• Treatment of opioid-induced constipation in patients with chronic noncancer pain, including those with chronic pain related to prior cancer or its treatment who do not require frequent (e.g., weekly) opioid dose escalation.

Contraindicated in:

• Hypersensitivity
• Known/suspected/history of GI obstruction
• Severe hepatic impairment
• Concurrent use of strong CYP3A4 inhibitors, strong CYP3A4 inducers, or other opioid antagonists
• Severe hepatic impairment
• Lactation: Lactation.

Use Cautiously in:

• Infiltrative GI tract malignancy, recent GI tract surgery, diverticular disease, ischemic colitis, or concurrent use of bevacizumab (↑ risk of GI perforation)
• Patients with disruption of the blood-brain barrier (may precipitate opioid withdrawal)
• OB: Use during pregnancy only if potential maternal benefit justifies potential fetal risk
• Pedi: Safety and effectiveness not established in children
• Geri: Blood levels are ↑ in elderly Japanese patients.

Derm: ↑sweating.

GI: abdominal pain, diarrhea, flatulence, GI PERFORATION, nausea, vomiting.

Neuro: headache.
Misc: (INCLUDING ANGIOEDEMA)HYPERSENSITIVITY REACTIONS , opioid withdrawal.

Drug-Drug:

• Strong CYP3A4 inhibitors, including clarithromycin and ketoconazole, may significantly ↑ levels and risk of toxicity; concurrent use contraindicated.
• Strong CYP3A4 inducers, including rifampin, may significantly ↓ levels and effectiveness; concurrent use contraindicated.
• Other opioid antagonists may precipitate opioid withdrawal; concurrent use contraindicated.
• Moderate CYP3A4 inhibitors, including diltiazem, erythromycin, and verapamil, may ↑ levels and risk of toxicity; ↓ naloxegol dose.
• Concurrent use of methadone for pain ↑ risk of stomach pain and diarrhea.
• Concurrent use of bevacizumab may ↑ risk of GI perforation.

Drug-Food:

• Grapefruit/grapefruit juice may ↑ levels and the risk of toxicity/adverse reactions; avoid concurrent use.

• Tablets: 12.5 mg; 25 mg;

• PO (Adults): 25 mg once daily; if poorly tolerated, ↓ dose to 12.5 mg once daily; Concurrent use of moderate CYP3A4 inhibitors: 12.5 mg once daily (careful monitoring recommended).

Movantik

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

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

Therapeutic Classification: laxatives

Pharmacologic Classification: opioid antagonists

Absorption: Systemic absorption follows oral administration. A high-fat meal ↑ absorption.

Distribution: Does not cross the blood-brain barrier.

Metabolism/Excretion: Primarily metabolized by the liver via the CYP3A4 isoenzyme; 68% excreted in feces, 16% in urine mostly as metabolites.

Half-life: 6–11 hr.

(spontaneous bowel movement)

• 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 the Medication Guide prior to starting therapy and with each Rx 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 females of reproductive potential to notify health care professional if pregnancy is planned or suspected and avoid breastfeeding during therapy; may cause opioid withdrawal in infant.

nal-OX-ee-gol