Rifampin reduces plasma concentrations and effects of zolpidem

Clinical Pharmacology and Therapeutics
K VillikkaPertti J Neuvonen

Abstract

Zolpidem is a short-acting imidazopyridine hypnotic drug that is metabolized mainly by CYP3A4. Rifampin (INN, rifampicin) is a potent inducer of many cytochrome P450 enzymes, and it greatly reduces the plasma concentrations and effects of, for example, midazolam, triazolam, and zopiclone. In this study, the effects of rifampin on the pharmacokinetics and pharmacodynamics of zolpidem were studied. In a randomized crossover study with two phases and a washout of 4 weeks, eight young healthy female volunteers took either 600 mg rifampin or placebo once a day for 5 days. On day 6, 20 mg zolpidem was administered orally. Plasma concentrations and effects of zolpidem were measured up to 10 hours. The total area under the plasma zolpidem concentration-time curve after administration of rifampin was 27% of that after administration of placebo (336 +/- 67 versus 1202 +/- 157 ng.hr/ml [mean value +/- SEM; p < 0.01]). Rifampin decreased the peak plasma concentration of zolpidem by 58%, that is, from 293 +/- 61 to 117 +/- 25 ng/ml (p < 0.01) and the elimination half-life from 2.5 +/- 0.2 to 1.6 +/- 0.1 hours (p < 0.01). A significant (p < 0.05) reduction in the effects of zolpidem was seen in all six pharmacodynamic tests after rifampin pr...Continue Reading

References

Nov 1, 1992·The Journal of Clinical Investigation·J C KolarsP B Watkins
Jan 1, 1992·Clinical Pharmacokinetics·K Venkatesan
Aug 1, 1987·Clinical Pharmacology and Therapeutics·E E OhnhausH Habicht
Jan 1, 1984·British Journal of Clinical Pharmacology·A N GriffithsA Richens
Sep 1, 1995·Clinical Pharmacokinetics·P Salvà, J Costa
Jan 1, 1996·Clinical Pharmacology and Therapeutics·J T BackmanP J Neuvonen
Jan 12, 1996·Journal of Chromatography. B, Biomedical Applications·F StankeG Bessard
Jan 1, 1997·Clinical Pharmacology and Therapeutics·K VillikkaP J Neuvonen
May 1, 1997·British Journal of Clinical Pharmacology·K VillikkaP J Neuvonen

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Citations

Feb 9, 2011·European Journal of Drug Metabolism and Pharmacokinetics·Laurian VlaseSorin E Leucuţa
Feb 18, 2003·American Journal of Respiratory and Critical Care Medicine·Henry M BlumbergUNKNOWN American Thoracic Society, Centers for Disease Control and Prevention and the Infectious Diseases Society
Sep 25, 2015·Neurology·Raoul SutterSarah Tschudin-Sutter
May 9, 2002·Drug Metabolism Reviews·Slobodan Rendic
Mar 20, 2012·Expert Opinion on Pharmacotherapy·David J Greenblatt, Thomas Roth
Mar 31, 2016·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Lisa M AlmondJane R Kenny
May 1, 2010·Expert Opinion on Drug Discovery·Masashi HonmaHiroshi Suzuki
Nov 29, 2001·The Annals of Pharmacotherapy·S E Lenhart, D J Buysse
Nov 26, 2010·Journal of Clinical Pharmacology·Laurian VlaseSorin E Leucuţa
Feb 1, 2000·Journal of Clinical Psychopharmacology·J S Markowitz, C L DeVane
Dec 17, 2009·European Journal of Clinical Pharmacology·Thomas M PolasekJohn O Miners
May 20, 2003·CNS Drugs·Leah M HesseDavid J Greenblatt
Mar 13, 2002·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·W W Yew
Jul 29, 2003·Clinical Pharmacokinetics·Mikko NiemiKari T Kivistö
May 1, 2008·Drug Metabolism and Pharmacokinetics·Motohiro Kato
Jun 19, 2012·Current Psychiatry Reports·Brett A EnglishStanford Jhee
Mar 29, 2011·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Yang XuGary L Skiles
Aug 2, 2008·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Magang ShouGary L Skiles
Aug 13, 2009·Drug Safety : an International Journal of Medical Toxicology and Drug Experience·Gary Zammit
Feb 22, 2012·Basic & Clinical Pharmacology & Toxicology·Pertti J Neuvonen
Jun 26, 1999·British Journal of Clinical Pharmacology·L L Von MoltkeR I Shader
Oct 12, 2011·Clinical and Experimental Pharmacology & Physiology·Laurian VlaseSorin Emilian Leucuţa
Dec 1, 1998·CNS Drug Reviews·David J Sanger, Henri Depoortere
Mar 10, 2021·CPT: Pharmacometrics & Systems Pharmacology·Kun WangYing C Ou
Jul 7, 2021·Antimicrobial Agents and Chemotherapy·Vianney TuloupSylvain Goutelle

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