Pharmacokinetics and pharmacodynamics of pravastatin alone and with cholestyramine in hypercholesterolemia

Clinical Pharmacology and Therapeutics
H Y PanD Brescia

Abstract

The pharmacokinetics, pharmacodynamics, and safety of pravastatin, a new selective 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitor, were evaluated during monotherapy and with subsequent concomitant cholestyramine therapy in 33 patients with primary hypercholesterolemia in this randomized study. After 4 weeks, pravastatin monotherapy (5 mg, 10 mg, and 20 mg twice daily) significantly decreased total cholesterol by 17% to 24% (p less than 0.001 versus baseline) and low-density lipoprotein cholesterol by 23% to 35% (p less than 0.001). High-density lipoprotein cholesterol increased by 8% to 9%, and triglycerides decreased by 6% to 9%. The area under the serum concentration-time curve and maximum serum concentration of pravastatin showed dose-proportionality; time to maximum serum concentration and serum elimination half-life were independent of dose. When added to pravastatin therapy, cholestyramine enhanced the lipid-lowering effects of pravastatin. After 4 weeks of combination therapy, total cholesterol was reduced by 32% to 38% (p less than 0.001 versus baseline), and low-density lipoprotein cholesterol was reduced by 47% to 56% (p less than 0.001). High-density lipoprotein cholesterol increased by 11% to 18% (p less ...Continue Reading

Citations

Feb 1, 1995·Journal of Clinical Pharmacology·J TriscariH Y Pan
Jun 13, 1998·European Journal of Drug Metabolism and Pharmacokinetics·S SigurbjörnssonG Sigurdsson
Aug 7, 2001·Current Atherosclerosis Reports·T A Jacobson
Apr 27, 2002·Heart Disease·N N Wong
May 31, 2002·Clinical Pharmacokinetics·David Williams, John Feely
Jul 16, 2008·Vascular and Endovascular Surgery·Russell H Samson
Mar 5, 2017·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Keith RiccardiLi Di
Jul 28, 2019·Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry·Lee M TathamAndrew Owen
May 23, 2007·Clinical Drug Investigation·Heleen E WiersmaChris J van Boxtel
Nov 9, 2019·Drug Metabolism and Disposition : the Biological Fate of Chemicals·Christine M BowmanJialin Mao
Feb 1, 1992·Journal of Clinical Pharmacology·C E HalstensonH Pan
Feb 1, 1992·Journal of Clinical Pharmacology·P J PentikainenJ D Rogers
Apr 3, 2015·Journal of Atherosclerosis and Thrombosis·Rong DaiFan Zhang
Apr 3, 2020·The Journal of Antimicrobial Chemotherapy·Perrine CourletUNKNOWN Swiss HIV Cohort Study
Sep 1, 1993·British Journal of Clinical Pharmacology·J TriscariH Y Pan
Oct 29, 2004·Clinical Pharmacokinetics·Michael R JonesPhilip Mathew
Jul 31, 2020·Expert Opinion on Drug Metabolism & Toxicology·Takeshi HirotaIchiro Ieiri
Aug 18, 2009·Fundamental & Clinical Pharmacology·Zeljko Reiner
Sep 15, 2006·Seminars in Dialysis·Jia LiuMitchell H Rosner
Mar 16, 2002·The Annals of Pharmacotherapy·Joanne M DonovanSteven K Burke
Feb 9, 2000·Pharmacology & Therapeutics·A CorsiniF Bernini
Aug 1, 1994·Disease-a-month : DM·R S RosensonC C Tangney
Nov 21, 2017·ACS Chemical Neuroscience·Jeffrey J SutherlandTimothy P Ryan
Feb 17, 2009·Endocrinology and Metabolism Clinics of North America·Runhua Hou, Anne Carol Goldberg

❮ Previous
Next ❯

Related Concepts

Related Feeds

ApoE, Lipids & Cholesterol

Serum cholesterol, triglycerides, apolipoprotein B (APOB)-containing lipoproteins (very low-density lipoprotein (VLDL), immediate-density lipoprotein (IDL), and low-density lipoprotein (LDL), lipoprotein A (LPA)) and the total cholesterol/high-density lipoprotein (HDL) cholesterol ratio are all connected in diseases. Here is the latest research.