Drugs online research references
Metabolism. 1986 May;35(5):387-93.
Effect of gemfibrozil on lipids, apoproteins, and postheparin lipolytic activities in normolipidemic subjects.
Gnasso A, Lehner B, Haberbosch W, Leiss O, von Bergmann K, Augustin J.
The lipid lowering agent Gemfibrozil was tested in 8 normolipidemic subjects during a three-month intake. Plasma triglycerides decreased by 41% and Very Low Density Lipoprotein (VLDL) triglycerides decreased by 54%. The reduction of plasma cholesterol, less marked (by 10%), was due to a decrease of Low Density Lipoprotein by 20% while High Density Lipoprotein (HDL) increased up to 30%. The separation of HDL demonstrated that only HDL3 were increased. The determination of the apoproteins in plasma and lipoprotein fractions showed similar results with a decrease of apo B (by 20%) and an increase of apo A-I and apo A-II, mainly in the HDL3 fraction. Plasma postheparin lipolytic activities (PHLA) were not influenced by the therapy and no correlation was found between these activities and any of the plasma or lipoprotein lipids. The apo C-III/apo C-II ratio in VLDL decreased by 30%; however, no correlation was found between this ratio in plasma as well as VLDL and triglycerides. In addition, the Intra Venous Fat Tolerance Test did not demonstrate any improvement of the clearance of exogenous fat. The lipid lowering efficacy of Gemfibrozil, its collateral effects, and the possible mechanisms of action are discussed.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=3458020&dopt=Abstract
Biochem Pharmacol. 1995 May 11;49(9):1213-21.
Effect of gemfibrozil on lipid biosynthesis from acetyl-CoA derived from peroxisomal beta-oxidation.
Hashimoto F, Ishikawa T, Hamada S, Hayashi H.
Department of Physiological Chemistry, Faculty of Pharmaceutical Sciences, Josai University, Saitama, Japan.
The effect of gemfibrozil, a peroxisome proliferator, on lipid biosynthesis from acetyl-CoA derived from peroxisomal beta-oxidation was studied. The specific activity of the peroxisomal fatty acyl-CoA beta-oxidation system of rats fed a chow containing 0.2% gemfibrozil for 2 weeks was approximately five times higher than that of control rats. When [1-14C]lignoceric acid, a very-long-chain fatty acid which is degraded exclusively by the peroxisomal beta-oxidation system at first, was injected into rats treated with gemfibrozil, radioactivity and content of bile acid in the bile were enhanced to approximately 2.2 and 3.5 times the control, respectively. Gemfibrozil increased the radioactivity and content of chenodeoxycholic acid more than that of cholic acid. The incorporation of radioactivity into cholesterol in the bile was as much as 4.5 times greater than the control, and content was 2.6 times greater. In the liver, incorporation of [14C]lignoceric acid into the simple lipids phosphatidylethanolamine and phosphatidylcholine was unaffected by gemfibrozil. The radioactivity and content of cholesterol separated from the simple lipids were also virtually unaffected. However, the specific activities of 3-hydroxy-3-methylglutararyl-CoA reductase (rate-limiting enzyme of cholesterol synthesis) of peroxisomes and microsomes were remarkably stimulated by gemfibrozil treatment. These results suggest that biosyntheses of cholesterol and bile acid from acetyl-CoA derived from peroxisomal beta-oxidation are stimulated by gemfibrozil, due at least in part to activation of the peroxisomal beta-oxidation system and 3-hydroxy-3-methylglutaryl-CoA reductase of peroxisomes and/or microsomes. Most peroxisomal proliferators (e.g. clofibrate) have been known to inhibit 3-hydroxy-3-methylglutaryl-CoA reductase activity. Therefore, gemfibrozil is expected to be a very useful tool for elucidating the relationship between peroxisomes and the biosyntheses of cholesterol and bile acid.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=7763302&dopt=Abstract
Ann Acad Med Singapore. 1989 May;18(3):269-71.
A pilot study on intensive lipid lowering--a new approach to cardiac rehabilitation.
Yuen Y, Foo SK, Oon CH.
Department of Rehabilitation Medicine, Singapore General Hospital.
The deleterious effects of raised plasma lipids on the progression of coronary artery disease has been well established. Recent research data suggests that intensive lipid lowering represents a new approach to Cardiac Rehabilitation. There was a total of twenty-four participants with twenty-one (87.5%) males and three (12.5%) females. There were seventeen Chinese (70.8%), six Indians (25%) and one Malay (4.2%). Their ages ranged from group forty to forty-nine, five participants (20%); fifty to fifty-nine, twelve participants (50%); sixty to sixty-nine, six participants (25%) and seventy to seventy-nine, one participant (5%). In this study, twelve individuals were treated with Cholestyramine, seven by Gemfibrozil, four by Clofibrate and three by Bezafibrate. The duration of antilipid treatment ranged from two to eighteen months (mean eight months). Side effects were reported in twelve patients (50%) on Cholestyramine who complained of constipation while one (4%) on Bezafibrate had abnormal liver function tests (raised SGOT and SGPT). All patients had been on an exercise and diet control program for one year which they were enrolled in an intensive lipid-lowering protocol. The pre and post treatment lipid profiles with lipid-lowering agents showed 18% reduction for Triglycerides, 15% reduction for Total Cholesterol, 5% increase for HDL-Cholesterol, 19% decrease in LDL Cholesterol, 19% decrease in Total Cholesterol: HDL ratios. The initial results suggest that an intensive lipid-lowering strategy in a Cardiac Rehabilitation Program appears to have a beneficial effect on lipid profiles and represents an expanded approach to lipid management involving exercise, nutrition and pharmacological intervention.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2774472&dopt=Abstract
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