Oxycodone/naloxone

Dosage Forms & Strengths

oxycodone/naloxone

extended-release tablet: Schedule II

• 10 mg/5 mg
• 20 mg/10 mg
• 40 mg/20 mg

Chronic Pain

Indicated 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

Use as first opioid analgesic or in non-opioid tolerant patients

• Starting dose: 10 mg/5 mg PO q12hr
• Use of higher starting doses in patients who are not opioid tolerant may cause fatal respiratory depression

Titration and maintenance

• May be up-titrated from current dose by increasing by 10 mg/5 mg q12hr q1-2 days as needed based on efficacy, safety, and tolerability
• Not to exceed daily dose of 80 mg/40 mg (ie, 40 mg/20 mg q12hr)
• If breakthrough pain experienced, assess need for a dosage increase or a rescue dose of an immediate-release analgesic

Opioid tolerant patients

• Patients who are opioid tolerant are those receiving the following for ≥1 week:
• -≥60 mg/day PO morphine
• -≥25 mcg/hr transdermal fentanyl
• -≥30 mg/day PO oxycodone
• -≥8 mg/day PO hydromorphone
• -≥25 mg/day PO oxymorphone, OR
• -Equianalgesic dose of another opioid

Conversion to oxycodone/naloxone

Conversion from other PO oxycodone

• Administer one-half of the patient's total daily PO oxycodone dose as Targiniq ER q12hr
• Not to exceed daily dose of 80 mg/40 mg (ie, 40 mg/20 mg q12hr)

Conversion from other opioids

• Discontinue all other around-the-clock opioid drugs when initiating oxycodone/naloxone
• When converting patients to oxycodone/naloxone, it is safer to underestimate a patient’s 24-hr oral oxycodone requirements and provide rescue medication (eg, immediate-release opioid) than to overestimate the 24-hr oral oxycodone requirements, which could result in adverse reactions
• First convert current opioid to equivalent daily PO morphine dose, and then convert the morphine equivalent daily dose to the recommended oxycodone/naloxone dose (see Prescribing information for conversion table and example)
• Then convert from equivalent daily PO morphine dose to oxycodone/naloxone (see following):
• -Morphine 20 mg to <70 mg PO: 10 mg/5 mg PO q12hr
• -Morphine 70 mg to <110 mg PO: 20 mg/10 mg PO q12hr
• -Morphine 110 mg to <150 mg PO: 30 mg/15 mg PO q12hr
• -Morphine 150-160 mg PO: 40 mg/20 mg PO q12hr

Conversion from methadone

• Close monitoring is essential when converting from methadone to other opioid agonists
• The ratio between methadone and other opioid agonists may vary widely as a function of previous dose exposure
• Methadone has a long half-life and can accumulate in plasma

Conversion from transdermal fentanyl

• May initiate oxycodone/naloxone 18 hr after removing transdermal fentanyl patch
• A conservative estimated dose of ~10 mg/5 mg q12hr oxycodone/naloxone should be substituted for each 25 mcg/hr fentanyl patch
• Not to exceed daily dose of 80 mg/40 mg (ie, 40 mg/20 mg q12hr)
• Monitor closely during conversion; limited documented experience with this conversion

Conversion from transdermal buprenorphine

• Transdermal buprenorphine <20 mcg/hr: oxycodone/naloxone 10 mg/5 mg q12hr oxycodone/naloxone
• Not to exceed daily dose of 80 mg/40 mg (ie, 40 mg/20 mg q12hr)
• Monitor closely during conversion; limited documented experience with this conversion

Dosage Modifications

Hepatic impairment

• Mild: Reduce dose by one-third to one-half of the usual starting dose followed by careful titration
• Moderate-to-severe: Contraindicated

Renal impairment

• Reduce dose by one-half of the usual starting dose followed by careful dose titration

Dosing Considerations

Not indicated for prn analgesic

Administration

May take with or without food

Tablets must be swallowed intact and are not to be cut, broken, chewed, crushed, or dissolved (risk of rapid release and absorption of potentially fatal overdose)

Do not abruptly discontinue in a physically dependent patient; use a gradual downward titration to prevent withdrawal (see Prescribing information for suggested taper schedule)

<18 years: Safety and efficacy not established

See adult dosing

Higher oxycodone AUC (18% increase) and higher naloxone AUC (82% increase) for patients aged ≥65 yr compared with younger patients

Oxycodone & Naloxone may be found in some form under the following brand names:

• Targiniq

Tell your doctor about all the medicines you take, including prescription and non­prescription medicines, vitamins, and herbal supplements. Especially tell your doctor if you take:

• Central Nervous System (CNS) depressants such as sedatives, anxiolytics, hypnotics, neuroleptics, other opioids

• Medications that block the protein enzyme (CYP3A4) in the body such as:
  • macrolide antibiotics (clarithromycin, telithromycin)
  • HIV protease inhibitors (indinavir, nelfinavir, ritonavir, saquinavir)
  • HCV protease inhibitors (boceprevir, telaprevir)
  • antifungals (ketoconazole, itraconazole, posaconazole, voriconazole)
  • conivaptan (Vaprisol)
  • delavirdine (Rescriptor)
• Medications that increase the protein enzyme CYP3A4 in the body such as:
  • carbamazepine (Tegretol, Equetro, Carbatrol)
  • phenobarbital
  • phenytoin (Dilantin)
  • rifampin (Rifadin)
  • St John's wort
  • nimodipine (Nimotop)

This is not a complete list of oxycodone/naloxone drug interactions. Ask your doctor or pharmacist for more information.

Store Targiniq at room temperature, away from heat, moisture and light.

Store Targiniq and all medicines out of the reach of children.

Do not drink alcohol while taking Targiniq.