Buprenorphine 0.4, 2, 8mg

Introduction

Buprenorphine is an Agonist-Antagonist Opioid analgesic that displays high binding affinity but low intrinsic activity at the µ receptor. It functions as an antagonist at the δ and κ receptors and for this reason is referred to as a "mixed agonist-antagonist." Although buprenorphine is used as an analgesic, it can antagonize the action of more potent µ agonists such as morphine

Indication


Treatment of Opioid dependence and control of moderate to severe pain.

Pharmacokinetics

Bioavailability: 30%
Bound to plasma proteins: 96%
Metabolism: metabolism takes place in the liver by oxidation via the cytochrome P450 isoenzyme CYP3A4 to the pharmacologically active metabolite N-dealkylbuprenorphine (norbuprenorphine), and by conjugation to glucuronide metabolites.
Half-life of Elimination: 37 hours
Pharmacodynamics
  • Contra-indications:
Hypersensitivity to buprenorphine or to any of the excipients, severe respiratory insufficiency, severe hepatic insufficiency, acute alcoholism or delirium tremens
  • Cautions:
This product should be used with caution in patients with:
  • Asthma or respiratory insufficiency (cases of respiratory depression have been reported with buprenorphine.
  • Renal insufficiency (30% of the administered dose is eliminated by the renal route, thus renal elimination may be prolonged).
  • Hepatic insufficiency, hepatic metabolism of buprenorphine may be altered- Head injuries.
  • Increased intracranial pressure
  • Hypotension
  • Prostatic hypertrophy
  • Urethral stenosis
  • This medicinal product contains lactose. Patients with rare hereditary problems of galactose intolerance, the Lapp lactase deficiency or glucose-galactose mal absorption should not take this medicine.
  • The tablet should not be swallowed, crushed or chewed.

Side-effects:

Buprenorphine can cause drowsiness, dizziness, headache, hypotention, miosis, nausea and sweat. Increased intracranial pressure and respiratory depression. Other side effects include: confusion, anxiety, blurred vision, bradycardia, tachycardia, hypotension, constipation, urinary retention, hypoventilation and itching.

Dosage

Faran Shimi pharmaceutical Co. manufacture 3 dose of Buprenorphine: 0.4, 2 and 8 mg as Sublingual Tablet.
Moderate to severe pain by sublingual administration: 0.2-0.4mg every 6-8 hours.
For CHILD: over 6 years, 16-25 Kg, 0.1mg every 6-8 hours
25-37.5 Kg, 0.1-0.2mg every 6-8 hours
37.5-50 Kg, 0.2-0.3 mg every 6-8 hours

Advantages

  • Buprenorphine is effective in reducing the pain and discomfort of opioid withdrawals as well as the cravings associated with withdrawals.
  • Buprenorphine is also easier to use than methadone as each dose is longer lasting and can be taken at home.