The efficacy and safety of bile Acid binding agents, opioid antagonists, or rifampin in the treatment of cholestasis-associated pruritus

Am J Gastroenterol. 2007 Jul;102(7):1528-36. doi: 10.1111/j.1572-0241.2007.01200.x. Epub 2007 Mar 31.


Objectives: The objective of this review was to evaluate the efficacy and safety of rifampin, opioid antagonists, or bile acid binding agents in the treatment of cholestasis-related pruritus (CAP) from available randomized controlled trial evidence.

Methods: In addition to a comprehensive gray literature search, the Cochrane Library, MEDLINE, EMBASE, PubMed, and Web of Science were searched. Only full-text RCTs in participants (>75% adult) with CAP on at least one of the three medications were included. The primary outcome was change in pruritus score, recorded as a continuous or dichotomous outcome. Two independent reviewers performed trial selection and quality assessment.

Results: From 487 citations, 12 RCTs were included. Rifampin (standardized mean difference [SMD]-1.62, 95% CI -3.05 to -0.18) and opioid antagonists (SMD -0.68, 95% CI -1.19 to -0.17) significantly reduced CAP. The two cholestyramine studies were too heterogeneous to pool. Although cholestyramine (P= 0.35) and rifampin (P= 0.96) were not associated with greater side effects compared with placebo, opioid antagonists were (number needed to harm = 2.6, 95% CI 1.4-25).

Conclusions: The available RCTs are small, few in number, and use varying scales for measuring pruritus. Although both opioid antagonists and rifampin demonstrated a reduction in pruritus, there were insufficient data to judge the efficacy of cholestyramine. Opioid antagonists were associated with transient side effects in a significant proportion of patients. A longer well-designed randomized controlled trial is needed to confirm the efficacy of bile acid binding agents and accurately assess adverse events.

Publication types

  • Review

MeSH terms

  • Anticholesteremic Agents / therapeutic use
  • Cholestasis / complications*
  • Cholestyramine Resin / therapeutic use*
  • Humans
  • Leprostatic Agents / therapeutic use*
  • Narcotic Antagonists / therapeutic use*
  • Pruritus / drug therapy*
  • Pruritus / etiology
  • Randomized Controlled Trials as Topic
  • Rifampin / therapeutic use*
  • Treatment Outcome


  • Anticholesteremic Agents
  • Leprostatic Agents
  • Narcotic Antagonists
  • Cholestyramine Resin
  • Rifampin