葛兰素史克制药公司（GSK）及Adolor公司合作开发的肠道疾病治疗新药Entereg（爱维莫潘alvimopan）通过了美国FDA的批准，该药用于治疗腹部外科手术后出现的肠梗阻。一些患者在接受肠切除术之后通常会出现肠梗阻，导致肠道排便、排气障碍。Entereg可以促进肠道机能的恢复，让患者能在术后尽早恢复正常饮食。
Entereg(爱维莫潘,Alvimopan)在临床研究的各项资料研究都表明，对在临床应用的效果显著。
属于外周阿片受体拮抗剂，其与甲基纳屈酮的组织分布形式不同,仅可与胃肠壁上的阿片受体结合,且由于只能口服才能起效而仅有口服剂型。该药与μ受体的亲和力强于κ受体及σ受体,且与μ受体的亲和力比纳洛酮强。

【商用名】Entereg
【通用名】爱维莫潘胶囊
【商品英文名】Entereg
【英文名】Alvimopan Capsule
【汉语拼音】AiWeiMoPanJiaoNang
【化学名】2-([(2S)-2-([(3R,4R)-4-(3-羟基苯基)-3,4-二甲基哌啶-1-基]甲基)-3-苯基丙酰]氨基)乙酸。
【分子式】C25H36N2O6
【分子量】424.53
【主要成分】爱维莫潘
【性状】本品为胶囊剂，胶囊为谈蓝色，胶囊外壳上有黑色墨水印的“ADL2698”字样。
【适应症】爱维莫潘可促进大肠或小肠部分切除一期吻合术后患者胃肠道功能的恢复，是FDA批准的首个也是迄今惟一一直用于该适应症的药物。
【用量用法】成人推荐给药方案为：术前30分钟至5小时口服12mg，术后第一天开始，12mg/次，1天2次，连续给药7天，且仅限于住院患者短期使用（最多服用15次）。
【药理毒理】爱维莫潘经口服给药后可与胃肠道μ-阿片受体竞争性结合，对阿片类镇痛药的胃肠道副反应产生拮抗作用，同时不会影响后者的中枢镇痛效应。而且，其在体内循环中会出现一种酰胺水解物。一般将这种酰胺水解物当作是爱维莫潘的“代谢物”，但实际上，它是肠内菌群代谢的特有产物，同时它也是一种μ-阿片受体拮抗剂，Ki为0.8nM（0.3ng/mL）。这种“代谢物”中位达峰时间为36小时，其血浆浓度个体差异很大；爱维莫潘12mg，1天2次，连续5天给药后，此“代谢物”血浆浓度在体内出现蓄积，其平均峰浓度为35.73±35.29ng/mL。与健康受试者相比，爱维莫潘及其“代谢物”在术后感染（POI）病人体内的血浆浓度更高（分别达到前者的1.9倍和1.4倍左右）。
【药代动力学】爱维莫潘是一种外周性μ-阿片受体拮抗剂，Ki为0.4nM（0.2ng/mL）。体外研究显示，爱维莫潘在1～10μM浓度范围内，对70多种非阿片受体、酶及离子通道无活性。
【不良反应】在临床试验中，爱维莫潘组发生率超过3%的不良事件主要包括：贫血、胃气胀、消化不良、便秘、低血钾、背痛和尿潴留等。
【注意事项】高脂饮食会影响爱维莫潘口服吸收的程度和速度，其峰浓度和AUC会因此而分别降低大约38%和21%，达峰时间会因此而延长1小时左右。
【禁忌】在服用爱维莫潘前，给予治疗剂量阿片类药物连续治疗7天以上的患者。
【药物相互作用】体外研究显示，爱维莫潘不是细胞色素P450酶系和P糖蛋白的底物、抑制剂或诱导剂，因此，爱维莫潘与细胞色素P450酶系和P糖蛋白的底物、抑制剂或诱导剂之间不存在具有临床意义的相互作用。群体药代动力学研究显示，爱维莫潘的药代动力学不受抗酸药或抗生素的影响，但爱维莫潘“代谢物”的血浆浓度在服用抗酸药或术前口服抗生素的患者中明显下降（分别降低49%和81%），不过，由于爱维莫潘“代谢物”对患者临床疗效影响不大，因此，上述患者无需改变给药剂量。爱维莫潘是一种外周性μ-阿片受体拮抗剂，不会引起药物滥用或药物依赖性问题。
【批准文号】
【规格】12mg/粒*30粒/盒
【贮藏】密封，阴凉干燥保存。
【有效期】两年。
【生产商】葛兰素史克公司
ENTEREG CAP 12MG (D/S INST) 30

Entereg

Generic name: Alvimopan

What is Entereg?

Entereg is used to accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis.

What is the most important information I should know about Entereg?

Entereg is only used in a hospital setting and for no more than 7 days after bowel resection surgery.

Who should not take Entereg?

Do not take Entereg if you have taken any opioid medication for more than 7 consecutive days immediately prior to taking Entereg. Do not take Entereg if you have any kidney or liver problems. Safety has not been established in children.

What should I tell my doctor before I take the first dose of Entereg?

Tell your doctor about all prescription, over-the-counter, and herbal medications you are taking before beginning treatment with Entereg. Also, talk to your doctor about your complete medical history, especially if you have a history of kidney or liver problems, or are pregnant or breastfeeding. Tell your doctor if you have taken any opioid medication for more than 7 consecutive days immediately prior to taking Entereg.

What is the usual dosage?

The information below is based on the dosage guidelines your doctor uses. Depending on your condition and medical history, your doctor may prescribe a different regimen. Do not change the dosage or stop taking your medication without your doctor's approval.

Adults: The typical dose is 12 milligrams (mg) given 30 minutes to 5 hours prior to surgery, followed by 12 mg twice daily for up to 7 days for a maximum of 15 doses.

How should I take Entereg?

Take Entereg before eating, as prescribed by your doctor.

What should I avoid while taking Entereg?

Avoid the use of any opioid medications before or during treatment with Entereg.

What are possible food and drug interactions associated with Entereg?

If Entereg is taken with certain other drugs, the effects of either could be increased, decreased, or altered. It is especially important to check with your doctor before combining Entereg with high-fat meals or opioids.

What are the possible side effects of Entereg?

Side effects cannot be anticipated. If any develop or change in intensity, tell your doctor as soon as possible. Only your doctor can determine if it is safe for you to continue taking this drug.

Side effects may include: anemia, constipation, dyspepsia, flatulence, low potassium levels, back pain, urinary retention

Can I receive Entereg if I am pregnant or breastfeeding?

Avoid Entereg during pregnancy and breastfeeding. Talk with your doctor before taking this drug if you are pregnant, plan to become pregnant, or are breastfeeding.

What should I do if I miss a dose of Entereg?

Entereg is only administered in a hospital setting.

How should I store Entereg?

Entereg is only administered in a hospital setting.