التفاصيل البيبلوغرافية
| العنوان: |
Safety, Tolerability, and Pharmacokinetics of Raltegravir After Single and Multiple Doses in Healthy Subjects. |
| المؤلفون: |
Iwamoto, M., Wenning, L. A., Petry, A. S., Laethem, M., De Smet, M., Kost, J. T., Merschman, S. A., Strohmaier, K. M., Ramael, S., Lasseter, K. C., Stone, J. A., Gottesdiener, K. M., Wagner, J. A. |
| المصدر: |
Clinical Pharmacology & Therapeutics; Feb2008, Vol. 83 Issue 2, p293-299, 7p, 1 Diagram, 3 Charts, 2 Graphs |
| مصطلحات موضوعية: |
HIV, PHARMACOKINETICS, THERAPEUTICS, CHEMICAL kinetics, PHARMACOLOGY |
| مستخلص: |
Raltegravir is a novel human immunodeficiency virus-1 integrase inhibitor with potent in vitro activity (95% inhibitory concentration (IC95)=33 nM in 50% human serum). Three double-blind, randomized, placebo-controlled, pharmacokinetic, safety, and tolerability studies were conducted: (1) single-dose escalation study (10–1,600 mg), (2) multiple-dose escalation study (100–800 mg q12 h×10 days), and (3) single-dose female study (400 mg). Raltegravir was rapidly absorbed with a terminal half-life (t½) ∼7–12 h. Approximately 7–14% of raltegravir was excreted unchanged in urine. Area under the curve (AUC)0–∞ was similar between male and female subjects. After multiple-dose administration, steady state was achieved within 2 days; there was little to modest accumulation of raltegravir. Trough levels were >33 nM for dose levels of 100 mg and greater. Raltegravir is generally well tolerated at doses of up to 1,600 mg/day given for up to 10 days and exhibits a pharmacokinetic profile supportive of twice-daily dosing with multiple doses of 100 mg and greater achieving trough levels >33 nM.Clinical Pharmacology & Therapeutics (2008) doi:10.1038/sj.clpt.6100281 [ABSTRACT FROM AUTHOR] |
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| قاعدة البيانات: |
Complementary Index |