Symproic 0.2mg Tablets
It is used to treat constipation caused by some pain drugs.
Drug Class
Opioid-induced constipation agent
Pharmacologic Class
Peripherally acting mu-opioid receptor antagonist (PAMORA)
Pregnancy Category
Category C
FDA Approved
Jan 2017
DEA Schedule
Not Controlled
Overview
What is this medicine?
Symproic (naldemedine) is a medication used to treat constipation caused by opioid pain medicines. It works by blocking the effects of opioids specifically in the gut, helping you have bowel movements without affecting the pain relief from your opioid medication.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food.
Storing and Disposing of Your Medication
Keep your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom. It's essential to keep all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses.
To use this medication correctly, follow your doctor's instructions and read all the information provided. You can take this medication with or without food.
Storing and Disposing of Your Medication
Keep your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom. It's essential to keep all medications in a safe location, out of the reach of children and pets.
Missing a Dose
If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Take Symproic once daily, with or without food, at the same time each day.
- Continue to take your opioid pain medication as prescribed.
- Maintain adequate fluid intake and dietary fiber, as recommended by your healthcare provider.
- Engage in regular physical activity, if able, to help promote bowel regularity.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
0.2 mg orally once daily
Dose Range:
0.2 - 0.2 mg
Condition-Specific Dosing:
opioid-induced constipation (OIC) in adults with chronic non-cancer pain:
0.2 mg orally once daily
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established
Adolescent:
Not established
Dose Adjustments
Renal Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
0.2 mg orally once daily; monitor for adverse reactions. Avoid use in patients with end-stage renal disease (ESRD) on dialysis.
Dialysis:
Avoid use in patients with ESRD on dialysis due to increased exposure and lack of data.
Hepatic Impairment:
Mild:
No dosage adjustment necessary
Moderate:
No dosage adjustment necessary
Severe:
0.2 mg orally once daily; monitor for adverse reactions. Avoid use in patients with severe hepatic impairment (Child-Pugh Class C).
Pharmacology
Mechanism of Action
Naldemedine is a peripherally acting mu-opioid receptor antagonist (PAMORA). It selectively antagonizes opioid binding at mu-opioid receptors in the gastrointestinal tract, thereby reducing the constipating effects of opioids without reversing central opioid analgesia. Naldemedine is a substrate for P-glycoprotein (P-gp) and is minimally able to cross the blood-brain barrier.
Pharmacokinetics
Absorption:
Bioavailability:
Not precisely quantified, but well absorbed
Tmax:
0.75 - 1.5 hours
FoodEffect:
Food does not significantly affect the absorption of naldemedine, but may delay Tmax by approximately 2 hours.
Distribution:
Vd:
104 L (apparent volume of distribution)
ProteinBinding:
93-94%
CnssPenetration:
Limited
Elimination:
HalfLife:
11 hours (terminal half-life)
Clearance:
Not precisely quantified, but primarily hepatic and renal
ExcretionRoute:
Fecal (approximately 57%), Renal (approximately 35%)
Unchanged:
Approximately 1-2% (renal)
Pharmacodynamics
OnsetOfAction:
Within 24 hours for first spontaneous bowel movement (SBM)
PeakEffect:
Not directly applicable for bowel function, but sustained effect with daily dosing
DurationOfAction:
24 hours (consistent with once-daily dosing)
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Attention Immediately
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach or bowel problems, such as:
+ Severe stomach pain or swelling that worsens or persists
+ Vomiting blood or material that looks like coffee grounds
+ Persistent upset stomach or vomiting
+ Black, tarry, or bloody stools
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Diarrhea
Stomach pain
Upset stomach
Vomiting
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Although rare, this medication can cause severe and potentially life-threatening side effects. If you experience any of the following symptoms, contact your doctor or seek medical help right away:
Signs of an allergic reaction, such as:
+ Rash
+ Hives
+ Itching
+ Red, swollen, blistered, or peeling skin with or without fever
+ Wheezing
+ Tightness in the chest or throat
+ Trouble breathing, swallowing, or talking
+ Unusual hoarseness
+ Swelling of the mouth, face, lips, tongue, or throat
Stomach or bowel problems, such as:
+ Severe stomach pain or swelling that worsens or persists
+ Vomiting blood or material that looks like coffee grounds
+ Persistent upset stomach or vomiting
+ Black, tarry, or bloody stools
Other Possible Side Effects
Like all medications, this drug can cause side effects. While many people may not experience any side effects or only minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects or any other unusual symptoms that bother you or do not go away, contact your doctor or seek medical help:
Diarrhea
Stomach pain
Upset stomach
Vomiting
Reporting Side Effects
This list is not exhaustive, and you may experience other side effects. If you have questions or concerns about side effects, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
Seek Immediate Medical Attention If You Experience:
- Severe or worsening abdominal pain
- Diarrhea that is severe or persistent
- Symptoms of opioid withdrawal (e.g., sweating, chills, muscle aches, yawning, runny nose, watery eyes, anxiety, restlessness, tremor, abdominal cramps, muscle spasms). If these occur, contact your doctor immediately.
- Signs of allergic reaction (e.g., rash, itching, swelling, severe dizziness, trouble breathing)
Before Using This Medicine
Before Taking This Medication: Important Information to Share with Your Doctor
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a current or past bowel blockage.
If you have liver disease.
If you are taking any of the following medications: carbamazepine, phenytoin, rifampin, or St. John's wort.
If you are using another medication similar to this one. If you are unsure, consult your doctor or pharmacist for clarification.
If you are breastfeeding. Note that you should not breastfeed while taking this medication and for at least 3 days after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.
It is essential to inform your doctor about the following:
Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the symptoms you experienced.
If you have a current or past bowel blockage.
If you have liver disease.
If you are taking any of the following medications: carbamazepine, phenytoin, rifampin, or St. John's wort.
If you are using another medication similar to this one. If you are unsure, consult your doctor or pharmacist for clarification.
If you are breastfeeding. Note that you should not breastfeed while taking this medication and for at least 3 days after your last dose.
This list is not exhaustive, and it is crucial to discuss all your medications (including prescription, over-the-counter, natural products, and vitamins) and health issues with your doctor and pharmacist. They will help determine if it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dosage of any medication without first consulting your doctor.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Before using a laxative with this drug, consult with your doctor to discuss potential interactions.
This medication is specifically designed for patients who are currently taking opioid pain medications. If you stop taking your opioid pain medication, notify your doctor immediately. Additionally, the effectiveness of this drug may be reduced in individuals who have been taking opioid pain medications for less than 4 weeks.
Be aware that this medication can cause signs of opioid withdrawal, such as excessive sweating, chills, diarrhea, stomach pain, anxiety, irritability, or yawning. If you experience any of these symptoms, contact your doctor right away.
If you are pregnant or planning to become pregnant, consult with your doctor to discuss the benefits and risks of using this medication during pregnancy. Using this drug during pregnancy may cause withdrawal symptoms in the unborn baby, and your doctor will need to monitor the baby's health after the medication is administered.
This medication is specifically designed for patients who are currently taking opioid pain medications. If you stop taking your opioid pain medication, notify your doctor immediately. Additionally, the effectiveness of this drug may be reduced in individuals who have been taking opioid pain medications for less than 4 weeks.
Be aware that this medication can cause signs of opioid withdrawal, such as excessive sweating, chills, diarrhea, stomach pain, anxiety, irritability, or yawning. If you experience any of these symptoms, contact your doctor right away.
If you are pregnant or planning to become pregnant, consult with your doctor to discuss the benefits and risks of using this medication during pregnancy. Using this drug during pregnancy may cause withdrawal symptoms in the unborn baby, and your doctor will need to monitor the baby's health after the medication is administered.
Overdose Information
Overdose Symptoms:
- Exaggerated adverse effects such as severe abdominal pain
- Diarrhea
- Potentially opioid withdrawal symptoms if taken by someone not on chronic opioids
What to Do:
Seek immediate medical attention or call Poison Control at 1-800-222-1222. Treatment is supportive.
Drug Interactions
Major Interactions
- Strong CYP3A inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir): Concomitant use significantly increases naldemedine exposure, potentially increasing adverse reactions. Avoid coadministration.
- Strong CYP3A inducers (e.g., rifampin, carbamazepine, phenytoin, St. John's Wort): Concomitant use significantly decreases naldemedine exposure, potentially reducing efficacy. Avoid coadministration.
Moderate Interactions
- Moderate CYP3A inhibitors (e.g., erythromycin, diltiazem, verapamil, fluconazole): May increase naldemedine exposure. Monitor for adverse reactions.
- P-glycoprotein (P-gp) inhibitors (e.g., cyclosporine, quinidine, verapamil, amiodarone): May increase naldemedine exposure. Monitor for adverse reactions.
Confidence Interactions
Monitoring
Baseline Monitoring
Renal function (eGFR, creatinine)
Rationale: To assess need for dose adjustment in severe renal impairment and to avoid use in ESRD on dialysis.
Timing: Prior to initiation
Hepatic function (Child-Pugh score, LFTs)
Rationale: To assess need for dose adjustment in severe hepatic impairment and to avoid use in Child-Pugh Class C.
Timing: Prior to initiation
Current opioid regimen and duration
Rationale: To confirm appropriate indication (chronic non-cancer pain, opioid-induced constipation).
Timing: Prior to initiation
Routine Monitoring
Bowel movement frequency and consistency
Frequency: Daily or as needed
Target: Regular, spontaneous bowel movements
Action Threshold: Lack of improvement or worsening constipation after several days of therapy; signs of opioid withdrawal.
Signs/symptoms of opioid withdrawal (e.g., abdominal pain, nausea, vomiting, diarrhea, sweating, piloerection, chills, tremor, restlessness, anxiety, yawning, rhinorrhea, lacrimation)
Frequency: Regularly, especially during initial therapy
Target: Absence of withdrawal symptoms
Action Threshold: Presence of withdrawal symptoms; consider discontinuing naldemedine or reducing opioid dose if clinically appropriate.
Abdominal pain/discomfort
Frequency: Regularly
Target: Absence or reduction of pain
Action Threshold: Severe or worsening abdominal pain; consider discontinuing if severe or persistent.
Symptom Monitoring
- Abdominal pain
- Diarrhea
- Nausea
- Vomiting
- Flatulence
- Signs of opioid withdrawal (e.g., sweating, chills, piloerection, yawning, rhinorrhea, lacrimation, anxiety, restlessness, tremor, abdominal cramps, muscle spasms)
Special Patient Groups
Pregnancy
Category C. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus. Animal studies showed adverse effects at doses higher than clinical exposure.
Trimester-Specific Risks:
First Trimester:
Potential for fetal harm based on animal data; avoid if possible.
Second Trimester:
Potential for fetal harm based on animal data; avoid if possible.
Third Trimester:
Potential for fetal harm based on animal data; avoid if possible. Risk of opioid withdrawal in the neonate if the mother is opioid-dependent.
Lactation
L3 (Moderately Safe). Naldemedine is excreted into breast milk in animals. It is unknown if it is excreted in human milk. Given the potential for serious adverse reactions, including opioid withdrawal in a breastfed infant, advise women not to breastfeed during treatment with naldemedine and for 3 days after the last dose.
Infant Risk:
Potential for opioid withdrawal symptoms in breastfed infants if the mother is opioid-dependent; potential for other adverse effects.
Pediatric Use
Safety and effectiveness have not been established in pediatric patients. Not recommended for use in this population.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly patients and younger patients, but greater sensitivity of some older individuals cannot be ruled out. No dosage adjustment is required based on age alone.
Clinical Information
Clinical Pearls
- Naldemedine is specifically for opioid-induced constipation (OIC) in patients with chronic non-cancer pain. It is not indicated for other types of constipation.
- Patients should continue their opioid therapy as prescribed while taking naldemedine.
- Monitor for symptoms of opioid withdrawal, especially during the initial days of therapy, as this indicates central opioid receptor antagonism, which is not the intended effect.
- Avoid concomitant use with strong CYP3A inhibitors or inducers due to significant drug interactions.
- Patients with severe renal impairment (ESRD on dialysis) or severe hepatic impairment (Child-Pugh Class C) should avoid naldemedine due to increased exposure and lack of safety data.
- If severe or persistent abdominal pain occurs, discontinue naldemedine and investigate the cause.
Alternative Therapies
- Methylnaltrexone (Relistor)
- Naloxegol (Movantik)
- Lubiprostone (Amitiza)
- Linaclotide (Linzess)
- Prucalopride (Motegrity)
- Traditional laxatives (e.g., stool softeners, osmotic laxatives, stimulant laxatives)
Cost & Coverage
Average Cost:
$400 - $600 per 30 tablets
Insurance Coverage:
Tier 2 or 3 (Non-preferred brand)
General Drug Facts
If your symptoms or health issues persist or worsen, it is essential to contact your doctor promptly. To ensure safe and effective treatment, never share your medication with others or take someone else's medication.
This medication is accompanied by a Medication Guide, which provides crucial information for patients. It is vital to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount consumed, and the time it occurred.
This medication is accompanied by a Medication Guide, which provides crucial information for patients. It is vital to read this guide carefully and review it again whenever your prescription is refilled. If you have any questions or concerns about this medication, consult your doctor, pharmacist, or other healthcare provider for guidance.
In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When reporting the incident, be prepared to provide detailed information, including the name of the medication taken, the amount consumed, and the time it occurred.