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Ezetimibe.

机译：ezetimibe。

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Ezetimibe is the first of a new class of drugs that specifically reduces the intestinal absorption of cholesterol. The drug is absorbed into the intestinal epithelial cell and remains associated in great part with the apical cell membrane where it is believed to interfere with the putative sterol transporter system. This apparently prevents both free cholesterol and plant sterols (phytosterols) from being transported into the cell from the intestinal lumen. The mechanism is very different from the reduction produced by phytosterol esters and phytostanol esters that have been documented previously as interfering with the micellar presentation of sterols to the cell surface. The drug is rapidly absorbed and glucuronidated in the intestinal cell before secretion into the blood. Ezetimibe is avidly taken up by the liver from the portal blood and excreted into the bile, resulting in low peripheral blood concentrations. The glucuronide conjugate is hydrolyzed and absorbed and is equally effective in inhibiting sterol absorption. This enterohepatic recycling is responsible for a half-life in the body of more than 20 h. The principle medical benefit appears to be a reduction in low-density lipoprotein cholesterol (LDLc). There is also a reduction in the cholesterol content of chylomicrons, which may provide some reduction in the atherogenic potential of the plasma lipoprotein pool. Triglycerides fall moderately and a modest rise in high-density lipoprotein cholesterol (HDLc) has been consistently observed in groups of treated patients. The maximum mean reduction of LDL cholesterol is approximately 20-25% in small studies at the maximal dose tested of 40 mg/day and the reduction is usually in the 16-20% range at the dosage of 10 mg/day. Most subsequent studies have been completed with the 10 mg/day dose. The medication is effective as a single daily dose due to its long residence time in the body. Combinations of ezetimibe with all available statins have been completed and demonstrate LDLc reductions of approximately 25% as additive effects to any statin dose alone. There are also small additional increases in HDL (2-3%) and reductions in triglycerides (10-15%). Additive effects to statin therapy have also been documented in patients with homozygous familial hypercholesterolemia. Reduction of plant sterols has been demonstrated in phytosterolemia, offering the first drug treatment for this rare inherited disease. (c) Prous Science 2003. All rights reserved.
机译：Ezetimibe是第一类专门减少胆固醇的肠道吸收的新药物中的第一个。该药物被吸收到肠上皮细胞中，并在很大程度上与顶端细胞膜保持相关，其中被认为干扰推定的甾醇转运系统。这显然可以防止游离胆固醇和植物甾醇（植物甾醇）从肠腔输送到细胞中。该机制与植物甾醇酯和先前被记录的植物甾烷醇酯产生的减少非常不同，以便干扰甾醇对细胞表面的胶束呈递。在分泌到血液之前，药物在肠细胞中迅速吸收和血糖化。 ezetimibe被肝脏从门耳血液射击并排出到胆汁中，导致外周血浓度低。葡糖醛酸缀合物是水解和吸收的，并且同样有效抑制甾醇吸收。这种Enterohepatic再循环负责超过20小时的半衰期。该原理医疗益处似乎是低密度脂蛋白胆固醇（LDLC）的降低。 Chylomicrons的胆固醇含量还减少，这可以在血浆脂蛋白池的静脉内潜力中产生一些降低。在治疗患者组中一直观察到甘油三酯中度和高密度脂蛋白胆固醇（HDLC）的温度升高。 LDL胆固醇的最大平均值降低约为20-25％，在40mg /天测试的最大剂量的小型研究中，并且还原通常在10mg /天的10mg /天的16-20％范围内。大多数后续研究已经完成了10毫克/天剂量。由于其在体内的长停留时间，药物作为单一的每日剂量是有效的。 ezetimibe与所有可用的他汀类药物的组合已经完成，并证明LDLC减少约25％作为单独的任何沙特汀剂量的添加剂效应。 HDL（2-3％）的额外增加还增加了甘油三酯（10-15％）的额外增加。纯合家族高胆固醇血症患者还记录了对他汀类药物治疗的添加剂效应。在植物甾司抑血症中证实了植物甾醇的减少，为该罕见的遗传疾病提供了第一种药物治疗方法。 （c）2003年律师科学。保留所有权利。

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