naldemedine tosylate: prescribing and clinical use
Focused clinical detail for use alongside current product information, local policy and patient-specific assessment.
naldemedine tosylate: clinical details
Prescribing considerations
- Confirm constipation is opioid-induced and that the adult has previously received laxative treatment.
- Stop naldemedine when the causative opioid analgesic is discontinued.
- Use caution where gastrointestinal-wall integrity may be impaired, including peptic ulcer disease, Crohn’s disease, gastrointestinal malignancy, peritoneal metastases or acute colonic pseudo-obstruction.
- Use caution in people with blood–brain barrier disruption because opioid withdrawal or reduced analgesia may be more likely.
- Experience is limited in older adults aged 75 years or above, severe renal impairment, very high opioid exposure and constipation caused by partial mu-opioid agonists.
- Use is not recommended in severe hepatic impairment.
Contraindications and cautions
- Hypersensitivity to naldemedine or a tablet excipient.
- Known or suspected gastrointestinal obstruction or perforation.
- Increased risk of recurrent gastrointestinal obstruction.
Monitoring
- Assess severe, persistent or worsening abdominal pain promptly and discontinue if obstruction or perforation is suspected.
- Monitor severe diarrhoea or abdominal pain for dehydration.
- Monitor for opioid withdrawal and reduced analgesia, especially when the blood–brain barrier may be disrupted.
- Monitor clinically when initiating treatment in severe renal impairment and in people with a recent myocardial infarction, stroke or transient ischaemic attack.
- Review interacting medicines that inhibit or induce CYP3A or inhibit P-glycoprotein.
Clinical pharmacology
Naldemedine antagonises mu-, delta- and kappa-opioid receptors and acts predominantly in peripheral tissues such as the gastrointestinal tract. Its size, polarity and P-glycoprotein substrate activity limit central nervous system penetration. It is metabolised mainly through CYP3A, with a smaller UGT1A3 contribution.
Formulation and product differences
- The selected UK product is a yellow, round, film-coated oral tablet supplied in aluminium blisters.
- The tablet is essentially sodium-free and should remain in its original packaging to protect it from light and moisture.
naldemedine tosylate preparations and strengths
Tablet
Route: Oral
Strengths: 200 micrograms
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.
Sources
These sources were used to prepare and review this medicine page.
Prepared and reviewed by the iatroX editorial team.