API

Drug classification

Buprenorphine: Opioid partial agonist; Naloxone: Opioid antagonist; Combination: Opioid dependence therapy.

Dosage form

Tablet

API strength per dosage

Buprenorphine Hydrochloride EP Eq to…

Dose

Adults: Initial dose 2 mg buprenorphine/0.5 mg naloxone sublingually, titrate to 8–16 mg/2–4 mg once daily; maximum 24 mg/6 mg daily. Not recommended for pediatric patients. Use caution and lower initial doses in elderly or hepatic impairment. Adjust dose based on clinical response.

Mechanism of action

Buprenorphine acts as a partial agonist at the μ-opioid receptor (MOR) and antagonist at the κ-opioid receptor (KOR); naloxone is a competitive antagonist at the μ-opioid receptor, deterring misuse by precipitating withdrawal if administered parenterally.

Indications

Opioid dependence, maintenance treatment of opioid dependence, detoxification of opioid dependence.

Side effects

Respiratory depression, sedation, constipation, headache, nausea, vomiting, sweating, insomnia, dizziness, hypotension, hepatic dysfunction, precipitated withdrawal, allergic reactions, QT prolongation, orthostatic hypotension.

Pregnancy category

Category C

Precautions

Risk of respiratory depression, potential for misuse and dependence, hepatic impairment, renal impairment, concurrent CNS depressant use, hypotension, head injury, pregnancy and breastfeeding, withdrawal symptoms on abrupt discontinuation, interactions with CYP3A4 inhibitors or inducers, not for use in opioid-naïve patients, caution in elderly or debilitated patients.

Contraindications

Hypersensitivity to buprenorphine, naloxone, or excipients, severe respiratory depression, acute severe asthma, paralytic ileus, severe hepatic impairment, acute alcoholism, delirium tremens.