & Oncologic:

  • Decreased Hemoglobin
  • Decreased Platelet Count
  • Decreased Red Blood Cells
  • Febrile Neutropenia
  • Neutropenia
  • Anemia
  • Hemorrhage
  • Iron Deficiency Anemia
  • Leukopenia

• Hepatic:

  • Increased Serum Alanine Aminotransferase

• Hypersensitivity:

  • Hypersensitivity Reaction

• Infection:

  • Herpes Simplex Infection
  • Infection
  • Sepsis

• Neuromuscular & Skeletal:

  • Asthenia
  • Limb Pain
  • Arthralgia
  • Back Pain
  • Musculoskeletal Pain
  • Myalgia
  • Tremor
  • Arthritis
  • Laryngospasm
  • Neck Pain
  • Ostealgia
  • Pathological Fracture

• Ophthalmic:

  • Blurred Vision
  • Amblyopia

• Respiratory:

  • Cough
  • Dyspnea
  • Oropharyngeal Pain
  • Bronchitis
  • Epistaxis
  • Flu-Like Symptoms
  • Laryngismus
  • Pharyngitis
  • Pulmonary Disease
  • Rhinitis
  • Sinusitis

• Miscellaneous:

  • Seroma
  • Accidental Injury

Side effects of Oxycodone (Oxycontin) Frequency Not Defined:

• Cardiovascular:

  • Circulatory Depression
  • Shock

• Central Nervous System:

  • Depersonalization

• Respiratory:

  • Respiratory Depression

Contraindications to Oxycodone (Oxycontin):

• Hypersensitivity to oxycodone and any component of the formulation (eg anaphylaxis or angioedema);
• Significant respiratory depression
• hypercapnia
• Acute or severe bronchial asthma in unmonitored settings or without resuscitative devices;
• GI obstruction, including paralytic ileus (known and suspected).

There is not much evidence of cross-reactivity between opioids and allergenic opioids. Cross-sensitivity is possible due to similarities in chemical structure or pharmacologic effects.

Canadian labeling:

• Additional contraindications not listed in the US labeling:
• Hypersensitivity to other opioids
• Suspected surgical abdomen (eg acute appendicitis, pancreatitis).
• Any disease or condition that impairs the transit of the bowel
• Mild pain can be managed by other pain medication (immediate release, or suppository).
• You can manage mild, intermittent or short-duration pain with pain medication or extended-release for acute pain.
• Chronic obstructive breathing
• Status asthmaticus
• Cor pulmonale
• Acute alcoholism
• delirium tremens
• convulsive disorders
• severe CNS depression
• Increased cerebrospinal and intracranial pressure
• Head injury
• Monoamine oxidase inhibitors (concomitant or within 14 days after therapy)
• Pregnant women and during labor and birth
• Breastfeeding

Warnings and precautions

• CNS depression:

  • CNS depression can lead to mental or physical impairments.
  • Patients should be cautious about driving or operating machinery that requires mental alertness.

• Constipation

  • Constipation can be a problem in patients with unstable angina or post-myocardial injury. 
  • To reduce constipation, consider preventive measures such as stool softener or increased fiber.

• Hypotension

  • This drug may cause severe hypotension, including orthostatic hypotension and hypotension.
  • Patients with cardiovascular disease (including acute MI), hypovolemia, or drugs that exaggerate hypotensive effects (including general anesthetics or phenothiazines) should be cautious.
  • After dose adjustment or initiation, be aware of hypotension symptoms. Patients suffering from circulatory shock should not take this medication.

• Phenanthrene hypersensitivity:

  • Use cautiously in patients with hypersensitivity reactions to other phenanthrene-derivative opioid agonists (codeine, hydrocodone, hydromorphone, levorphanol, oxymorphone).

• Respiratory depression [US Boxed Warning]

  • You may experience severe, life-threatening or fatal respiratory depression. You should be aware of respiratory depression during dose escalation or beginning.
  • Take ER tablets whole. Crushing, chewing, and dissolving them can result in rapid release and potentially fatal doses.
  • The sedative effects of opioids can be exaggerated by carbon dioxide retention due to opioid-induced respiratory depression.

• Conditions abdominales:

  • Patients with acute abdominal conditions may not be diagnosed or treated appropriately.

• Adrenocortical Insufficiency

  • Patients with Addison disease or adrenocortical impairment should be cautious.
  • Dose adjustment may be necessary. Long-term opioid abuse can cause secondary hypogonadism. This may lead to infertility, sexual dysfunction, mood disorders, and osteoporosis.

• Insufficiency of the biliary tract:

  • Patients with biliary dysfunction (including acute pancreatitis) should be cautious. It may cause constriction or obstructive effects.

• CNS depression/coma:

  • Patients with impaired consciousness and coma should not be used as they are more susceptible to the intracranial effects CO2 retention.

• Delirium tremens:

  • Patients with delirium-tremens should be cautious.

• Head trauma

  • Patients with intracranial injuries, intracranial lesion or elevated intracranial pressure should be used with extreme caution. ICP could become significantly elevated.

• Hepatic impairment

  • Patients with hepatic dysfunction should be cautious; oxycodone clearance could decrease.

• Mental health conditions

  • Patients with mental health conditions such as depression, anxiety disorders, and post-traumatic stress disorder should be cautious when using opioids for chronic pain.
  • There is a greater risk of opioid overdose and opioid dependency. It is best to have more frequent monitoring.

• Obesity:

  • Patients who are obese or morbidly overweight should be treated with caution.

• Prostatic hyperplasia/urinary restriction:

  • Patients with prostatic hyperplasia or urinary stricture should be cautious. Dose adjustment may be necessary.

• Psychosis:

  • Patients with toxic psychosis should be treated cautiously

• Renal impairment

  • Patients with kidney dysfunction should be cautious; oxycodone clearance could decrease.

• Respiratory disease

  • Patients with severe chronic obstructive lung disease or cor pulmonale should be treated with caution.
  • Also, patients with hypoxia, hypercapnia, and significantly low respiratory reserve may experience respiratory depression.
  • You might consider using non-opioid analgesics for these patients.

• Seizures:

  • Patients with seizure disorders should be cautious. It may exaggerate or cause seizures.

• Sleep-disordered breathing

  • Patients with sleep-disordered sleeping disorders, such as HF or obesity, should be cautious about chronic pain. 
  • Patients with severe or moderate sleep-disordered sleeping should avoid opioids.

• Thyroid dysfunction:

  • Patients with thyroid dysfunction should be cautious.

Oxycodone: Drug Interaction

Risk Factor C (Monitor therapy)
Alizapride	May enhance the CNS depressant effect of CNS Depressants.
Amphetamines	May enhance the analgesic effect of Opioid Agonists.
Anticholinergic Agents	May enhance the adverse/toxic effect of Opioid Agonists. Specifically, the risk for constipation and urinary retention may be increased with this combination.
Aprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Bosentan	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Brimonidine (Topical)	May enhance the CNS depressant effect of CNS Depressants.
Bromopride	May enhance the CNS depressant effect of CNS Depressants.
Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Cannabis	May enhance the CNS depressant effect of CNS Depressants.
Chlorphenesin Carbamate	May enhance the adverse/toxic effect of CNS Depressants.
Clofazimine	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
CYP3A4 Inducers (Moderate)	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
CYP3A4 Inhibitors (Moderate)	May enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Moderate) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite Oxymorphone may also be increased.
Deferasirox	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Desmopressin	Opioid Agonists may enhance the adverse/toxic effect of Desmopressin.
Dimethindene (Topical)	May enhance the CNS depressant effect of CNS Depressants.
Diuretics	Opioid Agonists may enhance the adverse/toxic effect of Diuretics. Opioid Agonists may diminish the therapeutic effect of Diuretics.
Dronabinol	May enhance the CNS depressant effect of CNS Depressants.
Duvelisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Erdafitinib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Erdafitinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Fosaprepitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Fosnetupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Gastrointestinal Agents (Prokinetic)	Opioid Agonists may diminish the therapeutic effect of Gastrointestinal Agents (Prokinetic).
Ivosidenib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Kava Kava	May enhance the adverse/toxic effect of CNS Depressants.
Larotrectinib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Lofexidine	May enhance the CNS depressant effect of CNS Depressants. Management: Drugs listed as exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Magnesium Sulfate	May enhance the CNS depressant effect of CNS Depressants.
MetyroSINE	CNS Depressants may enhance the sedative effect of MetyroSINE.
Minocycline	May enhance the CNS depressant effect of CNS Depressants.
Nabilone	May enhance the CNS depressant effect of CNS Depressants.
Netupitant	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Palbociclib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Pegvisomant	Opioid Agonists may diminish the therapeutic effect of Pegvisomant.
Piribedil	CNS Depressants may enhance the CNS depressant effect of Piribedil.
Pramipexole	CNS Depressants may enhance the sedative effect of Pramipexole.
Ramosetron	Opioid Agonists may enhance the constipating effect of Ramosetron.
RifAMPin	May decrease the serum concentration of OxyCODONE.
ROPINIRole	CNS Depressants may enhance the sedative effect of ROPINIRole.
Rotigotine	CNS Depressants may enhance the sedative effect of Rotigotine.
Rufinamide	May enhance the adverse/toxic effect of CNS Depressants. Specifically, sleepiness and dizziness may be enhanced.
Sarilumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Selective Serotonin Reuptake Inhibitors	CNS Depressants may enhance the adverse/toxic effect of Selective Serotonin Reuptake Inhibitors. Specifically, the risk of psychomotor impairment may be enhanced.
Serotonin Modulators	Opioid Agonists may enhance the serotonergic effect of Serotonin Modulators. This could result in serotonin syndrome. Exceptions: Nicergoline.
Siltuximab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Simeprevir	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
St John's Wort	May decrease the serum concentration of OxyCODONE.
Succinylcholine	May enhance the bradycardic effect of Opioid Agonists.
Tetrahydrocannabinol	May enhance the CNS depressant effect of CNS Depressants.
Tetrahydrocannabinol and Cannabidiol	May enhance the CNS depressant effect of CNS Depressants.
Tocilizumab	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers).
Risk Factor D (Consider therapy modification)
Alvimopan	Opioid Agonists may enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation.
Blonanserin	CNS Depressants may enhance the CNS depressant effect of Blonanserin.
Chlormethiazole	May enhance the CNS depressant effect of CNS Depressants. Management: Monitor closely for evidence of excessive CNS depression. The chlormethiazole labeling states that an appropriately reduced dose should be used if such a combination must be used.
CNS Depressants	May enhance the CNS depressant effect of OxyCODONE. Management: Avoid concomitant use of oxycodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
CYP3A4 Inducers (Strong)	May increase the metabolism of CYP3A4 Substrates (High risk with Inducers). Management: Consider an alternative for one of the interacting drugs. Some combinations may be specifically contraindicated. Consult appropriate manufacturer labeling.
CYP3A4 Inhibitors (Strong)	May enhance the adverse/toxic effect of OxyCODONE. CYP3A4 Inhibitors (Strong) may increase the serum concentration of OxyCODONE. Serum concentrations of the active metabolite oxymorphone may also be increased.
Dabrafenib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Seek alternatives to the CYP3A4 substrate when possible. If concomitant therapy cannot be avoided, monitor clinical effects of the substrate closely (particularly therapeutic effects).
Droperidol	May enhance the CNS depressant effect of CNS Depressants. Management: Consider dose reductions of droperidol or of other CNS agents (eg, opioids, barbiturates) with concomitant use. Exceptions to this monograph are discussed in further detail in separate drug interaction monographs.
Enzalutamide	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Concurrent use of enzalutamide with CYP3A4 substrates that have a narrow therapeutic index should be avoided. Use of enzalutamide and any other CYP3A4 substrate should be performed with caution and close monitoring.
Flunitrazepam	CNS Depressants may enhance the CNS depressant effect of Flunitrazepam.
HYDROcodone	CNS Depressants may enhance the CNS depressant effect of HYDROcodone. Management: Avoid concomitant use of hydrocodone and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
Lorlatinib	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Avoid concurrent use of lorlatinib with any CYP3A4 substrates for which a minimal decrease in serum concentrations of the CYP3A4 substrate could lead to therapeutic failure and serious clinical consequences.
Methotrimeprazine	CNS Depressants may enhance the CNS depressant effect of Methotrimeprazine. Methotrimeprazine may enhance the CNS depressant effect of CNS Depressants. Management: Reduce adult dose of CNS depressant agents by 50% with initiation of concomitant methotrimeprazine therapy. Further CNS depressant dosage adjustments should be initiated only after clinically effective methotrimeprazine dose is established.
MiFEPRIStone	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Minimize doses of CYP3A4 substrates, and monitor for increased concentrations/toxicity, during and 2 weeks following treatment with mifepristone. Avoid cyclosporine, dihydroergotamine, ergotamine, fentanyl, pimozide, quinidine, sirolimus, and tacrolimus.
Mitotane	May decrease the serum concentration of CYP3A4 Substrates (High risk with Inducers). Management: Doses of CYP3A4 substrates may need to be adjusted substantially when used in patients being treated with mitotane.
Monoamine Oxidase Inhibitors	OxyCODONE may enhance the serotonergic effect of Monoamine Oxidase Inhibitors. This could result in serotonin syndrome. Management: Seek alternatives when possible. Avoid use of oxycodone/naltrexone during and within 14 days after monoamine oxidase inhibitor treatment. Non-US labeling for some oxycodone products states that such use is contraindicated.
Nalmefene	May diminish the therapeutic effect of Opioid Agonists. Management: Avoid the concomitant use of nalmefene and opioid agonists. Discontinue nalmefene 1 week prior to any anticipated use of opioid agonistss. If combined, larger doses of opioid agonists will likely be required.
Naltrexone	May diminish the therapeutic effect of Opioid Agonists. Management: Seek therapeutic alternatives to opioids. See full drug interaction monograph for detailed recommendations.
Perampanel	May enhance the CNS depressant effect of CNS Depressants. Management: Patients taking perampanel with any other drug that has CNS depressant activities should avoid complex and high-risk activities, particularly those such as driving that require alertness and coordination, until they have experience using the combination.
PHENobarbital	May enhance the CNS depressant effect of OxyCODONE. PHENobarbital may decrease the serum concentration of OxyCODONE. Management: Avoid use of oxycodone and phenobarbital when possible. Monitor for respiratory depression/sedation. Because phenobarbital is also a strong CYP3A4 inducer, monitor for decreased oxycodone efficacy and withdrawal if combined.
Primidone	May enhance the CNS depressant effect of OxyCODONE. Primidone may decrease the serum concentration of OxyCODONE. Management: Avoid use of oxycodone and primidone when possible. Monitor for respiratory depression/sedation. Because primidone is also a strong CYP3A4 inducer, monitor for decreased oxycodone efficacy and withdrawal if combined.
Sincalide	Drugs that Affect Gallbladder Function may diminish the therapeutic effect of Sincalide. Management: Consider discontinuing drugs that may affect gallbladder motility prior to the use of sincalide to stimulate gallbladder contraction.
Sodium Oxybate	May enhance the CNS depressant effect of CNS Depressants. Management: Consider alternatives to combined use. When combined use is needed, consider minimizing doses of one or more drugs. Use of sodium oxybate with alcohol or sedative hypnotics is contraindicated.
Stiripentol	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors). Management: Use of stiripentol with CYP3A4 substrates that are considered to have a narrow therapeutic index should be avoided due to the increased risk for adverse effects and toxicity. Any CYP3A4 substrate used with stiripentol requires closer monitoring.
Suvorexant	CNS Depressants may enhance the CNS depressant effect of Suvorexant. Management: Dose reduction of suvorexant and/or any other CNS depressant may be necessary. Use of suvorexant with alcohol is not recommended, and the use of suvorexant with any other drug to treat insomnia is not recommended.
Tapentadol	May enhance the CNS depressant effect of CNS Depressants. Management: Avoid concomitant use of tapentadol and benzodiazepines or other CNS depressants when possible. These agents should only be combined if alternative treatment options are inadequate. If combined, limit the dosages and duration of each drug.
Voriconazole	May enhance the adverse/toxic effect of OxyCODONE. Voriconazole may increase the serum concentration of OxyCODONE. Management: A reduced oxycodone dose may be necessary with concurrent voriconazole. Increased frequency and duration of monitoring for oxycodone-related adverse effects is recommended.
Zolpidem	CNS Depressants may enhance the CNS depressant effect of Zolpidem. Management: Reduce the Intermezzo brand sublingual zolpidem adult dose to 1.75 mg for men who are also receiving other CNS depressants. No such dose change is recommended for women. Avoid use with other CNS depressants at bedtime; avoid use with alcohol.
Risk Factor X (Avoid combination)
Azelastine (Nasal)	CNS Depressants may enhance the CNS depressant effect of Azelastine (Nasal).
Bromperidol	May enhance the CNS depressant effect of CNS Depressants.
Conivaptan	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Eluxadoline	Opioid Agonists may enhance the constipating effect of Eluxadoline.
Fusidic Acid (Systemic)	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Idelalisib	May increase the serum concentration of CYP3A4 Substrates (High risk with Inhibitors).
Opioids (Mixed Agonist / Antagonist)	May diminish the analgesic effect of Opioid Agonists. Management: Seek alternatives to mixed agonist/antagonist opioids in patients receiving pure opioid agonists, and monitor for symptoms of therapeutic failure/high dose requirements (or withdrawal in opioid-dependent patients) if patients receive these combinations.
Orphenadrine	CNS Depressants may enhance the CNS depressant effect of Orphenadrine.
Oxomemazine	May enhance the CNS depressant effect of CNS Depressants.
Paraldehyde	CNS Depressants may enhance the CNS depressant effect of Paraldehyde.
Thalidomide	CNS Depressants may enhance the CNS depressant effect of Thalidomide.

Monitoring Parameters:

• Pain relief
• respiratory and mental status
• blood pressure
• bowel function
• signs/symptoms of misuse, abuse, and addiction
• signs or symptoms of hypogonadism or hypoadrenalism.

Alternate recommendations:

• Chronic pain (long-term therapy outside of end-of-life or palliative care, active cancer treatment, sickle cell disease, or medication-assisted treatment for opioid use disorder):
  • Assess benefits/risks of opioid therapy within 1 to 4 weeks of beginning treatment and with dose increases. Reassess benefits/risks every 3 months during therapy or more frequently in patients at increased risk of overdose or opioid use disorder.
  • Urine drug testing is recommended before starting and re-checking should be considered at least annually (includes controlled prescription medications and illicit drugs of abuse).
  • State prescription drug monitoring program (PDMP) data should be reviewed by clinicians before starting and periodically during therapy (frequency ranging from every prescription to every 3 months).

How to administer Oxycodone (Oxycontin)?

To avoid constipating side effects, it is important to use the right laxatives. For persistent nausea, antiemetics may be required. Some dosage forms are not suitable for administration through feeding tubes (eg gastric, NG).

Extended-release forms of dosage:

Tablet

• Do not eat the tablet. Take the tablet whole. Do not moisten or dissolve, break, chew, or cut extended-release tablets.
• Extended-release tablets should only be taken one at a given time. Each tablet should be followed immediately by water.

Capsule

• Each dose should be taken with food, and the exact same amount.
• Patients with difficulty swallowing may open a capsule and sprinkle the contents on soft foods such as yogurt, applesauce, or jam.
• To ensure that all contents are gone, rinse your mouth immediately.
• You can also administer the contents of the capsule via a nasogastric tube (NG) or a gastrostomy tube, (G-tube).
• First, flush the tube with water. Next, pour the capsule contents directly into it.
• Do not mix capsule contents with any fluid that will be used for flushing them through the tube. 
• Once contents are in the tube, flush it with 15 mL water, milk or any liquid nutritional supplement. Then, flush it again with 10 mL.

Forms of immediate-release medication:

Capsule

• Do not eat.

Oral solution

• You can take it with or without food.
• It is available in two strengths: 1 mg/mL or a concentrated oral solution (20mg/mL).
• To avoid confusion between different concentrations, caution should be taken.
• Prescriptions should clearly state the dose and the concentration in milligrams (mg) of Oxycodone.
• To ensure that the concentration of the oral solution is accurately administered, the enclosed calibrated syringe must be used. 
• Concentrated oral solution (20 mg/mL should not be used by opioid-tolerant patients who have taken >=30 mg/day oxycodone for >=1 Week.

Tablets

• Without an abuse-deterrent
  • Do not eat. If taken with food, the onset of symptoms may be delayed.
• Abuse-deterrent
  • Do not take the tablets with any other food. Do not crush, chew or disintegrate the tablets. The inactive ingredient in the tablets can cause irritation and nasal burning.
  • Before placing the tablet in your mouth, it should not be wet.

Suppository [Canadian Product]:

• Do not administer rectally. Do not crush, break, or disintegrate the suppositories.

Mechanism of action of Oxycodone (Oxycontin):

The CNS binds to the opiate receptors, which causes inhibition of ascending pain pathways. This alters the perception and response to pain.

The beginning of action

• Pain relief: Instant release in 10 to 15 minutes

Peak effect:

• Immediate-release: 0.5 to 1 hour

Duration:

• Immediate-release: 3 to 6 hours;
• Extended-release: ≤12 hours

Distribution:

• It is distributed to skeletal muscle, liver, intestinal tract, lungs, spleen, and brain

Protein binding:

• 38% to 45%

Metabolism:

• Hepatically via CYP3A4 to noroxycodone (has weak analgesic), noroxymorphone, and alpha- and beta-noroxycodol. CYP2D6 mediated metabolism produces oxymorphone (has analgesic activity; low plasma concentrations [<15%]), alpha- and beta-oxymorphol.

Bioavailability:

• Extended-release tablet, immediate release: 60% to 87%;
• The extended-release capsule is not bioequivalent to the extended-release tablet; however, the AUC is similar in a fed state

Half-life:

• Apparent:
  • Immediate-release: 3.2 to ~4 hours;
  • Extended-release tablet: 4.5 hours;
  • Extended-release capsule: 5.6 hours

Elimination:

• Children 2 to 10 years: 1.8 hours (range: 1.2 to 3 hours);
• Adults: 3.7 hours
• Adults with CrCl <60 mL/minute:
  • Half-life increases by 1 hour, but peak oxycodone concentrations increase by 50%, and AUC increases by 60%
• Adults with mild to moderate hepatic impairment:
  • Half-life increases by 2.3 hours, peak oxycodone concentrations increase by 50%, and AUC increases by 95%

Time to peak, plasma:

• Immediate-release: 1.2 to 1.9 hours;
• Extended-release: 4 to 5 hours

Excretion:

• Urine (~19% as parent; >64% as metabolites)

International Brand Names of Oxycodone:

• Oxaydo
• OxyCONTIN
• Roxicodone
• RoxyBond
• Xtampza ER
• ACT Oxycodone CR
• APO-Oxycodone CR
• Oxy-IR
• OxyNEO
• PMS-OxyCODONE
• PMSOxyCODONE CR
• Supeudol
• Supeudol 10
• Supeudol 20
• Abtard
• Alnagon
• Dancex
• Endone
• Epethinan
• Ircodon
• Lynlor
• MOxy
• Novacodone
• Orionox
• Oxycod
• OxyContin
• Oxycontin
• Oxycontin CR
• Oxycontin LP
• Oxycontin Neo
• Oxyfast
• Oxygesic
• Oxyneo
• Oxynorm
• OxyNorm
• Oxynorm IV
• Plexicodim
• Reltebon

Oxycodone Brand Names in Pakistan:

No Brands Available in Pakistan.