Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids

Charles A. Peloquin, Amy E. Bulpitt, George S. Jaresko, Roger W. Jelliffe, James M. Childs, David E. Nix

Research output: Contribution to journalArticle

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Abstract

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 (C(max)) of 4.5 ± 1.0 μg/ml, time to maximum concentration of drug in serum (T(max)) of 2.5 ± 0.9 h, and area under the concentration-time curve from 0 h to infinity (AUC(0-∞)) of 28.9 ± 4.7 μg · h/ml. In the presence of antacids, subjects had a mean C(max) of 3.3 ± 0.5 μg/ml, T(max) of 2.9 ± 1.2 h, and AUC(0-∞) of 27.5 ± 5.9 μg · h/ml. In the presence of the Food and Drug Administration high-fat meal, subjects had a mean C(max) of 3.8 ± 0.8 μg/ml, T(max) of 3.2 ± 1.3 h, and AUC(0- ∞) of 29.6 ± 4.7 μg · h/ml. These reductions in C(max), delays in T(max), and modest reductions in AUC(0-∞) can be avoided by giving EMB on an empty stomach whenever possible.

Original languageEnglish (US)
Pages (from-to)568-572
Number of pages5
JournalAntimicrobial Agents and Chemotherapy
Volume43
Issue number3
StatePublished - Mar 1999

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Ethambutol
Antacids
Fasting
Pharmacokinetics
Area Under Curve
Food
Serum
Pharmaceutical Preparations
Meals
Fats
Mycobacterium avium Complex
United States Food and Drug Administration
Aluminum
Mycobacterium tuberculosis
Gas Chromatography-Mass Spectrometry
Cross-Over Studies
Magnesium
Stomach
Body Weight
Infection

ASJC Scopus subject areas

  • Pharmacology (medical)

Cite this

Peloquin, C. A., Bulpitt, A. E., Jaresko, G. S., Jelliffe, R. W., Childs, J. M., & Nix, D. E. (1999). Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids. Antimicrobial Agents and Chemotherapy, 43(3), 568-572.

Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids. / Peloquin, Charles A.; Bulpitt, Amy E.; Jaresko, George S.; Jelliffe, Roger W.; Childs, James M.; Nix, David E.

In: Antimicrobial Agents and Chemotherapy, Vol. 43, No. 3, 03.1999, p. 568-572.

Research output: Contribution to journalArticle

Peloquin, CA, Bulpitt, AE, Jaresko, GS, Jelliffe, RW, Childs, JM & Nix, DE 1999, 'Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids', Antimicrobial Agents and Chemotherapy, vol. 43, no. 3, pp. 568-572.
Peloquin CA, Bulpitt AE, Jaresko GS, Jelliffe RW, Childs JM, Nix DE. Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids. Antimicrobial Agents and Chemotherapy. 1999 Mar;43(3):568-572.
Peloquin, Charles A. ; Bulpitt, Amy E. ; Jaresko, George S. ; Jelliffe, Roger W. ; Childs, James M. ; Nix, David E. / Pharmacokinetics of ethambutol under fasting conditions, with food, and with antacids. In: Antimicrobial Agents and Chemotherapy. 1999 ; Vol. 43, No. 3. pp. 568-572.
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