【商用名】ENTEREG
【通用名】爱维莫潘胶囊

Entereg (爱维莫潘(alvimopan))胶囊使用说明

批准日期：2008年5月20日；公司：Adolor Corporation

一般描述：ENTEREG胶囊含爱维莫潘，一种外周作用μ-阿片受体(PAM－OR)拮抗剂。化学上，爱维莫潘是单一立体异构体 [[2(S)-[[4(R)-(3-hydroxyphenyl)-3(R),4-dimethyl-1-piperidinyl]methyl]-1-oxo-3- phenylpropyl] amino]acetic acid dihydrate。其结构式如下：
 
适应证：ENTEREG是一种外周作用μ-阿片受体拮抗剂适用于适用部分大或小肠外科切除与一期吻合术后上和下消化道加速恢复时间。

剂量和用法：术前30分钟至5小时给予12 mg接着每天2次直至7天，最多给药15次。

禁忌证：
ENTEREG给药前连续7天以上治疗剂量的阿片类。

不良反应：
最常见不良反应(发生率 ≥3%和≥1%安慰剂)在肠切除术患者是贫血、消化不良、低钾血症、背痛和尿潴留。

黑框警告：
仅为短期住院  ENTEREG只能为在短期(15天)住院患者买到。只有注册医院和符合取得支持和教育计划(E.A.S.E.?)的医院可以使用ENTEREG。

在特殊人群中的使用

肝功能受损：

有轻度至中度肝功能受损患者不需要调整剂量，但应被监查不良作用。对严重肝功能受损患者不推荐用ENTEREG。
肾功能受损：尚未在末期肾病患者中研究爱维莫潘。在这些患者中不推荐使用ENTEREG。轻度至严重肾功能受损患者不需要调整剂量但应监查其不良作用。

友情提示：ENTEREG为管制药。

Information on ENTEREG

WARNING: FOR SHORT-TERM HOSPITAL USE ONLY
ENTEREG is available only for short-term (15 doses) use in hospitalized patients. Only hospitals that have registered in and met all of the requirements for the ENTEREG Access Support and Education (E.A.S.E.) program may use ENTEREG.

INDICATIONS 
Entereg is an oral, peripherally-acting, mu-opioid receptor (PAMOR) antagonist. Following oral administration, alvimopan antagonizes the peripheral effects of opioids on gastrointestinal motility and secretion by competitively binding to gastrointestinal tract mu-opioid receptors.
Entereg is specifically indicated to accelerate the time to upper and lower gastrointestinal recovery following partial large or small bowel resection surgery with primary anastomosis.

USAGE Dosage
Entereg is supplied as a tablet designed for oral administration. The recommended initial dose of the drug is 12 mg administered 30 minutes to 5 hours prior to surgery followed by 12 mg twice daily beginning the day after surgery for a maximum of 7 days or until discharge. Patients should not receive more than 15 doses of Entereg. 
 
Usual Dosage in Adults
For hospital use only. The recommended adult dosage of ENTEREG is 12 mg administered 30 minutes to 5 hours prior to surgery followed by 12 mg twice daily beginning the day after surgery for a maximum of 7 days or until discharge. Patients should not receive more than 15 doses of ENTEREG.

Special Populations
Geriatric Use: No dosage adjustment is necessary in elderly patients.
Hepatic Impairment: No dosage adjustment is necessary in patients with mild-to-moderate hepatic impairment (Child-Pugh Class A and B).  ENTEREG is not recommended for use in patients with severe hepatic impairment (Child-Pugh Class C).
Renal Impairment: No dosage adjustment is necessary in patients with mild-to-severe renal impairment, but they should be monitored for adverse effects. ENTEREG is not recommended for use in patients with end-stage renal disease.
Race: No dosage adjustment is necessary in Black, Hispanic and Japanese patients, however, due to observed 2-fold greater ENTEREG plasma concentrations in healthy male Japanese subjects, Japanese patients should be monitored for possible adverse effects.
 
WARNINGS AND PRECAUTIONS
1 Myocardial Infarction in a 12 Month Study in Patients treated with Opioids for Chronic Pain
There were more reports of myocardial infarctions in patients treated with alvimopan 0.5 mg twice daily compared with placebo-treated patients in a 12-month study of patients treated with opioids for chronic pain.  In this study, the majority of myocardial infarctions occurred between 1 and 4 months after initiation of treatment.  This imbalance has not been observed in other studies of alvimopan, including studies in patients undergoing bowel resection surgery who received alvimopan 12 mg twice daily for up to 7 days.  A causal relationship with alvimopan has not been established.
2 Distribution Program for ENTEREG
ENTEREG is available only to hospitals that enroll in the E.A.S.E. program.  To enroll in the E.A.S.E. program, the hospital must acknowledge that: 
-hospital staff who prescribe, dispense, or administer ENTEREG have been provided the educational materials on the need to limit use of ENTEREG to short-term, inpatient use;
-patients will not receive more than 15 doses of alvimopan; and 
-ENTEREG will not be dispensed to patients after they have been discharged from the hospital.
3 Opioid Tolerance and Gastrointestinal-Related Adverse Effects
Patients recently exposed to opioids are expected to be more sensitive to the effects of μ-opioid receptor antagonists, such as ENTEREG.  Since ENTEREG acts peripherally, clinical signs and symptoms of increased sensitivity would likely be limited to the gastrointestinal tract (e.g., abdominal pain, nausea and vomiting, diarrhea).  Patients receiving more than 3 doses of an opioid within the week prior to surgery were not studied in the postoperative ileus clinical trials; therefore, ENTEREG 12 mg capsules should be administered with caution to these patients.
4 Severe Hepatic Impairment
In patients with severe hepatic impairment, there is a potential for 10-fold higher plasma levels of drug.  There are no studies of ENTEREG in patients with severe hepatic impairment undergoing bowel resection.  Because of the limited data available, ENTEREG is not recommended for use in patients with severe hepatic impairment.
5 End-Stage Renal Disease
No studies have been conducted with end-stage renal disease. ENTEREG is not recommended for use in these patients.
6 Bowel Obstruction
Use of ENTEREG in patients undergoing surgery for correction of complete bowel obstruction is not recommended.

ENTEREG

Indications for ENTEREG

To accelerate the time to upper and lower gastrointestinal recovery after partial large or small bowel resection surgery with primary anastomosis.

Adult dose for ENTEREG

12mg orally 30min to 5 hours before surgery, then 12mg twice daily starting on 1st post-op day for up to 7 days or until hospital discharge (max 15 doses).

Children's dosing for ENTEREG

Not recommended.

Contraindications for ENTEREG

Opioid use, at therapeutic doses, for >7 consecutive days prior.

Warnings/Precautions for ENTEREG

For hospital use only. Severe hepatic impairment or end stage renal disease: not recommended. Mild-to-severe renal dysfunction or mild-to-moderate hepatic impairment (monitor; discontinue if adverse reactions occur). Recent (within 1 week) use of more than 3 doses of opioids. Pregnancy (Cat.B). Nursing mothers.

Adverse Reactions for ENTEREG

Dyspepsia, constipation, flatulence, back pain, urinary retention.

Notes for ENTEREG

Available only to hospitals that enroll in Entereg Access and Support Program (EASE). For more information, and to enroll, call (866)-4ADOLOR.

How is ENTEREG supplied?

Caps—30

【-原产地英文商品名-】ENTEREG 12 MG CAPSULE
【-原产地英文药品名-】ALVIMOPAN
【-原产地英文化合物名称】[[(2S)-2-[[(3R,4R)-4-(3- hydroxyphenyl)-3,4-dimethylpiperidin-1-yl] methyl]-3-phenylpropanoyl]amino]
【-中文参考商品名-】ENTEREG胶囊 12毫克/粒 30粒/盒
【-中文参考药品名-】爱维莫潘
【-中文参考化合物名称-】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
【-临床试验期-】完成
【-中文适应病症参考】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
【-批准有效期-】两年
【-生产厂家中文参考】ADOLOR
【-生产厂家英文名-】ADOLOR