Movantik (naloxegol oxalate)

Dosage of naloxegol oxalate is expressed in terms of naloxegol.

The recommended adult dosage of naloxegol for the management of opiate-induced constipation in patients with chronic non-cancer-related pain is 25 mg once daily in the morning. If patients cannot tolerate the 25-mg daily dosage, dosage of naloxegol may be reduced to 12.5 mg once daily in the morning.

If concomitant use of moderate cytochrome P-450 (CYP) 3A4 inhibitors (e.g., diltiazem, erythromycin, verapamil) is unavoidable, dosage of naloxegol should be reduced to 12.5 mg once daily, and the patient should be monitored for adverse effects. (See Drug Interactions.)

Naloxegol oxalate is administered orally on an empty stomach at least 1 hour before or 2 hours after the first meal of the day. For patients who have cannot swallow naloxegol oxalate tablets whole, the tablet may be crushed to a powder and mixed with 120 mL of water in a glass; the resulting mixture should be stirred and then swallowed immediately. To ensure consumption of the entire dose, the glass should be rinsed with 120 mL of water; the resulting mixture should be stirred and then swallowed immediately.

For administration through a nasogastric tube, the nasogastric tube should first be flushed with 30 mL of water using a 60-mL syringe. The tablet should then be crushed to a powder and mixed with approximately 60 mL of water in a container. The resulting mixture should be drawn up into the 60-mL syringe and administered through the nasogastric tube. To facilitate delivery of the entire dose, the container should be rinsed with approximately 60 mL of water, the mixture should be drawn up into the same syringe, and the entire contents of the syringe should be used to flush the nasogastric tube.

Plasma concentrations of naloxegol attained when a crushed naloxegol oxalate tablet is mixed in water and administered either orally or through a nasogastric tube are comparable to those attained following oral administration of an intact tablet of the drug.

No dosing information is available for this tab.

No dosing information is available for this tab.

Naloxegol is metabolized principally by cytochrome P-450 (CYP) 3A isoenzymes and is a substrate, but not a clinically important inhibitor, of P-glycoprotein (P-gp). Naloxegol did not inhibit CYP 1A2, 2C9, 2C19, 2D6, or 3A4 nor substantially induce CYP 1A2, 2B6, or 3A4 in vitro at clinically relevant concentrations, and is not expected to alter metabolic clearance of drugs metabolized by these enzymes.

Naloxegol does not substantially inhibit breast cancer resistance protein (BCRP), organic anion transporter (OAT) 1 or 3, organic cation transporter (OCT) 2, or organic anion transport protein (OATP) 1B1 or 1B3.

There are no contraindication interactions for this drug.

There are no severe interactions for this drug.

There are no moderate interactions for this drug.

Because of the potential for GI perforation, naloxegol is contraindicated in patients with known or suspected GI obstruction and in patients at increased risk for recurrent GI obstruction (see GI Perforation under Cautions: Warnings/Precautions).

Naloxegol is contraindicated in patients receiving potent inhibitors of cytochrome P-450 (CYP) isoenzyme 3A4 (CYP3A4) (e.g., clarithromycin, ketoconazole) because of the potential for increased exposure to naloxegol and precipitation of opiate withdrawal (see Drug Interactions).

Naloxegol also is contraindicated in patients with known serious or severe hypersensitivity reactions to the drug or any ingredient in the formulation.

There are no contraindication contraindications for this drug.

There are no severe contraindications for this drug.

There are no moderate contraindications for this drug.

Adverse effects reported in 3% or more of patients receiving naloxegol 12.5 or 25 mg daily and at an incidence greater than that observed with placebo include abdominal pain, diarrhea, nausea, flatulence, vomiting, headache, and hyperhidrosis.

There are no severe adverse reactions for this drug.

There are no less severe adverse reactions for this drug.

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Safety and efficacy of naloxegol have not been established in pediatric patients.

Category C. (See Users Guide.)

Naloxegol should be used in pregnant women only if the potential benefits justify the potential risk to the fetus. There are no adequate and well-controlled studies of naloxegol in pregnant women. Because of the immature fetal blood-brain barrier, use of naloxegol during pregnancy may precipitate opiate withdrawal in the fetus. No adverse effects of the drug on embryofetal development have been observed in animal reproduction studies.

It is not known whether naloxegol is distributed into human milk; however, naloxegol is distributed into milk in rats and is absorbed in nursing rat pups. Because of the potential for serious adverse effects, including opiate withdrawal, in nursing infants, a decision should be made whether to discontinue nursing or the drug, taking into account the importance of the drug to the woman.

In clinical studies of naloxegol, 11% of patients were 65 years of age and older, while 2% were 75 years of age and older. Although no overall differences in efficacy or safety were observed between geriatric patients and younger adults, and other clinical experience revealed no evidence of age-related differences in response, the possibility that some older patients may exhibit increased sensitivity to the drug cannot be ruled out.

Naloxegol exposure was higher in healthy geriatric Japanese individuals compared with younger individuals; however, no dosage adjustment is required in geriatric patients.