(trade name)


Therapeutic: laxatives
Pharmacologic: opioid antagonists
Pregnancy Category: C


Treatment of opioid-caused constipation (OIC) in patients receiving chronic opioids for chronic non-cancer pain when traditional laxatives have failed.


Acts peripherally as a mu receptor antagonist, blocking opioid receptors in the GI tract.

Therapeutic effects

Blocks constipating effects of opioids on the GI tract without loss of analgesia.


Absorption: Systemic absorption follows oral administration. A high-fat meal ↑ absorption.
Distribution: Does not cross the blood-brain barrier.
Metabolism and Excretion: Metabolized primarily by the CYP3A4 enzyme system; 68% excreted in feces, 16% in urine mostly as metabolites.
Half-life: 6–11 hr.

Time/action profile (spontaneous bowel movement)

POwithin 24 hrunknownunknown


Contraindicated in: Hypersensitivity; Known/suspected/history of gastrointestinal obstruction; Severe hepatic impairment; Concurrent use of strong CYP3A4 inhibitors, strong CYP3A4 inducers, other opioid antagonists or grapefruit/grapefruit juice; Severe hepatic impairment; Lactation: May precipitate opioid withdrawal in infant.
Use Cautiously in: Patients with disruption of the blood-brain barrier (may precipitate opioid withdrawal); Geriatric: Blood levels are ↑ in elderly Japanese patients; Obstetric: May precipitate fetal opioid withdrawal (use only if potential benefit justifies potential risk to fetus); Pediatric: Safe and effective use in children has not been established.

Adverse Reactions/Side Effects

Central nervous system

  • headache


  • gastrointestinal perforation (life-threatening)
  • abdominal pain (most frequent)
  • diarrhea
  • flatulence
  • nausea
  • vomiting


  • sweating


  • opioid withdrawal


Drug-Drug interaction

Concurrent use of strong CYP3A4 inhibitors including clarithromycin and ketoconazole ↑ risk of toxicity/adverse reactions and is contraindicated.Concurrent use of moderate CYP3A4 inhibitors including diltiazem, erythromycin, and verapamil may also↑ risk of toxicity/adverse reactions; dose reduction and careful monitoring recommended.Concurrent use of strong CYP3A4 inducers including rifampin may ↓ blood levels/effectiveness and is contraindicated.Concurrent use of other opioid antagonists may precipitate opioid withdrawal and is contraindicated.Concurrent use of methadone for pain ↑ risk of stomach pain and diarrhea.Grapefruit/grapefruit juice may ↑ blood levels and the risk of toxicity/adverse reactions and should be avoided.


Oral (Adults) 25 mg once daily, if poorly tolerated decrease dose to 12.5 mg; concurrent use of moderate CYP3A4 inhibitors—12.5 mg daily (careful monitoring recommended).

Renal Impairment

Oral (Adults) CCr <60 mL/min—12.5 mg daily initially, may be cautiously increased to 25 mg/day if necessary with careful monitoring.


Tablets: 12.5 mg, 25 mg

Nursing implications

Nursing assessment

  • Assess bowel sounds and frequency, quantity, and consistency of stools periodically during therapy.
  • Monitor pain intensity during therapy. Naloxegol does not affect pain or effects of opioid analgesics on pain control. Discontinue naloxegol if opioid analgesic is discontinued.
  • Monitor for signs and symptoms of gastrointestinal perforation (severe, persistent or worsening abdominal pain) periodically during therapy. Discontinue naloxegol if symptoms occur.

Potential Nursing Diagnoses

Constipation (Indications)
Diarrhea (Adverse Reactions)


  • Discontinue all maintenance laxative therapy before starting naloxegol. If a suboptimal response occurs with naloxegol, laxatives may be used after 3 days.
  • Oral: Administer on an empty stomach at least 1 hr before first meal in morning or 2 hrs after meal. Swallow tablet whole; do not break, crush, or chew.
    • Avoid grapefruit and grapefruit juice during therapy.

Patient/Family Teaching

  • Instruct patient to take naloxegol on an empty stomach as directed. Laxatives should be stopped before starting naloxegol, but may be restarted after 3 days if needed. Advise patient to read Medication Guide prior to starting therapy and with each refill in case of changes.
  • Caution patient to avoid grapefruit and grapefruit juice during therapy.
  • Advise patient to notify health care professional immediately if stomach pain that does not go away occurs.
  • Advise patient to notify health care professional if signs and symptoms of opioid withdrawal (sweating, chills, diarrhea, stomach pain, anxiety, irritability, yawning) occur. Patients taking methadone for pain are at increased risk for stomach pain and diarrhea.
  • Instruct patient to stop taking naloxegol if they stop taking opioid medications.
  • Instruct patient to notify health care professional of all Rx or OTC medications, vitamins, or herbal products being taken and consult health care professional before taking any new medications.
  • Advise female patients to notify health care professional if pregnancy is planned or suspected or if breastfeeding.

Evaluation/Desired Outcomes

  • Relief of opioid induced constipation, especially if opioid therapy has been for 4 wks or more.
References in periodicals archive ?
At the present time, three of these agents are not yet available: finafloxacin otic suspension (Xtoro) for acute otitis externa, naloxegol (Movantik) for opioid-induced constipation in adults with chronic noncancer pain, and peginterferon beta-la (Plegridy) for relapsing multiple sclerosis.
LONDON, June 19, 2014 /PRNewswire/ -- AstraZeneca today announced that the New England Journal of Medicine (NEJM) has published results of two pivotal Phase III studies - KODIAC-4 and KODIAC-5 of naloxegol, an investigational treatment for opioid-induced constipation (OIC).
Naloxegol, which has the potential to be the first FDA approved once-daily oral treatment for patients with OIC, is a peripherally-acting mu-opioid receptor antagonist (PAMORA) studied in adult patients with chronic non-cancer pain experiencing OIC.
Primary endpoint data from the KODIAC-4 and -5 studies showed that more OIC patients treated with naloxegol 25 mg had a consistent response of increased spontaneous bowel movements (SBMs) through 12 weeks of treatment compared to placebo[44% vs.
Washington, June 8 ( ANI ): A new research has revealed that the drug naloxegol may be able to help patients suffering constipation caused by pain relief medicines.
Naloxegol is an investigational peripherally-acting mu-opioid receptor antagonist, which has been specifically designed for the treatment of opioid-induced constipation (OIC), a common and often debilitating side effect of prescription medicines used to treat osteoarthritis and chronic back pain.
Others include Plecanatide, Xifaxan (rifaximin), Asimadoline and Naloxegol (PEG-naloxol), most of which have demonstrated high safety and efficacy profiles in clinical trials.
Treatment with opioid receptor-antagonist naloxegol significantly improved opioid-associated constipation, compared with placebo, without affecting pain scores or daily opioid requirements, according to data from two identical double-blind studies.
Outpatients with noncancer pain who were given 25 mg of naloxegol showed a significantly shorter time to first spontaneous bowel movement after treatment, compared with those given placebo--a median time of 5.
Treatment with naloxegol was also associated with a significantly greater number of spontaneous bowel movements over the course of the 12-week study period, compared with placebo, and an increase in the mean number of days per week with one or more spontaneous bowel movements.
clarithromycin, ketoconazole) because these medications can significantly increase exposure to naloxegol which may precipitate opioid withdrawal symptoms