Document Detail

Pharmacokinetics of rifampin under fasting conditions, with food, and with antacids.
MedLine Citation:
PMID:  9925057     Owner:  NLM     Status:  MEDLINE    
STUDY OBJECTIVES: Determine the intrasubject and intersubject variability in, and the effects of food or antacids on, the pharmacokinetics of rifampin (RIF). DESIGN: Randomized, four-period crossover phase I study. SUBJECTS: Fourteen healthy male and female volunteers. INTERVENTIONS: Subjects ingested single doses of RIF, 600 mg, under fasting conditions twice, with a high-fat meal, and with aluminum-magnesium antacid. They also received standard doses of isoniazid, pyrazinamide, and ethambutol. MEASUREMENTS AND MAIN RESULTS: Serum was collected for 48 h and assayed by high-pressure liquid chromatography. Data were analyzed using noncompartmental methods and a compartmental analysis using nonparametric expectation maximization. Both fasting conditions produced similar results: a mean RIF maximal serum concentration (Cmax) of 10.54+/-3.18 microg/mL, the time at which it occurred (Tmax) of 2.42+/-1.32 h, and the area under the curve from time zero to infinity (AUC0-infinity) of 57.15+/-13.41 microg x h/mL. These findings are similar to those reported previously. Antacids did not alter these parameters (Cmax of 10.89+/-5.22 microg/mL, Tmax of 2.36+/-1.28 h, and AUC0-infinity of 58.37+/-18.49 microg x h/mL). In contrast, the Food and Drug Administration high-fat meal reduced RIF Cmax by 36% (7.27+/-2.29 microg/mL), nearly doubled Tmax (4.43+/-1.09 h), but reduced AUC0-infinity by only 6% (55.20+/-14.48 microg x h/mL). CONCLUSIONS: These changes in Cmax, Tmax, and AUC0-infinity can be avoided by giving RIF on an empty stomach whenever possible.
C A Peloquin; R Namdar; M D Singleton; D E Nix
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Publication Detail:
Type:  Clinical Trial; Clinical Trial, Phase I; Journal Article; Randomized Controlled Trial; Research Support, U.S. Gov't, P.H.S.    
Journal Detail:
Title:  Chest     Volume:  115     ISSN:  0012-3692     ISO Abbreviation:  Chest     Publication Date:  1999 Jan 
Date Detail:
Created Date:  1999-02-05     Completed Date:  1999-02-05     Revised Date:  2007-11-14    
Medline Journal Info:
Nlm Unique ID:  0231335     Medline TA:  Chest     Country:  UNITED STATES    
Other Details:
Languages:  eng     Pagination:  12-8     Citation Subset:  AIM; IM    
Department of Medicine, National Jewish Medical and Research Center, School of Pharmacy, University of Colorado, Denver 80206, USA.
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MeSH Terms
Antacids / administration & dosage*
Antibiotics, Antitubercular / administration & dosage,  pharmacokinetics*
Cross-Over Studies
Drug Interactions
Drug Therapy, Combination
Fasting / physiology*
Food-Drug Interactions / physiology*
Metabolic Clearance Rate / physiology
Rifampin / administration & dosage,  pharmacokinetics*
Grant Support
Reg. No./Substance:
0/Antacids; 0/Antibiotics, Antitubercular; 13292-46-1/Rifampin
Erratum In:
Chest 1999 May;115(5):1485

From MEDLINE®/PubMed®, a database of the U.S. National Library of Medicine

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