Buprenorphine

Indications
 Sublingual
Moderate to severe pain
Adult: 200-400 mcg every 6-8 hr.
Child: >6 yr: 37.5-50 kg: 200-300 mcg; 25-37.5 kg: 100-200 mcg; 16-25 kg: 100 mcg. To be given every 6-8 hr.
Parenteral
Moderate to severe pain
Adult: 300-600 mcg IM or slow IV Inj repeated every 6-8 hr if needed.
Child: >6 mth: 3-6 mcg/kg every 6-8 hr. Max: 9 mcg/kg every 6-8 hr.
Intramuscular
Premedication before anaesthesia
Adult: 300 mcg. May also be given sublingually at 400 mcg.
Intravenous
As a perioperative analgesic supplement
Adult: 300-450 mcg via slow IV inj.
Contraindications
 Acute alcoholism; convulsive disorders; head injuries; increased intracranial pressure; comatose patients; resp depression and obstructive airway disease; patients on established opioid agonists.
Warnings / 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.
Adverse Reactions
 Sedation, nausea, dizziness, vertigo, hypotension, miosis, headache, hypoventilation, resp or CNS depression; tachycardia, bradycardia, urinary retention, coma, vomiting, drowsiness, sweating, confusion, dry mouth, diaphoresis, withdrawal syndrome.
Drug 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.
See Below for More buprenorphine Drug Interactions
Mechanism of Actions
 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.
Absorption: Rapidly absorbed through the muscles (IM), buccal mucosa (sublingual); peak plasma concentrations after 90 minutes (sublingual).
Distribution: Enters breast milk. Protein-binding: 96%.
Metabolism: Minimal 1st-pass effect; converted to N-dealkylbuprenorphine and conjugated metabolites. There is enterohepatic recirculation.
Excretion: Via faeces (mainly unchanged), via urine (small amounts as unchanged); 1.2-7.2 hr (elimination half-life).
Storage Conditions
 Intramuscular: Store at 15-30°C. Intravenous: Store at 15-30°C. Parenteral: Store at 15-30°C. Sublingual: Store at 15-30°C.
ATC Classification
 N02AE01 - buprenorphine ; Belongs to the class of oripavine derivative opioids. Used to relieve pain.
N07BC01 - buprenorphine ; Belongs to the class of drugs used in the management of opioid dependence.
Storage
 Intramuscular: Store at 15-30°C. Intravenous: Store at 15-30°C. Parenteral: Store at 15-30°C. Sublingual: Store at 15-30°C.
Available As
  • Buprenorphine 0.2 mg
  • Buprenorphine 0.3 mg

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