Clinical Pharmacology Details


Buprenorphine


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Indications & Dose:

Moderate to severe pain


Note: Parenteral dose of 0.3 mg equivalent to 10 mg morphine


Adult


Tab: 200-400mcg sublingually 6-8 hrly or as reqd.


• IM/IV 0.3 mg q6h prn (reduce dosage by half in the elderly, debilitated patients, or in the presence of respiratory disease); repeat once (up to 0.3 mg) prn 30 60 min after initial dose


Child >2 yr


• IM/IV 2 p.g/kg/dose q6 8h prn Premedication: By sublingual administration, 400 micrograms. By intramuscular injection, 300 micrograms. Intra-operative analgesia, by slow intra-venous injection, 300-450 micrograms


I.V. OR I.M. INJECTION (BUPRENEX) Adults and children age 12 and over. 0.3 mg every 6 hr or more, p.r.n. A second 0.3-mg dose may be given 30 to 60 min after first dose, if needed.


DOSAGE ADJUSTMENT


for patients not at high risk for opioid toxicity, I.M. dose increased to 0.6 mg or frequency increased to every 4 hr, if needed, depending on pain severity and patient response. For elderly or debilitated patients and patients who have respiratory disease or also use


another CNS depressant, I.V. or I.M. dose reduced by half. Children ages 2 to 12. 0.002 to 0.006 mg/ kg every 4 to 6 hr, p.r.n. > To control moderate to severe chronic pain in patients requiring a continuous, around-the-clock opioid analgesic for an extended period of time TRANSDERMAL PATCH


Opioid-naive adults and adults whose daily dose of oral morphine or equivalent was less than 30 rag. Initial: 5 mcg/hr, increased after 72 hr, as needed, to 10 mcg/hr. Maximum: 20 mcg/hr. Adults whose daily dose of oral morphine or equivalent was between 30 and 80 mg. Initial: 10 mcg/hr, increased after 72 hr, as needed, to 20 mcg/hr.


Maximum: 20 mcg/hr.


DOSA6E ADJUSTMENT


¥or patient with mild to moderate hepatic impairment, initial dosage begun at 5 mcg/hr.


>• To treat opioid dependence


SUBLINGUAL TABLETS (SUBUTEX)


Adults. 12 to 16 mg daily. 

Contraindications:

Hypersensitivity to buprenorphine or its components 

Side Effects:

Cautions:

Precautions:

Addictive personality, narcotic dependent patients (may cause withdrawal), increased intracranial pressure, respiratory depression, hepatic disease, renal disease, hypothyroidism, biliary tract dysfunction, prostatic hypertrophy

Interaction:

DRUGS


CNS depressants, MAO inhibitors: Additive hypotensive and respiratory and CNS depressant effects of these drugs opioid analgesics: Reduced therapeutic effects if buprenorphine is given before another opioid analgesic.


 

Warnings:

Adverse Effects:

Lactations:

Safe use in labor and delivery has not been established; excretion into breast milk unknown 

Special Precautions:

Counselling:

Side Effects Or Adverse Reactions:

CNS: Coma, confusion, depression, dizziness, euphoria, hallucinations, headache, nervousness, paresthesia, psychosis, sedation, slurred speech, tremor, weakness


CV: Bradycardia, hypertension, hypotension, tachycardia


EENT: Blurred vision, conjunctivitis, diplopia, miosis, tinnitus


GI: Constipation, dry mouth, dyspepsia, flatulence, loss of appetite, nausea


GU: Urinary retention


RESP: Apnea, cyanosis, dyspnea, respiratory depression


SKIN: Injection site reactions, pallor, pruritus, rash, sweating, urticaria 

Patient And Carer Advice: