Home Drug Guide Buprenorphine

Drug Guide

Generic Name

Buprenorphine

Brand Names Butrans, Sublocade, Brixadi

Classification

Therapeutic: Opioid dependence agent, Analgesic

Pharmacological: Partial opioid agonist

FDA Approved Indications

Management of pain in patients requiring continuous opioid analgesia long-term
Treatment of opioid dependence (for Sublocade) and opioid addiction

Mechanism of Action

Buprenorphine binds to mu-opioid receptors with high affinity as a partial agonist, producing analgesic effects and reducing withdrawal symptoms and cravings in opioid dependence, with a ceiling effect for respiratory depression.

Dosage and Administration

Adult: Dosage varies by formulation: For patches (Butrans), typically 5-20 mcg/hour applied weekly; for Sublocade, 300 mg first month, then 100 mg monthly; for Brixadi, 376 mg weekly or 675 mg every 2 weeks.

Pediatric: Not approved for pediatric use.

Geriatric: Start at lower doses and monitor closely due to age-related changes in drug metabolism and increased sensitivity.

Renal Impairment: Adjustments may be required; consult specific product labeling.

Hepatic Impairment: Use with caution; initiate at lower doses, especially in severe hepatic impairment.

Pharmacokinetics

Absorption: Well absorbed through skin (patch), IM, or subcutaneous injection.

Distribution: Widely distributed; crosses blood-brain barrier.

Metabolism: Primarily via CYP3A4 and CYP2C8 enzymes.

Excretion: Excreted mainly in feces; some renal excretion.

Half Life: Approximately 24-60 hours, depending on formulation and individual factors.

Contraindications

Hypersensitivity to buprenorphine or any components.
Severe respiratory depression.
Acute bronchial asthma in an unmonitored setting.

Precautions

Use with caution in patients with head injuries, increased intracranial pressure, or hepatic impairment.
Potential for abuse and dependency; monitor for signs of misuse.

Adverse Reactions - Common

Nausea (Common)
Vomiting (Common)
Itching or rash at application site (patch) (Common)
Dizziness (Common)
Constipation (Common)

Adverse Reactions - Serious

Respiratory depression (Rare)
Hepatic injury (Rare)
Allergic reactions including angioedema (Rare)

Drug-Drug Interactions

CNS depressants (e.g., benzodiazepines, other opioids), CYP3A4 inhibitors and inducers.
Addictive substances.

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Monitor respiratory status, level of consciousness, and pain levels.

Diagnoses:

Ineffective airway clearance related to respiratory depression.
Risk for dependency or misuse.

Implementation: Administer as prescribed; monitor for adverse effects; educate about proper use and disposal.

Evaluation: Assess effectiveness of pain control or addiction management, monitor for adverse reactions, and signs of misuse.

Patient/Family Teaching

Do not abruptly stop medication.
Use exactly as prescribed.
Report signs of respiratory depression or allergic reactions.
Proper disposal of unused medication.

Special Considerations

Black Box Warnings:

Risk of opioid addiction, abuse, and misuse.
The potential for respiratory depression, especially at initiation or dose escalation.

Genetic Factors: CYP3A4 variability can affect metabolism.

Lab Test Interference: May affect liver function tests.

Overdose Management

Signs/Symptoms: Respiratory depression, sedation, pinpoint pupils.

Treatment: Administer naloxone; support airway and breathing; provide symptomatic and supportive care.

Storage and Handling

Storage: Store at room temperature away from light and moisture.

Stability: Stable under recommended storage conditions.