European Journal of Clinical Pharmacology

, Volume 11, Issue 4, pp 287–293 | Cite as

Stimulation of drug metabolism by rifampicin in patients with cirrhosis or cholestasis measured by increased hexobarbital and tolbutamide clearance

  • W. Zilly
  • D. D. Breimer
  • E. Richter


Eleven patients with hepatic cirrhosis or cholestasis were treated with rifampicin for 7 to 132 days. Ten patients received hexobarbital (7.32 mg/kg) and five received tolbutamide (20 mg/kg) by i.v. infusion prior to and after rifampicin treatment; plasma concentrations of the two test compounds were determined during and after infusion. The average elimination half-life of hexobarbital had decreased from 624 to 262 min and that of tolbutamide from 292 to 160 min following rifampicin treatment. It was calculated that the metabolic clearance of hexobarbital had increased more than two-fold and that of tolbutamide almost two-fold. The results suggest that rifampicin is able to stimulate hepatic drug metabolism in patients with liver disease. It was apparent in general that the induction did not lead to improvement of hepatocellular function during disease as judged by laboratory findings.

Key words

Rifampicin induction of drug metabolism cirrhosis cholestasis hexobarbital kinetics tolbutamide kinetics plasma concentrations 


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Copyright information

© Springer-Verlag 1977

Authors and Affiliations

  • W. Zilly
    • 1
  • D. D. Breimer
    • 2
  • E. Richter
    • 1
  1. 1.Department of Internal MedicineUniversity of WürzburgGermany
  2. 2.Department of Pharmacology, Subfaculty of PharmacyUniversity of LeidenThe Netherlands

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