Buprenorphine

Indications

Buprenorphine is used for: Pain, Anaesthesia, Opioid dependence

Adult Dose

Adult: Sublingual Moderate to severe pain 200-400 mcg 6-8 hrly. IV Perioperative analgesia 300-450 mcg via slow inj. IV/IM Moderate to severe pain 300-600 mcg 6-8 hrly. IM Anesth premed 300 mcg. Elderly: Moderate-to-Severe Pain 0.15 mg IV/IM q6hr; for IV, administered slowly over 2 minutes

Child Dose

Moderate-to-Severe Pain <2 years: Safety and efficacy not established 2-12 years: 2-6 mcg/kg slow IV/IM q4-6hr PRN >12 years: As in adults

Renal Dose

Administration

V Preparation Solution: Dilute to final concentration of 15 mcg/mL in D5W, D5/NS, NS, or LR Administer via controlled infusion device IV/IM Administration Administer by deep IM injection, by slow IV injection over >2 minutes, or by continuous IV infusion Also may be given by epidural injection at concentration of 6-30 mcg/mL

Contra Indications

Acute alcoholism; convulsive disorders; head injuries; increased intracranial pressure; comatose patients; resp depression and obstructive airway disease; patients on established opioid agonists.

Precautions

Hepatic or renal disease; pregnancy, lactation; hypothyroidism; adrenocortical insufficiency; asthma; prostatic hyperplasia; shock; hypotension; inflammatory or obstructive bowel disorders; myasthaenia gravis; infants/neonates. Reduce dose in elderly and debilitated patients. May precipitate withdrawal symptoms in narcotic addicts. Lactation: Drug enters breast milk; use not recommended

Pregnancy-Lactation

Interactions

Plasma-buprenorphine concentrations may be affected when co-administered with drugs that induce or inhibit cytochrome P450 isoenzyme CYP3A4. Enhanced depressant effects with other CNS depressants e.g. alcohol, anaesthetics, anxiolytics, hypnotics, TCAs and antipsychotics. Potentially Fatal: Diazepam may produce resp and cardiac collapse.

Adverse Effects

Side effects of Buprenorphine : >10% Sedation (2/3 of patients) 1-10% Dizziness,Headache,Hypotension,Hypoventilation,Miosis,Nausea,Sweating,Vertigo,Vomiting <1% Abdominal cramps,Amblyopia,Apnea,Blurred vision,Bradycardia,Coma,Confusion,Conjunctivitis,Constipation,Cyanosis,Depersonalization,Diplopia,Dreaming,Dry mouth,Dyspepsia,Dyspnea,Electrocardiographic (ECG) abnormalities,Euphoria,Fatigue,Flatulence,Hallucinations,Hypertension,Injection-site reactions,Malaise,Mental depression,Mydriasis,Nervousness,Paresthesia,Pruritus,Psychosis,Respiratory depression,Slurred speech,Tachycardia,Urticaria

Mechanism of Action

Buprenorphine exerts its analgesic effect by binding to the mu-opioid receptors in the CNS. It has a longer duration of analgesic action than morphine. Its partial agonist activity gives it a low level of physical dependence. Buprenorphine and morphine show similar dose-related resp depressant effect.