Journal Article

The Pharmacokinetic and Pharmacodynamic Profile of Tigecycline

Alison K. Meagher, Paul G. Ambrose, Thaddeus H. Grasela and J. Ellis Grosse

in Clinical Infectious Diseases

Published on behalf of Infectious Diseases Society of America

Volume 41, issue Supplement_5, pages S333-S340
Published in print September 2005 | ISSN: 1058-4838
Published online September 2005 | e-ISSN: 1537-6591 | DOI: https://dx.doi.org/10.1086/431674
The Pharmacokinetic and Pharmacodynamic Profile of Tigecycline

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Tigecycline, a first-in-class expanded-spectrum antimicrobial agent, has demonstrated efficacy in the treatment of complicated intra-abdominal and skin and skin-structure infections. This new antibiotic is available as an intravenous formulation and exhibits linear pharmacokinetics. It is rapidly distributed and has a large volume of distribution, indicating extensive tissue penetration. After a 100-milligram loading dose, followed by 50 milligrams every 12 h, the steady-state maximum concentration in serum after a 1-h infusion is ∼0.6 µg/mL, the 24-h steady-state area under the concentration–time curve is ∼5–6 µg•h/mL, and the terminal elimination half-life is ∼40 h. The major route of elimination of tigecycline is through the feces, primarily as unchanged drug. The pharmacokinetic profile is not affected by severe or end-stage renal disease, nor is it significantly altered by hemodialysis. The pharmacokinetics of tigecycline are also not affected by food, although tolerability is increased if the drug is administered following a meal.

Journal Article.  5273 words.  Illustrated.

Subjects: Infectious Diseases ; Immunology ; Public Health and Epidemiology ; Microbiology

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