naloxegol (Rx)

Brand and Other Names:Movantik
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Dosing & Uses

AdultPediatric

Dosage Forms & Strengths

tablet

  • 12.5mg
  • 25mg
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Opioid-Induced Constipation

Peripherally acting mu-opioid receptor antagonist (PAMORA) indicated for opioid-induced constipation in adults with chronic noncancer pain

25 mg PO qDay in morning; give at least1 hr ac or 2 hr pc

Decrease dose to 12.5 mg/day if patient unable to tolerate 25 mg/day

Also see Administration

Dosage Modifications

Coadministration with strong CYP3A4 inducers: Not recommended

Coadministration with CYP3A4 inhibitors

  • Strong CYP3A4 inhibitors: Contraindicated
  • Moderate CYP3A4 inhibitors: Avoid coadministration; if unavoidable, reduce dose to 12.5 mg qDay

Renal impairment

  • Mild: No dosage adjustment required
  • CrCl <60 mL/min (ie, moderate, severe, or end-stage renal disease): Decrease starting dose to 12.5 mg/day; if this dose is well tolerated, but OIC symptoms continue, may increase to 25 mg/day (monitor for potential adverse effects associated with higher exposure)

Hepatic impairment

  • Mild-to-moderate: No dosage adjustment required
  • Severe: Avoid use

Safety and efficacy not established

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Interactions

Interaction Checker

and naloxegol

No Results

     activity indicator 
    No Interactions Found
    Interactions Found

    Contraindicated

      Serious - Use Alternative

        Significant - Monitor Closely

          Minor

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            Adverse Effects

            >10%

            Abdominal pain (12-21%)

            GI effects

            • Patients receiving methadone as therapy for their pain condition have a higher frequency of GI adverse reactions than patients receiving other opioids
            • 12.5 mg/day of naloxegol: 39% (methadone) vs 26% (other opioid)
            • 25 mg/day of naloxegol: 75% (methadone) vs 34% (other opioid)

            1-10%

            Diarrhea (6-9%)

            Nausea (7-8%)

            Flatulence (3-6%)

            Vomiting (3-5%)

            Headache (4%)

            Opioid withdrawal (1-3%)

            Hyperhidrosis (<1-3%)

            Postmarketing Reports

            Severe abdominal pain and/or diarrhea

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            Warnings

            Contraindications

            Known serious or severe hypersensitivity reaction

            Known or suspected GI obstruction and patients at increased risk of recurrent obstruction; increases risk for GI perforation

            Coadministration with strong CYP3A4 inhibitors; can significantly increase naloxegol systemic exposure, which may precipitate opioid withdrawal symptoms

            Cautions

            GI perforation reported with other PAMORA in patients with conditions associated with reduced structural integrity in the wall of the GI tract (eg, PUD, Ogilvie syndrome, diverticular disease, infiltrative GI malignancies, peritoneal metastases, Crohn disease); monitor for development of severe, persistent, or worsening abdominal pain; discontinue naloxegol in patients who develop these symptoms

            Monitor for development of severe abdominal pain and /or diarrhea symptoms after initiating treatment and discontinue if severe symptoms develop; consider restarting therapy at 12.5 mg once daily if appropriate

            Symptoms consistent with opioid withdrawal (eg, hyperhidrosis, chills, diarrhea, abdominal pain, anxiety, irritability, yawning) reported

            Higher frequency of GI adverse effects related to opioid withdrawal reported in patients receiving methadone than other opioid analgesics

            Patients with disruption to the blood-brain barrier may be at increased risk for opioid withdrawal or reduced analgesia; consider overall risk benefit in patients with disruptions to blood-brain barrier; monitor for symptoms of opioid withdrawal

            Avoid coadministration with other opioid antagonists

            Severe abdominal pain and/or diarrhea

            • Severe abdominal pain and/or diarrhea reported, some of which resulted in hospitalization
            • Most cases were with the 25 mg dose
            • Symptoms generally occurred within a few days after initiating naloxegol
            • Monitor and discontinue therapy if severe symptoms occur
            • Consider restarting at 12.5 mg qDay, if appropriate
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            Pregnancy & Lactation

            Pregnancy Category: C

            Lactation: Unknown if distributed in human breast milk; patient should be advised against breast feeding during treatment; a decision should be made to discontinue nursing or discontinue the drug taking into account the importance of the drug to the patient

            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.

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            Pharmacology

            Mechanism of Action

            Peripherally acting mu-opioid receptor antagonist (PAMORA); contains naloxegol oxalate (pegylated derivative of naloxone)

            Antagonism of gastrointestinal mu-opioid receptors by naloxegol inhibits the opioid-induced delay of GI transit time

            Absorption

            Peak plasma time: <2 hr; secondary peak occurs in most patients 0.4-3 hr after the first peak

            High-fat meal increases extent and rate of absorption; Cmax and AUC increased by ~30% and 45%, respectively

            Distribution

            Protein bound: Low (~4.2%)

            Vd: 968-2140 L

            Metabolism

            Substrate of CYP3A and P-gp

            Elimination

            Excretion: 68% feces (~16% unchanged); 16% urine (<6% unchanged)

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            Administration

            Oral Administration

            Discontinue all maintenance laxative therapy prior to initiating naloxegol

            Laxatives can be used PRN if there is suboptimal response to naloxegol after 3 days

            Alteration in analgesic dosing regimen prior to initiating is not required

            Naloxegol is efficacious in patients who have taken opioids for at least 4 wk; sustained opioid exposure prior to starting may increase sensitivity to naloxegol effects

            Take on empty stomach at least 1 hr before first meal of the day or 2 hr after the meal

            For patients who are unable to swallow tablet whole, tablet can be crushed and given orally or administered via nasogastric tube

            Avoid grapefruit or grapefruit juice during treatment with naloxegol

            Discontinue if treatment with opioid pain medication is also discontinued

            If unable to swallow tablet whole

            • Tablet can be crushed to a powder, mixed with 120 mL of water and drunk immediately; refill the glass with 120 mL of water, stir, and drink contents to assure whole tablet is consumed
            • Administer by NG-tube
              • Flush the NG tube with 30 mL of water using a 60 mL syringe
              • Crush the tablet to a powder in a container and mix with ~60 mL of water
              • Draw up the mixture using the 60 mL syringe and administer the syringe contents through the NG tube
              • Add ~60 mL of water to the same container used to prepare the dose
              • Draw up the water using the same 60 mL syringe and use all the water to flush the NG tube and any remaining medicine from the NG tube into the stomach
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            Formulary

            FormularyPatient Discounts

            Adding plans allows you to compare formulary status to other drugs in the same class.

            To view formulary information first create a list of plans. Your list will be saved and can be edited at any time.

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            • View the formulary and any restrictions for each plan.
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            • Compare formulary status to other drugs in the same class.
            • Access your plan list on any device – mobile or desktop.

            The above information is provided for general informational and educational purposes only. Individual plans may vary and formulary information changes. Contact the applicable plan provider for the most current information.

            Tier Description
            1 This drug is available at the lowest co-pay. Most commonly, these are generic drugs.
            2 This drug is available at a middle level co-pay. Most commonly, these are "preferred" (on formulary) brand drugs.
            3 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs.
            4 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            5 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            6 This drug is available at a higher level co-pay. Most commonly, these are "non-preferred" brand drugs or specialty prescription products.
            NC NOT COVERED – Drugs that are not covered by the plan.
            Code Definition
            PA Prior Authorization
            Drugs that require prior authorization. This restriction requires that specific clinical criteria be met prior to the approval of the prescription.
            QL Quantity Limits
            Drugs that have quantity limits associated with each prescription. This restriction typically limits the quantity of the drug that will be covered.
            ST Step Therapy
            Drugs that have step therapy associated with each prescription. This restriction typically requires that certain criteria be met prior to approval for the prescription.
            OR Other Restrictions
            Drugs that have restrictions other than prior authorization, quantity limits, and step therapy associated with each prescription.
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