Relistor

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Relistor

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Method of action: Laxative

Treatment option:

Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Relistor

Property Description
Active Ingredient Methylnaltrexone Bromide
Dosage Form(s) Oral Tablet, Solution for Injection
Pharmacological Class Peripheral Opioid Receptor Antagonist (P-ORA)
General Purpose Counteracts opioid effects in the bowel
Origin Synthetic derivative (Quaternary structure)

What Type of Medication is Relistor (Methylnaltrexone Bromide)?

Relistor is the prescription-only medication whose active component is Methylnaltrexone Bromide. It is classified as a Peripheral Opioid Receptor Antagonist (P-ORA), a specific pharmacological class. The drug is a synthetic derivative of the opioid antagonist naltrexone; however, its distinctive quaternary structure prevents it from efficiently crossing the Blood-Brain Barrier (BBB). This chemical design is the differentiating factor for Methylnaltrexone Bromide as it targets the gastrointestinal (GI) tract without interfering with the opioid's central pain-relieving effects, making it a single-ingredient product.

Composition and Available Forms of Methylnaltrexone Bromide

The medication is composed exclusively of the active ingredient Methylnaltrexone Bromide. It is supplied in two distinct pharmaceutical preparations for adult patients. These dosage forms include an oral tablet and a sterile aqueous solution for injection provided in both unit-dose vials and pre-filled syringes for subcutaneous injection (SC injection). The availability of both the oral and subcutaneous options allows for flexibility in the route of administration for patient groups experiencing chronic non-cancer pain or advanced illness.

What is the General Purpose of a Peripheral Opioid Receptor Antagonist?

The general purpose of a P-ORA is the restoration of bowel function and motility. It achieves this by performing selective peripheral mu-opioid receptor blockade within the gut, thereby counteracting the constipating effects caused by opioid pain medication. Methylnaltrexone Bromide is clinically recognized as an adjunct therapy intended to address Opioid-induced Constipation (OIC) in adult patients whose symptoms have not responded adequately to conventional laxatives. This targeted action supports patients who require chronic opioid therapy by providing a specific solution for OIC that avoids compromising their central pain management.

Regulatory References

  1. Methylnaltrexone: MedlinePlus Drug Information

What side effects are possible with Relistor?

Possible Side Effects and Safety Information

Relistor (methylnaltrexone bromide) is a medication that requires careful consideration of its potential adverse reactions, which are primarily gastrointestinal in nature. Safety information is based on governmental regulatory documents, including those from the FDA and EMA.

Common and Very Common Adverse Reactions

Clinical studies indicate that the most frequent side effects are related to the gastrointestinal system and are often mild to moderate. Very common reactions (occurring in 1 out of 10 people or more) can include abdominal pain, nausea, diarrhea, and flatulence. Common reactions (occurring in 1 out of 100 people to less than 1 out of 10) can include dizziness, vomiting, hyperhidrosis (increased sweating), and opioid-withdrawal-like symptoms.

Serious and Clinically Significant Adverse Reactions

  • Gastrointestinal Perforation: Rare cases of a tear in the stomach or intestinal wall have been reported in post-marketing experience, particularly in patients with advanced illness and conditions that compromise the structural integrity of the GI tract (e.g., peptic ulcer, cancer). Due to this risk, the drug is contraindicated in patients with known or suspected mechanical gastrointestinal obstruction.
  • Opioid Withdrawal: Symptoms consistent with opioid withdrawal, such as chills, anxiety, rhinorrhea, and abdominal pain, have occurred. Patients with disruptions to the blood-brain barrier may be at increased risk.
  • Severe Diarrhea: If severe or persistent diarrhea develops, it is an official caution that treatment should be discontinued.

Population-Specific Safety Notes

A dose reduction is recommended for patients with severe renal impairment (creatinine clearance <30 mL/min). Caution is advised when using the medication in patients with known or suspected GI tract lesions, and its use is generally not recommended in patients with end-stage renal impairment requiring dialysis. Additionally, due to the potential risk of precipitating opioid withdrawal in a fetus or breastfed infant, the use of Relistor during pregnancy and lactation is generally not recommended.

Overdose and Emergency Response

Overdose and When to Seek Help

Overdose with methylnaltrexone bromide is characterized by an exaggeration of its pharmacological action and potential systemic effects, as documented in regulatory information. These presentations require specific management and monitoring.

Documented Manifestations: Overdose may present with signs associated with an exaggerated peripheral antagonist effect, including symptoms consistent with opioid withdrawal such as chills, rhinorrhea, and diaphoresis (sweating). High exposure has also been documented to cause orthostatic hypotension and related systemic effects, such as dizziness or faintness. Severe or persistent diarrhea is another documented presentation that warrants physician consultation.

Urgent Medical Action: The most critical concern documented in regulatory labeling is the risk of gastrointestinal (GI) perforation, especially in vulnerable patients. Immediate medical attention must be sought if the patient develops severe, persistent, or worsening abdominal pain. Following suspected overdose, the prescribed clinical course is symptomatic and supportive management, as no specific antidote is available. Patients must be closely monitored for signs of both opioid withdrawal and orthostatic hypotension to ensure appropriate care.

Special Consideration: Patients with severe renal impairment are noted to have a risk for increased systemic exposure to the drug, which may heighten the potential for adverse effects following a high-exposure event.

Therapeutic Uses of Relistor

What Relistor Treats: Main Uses and Benefits

This medication may be part of symptomatic management for constipation linked to opioid pain medication. It is commonly used when short-term symptomatic assistance is needed.

Targeted Therapeutic Support

This medication is primarily used for adult patients with Opioid-Induced Constipation (OIC) when prior treatment with non-specific laxatives has not been sufficient. It is applied in addressing symptom clusters that interfere with daily comfort, such as infrequent bowel movements and the physical discomfort from incomplete evacuation. The treatment is relevant in contexts marked by increased discomfort where symptoms may intensify temporarily.

“It helps to provide support that assists with maintaining functional stability and contributes to easing the overall symptom load.”

The treatment plays a role in managing OIC in individuals receiving sustained opioid pain relief for chronic non-cancer pain or advanced illness. This supportive role may assist with maintaining functional stability when managing conditions where symptoms create noticeable physiological strain.

Quick Fact: Use in Refractory OIC Contexts The medication is considered relevant in clinical settings that involve acute or unstable symptom patterns, supporting patients during episodes of heightened discomfort.

Eligibility and Restrictions for Use

Relistor is an opioid antagonist intended solely for the treatment of opioid-induced constipation (OIC) in adult patients (18 years and older).


Contraindicated Populations

Use of Relistor is strictly contraindicated and must be avoided in certain patients due to the risk of gastrointestinal perforation. These include patients with a known or suspected mechanical gastrointestinal obstruction, those at increased risk of recurrent obstruction, or individuals with an acute surgical abdomen. The drug is also prohibited for anyone with a known hypersensitivity to methylnaltrexone bromide or its components.


Use Restrictions and Limitations

Official labeling defines several groups for whom use is restricted or not recommended:

  • Pediatric Patients: Safety and effectiveness have not been established for children under 18 years of age.
  • Constipation Type: It must not be used to treat constipation that is not induced by opioids.
  • Severe Organ Impairment: Use is not recommended for patients with severe hepatic impairment (Child-Pugh Class C) or those with end-stage renal impairment requiring dialysis.
  • Pregnancy/Lactation: Use during pregnancy is generally avoided as it may precipitate opioid withdrawal in a fetus. Breastfeeding is not recommended due to the potential risk of adverse reactions in the infant.

What should I know about interactions with other medicines?

Interactions with Other Medicines and Products

The interaction profile for Methylnaltrexone Bromide, the active ingredient in Relistor, is defined by specific pharmacodynamic and pharmacokinetic patterns documented in regulatory sources. This information is critical for determining appropriate administration conditions.

Pharmacodynamic Interactions

Co-administration with other opioid antagonists carries a documented risk of precipitating opioid withdrawal. This is due to an additive effect on opioid receptor blockade and is a key caution for patients physically dependent on opioid therapy.

Pharmacokinetic and Exposure Alterations

Interacting Factor Interaction Effect
High-Fat Meal (Oral Tablet) Administration of the oral tablet with a high-fat meal results in a documented increase in systemic drug exposure (AUC and Cmax).
Severe Hepatic Impairment Patients with severe liver disease (Child-Pugh Class C) exhibit a formal increase in exposure compared to individuals with normal hepatic function.
Metabolic Enzyme Inhibitors Strong inhibitors of P-glycoprotein (P-gp), CYP3A4, or CYP2D6 do not result in clinically relevant interactions and do not require mandatory co-administration restrictions.

Timing and Restrictions

No mandatory time-based separation rules for co-administering this medication with other medicinal products are documented in official regulatory labels. The official interaction profile primarily highlights specific caution required for co-administration with other opioid antagonists and the influence of food on the oral dosage form.

Mechanism of Action

Methylnaltrexone Bromide acts as a selective antagonist at the peripheral mu-opioid receptor, which is the primary molecular target located within the walls of the Gastrointestinal (GI) tract and the Enteric Nervous System (ENS). The drug physically blocks these receptors, displacing the opioid molecules and reversing the profound inhibitory signal imposed on the gut.

The drug’s structure, a quaternary amine, prevents it from efficiently crossing the Blood-Brain Barrier (BBB). This pharmacochemical restriction ensures that the drug can reverse mu-opioid receptor inhibition in the gut while maintaining the mu-receptor activity in the Central Nervous System (CNS).

By reversing the inhibitory signaling, the drug reactivates intestinal peristalsis (coordinated smooth muscle contractions) and supports the normalization of fluid and electrolyte transport across the gut lining. Opioid action typically increases water absorption and decreases secretion; the mechanism of action reverses this sequence. The re-establishment of both motility and fluid balance in the gut is the ultimate physiological consequence of the antagonism.

Dosage and Administration Information

How Relistor is Used: Official Administration Guidelines

Relistor (methylnaltrexone bromide) is administered via two distinct official routes: the oral tablet (150 mg strength) and the solution for subcutaneous injection (SC injection) available in 8 mg and 12 mg single-use preparations. The general usage pattern is strictly defined by the patient’s underlying condition and the specific formulation used.

Standard Dosing Regimens and Frequency

The frequency and dose of the medication are context-dependent:

Indication Dosage Form and Dose Frequency Pattern
OIC in Chronic Non-Cancer Pain (CNCP) Oral: 450 mg (three 150 mg tablets) Once daily
OIC in Chronic Non-Cancer Pain (CNCP) SC Injection: 12 mg Once daily
OIC in Advanced Illness/Palliative Care SC Injection: 8 mg or 12 mg (weight-based) Intermittent, as needed (not more than once every 24 hours)

Administration Conditions and Adjustments

For the oral tablets, administration must occur on an empty stomach with water, at least 30 minutes before the first meal of the day to support the intended systemic delivery. The subcutaneous solution is administered into the thigh, abdomen, or upper arm, and rotation of the injection sites is a mandatory procedural step.

A critical requirement across both dosage forms is a mandatory dose reduction for patients with moderate to severe renal impairment (Creatinine Clearance < 60 mL/min). The dose is reduced to 150 mg once daily for the oral form and typically 6 mg once daily for the SC form in this population. If a dose is missed, patients should take the next dose as soon as possible, but must not exceed one dose per 24 hours. These precise instructions establish the standardized protocol for the medication’s use.

Recent Clinical Evidence

Research Evidence / Overview of Studies

Phase 2 and 3 Trials for Opioid-Induced Constipation (OIC)

The main body of research focuses on the compound's profile when studied for opioid-induced constipation (OIC) in patients with chronic non-cancer pain. These studies primarily evaluated its potential effect on bowel function and stool consistency in this patient group.

Research Focus on Compound Characteristics

Studies investigated the compound's characteristics.

Key Research Findings

  • Bowel Function: Two Phase 3 trials reported observed changes in the frequency of spontaneous bowel movements (SBM) compared to placebo in the patient groups studied. The trials aimed to assess the effect over a sustained period of time.
  • Duration of Effect: A large-scale study investigated the duration of effect and reported findings related to maintenance of SBM frequency over several weeks of continuous use.
  • Dosing Strategies Investigated: Research examined various dose levels. Higher doses were investigated but did not consistently report a greater difference in outcomes.

Studies in Other Conditions (Off-Label Research)

Limited research has also explored the compound's use in conditions beyond its primary focus, such as OIC in patients with advanced illness.

Advanced Illness OIC

  • One pilot study examined whether the compound showed an effect on bowel function in individuals with advanced illness, where opioid use is common.
  • The study design focused on patients who had not responded adequately to traditional laxative regimens.

Combination Therapies

  • Some researchers evaluated whether the compound, when combined with other specific OIC treatments, affected the overall speed of action or patient response.
  • Early findings from this area of research were mixed.

Research Findings on Tolerability

Clinical trials collected information on common events, focusing primarily on what was observed. The studies provided insight into patient tolerability across different dosing periods.

  • Reported Events: The most frequently reported adverse events included abdominal pain and flatulence.
  • Cardiovascular Monitoring: Specific trials were conducted to monitor any changes in heart rate or blood pressure across the duration of treatment. These studies contribute to the overall body of research exploring the compound’s effects.

Frequently Asked Questions (FAQ)

Common questions about Relistor (FAQ)


Q: Is Relistor the same as a regular laxative?

Relistor is classified by regulatory agencies as a Peripherally Acting μ-Opioid Receptor Antagonist (PAMORA), which is a specific type of drug that works by blocking the effects of opioids in the gut. It is not a traditional laxative, as it targets a specific problem caused by opioids. Official guidance indicates it is used for patients who have not responded adequately to conventional laxative treatments.


Q: Can I use Relistor with other pain medications?

Official product information states that Relistor is designed to counteract the constipating effects of opioid pain medications without interfering with the central pain relief they provide. However, co-administering Relistor with other opioid antagonists (medications that block opioid receptors) carries a documented risk of precipitating opioid withdrawal symptoms.


Q: Can Relistor affect my mood or make me feel anxious?

According to official safety information, symptoms consistent with opioid withdrawal have been reported as adverse reactions. These symptoms may include physical effects like chills and sweating, as well as psychological effects such as anxiety.


Q: Is there a difference in how the tablet and injection forms work?

Both the oral tablet and the injection contain the same active ingredient, methylnaltrexone, and share the same core mechanism of action. However, clinical trial comparisons reviewed by regulatory bodies reported that the subcutaneous (SC) injection showed numerically higher effectiveness than the oral tablet when used at the approved doses.


Q: Are there any laboratory tests needed before starting Relistor?

Official administration guidelines require mandatory dose adjustments for patients with moderate to severe renal impairment (kidney problems) or caution for those with severe hepatic impairment (liver problems). A healthcare professional typically uses these criteria to determine if assessment of kidney and liver function is needed before the medication is prescribed.


Q: Can Relistor make me dizzy or tired?

Regulatory documents list dizziness as a common adverse reaction that has been reported in clinical studies. Official adverse event reporting does not specifically include general fatigue or being tired as a common side effect.


Q: Does Relistor cause electrolyte issues?

The drug's mechanism of action is described in official sources as helping to restore disrupted fluid and electrolyte transport in the gut. While specific electrolyte imbalances are not listed as a primary adverse reaction, severe diarrhea is noted as a serious event in the product labeling.


Q: Why is Relistor sometimes called a peripherally acting mu-opioid receptor antagonist (PAMORA)?

Relistor is officially classified and described using the specific pharmacological acronym PAMORA. This term stands for Peripherally Acting μ-Opioid Receptor Antagonist, which precisely describes how the medication works only on the opioid receptors in the body's periphery, mainly the gut.


Q: How quickly should I expect Relistor to start working?

According to clinical trial data, a laxation response (bowel movement) after the first dose of the injection typically occurs within 4 hours for approximately half of the patients studied. Official information notes that the effect may begin as quickly as 30 minutes in some individuals.


Q: Can older adults (seniors) use Relistor safely?

Official medical information indicates that studies have not demonstrated problems specific to the elderly that would limit the use of the drug in this population. However, because kidney function often changes with age, dose adjustments are formally recommended for individuals with renal impairment, which is more common in older adults.


Q: Is Relistor a controlled substance?

Relistor is regulated as a prescription-only medicine in the United States and Canada. According to the U.S. Drug Enforcement Administration's schedules, the active ingredient, methylnaltrexone bromide, is not listed as a controlled substance.


Q: Does Relistor cause a sudden urge to go to the bathroom?

Official clinical guidance cautions that, particularly with the injection form, the laxative effect can begin quickly, which is why having ready access to toilet facilities or assistance is noted in the product information. This effect involves reactivating natural muscle contractions in the gut.


Q: What if Relistor doesn't work for me?

Official patient resources state that consulting a healthcare professional is indicated if the medication does not result in a bowel movement after taking it for 3 days.


Q: Does Relistor have a black box warning?

Official documentation confirms that Relistor does not carry a Black Box Warning (also known as a Boxed Warning) from the FDA. However, it is contraindicated in patients with a known or suspected mechanical gastrointestinal obstruction due to the serious risk of perforation.


Q: What are the signs of an allergic reaction to Relistor?

Regulatory sources indicate that signs of a severe allergic reaction (hypersensitivity) may include developing hives, experiencing difficult breathing, or showing swelling of the face, lips, tongue, or throat.


Q: Can I take Relistor with alcohol?

While official drug labels may not specifically detail an interaction with alcohol, some official interaction analysis resources list an interaction between methylnaltrexone and alcohol that warrants caution.


Q: Why might a doctor switch me from the tablet to the injection?

Based on clinical trial data reviewed by regulatory bodies, the subcutaneous (SC) injection form is reported to have shown numerically higher effectiveness compared to the oral tablet when used in comparative studies.


Q: Does Relistor interact with grapefruit juice?

Official drug information indicates that Relistor is the only medication in its class that is not metabolized by the CYP450 enzyme pathway, including the CYP3A4 enzyme. This is a key difference because many drug interactions occur through this pathway; official information indicates there is no clinically significant interaction with strong inhibitors of this enzyme, such as grapefruit juice.


Q: What if I have an ostomy? Can I still use Relistor?

Official clinical guidance indicates that the use of methylnaltrexone has not been studied in patients who have undergone a colostomy or who have a peritoneal catheter. Official guidance notes that the medication’s use requires caution in these patient groups due to the limited research.


Q: What is the typical duration of effect after a dose of Relistor?

Studies examining drug levels in the body show that the elimination half-life of methylnaltrexone in healthy adults ranges from 7.8 to 13.4 hours. The half-life is a measure of the time it takes for the drug concentration in the body to decrease by half, which relates to the total duration of the drug's activity.

How should Relistor be stored and disposed of?

How to Store and Dispose of Relistor?

The storage of Relistor (Methylnaltrexone) must adhere to the requirements specified for its dosage form.


Official Storage Conditions

Dosage Form Required Storage Temperature Protection Constraints
Injection Controlled room temperature (20 C to 25 C) Store in the original carton to protect from light. Do not freeze.
Oral Tablet Controlled room temperature (20 C to 25 C) Store in the original container, kept tightly closed.

Stability and Safety Requirements

Relistor injection vials are for single use only, and any unused solution must be discarded immediately. The medicine must be kept out of the sight and reach of children.

Disposal Instructions

Do not dispose of Relistor in household waste or wastewater. Unused or expired medication, including used pre-filled syringes, must be disposed of according to local regulatory requirements for pharmaceutical waste and sharps disposal.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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