Drug reference
Methylnaltrexone bromide is a peripherally acting opioid-receptor antagonist. It therefore blocks the gastro-intestinal (constipating) effects of opioids without altering their central analgesic effects.
PDF page 90
Opioid-induced constipation in patients with chronic pain (except palliative care patients with advanced illness) ▶BY SUBCUTANEOUS INJECTION ▶Adult: 12 mg once daily if required, to be given as 4–7 doses weekly Adjunct to other laxatives in opioid-induced constipation in palliative care ▶BY SUBCUTANEOUS INJECTION ▶Adult (body-weight up to 38 kg): 150 micrograms/kg once daily on alternate days for maximum duration of treatment 4 months, two consecutive doses may be given 24 hours apart if no response to treatment on the preceding day ▶Adult (body-weight 38–61 kg): 8 mg once daily on alternate days for maximum duration of treatment 4 months, two consecutive doses may be given 24 hours apart if no response to treatment on the preceding day ▶Adult (body-weight 62–114 kg): 12 mg once daily on alternate days for maximum duration of treatment 4 months, two consecutive doses may be given 24 hours apart if no response to treatment on the preceding day ▶Adult (body-weight 115 kg and above): 150 micrograms/kg once daily on alternate days for maximum duration of treatment 4 months, two consecutive doses may be given 24 hours apart if no response to treatment on the preceding day
PDF page 90
▶May act within 30–60 minutes.
PDF page 90
Acute surgical abdominal conditions. gastro-intestinal obstruction
PDF page 90
Diverticular disease (when active). faecal impaction. gastro-intestinal tract lesions (known or suspected). patients with colostomy. patients with peritoneal catheter
PDF pages 90, 91
Palliative care For further information on the use of methylnaltrexone in palliative care, see www.medicinescomplete.com/#/content/palliative/opioid- antagonists-therapeutic-target-outside-the-cns. l HANDLING AND STORAGE Protect from light.
PDF page 91
▶Common or very common Abdominal pain. diarrhoea. dizziness. gastrointestinal disorders. nausea. opioid withdrawal-like syndrome. vomiting Overdose Symptoms of overdosage include orthostatic hypotension.
PDF page 91
Manufacturer advises avoid unless essential—toxicity at high doses in animal studies.
PDF page 91
Manufacturer advises use only if potential benefit outweighs risk—present in milk in animal studies.
PDF page 91
Manufacturer advises avoid in severe impairment (no information available).
PDF page 91
Dose adjustments If eGFR less than 30 mL/minute/1.73 m2, reduce dose as follows: body-weight under 62 kg, 75 micrograms/kg on alternate days; body-weight 62–114 kg, 8 mg on alternate days; body-weight over 114 kg, 75 micrograms/kg on alternate days.
PDF page 91
Rotate injection site.
PDF page 91
There can be variation in the licensing of different medicines containing the same drug. Solution for injection ▶Relistor (Bausch & Lomb UK Ltd) Methylnaltrexone bromide 20 mg per 1 ml Relistor 12mg/0.6ml solution for injection vials | 1 vial P £21.05 | 7 vial P £147.35
PDF page 91
12 mg once daily if required, to be given as
First-line fragment. Read the complete Indications and Dose section above.
PDF page 90
150 micrograms/kg once
First-line fragment. Read the complete Indications and Dose section above.
PDF page 90
8 mg once daily on
First-line fragment. Read the complete Indications and Dose section above.
PDF page 90
12 mg once daily on
First-line fragment. Read the complete Indications and Dose section above.
PDF page 90
150 micrograms/kg
First-line fragment. Read the complete Indications and Dose section above.
PDF page 90
