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Alvimopan (Monograph)

Brand name: Entereg
Drug class: Opioid Antagonists

Medically reviewed by Drugs.com on May 10, 2024. Written by ASHP.

Warning

Risk Evaluation and Mitigation Strategy (REMS):

FDA approved a REMS for alvimopan to ensure that the benefits outweigh the risks. The REMS may apply to one or more preparations of alvimopan and consists of the following: elements to assure safe use and implementation system. (See Restricted Distribution Program under Dosage and Administration.) See https://www.accessdata.fda.gov/scripts/cder/rems/.

Warning

  • Only for short-term (15 doses) use in hospitalized patients. (See MI under Cautions.)

  • For use only by hospitals enrolled in the Entereg Access Support and Education (EASE) program. (See Restricted Distribution Program under Dosage and Administration.)

Introduction

Peripherally acting μ-opiate receptor antagonist.

Uses for Alvimopan

Postoperative Ileus

Acceleration of upper and lower GI recovery following partial large or small bowel resection with primary anastomosis.

Efficacy for management of postoperative ileus in women undergoing total abdominal hysterectomy [off-label] under general anesthesia not established to date.

Alvimopan Dosage and Administration

General

Restricted Distribution Program

Administration

Oral Administration

Preoperative dose administered in fasting patients in clinical studies; postoperative doses administered without regard to meals in studies.

Dosage

Available as alvimopan dihydrate; dosage expressed in terms of anhydrous alvimopan.

Adults

Postoperative Ileus
Oral

12 mg administered 0.5–5 hours prior to surgery followed by 12 mg twice daily beginning the day after surgery for a maximum of 7 days or until discharge.

Administer no more than 15 doses.

Prescribing Limits

Adults

Postoperative Ileus
Oral

Maximum of 15 doses over 7 days postoperatively in hospitalized patients.

Special Populations

Hepatic Impairment

No dosage adjustment required in patients with mild to moderate hepatic impairment (Child-Pugh class A or B). Not recommended in severe hepatic impairment. (See Hepatic Impairment under Cautions.)

Renal Impairment

No dosage adjustment required in patients with mild to severe renal impairment. Not recommended in patients with end-stage renal disease. (See Renal Impairment under Cautions.)

Geriatric Patients

Dosage adjustment based on age not needed.

Crohn’s Disease

No dosage adjustment required. (See Special Populations under Pharmacokinetics.)

Cautions for Alvimopan

Contraindications

Warnings/Precautions

Restricted Distribution Program

Only for short-term (15 doses) use in hospitalized patients. For use only by hospitals enrolled in the EASE program. (See Restricted Distribution Program under Dosage and Administration.)

MI

May be associated with increased incidence of MI when used long term; not found with short-term (i.e., ≤7 days) use following bowel resection. Causal relationship not established. (See Boxed Warning and see Restricted Distribution Program under Dosage and Administration.)

Recent Opiate Use

Increased sensitivity to alvimopan possible with recent exposure to opiates; manifests principally as GI symptoms (e.g., abdominal pain, nausea, vomiting, diarrhea). Use caution in patients who have received >3 doses of an opiate within 1 week prior to surgery. (See Contraindications under Cautions.)

Bowel Obstruction

Not recommended for use in patients undergoing surgical correction of complete bowel obstruction.

Specific Populations

Pregnancy

Category B.

Lactation

Distributed into milk in rats; not known whether distributed into human milk. Use caution.

Pediatric Use

Safety and efficacy not established in children <18 years of age.

Geriatric Use

No substantial differences in safety and efficacy relative to younger adults, but increased sensitivity cannot be ruled out.

Hepatic Impairment

Slight increase in plasma alvimopan concentrations possible in patients with mild to moderate hepatic impairment (Child-Pugh class A or B). Monitor for adverse effects (e.g., diarrhea, abdominal pain or cramping) that may indicate alvimopan or metabolite accumulation; discontinue if such effects occur. (See Hepatic Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Use not recommended in patients with severe hepatic impairment (Child-Pugh class C). Substantially increased plasma concentrations possible.

Renal Impairment

Monitor for possible adverse effects in patients with renal impairment. Closely monitor those with severe renal impairment for adverse effects (e.g., diarrhea, abdominal pain or cramping) that may indicate elevated alvimopan or metabolite concentrations; discontinue if such effects occur. (See Renal Impairment under Dosage and Administration and see Special Populations under Pharmacokinetics.)

Not studied in patients with end-stage renal disease. Use not recommended.

Common Adverse Effects

Constipation, hypokalemia, flatulence, dyspepsia, anemia, back pain, urinary retention.

Drug Interactions

Does not inhibit CYP isoenzymes 1A2, 2C9, 2C19, 3A4, 2D6, or 2E1 or induce isoenzymes 1A2, 2B6, 2C9, 2C19, or 3A4.

Alvimopan does not inhibit P-glycoprotein; alvimopan and its metabolite are substrates for P-glycoprotein.

Drugs Affecting or Metabolized by Hepatic Microsomal Enzymes

Pharmacokinetic interaction unlikely.

Drugs Affecting or Affected by P-glycoprotein Transport

Pharmacokinetic interactions unlikely with mild-to-moderate P-glycoprotein inhibitors. The effect of potent P-glycoprotein inhibitors is unknown.

Pharmacokinetic interactions with P-glycoprotein substrates are unlikely.

Specific Drugs

Drug

Interaction

Comments

Antibiotics (preoperative oral antibiotics)

Decreased plasma concentrations of alvimopan metabolite; no alteration in alvimopan pharmacokinetics

No dosage adjustment necessary

Histamine H2-receptor antagonists

Decreased plasma concentrations of alvimopan metabolite; no alteration in alvimopan pharmacokinetics

No dosage adjustment necessary

Morphine

Pharmacokinetic interaction unlikely (no change in morphine pharmacokinetics); alvimopan does not reverse analgesic effects

No dosage adjustment necessary

Proton-pump inhibitors

Decreased plasma concentrations of alvimopan metabolite; no alteration in alvimopan pharmacokinetics

No dosage adjustment necessary

Alvimopan Pharmacokinetics

Absorption

Bioavailability

Absolute bioavailability averages 6% (range 1–19%).

Food

High-fat meal decreases rate and extent of absorption.

Distribution

Extent

Does not readily cross blood-brain barrier.

Distributed into milk in rats; not known whether distributed into human milk.

Plasma Protein Binding

Alvimopan: 80%. Metabolite: 94%. Bound to albumin.

Elimination

Metabolism

Metabolized by intestinal flora to active metabolite; metabolite not required for pharmacologic activity.

No substantial hepatic metabolism.

Elimination Route

Excreted principally via biliary secretion (65%) and in the urine (35%).

Half-life

10–17 hours.

Special Populations

Exposure to alvimopan is 1.5-fold to twofold higher in patients with mild or moderate hepatic impairment (Child-Pugh class A or B); accumulation possible after multiple doses. Exposure may be increased approximately tenfold in patients with severe hepatic impairment (Child-Pugh class C).

Exposure to metabolite is twofold to fivefold higher in patients with moderate or severe renal impairment. Alvimopan half-life is prolonged in patients with severe renal impairment. Accumulation of alvimopan and metabolite is possible after multiple doses in patients with severe renal impairment. Not studied in patients with end-stage renal disease.

Exposure to alvimopan is twofold higher in patients with quiescent Crohn’s disease relative to healthy individuals or those with active Crohn’s disease; metabolite concentrations are lower in patients with Crohn’s disease.

Stability

Storage

Oral

Capsules

25°C (may be exposed to 15–30°C).

Actions

Advice to Patients

Additional Information

The American Society of Health-System Pharmacists, Inc. represents that the information provided in the accompanying monograph was formulated with a reasonable standard of care, and in conformity with professional standards in the field. Readers are advised that decisions regarding use of drugs are complex medical decisions requiring the independent, informed decision of an appropriate health care professional, and that the information contained in the monograph is provided for informational purposes only. The manufacturer’s labeling should be consulted for more detailed information. The American Society of Health-System Pharmacists, Inc. does not endorse or recommend the use of any drug. The information contained in the monograph is not a substitute for medical care.

Preparations

Excipients in commercially available drug preparations may have clinically important effects in some individuals; consult specific product labeling for details.

Please refer to the ASHP Drug Shortages Resource Center for information on shortages of one or more of these preparations.

Distribution of alvimopan is restricted. (See Restricted Distribution Program under Dosage and Administration.)

Alvimopan

Routes

Dosage Forms

Strengths

Brand Names

Manufacturer

Oral

Capsules

12 mg (of anhydrous alvimopan)

Entereg

Adolor

AHFS DI Essentials™. © Copyright 2024, Selected Revisions May 10, 2024. American Society of Health-System Pharmacists, Inc., 4500 East-West Highway, Suite 900, Bethesda, Maryland 20814.

† Off-label: Use is not currently included in the labeling approved by the US Food and Drug Administration.

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Frequently asked questions