Home Drug Guide Buprenorphine Hydrochloride

Drug Guide

Generic Name

Buprenorphine Hydrochloride

Brand Names Buprenex, Subutex, Probuphine, Belbuca

Classification

Therapeutic: Opioid dependence and pain management

Pharmacological: Partial opioid agonist

FDA Approved Indications

Moderate to severe pain; opioid use disorder (OUD)

Mechanism of Action

Buprenorphine binds as a partial agonist to the mu-opioid receptor and as an antagonist at the kappa-opioid receptor, providing analgesia and reducing cravings and withdrawal symptoms in opioid dependence.

Dosage and Administration

Adult: Dosing varies by formulation and indication; for pain, typically 0.3 mg to 0.6 mg IV or IM initially, titrated as needed; for OUD, sublingual tablets start at 2-8 mg per day, titrated up to a stabilized dose; implants (Probuphine) are administered as four subdermal rods.

Pediatric: Use is not well established; consult specific guidelines for pediatric patients.

Geriatric: Use with caution; start at lower doses due to increased sensitivity and potential for reduced metabolism.

Renal Impairment: Adjust dose carefully; monitor renal function.

Hepatic Impairment: Use with caution; hepatic impairment may alter metabolism.

Pharmacokinetics

Absorption: Rapid and complete with Sublingual and buccal formulations.

Distribution: Extensive, with a high volume of distribution.

Metabolism: Metabolized mainly in the liver via CYP3A4 and CYP2C8 to norbuprenorphine.

Excretion: Excreted primarily in feces and urine.

Half Life: Approx. 24-60 hours, depending on formulation and route.

Contraindications

Hypersensitivity to buprenorphine or any component.
Respiratory depression, caution in severe respiratory impairment.

Precautions

Monitor for signs of overdose; risk of withdrawal symptoms in opioid-dependent individuals discontinuing therapy.
Use with caution in patients with head injury, increased intracranial pressure, or biliary tract disease.

Adverse Reactions - Common

Nausea or vomiting (Common)
Constipation (Common)
Dizziness or sedation (Common)

Adverse Reactions - Serious

Respiratory depression (Serious, rare but possible)
Hepatotoxicity (Rare)
Allergic reactions including rash, angioedema (Rare)

Drug-Drug Interactions

CNS depressants, sedatives, tranquilizers, other opioids, CYP3A4 inhibitors and inducers

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Assessment: Assess pain and opioid dependence; monitor respiratory status, vital signs, and signs of misuse or addiction.

Diagnoses:

Impaired Gas Exchange related to respiratory depression
Risk for Addiction

Implementation: Administer as prescribed; monitor for overdose symptoms; educate patient on proper use.

Evaluation: Evaluate pain relief effectiveness and signs of adverse reactions.

Patient/Family Teaching

Do not operate machinery or drive until effects are known.
Avoid alcohol and other CNS depressants.
Report signs of respiratory depression or allergic reactions immediately.

Special Considerations

Black Box Warnings:

Risk of addiction, abuse, and misuse leading to death.
Hepatic impairment can affect drug metabolism.

Genetic Factors: Metabolism may vary due to CYP3A4 activity.

Lab Test Interference: May affect liver function tests.

Overdose Management

Signs/Symptoms: Respiratory depression, sedation, hypotension, coma.

Treatment: Supportive care, oxygen, naloxone administration, airway management.

Storage and Handling

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

Stability: Stable under recommended conditions for duration specified in the product label.