Formulary
Naloxegol: Indications, Dosing, Side Effects and Interactions
Naloxegol is a peripherally acting opioid receptor antagonist.
MedNext Academy | 3 min read
Naloxegol: Indications, Dosing, Side Effects and Interactions
Naloxegol is a peripherally acting opioid receptor antagonist.
Drug action
Naloxegol is a peripherally acting opioid receptor antagonist. It therefore decreases the constipating effects of opioids without altering their central analgesic effects.
Indications and dose
**Opioid-induced constipation when response to laxatives inadequate**
- **Adult** (By Mouth): 25 mg once daily, to be taken in the morning.
Cautions
Alzheimer's disease (advanced); cardiovascular disease; CNS metastases; congestive heart failure (symptomatic); Crohn's disease; diverticulitis (active or recurrent); multiple sclerosis (active); peptic ulcer disease (severe); primary brain malignancies; QT interval over 500 milliseconds; recent history of myocardial infarction (within 6 months) Cautions, further information Disruptions to blood-brain barrier Manufacturer advises caution in patients with clinically important disruptions to the blood-brain barrier (e.g. advanced Alzheimer's disease, active multiple sclerosis, primary brain malignancies)-risk of uptake into the CNS. Cardiovascular disorders Safety and efficacy has not been established in patients with these conditions.
Contraindications
Gastro-intestinal or peritoneum malignancy (risk of gastro-intestinal perforation); known or suspected gastro-intestinal obstruction; patients at risk of recurrent gastro-intestinal obstruction; recurrent or advanced ovarian cancer (risk of gastro-intestinal perforation); vascular endothelial growth factor (VEGF) inhibitor treatment (risk of gastro-intestinal perforation)
Side effects
Common or very common Abdominal pain; diarrhoea; flatulence; headache; hyperhidrosis; nasopharyngitis; nausea; vomiting Uncommon Withdrawal syndrome Side-effects, further information Manufacturer advises that gastrointestinal side-effects typically occur shortly after initiation of treatment - consider reducing the dose.
Interactions
**Severe interactions:**
- Opioid receptor antagonists Naloxegol [CYP3A4 substrate] Although not studied, voriconazole is likely to significantly increase the plasma concentrations of naloxegol.
Pregnancy
Manufacturer advises avoid-limited data available but toxicity at high doses in animal studies; theoretical risk of opioid withdrawal in fetus.
Breast feeding
Manufacturer advises avoid-present in milk in animal studies and theoretical risk of opioid withdrawal in breast-fed infants.
Hepatic impairment
Manufacturer advises avoid in severe impairment (no information available).
Renal impairment
Dose adjustments Manufacturer advises lower initial dose in moderate to severe impairment-initially 12.5 mg daily, increase to 25 mg if well tolerated.
Medicinal forms
Clinical governance
**Author:** MedNext Clinical Team. **Clinical reviewer:** Dr Shameer Deen, MBBS, MS, MRCS. **Sources:** BNF, Indian Pharmacopoeia, CIMS India. **Correction:** Report errors at support@mednext.academy.
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