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Antimicrobial Agents and Chemotherapy, March 1999, p. 568-572, Vol. 43, No. 3
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.

Pharmacokinetics of Ethambutol under Fasting Conditions, with Food, and with Antacids

Charles A. Peloquin,1,2,3,* Amy E. Bulpitt,1 George S. Jaresko,4,5 Roger W. Jelliffe,5,6 James M. Childs,1 and David E. Nix7

Department of Medicine, National Jewish Medical and Research Center,1 and School of Pharmacy2 and School of Medicine,3 University of Colorado, Denver, Colorado; School of Pharmacy,4 Laboratory of Applied Pharmacokinetics,5 and School of Medicine,6 University of Southern California, Los Angeles, California; and College of Pharmacy, University of Arizona, Tucson, Arizona7

Received 12 March 1998/Returned for modification 13 August 1998/Accepted 7 December 1998

Ethambutol (EMB) is the most frequent "fourth drug" used for the empiric treatment of Mycobacterium tuberculosis and a frequently used drug for infections caused by Mycobacterium avium complex. The pharmacokinetics of EMB in serum were studied with 14 healthy males and females in a randomized, four-period crossover study. Subjects ingested single doses of EMB of 25 mg/kg of body weight under fasting conditions twice, with a high-fat meal, and with aluminum-magnesium antacid. Serum was collected for 48 h and assayed by gas chromatography-mass spectrometry. Data were analyzed by noncompartmental methods and by a two-compartment pharmacokinetic model with zero-order absorption and first-order elimination. Both fasting conditions produced similar results: a mean (± standard deviation) EMB maximum concentration of drug in serum (Cmax) of 4.5 ± 1.0 µg/ml, time to maximum concentration of drug in serum (Tmax) of 2.5 ± 0.9 h, and area under the concentration-time curve from 0 h to infinity (AUC0-infinity ) of 28.9 ± 4.7 µg · h/ml. In the presence of antacids, subjects had a mean Cmax of 3.3 ± 0.5 µg/ml, Tmax of 2.9 ± 1.2 h, and AUC0-infinity of 27.5 ± 5.9 µg · h/ml. In the presence of the Food and Drug Administration high-fat meal, subjects had a mean Cmax of 3.8 ± 0.8 µg/ml, Tmax of 3.2 ± 1.3 h, and AUC0-infinity of 29.6 ± 4.7 µg · h/ml. These reductions in Cmax, delays in Tmax, and modest reductions in AUC0-infinity can be avoided by giving EMB on an empty stomach whenever possible.

* Corresponding author. Mailing address: Infectious Disease Pharmacokinetics Laboratory, National Jewish Medical and Research Center, 1400 Jackson St., Denver, CO 80206. Phone: (303) 398-1427. Fax: (303) 270-2229. E-mail: peloquinc{at}njc.org.

Antimicrobial Agents and Chemotherapy, March 1999, p. 568-572, Vol. 43, No. 3
0066-4804/99/$04.00+0
Copyright © 1999, American Society for Microbiology. All rights reserved.


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