Summary
Neomycin and a benzodiazepine derivative (RO16-0521) inhibit similarly cholesterol absorption in man but the serum cholesterol level is reduced only by neomycin. Reason(s) for the difference are unknown. Ketoconazole inhibits 14α-demethylation of lanosterol so that cholesterol synthesis is reduced. The agent inhibits also cholesterol absorption. The serum cholesterol level is reduced by about 20%, the lowering being potentiated by a simultaneous cholestyramine treatment.
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Kes↭iemi YA, Miettinen TA (1987) Cholesterol absorption efficiency regulates plasma cholesterol level in the Finnish population. Eur J Clin Invest 17: 391–395
Miettinen TA, Kesäniemi YA (1989) Cholesterol absorption: regulation of cholesterol synthesis and elimination and within-population variations of serum cholesterol levels. Am J Clin Nutr 49: 629–635
Kesäniemi YA, Miettinen TA (1989) Serum cholesterol lowering by inhibition of cholesterol absorption. Proceedings of the 6th Symposium on Atherosclerosis, 1988. In: Crepaldi G, et al (eds) Atherosclerosis, vol VIII. Elsevier Science, Amsterdam, pp 791–794
Miettinen TA (1991) Cholesterol metabolism during hypolipidemic treatment with inhibitors of cholesterol synthesis. Proceedings of the 5th European Symposium on Metabolism, Padova. Excerpta Medica congress series. Excerpta Medica, Amsterdam (in press)
Kesäniemi YA, Grundy SM (1984) Turnover of low density lipoproteins during inhibition of cholesterol absorption by neomycin. Arteriosclerosis 4: 41–48
Sedaghat A, Samuel P, Crouse JR, Ahrens EH Jr (1975) Effects of neomycin on absorption, synthesis, and/or flux of cholesterol in man. J Clin Invest 55: 12–21
Miettinen TA (1979) Effect of neomycin alone and in combination with cholestyramine on serum cholesterol and fecal steroids in hypercholesterolemic subjects. J Clin Invest 64: 1485–1493
Miettinen TA (1982) Effects of neomycin alone and in combination with cholestyramine on serum methyl sterols and conversion of acetate and mevalonate to cholesterol. Scand J Clin Lab Invest 42: 189–196
Tilvis RS, Miettinen TA (1986) Serum plant sterols and their relation to cholesterol absorption. Am J Clin Nutr 43: 92–97
Lengsfeld H, Aeppli L, Bonetti EP, et al (1983) Ro 16.0521: a new selective inhibitor of intestinal absorption of cholesterol. Pharmacological and toxicological data. (Roche research report no B-103'142) Hoffmann-La Roche, Basle
Miettinen TA (1984) Cholesterol and bile acid synthesis in two families with homozygous and heterozygous hypercholesterolemia. Arteriosclerosis 4: 383–388
Van den Bosche H, Willemsens G, Cools W, Cornellissen F, Lauwers WF, van Cutsem JM (1980) In vitro and in vivo effects of the antimycotic drug ketoconazole on sterol synthesis. Antimicrobiol Agents Chemother 17: 922–928
Trachtenberg J, Pont A (1984) Ketoconazole therapy for advanced prostate cancer. Lancet II: 433–435
Miettinen TA, Valtonen VV (1984) Ketoconazole and cholesterol synthesis. Lancet II: 1271
Miettinen TA (1988) Cholesterol metabolism during ketoconazole treatment. J Lipid Res 29: 43–51
Gylling H, Vanhanen H, Miettinen TA (1991) Hypolipidemic effect and mechanism of ketoconazole without and with cholestyramine in familial hypercholesterolemia. Metabolism (in press)
Miettinen TA, Tikkanen M, Helve E, Ojala JP (1990) Inhibition of dietary cholesterol absorption during lovastatin (Mevinolin) treatment. Drugs Investigation 2 [Suppl 2]: 29–35
Vanhanen H, Miettinen TA (1990) Ketoconazole, cholesterol, and LDL apoprotein B concentration and kinetics in familial hypercholesterolemia (FH). Circulation 82 [Suppl III]: 6
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Kesäniemi, Y.A., Miettinen, T.A. Inhibition of cholesterol absorption by neomycin, benzodiazepine derivatives and ketoconazole. Eur J Clin Pharmacol 40, S65–S67 (1991). https://doi.org/10.1007/BF01409412
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DOI: https://doi.org/10.1007/BF01409412