1.6.6 Peripheral opioid-receptor antagonists

Methylnaltrexone bromide

• Solution for injection 20mg in 1ml (£21.05 = 0.6ml vial)

Indications

• Opioid-induced constipation in patients receiving palliative care, when response to other laxatives is inadequate

Dose

• By subcutaneous injection, for adults:
  • Body-weight up to 38kg, 150 micrograms/kg once daily on alternate days
  • Body-weight 38–61kg, 8mg once daily on alternate days
  • Body-weight 62–114kg, 12mg once daily on alternate days
  • Body-weight 115kg and over, 150 micrograms/kg once daily on alternate days
• The interval between administrations may be varied but not more than once a day

Notes

1. Treatment can result in the rapid onset of a bowel movement (i.e. within 30 to 60 minutes)
2. In palliative care patients, treatment is added to usual laxative therapy which may subsequently require review
3. Consult Summary of Product Characteristics (SPC) for dosing adjustments in renally impaired patients
4. The SPC states that methylnaltrexone bromide has not been studied in adult patients with advanced illness in clinical trials beyond 4 months

Naloxegol

• Tablets 12.5mg, 25mg (£51.52 = 25mg daily)

Indications

• For the treatment of opioid induced constipation in adults whose constipation has not adequately responded to laxatives
  • Naloxegol should only be initiated in patients in whom opioids are effectively treating the pain

Dose

• 25mg once daily, to be taken in the morning
• Certain patients may require a dose reduction to 12.5mg daily; consult manufacturers SPC for further details

Notes

1. For use in accordance with NICE TA345 Naloxegol for treating opioid‑induced constipation (July 2015)
   
   1. An inadequate response to laxatives is defined as opioid-induced constipation symptoms of at least moderate severity in at least 1 of the 4 stool symptom domains (that is, incomplete bowel movement, hard stools, straining or false alarms) while taking at least 1 laxative class for at least 4 days during the prior 2 weeks
2. For use in primary care following recommendation from a member of the palliative care team only. In all other indications, naloxegol should be restricted to secondary care use
3. Patients should be advised to report severe, persistent or worsening gastro-intestinal effects (such as abdominal pain)

Naldemedine

• Tablets 200 micrograms

Notes

1. NICE TA651: Naldemedine (Rizmoic) is recommended, within its marketing authorisation, as an option for treating opioid-induced constipation in adults who have had laxative treatment (September 2020)

 

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