Pharmacy Guide
Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
Pharmacy Guide
Patient leaflets and SmPCs, drug interaction checker, official dosages and NHS pharmacy opening hours — all in one place.
Relistor 12 mg Solution for injection in pre-filled syringes
⚠ This medicine appears to have been discontinued
The electronic medicines compendium (emc) no longer publishes a Summary of Product Characteristics for this product, which usually means it is no longer marketed in the UK. The patient leaflet below is kept for reference, but the product may not be available.
If you were prescribed this medicine, other products containing Methylnaltrexone bromide may still be available. Do not stop your treatment — ask your pharmacist or GP what to use instead.
What it is and what it is used for
for
Relistor contains an active substance called methylnaltrexone bromide which acts by blocking the side effects of opioid pain medicines that affect the bowel. It treats constipation that is caused by medicines for moderate to severe pain called opioids (for example morphine or codeine). It is used for patients when other medicines for constipation, called laxatives, have not worked well enough. Opioids are prescribed by your doctor. Your doctor will tell you whether you should stop or continue taking your usual laxatives when you start using this medicine. This medicine is for use in adults (aged 18 and over). 2.
What you need to know before you take it
e Relistor
Do not use Relistor if you are allergic to methylnaltrexone bromide or any of the other ingredients of this medicine (listed in section 6). If you or your doctor know that your bowels were or are obstructed or your bowels are in a state where there is an immediate need for surgical intervention (which has to be diagnosed by your doctor). Warnings and precautions Talk to your doctor or pharmacist before using Relistor If you have severe stomach symptoms which continue or get worse, contact your doctor immediately because these could be symptoms of a hole developing in the bowel wall (intestinal perforation). See section 4. If you have Crohn ́s disease or gastrointestinal ulcers
–
If you feel sick, vomit, shiver, sweat, have belly pain and/or feel a fast heart beat shortly after taking Relistor talk to your doctor If you have severe liver or kidney disease. If you develop severe or persistent diarrhoea (passing of frequent watery stools), discontinue therapy and contact your doctor immediately. It is important to be near a toilet with assistance available if necessary, since bowel movement may happen within 30 minutes after injection of the medicine. Please talk to your doctor if you experience stomach ache which continues, nausea, (feeling sick) or vomiting (being sick) that is new or becomes worse. Please also talk to your doctor if you have a colostomy, a tube in your abdomen (peritoneal catheter), or suffer from diverticular disease or faecal impaction as this medicine should be used carefully in these circumstances. If you are receiving supportive care for your advanced illness, this medicine will only be used for a limited period of time which will usually be less than 4 months.. This medicine should not be used for treatment of patients with constipation which is not related to opioid use. If you have suffered from constipation before you had to take opioids (for pain), please talk to your doctor.
Children and adolescents Do not give this medicine to children and adolescents under the age of 18 because the potential risks and benefits are not known. Other medicines and Relistor Tell your doctor or pharmacist if you are taking, have recently taken, or might take any other medicines. Your doctor may allow you to take other medicines, including those used for constipation. Pregnancy and breast-feeding The effects of methylnaltrexone bromide in pregnant women are not known. Your doctor will decide if you can use Relistor if you are pregnant. Women using this medicine should not breast-feed, since it is not known if methylnaltrexone bromide passes into human breast milk. If you are pregnant or breastfeeding, think you may be pregnant or are planning to have a baby, ask your doctor or pharmacist for advice before taking this medicine. Driving and using machines Dizziness is a common side effect of this medicine. This may have an effect on your ability to drive and use machines. Important information about some of the ingredietns of Relistor This medicine contains less than 1 mmol sodium (23 mg) per dose i.e., essentially "sodium free." 3.
How to take it
Relistor
Always use this medicine exactly as your doctor has told you. Check with your doctor or pharmacist if you are not sure. The recommended dose for patients with long-term pain (except patients receiving supportive care for advanced illness) is 12 mg methylnalrexone bromide (0.6 mL of solution) given as an injection under the skin , as needed, but at least given 4 times a week and up to once a day (7 times a week).
The 8 mg pre-filled syringe will only be used to treat these patients if the dose needs to be decreased because of another medical problem. The recommended dose for patients receiving supportive care in advanced illness is 8 mg methylnaltrexone bromide (0.4 mL of solution) for patients weighing 38-61 kg or 12 mg (0.6 mL of solution) for patients weighing 62-114 kg. The dose is given every 48 hours (every two days) as an injection under the skin. Your doctor will determine your dose. If you weigh less than 38 kg or more than 114 kg you should use Relistor vials because the correct dose cannot be accurately delivered with these pre-filled syringes. This medicine is given by an injection under the skin (by subcutaneous injection) in either (1) your upper legs (thighs), (2) your abdomen (stomach), and (3) your upper arm (if not self-injecting). (See INSTRUCTIONS FOR PREPARING AND GIVING AN INJECTION OF RELISTOR at the end of this leaflet.) You may have a bowel movement within a few minutes to a few hours of the injection; therefore, it is recommended to have a toilet facility or bedpan near you. If you use more Relistor than you should If you have used more of this medicine than you should (either by injecting too much on a single occasion or by using more than one injection in 24 hours), you may feel dizzy when standing up, so talk to a doctor or pharmacist immediately. Always have the outer carton of the medicine with you, even if it is empty. If you forget to use Relistor If you forget a dose, talk to your doctor or pharmacist as soon as possible. Do not take a double dose to make up for a forgotten dose. If you stop using Relistor You should talk to a doctor or pharmacist if you want to stop using this medicine. If you have any further questions on the use of this medicine, ask your doctor or pharmacist. 4.
Possible side effects
Like all medicines, this medicine can cause side effects, although not everybody gets them. Cases of a hole developing in the bowel wall (gastrointestinal perforation) have been reported in patients using Relistor. How often this happens is not known from the data that is available. If you get a stomach ache that is either severe or will not go away, stop taking this medicine and call your doctor straight away. The following side effects are very common and may affect more than 1 in 10 people. If you experience any of these side effects, which are either severe or will not go away, you should talk to your doctor: •
Abdominal pain (belly ache)
•
Nausea (feeling sick)
•
Diarrhoea (passing of frequent watery stools)
•
Flatulence (passing wind)
Other common side effects that may affect up to 1 in 10 people are: •
Dizziness (light-headed)
•
Opioid-withdrawal-like symptoms (any of the following: feeling cold, shivering, runny nose, sweating, hair standing on end, blushing, fast heart beat)
•
Reaction at the site of injection (e.g., stinging, burning, pain, redness, oedema)
•
Vomiting
Reporting of side effects If you get any side effects, talk to your doctor or pharmacist. This includes any possible side effects not listed in this leaflet. You can also report side effects directly via the Yellow Card Scheme at www.mhra.gov.uk/yellowcard or search for MHRA Yellow Card in the Google Play or Apple App Store. By reporting side effects you can help provide more information on the safety of this medicine. 5.
How to store it
Relistor
Keep this medicine out of the sight and reach of children. Do not use this medicine after the expiry date which is stated on the carton, tray lid and syringe label after EXP. The expiry date refers to the last day of that month. Store below 30°C. Keep the pre-filled syringe in the outer carton in order to protect from light. Only use this medicine if the solution is clear, colourless to pale yellow, and does not contain flakes or particles. Do not throw away any medicines via wastewater or household waste. Ask your pharmacist how to thow away medicines that you no longer use. These measures will help to protect the environment. 6.
Contents of the pack and other information
What Relistor contains The active substance is methylnaltrexone bromide. Each syringe of 0.4 mL contains 8 mg methylnaltrexone bromide. Each syringe of 0.6 mL contains 12 mg methylnaltrexone bromide. One mL of solution contains 20 mg methylnaltrexone bromide. The other ingredients are sodium chloride, sodium calcium edetate, glycine hydrochloride, water for injections, hydrochloric acid (to adjust pH) and sodium hydroxide (to adjust pH). What Relistor looks like and contents of the pack Relistor is a solution for injection. It is clear, colourless to pale yellow, and does not contain flakes or particles. The following packs are available:
Pack containing 4, 7, 8 or 10 pre-filled syringes with a needle shield. Not all pack sizes may be marketed. Marketing Authorisation Holder Bausch Health Ireland Limited 3013 Lake Drive Citywest Business Campus Dublin 24, D24PPT3 Ireland Manufacturer Bausch Health Poland Sp. z o. o., ul. Kosztowska 21, 41-409 Mysłowice, Poland
This leaflet was last revised in 01/2024 ————————————————————————————————————————–PATIENT CHECKLIST This section contains important questions that you will need to answer before you take Relistor, and during treatment with Relistor. If you answer No to any of the following questions during the course of treatment with your medicine please contact your doctor, nurse or pharmacist. 1. 2. 3. 4. 5.
Are you receiving opioid therapy (for example morphine or codeine) for your illness? Has it been 48 hours or longer since your last bowel movement? Are you familiar with the technique of self injection or have you discussed this with your doctor (or nurse or pharmacist)? Are you mobile enough to reach the toilet, or do you have a caregiver looking after you who can help? Do you have a contact number for your community nurse or the health centre?
INSTRUCTIONS FOR PREPARING AND GIVING AN INJECTION OF RELISTOR This section is divided into the following subsections: Introduction Step 1: Preparing for an injection Step 2: Choosing and preparing an injection site Step 3: Injecting Relistor pre-filled syringe Step 4: Disposing of supplies
Introduction The following instructions explain how to prepare and give an injection of Relistor when using a prefilled syringe. Please read and follow them step by step. You will be instructed by your doctor, nurse or pharmacist on the techniques of self-injection. Do not attempt to administer an injection until you are sure that you understand how to prepare and give an injection. Important notes: • • •
Do not use a Relistor pre-filled syringe more than one time, even if there is medicine in the syringe. Safely throw away the Relistor pre-filled syringe after use (Step 4). To avoid needle-stick injuries, do not recap used needles.
Gather the supplies you will need for your injection: 1. 2. 3. 4.
Relistor pre-filled syringe Alcohol swab Cotton ball or gauze Adhesive plaster
Step 1: Preparing for an injection 1. Select a flat, clean, well-lit working surface where you can lay out the contents of your Relistor carton. Make sure you have set aside a proper amount of time to complete the injection. 2. Wash your hands thoroughly with soap and warm water.
3. Look at the pre-filled syringe. Make sure that the dose prescribed by your doctor matches the dose on the pre-filled syringe label.
4. Make sure the liquid in the pre-filled syringe is clear and colourless to pale yellow, and does not have any particles in it. If not, do not use the pre-filled syringe and call your nurse, doctor or pharmacist. 5. Firmly hold the barrel of the pre-filled syringe and pull the needle cap straight off. Do not touch the needle or allow it to touch any surface.
Step 2: Choosing and preparing an injection site 1. The three areas of the body recommended for injection of Relistor are: (1) your upper legs (thighs), (2) your abdomen (stomach), and (3) your upper arm (only if injecting another person).
2. It is recommended to move to a different site each time an injection is given. Avoid repeated injections at the exact same spot previously used. Do not inject into areas where the skin is tender, bruised, red, or hard. Avoid areas with scars or stretch marks. 3. Clean the injection site with an alcohol swab and let it dry. Do not touch this area again before giving the injection.
Step 3: Injecting Relistor pre-filled syringe 1. Hold the syringe in one hand like a pencil. Use the other hand to gently pinch the cleaned area of skin and hold it firmly.
2. Push the full length of the needle into the skin at a slight angle (45 degrees) with a quick, short motion.
3. After the needle is inserted, let go of the skin and slowly push the plunger all the way down until the pre-filled syringe is empty.
4. Quickly pull the needle out of the skin, being careful to keep it at the same angle as it was inserted. Release your thumb from the plunger to allow the protective sleeve to cover the needle. There may be a little bleeding at the injection site.
5. You can press a cotton ball or gauze over the injection site. Do not rub the injection site. If needed, you may cover the injection site with a plaster.
Step 4: Disposing of supplies The pre-filled syringe should NEVER be reused. NEVER recap the needle. Dispose of the pre-filled syringe as instructed by your doctor, nurse or pharmacist. Place used pre-filled syringe in a closable, puncture-resistant container. You may use a sharps container (such as a yellow biohazard container). Ask your doctor, nurse or pharmacist for instructions on the right way to throw away (dispose of) the container. There may be local laws about how you should throw away used needles and syringes.
Frequently asked questions about Relistor 12 mg Solution for injection in pre-filled syringes
How do I take Relistor 12 mg Solution for injection in pre-filled syringes?
Relistor 12 mg Solution for injection in pre-filled syringes comes as injection containing 12mg. Always follow the dose your doctor or pharmacist has given you, and read the leaflet that comes with the medicine.
What is the active substance in Relistor 12 mg Solution for injection in pre-filled syringes?
The active substance in Relistor 12 mg Solution for injection in pre-filled syringes is methylnaltrexone bromide.
Where does this information come from?
This leaflet reproduces the patient information leaflet approved for Relistor 12 mg Solution for injection in pre-filled syringes, as published on the electronic medicines compendium (emc). The version printed inside your medicine’s packaging is the one that applies to you.
Can I get Relistor 12 mg Solution for injection in pre-filled syringes without a prescription?
Whether a medicine is available over the counter or on prescription only depends on its licence. Check the leaflet, or ask your pharmacist — they can tell you straight away.
About this leaflet
The text above reproduces the patient information leaflet approved for this medicine, restructured for easier reading.
- Source: electronic medicines compendium (emc), Datapharm
- Active substance: methylnaltrexone bromide
- Official document: view the original leaflet on emc →
⚕For healthcare professionals — Summary of Product Characteristics (SmPC)Full SmPC: dosage, interactions, contraindications, warnings+
4.1. Therapeutic indications
Relistor is indicated for the treatment of opioid-induced constipation when response to laxative therapy has not been sufficient in adult patients, aged 18 years and older.
4.2. Posology and method of administration
Posology
Opioid-induced constipation in adult patients with chronic pain (except palliative care patients with advanced illness)
The recommended dose of methylnaltrexone bromide is 12 mg (0.6 mL of solution) subcutaneously, as needed, given as at least 4 doses weekly up to once daily (7 doses weekly).
In these patients, the treatment with usual laxatives should be stopped when commencing treatment with Relistor (see section 5.1).
Opioid-induced constipation in adult patients with advanced illness (palliative care patients)
The recommended dose of methylnaltrexone bromide is 8 mg (0.4 mL of solution) (for patients weighing 38-61 kg) or 12 mg (0.6 mL of solution) (for patients weighing 62-114 kg).
The usual administration schedule is one single dose every other day. Doses may also be given with longer intervals, as per clinical need.
Patients may receive two consecutive doses 24 hours apart, only when there has been no response (bowel movement) to the dose on the preceding day.
Patients weighing less than 38 kg or greater than 114 kg should use Relistor vials because the recommended mg/kg dose cannot be accurately delivered with the pre-filled syringe.
In palliative care patients, Relistor is added to usual laxative treatment (see section 5.1).
Special populations
Elderly population
No dose adjustment is recommended based on age (see section 5.2).
Patients with renal impairment
In patients with severe renal impairment (creatinine clearance less than 30 mL/min), the dose of methylnaltrexone bromide should be reduced from 12 mg to 8 mg (0.4 mL of solution) for those weighing 62 to 114 kg. Patients with severe renal impairment whose weight falls outside the 62 to 114 kg range (see section 5.2) need to reduce their mg/kg dose by 50 %. These patients should use Relistor vials and not the pre-filled syringe. There are no data available from patients with end-stage renal impairment on dialysis, and methylnaltrexone bromide is not recommended in these patients (see section 4.4).
Patients with hepatic impairment
No dose adjustment is necessary in patients with mild to moderate hepatic impairment (see section 5.2).
There are no data available from patients with severe hepatic impairment (Child-Pugh Class C), and methylnaltrexone bromide is not recommended in these patients (see section 4.4).
Paediatric population
The safety and efficacy of Relistor in children less than 18 years has not been established. No data are available.
Method of administration
Relistor is given as a subcutaneous injection.
It is recommended to rotate injection sites. It is not recommended to inject into areas where the skin is tender, bruised, red, or hard. Areas with scars or stretch marks should be avoided.
The three areas of the body recommended for injection of Relistor are upper legs, abdomen, and upper arms.
Relistor can be injected without regard to food.
4.3. Contraindications
Hypersensitivity to the active substance or to any of the excipients listed in section 6.1.
Use of methylnaltrexone bromide in patients with known or suspected mechanical gastrointestinal obstruction, patients at increased risk for recurrent obstruction or in patients with acute surgical abdomen is contraindicated due to the potential for gastrointestinal perforation.
4.4. Special warnings and precautions for use
Severity and worsening of symptoms
Patients should be advised to promptly report severe, persistent, and/or worsening symptoms.
If severe or persistent diarrhoea occurs during treatment, patients should be advised not to continue therapy with methylnaltrexone bromide and consult their physician.
Constipation not related to opioid use
The activity of methylnaltrexone bromide has been studied in patients with constipation induced by opioids. Therefore, Relistor should not be used for treatment of patients with constipation not related to opioid use.
Rapid onset of bowel movements
Data from clinical trials suggest treatment with methylnaltrexone bromide can result in the rapid onset (within 30 to 60 minutes on average) of a bowel movement.
Duration of treatment
Opioid-induced constipation in adult patients with advanced illness
Methylnaltrexone bromide treatment has not been studied in adult patients with advanced illness in clinical trials for longer than 4 months, and should therefore only be used for a limited period (see section 5.1).
Hepatic or renal impairment
Methylnaltrexone bromide is not recommended in patients with severe hepatic impairment or with end-stage renal impairment requiring dialysis (see section 4.2).
Gastrointestinal (GI) conditions and GI perforation
Methylnaltrexone bromide should be used with caution in patients with known or suspected lesions of the GI tract.
Use of methylnaltrexone bromide in patients with colostomy, peritoneal catheter, active diverticular disease or fecal impaction has not been studied. Therefore, Relistor should only be administered with caution in these patients.
Cases of GI perforation have been reported in the postauthorisation period after use of methylnaltrexone bromide in patients with conditions that may be associated with localized or diffuse reduction of structural integrity in the wall of the gastrointestinal tract (e.g., peptic ulcer disease, pseudo obstruction (Ogilvie's syndrome), diverticular disease, infiltrative gastrointestinal tract malignancies or peritoneal metastases). The overall risk-benefit profile should be taken into account when using methylnaltrexone bromide in patients with these conditions or other conditions which might result in impaired integrity of the gastrointestinal tract wall (e.g., Crohn's disease). Patients should be monitored for severe, persistent, or worsening abdominal pain; methylnaltrexone bromide should be discontinued if this symptom occurs.
Opioid withdrawal
Symptoms consistent with opioid withdrawal, including hyperhidrosis, chills, vomiting, abdominal pain, palpitations, and blushing have occurred in patients treated with methylnaltrexone bromide. Patients having disruptions to the blood-brain barrier may be at increased risk for opioid withdrawal and/or reduced analgesia. This should be taken into account when prescribing methylnaltrexone bromide for such patients.
Sodium content
This medicinal product contains less than 1 mmol sodium (23 mg) per dose, i.e. essentially sodium-free.
4.5. Interaction with other medicinal products and other forms of interaction
Methylnaltrexone bromide does not affect the pharmacokinetics of medicinal products metabolised by cytochrome P450 (CYP) isozymes. Methylnaltrexone bromide is minimally metabolised by CYP isozymes. In vitro metabolism studies suggest that methylnaltrexone bromide does not inhibit the activity of CYP1A2, CYP2E1, CYP2B6, CYP2A6, CYP2C9, CYP2C19 or CYP3A4, while it is a weak inhibitor of the metabolism of a model CYP2D6 substrate. In a clinical drug interaction study in healthy adult male subjects, a subcutaneous dose of 0.3 mg/kg of methylnaltrexone bromide did not significantly affect the metabolism of dextromethorphan, a CYP2D6 substrate.
The organic cation transporter (OCT)-related drug-drug interaction potential between methylnaltrexone bromide and an OCT inhibitor was studied in 18 healthy subjects by comparing the single-dose pharmacokinetic profiles of methylnaltrexone bromide before and after multiple 400 mg doses of cimetidine. The renal clearance of methylnaltrexone bromide was reduced following multiple-dose administration of cimetidine (from 31 L/h to 18 L/h). However, this resulted in a small reduction in total clearance (from 107 L/h to 95 L/h). Consequently, no meaningful change in AUC of methylnaltrexone bromide, in addition to Cmax, was observed before and after multiple-dose administration of cimetidine.
4.6. Fertility, pregnancy and lactation
Pregnancy
There are no adequate data with the use of methylnaltrexone bromide in pregnant women. Studies in animals have shown reproductive toxicity at high doses (see section 5.3). The potential risk for humans is unknown. Methylnaltrexone bromide should not be used during pregnancy unless clearly necessary.
Breast-feeding
It is unknown whether methylnaltrexone bromide is excreted in human breast milk. Animal studies have shown excretion of methylnaltrexone bromide in breast milk. A decision on whether to continue/discontinue breast-feeding or to continue/discontinue therapy with methylnaltrexone bromide should be made, taking into account the benefit of breast-feeding to the child and the benefit of methylnaltrexone bromide therapy to the woman.
Fertility
Subcutaneous injections of Relistor at 150 mg/kg/day decreased fertility in rats. Doses up to 25 mg/kg/day (18 times the exposure [AUC] in humans at a subcutaneous dose of 0.3 mg/kg) did not affect fertility or general reproductive performance.
4.7. Effects on ability to drive and use machines
Methylnaltrexone bromide has minor influence on the ability to drive and use machines. Dizziness may occur, and this may have an effect on the ability to drive and use machines (see section 4.8).
4.8. Undesirable effects
Summary of the safety profile
The most common adverse reactions in all patients exposed to methylnaltrexone bromide during all phases of placebo-controlled studies were abdominal pain, nausea, diarrhoea and flatulence. Generally, these reactions were mild or moderate.
Tabulated list of adverse reactions
The adverse reactions are classified as: very common (≥1/10); common (≥1/100 to <1/10); uncommon (≥1/1,000 to <1/100); rare (≥1/10,000 to <1/1,000); very rare (<1/10,000) and not known (cannot be estimated from the available data). Within each frequency grouping, adverse reactions are presented in order of decreasing seriousness.
Nervous system disorders
Common: Dizziness
Common: opioid-withdrawal-like symptoms ( like chills, tremor, rhinorrhea, piloerection, hot flush, palpitation, hyperhidrosis, vomiting, abdominal pain)
Gastrointestinal disorders
Not known: Gastrointestinal perforation (see section 4.4)
Common: Vomiting
Very common: Abdominal pain, nausea, diarrhoea, flatulence
Skin and subcutaneous tissue disorders
Common: Injection site reactions (e.g. stinging, burning, pain , redness, oedema)
Reporting of suspected adverse reactions
Reporting suspected adverse reactions after authorisation of the medicinal product is important. It allows continued monitoring of the benefit/risk balance of the medicinal product. Healthcare professionals are asked to report any suspected adverse reactions via the national reporting system listed in Appendix V.
4.9. Overdose
A study of healthy volunteers noted orthostatic hypotension associated with a dose of 0.64 mg/kg administered as an intravenous bolus.
In the event of an overdose, signs and symptoms of orthostatic hypotension should be monitored and reported to a physician. Treatment should be initiated as appropriate.
🇷🇴 Known in Romania as
Medicines sold in Romania with the same active substance: Cunoscut în România ca
- RELISTOR 12 mg/0,6 ml prescriptionMETHYLNALTREXONUM · injection / infusion
Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Romanian medicines in the UK →
🇵🇱 Known in Poland as
Medicines sold in Poland with the same active substance: W Polsce znany jako
- RelistorMethylnaltrexoni bromidum · injection / infusion
Same active substance. The strength, the form and whether you need a prescription can differ. Always ask a pharmacist before you switch. Polish medicines in the UK →
💬 Ask about this leaflet
Ask anything about Relistor 12 mg Solution for injection in pre-filled syringes. The assistant answers only from this leaflet — if the leaflet does not cover it, it will say so. It does not give medical advice.
Answers come from the patient leaflet published on the electronic medicines compendium (emc). They are not medical advice. Ask a pharmacist or your GP if you are unsure. For urgent help call NHS 111, or 999 in an emergency.