英文药名: Xenical(Orlistat Capsules)

中文药名: 赛尼可（奥利司他胶囊）

生产厂家: Roche Pharmaceuticals

【类别】消化系统其他药物
【中文别名】奥利司他
【英文名】xenical
【英文别名】Orlistat Capsules
【分子式或成分】本品的主要活性成分为奥利司他。赋形剂包括 ：微晶纤维素，羟乙酸淀粉钠，聚乙烯吡咯烷酮，十二烷硫酸钠和滑石。胶囊外壳含有明胶、靛蓝二磺酸钠(E132)，二氧化钛。
规格

胶囊剂：120mg* 84胶囊
药理

赛尼可是长效和强效的特异性胃肠道脂肪酶抑制剂，它通过与胃和小肠腔内胃脂肪酶和胰脂肪酶的活性丝氨酸部位形成共价键使酶失活而发挥治疗作用，失活的酶不能将食物中的脂肪，主要是甘油三酯水解为可吸收的游离脂肪酸和单酰基甘油。未消化的甘油三酯不能被身体吸收，从而减少热量摄入，控制体重。该药无需通过全身吸收发挥药效。
药动学

吸收 ：对体重正常和肥胖志愿者的研究表明，机体对奥利司他的吸收量极微，口服后8小时测不出完整的奥利司他血浆浓度(< 5 ng/mL)。通常治疗剂量的奥利司他全身吸收极其有限，无蓄积，血浆中仅偶尔可测出完整的奥利司他，浓度很低(< 10 ng/mL或0.02 ?m)。
分布 ：由于奥利司他几乎不被吸收，所以难以测定其分布容积，全身的药代动力学也不能检测。在体外，99%以上的奥利司他与血浆蛋白结合(脂蛋白、白蛋白是主要的结合蛋白)。奥利司他很少与红细胞结合。
代谢 ：动物试验提示，奥利司他的代谢主要集中在胃肠道壁。在肥胖患者中进行的研究显示，在极少部分被全身吸收的药物成分中有两种主要的代谢产物，M1(4-环内酯环水解产物)和M3(M1附着一个N-甲酰基亮氨酸裂解产物)占全部血浆浓度的42%。M1和M3具有一个开放的b-内酯环对脂酶抑制活性极弱(与奥利司他相比，分别低1000倍和2500倍)。治疗剂量时，M1和M3的抑酶活性及血浆浓度很低(平均为M1-26 ?g/mL和M3-108 ?g/mL)，因此这两种代谢产物不具有药理意义。
清除 ：对正常体重和肥胖者的研究表明，未吸收的药物主要通过粪便排出体外。所服用剂量的大约97%是从粪便排泄，其中83%是原形奥利司他，奥利司他所有相关物的累计肾排泄量低于2%。药物彻底排出(粪便和尿液)需要3-5天。对于正常体重者和肥胖受试者，奥利司他的代谢是很相似的。奥利司他、M1和M3均可以经胆汁排泄。测定粪便中脂肪含量表明，本药的药效在给药后24-48小时即可显现，停止治疗后48-72小时，粪便中脂肪含量便恢复到治疗前水平。
适应症

赛尼可结合微低热能饮食适用于肥胖和体重超重者包括那些已经出现与肥胖相关的危险因素的患者的长期治疗。赛尼可具有长期的体重控制（减轻体重、维持体重和预防反弹）的疗效。服用赛尼可可以降低与肥胖相关的危险因素和与肥胖相关的其它疾病的发病率，包括高胆固醇血症、2型糖。
用法用量

成人：推荐剂量为餐时或餐后一小时内服120mg胶囊一粒。如果有一餐未进或食物中不含脂肪，则可省略一次服药。长期服用赛尼可的治疗效果（包括控制体重和改善危险因素）可的持续。病人的膳食应营养均衡，微低热能，大约30%热能来自脂肪，食物中应富含水果和蔬菜。脂肪、碳水化合物和蛋白质的摄入应分布于每日三餐。没有证据表明超过每日三次/每次120mg能增强疗效。对老年人无需调整剂量。
如果您有任何疑问，请遵医嘱。
不良反应

主要引起胃肠道不良反应，其与药物阻止摄入脂肪的吸收的药理作用有关。常见不良反应为：油性斑点，胃肠排气增多，大便紧急感，脂肪（油）性大便，脂肪泻，大便次数增多和大便失禁。通常在服用赛尼可的病人中较多出现的胃肠道急性反应有：腹痛/腹部不适、胃肠胀气、水样便、软便、直肠痛/直肠部不适、牙齿不适、牙龈不适。观察到的其它少见不良事件有：上呼吸道感染、下呼吸道感染、流行性感冒、头痛、月经失调、焦虑、疲劳、泌尿道感染。偶有对本品才敏的报道。主要的临床表现为瘙痒、皮疹、荨麻疹、血管神经性水肿和过敏反应。
注意事项

经过最多不超过两年的奥利司他治疗，大部分病 人维生素A、D、E、K和β胡萝卜素水平仍在正常范围内。为了保证有足够的营养物质，可以考虑补充复合维生素。应该教育病人遵从膳食指导（见剂量和用法）。当赛尼可与高脂成分饮食（比如一天2000卡热能中，超过30%的热能来源于67克以上的脂肪供给）合用时，发生胃肠道事件（见不良反应）的可能怀会增加。每日脂肪摄入量应分布在三顿主餐中。当赛尼可与脂肪含量很高的某一餐同服时，发生胃肠道反应的可能性增加。在2型糖尿病患者中，赛尼可在导致体重减轻的同时常常伴随着血糖控制的改善，从而可能或需要减少口服降糖药的剂量（比如磺酰脲类药物）。
赛尼可与环孢霉素联合用药时可造成后者血浆浓度的降低。因此建议在赛尼可与环孢霉素联合用药时应对后者的血清浓度进行比通常情况下更为密切的监测（见药物相互作用）。患慢性吸收不良综合征或胆汁郁积症及对奥利司他或药物制剂中任何一种其他成分过敏的患者禁用。
相互作用

在药代动力学研究中，没有观察到奥利司他与酒精、地高辛、二甲双胍、硝苯地平、口服避孕药、苯妥英类，普伐他汀或华法令之间有药物相互作用。已经观察到在与赛尼可同服时，维生素D、E和β胡萝卜素的吸收减少。如果需要补充复合维生素，应在服用赛尼可至少2小时后服用。或在睡觉前服用。与赛尼可同时服用时，已观察到环孢霉素A的血浆浓度降低。因此，当赛尼可和环孢霉素A同时给药时，应加强对环孢霉素A血浆浓度的监测（见注意事项）。

Xenical (Orlistat Capsules)

Manufactured by: Roche Pharmaceuticals

This product requires a valid prescription

Xenical (Orlistat) Capsules 120mg x 84 is a medicine used to treat obesity.

Xenical (Orlistat Capsules) is a gastrointestinal lipase inhibitor used in the management of obesity in adult and adolescent patients age 12 and older. Xenical Orlistat Capsules) may be used during the weight loss phase or following weight loss to assist in weight management. Xenical (Orlistat Capsules) works by inhibiting the digestion of fats from the diet and should be used with a reduced-calorie diet. Buy Xenical (Orlistat Capsules) from Canada for the lowest prices guaranteed. Do not take your medicine more often than directed

You should use Xenical (Orlistat Capsules) with a reduced-calorie diet that contains no more than about 30% of the calories from fat. Divide your daily intake of fat, carbohydrates, and protein evenly over your 3 main meals. You should try to follow a healthy eating plan as prescribed by your doctor such as the one developed by the American Heart Association. Following this eating plan can help reduce the possible GI side effects from Xenical (Orlistat Capsules).

Xenical (Orlistat Capsules) is taken by mouth and swallowed with a drink of liquid. Follow the directions on the prescription label. You can take Xenical (Orlistat Capsules) with each main meal that contains about 30% of the calories from fat. Or you can take the capsule one hour after the meal. If you occasionally miss a meal or have a meal without fat, you can omit that dose of Xenical (Orlistat Capsules). Doses greater than 120 mg three times per day have not been shown to increase weight loss.

These drugs may interact with Xenical (Orlistat Capsules):

•Dietary supplements, such as beta-carotene and vitamins A, D, E, and K
•warfarin
•cyclosporine
•pravastatin
•drugs used to treat diabetes

Xenical (Orlistat Capsules) blocks some of the fat that you eat from being absorbed by your body. Xenical (Orlistat Capsules) is used in the management of obesity including weight loss and weight maintenance when used with a reduced-calorie diet. Xenical Capsules (Xenical (Orlistat Capsules) may also be used for purposes other than those listed in this medication guide.

Xenical (Orlistat Capsules) may decrease your body's absorption of some fat-soluble vitamins. To ensure adequate nutrition, your doctor may recommend taking a multivitamin that contains vitamins D, E, K, and beta-carotene. Take your vitamin supplement once a day, at least 2 hours before or after a dose of Xenical Capsules (Orlistat).

Do not take Xenical (Orlistat Capsules) without first talking to your doctor if you have
• chronic mal-absorption syndrome (an inability to absorb food and nutrients properly), or
• gallbladder problems

Before taking Xenical Capsules (Orlistat), talk to your doctor if you
• have a history of kidney stones,
• have diabetes,
• have anorexia or bulimia,
• take any other weight-loss medicine, or
• take cyclosporine (Sandimmune, Neoral)

You may not be able to take Xenical Capsules (Orlistat), or you may require a dosage adjustment or special monitoring during your treatment if you have any of the conditions listed above. Xenical (Orlistat Capsules) is in the FDA pregnancy category B. This means that it is not expected to harm an unborn baby. Do not take Xenical Capsules without first talking to your doctor if you are pregnant. It is not known whether Xenical Capsules passes into breast milk. Do not take Xenical Capsules without first talking to your doctor if you are breast-feeding a baby.

Take Xenical/Orlistat Capsules exactly as directed by your doctor. If you do not understand these directions, ask your pharmacist, nurse, or doctor to explain them to you.

Take each Xenical dose with a full glass of water.

Xenical Capsules are usually taken with each main meal that contains fat. Xenical Capsules can be taken during meals or up to one hour after a meal. Each time you take Xenical Capsules, your meal should contain no more than about 30% of calories from fat. Evenly divide your daily intake of fat, carbohydrates, and protein over three main meals a day. Talk to your doctor about following a healthy eating plan. If you miss a meal, or if you have a meal without fat, you can skip your dose of Xenical Capsules (Xenical (Orlistat Capsules)) for that meal also. If Xenical Capsules are taken with any one meal that is very high in fat, there is an increased chance of digestive side effects.

Do not take more of Xenical than has been prescribed for you. Xenical doses greater than 120 mg three times a day have not been shown to provide an additional weight-loss benefit. Xenical (Orlistat Capsules) may decrease your body's absorption of some fat-soluble vitamins. To ensure adequate nutrition, your doctor may recommend taking a multivitamin that contains vitamins D, E, K, and beta-carotene. Take your vitamin supplement once a day, at least 2 hours before or after a dose of Xenical Capsules.

Xenical should be stored at room temperature and away from moisture and heat.

If you miss a dose of Xenical, take your missed dose within one hour after a meal. If more than one hour has passed since your last meal, skip the dose you missed and take only your next regularly scheduled dose as directed. Do not take a double dose of Xenical.

If you miss a meal, or if you have a meal without fat, you can skip your dose of Xenical Capsules for that meal also.

You may want to speak to your doctor about less serious side effects of Xenical/Orlistat capsules such as:
• oily spotting;
• oily or fatty stools;
• orange or brown colored oil in your stool;
• gas with discharge, an oily discharge;
• an urgent need to go to the bathroom;
• an inability to control bowel movements, or;
• an increased number of bowel movements

The bowel changes listed above are a natural effect of blocking fat and indicate that Xenical Capsules are working. They generally occur early in treatment, particularly after meals containing higher amounts of fat than are recommended. These symptoms are usually temporary and lessen or disappear as you continue treatment and keep to your recommended diet of meals containing 30% fat.

Xenical/Orlistat side effects other than those listed here may also occur. Talk to your doctor about any Xenical/Orlistat side effect that seems unusual or that is especially bothersome. You should not take Xenical without first talking to your doctor if you are taking any of the following medicines:

• Cyclosporine (Neoral, Sandimmune)
• Warfarin (Coumadin).

Xenical Capsules may decrease your body's absorption of some fat-soluble vitamins. To ensure adequate nutrition, your doctor may recommend taking a multivitamin that contains vitamins D, E, K, and beta-carotene. Take your vitamin supplement once a day, at least 2 hours before or after a dose of Xenical Capsules (Xenical (Orlistat Capsules)).

Please remember that there can be many prescription and over-the-counter drugs other than those listed here that can interact with Xenical Capsules. You must speak to your doctor and/or pharmacist before taking Xenical with any other prescription or over-the-counter medicines including vitamins, minerals, and herbal products.

Only your doctor can give you a personalized consultation and assessment to see if Xenical capsules will work for you.