naldemedine tosylate at a glance
Medicine class
Peripherally acting mu-opioid receptor antagonist (PAMORA)
Licensed use
Opioid-induced constipation in adults previously treated with a laxative
Food
The tablet can be taken with or without food
Laxatives
It may be used with or without laxatives
What is naldemedine tosylate used for?
Its UK licensed indication is:
Treatment of opioid-induced constipation in adults who have previously received laxative treatment.
How does naldemedine tosylate work?
Opioids activate receptors in the gut as well as the brain, slowing bowel movement and reducing intestinal secretions. Naldemedine blocks opioid receptors mainly outside the brain, particularly in the gastrointestinal tract, reducing constipation while being designed to preserve centrally mediated pain relief.
naldemedine tosylate preparations and strengths
Tablet
Route: Oral
Strengths: 200 micrograms
How to take naldemedine tosylate
Swallow the film-coated tablet as prescribed. It can be taken with or without food and with or without laxatives. Do not alter the opioid pain medicine solely because naldemedine is being started. Ask the prescriber about stopping naldemedine if opioid treatment is stopped.
Avoid large amounts of grapefruit juice because this can increase naldemedine exposure and adverse effects.
Keep tablets in their original packaging to protect them from light and moisture.
naldemedine tosylate side effects
Common or expected effects
- Diarrhoea
- Abdominal pain or discomfort
- Nausea
- Vomiting
Get urgent medical advice
- Severe, persistent or worsening abdominal pain, particularly if bowel obstruction or perforation is possible
- Severe diarrhoea or abdominal pain causing dehydration
- A serious allergic reaction, including facial or throat swelling or difficulty breathing
- A cluster of opioid-withdrawal symptoms such as sweating, muscle aches, runny nose, fever, diarrhoea, vomiting or insomnia
naldemedine tosylate in pregnancy
There are no adequate human pregnancy data. Naldemedine could cause opioid withdrawal in the fetus because the fetal blood–brain barrier is immature. It should generally be avoided unless a specialist considers treatment clinically necessary.
naldemedine tosylate while breastfeeding
It is unknown whether naldemedine enters human milk, and opioid withdrawal in a breastfed infant is theoretically possible when the mother takes an opioid. The product information advises against breastfeeding during treatment; discuss alternatives with the prescriber or an infant-feeding specialist.
naldemedine tosylate interactions
Check prescription, non-prescription and herbal products before treatment, particularly medicines affecting CYP3A or P-glycoprotein.
Strong CYP3A inhibitors, including itraconazole, ketoconazole, clarithromycin and some HIV protease inhibitors
They can increase naldemedine exposure and adverse effects; combined use should usually be avoided.
Grapefruit juice
Large amounts may increase naldemedine exposure and the likelihood of adverse effects.
Strong CYP3A inducers, including rifampicin, carbamazepine, phenytoin, phenobarbital and St John’s wort
They can substantially reduce naldemedine exposure and effectiveness; combined use is not recommended.
Common questions about naldemedine tosylate
Answers are fully visible for fast scanning and source review.
Why is naldemedine tosylate prescribed?
It treats constipation caused by opioid pain medicines in adults who have previously been treated with a laxative.
Is naldemedine tosylate a conventional laxative?
No. It is a PAMORA that directly blocks the constipating effects of opioids at receptors in the gut.
Can naldemedine tosylate be taken with food?
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.