Buprenorphine
Mechanism :
It is an opioid analgesic used in the treatment of intractable pain and cyanotic spells. It is 25 times more potent than morphine and has a longer duration of action.
Indication :
- Injection: Management of moderate to severe pain.
- Sub lingual tablets: Treatment of opioid dependence.
Contraindications :
Hypersensitivity to buprenorphine or any of its components.
Dosing :
<2 years:
Safety and efficacy not established.
Management of mild to moderate pain:
2-12 years: 2-6 mcg/kg slow IV/IM every 4-6 hours.
>12 years (same as adults): 0.3 mg IV/IM every 6 hours. When given IV, administer slowly over 2 minutes; may be repeated once (up to 0.3 mg) if required 30-60 minutes after initial dose.
Adverse Effect :
Asthenia, chills, headache, infection, abdominal pain, back pain, withdrawal syndrome, dizziness, confusion, fatigue, nervousness, slurred speech, paresthesia, somnolence, tinnitus, tremor, coma, convulsions, elevated cerebrospinal fluid pressure, hypoventilation, cyanosis, constipation, diarrhea, nausea, vomiting, rash, hives, pruritus, bronchospasm, angioneurotic edema, anaphylactic shock, vasodilation, orthostatic hypotension, chest pain, sweating, blurred vision, conjunctivitis, amblyopia, and miosis, euphoria, depersonalization, depression, dreaming, psychosis, auditory and visual hallucinations, urinary retention.
Interaction :
CNS depressants: Increased CNS depression may occur in patients receiving concurrent CNS depressants (e.g., narcotic analgesics, general anesthetics, benzodiazepines, phenothiazines, tranquilizers, sedative/hypnotics, or alcohol)
Diazepam: Respiratory and cardiovascular collapse with concurrent use of diazepam.
Alvimopan: Increases levels of buprenorphine by receptor binding competition and its concurrent use is contraindicated.
Renal Dose :
Dose in Renal Impairment GFR (mL/min)
| 20-50 | Dose as in normal renal function |
| 10-20 | Dose as in normal renal function, but avoid very large doses |
| <10 | Reduce dose by 25–50% initially and increase as tolerated; avoid very large single doses Transdermal: Dose as in normal renal function |
Dose in Patients undergoing Renal Replacement Therapies
| CAPD | Dialysed. Dose as in GFR<10 mL/ min |
| HD | Dialysed. Dose as in GFR<10 mL/ min |
| HDF/High flux | Dialysed. Dose as in GFR<10 mL/ min |
| CAV/VVHD | Not dialysed. Dose as in GFR=10– 20 mL/min |
Hepatic Dose :
Immediate release injectables
Specific guidelines for dosage adjustments in hepatic impairment are not available. Adjust dosing as per clinical response.
Extended-release subcutaneous injections
Mild hepatic impairment: No dosage adjustments required.
Moderate to severe hepatic impairment: Use is contraindicated.
Sublingual dosage forms and buccal films
Mild to moderate hepatic impairment: Use is contraindicated.
Severe hepatic impairment: Start with a reduced dose and increase to 50% recommended dose.
Transdermal patch and subdermal implants
Consider the use of an alternate analgesic in patients with severe hepatic impairment.