近日，美国批准胰脂酶Zenpep(胰腺酶制剂，PEP)缓释胶囊用于治疗囊性纤维化(CF)或其他疾病引起的胰腺外分泌机能不全(EPI)。
Zenpep是一种高稳定性制剂，提取自猪的胰腺，其生物学特性类似于在消化中不可或缺的人类内源性胰腺分泌物。Zenpep可替代缺失的胰腺酶，以促进食物的消化和吸收。
Zenpep每天的总剂量不应超过10000 LU/(kg·d)，如果单餐剂量超过2500LU/(kg·d)，应谨慎服用。应努力确保Zenpep不被咀嚼或含化，以免刺激口腔黏膜。胶囊或胶珠应配以足量液体送服，迅速吞咽。当必要时，Zenpep胶囊可与食物混合后服用。
批准日期：2009年9月8日  公司：Eurand公司
ZENPEP®（胰脂肪酶[LIPASE/PROTEASE/AMYLASE]）缓释胶囊  供口服使用
美国首次批准：2009年
作用机制
ZENPEP中的胰酶催化脂肪水解为单甘油酯，甘油和游离脂肪酸，蛋白质成肽和氨基酸，以及淀粉成为糊精和短链糖，例如十二指肠和近端小肠中的麦芽糖和麦芽三糖， 如胰腺生理分泌的消化酶。
适应症和用法
ZENPEP是猪来源的脂肪酶，蛋白酶和淀粉酶的组合，指示用于治疗由于囊性纤维化或其他病症引起的外分泌胰腺功能不全
剂量和给药
剂量
ZENPEP与任何其他胰脂肪酶产品不可互换。
婴儿（长达12个月）
婴儿可以每120mL配方或每次母乳喂养给予3000个脂肪酶单位（一个胶囊）。
在给药前不要将ZENPEP胶囊内容物直接混入配方奶粉或母乳中。
儿童年龄大于12个月和小于4岁
酶剂量应该从1,000个脂肪酶单位/kg体重/餐开始，最大为每个膳食2500个脂肪酶单位/kg体重（或小于或等于10000个脂肪酶单位/kg体重每天），或更少超过每天摄入的4000个脂肪酶单位/g脂肪。
儿童4岁及以上和成人
酶剂量应该从500个脂肪酶单位/ kg体重/餐开始，最大为每个膳食2,500个脂肪酶单位/kg体重（或小于或等于10,000个脂肪酶单位/kg体重每天），或更少超过每天摄入的4000个脂肪酶单位/g脂肪。
剂量限制
剂量不应超过囊性纤维化基金会共识会议指南规定的建议最大剂量
行政
ZENPEP应该整个吞下。对于不能吞咽完整胶囊的婴儿或患者，可将内容物撒在软酸性食物例如苹果酱上。
剂量形式和强度
胶囊：3000USP单位的脂肪酶; 10000 USP单位的蛋白酶; 16000USP单位的淀粉酶。胶囊有白色不透明的帽和身体，印有“APTALIS 3”
胶囊：5000USP单位的脂肪酶; 17000 USP单位的蛋白酶; 27000 USP单位的淀粉酶。胶囊有一个白色不透明的帽和身体，印有“APTALIS 5”
胶囊：10000USP单位的脂肪酶; 34000 USP单位的蛋白酶; 55,000 USP单位的淀粉酶。胶囊具有黄色不透明盖和白色不透明体，印有“APTALIS 10”
胶囊：15000 USP单位的脂肪酶; 51000 USP单位的蛋白酶; 82,000 USP单位的淀粉酶。胶囊有一个红色不透明的帽和白色不透明的身体，印有“APTALIS 15”
胶囊：20000USP单位的脂肪酶; 68000 USP单位的蛋白酶; 109000 USP单位的淀粉酶。胶囊具有绿色不透明盖和白色不透明体，印有“APTALIS 20”
胶囊：25000USP单位的脂肪酶; 85000 USP单位的蛋白酶; 136000 USP单位的淀粉酶。胶囊具有蓝色不透明帽和白色不透明体，印有“APTALIS 25”
胶囊：40000 USP单位的脂肪酶; 136000 USP单位的蛋白酶; 218000USP单位的淀粉酶。胶囊具有橙色不透明帽和白色不透明体，印有“APTALIS 40”
禁忌症
没有
警告和注意事项
纤维结肠病与胰腺酶替代的高剂量使用有关。当ZENPEP的剂量超过2,500脂肪酶单位/kg体重/餐（或大于10000脂肪酶单位/ kg体重/天）时，请谨慎行事。
为了避免刺激口腔粘膜，不要咀嚼ZENPEP或留在口中。
在对患有痛风，肾损伤或高尿酸血症的患者开具ZENPEP时应小心。
存在所有胰腺酶产物（包括ZENPEP）的病毒传播的理论风险。
向对猪来源的蛋白质具有已知过敏反应的患者施用胰脂肪酶时要小心。
不良反应
最常见的不良事件（≥ZENPEP治疗的患者的≥6％）是腹痛，胃肠胀气，头痛，咳嗽，体重减轻，早饱和挫伤。
在特定人群中使用
儿科患者：
在1至17岁的儿科患者中评估ZENPEP的安全性和有效性。
在儿科患者中具有不同胰脂肪酶制剂的胰酶产品的安全性和功效已经在医学文献和临床经验中描述。

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注：以下产品不同各和不同价格，采购以咨询为准！
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ZENPEP CAP 25000U 100  LIPASE/PROTEASE/AMYLASE     42865-0305-02 
ZENPEP CAP 40000U 100  LIPASE/PROTEASE/AMYLASE     42865-0307-02 
ZENPEP CAP 3000U 100  LIPASE/PROTEASE/AMYLASE     42865-0304-02 
ZENPEP CAP 5000U 100  LIPASE/PROTEASE/AMYLASE     42865-0300-02 
ZENPEP CAP 10000U 100  LIPASE/PROTEASE/AMYLASE     42865-0306-02 
ZENPEP CAP 15000U 100  LIPASE/PROTEASE/AMYLASE     42865-0302-02 
ZENPEP CAP 20000U 100  LIPASE/PROTEASE/AMYLASE     42865-0303-02 
Zenpep(Pancrelipase Delayed Release Capsules)
General Information
The pancreatic enzymes in Zenpep catalyze the hydrolysis of fats to monoglycerol, glycerol and fatty acids, protein into peptides and amino acids, and starch into dextrins and short chain sugars in the duodenum and proximal small intestine, thereby acting like digestive enzymes physiologically secreted by the pancreas.
Zenpep is specifically indicated for the treatment of exocrine pancreatic insufficiency due to cystic fibrosis or other conditions.
Zenpep is supplied as a capsule for oral administration. The recommended initial dose of the drug is as follows:
Infants (up to 12 months)
2,000 to 4,000 lipase units per 120mL of formula or per breast-feeding. Do not mix Zenpep capsule contents directly into formula or breast milk prior to administration.
Children Older than 12 Months and Younger than 4 Years
1,000 lipase units/kg of body weight per meal for children less than age 4 years to a maximum of 2,500 lipase units/kg of body weight per meal (or less than or equal to 10,000 lipase units/kg of body weight per day), or less than 4,000 lipase units/g fat ingested per day.
Children 4 Years and Older and Adults
dosing should begin with 500 lipase units/kg of body weight per meal for those older than age 4 years to a maximum of 2,500 lipase units/kg of body weight per meal (or less than or equal to 10,000 lipase units/kg of body weight per day), or less than 4,000 lipase units/g fat ingested per day. Zenpep should be taken during meals or snacks, with sufficient fluid. Zenpep capsules and capsule contents should not be crushed or chewed.
Limitations on Dosing
Doses greater than 2,500 lipase units/kg of body weight per meal (or greater than 10,000 lipase units/kg of body weight per day) should be used with caution and only if they are documented to be effective by 3-day fecal fat measures that indicate a significantly improved coefficient of fat absorption.
FDA Approval
The FDA approval of Zenpep was based on the results of two clinical studies in patients with exocrine pancreatic insufficiency (EPI) associated with cystic fibrosis (CF).
Study One
This randomized, double-blind, placebo-controlled, crossover study enrolled 34 patients, ages 7 to 23 years. Results are from 32 subjects who completed both double-blind treatment periods, and were included in the efficacy analysis population. The subjects were randomized to receive Zenpep or matching placebo for 6 to 7 days of treatment, followed by crossover to the alternate treatment for an additional 6 to 7 days. The mean dose during the controlled treatment periods ranged from a mean dose of 3,900 lipase units per kilogram per day to 5,700 lipase units per kilogram per day.
All patients consumed a high-fat diet (greater than or equal to 100 grams of fat per day) during the treatment period. The primary efficacy endpoint was the mean difference in the coefficient of fat absorption (CFA) between Zenpep and placebo treatment. Mean CFA was 88% with Zenpep treatment compared to 63% with placebo treatment. The mean difference in CFA was 26 percentage points in favor of Zenpep treatment (p<0.001). Subgroup analyses of the CFA results showed that mean change in CFA was greater in patients with lower no-treatment (placebo) CFA values than in patients with higher no-treatment (placebo) CFA values.
Study Two
All subjects in this study were transitioned to Zenpep from their usual PEP treatment. After a 4-14 days screening period on the current PEP, subjects received Zenpep at individually titrated doses ranging between 2,300 and 10,000 lipase units per kg body weight per day, with a mean of approximately 5000 lipase units per kg body weight per day (not to exceed 2,500 lipase units per kilogram per meal) for 14 days. There was no wash-out period. Overall, patients showed similar control of fat malabsorption by spot fecal fat testing when switched to Zenpep treatment at similar doses.
Mechanism of Action
The pancreatic enzymes in Zenpep catalyze the hydrolysis of fats to monoglycerol, glycerol and fatty acids, protein into peptides and amino acids, and starch into dextrins and short chain sugars in the duodenum and proximal small intestine, thereby acting like digestive enzymes physiologically secreted by the pancreas.
https://dailymed.nlm.nih.gov/dailymed/drugInfo.cfm?setid=556265b0-8757-11de-8a39-0800200c9a66