Crenier L, Sternon J
Service d'Endocrinologie, Hôpital Erasme et C.U.M.G.-U.L.B.
Rev Med Brux. 1999 Jun;20(3):159-63.
Orlistat, a potent inhibitor of the pancreatic and intestinal lipases, is the first member of a new therapeutic class approved for the treatment of obesity. Its administration with fat-containing foods results in a partial inhibition of triglyceride hydrolysis in the digestive lumen and subsequent reduction of the free fatty acids and monoglycerides absorption. At the usual dosage of 120 mg tid, about 30% of ingested fat are excreted non digested in feces. When administered with a mildly hypocaloric diet, orlistat contributes to loss of weight by a additional caloric deficit and promotes further compliance of the obese patient to the dietary recommendations. Several double-blinded, placebo-controlled studies have shown a statistically significant loss of weight of about 10% when orlistat was prescribed with a well balanced, mildly hypocaloric diet to obese patients during one year. Moreover, small but significant beneficial changes in the serum lipid levels occurred in these patients. Because the orlistat molecule is not reabsorbed, its side effects are mostly due to the gastrointestinal effects and consist in steatorhea after fatty meals. However, the treatment is generally well tolerated. Since the recent withdrawal from the worldwide market of the anorectic agents, phentermine and fenfluramine, orlistat is at this time the only drug approved by the European Community for the treatment of obesity. However, its long-term value are not currently known.
奥利司他是一种强效的胰腺和肠道脂肪酶抑制剂,是获批用于治疗肥胖症的新型治疗类别中的首个药物。它与含脂肪食物一同服用会导致消化腔内甘油三酯水解受到部分抑制,进而减少游离脂肪酸和单酸甘油酯的吸收。在120毫克每日三次的常规剂量下,约30%摄入的脂肪会未经消化随粪便排出。当与轻度低热量饮食一同服用时,奥利司他通过额外的热量亏空有助于体重减轻,并促使肥胖患者进一步遵守饮食建议。多项双盲、安慰剂对照研究表明,当在一年内为肥胖患者开具奥利司他并搭配营养均衡的轻度低热量饮食时,体重有统计学意义的显著减轻约10%。此外,这些患者的血脂水平出现了虽小但显著的有益变化。由于奥利司他分子不会被重新吸收,其副作用主要是胃肠道影响,表现为餐后脂肪泻。然而,该治疗总体耐受性良好。自从食欲抑制剂芬特明和芬氟拉明近期从全球市场撤市以来,奥利司他目前是欧洲共同体批准用于治疗肥胖症的唯一药物。然而,其长期价值目前尚不清楚。