Buprenorphine (Transdermal)

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[edit] BRAND NAMES

[edit] STRUCTURE

Buprenorphine.jpg

[edit] MECHANISM OF ACTION

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.

[edit] INDICATIONS

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

INITIAL DOSING

  • 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.


TITRATION:

  • 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.

[edit] CONTRAINDICATIONS

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

[edit] WARNINGS AND PRECAUTIONS

  • 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

[edit] INTERACTIONS

  • 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.

[edit] PREGNANCY AND LACTATION

  • 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.

[edit] SIDE EFFECTS

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

[edit] RELATED LINKS

[edit] REFERENCES