Single- and multiple-dose pharmacokinetics of pioglitazone in adolescents with type 2 diabetes

Michael Christensen, Bernd Meibohm, Edmund V. Capparelli, Pedro Velasquez-Mieyer, George A. Burghen, William V. Tamborlane

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Abstract

This study assessed the single- and multiple-dose pharmacokinetics of 3 doses (15 mg, 30 mg, and 45 mg) of pioglitazone in 36 adolescents with type 2 diabetes. Blood samples were obtained over a 48-hour interval after the first dose (day 1) and over a 72-hour interval after the last dose (day 15) of pioglitazone and were assayed for pioglitazone and active metabolites (M-III and M-IV). Pioglitazone systemic exposure increased dose dependently but was less than dose proportional during multiple dosing. The median peak pioglitazone concentration occurred at 2 hours. The mean half-life was 8 to 9 hours for pioglitazone and 24 to 32 hours for M-III and M-IV, with similar values at each dose level. During multiple dosing, accumulation for pioglitazone was negligible, but it reached 2.5- to 3.0-fold for M-III and M-IV. The sustained total serum concentration of active compounds during multiple dosing provides the basis for once-daily dose administration of pioglitazone in adolescents.

Original languageEnglish (US)
Pages (from-to)1137-1144
Number of pages8
JournalJournal of Clinical Pharmacology
Volume45
Issue number10
DOIs
StatePublished - Oct 1 2005

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pioglitazone
Type 2 Diabetes Mellitus
Pharmacokinetics

All Science Journal Classification (ASJC) codes

  • Pharmacology
  • Pharmacology (medical)

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Single- and multiple-dose pharmacokinetics of pioglitazone in adolescents with type 2 diabetes. / Christensen, Michael; Meibohm, Bernd; Capparelli, Edmund V.; Velasquez-Mieyer, Pedro; Burghen, George A.; Tamborlane, William V.

In: Journal of Clinical Pharmacology, Vol. 45, No. 10, 01.10.2005, p. 1137-1144.

Research output: Contribution to journalArticle

Christensen, Michael ; Meibohm, Bernd ; Capparelli, Edmund V. ; Velasquez-Mieyer, Pedro ; Burghen, George A. ; Tamborlane, William V. / Single- and multiple-dose pharmacokinetics of pioglitazone in adolescents with type 2 diabetes. In: Journal of Clinical Pharmacology. 2005 ; Vol. 45, No. 10. pp. 1137-1144.
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