TREATING OPIOID-INDUCED CONSTIPATION (OIC)

OIC IS A COMMON, UNDERTREATED CONDITION AMONG PATIENTS TAKING OPIOIDS²

According to a European expert consensus statement:

OIC affects between

41-57%

of patients taking opioids for pain…²

…and around

51-87%

of advanced cancer patients who
are prescribed opioids²

OIC IS DIFFERENT TO FUNCTIONAL CONSTIPATION⁷

Unlike functional constipation, OIC has a specific mechanism of action which can be targeted.⁶
Opioid drugs bind to specific opioid receptors found throughout the enteric nervous system directly causing OIC.²

WHEN LAXATIVES ARE NOT ENOUGH IN OIC

Laxatives are used first-line to treat OIC, but they do not address the underlying pathophysiological mechanism^8,9
In a survey of patients with cancer and non-cancer pain taking opioids and laxatives, 81% reported persistent constipation⁸

The percentage of patients taking laxatives for OIC and still experiencing inadequate symptoms control, in different studies range from 40-94%, due to variability in patient populations, study design, differences in laxative use and reporting bias⁹

HOW RIZMOIC^® WORKS

A TARGETED APPROACH TO OIC: RIZMOIC^® CAN HELP WHEN LAXATIVES ARE NOT ENOUGH^1,5,6

Rizmoic^® is a peripherally acting mu (μ) opioid receptor antagonist (PAMORA) that directly targets the GI mechanism that causes OIC¹

Rizmoic^® decreases the constipating effects of opioids without reversing their analgesic effects¹

TARGETED ACTION

Rizmoic^® binds to the mu (µ) opioid receptors (MOP), thereby blocking the opioid from binding to these receptors in the GI tract^1,8

DOES NOT CROSS THE BBB¹

Rizmoic^® is a naltrexone derivative with an additional side chain, which reduces its ability to cross the BBB¹
Rizmoic^® is expected to exert its anti-constipating effects on opioids without reversing their CNS-related analgesic effects¹

RIZMOIC^®: A SIMPLE, ONCE-DAILY ORAL TREATMENT FOR PATIENTS WITH OIC¹

For you, prescribing Rizmoic^® means:

Straightforward initiation:
No need to adjust analgesic dose or stop ongoing laxative therapy before starting treatment
Flexibility:
Use with or without laxative(s)
Clear criteria for special populations:
No dose adjustments for:

Patients aged over 65 years
Caution required for patients >75 years

Patients with renal failure
Clinical monitoring required for patients with severe renal impairment

Patients with mild to moderate hepatic failure Not recommended for patients with severe hepatic impairment

For your patients, taking Rizmoic^® means:

Convenience of an oral route of administration
Simplicity of a single tablet per day, reducing pill burden
Choice to take it any time of day (ideally at the same time each day)
Flexibility of being able to take with or without food
Improvements to quality of life (sustained up to 52 weeks)¹⁰

RIZMOIC^® CLINICAL DATA

RIZMOIC^® IMPROVES OIC-RELATED SYMPTOMS AND PATIENTS’ QOL¹⁰

Rizmoic^® has proven clinical efficacy and improvements to QoL for both
cancer and non-cancer patients with OIC^5,6,10

Clinical efficacy

Rizmoic^® significantly improved spontaneous bowel movement (SBM) vs. placebo over 12 weeks, achieving at least 3 SBMs per week, in two studies of non-cancer patients with OIC⁵
More patients achieved at least 3 SBMs with Rizmoic^® versus placebo after 14 days, regardless of dose of opioid analgesic, in a study of cancer patients (primarily lung and breast) with a mean SBM of 1 per week⁶
Rizmoic^® achieved a timely onset of relief from OIC, with a median time to first SBM of 4.7 hours from baseline vs. 26.6 hours for placebo (secondary endpoint, p<0.0001)¹¹

QoL improvement

Rizmoic^® patients with non-cancer chronic pain reported significant improvements in QoL vs. placebo in a 52-week randomised controlled study (p<0.001 at all time points)¹⁰
Cancer patients on Rizmoic^® reported significant improvements from baseline in QoL in a 12-week open-label extension study – including reduction in physical or psychological discomfort and worries and concerns¹¹

RIZMOIC^® IS WELL TOLERATED IN PATIENTS ON LONG-TERM OPIOID THERAPY FOR CHRONIC PAIN^1,11

Rizmoic^® must not be used in patients with known or suspected GI obstruction or in patients at increased risk of recurrent obstruction, due to the potential for GI perforation.¹ In patients with chronic non-cancer pain and OIC the most commonly reported side effects are diarrhoea, abdominal pain, nausea and vomiting.¹ In patients with cancer and OIC, diarrhoea is very common and abdominal pain is common.¹

Please consult the Rizmoic^® SmPC for full safety information.

RIZMOIC^® TARGETED THERAPY:
TREAT OIC AT THE SOURCE AND HELP BRING RELIEF TO YOUR PATIENTS¹

Targets the cause of OIC without counteracting the effect of opioids¹
Proven clinical efficacy and improvements to QoL in OIC⁹
Easy administration with a once-daily tablet¹
Flexibility of taking with or without food, and using with or without a laxative¹

Simple initiation with no dose adjustments needed and suitable in mild, moderate or severe renal impairment¹
A peripherally acting mu (μ) opioid receptor antagonist (PAMORA) that has been studied in cancer and non-cancer pain – with demonstrated efficacy in both^5,6,10
Recommended by NICE and SMC as a cost effective treatment for OIC^12,13

ViatrisConnect is a promotional website
intended for UK healthcare professionals.

Do you have patients who have been prescribed Rizmoic^®?
They can find useful information and resources on the patient page of the website: click here

Additional resources

Abbreviations
BBB, blood-brain barrier; BM, bowel movement; CNS, central nervous system; GI, gastrointestinal; HCP, healthcare professional; MOP, mu opioid receptor; NICE, National Institute for Health and Care Excellence; OIC, opioid-induced constipation; PAMORA, peripherally acting mu receptor antagonist; PIL, Patient Information Leaflet; QoL, quality of life; SBM, spontaneous bowel movement; SMC, Scottish Medicines Consortium; SmPC, Summary of Product Characteristics; TA, Technology Appraisal.

References

Rizmoic^® 200 mcg SmPC.
Farmer AD, et al. United Eur Gastroenterol J 2019;7(1):7–20.
Bowel Interest Group. The Cost of Opioid-Induced Constipation. 2022. Available from: https://bowelinterestgroup.co.uk/wp-content/uploads/2022/07/Cost-of-Opioid-Induced-Constipation-Report-1.pdf. Last accessed August 2025.
ALMouaalamy N. Cureus 2021;13(4):e14386.
Hale M, et al. Lancet Gastroenterol Hepatol 2017;2(8):555–564.
Katakami N, et al. J Clin Oncol 2017;35(34):3859–3866.
Gupta A. JFP OIC Newsletter. Available from: https://www.mdedge.com/jfp/custom/improving-recognition-and-diagnosis-opioid-induced-constipation-clinical-practice-0. Last accessed August 2025.
Streicher JM and Bilsky EJ. J Pharm Pract 2018;31(6):658-669. 9.
Hale ME, et al. Ther Adv Gastroenterol 2021;14:1–11.
Webster LR, et al. Pain 2018;159(5):987–994.
Katakami N, et al. Ann Oncol 2018;29:1461–1467. 12.
NICE TA651. Naldemedine for treating opioid-induced constipation. Available from: https://www.nice.org.uk/guidance/ta651. Last accessed August 2025.
SMC. Naldemedine 200 micrograms film-coated tablets (Rizmoic^®). Available from: https://scottishmedicines.org.uk/medicines-advice/naldemedine-rizmoic-full-smc2242/. Last accessed August 2025.

Prescribing Information

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PRESCRIBING INFORMATION: Rizmoic^® 200 micrograms film-coated tablets (Each tablet contains 200 micrograms naldemedine (as tosylate))
Please refer to Summary of Product Characteristics (SmPC) before prescribing.

Indication: Rizmoic^® is indicated for the treatment of opioid-induced constipation (OIC) in adult patients who have previously been treated with a laxative.

Presentation: Film-coated tablet. Round, approximately 6.5 mm diameter, yellow tablet debossed with '222' and Shionogi logo on one side and '0.2' on the other side.

Dosage and administration: Oral use. The recommended dose of naldemedine is 200 micrograms (one tablet) daily, with or without food. Rizmoic^® may be used with or without laxative(s). It may be taken at any time of the day but it is recommended to be taken at the same time every day. Alteration of the analgesic dosing regimen prior to initiating Rizmoic^® is not required. Rizmoic^® must be discontinued if treatment with the opioid pain medicinal product is discontinued.

Contraindications: Hypersensitivity to the active substance or to any of the excipients. Patients with known or suspected gastrointestinal obstruction or perforation or patients at increased risk of recurrent obstruction, due to the potential for gastrointestinal (GI) perforation.

Warning and precautions: Rizmoic^® must not be used in patients with known or suspected GI obstruction or in patients at increased risk of recurrent obstruction, due to the potential for GI perforation (see section 4.3 of the SmPC for further information). Caution with regards to the use of naldemedine should be exercised in patients with any conditions which might result in impaired integrity of the gastrointestinal tract wall (e.g. peptic ulcer disease, Ogilvie’s syndrome, malignancy of the GI tract, Crohn’s disease). Patients should be monitored for the development of severe, persistent or worsening abdominal pain. If obstruction or perforation are suspected, Rizmoic^® must be discontinued. Abdominal adverse reactions (e.g. abdominal pain, vomiting and diarrhoea) have been reported with Rizmoic^®. Opioid withdrawal syndrome is a cluster of three or more of the following signs or symptoms: dysphoric mood, nausea or vomiting, muscle aches, lacrimation or rhinorrhea, pupillary dilation or piloerection or sweating, diarrhoea, yawning, fever or insomnia. Patients should be advised to discontinue Rizmoic^® and to contact their physician if opioid withdrawal occurs. Patients having disruptions to the blood-brain barrier (e.g., primary brain malignancies, central nervous system (CNS) metastases or other inflammatory conditions, active multiple sclerosis and advanced Alzheimer’s disease) may be at increased risk of opioid withdrawal or reduced analgesia. Patents with a recent history of myocardial infarction, stroke or transient ischaemic attack should be clinically monitored when taking Rizmoic^®. Patients with severe renal impairment should be clinically monitored when initiating therapy with this medicine. Rizmoic^® has not been studied in patients with severe hepatic impairment. The use of naldemedine is not recommended in these patients. Concomitant use with strong CYP3A inhibitors should be avoided. Please refer to SmPC for further information.

Interaction with other medicinal products: Naldemedine is primarily metabolised by CYP3A with some contribution from UGT1A3 and is a substrate of P-glycoprotein (P-gp). Concomitant use of strong CYP3A inhibitors such as grapefruit juice, itraconazole, ketoconazole, ritonavir, indinavir, saquinavir, telithromycin and clarithromycin should be avoided. If use with strong CYP3A inhibitors is unavoidable, monitor for adverse reactions. Rifampicin, a strong CYP3A inducer, significantly decreased exposure to naldemedine by 83% . Concomitant use of strong CYP3A inducers such as St. John’s wort (Hypericum perforatum), rifampicin, carbamazepine, phenobarbital and phenytoin is not recommended. Concomitant use of moderate CYP3A inhibitors such as fluconazole, may increase the plasma concentration of naldemedine. If used with moderate CYP3A inhibitors, monitor for adverse reactions. There is no risk of interaction with concomitant use of mild CYP3A inhibitors.

Pregnancy and lactation: There are no data from the use of naldemedine in pregnant women. Naldemedine should not be used during pregnancy unless the clinical condition of the woman requires treatment with naldemedine. Naldemedine should not be used during breast-feeding.

Effects on ability to drive and use machines: Naldemedine has no or negligible influence on the ability to drive and use machines.

Undesirable effects:

Chronic non-cancer pain and opioid induced constipation: Common: diarrhoea, abdominal pain, nausea, vomiting Uncommon: Opioid withdrawal syndrome.
Cancer and opioid induced constipation: Very Common: diarrhoea Common: Abdominal pain Uncommon: Opioid withdrawal syndrome. For details on uncommon, rare, very rare and unknown undesirable effects, please refer to the SmPC.

Legal Category: POM Marketing Authorisation Number: PLGB 50999/0003 MAH: Shionogi B.V. Herengracht 464, 1017 CA Amsterdam, Netherlands NHS Price: Pack size 30: £44.70 Date of Revision of Prescribing Information: February 2025, UK-RIZM-2024-00048

The SmPC for this product, including adverse reactions, precautions, contra-indications, and method of use can be found at: http://www.mhra.gov.uk/Safetyinformation/Medicinesinformation/SPCandPILs/index.htm and from Viatris Medical Information, Building 4, Trident Place, Hatfield Business Park, Mosquito Way, Hatfield, Hertfordshire, AL10 9UL, phone no. 01707 853000, Email: info.uk@viatris.com

Adverse events should be reported

Please report suspected adverse drug reactions (ADRs) to the MHRA through the Yellow Card scheme. You can report via the Yellow Card website www.mhra.gov.uk/yellowcard, the free Yellow Card app available from the Apple App Store or Google Play Store or some clinical IT systems (EMIS/SystmOne/Vision/MiDatabank) for healthcare professionals. Alternatively, you can report suspected adverse drug reactions to the Yellow Card scheme by calling 0800 731 6789 for free, Monday to Friday between 9am and 5pm. You can leave a message outside of these hours. When reporting please provide as much information as possible. By reporting adverse drug reactions you can help provide more information on the safety of this medicine. You can also report directly to the manufacturer at pv.uk@viatris.com

UK-RIZM-2024-00041 August 2025