OxyContin

What is OxyContin?

• OXYCONTIN® (oxycodone hydrochloride) extended-release tablets is an opioid agonist used for treatment of moderate to severe pain.

What are the uses of this medicine?

This medicine is for the management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatment options are inadequate in:

• Adults; and
• Opioid-tolerant pediatric patients 11 years of age and older who are already receiving and tolerate a minimum daily opioid dose of at least 20 mg oxycodone orally or its equivalent.

Limitations of Use:

• A long-acting (extended-release) opioid pain medicine that can put you at risk for overdose and death. Even if you take your dose correctly as prescribed you are at risk for opioid addiction, abuse, and misuse that can lead to death.
• Not for use to treat pain that is not around-the-clock.
• Not for use in children less than 11 years of age and who are not already using opioid pain medicines regularly to manage pain severe enough to require daily around-the-clock long-term treatment of pain with an opioid.

How does this medicine work?

• Oxycodone is a full opioid agonist and is relatively selective for the mu receptor, although it can bind to other opioid receptors at higher doses.
• The principal therapeutic action of oxycodone is analgesia.
• Like all full opioid agonists, there is no ceiling effect to analgesia for oxycodone.
• Clinically, dosage is titrated to provide adequate analgesia and may be limited by adverse reactions, including respiratory and CNS depression.
• The precise mechanism of the analgesic action is unknown.
• However, specific CNS opioid receptors for endogenous compounds with opioid-like activity have been identified throughout the brain and spinal cord and are thought to play a role in the analgesic effects of this drug.

Who Should Not Use this medicine ?

This medicine cannot be used in patients with:

• Significant respiratory depression
• Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment
• Known or suspected gastrointestinal obstruction, including paralytic ileus
• Hypersensitivity

What drug interactions can this medicine cause?

• The concomitant use of OXYCONTIN and CYP3A4 inhibitors(eg: Macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g. ketoconazole), protease inhibitors (e.g., ritonavir)) can increase the plasma concentration of oxycodone, resulting in increased or prolonged opioid effects. If concomitant use is necessary, consider dosage reduction of OXYCONTIN until stable drug effects are achieved. Monitor patients for respiratory depression and sedation at frequent intervals.
• The concomitant use of OXYCONTIN and CYP3A4 inducers (eg: Rifampin, carbamazepine, phenytoin) can decrease the plasma concentration of oxycodone. If concomitant use is necessary, consider increasing the OXYCONTIN dosage until stable drug effects are achieved.
• The concomitant use of benzodiazepines or other CNS depressants, including alcohol, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death.
• The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system has resulted in serotonin syndrome.
• The use of OXYCONTIN is not recommended for patients taking MAOIs (eg: phenelzine, tranylcypromine, linezolid) or within 14 days of stopping such treatment.
• Avoid concomitant use with Mixed Agonist/Antagonist and Partial Agonist Opioid Analgesics.
• Due to the risk of respiratory depression with concomitant use of skeletal muscle relaxants and opioids, consider prescribing naloxone for the emergency treatment of opioid overdose.
• Opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone.
• The concomitant use of anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus.

Is this medicine FDA approved?

• FDA approved this drug in the year of 2013.

How should this medicine be used?

• OXYCONTIN should be prescribed only by healthcare professionals who are knowledgeable in the use of potent opioids for the management of chronic pain.

Recommended Dosage:

• OXYCONTIN 60 mg and 80 mg tablets, a single dose greater than 40 mg, or a total daily dose greater than 80 mg are only for use in patients in whom tolerance to an opioid of comparable potency has been established.
• Patients considered opioid-tolerant are those taking, for one week or longer, at least 60 mg oral morphine per day, 25 mcg transdermal fentanyl per hour, 30 mg oral oxycodone per day, 8 mg oral hydromorphone per day, 25 mg oral oxymorphone per day, 60 mg oral hydrocodone per day, or an equianalgesic dose of another opioid.
• Use the lowest effective dosage for the shortest duration consistent with individual patient treatment goals.
• Individualize dosing based on the severity of pain, patient response, prior analgesic experience, and risk factors for addiction, abuse, and misuse.
• Discuss availability of naloxone with the patient and caregiver and assess each patient’s need for access to naloxone, both when initiating and renewing treatment with OXYCONTIN. Consider prescribing naloxone based on the patient’s risk factors for overdose .
• Do not abruptly discontinue OXYCONTIN in a physically dependent patient because rapid discontinuation of opioid analgesics has resulted in serious withdrawal symptoms, uncontrolled pain, and suicide.

Adults:

• For opioid-naïve and opioid non-tolerant patients, initiate with 10 mg tablets orally every 12 hours.

Pediatric Patients 11 Years of Age and Olderː

• For use only in pediatric patients 11 years and older already receiving and tolerating opioids for at least 5 consecutive days with a minimum of 20 mg per day of oxycodone or its equivalent for at least two days immediately preceding dosing with OXYCONTIN.

Geriatric Patients:

• In debilitated, opioid non-tolerant geriatric patients, initiate dosing at one third to one half the recommended starting dosage and titrate carefully.

Patients with Hepatic Impairment:

• Initiate dosing at one third to one half the recommended starting dosage and titrate carefully.

Administration

• Do not change your dose. Take OXYCONTIN exactly as prescribed by your healthcare provider. Use the lowest dose possible for the shortest time needed.
• Take your prescribed dose every 12 hours at the same time every day. Do not take more than your prescribed dose in 12 hours. If you miss a dose, take your next dose at your usual time.
• Swallow OXYCONTIN whole. Do not cut, break, chew, crush, dissolve, snort, or inject OXYCONTIN because this may cause you to overdose and die.
• OXYCONTIN should be taken 1 tablet at a time. Do not pre-soak, lick, or wet the tablet before placing in your mouth to avoid choking on the tablet.
• Call your healthcare provider if the dose you are taking does not control your pain.
• Do not stop taking OXYCONTIN without talking to your healthcare provider.
• Dispose of expired, unwanted, or unused OXYCONTIN by promptly flushing down the toilet, if a drug take-back option is not readily available. Visit www.fda.gov/drugdisposal for additional information on disposal of unused medicines.

What are the dosage forms and brand names of this medicine?

This medicine is available in fallowing doasage form:

• As Extended-release tablets: 10 mg, 15 mg, 20 mg, 30 mg, 40 mg, 60 mg, and 80 mg.

This medicine is available in fallowing brand namesː

• OXYCONTIN

What side effects can this medication cause?

The most common side effects of this medicine include:

• constipation
• nausea
• sleepiness
• vomiting
• tiredness
• headache
• dizziness
• abdominal pain

What special precautions should I follow?

• Serious, life-threatening, or fatal respiratory depression may occur. Monitor closely, especially upon initiation or following a dose increase. Instruct patients to swallow OXYCONTIN tablets whole to avoid exposure to a potentially fatal dose of oxycodone.

While taking OXYCONTIN DO NOT:

• Drive or operate heavy machinery until you know how OXYCONTIN affects you. OXYCONTIN can make you sleepy, dizzy, or lightheaded.
• Drink alcohol, or use prescription or over-the-counter medicines that contain alcohol. Using products containing alcohol during treatment with OXYCONTIN may cause you to overdose and die.
• Cases of adrenal insufficiency have been reported with opioid use, more often following greater than one month of use. If diagnosed, treat with physiologic replacement of corticosteroids, and wean patient off of the opioid.
• OXYCONTIN may cause severe hypotension, including orthostatic hypotension and syncope in ambulatory patients. Monitor during dosage initiation and titration. Avoid use of OXYCONTIN in patients with circulatory shock.
• In patients who may be susceptible to the intracranial effects of CO2 retention (e.g., those with evidence of increased intracranial pressure or brain tumors), OXYCONTIN may reduce respiratory drive, and the resultant CO2 retention can further increase intracranial pressure. Monitor such patients for signs of sedation and respiratory depression, particularly when initiating therapy with OXYCONTIN.
• There have been post-marketing reports of difficulty in swallowing OXYCONTIN tablets. These reports included choking, gagging, regurgitation and tablets stuck in the throat. Consider use of an alternative analgesic.
• OXYCONTIN exposes users to risks of addiction, abuse and misuse, which can lead to overdose and death. Assess patient’s risk before prescribing and monitor regularly for these behaviors and conditions.
• Accidental ingestion of OXYCONTIN, especially by children, can result in a fatal overdose of oxycodone.
• Prolonged use of OXYCONTIN during pregnancy can result in neonatal opioid withdrawal syndrome, which may be life-threatening if not recognized and treated.
• Concomitant use with CYP3A4 inhibitors (or discontinuation of CYP3A4 inducers) can result in a fatal overdose of oxycodone.
• Concomitant use of opioids with benzodiazepines or other central nervous system (CNS) depressants, including alcohol, may result in profound sedation, respiratory depression, coma, and death.

What to do in case of emergency/overdose?

Symptoms of overdosage may include:

• respiratory depression
• somnolence progressing to stupor or coma
• skeletal muscle flaccidity
• cold and clammy skin
• constricted pupils
• pulmonary edema
• bradycardia
• hypotension
• partial or complete airway obstruction
• atypical snoring
• death

Management of overdosage:

• In case of overdose, priorities are the reestablishment of a patent and protected airway and institution of assisted or controlled ventilation, if needed.
• Employ other supportive measures (including oxygen, vasopressors) in the management of circulatory shock and pulmonary edema as indicated. Cardiac arrest or arrhythmias will require advanced life support techniques.
• Opioid antagonists, such as naloxone, are specific antidotes to respiratory depression resulting from opioid overdose.
• OXYCONTIN will continue to release oxycodone and add to the oxycodone load for 24 to 48 hours or longer following ingestion, necessitating prolonged monitoring.
• In an individual physically dependent on opioids, administration of the recommended usual dosage of the antagonist will precipitate an acute withdrawal syndrome.

Can this medicine be used in pregnancy?

• Prolonged use of opioid analgesics during pregnancy may cause neonatal opioid withdrawal syndrome.
• There are no available data with OXYCONTIN in pregnant women to inform a drug-associated risk for major birth defects and miscarriage.

Can this medicine be used in children?

• The safety and efficacy of OXYCONTIN have been established in pediatric patients ages 11 to 16 years.
• Not for use in children less than 11 years of age and who are not already using opioid pain medicines regularly to manage pain severe enough to require daily around-the-clock long-term treatment of pain with an opioid.

What are the active and inactive ingredients in this medicine?

Active ingredients:

• Oxycodone hydrochloride

Inactive ingredients:

• Butylated hydroxytoluene
• Hypromelloses
• Polyethylene glycol 400
• Magnesium stearate
• Titanium dioxide
• Ferric oxide yellow
• FD&C blue no. 2
• Aluminum oxide
• Hydroxypropyl cellulose, unspecified

Who manufactures and distributes this medicine?

• Manufactured by: Purdue Pharma L.P., Stamford, CT.

What should I know about storage and disposal of this medication?

• Store at 25°C (77°F); excursions permitted between 15°-30°C (59°-86°F).
• Store OXYCONTIN securely and dispose of properly.
• Dispense in tight, light-resistant container.

• Dailymed label info on OxyContin
• FDA OxyContin

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