naloxegol

(redirected from Movantik)

naloxegol

(nal-ox-ee-gol),

Movantik

(trade name)

Classification

Therapeutic: laxatives
Pharmacologic: opioid antagonists
Pregnancy Category: C

Indications

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

Action

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.

Pharmacokinetics

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)

ROUTEONSETPEAKDURATION
POwithin 24 hrunknownunknown

Contraindications/Precautions

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

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

Dermatologic

  • sweating

Miscellaneous

  • opioid withdrawal

Interactions

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.

Route/Dosage

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.

Availability

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)

Implementation

  • 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 ?
The AstraZeneca agreement also includes NKTR-119, an earlier stage development program that is a co-formulation of MOVANTIK and an opioid.
AstraZeneca today announced that the US Food and Drug Administration (FDA) approved MOVANTIK (naloxegol) tablets C-II as the first once-daily oral peripherally-acting mu-opioid receptor antagonist (PAMORA) medication for the treatment of opioid-induced constipation (OIC), in adult patients with chronic, non-cancer pain.
The FDA approval of MOVANTIK provides a new treatment option for adult patients with chronic non-cancer pain suffering from opioid-induced constipation, a common side effect of opioid therapy, said Dr.
Food and Drug Administration today approved Movantik (naloxegol), an oral treatment for opioid-induced constipation in adults with chronic non-cancer pain.
Movantik belongs to a class of drugs called peripherally acting opioid receptor antagonists, which are used to decrease the constipating effects of opioids.
The Prescription Drug User Fee Act (PDUFA) date set by the FDA for MOVANTIK is 16 September 2014.
AstraZeneca announced today that the majority of US Food and Drug Administration (FDA) Anesthetic and Analgesic Drug Products Advisory Committee (DPAC) members voted that the FDA should not require cardiovascular outcomes trials for the peripherally-acting mu-opioid receptor antagonist (PAMORA) class of drugs, which includes MOVANTIK (naloxegol oxalate), an investigational treatment for opioid-induced constipation (OIC) for patients with chronic non-cancer pain.
We look forward to the outcome of the FDA s review of the New Drug Application for MOVANTIK and the potential to provide patients with chronic non-cancer pain affected by OIC with an additional treatment option.
0 million milestone payment from AstraZeneca following the first commercial sale of MOVANTIK in the U.
Under the terms of the agreement, in addition to the $40 million milestone payment announced today, Nektar received a $100 million milestone payment upon first commercial sale of MOVANTIK in the U.
Examples of forward-looking statements include, among others, statements we make regarding the potential of MOVANTIK, AstraZeneca's planned commercial launch of MOVANTIK in Europe and Canada, the enrollment status of the SUMMIT-07 efficacy study of NKTR-181, the projected start date of the clinical program for NKTR-214, Baxalta's regulatory and commercial launch plans for ADYNOVATE, and the value and potential of our polymer conjugate technology and research and development pipeline.
launch of Movantik by AstraZeneca is progressing well and this first-in-class medicine to treat OIC is now being made available in several European countries," said Howard W.