Drugs online research references
Br J Pharmacol. 1995 Dec;116(8):3337-43.
Different effects of fibrates on the microsomal fatty acid chain elongation and the acyl composition of phospholipids in guinea-pigs.
Vazquez M, Alegret M, Lopez M, Rodriguez C, Adzet T, Merlos M, Laguna JC.
Dept. Farmacologia y Quimica Terapeutica, Facultad de Farmacia, Nucleo Universitario de Pedralbes, Barcelona, Spain.
1. The effects in vitro and in vivo of three fibric acid derivatives, clofibrate (CFB), bezafibrate (BFB) and gemfibrozil (GFB) on some enzyme activities related to fatty acid biosynthesis, namely palmitoyl-CoA synthetase and hydrolases (microsomal and cytosolic), NADH and NADPH cytochrome c reductases and acyl-CoA elongases were investigated in guinea-pigs. 2. The three fibrates inhibited acyl-CoA elongation in vitro, irrespective of the substrate of elongation used (saturated, monounsaturated, polyunsaturated) and with an order of potency GFB > BFB > CFB. In the case of GFB, inhibition occurred at concentrations that can be reached in vivo. 3. Microsomal palmitoyl-CoA hydrolase and synthetase were also inhibited in vitro (GFB > or = BFB > CFB), whereas NADH cytochrome c reductase activity was increased by GFB. Nevertheless, the magnitude of changes were lower than those observed in elongation activities. 4. Treatment with fibrates did not produce peroxisomal proliferation in guinea-pigs, as measured by peroxisomal beta-oxidation activity and liver weight/body weight ratio. Nevertheless, fibrates provoked a reduction in plasma cholesterol and triglycerides, at least in GFB- and BFB-treated animals. 5. Fatty acid elongation was significantly modified by GFB treatment in vivo. The remaining enzyme activities studied were only slightly changed by fibrate treatment. 6. Treatment with BFB and to a lesser extent with CFB, increased the relative proportion of MUFA (palmitoleic and oleic acids) in microsomal phospholipids, whereas PUFA (mainly linoleic acid) decreased. GFB behaved differently, increasing palmitic and linoleic acids and decreasing stearic and oleic acids. The latter changes are attributable to an inhibition of elongation activity by GFB. 7. The changes observed after fibrate treatment in both rats and guinea-pigs, as they are not directly related to peroxisome proliferation, could be more reliably extrapolated to man than those observed only in rats.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8719816&dopt=Abstract
Metabolism. 1989 Oct;38(10):939-45.
Gemfibrozil improves abnormalities of lipid metabolism in patients on continuous ambulatory peritoneal dialysis: the role of postheparin lipases in the metabolism of high-density lipoprotein subfractions.
Chan MK.
Department of Medicine, University of Hong Kong, Queen Mary Hospital.
Twenty-five CAPD patients were given gemfibrozil in increasing doses for a total of 14 weeks. Parameters of lipid metabolism including serum total cholesterol, LDL cholesterol, HDL cholesterol, HDL2 cholesterol, HDL3 cholesterol triglyceride, apolipoprotein A-1, apolipoprotein B, postheparin lipoprotein lipase, and hepatic lipase activities were measured before the commencement, at every increment in the dose of gemfibrozil and 4 weeks after discontinuation of therapy. Gemfibrozil normalized the deranged parameters of lipid metabolism. Thus, with treatment, serum triglyceride, and total cholesterol, LDL cholesterol and apo B decreased, whereas serum HDL cholesterol, HDL2, and HDL3 (predominantly the latter subfraction), hepatic lipoprotein lipase activities increased. Apo A-1 did not change significantly. Even in normotriglyceridemic patients serum HDL cholesterol increased. The side effects consisted of muscle aches and a significant rise in serum CPK. Gemfibrozil produced a significant decrease in gamma-GT activities. A possible mechanism for the interconversion between HDL2 and HDL3 that resulted in a preferential increase in the latter was discussed. It was concluded that gemfibrozil, in a dose not exceeding 300 mg twice a day favorably improved the risk factor for ischemic heart disease in CAPD patients.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=2507877&dopt=Abstract
Biochem Pharmacol. 1993 Nov 17;46(10):1791-6.
Fibrates modify rat hepatic fatty acid chain elongation and desaturation in vitro.
Sanchez RM, Vinals M, Alegret M, Vazquez M, Adzet T, Merlos M, Laguna JC.
Dept. Farmacologia y Quimica Terapeutica, Facultad de Farmacia, Nucleo Universitario de Pedralbes, Barcelona, Spain.
Three fibric acid derivatives, clofibric acid (CFB), bezafibrate (BFB), and gemfibrozil (GFB), mainly used in the treatment of hypertriglyceridaemic or mixed hyperlipidaemic states, have been tested for their ability to modify fatty acid chain elongation and desaturation in vitro. Both endogenous and exogenous (saturated, monounsaturated and polyunsaturated) fatty acid elongations were inhibited by fibrates at concentrations well within the physiological range (IC50 values for GFB were between 0.1 and 0.3 mM). The potency order was GFB > BFB > CFB. Inhibition was not due to an impairment of the activation step from free fatty acids to acyl-CoAs, as palmitoyl-CoA synthetase was only slightly inhibited (IC50 value for GFB = 2.8 mM). Fibrates (GFB) appeared to behave as mixed non-competitive inhibitors with respect to malonyl-CoA when the rate limiting step of elongation, the condensing enzyme, is assayed. Further, delta 6 and delta 5 desaturates were inhibited by the three drugs (GFB > BFB > CFB), although not to the same extent as the elongation system. In contrast, delta 9 desaturase activity was not affected by fibrates.
online pharmacy ref source: www.ncbi.nlm.nih.gov/entrez/query.fcgi?cmd=Retrieve&db=PubMed&list_uids=8250965&dopt=Abstract
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