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Naloxegol

Antidote · Gastrointestinal Agent

AntidoteGastrointestinal AgentATC A06AH02
CDSCO approvedSchedule HATC A06AH02
EXCRETION
not curated
INTERACTIONS
12 major
SEVERE in our sources
PREGNANCY
and breast-feeding
FDA category + note
Top interactionssee all 12
  • AmprenavirSevereDatabaseDDInter
  • ApalutamideSevereDatabaseDDInter
  • AprepitantSevereDatabaseDDInter
  • AtazanavirSevereDatabaseDDInter

Mechanism

Naloxegol is pegylated naloxone, which limits its penetration into the central nervous system (CNS). Its primary mechanism involves peripheral μ-opioid receptor antagonism. This action mitigates constipation by counteracting the opioid effect in the gut.

Indications

Opioid-induced constipation when response to other laxatives is inadequatePostoperative ileus following bowel resection surgeryOpioid-induced constipation (in adults)

Dosing

Adult
consistency. g In patients with hard stools, a high dose of an oral macrogol (such as macrogol 3350 with potassium chloride, sodium bicarbonate and sodium chloride) may be considered. In those with soft stools, or with hard stools after a few days treatment with a macrogol, an oral stimulant laxative should be started or added to the previous treatment.…

Pharmacokinetics

Peak effect
About 2 h, with a secondary peak 0.4 to 3 h after the first
Half-life
6–11 h (variable)
Metabolism
Primarily by hepatic CYP3A
Excretion
68% in feces, 16% in urine

Contraindications

  • Concomitant administration with voriconazole (due to increased side effects of naloxegol)
  • Known or suspected GI obstruction

Side effects

Common
DiarrheaAbdominal painFlatulenceNauseaVomiting
Serious
  • Opioid withdrawal (may be precipitated in patients with a compromised blood-brain barrier)

Pregnancy & lactation

Pregnancy

and breast-feeding

Drug interactions

Amprenavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Apalutamide
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Aprepitant
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Atazanavir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Berotralstat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Boceprevir
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Carbamazepine
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ceritinib
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Chloramphenicol
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Ciprofloxacin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Clarithromycin
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Cobicistat
Severe
Database

Drug interaction classified as: metabolism

Source: DDInter

Related guidelines

Other Antidote drugs

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Sources: Goodman & Gilman 14e, BNF·Verified: 2026-05-13 · House clinical team