PMID: 2126139Sep 1, 1990Paper

Pharmacology and mechanism of action of the new HMG-CoA reductase inhibitors

Pharmacological Research : the Official Journal of the Italian Pharmacological Society
C R Sirtori

Abstract

The new inhibitors of hydroxymethylglutaryl coenzyme A (HMG-CoA) reductase are synthetic compounds, of fungal origin, inhibiting a key and unidirectional enzyme in the sterol biosynthetic pathway. Lovastatin, simvastatin and pravastatin, currently available, differ, to some extent: lovastatin and simvastatin are inactive pro-drugs, undergoing conversion by the liver, most of their metabolites active. Pravastatin is instead active per se with mostly inactive metabolites. Distribution of the drugs and of their metabolites in different tissues, also depending upon the relative inhibitory activity, may result in different cholesterol lowering potency as well as in, eventually, some tissue selectivity. Otherwise, the plasma kinetics of the three agents is rather short, usually with a progressive decay of activity within 24 h from administration. Enzyme inhibition results in the upregulation of high affinity receptors for low density lipoproteins (LDL), whose clearance is markedly raised after treatment. Otherwise, HMG-CoA reductase inhibitors do not affect to a significant extent the levels and/or composition of the other major lipoprotein fractions.

Citations

Nov 1, 1993·Cardiovascular Drugs and Therapy·C R Sirtori, S Colli
Jun 5, 2008·Cancer Immunology, Immunotherapy : CII·J E FildesN Yonan
Mar 25, 2014·Pharmacological Research : the Official Journal of the Italian Pharmacological Society·Cesare R Sirtori
Dec 19, 2015·Expert Review of Cardiovascular Therapy·Joost Besseling, Barbara A Hutten
Nov 1, 1995·The American Journal of the Medical Sciences·H SasakiN Tada
Sep 12, 1991·Biochemical Pharmacology·B C SallustioR Zacest
Dec 9, 2009·Expert Opinion on Drug Safety·Fabrizio MontecuccoFrançois Mach
Nov 6, 1998·FEBS Letters·D C LambS L Kelly
May 23, 2012·Journal of Cardiovascular Medicine·Bing DuLing Qin
Jan 4, 2020·Diabetes Therapy : Research, Treatment and Education of Diabetes and Related Disorders·Tsvetalina TankovaReneta Petkova
Jan 21, 1993·International Journal of Cancer. Journal International Du Cancer·A C MillerD Samid
Aug 11, 2001·Drug Resistance Updates : Reviews and Commentaries in Antimicrobial and Anticancer Chemotherapy·David LambSteven Kelly

❮ 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.