Generic Name and Formulations:
Buprenorphine 5mcg/hr, 7.5mcg/hr, 10mcg/hr, 15mcg/hr, 20mcg/hr; transdermal patch.
Purdue Pharma L.P.
Indications for BUTRANS:
Management of pain severe enough to require daily, around-the-clock, long-term opioid treatment and for which alternative treatments are inadequate.
Limitations Of use:
Not for use as an as-needed (prn) analgesic. Use only if alternative treatment options (eg, non-opioid analgesics, immediate-release opioids) are ineffective, not tolerated, or otherwise inadequate to provide sufficient management of pain.
Use lowest effective dose for shortest duration. Apply one patch to clean, dry, hairless, intact skin on upper outer arm, upper chest, upper back, or side of chest every 7 days. Cleanse application site with water only. Do not cut patch. Rotate sites (allow ≥21 days before reapplication to same site). Individualize. ≥18yrs: Opioid-naive, or oral morphine equivalents <30mg/day: one 5mcg/hr patch. Doses of 7.5, 10, 15, 20mcg/hr: for opioid-tolerant patients only. Conversion from oral morphine equivalents 30–80mg/day: taper current opioids for up to 7 days to ≤30mg/day oral morphine equivalents before starting, then initiate with Butrans 10mcg/hr patch; may use short-acting analgesics until Butrans efficacy is attained. Conversion from oral morphine equivalents >80mg/day: consider alternative. For all: may adjust dose every 3 days in increments of 5mcg/hr, 7.5mcg/hr or 10mcg/hr; max 2 patches of each strength per titration. Max one 20mcg/hr patch per week. Concomitant use or discontinuation of CYP3A4 inhibitors or inducers: monitor closely and consider dose adjustments (see full labeling). Withdraw gradually every 7 days.
<18yrs: not established.
Significant respiratory depression. Acute or severe bronchial asthma in an unmonitored setting or in the absence of resuscitative equipment. Known or suspected GI obstruction, including paralytic ileus.
Addiction, abuse, and misuse. Risk evaluation and mitigation strategy (REMS). Life-threatening respiratory depression. Accidental exposure. Neonatal opioid withdrawal syndrome. Risks from concomitant use with benzodiazepines or other CNS depressants.
Not for use in the management of addictive disorders. Abuse potential (monitor). Life-threatening respiratory depression; monitor within first 24–72hrs of initiating therapy and following dose increases. Accidental exposure may cause fatal overdose (esp. in children). COPD, cor pulmonale, decreased respiratory reserve, hypoxia, hypercapnia, or pre-existing respiratory depression; monitor and consider non-opioid analgesics. Increased risk of QT prolongation with doses >20mcg/hr; avoid with history of long QT syndrome. Hypokalemia. Unstable cardiac disease (eg, unstable atrial fibrillation, symptomatic bradycardia, unstable CHF, active MI). Adrenal insufficiency. Head injury. Increased intracranial pressure, brain tumors; monitor. Seizure disorders. CNS depression. Impaired consciousness, coma, shock; avoid. Biliary tract disease. Acute pancreatitis. Fever. Drug abusers. Severe hepatic impairment: consider alternative. If at risk for hepatotoxicity (eg, history of alcohol or IV drug abuse, liver disease); obtain baseline liver enzyme levels and monitor periodically. Avoid external heat (eg, thermal wraps, sunlamps); risk of overdose. Reevaluate periodically. Avoid abrupt cessation. Elderly. Cachectic. Debilitated. Pregnancy; potential neonatal opioid withdrawal syndrome during prolonged use. Labor & delivery, nursing mothers: not recommended.
Opioid (partial agonist-antagonist).
Increased risk of hypotension, respiratory depression, sedation with benzodiazepines or other CNS depressants (eg, non-benzodiazepine sedatives/hypnotics, anxiolytics, general anesthetics, phenothiazines, tranquilizers, muscle relaxants, antipsychotics, alcohol, other opioids); reserve concomitant use in those for whom alternative options are inadequate; limit dosages/durations to minimum required; monitor. Avoid concomitant Class 1A (eg, quinidine, procainamide, disopyramide) or Class III antiarrhythmics (eg, sotalol, amiodarone, dofetilide). During or within 14 days of MAOIs: not recommended. Risk of serotonin syndrome with serotonergic drugs (eg, SSRIs, SNRIs, TCAs, triptans, 5-HT3 antagonists, mirtazapine, trazodone, tramadol, MAOIs, linezolid, IV methylene blue); monitor and discontinue if suspected. Avoid concomitant mixed agonist/antagonist opioids (eg, butorphanol, nalbuphine, pentazocine) or partial agonist (eg, buprenorphine); may reduce effects and precipitate withdrawal symptoms. Potentiated by CYP3A4 inhibitors (eg, macrolides, azole antifungals, protease inhibitors). Antagonized by CYP3A4 inducers (eg, rifampin, carbamazepine, phenytoin). May antagonize diuretics; monitor. Paralytic ileus may occur with anticholinergics.
Nausea, headache, application site reactions (pruritus, erythema, rash; discontinue if severe), dizziness, constipation, somnolence, vomiting, dry mouth; respiratory depression, severe hypotension, syncope, hypersensitivity reactions.
Hepatic (CYP3A4); 96% protein bound.
Biliary, fecal, renal.
Patch—4 (w. disposal units)