Version May 2024
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.
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 Alvimopan REMS Program.
Note: For short-term hospital use only.
Postoperative ileus: Oral: 12 mg 30 minutes to 5 hours prior to surgery, followed by 12 mg twice daily beginning the day after surgery until discharge for a maximum of 7 days (maximum total treatment: 15 doses [180 mg total])
Mild to severe impairment: No dosage adjustment necessary; use with caution.
ESRD: Use not recommended.
Mild to moderate impairment (Child-Pugh class A or B): No dosage adjustment necessary; use with caution.
Severe impairment (Child-Pugh class C): Use not recommended.
Refer to adult dosing.
The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. 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
Use of opioids at therapeutic doses for more than 7 consecutive days immediately prior to alvimopan
Significant drug interactions exist, requiring dose/frequency adjustment or avoidance. Consult drug interactions database for more information.
Concerns related to adverse effects:
• Cardiovascular effects: [US Boxed Warning]: A trend towards an increased incidence of myocardial infarction (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 to 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 end-stage renal disease.
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: [US Boxed Warning]: For short-term (≤15 doses) use through the Alvimopan REMS Program. Only hospitals that have enrolled in and met all requirements for the program may use alvimopan (further information is available at https://www.alvimopanrems.com or 1-800-278-0340). The Alvimopan REMS Program restricts use to hospitalized patients; it will not be dispensed to patients who have been discharged from the hospital.
Excipient information presented when available (limited, particularly for generics); consult specific product labeling.
Capsule, Oral:
Entereg: 12 mg
Generic: 12 mg
Yes
Capsules (Alvimopan Oral)
12 mg (per each): $188.53 - $207.30
Capsules (Entereg Oral)
12 mg (per each): $218.21
Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.
Oral: For short-term hospital use only. Administer first dose 30 minutes to 5 hours prior to surgery. May be administered without regard to food.
Postoperative ileus: To accelerate the time to upper and lower GI recovery following surgeries including partial bowel resection with primary anastomosis
Alvimopan may be confused with almotriptan
None known.
Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.
Loperamide: May enhance the adverse/toxic effect of Alvimopan. Specifically, alvimopan gastrointestinal adverse effects may be increased. Loperamide may diminish the therapeutic effect of Alvimopan. Management: Consider avoiding coadministration of alvimopan and loperamide due to the risk of gastrointestinal adverse effects and pharmacologic antagonism. Risk D: Consider therapy modification
Methylnaltrexone: May enhance the adverse/toxic effect of Opioid Antagonists. Specifically, the risk for opioid withdrawal may be increased. Risk X: Avoid combination
Naldemedine: Opioid Antagonists may enhance the adverse/toxic effect of Naldemedine. Specifically, the risk for opioid withdrawal may be increased. Risk X: Avoid combination
Naloxegol: Opioid Antagonists may enhance the adverse/toxic effect of Naloxegol. Specifically, the risk for opioid withdrawal may be increased. Risk X: Avoid combination
Opioid Agonists: 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. Risk D: Consider therapy modification
When administered with a high-fat meal, extent and rate of absorption may be reduced (Cmax and AUC decreased by ~38% and 21%, respectively). Management: May administer with or without food.
Adverse events have not been observed in animal reproduction studies.
It is not known if alvimopan is present in breast milk.
According to the manufacturer, the decision to breastfeed during therapy should consider the risk of infant exposure, the benefits of breastfeeding to the infant, and benefits of treatment to the mother.
High-fat meals may decrease the rate and extent of absorption
GI adverse reactions (eg, abdominal pain, cramping, diarrhea) in patients receiving more than 3 doses of an opioid within the week prior to surgery, patients with mild to moderate hepatic impairment, with severe renal impairment, or in patients who are Japanese.
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 to 40 L
Protein binding: Parent drug: 80%; metabolite: 94% (both primarily to albumin)
Metabolism: Hydrolyzed to an amide hydrolysis compound (active metabolite) by gut microflora; further metabolism of active metabolite to glucuronide conjugates and other minor metabolites.
Bioavailability: ~6% (range: 1% to 19%)
Half-life elimination: 10 to 17 hours
Time to peak, plasma: Parent drug: ~2 hours; Metabolite: 36 hours
Excretion: Urine (~35% as unchanged drug and metabolites); feces (via biliary excretion)
Altered kidney function: 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.
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.
آیا می خواهید مدیلیب را به صفحه اصلی خود اضافه کنید؟
