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Alvimopan


General


Pronunciation

(al VI moe pan)


Brand Names: U.S.

  • Entereg

Indications


Use: Labeled Indications

Postoperative ileus: To accelerate the time to upper and lower GI recovery following surgeries including partial bowel resection with primary anastomosis


Contraindications


Patients who have taken therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan


ALERT: U.S. Boxed Warning

Myocardial infarction:

There was a greater incidence of myocardial infarction (MI) in alvimopan-treated patients compared to placebo-treated patients in a 12-month clinical trial, although a causal relationship has not been established. In short-term trials with alvimopan, no increased risk of MI was observed.

Appropiate use:

Because of the potential risk of MI with long-term use, alvimopan is available only through a restricted program for short-term use (15 doses) under a Risk Evaluation and Mitigation Strategy (REMS) called the ENTEREG Access Support and Education (E.A.S.E.) Program.


Dosing and Administration


Dosing: Adult

Note: For hospital use only.

Management of postoperative ileus: Oral:

Initial: 12 mg administered 30 minutes to 5 hours prior to surgery

Maintenance: 12 mg twice daily beginning the day after surgery for a maximum of 7 days or until discharged from hospital (maximum total treatment: 15 doses)


Dosing: Geriatric

Refer to adult dosing.


Dosing: Renal Impairment

Mild-to-severe impairment: No adjustment needed; use caution.

ESRD: Use not recommended.


Dosing: Hepatic Impairment

Mild-to-moderate impairment (Child-Pugh class A or B): No adjustment needed; use caution.

Severe impairment (Child-Pugh class C): Use not recommended.


Administration

Patient must be hospitalized. Initial dose should be administered 30 minutes to 5 hours prior to surgery. May be administered with or without food.


Dietary Considerations

Take with or without food; high-fat meals may decrease the rate and extent of absorption


Storage

Store at 25 ‚ °C (77 ‚ °F); excursions permitted to 15 ‚ °C to 30 ‚ °C (59 ‚ °F to 86 ‚ °F).


Dosage Forms/Strengths


Dosage Forms

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Capsule, Oral:

Entereg: 12 mg


Drug Interactions

Analgesics (Opioid): May enhance the adverse/toxic effect of Alvimopan. This is most notable for patients receiving long-term (i.e., more than 7 days) opiates prior to alvimopan initiation. Management: Alvimopan is contraindicated in patients receiving therapeutic doses of opioids for more than 7 consecutive days immediately prior to alvimopan initiation. Consider therapy modification

Methylnaltrexone: May enhance the adverse/toxic effect of Opioid Antagonists. Specifically, the risk for opioid withdrawal may be increased. Avoid combination

Naloxegol: Opioid Antagonists may enhance the adverse/toxic effect of Naloxegol. Specifically, the risk for opioid withdrawal may be increased. Avoid combination


Adverse Reactions


Note: Incidence reported limited to bowel resection patients only.

1% to 10%:

Endocrine & metabolic: Hypokalemia (10%)

Gastrointestinal: Dyspepsia (2% to 7%)

Genitourinary: Urinary retention (3%)

Hematologic and oncologic: Anemia (5%)

Neuromuscular & skeletal: Back pain (3%)

Frequency not defined:

Cardiovascular: Myocardial infarction


Warnings/Precautions


Special Populations: Renal Function Impairment

The half-life was comparable in patients with mild or moderate renal function impairment. There may be drug accumulation in patients with severe renal function impairment receiving multiple doses.


Special Populations: Hepatic Function Impairment

Drug exposure tended to be higher in patients with mild or moderate hepatic function impairment compared with healthy controls. There were no consistent effects on Cmax or half-life in patients with hepatic function impairment.


Warnings/Precautions

Concerns related to adverse effects:

- Cardiovascular effects: [U.S. Boxed Warning]: A trend towards an increased incidence of MI was observed in alvimopan (low dose) treated patients compared to placebo in a 12-month study in patients treated with opioids for chronic pain. Other short-term studies have not observed this trend and a causal relationship has not been found. MI was generally observed more frequently in the initial 1-4 months of treatment.

Disease-related concerns:

- Anastomosis: Use not recommended in patients having gastric or pancreatic anastomosis.

- Complete bowel obstruction: Use not recommended in patients undergoing surgery for complete bowel obstruction.

- Hepatic impairment: Use with caution in patients with mild-to-moderate hepatic impairment (Child-Pugh classes A and B); use not recommended with severe impairment (Child-Pugh class C).

- Renal impairment: Use with caution in patients with renal impairment; use not recommended in patients with ESRD.

Concurrent drug therapy issues:

- Opioids: Use with caution in patients recently exposed to opioids; may be more sensitive to gastrointestinal adverse effects (eg, abdominal pain, diarrhea, nausea and vomiting). Contraindicated in patients who have received therapeutic opioids for >7 consecutive days immediately prior to use.

Special populations:

- Japanese patients: Patients of Japanese descent should be monitored closely for gastrointestinal side effects (eg, abdominal pain, cramping, diarrhea) due to possibility of greater drug exposure; discontinue use if side effects occur.

Other warnings/precautions:

- Appropriate use: [U.S. Boxed Warning]: For short-term ( ≤15 doses) hospital use only. Only hospitals that have registered through the ENTEREG Access Support and Education (E.A.S.E. ¢ „ ¢) Program and met all requirements may use. It will not be dispensed to patients who have been discharged from the hospital.


Pregnancy Risk Factor

B


Pregnancy Considerations

Adverse events have not been observed in animal reproduction studies.


Actions


Pharmacology

An opioid receptor antagonist which blocks opioid binding at the mu receptor; alvimopan has restricted ability to cross the blood-brain barrier at therapeutic doses. It selectively and competitively binds to the GI tract mu opioid receptors and antagonizes the peripheral effects of opioids on gastrointestinal motility and secretion. Does not affect opioid analgesic effects or induce opioid withdrawal symptoms.


Distribution

Vd: 20-40 L


Metabolism

Hydrolyzed to an amide hydrolysis compound (active metabolite) by gut microflora; further metabolism of active metabolite to glucuronide conjugates and other minor metabolites


Excretion

Urine (~35% as unchanged drug and metabolites); feces (via biliary excretion)


Time to Peak

Plasma: Parent drug: ~2 hours; Metabolite: 36 hours


Half-Life Elimination

10-17 hours


Protein Binding

Parent drug: 80%; metabolite: 94% (both primarily to albumin)


Patient and Family Education


Patient Education

- Discuss specific use of drug and side effects with patient as it relates to treatment. (HCAHPS: During this hospital stay, were you given any medicine that you had not taken before? Before giving you any new medicine, how often did hospital staff tell you what the medicine was for? How often did hospital staff describe possible side effects in a way you could understand?)

- Patient may experience flatulence. Have patient report immediately to prescriber signs of low potassium (muscle pain or weakness, muscle cramps, or an abnormal heartbeat), severe constipation, loss of strength and energy, angina, tachycardia, severe dizziness, passing out, severe headache, severe nausea, vomiting, bradycardia, severe abdominal pain, abdominal cramps, urinary retention, or change in amount of urine passed (HCAHPS).

- Educate patient about signs of a significant reaction (eg, wheezing; chest tightness; fever; itching; bad cough; blue skin color; seizures; or swelling of face, lips, tongue, or throat). Note: This is not a comprehensive list of all side effects. Patient should consult prescriber for additional questions.

Intended Use and Disclaimer: Should not be printed and given to patients. This information is intended to serve as a concise initial reference for healthcare professionals to use when discussing medications with a patient. You must ultimately rely on your own discretion, experience and judgment in diagnosing, treating and advising patients.

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