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Enzyme Kinetics and Drugs as Enzyme Inhibitors
Published in Peter Grunwald, Pharmaceutical Biocatalysis, 2019
Another established hypolipidemic drug is Ezetimibe; it acts as a cholesterol absorption inhibitor that blocks the intestinal absorption of both biliary and dietary cholesterol (Bays et al., 2008); it is safe and well tolerated and used—in combination with or as an alternative to statins–to reduce the LDL-cholesterol level to about 30 to 50 mg/dL (O‘Keefe, et al., 2017). Ezetimibe works by inhibiting the intestinal cholesterol absorption by selectively blocking the cholesterol transport protein Niemann Pick C1 like 1 (NPC1L1) protein in the jejunal brush border (Phan et al., 2012). The molecular mechanism of sterol uptake from the lumen of the small intestine that contribute to plasma cholesterol levels was detected by Altman et al., 2004; these authors also demonstrated that Ezetimibe had no effect on NPC1L1 knockout mice concerning the observed reduction in absorbed cholesterol.
Estimation of non-alcoholic steatohepatitis (NASH) disease using clinical information based on the optimal combination of intelligent algorithms for feature selection and classification
Published in Computer Methods in Biomechanics and Biomedical Engineering, 2023
The predominant selected features are as follows: Ezetimibe, BMI, GPT, TC, HDL, Lp(a), Loge(Lp(a)), TG, Cre, HbA1c, Fibrate, and Sex. In interpreting the risk factors for fatty liver, BMI, one of the most basic indicators of obesity, plays a potent role in changing the risk of liver malfunction (Fan et al. 2018). This investigation shows that a high BMI can increase the risk of NASH by 14 times more than an average BMI. The GPT index is highly correlated with fatty liver, diabetes, and pre-diabetes, and it is an important index in determining the metabolism of glucose breakdown (Rückert et al. 2011). Therefore, in some lectures, fatty liver is introduced relative to two enzymes associated with glucose, one of which is GPT. According to investigations, some factors of fatty liver and type 2 diabetes are affected by an increment in triglycerides and LDL and a reduction in HDL (Toledo et al. 2006). Lp(a) characteristic is the low density of lipoprotein which is known as bad cholesterol (Zheng et al. 2022). A high level of this index can cause the generation of blood platelets and their deposition in blood veins. It may initially start from the liver’s vein and increase the liver’s difficulties. Ezetimibe drugs have a constructive role of fatty liver disease treatment (Jun and Cheon 2019). The clinical results of these drugs show that Ezetimibe is effective in improving liver tissue. They show that Ezetimibe can improve the level of liver enzymes and mitigate the severity of steatosis and ballooning. Studies also show that the combination of Ezetimibe and Statin can help regulate the state of liver enzymes.
The role of cardiac computed tomography in pre-participation screening of mature athletes
Published in European Journal of Sport Science, 2022
Georgios A. Christou, Asterios P. Deligiannis, Evangelia J. Kouidi
Athletes diagnosed with coronary atherosclerosis should be counselled to adopt a healthier diet, emphasizing the decrease in intake of saturated and trans fatty acids, quit smoking and initiate statin treatment (Mach et al., 2020). Considering that the tolerability of statin treatment in athletes has been found to be decreased due to muscle complaints, statins with the lowest potential for myopathy should be preferentially used, such as fluvastatin, pravastatin and pitavastatin, with the possible addition of ezetimibe in order to achieve the target levels of low density lipoprotein-cholesterol in a tolerable manner (Christou et al., 2020; Christou, Kouidi, Deligiannis, & Kiortsis, 2017; Mach et al., 2020). However, follow up evaluations of statin-treated athletes should not rely on measurement of CACS, since CACS is expected to increase by statin treatment and possibly does not reflect the changes in coronary atheroma volume (Grundy et al., 2019; Puri et al., 2015).