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Relistor vs Symproic
Introduction
For patients dealing with opioid-induced constipation (OIC), certain drugs that are designed to alleviate the uncomfortable side effects of opioid use can provide significant relief. Relistor and Symproic are two such drugs that are prescribed for OIC. These medications work on the same basic principle, but they do exhibit some differences in their mechanisms of action.
Relistor, also known as methylnaltrexone bromide, works by blocking the opioid receptors in the gut without affecting those found in the brain, thereby reducing constipation symptoms without impacting pain management. On the other hand, Symproic or naldemedine binds to peripheral mu-opioid receptors within your gastrointestinal tract and inhibits their ability to slow bowel movement induced by opioids.
Both these medicines aim at improving your quality of life while you continue your required opioid regimen for pain management. Always consult with a healthcare provider before switching between these medications due to potential variations in individual response and side effect profile.
Relistor vs Symproic Side By Side
| Attribute | Relistor | Symproic |
|---|---|---|
| Brand Name | Relistor | Symproic |
| Contraindications | Should not be taken if using opioids for acute pain management, avoid grapefruit or grapefruit juice | Should not be taken if using opioids for acute pain management, avoid grapefruit or grapefruit juice |
| Cost | Approximately $2,700 for 90 tablets (12 mg) | Approximately $380 for 30 tablets (0.2 mg) |
| Generic Name | Methylnaltrexone Bromide | Naldemedine |
| Most Serious Side Effect | Severe stomach pain or diarrhea, symptoms of opioid withdrawal, reduced adrenal function | Severe stomach pain, bowel problems like bloody stools or lack of bowel movements, signs of opioid withdrawal |
| Severe Drug Interactions | May cause withdrawal symptoms in people with a physical dependence on opioids if taken incorrectly | May cause withdrawal symptoms in people with a physical dependence on opioids if taken incorrectly |
| Typical Dose | Oral dosages range from 12-24 mg/day, with 12 mg/day being sufficient for most | 0.2 mg/day, can be increased to 0.3 mg/day if insufficient response |
What is Relistor?
Methylnaltrexone (the generic name for Relistor) was a major advancement in the treatment of opioid-induced constipation. This medication, first approved by the FDA in 2008, works by blocking the effects of opioids on your digestive system without affecting their pain-relieving properties. It is commonly prescribed to individuals who are taking opioids for chronic non-cancer-related pain and suffering from constipation as a side effect.
On the other hand, Naldemedine (the generic name for Symproic), another drug used to treat opioid-induced constipation, was approved by FDA later - in 2017. Similar to Relistor, it also reduces constipation caused by opioids but does not interfere with their analgesic impact.
While both drugs act similarly and have comparable efficacy rates, there are some differences worth noting. For instance, while Relistor can be administered via injection or oral tablet form depending upon patient need and response rate; Symproic only comes as an orally taken tablet. Both medications may cause side effects like stomach pain or diarrhea but these symptoms often go away after several days of use.
What conditions is Relistor approved to treat?
Relistor and Symproic are both approved for the treatment of opioid-induced constipation, specifically:
- Opioid-induced constipation in adults with chronic non-cancer pain
- Opioid-induced constipation in adults with advanced illness or with pain caused by active cancer who require opioid dosage escalation.
How does Relistor help with these illnesses?
Relistor helps to manage opioid-induced constipation by blocking the action of opioids in the gut. It does this by binding and inhibiting peripheral mu-opioid receptors, so that their activation can be prevented for longer periods of time. Mu-opioid receptors are proteins found throughout the body, including in the gastrointestinal tract, where they slow down bowel movements when activated by opioids. This slowing down is what often causes constipation in individuals taking opioids for pain relief. Therefore, by inhibiting these receptors, Relistor can counteract the negative effects of opioids on bowel function and help patients manage their condition and stabilize their digestion.
What is Symproic?
Symproic is a brand name for naldemedine, which is a peripherally-acting mu-opioid receptor antagonist (PAMORA) that functions by blocking opioid receptors in the gut. It specifically counteracts the constipating effects caused by opioids without affecting their analgesic properties. Symproic was first approved by the FDA in 2017 and does not cross the blood-brain barrier, meaning it doesn't have any impact on centrally mediated opioid effects. This particular characteristic means that its side-effect profile differs from central nervous system acting drugs; for instance, it does not cause sedation or cognitive impairment. The mechanism of action can be beneficial particularly in patients suffering from opioid-induced constipation who do not respond well to typical laxatives or stool softeners.
What conditions is Symproic approved to treat?
Symproic is approved for the treatment of opioid-induced constipation (OIC) in adult patients who have chronic non-cancer pain. The effectiveness of Symproic has been established based on:
- Its capacity to increase bowel movements and reduce the need for rescue laxative use
- Improvement in symptoms of OIC including incomplete evacuation, hard stools, straining, and stomach discomfort.
How does Symproic help with these illnesses?
Naldemedine, the active ingredient in Symproic, acts as an opioid antagonist and plays a significant role in managing opioid-induced constipation. It works primarily within the gastrointestinal system by blocking opioid receptors there, thus reducing their potential to slow bowel movements. This mechanism directly counteracts one of the common side effects from long-term treatment with opioids: constipation. Relistor also addresses this issue but may be less suitable for certain patients due to its method of administration or possible adverse reactions. In contrast, Symproic has been seen as a more user-friendly option because it is orally administered and generally causes fewer side effects than other drugs used for similar purposes. Therefore, if you are struggling with opioid-induced constipation and find that typical laxatives aren't providing relief, Symproic might be considered a viable alternative treatment.
How effective are both Relistor and Symproic?
Both methylnaltrexone (Relistor) and naldemedine (Symproic) have established histories of success in treating opioid-induced constipation, and they were approved by the FDA within a decade of each other. Since they act on the same type of receptor but with different mechanisms, they may be prescribed under different circumstances. A direct clinical comparison between Relistor and Symproic has not yet been conducted; however, both drugs have shown efficacy in managing symptoms of opioid-induced constipation through separate clinical trials.
A 2008 review on methylnaltrexone demonstrated that it is effective in alleviating symptoms associated with opioid-induced constipation within 4 hours after injection. Its side effect profile is generally favorable compared to laxatives, leading to fewer gastrointestinal complaints such as abdominal pain or diarrhea. The study also reported that methylnaltrexone does not cross the blood-brain barrier due to its quaternary amine structure, which means it doesn’t interfere with the analgesic effects of opioids.
The approval for naldemedine came later in 2017 following positive results from two clinical trials showing its effectiveness against placebo over a span of 12 weeks. Despite being considered second-line treatment after non-pharmacological interventions and traditional laxatives fail, Symproic has proven itself as an important player in managing OIC when other treatments are insufficient. Similar to Relistor, Symproic works peripherally without affecting central nervous system activity thereby preserving the pain relief provided by opioids.
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At what dose is Relistor typically prescribed?
Oral dosages of Relistor range from 12-24 mg/day for adults, but studies have indicated that 12 mg/day is sufficient for treating opioid-induced constipation in most people. For Symproic, the recommended dosage is a fixed 0.2 mg once daily and can be taken with or without food. In either population, if there's no response to the medication after three days, consult your healthcare provider. The maximum dose of Relistor should not exceed 24mg per day while Symproic should not go beyond its fixed dose of 0.2 mg per day in any case.
At what dose is Symproic typically prescribed?
Symproic treatment typically begins with a dosage of 0.2 mg/day, taken as one pill once daily at any time of day, without regard to the timing of opioid use. If there is insufficient response to treatment after a week or two, your healthcare provider may increase the dose up to 0.3 mg/day. The maximum recommended dose for Symproic is 0.3 mg per day. It's important not to exceed this limit and always consult your healthcare provider for personalized advice about medication adjustments based on your medical condition and response.
What are the most common side effects for Relistor?
Side effects associated with Relistor can include:
- Stomach pain or discomfort
- Nausea
- Diarrhea, which can sometimes be severe
- Excessive sweating
- Hot flush or redness in the face (similar to vasodilation)
- Anxiety and restlessness
- Tremors
In contrast, Symproic has its own set of potential adverse reactions:
- Abdominal pain or discomfort
- Gas, bloating, distension
- Headache
-Nausea and vomiting -Dry mouth -Fatigue and asthenia (general weakness) -Increased liver enzymes
As always, it's important to consult your healthcare provider if you experience any undesirable side effects from these medications.
Are there any potential serious side effects for Relistor?
Although both Relistor and Symproic are generally well-tolerated, they can sometimes cause serious side effects. These include:
- Allergic reactions: symptoms may include hives, difficulty breathing, or swelling of the face, lips, tongue or throat.
- Severe stomach pain or diarrhea
- Symptoms of opioid withdrawal: feeling very hot or cold, sweating more than usual, body aches, feeling jittery/nervousness/anxiety/restlessness/agitation/shaking/tremors/dizziness/high blood pressure/fast heartbeat
- Reduced adrenal function: long-lasting fatigue; muscle weakness; loss of appetite; weight loss; abdominal pain.
If you experience any of these symptoms while taking either Relistor or Symproic it is important to seek medical help immediately. Be sure to discuss all potential side effects with your healthcare provider before starting treatment.
What are the most common side effects for Symproic?
The side effects of Symproic include:
- Stomach pain or discomfort
- Gas, nausea, and vomiting
- Headache, dizziness
- Abnormal sweating
- Changes in appetite leading to weight loss or gain
- Insomnia and other sleep disturbances
- Fast heartbeat that could potentially lead to palpitations
- Rash or itching skin Increased frequency of urination can also be a concerning side effect. In certain cases, patients have reported feeling agitated and experiencing muscle or joint pain. If you notice any significant changes while on this medication, it's essential to consult your healthcare provider immediately for guidance.
Are there any potential serious side effects for Symproic?
Symproic, while generally well tolerated, may in rare cases produce severe side effects. If you notice any of the following symptoms after taking Symproic, it is crucial to seek immediate medical attention:
- Signs of a serious allergic reaction such as hives; difficulty breathing or swallowing; swelling of your face, lips, tongue or throat
- Severe stomach pain that won't go away
- Bowel problems like bloody stools or lack of bowel movements
- Nausea and vomiting which could be signs of opioid withdrawal
- Rapid heartbeat
It's important to note these side effects are uncommon. However if they occur when taking Symproic, they should be taken seriously and require prompt medical consultation.
Contraindications for Relistor and Symproic?
Both Relistor and Symproic, along with most other opioid antagonist medications, may cause withdrawal symptoms in some people. If you notice signs of opioid withdrawal such as sweating, chills, diarrhea or increased heart rate after taking these drugs, please seek immediate medical attention.
Neither Relistor nor Symproic should be taken if you are concurrently using opioids for acute pain management. Always inform your healthcare provider about all the medications you are currently taking; switching from opioids to opioid antagonists like Relistor and Symproic requires careful medical supervision to prevent sudden onset of severe withdrawal symptoms.
You should also avoid consuming grapefruit or grapefruit juice while on these medications as it can increase the concentration of active drug ingredients in your blood and potentially enhance side effects. It is always recommended to discuss any dietary restrictions with your healthcare provider when starting a new medication regimen.
How much do Relistor and Symproic cost?
For the brand-name versions of these drugs:
- The cost for 90 tablets of Relistor (12 mg) is approximately $2,700 which works out to about $30/day irrespective of your dose.
- The cost for 30 tablets of Symproic (0.2 mg) averages around $380, working out to roughly $13/day.
Thus, if you are considering either drug for opioid-induced constipation relief, Symproic tends to be less expensive on a per-day treatment basis. However, it's important that price should not be your primary consideration in determining which of these drugs is best suited for you as they might have different side effects or interactions with other medications you are taking.
As far as generic versions go:
Currently, there isn't a generic version available in the U.S. market for either Relistor (methylnaltrexone bromide) or Symproic (naldemedine). Therefore costs remain significantly higher compared to other more common medications that do offer generic alternatives. As always consult with your healthcare provider before making any decisions regarding medication adjustments based on pricing alone.
Popularity of Relistor and Symproic
Methylnaltrexone bromide, available under the brand name Relistor, was estimated to have been prescribed to just over 700 thousand people in the US in 2020. Methylnaltrexone accounted for nearly a quarter of prescriptions aimed at treating opioid-induced constipation (OIC) in adults with chronic non-cancer pain. This medication is considered a peripheral mu-opioid receptor antagonist and its use has seen an upward trend since it gained FDA approval.
Naldemedine, sold under the brand Symproic, also treats OIC but saw fewer prescriptions compared to Relistor within that same year - about half a million were written for this drug. In general terms, Naldemedine accounts for approximately 20% of all medications prescribed specifically to treat OIC among adults suffering from persistent non-malignant pain. The prevalence of naldemedine has remained steady since it entered the market as another option beside methylnaltrexone.
Conclusion
Both Relistor (methylnaltrexone) and Symproic (naldemedine) have been proven effective in treating opioid-induced constipation, a common side effect of chronic opioid use for pain management. These medications are backed by rigorous clinical studies and meta-analyses indicating their effectiveness over placebo treatments. In some cases, these drugs may be used concurrently with laxatives or stool softeners to manage severe cases of opioid-induced constipation.
The two medications work differently: Relistor works by blocking the action of opioids on mu-opioid receptors in the gut without affecting analgesia in the central nervous system; Symproic also acts peripherally at these same receptors but is structurally different from methylnaltrexone.
While both drugs are available as brand-name prescriptions, they represent significant cost considerations for patients paying out-of-pocket due to lack of generic alternatives. Starting either drug might require an adjustment period before effects become noticeable.
The side effect profiles for both drugs are generally similar, with abdominal pain being among the most common adverse reactions reported. Both can cause withdrawal symptoms in people with a physical dependence on opioids if taken incorrectly or at higher-than-recommended doses. Patients starting treatment should immediately contact their healthcare provider if they experience severe stomach pain or diarrhea, signs of potential serious gastrointestinal conditions associated with these medications.
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Refrences
- Greenwood-Van Meerveld, B. (2008, December). Methylnaltrexone in the treatment of opioid-induced constipation. Clinical and Experimental Gastroenterology. Informa UK Limited.http://doi.org/10.2147/ceg.s3889
- Blair, H. A. (2019, July). Naldemedine: A Review in Opioid-Induced Constipation. Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40265-019-01160-7
- Yuan, C.-S. (2007, June). Methylnaltrexone Mechanisms of Action and Effects on Opioid Bowel Dysfunction and Other Opioid Adverse Effects. Annals of Pharmacotherapy. SAGE Publications.http://doi.org/10.1345/aph.1k009
- Galligan, J. J., & Sternini, C. (2016). Insights into the Role of Opioid Receptors in the GI Tract: Experimental Evidence and Therapeutic Relevance. Handbook of Experimental Pharmacology. Springer International Publishing.http://doi.org/10.1007/164_2016_116
- Blair, H. A. (2019, July). Naldemedine: A Review in Opioid-Induced Constipation. Drugs. Springer Science and Business Media LLC.http://doi.org/10.1007/s40265-019-01160-7
- Rauck, R. L., Slatkin, N. E., Stambler, N., & Israel, R. J. (2018, December). Safety of oral methylnaltrexone for opioid-induced constipation in patients with chronic noncancer pain. Journal of Pain Research. Informa UK Limited.http://doi.org/10.2147/jpr.s170086
- Argoff, C. E. (2020, June 16). Opioid-induced Constipation. The Clinical Journal of Pain. Ovid Technologies (Wolters Kluwer Health).http://doi.org/10.1097/ajp.0000000000000852