alvimopan


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alvimopan

(al-vi-mo-pan) ,

Entereg

(trade name)

Classification

Therapeutic: gastric stimulant
Pharmacologic: opioid antagonists
Pregnancy Category: B

Indications

Speed time to upper/lower GI recovery following partial bowel resection surgery with primary anastamosis.

Action

Acts peripherally as μ-opioid receptor antagonist which speeds recovery of bowel function after to partial large or small bowel resection surgery with anastomosis surgery.

Therapeutic effects

Accelerated time to bowel recovery following primary anastamotic surgery.

Pharmacokinetics

Absorption: 6% absorbed following oral administration.
Distribution: Does not cross the blood-brain barrier.
Protein Binding: alvimopan—80% bound to albumin; metabolite—94% bound to albumin.
Metabolism and Excretion: Converted by bacterial flora in the GI tract to an active metabolite; elimination is mostly via biliary secretion, followed by conversion by bacterial flora. Elimination of unabsorbed drug and metabolites is via feces and urine.
Half-life: alvimopan—10–17 hr; metabolite—10–18 hr.

Time/action profile (blood leves)

ROUTEONSETPEAKDURATION
POunknown2 hr12 hr

Contraindications/Precautions

Contraindicated in: Therapeutic doses of opioid analgesics for more than 7 consecutive days before initiation of alvimopan; Severe hepatic impairment or end-stage renal disease.
Use Cautiously in: More than 3 doses of opioids within the wk prior to surgery (↑ sensitivity to effects and adverse reactions including abdominal pain, nausea, vomiting and diarrhea); Mild to moderate hepatic or renal impairment (↑ risk of adverse reactions); genetic implication Japanese patients (may have ↑ risk of adverse reactions); Geriatric: May have ↑ sensitivity to effects; Obstetric / Lactation: Use in pregnancy only if clearly needed; use cautiously during lactation; Pediatric: Safety not established.

Adverse Reactions/Side Effects

Cardiovascular

  • MI (life-threatening)

Gastrointestinal

  • constipation (most frequent)
  • dyspepsia (most frequent)
  • flatulence (most frequent)

Fluid and Electrolyte

  • hypokalemia

Genitourinary

  • urinary retention

Hematologic

  • anemia

Musculoskeletal

  • back pain

Interactions

Drug-Drug interaction

Previous (within 1 wk) opioid use ↑ risk of adverse reactions (avoid if therapeutic opioid doses used during prior wk, use cautiously if more than 3 doses have been used).

Route/Dosage

Oral (Adults) 12 mg for 30 min–5 hr prior to surgery, then 12 mg twice daily for up to 15 doses.

Availability

Capsules: 12 mg

Nursing implications

Nursing assessment

  • Assess bowel sounds and frequency, quantity, and consistency of stools periodically during therapy.
  • Lab Test Considerations: May cause anemia and hypokalemia.

Potential Nursing Diagnoses

Constipation (Indications)

Implementation

  • Must be administered only during hospitalization. Only available in hospitals enrolled in the Entereg Access Support and Education (E.A.S.E.) program.
  • Oral: Administer twice daily without regard to food for no more than 7 days.

Patient/Family Teaching

  • Explain purpose of alvimopan to patient.
  • Advise patient to notify health care professional if they have taken long term or intermittent opioid pain therapy, including any use of opioids in the wk prior to receiving alvimopan.

Evaluation/Desired Outcomes

  • Resolution of postoperative ileus following bowel resection.
References in periodicals archive ?
Therapeutic use: Alvimopan (1-3) is a peripherally acting, selective mu-opioid receptor antagonist with no detectable opioidagonistic effects.
Exton PA) and GlaxoSmithKline PLC said they are pulling an application from the FDA and stopping similar studies after seeing preliminary safety data from a study of Entereg, also known as alvimopan.
SAN ANTONIO -- Alvimopan is effective in relieving gastrointestinal adverse events associated with opioid administration, according to preliminary data.
The increase in SBMs was apparent within the first week of the study, was sustained throughout the entire treatment period, and returned toward baseline when alvimopan was discontinued.
GlaxoSmithKline (LSE: GSK ; NYSE:GSK) and Adolor Corporation (NASDAQ: ADLR) today presented at the American Pain Society Meeting in San Antonio, Texas, positive results from a Phase 2b clinical study of alvimopan (Entereg), an orally administered investigational drug that blocks peripheral mu-opioid receptors(1).
The results from some of the individual studies, which had all been previously reported, failed in some cases to show a statistically significant effect from alvimopan compared with placebo, added Dr.
Because of concerns that long-term use of alvimopan may be associated with an increased risk of myocardial infarction, ENTEREG is available only for short-term (15 doses) use in hospitalized patients.
In addition, GlaxoSmithKline (Glaxo) initiated an international Phase 3 clinical program to evaluate alvimopan for the treatment of opioid-induced bowel dysfunction (OBD) in chronic pain patients.
There were more reports of myocardial infarctions in patients treated with alvimopan 0.
Key events in Adolor's history, such as the in-licensing of alvimopan and our collaboration with GlaxoSmithKline, exemplify the integral role of business development in our business model," said Mr.
In January 2005, the FDA requested that the company provide information from the GlaxoSmithKline (GSK) European Phase 3 clinical study (SB-767905/001) of alvimopan in postoperative ileus and the company indicated its goal was to deliver the information in a time frame that would allow for a PDUFA date extension.
The Phase 2b study (SB-767905/011) evaluated alvimopan for the treatment of opioid-induced bowel dysfunction (OBD), which results from the use of opioids in patients suffering from chronic pain.