Drug Action
Naloxegol is a peripherally acting opioid receptor antagonist. It therefore decreases the constipating effects of opioids without altering their central analgesic effects.
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Drug reference
Naloxegol is a peripherally acting opioid receptor antagonist. It therefore decreases the constipating effects of opioids without altering their central analgesic effects.
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Opioid-induced constipation when response to laxatives inadequate ▶BY MOUTH ▶Adult: 25 mg once daily, to be taken in the morning
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DUE TO INTERACTIONS ▶Manufacturer advises reduce initial dose to 12.5 mg daily with concurrent use of moderate inhibitors of CYP3A4, increasing to 25 mg daily if well tolerated.
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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)
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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.
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NICE decisions ▶Naloxegol for treating opioid-induced constipation (July 2015) NICE TA345 Naloxegol (Moventig ®) is recommended as a possible treatment for opioid induced constipation in patients whose response to laxatives is inadequate. www.nice.org.uk/guidance/ta345
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→Appendix 1: naloxegol
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▶Common or very common Abdominal pain. diarrhoea. flatulence. headache. hyperhidrosis. nasopharyngitis. Gastro-intestinal system 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.
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Manufacturer advises avoid—limited data available but toxicity at high doses in animal studies; theoretical risk of opioid withdrawal in fetus.
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Manufacturer advises avoid—present in milk in animal studies and theoretical risk of opioid withdrawal in breast-fed infants.
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Manufacturer advises avoid in severe impairment (no information available).
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Dose adjustments Manufacturer advises lower initial dose in moderate to severe impairment—initially 12.5 mg daily, increase to 25 mg if well tolerated.
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Manufacturer advises tablets can be crushed, mixed with 120 mL of water and taken immediately if patients are unable to swallow tablets whole. The mixture may be administered via a nasogastric tube, if required.
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There can be variation in the licensing of different medicines containing the same drug. Tablet CAUTIONARY AND ADVISORY LABELS 23 ▶Moventig (Kyowa Kirin Ltd) Naloxegol (as Naloxegol oxalate) 12.5 mg Moventig 12.5mg tablets | 30 tablet P £55.20 DT = £55.20 Naloxegol (as Naloxegol oxalate) 25 mg Moventig 25mg tablets | 30 tablet P £55.20 DT = £55.20 Diarrhoea Diarrhoea (acute) Description of condition Diarrhoea is the abnormal passing of loose or liquid stools, with increased frequency, increased volume, or both. Acute diarrhoea is that which lasts less than 14 days, but symptoms usually improve within 2–4 days. It can result from infection, as a side-effect of a drug, or as an acute symptom of a chronic gastro-intestinal disorder (such as Inflammatory bowel disease p. 41 or Irritable bowel syndrome p. 51). It may also result from the accumulation of non-absorbed osmotically active solutes in the gastro-intestinal lumen (e.g. in lactase deficiency) or from the gastro-intestinal effects of secretory stimuli (other than the enterotoxins from an infection). It may also occur when intestinal motility or morphology is altered. Prompt investigation is required to identify or exclude any serious underlying cause if the patient has any red flag symptoms such as unexplained weight loss, rectal bleeding, persistent diarrhoea, a systemic illness, has received recent hospital treatment or antibiotic treatment, or following foreign travel (other than to Western Europe, North America, Australia or New Zealand). Aims of treatment The priority of acute diarrhoea treatment, as in gastro- enteritis, is the prevention or reversal of fluid and electrolyte depletion and the management of dehydration when it is present. This is particularly important in infants, frail and elderly patients, when excessive water and electrolyte loss and dehydration can be life-threatening. Treatment Most episodes of acute diarrhoea will settle spontaneously without the need for any medical treatment. g Oral rehydration therapy (ORT, such as disodium hydrogen citrate with glucose, potassium chloride and sodium chloride p. 1103; potassium chloride with sodium chloride p. 1101; potassium chloride with rice powder, sodium chloride and sodium citrate p. 1104) is the mainstay of treatment for acute diarrhoea to prevent or correct diarrhoea dehydration and to maintain the appropriate fluid intake once rehydration is achieved—see Fluids and electrolytes p. 1096. However, in patients with severe dehydration and in those unable to drink, immediate admission to hospital and urgent replacement treatment with an intravenous rehydration fluid is recommended—see Fluids and electrolytes p. 1096. The antimotility drug loperamide hydrochloride p. 71 is usually considered to be the standard treatment when rapid control of symptoms is required. It can also be used for mild- to-moderate travellers’ diarrhoea (e.g. where toilet amenities are limited or unavailable) but should be avoided in bloody or suspected inflammatory diarrhoea (febrile patients) and in cases of significant abdominal pain (which also suggests inflammatory diarrhoea). Loperamide hydrochloride is also the first-line treatment for patients with faecal incontinence [unlicensed indication] after the underlying cause of incontinence has been addressed. h Racecadotril is licensed as an adjunct to rehydration for the symptomatic treatment of uncomplicated acute diarrhoea in adults and children over 3 months. There is insufficient evidence to recommend adsorbent preparations (such as kaolin) in acute diarrhoea. Antibacterial drugs for acute diarrhoea g Ciprofloxacin p. 590 is occasionally used for prophylaxis against travellers’ diarrhoea, but routine use is not recommended. h See also Gastro-intestinal system infections, antibacterial therapy p. 535. Related drugs Other drugs used for diarrhoea: codeine phosphate p. 475, co-phenotrope p. 71, methylcellulose p. 59, rifaximin p. 609. Other drugs used for Diarrhoea Colesevelam hydrochloride, p. 209. Colestyramine, p. 210 ANTIDIARRHOEALS › ANTIPROPULSIVES eiiii F 467
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Manufacturer advises patients report severe, persistent or worsening gastro- intestinal effects (such as abdominal pain) to their prescriber.
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25 mg once daily, to be taken in the morning
First-line fragment. Read the complete Indications and Dose section above.
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