Generic Name

Buprenorphine Hydrochloride and Naloxone Hydrochloride

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Classification

FDA Approved Indications

• Treatment of opioid dependence

Mechanism of Action

Buprenorphine is a partial mu-opioid receptor agonist and kappa-opioid receptor antagonist, providing analgesia and reducing opioid withdrawal. Naloxone is an opioid antagonist that reverses respiratory depression and deterring misuse by precipitating withdrawal if injected. The combination reduces the potential for abuse.

Dosage and Administration

Adult: Typically once daily sublingually, dosages vary based on clinical response and titration, usually starting with 2-8 mg of buprenorphine; dosing adjustments are made accordingly.

Pediatric: Not approved for use in individuals under 16 years.

Geriatric: Use with caution; start at lower end of dosing range due to increased sensitivity.

Renal Impairment: Adjust dosage cautiously; monitor for accumulation.

Hepatic Impairment: Use with caution; hepatic function should be monitored.

Pharmacokinetics

Absorption: Good sublingual bioavailability (~30-50%)

Distribution: Widely distributed; crosses blood-brain barrier.

Metabolism: Primarily hepatic via CYP3A4; buprenorphine undergoes N-dealkylation, naloxone undergoes glucuronidation.

Excretion: Fecal and renal routes.

Half Life: Approximately 24-42 hours for buprenorphine; naloxone has a shorter half-life (~1-2 hours).

Contraindications

• Hypersensitivity to buprenorphine, naloxone, or any component of the formulation.
• Acute respiratory depression or comatose states.

Precautions

• Use cautiously in hepatic impairment, opioid-naïve individuals, and patients with a history of substance abuse. Monitor for signs of misuse, abuse, or addiction. Avoid use in pregnancy unless benefits outweigh risks.

Adverse Reactions - Common

• Headache (Common)
• Nausea (Common)
• Constipation (Common)
• insomnia (Common)

Adverse Reactions - Serious

• Respiratory depression (Uncommon)
• Hepatic toxicity (Uncommon)
• Precipitation of withdrawal symptoms if misused (Uncommon)

Drug-Drug Interactions

• CYP3A4 inhibitors/inducers affecting metabolism (e.g., ketoconazole, rifampin)
• Other central nervous system depressants

Drug-Food Interactions

N/A

Drug-Herb Interactions

N/A

Nursing Implications

Patient/Family Teaching

• Do not use other CNS depressants concurrently without medical advice.
• Take medication exactly as prescribed; do not self-adjust dose.
• Report any signs of adverse effects or withdrawal.

Special Considerations

Black Box Warnings:

• Potential for overdose and death, especially if misused or combined with CNS depressants.

Genetic Factors: Variations in CYP3A4 activity can affect metabolism.

Lab Test Interference: May alter liver function tests.

Overdose Management

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

Treatment: Naloxone administration, supportive respiratory care, and monitoring.

Storage and Handling

Storage: Store in a secure, dry place at room temperature.

Stability: Stable until the expiration date on the package.