Dosing and uses of Entereg (alvimopan)
Adult dosage forms and strengths
capsule
- 12mg
GI Recovery Post Bowel Resection
Indicated to accelerate time to upper and lower GI recovery following surgeries that include partial bowel resection with primary anastomosis
12 mg PO administered 30 minutes to 5 hours preoperative, THEN 12 mg PO q12hr beginning 1 day after surgery until discharge for a maximum of 7 days; patients should not receive >15 doses
Renal Impairment
Mild to severe impaiment: No dose adjustment necessary; use caution
Hepatic Impairment
Mild to moderate impairment: No dose adjustment necessary
Severe impairment: Use not recommended
Pediatric dosage forms and strengths
Safety and efficacy not established
Entereg (alvimopan) adverse (side) effects
1-10%
Constipation (10%)
Hypokalemia (9.5%)
Flatulence (8.7%)
Dyspepsia (7%)
Anemia (5.4%)
Back pain (3.4%)
Warnings
Black box warnings
Increased incidence of myocardial infarction was seen in a clinical trial of patients taking alvimopan for long-term use
Alvimopan is available only for short-term use (not to exceed 15 doses) in hospitalized patients
Only hospitals that have registered in and met all of the requirements for the Entereg (alvimopan) Access Support and Education (E.A.S.E) program may use this drug
Contact: 1-866-4ADOLOR (1-866-423-6567)
Contraindications
Taken >7 day of therapeutic opioids prior to taking alvimopan
>15 doses
Non-hospitalized patients
Cautions
Higher risk for MI observed in studies with long-term use (eg, chronic noncancer pain); not observed with postsurgical short-term use
Not recommended in severe hepatic impairment (10-fold higher serum levels), ESRD, bowel obstruction corrective surgery
Not studied in patients having pancreatic or gastric anastomosis; therefore, not recommended for use in these patients
Patients recently exposed to opioids are expected to be more sensitive to the effects of mu-opioid receptor antagonists, symptoms may include abdominal pain, nausea, vomiting, and diarrhea (see Contraindications)
High-fat meal reduces absorption
Available on through a restricted access program (see Black box warnings)
Pregnancy and lactation
Pregnancy category: B
Lactation: excretion in milk unknown; use with caution
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Entereg (alvimopan)
Mechanism of action
Peripheral mu-opioid receptor antagonist; limited ability to cross blood brain barrier so doesn't abolish opioid-induced analgesia nor cause withdrawal symptoms but decreases opioid-induced constipation
Pharmacokinetics
Peak Plasma Time: 2 hr
Bioavailability: 6%
Vd: 20-40 L
Protein Bound: drug 80%; metabolite 94%
Total Clearance: 402 mL/min
Half-Life, Terminal: 10-17 hr
Metabolism: Not by liver, gut microflora hydrolyzes to a metabolite
Excretion: Feces (via biliary excretion) & urine (35%)
