McNeely W, Benfield P
Adis International Limited, Auckland, New Zealand.
Drugs. 1998 Aug;56(2):241-9; discussion 250. doi: 10.2165/00003495-199856020-00007.
Orlistat (tetrahydrolipstatin) is an inhibitor of pancreatic and other lipases. As a pancreatic lipase inhibitor, it acts in the gastrointestinal lumen and is indicated for use in obesity. Serum total cholesterol and low density lipoprotein-cholesterol levels were reduced in obese, but otherwise healthy, patients during < or = 2 years' orlistat treatment; serum triglyceride and high density and very low density lipoprotein-cholesterol levels were unchanged in trials of < or = 12 weeks. Obese patients who were maintained on a hypocaloric diet and who received orlistat 360 mg/day for 12 weeks lost a significantly greater percentage of bodyweight than placebo recipients (5 vs 3.5%). In 2-year studies, weight loss was significantly greater in orlistat than in placebo recipients by the end of year 1; weight was further reduced or maintained in the second year, when a eucaloric diet was allowed, in orlistat but not placebo recipients. A greater proportion of orlistat than placebo recipients lost > 5% or > 10% of their initial bodyweight in 1- and 2-year studies.
奥利司他（四氢脂抑素）是一种胰腺脂肪酶及其他脂肪酶的抑制剂。作为一种胰腺脂肪酶抑制剂，它在胃肠道管腔中发挥作用，适用于肥胖症治疗。在为期≤2年的奥利司他治疗期间，肥胖但其他方面健康的患者血清总胆固醇和低密度脂蛋白胆固醇水平降低；在为期≤12周的试验中，血清甘油三酯以及高密度和极低密度脂蛋白胆固醇水平未发生变化。采用低热量饮食并每日服用360毫克奥利司他治疗12周的肥胖患者，其体重减轻的百分比显著高于服用安慰剂的患者（5%对3.5%）。在为期2年的研究中，到第1年末，服用奥利司他的患者体重减轻幅度显著大于服用安慰剂的患者；在第2年，当允许摄入热量正常的饮食时，服用奥利司他的患者体重进一步减轻或维持不变，而服用安慰剂的患者则不然。在1年和2年的研究中，与服用安慰剂的患者相比，更大比例服用奥利司他的患者体重减轻超过初始体重的5%或10%。
