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Lovastatin: A New Cholesterol‐Lowering Agent
Author(s) -
Krukemyer Julie J.,
Talbert Robert L.
Publication year - 1987
Publication title -
pharmacotherapy: the journal of human pharmacology and drug therapy
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 1.227
H-Index - 109
eISSN - 1875-9114
pISSN - 0277-0008
DOI - 10.1002/j.1875-9114.1987.tb03524.x
Subject(s) - lovastatin , reductase , cholesterol , hmg coa reductase , catabolism , endocrinology , medicine , familial hypercholesterolemia , pharmacology , chemistry , ldl receptor , lipoprotein , coenzyme a , enzyme , biochemistry , metabolism
Lovastatin is a potent new drug for lowering serum cholesterol through inhibition of 3‐hydroxy‐3‐methylglutaryl—coenzyme A reductase, the rate‐limiting enzyme for cholesterol biosynthesis. Metabolic studies with lovastatin in healthy volunteers and patients with hypercholesterolemia suggest reduced synthesis of low‐density lipoprotein cholesterol (LDL‐C) as well as enhanced catabolism LDL‐C mediated through LDL receptors as the principal mechanisms for lipid‐lowering effects. Total cholesterol and LDL‐C are reduced by 30% or more on average when added to baseline therapy, with the effects being more pronounced in nonfamilial than in familial hypercholesterolemia. Optimal dosing appears to be 20 mg given twice a day. The most common adverse effects are gastrointestinal, while the most serious are elevated transaminase levels and the potential for lens opacities. Lovastatin is the first of a new class of lipid‐lowering agents, and is effective when added to diet therapy or in combination with other drugs.