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Drug Metabolism & Disposition

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Research ArticleArticle

Disposition and Biotransformation of the Antiretroviral Drug Nevirapine in Humans

Paul Riska, Michael Lamson, Thomas MacGregor, John Sabo, Susan Hattox, Joseph Pav and James Keirns
Drug Metabolism and Disposition August 1999, 27 (8) 895-901;
Paul Riska
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Michael Lamson
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Thomas MacGregor
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John Sabo
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Susan Hattox
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Joseph Pav
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James Keirns
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Abstract

The pharmacokinetics and biotransformation of the antiretroviral agent nevirapine (NVP) after autoinduction were characterized in eight healthy male volunteers. Subjects received 200-mg NVP tablets once daily for 2 weeks, followed by 200 mg twice daily for 2 weeks. Then they received a single oral dose (solution) of 50 mg containing 100 μCi of [14C]NVP. Biological fluids were analyzed for total radioactivity, parent compound (HPLC/UV), and metabolites (electrospray liquid chromatography/mass spectroscopy and liquid chromatography/tandem mass spectroscopy). Mean recovery of radioactivity was 91.4%, with 81.3% excreted in urine and 10.1% recovered in the feces over a period of 10 days. Circulating radioactivity was evenly distributed between whole blood and plasma. At maximum plasma concentration, parent compound accounted for ∼75% of the circulating radioactivity. Mean plasma elimination half-lives for total radioactivity and NVP were 21.3 and 20.0 h, respectively. Several metabolites were identified in urine including 2-hydroxynevirapine glucuronide (18.6%), 3-hydroxynevirapine glucuronide (25.7%), 12-hydroxynevirapine glucuronide (23.7%), 8-hydroxynevirapine glucuronide (1.3%), 3-hydroxynevirapine (1.2%), 12-hydroxynevirapine (0.6%), and 4-carboxynevirapine (2.4%). Greater than 80% of the radioactivity in urine was made up of glucuronidated conjugates of hydroxylated metabolites of NVP. Thus, cytochrome P-450 metabolism, glucuronide conjugation, and urinary excretion of glucuronidated metabolites represent the primary route of NVP biotransformation and elimination in humans. Only a small fraction of the dose (2.7%) was excreted in urine as parent compound.

Footnotes

  • Send reprint requests to: Paul Riska, Ph.D., Department of Drug Metabolism and Pharmacokinetics, Boehringer Ingelheim Pharmaceuticals, Inc., 900 Ridgebury Rd., Ridgefield, CT 06877. E-mail:priska{at}rdg.boehringer-ingelheim.com

  • Abbreviations used are::
    NVP
    nevirapine
    SPE
    solid phase extraction
    LC/MS
    liquid chromatography/mass spectroscopy
    LC/MS/MS
    LC/tandem mass spectroscopy
    CYP
    cytochrome P-450
    • Received November 5, 1998.
    • Accepted April 27, 1999.
  • The American Society for Pharmacology and Experimental Therapeutics
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Drug Metabolism and Disposition: 27 (8)
Drug Metabolism and Disposition
Vol. 27, Issue 8
1 Aug 1999
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Research ArticleArticle

Disposition and Biotransformation of the Antiretroviral Drug Nevirapine in Humans

Paul Riska, Michael Lamson, Thomas MacGregor, John Sabo, Susan Hattox, Joseph Pav and James Keirns
Drug Metabolism and Disposition August 1, 1999, 27 (8) 895-901;

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Research ArticleArticle

Disposition and Biotransformation of the Antiretroviral Drug Nevirapine in Humans

Paul Riska, Michael Lamson, Thomas MacGregor, John Sabo, Susan Hattox, Joseph Pav and James Keirns
Drug Metabolism and Disposition August 1, 1999, 27 (8) 895-901;
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