Buprenorphine: how to use it right

Drug Alcohol Depend. 2003 May 21;70(2 Suppl):S59-77. doi: 10.1016/s0376-8716(03)00060-7.


The unique pharmacology of buprenorphine at the mu-opioid receptor (i.e. high affinity, low intrinsic activity and slow dissociation) results in buprenorphine having: (1) a good safety profile, (2) low physical dependence, and (3) flexibility in dose scheduling. Early studies assessed the effectiveness of buprenorphine for the treatment of opioid dependence using a sublingual solution formulation. More recently, a combination tablet (buprenorphine/naloxone in a 4:1 ratio) has been assessed with the goal of decreasing diversion and abuse. Controlled studies with buprenorphine solution, buprenorphine mono-tablet, and buprenorphine/naloxone combination tablet have uniformly demonstrated the effectiveness of buprenorphine for opioid dependence treatment and the combination tablet appears to decrease (but not eliminate) abuse potential. There is general agreement across studies regarding buprenorphine induction and maintenance dose schedules. The clinical effects of buprenorphine and buprenorphine/naloxone are similar and most patients can be treated initially with and maintained on a daily buprenorphine/naloxone dose of 4:1-24:6 mg. Dosing is possible on a less-than-daily schedule; however, multiples of the daily-dose should be administered to cover the increased interval between doses. If buprenorphine withdrawal is indicated, gradual dose reduction is recommended over a rapid dose reduction or abrupt cessation. Both tablet formulations are approved by the US FDA for opioid dependence treatment as Schedule III narcotics and are, therefore, available for use in office-based practice. The buprenorphine plus naloxone combination product should provide additional safeguards for use in office-based practice by decreasing risk of diversion, and office-based treatment should expand the availability of services to opioid dependent patients.

Publication types

  • Research Support, N.I.H., Extramural
  • Review

MeSH terms

  • Buprenorphine / administration & dosage*
  • Buprenorphine / adverse effects
  • Buprenorphine / pharmacokinetics
  • Clinical Trials as Topic / methods
  • Dosage Forms
  • Drug Administration Routes
  • Drug Combinations
  • Humans
  • Narcotic Antagonists / administration & dosage*
  • Narcotic Antagonists / adverse effects
  • Narcotic Antagonists / pharmacokinetics
  • Opioid-Related Disorders / drug therapy
  • Opioid-Related Disorders / metabolism


  • Dosage Forms
  • Drug Combinations
  • Narcotic Antagonists
  • Buprenorphine