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Chest. 1999 Jan;115(1):12-8.

Pharmacokinetics of rifampin under fasting conditions, with food, and with antacids.

Author information

1
Department of Medicine, National Jewish Medical and Research Center, School of Pharmacy, University of Colorado, Denver 80206, USA. peloquinc@njc.org

Erratum in

  • Chest 1999 May;115(5):1485.

Abstract

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.

PMID:
9925057
DOI:
10.1378/chest.115.1.12
[Indexed for MEDLINE]

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