Pharmacodynamics and pharmacokinetics of the HMG-CoA reductase inhibitors. Similarities and differences

Clinical Pharmacokinetics
H Lennernäs, G Fager

Abstract

Hypercholesterolaemia plays a crucial role in the development of atherosclerotic diseases in general and coronary heart disease in particular. The risk of progression of the atherosclerotic process to coronary heart disease increases progressively with increasing levels of total serum cholesterol or low density lipoprotein (LDL) cholesterol at both the individual and the population level. The statins are reversible inhibitors of the microsomal enzyme HMG-CoA reductase, which converts HMG-CoA to mevalonate. This is an early rate-limiting step in cholesterol biosynthesis. Inhibition of HMG-CoA reductase by statins decreases intracellular cholesterol biosynthesis, which then leads to transcriptionally upregulated production of microsomal HMG-CoA reductase and cell surface LDL receptors. Subsequently, additional cholesterol is provided to the cell by de novo synthesis and by receptor-mediated uptake of LDL-cholesterol from the blood. This resets intracellular cholesterol homeostasis in extrahepatic tissues, but has little effect on the overall cholesterol balance. There are no simple methods to investigate the concentration-dependent inhibition of HMG-CoA reductase in human pharmacodynamic studies. The main clinical variable is pla...Continue Reading

Associated Clinical Trials

Citations

Mar 29, 2001·Irish Journal of Medical Science·A HeereyA Kelly
Apr 9, 2013·Naunyn-Schmiedeberg's Archives of Pharmacology·Martin WernerMartin Hohenegger
Dec 13, 2005·Analytical and Bioanalytical Chemistry·Biljana Nigović
Apr 4, 2007·Rheumatology International·Karen H CostenbaderElizabeth W Karlson
Dec 10, 2003·Current Atherosclerosis Reports·Paolo Calabro, Edward T H Yeh
May 4, 2012·Molecular Neurobiology·Gunter P EckertWalter E Muller
May 25, 2013·Clinical Pharmacokinetics·Benoit ChauvinAnne-Marie Taburet
Jun 7, 2005·Clinical Immunology : the Official Journal of the Clinical Immunology Society·Hideo Kohka TakahashiMasahiro Nishibori
Feb 28, 2004·Il Farmaco·Kevser KircaliHassan Y Aboul-Enein
Mar 31, 2005·Seminars in Cell & Developmental Biology·Jean E VanceBarbara Karten
Aug 13, 2013·Experimental Cell Research·Fernanda Augusta de Lima Barbosa GuterresSheila Maria Brochado Winnischofer
Oct 5, 2001·The American Journal of Medicine·P H ChongC Franklin
Feb 9, 2000·Pharmacology & Therapeutics·A CorsiniF Bernini
Apr 13, 2000·Pharmacology & Therapeutics·K Nakagawa, T Ishizaki
Sep 5, 2002·International Journal of Cardiology·Jaffar Ali Raza, Assad Movahed
Apr 2, 2003·European Journal of Medicinal Chemistry·Yuan H ZhaoIan Cooper
Oct 12, 2000·Journal of the American College of Cardiology·J S ForresterS Kaul
Mar 13, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Pradeep SharmaRamesh Panchagnula
Nov 27, 2002·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Zhimeng Zhu, Len Neirinck
Aug 9, 2003·Journal of Chromatography. B, Analytical Technologies in the Biomedical and Life Sciences·Sidika ErtürkSevil Müge Cetin
Mar 17, 2001·British Journal of Pharmacology·K BogmanJ Drewe
Mar 22, 2006·The Pharmacogenomics Journal·L M MangraviteR M Krauss
Mar 26, 2004·Proceedings of the National Academy of Sciences of the United States of America·Harutaka KatanoJeffrey I Cohen
Aug 10, 2007·Journal of Toxicology and Environmental Health. Part a·Mathias B Forrester
Feb 22, 2002·Current Opinion in Nephrology and Hypertension·Domenic A Sica, Todd W B Gehr
Jul 14, 2010·The Journal of Trauma·Mary D FogertyAdrian Barbul
May 18, 2010·Alzheimer Disease and Associated Disorders·Alberto Serrano-PozoJohn H Growdon
Jan 5, 2002·The American Journal of Geriatric Cardiology·Domenic A Sica, Todd W B Gehr
May 5, 1999·Fundamental & Clinical Pharmacology·L BecquemontP Jaillon
Apr 28, 2005·International Journal of Clinical Practice·R Y A MukhtarJ P D Reckless

❮ 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.

Carotid Artery Diseases

Carotid artery disease is a group of pathological conditions of the carotid artery. Discover the latest research on carotid artery disease here.

Related Papers

International Journal of Computational Biology and Drug Design
Sergey ShityakovCarola Förster
Molecules : a Journal of Synthetic Chemistry and Natural Product Chemistry
Muhammad SaidMuhammad Rashid Khan
Journal of Advanced Pharmaceutical Technology & Research
Immadisetty Sri KrishnanjaneyuluMittineni Venkata Sunil Kumar
© 2021 Meta ULC. All rights reserved