There are dosing and treatment considerations to be aware of
- There are no well-controlled clinical studies evaluating the safety and efficacy with dosing more frequently than every 12 hours. OxyContin is designed to provide delivery of oxycodone over 12 hours
- While OxyContin tablets offer your patient every-12-hour dosing, there is a potential for abuse, addiction, and diversion of OxyContin that should be considered in your prescribing decisions
- Instruct patients to swallow OxyContin tablets whole, one tablet at a time, with enough water to ensure complete swallowing immediately after placing in the mouth. Instruct patients not to pre-soak, lick, or otherwise wet the tablet prior to placing in the mouth. Cutting, breaking, crushing, chewing, or dissolving OxyContin tablets will result in uncontrolled delivery of oxycodone and can lead to overdose or death
Clinically significant drug interactions with OxyContin®
Inhibitors of CYP3A4 and CYP2D6
The concomitant use of OxyContin and CYP3A4 inhibitors can increase the plasma concentration of oxycodone, resulting in increased or prolonged opioid effects. These effects could be more pronounced with concomitant use of OxyContin and CYP2D6 and CYP3A4 inhibitors, particularly when an inhibitor is added after a stable dose of OxyContin is achieved
After stopping a CYP3A4 inhibitor, as the effects of the inhibitor decline, the oxycodone plasma concentration will decrease, resulting in decreased opioid efficacy or a withdrawal syndrome in patients who had developed physical dependence to oxycodone
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
If a CYP3A4 inhibitor is discontinued, consider increasing the OxyContin dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal
Macrolide antibiotics (e.g., erythromycin), azole-antifungal agents (e.g., ketoconazole), protease inhibitors (e.g., ritonavir)
CYP3A4 inducers
The concomitant use of OxyContin and CYP3A4 inducers can decrease the plasma concentration of oxycodone [see Clinical Pharmacology (12.3)], resulting in decreased efficacy or onset of a withdrawal syndrome in patients who have developed physical dependence to oxycodone
After stopping a CYP3A4 inducer, as the effects of the inducer decline, the oxycodone plasma concentration will increase, which could increase or prolong both the therapeutic effects and adverse reactions, and may cause serious respiratory depression
If concomitant use is necessary, consider increasing the OxyContin dosage until stable drug effects are achieved. Monitor for signs of opioid withdrawal. If a CYP3A4 inducer is discontinued, consider OxyContin dosage reduction and monitor for signs of respiratory depression
Rifampin, carbamazepine, phenytoin
Benzodiazepines and other central nervous system (CNS) depressants
Due to additive pharmacologic effect, the concomitant use of benzodiazepines or other CNS depressants, including alcohol, can increase the risk of hypotension, respiratory depression, profound sedation, coma, and death
Reserve concomitant prescribing of these drugs for use in patients for whom alternative treatment options are inadequate. Limit dosages and durations to the minimum required. Follow patients closely for signs of respiratory depression and sedation
Benzodiazepines and other sedatives/hypnotics, anxiolytics, tranquilizers, muscle relaxants, general anesthetics, antipsychotics, other opioids, alcohol
Serotonergic drugs
The concomitant use of opioids with other drugs that affect the serotonergic neurotransmitter system has resulted in serotonin syndrome
If concomitant use is warranted, carefully observe the patient, particularly during treatment initiation and dose adjustment. Discontinue OxyContin if serotonin syndrome is suspected
Selective serotonin reuptake inhibitors (SSRIs), serotonin and norepinephrine reuptake inhibitors (SNRIs), tricyclic antidepressants (TCAs), triptans, 5-HT3 receptor antagonists, drugs that affect the serotonin neurotransmitter system (e.g., mirtazapine, trazodone, tramadol), monoamine oxidase (MAO) inhibitors (those intended to treat psychiatric disorders and also others, such as linezolid and intravenous methylene blue)
Monoamine oxidase inhibitors (MAOIs)
MAOI interactions with opioids may manifest as serotonin syndrome or opioid toxicity (e.g., respiratory depression, coma)
The use of OxyContin is not recommended for patients taking MAOIs or within 14 days of stopping such treatment
phenelzine, tranylcypromine, linezolid
Mixed agonist/antagonist and partial agonist opioid analgesics
May reduce the analgesic effect of OxyContin and/or precipitate withdrawal symptoms
Avoid concomitant use
butorphanol, nalbuphine, pentazocine, buprenorphine
Muscle relaxants
Oxycodone may enhance the neuromuscular blocking action of skeletal muscle relaxants and produce an increased degree of respiratory depression
Monitor patients for signs of respiratory depression that may be greater than otherwise expected and decrease the dosage of OxyContin and/or the muscle relaxant as necessary
Diuretics
Opioids can reduce the efficacy of diuretics by inducing the release of antidiuretic hormone
Monitor patients for signs of diminished diuresis and/or effects on blood pressure and increase the dosage of the diuretic as needed
Anticholinergic drugs
The concomitant use of anticholinergic drugs may increase risk of urinary retention and/or severe constipation, which may lead to paralytic ileus
Monitor patients for signs of urinary retention or reduced gastric motility when OxyContin is used concomitantly with anticholinergic drugs
