Thalidomide pharmacokinetics do not change with chronic administration

S. R. Donahue, J. M. Collins, D. A. Flockhart, D. R. Abernethy, C. B. Trapnell

Research output: Contribution to journalArticle

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Abstract

Thalidomide, an investigationl drug with immunomodulatory as well as teratogenic properties, is currently being evaluated for several clinical uses. Thalidomide-related compounds may be inducers of cytochrome P450 and could alter their own metabolism. Therefore, we evaluated thalidomide pharmacokinetics after initial and chronic dosing. Seven healthy surgically sterilized female subjects aged 21-45 received oral thalidomide 200 mg daily for 21 days. Plasma thalidomide concentrations were determined by HPLC on study days 1 and 21. The calculated pharmacokinetic parameters are summarized below: Study Day AUC (μ·ml-1-hr) t1/2 (hr) Cloral(1/hr) Cmax (μg·ml-1) tmax (hr) Day 1 33.0 ± 10.1 7.0 ±2.0 6.1 ±1.1 2.9 ±1.0 6.4 ±2.6 Day 21 40.6 ±18.5 7.3 ±2.7 4.9 ±1.5 3.7 ±1.2 5.9 ±3.1 (Values shown are mean±S.D.) In addition, the accumulation ratio (Day 21 AUC0-24/Day 1 AUC0→∞) was 1.2 ±0.4. None of the calculated parameters were different as determined by paired t-tests. We conclude that the pharmacokinetics of thalidomide do not change with three weeks of chronic dosing.

Original languageEnglish
Pages (from-to)236
Number of pages1
JournalClinical Pharmacology and Therapeutics
Volume61
Issue number2
StatePublished - 1997

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Thalidomide
Pharmacokinetics
Cytochrome P-450 Enzyme System
Area Under Curve
High Pressure Liquid Chromatography
Pharmaceutical Preparations

ASJC Scopus subject areas

  • Pharmacology

Cite this

Donahue, S. R., Collins, J. M., Flockhart, D. A., Abernethy, D. R., & Trapnell, C. B. (1997). Thalidomide pharmacokinetics do not change with chronic administration. Clinical Pharmacology and Therapeutics, 61(2), 236.

Thalidomide pharmacokinetics do not change with chronic administration. / Donahue, S. R.; Collins, J. M.; Flockhart, D. A.; Abernethy, D. R.; Trapnell, C. B.

In: Clinical Pharmacology and Therapeutics, Vol. 61, No. 2, 1997, p. 236.

Research output: Contribution to journalArticle

Donahue, SR, Collins, JM, Flockhart, DA, Abernethy, DR & Trapnell, CB 1997, 'Thalidomide pharmacokinetics do not change with chronic administration', Clinical Pharmacology and Therapeutics, vol. 61, no. 2, pp. 236.
Donahue SR, Collins JM, Flockhart DA, Abernethy DR, Trapnell CB. Thalidomide pharmacokinetics do not change with chronic administration. Clinical Pharmacology and Therapeutics. 1997;61(2):236.
Donahue, S. R. ; Collins, J. M. ; Flockhart, D. A. ; Abernethy, D. R. ; Trapnell, C. B. / Thalidomide pharmacokinetics do not change with chronic administration. In: Clinical Pharmacology and Therapeutics. 1997 ; Vol. 61, No. 2. pp. 236.
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