Buprenorphine (Transdermal)

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Buprenorphine is a μ-opioid receptors partial agonist. The opioid agonist activity is dose related. Buprenorphine also act as an antagonist at the κ-opioid receptors. Buprenorphine produces dose-related analgesia, it binds to and dissociates from the μ receptor slowly, which may account for the prolonged duration of analgesia and, in part, for the limited physical dependence potential observed with the drug.


Management of moderate to severe chronic pain.

[edit] DOSAGE

Each Buprenorphine Transdermal Patch provides delivery of buprenorphine continuously for 7 days and should be applied to the upper outer arm, upper chest, upper back, to a hairless or nearly hairless skin site


  • Buprenorphine (Transdermal) as the First Opioid Analgesic:
    • Initiate treatment with 5 mcg/hour.
  • Conversion from Other Opioids to Buprenorphine (Transdermal):
    • Prior Total Daily Dose of Opioid Less than 30 mg of Oral Morphine Equivalents per Day: Initiate treatment with 5 mcg/hour.
    • Prior Total Daily Dose of Opioid Between 30 mg to 80 mg of Oral Morphine Equivalents per Day: Initiate treatment with 10 mcg/hour. Patients may use short-acting analgesics as needed until analgesic efficacy with Buprenorphine (Transdermal) is attained.
    • Prior Total Daily Dose of Opioid Greater than 80 mg of Oral Morphine Equivalents per Day: Buprenorphine (Transdermal) 20 mcg/hour may not provide adequate analgesia for patients requiring greater than 80 mg/day oral morphine equivalents. Consider the use of an alternate analgesic.


  • Individually titrate to a dose that provides adequate analgesia and minimizes adverse reactions. The minimum Buprenorphine (Transdermal) titration interval is 72 hours. The maximum Buprenorphine (Transdermal) dose is 20 mcg/hour. Do not exceed the maximum dose due to the risk of QTc interval prolongation.


  • Severely impaired respiratory function
  • Acute or severe bronchial asthma
  • Known or suspected paralytic ileus
  • Known hypersensitivity to buprenorphine
  • Myasthenia gravis


  • Elderly, cachectic, and debilitated patients, and patients with chronic pulmonary disease: Monitor closely because of increased risk of respiratory depression.
  • Interaction with CNS depressants, especially benzodiazepines: Consider dose reduction of one or both drugs because of additive effects.
  • Avoid in patients with Long QT Syndrome, family history of Long QT Syndrome, or those taking Class IA or Class III antiarrhythmic medications.
  • Hypotensive effects: Monitor during dose initiation and titration.
  • Patients with head injury or increased intracranial pressure: Monitor for sedation and respiratory depression and avoid use of BUTRANS in patients with impaired consciousness or coma susceptible to intracranial effects of CO2 retention.
  • Buprenorphine may lower the seizure threshold in patients with a history of seizure disorder


  • CYP3A4 inducers: May increase clearance of buprenorphine.
  • Interaction with CNS depressants: Consider dose reduction of one or both drugs because of additive effects.
  • Muscle relaxants may enhance the action of Buprenorphine and produce an increased degree of respiratory depression.


  • Pregnancy Category C (US). Buprenorphine (Transdermal) should be used during pregnancy only if the potential benefit justifies the potential risk to the mother and the fetus
  • Nursing Mothers: Because of the potential for adverse reactions in nursing infants from Buprenorphine (Transdermal), a decision should be made whether to discontinue nursing or discontinue the drug, taking into account the importance of the drug to the mother.


Possible side effects include: Constipation, nausea, sleepiness, vomiting, tiredness, headache, dizziness, itching, redness or rash where the patch is applied.