Movantik 12.5mg Tablets
It is used to treat constipation caused by some pain drugs.
Drug Class
Peripherally-acting mu-opioid receptor antagonist (PAMORA)
Pharmacologic Class
Opioid antagonist
Pregnancy Category
Category C
FDA Approved
Sep 2014
DEA Schedule
Not Controlled
Overview
What is this medicine?
Movantik is a medication used to treat constipation caused by opioid pain medicines. It works by blocking the effects of opioids in your gut, helping you have more regular bowel movements without affecting the pain relief from your opioid medication.
How to Use This Medicine
Taking Your Medication Correctly
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication on an empty stomach, either at least 1 hour before or 2 hours after your first meal of the day.
If you have difficulty swallowing the medication whole, you can crush it and mix it with 4 ounces (120 mL) of water. Be sure to:
Drink the mixture immediately after preparing it.
Refill the glass with 120 mL of water, stir, and drink to ensure you get the full dose.
If you have a feeding tube, you can use this medication as directed by your healthcare provider. Remember to:
Flush the feeding tube after administering the medication.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store it at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist.
Check with your pharmacist for guidance on the best way to dispose of your medication. You may also have access to drug take-back programs in your area.
What to Do If You Miss 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 dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses.
To ensure you get the most benefit from your medication, follow these steps:
Take your medication exactly as directed by your doctor.
Read all the information provided with your medication and follow the instructions carefully.
Take your medication on an empty stomach, either at least 1 hour before or 2 hours after your first meal of the day.
If you have difficulty swallowing the medication whole, you can crush it and mix it with 4 ounces (120 mL) of water. Be sure to:
Drink the mixture immediately after preparing it.
Refill the glass with 120 mL of water, stir, and drink to ensure you get the full dose.
If you have a feeding tube, you can use this medication as directed by your healthcare provider. Remember to:
Flush the feeding tube after administering the medication.
Storing and Disposing of Your Medication
To keep your medication safe and effective:
Store it at room temperature in a dry place, away from the bathroom.
Keep all medications in a secure location, out of reach of children and pets.
Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so by your pharmacist.
Check with your pharmacist for guidance on the best way to dispose of your medication. You may also have access to drug take-back programs in your area.
What to Do If You Miss 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 dose, skip the missed dose and resume your regular schedule.
Do not take two doses at the same time or take extra doses.
Lifestyle & Tips
- Take Movantik on an empty stomach, at least 1 hour before your first meal of the day or 2 hours after a meal.
- Do not eat grapefruit or drink grapefruit juice while taking Movantik, as it can increase the amount of the drug in your body.
- Continue to take your opioid pain medication as prescribed.
- Maintain adequate hydration and fiber intake as recommended by your doctor.
- Report any severe or persistent abdominal pain, nausea, vomiting, or diarrhea to your doctor immediately.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
25 mg orally once daily. For patients unable to tolerate 25 mg, consider reducing to 12.5 mg once daily.
Dose Range:
12.5 - 25 mg
Condition-Specific Dosing:
concomitant moderate CYP3A4 inhibitors:
12.5 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 (CrCl 60-89 mL/min)
Moderate:
No dosage adjustment necessary (CrCl 30-59 mL/min)
Severe:
12.5 mg orally once daily (CrCl <30 mL/min)
Dialysis:
No dosage adjustment necessary for patients on hemodialysis or peritoneal dialysis; administer Movantik prior to dialysis.
Hepatic Impairment:
Mild:
No dosage adjustment necessary (Child-Pugh A)
Moderate:
No dosage adjustment necessary (Child-Pugh B)
Severe:
12.5 mg orally once daily (Child-Pugh C)
Pharmacology
Mechanism of Action
Naloxegol is a peripherally-acting mu-opioid receptor antagonist. It is a pegylated derivative of naloxone. Due to its pegylation, naloxegol has reduced passive permeability and is a substrate for P-glycoprotein (P-gp), limiting its ability to cross the blood-brain barrier. This allows it to antagonize opioid receptors in the gastrointestinal tract, reversing opioid-induced constipation, without reversing central opioid analgesia.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 6% (absolute bioavailability)
Tmax:
Approximately 2 hours
FoodEffect:
High-fat meal decreases Cmax by 35% and AUC by 12%. Administer on an empty stomach at least 1 hour before the first meal of the day or 2 hours after the meal.
Distribution:
Vd:
2000 L (apparent volume of distribution)
ProteinBinding:
Approximately 4% (low)
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 6-11 hours
Clearance:
Not available
ExcretionRoute:
Renal (approximately 16% as unchanged drug), Fecal (approximately 55% as unchanged drug)
Unchanged:
Approximately 16% (urine), 55% (feces)
Pharmacodynamics
OnsetOfAction:
Variable, typically within 24-48 hours for first spontaneous bowel movement
PeakEffect:
Not precisely defined for bowel function, but plasma concentrations peak around 2 hours.
DurationOfAction:
24 hours (allows once-daily dosing)
Safety & Warnings
Side Effects
Important Side Effects to Report to Your Doctor Right Away
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, seek medical attention immediately:
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
Severe stomach pain and diarrhea, which can occur within a few days of starting this medication and may require hospitalization
Tears in the stomach or bowel wall, which can be life-threatening, especially if you:
+ Take bevacizumab
+ Have a history of stomach or bowel problems, such as cancer, recent surgery, diverticulitis, or colitis
Symptoms of stomach or bowel problems, such as:
+ Severe swelling or pain in the stomach that worsens or persists
+ Vomiting blood or coffee ground-like material
+ Persistent upset stomach or vomiting
+ Black, tarry, or bloody stools
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, or if they bother you or persist, contact your doctor:
Stomach pain or diarrhea
Gas
Headache
Upset stomach or vomiting
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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, some people may experience severe and potentially life-threatening side effects while taking this medication. If you experience any of the following symptoms, seek medical attention immediately:
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
Severe stomach pain and diarrhea, which can occur within a few days of starting this medication and may require hospitalization
Tears in the stomach or bowel wall, which can be life-threatening, especially if you:
+ Take bevacizumab
+ Have a history of stomach or bowel problems, such as cancer, recent surgery, diverticulitis, or colitis
Symptoms of stomach or bowel problems, such as:
+ Severe swelling or pain in the stomach that worsens or persists
+ Vomiting blood or coffee ground-like material
+ Persistent upset stomach or vomiting
+ Black, tarry, or bloody stools
Other Possible Side Effects
Most people experience no side effects or only mild side effects while taking this medication. However, if you experience any of the following side effects, or if they bother you or persist, contact your doctor:
Stomach pain or diarrhea
Gas
Headache
Upset stomach or vomiting
This is not an exhaustive list of possible side effects. If you have questions or concerns about side effects, consult 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 stomach pain
- Diarrhea that is severe or does not stop
- Nausea or vomiting
- Symptoms of opioid withdrawal (e.g., sweating, chills, anxiety, irritability, runny nose, yawning, body aches)
- Allergic reaction symptoms (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 conditions and situations to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you have liver disease, as this may affect how your body processes the medication.
If you have a history of bowel blockage, as this may increase the risk of complications.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. Certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this medication and should be avoided.
If you are taking St. John's Wort, as it may reduce the effectiveness of this medication. Do not take St. John's Wort while using this drug.
If you are using another medication similar to this one, as this may increase the risk of adverse effects. If you are unsure, consult your doctor or pharmacist.
* If you are breastfeeding, as this medication may pass into breast milk and harm your baby. Do not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health problems, and concerns with your doctor and pharmacist to ensure safe treatment. Always check with your doctor before starting, stopping, or changing the dose of any medication to avoid potential interactions and complications.
It is essential to inform your doctor about the following conditions and situations to ensure safe treatment:
Any allergies you have, including allergies to this medication, its components, or other substances. Be sure to describe the allergic reaction and its symptoms.
If you have liver disease, as this may affect how your body processes the medication.
If you have a history of bowel blockage, as this may increase the risk of complications.
Any medications you are currently taking, including prescription and over-the-counter (OTC) drugs, natural products, and vitamins. Certain medications, such as those used to treat HIV, infections, seizures, and other conditions, may interact with this medication and should be avoided.
If you are taking St. John's Wort, as it may reduce the effectiveness of this medication. Do not take St. John's Wort while using this drug.
If you are using another medication similar to this one, as this may increase the risk of adverse effects. If you are unsure, consult your doctor or pharmacist.
* If you are breastfeeding, as this medication may pass into breast milk and harm your baby. Do not breastfeed while taking this medication.
This list is not exhaustive, and it is crucial to discuss all your medications, health problems, and concerns with your doctor and pharmacist to ensure safe treatment. Always check with your doctor before starting, stopping, or changing the dose of any medication to avoid potential interactions and complications.
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, consult with your doctor to discuss potential interactions.
To minimize potential interactions, avoid consuming grapefruit and grapefruit juice while taking this drug. 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 promptly, as this may lead to signs of opioid withdrawal.
Be aware of the symptoms of opioid withdrawal, which may include excessive sweating, chills, diarrhea, stomach pain, anxiety, irritability, or yawning. If you experience any of these symptoms, contact your doctor immediately. Additionally, if you are taking methadone for pain management, discuss this with your doctor, as the combination of methadone and this drug may increase the risk of stomach problems, such as diarrhea and stomach pain, compared to other pain medications.
The effectiveness of this drug may be reduced in individuals who have been taking pain medications for less than 4 weeks. If you are pregnant or planning to become pregnant, consult with your doctor to weigh the benefits and risks of using this medication during pregnancy. If this drug is used during pregnancy, it may cause withdrawal symptoms in the unborn baby, and your doctor will need to monitor the baby's health after the medication is administered.
To minimize potential interactions, avoid consuming grapefruit and grapefruit juice while taking this drug. 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 promptly, as this may lead to signs of opioid withdrawal.
Be aware of the symptoms of opioid withdrawal, which may include excessive sweating, chills, diarrhea, stomach pain, anxiety, irritability, or yawning. If you experience any of these symptoms, contact your doctor immediately. Additionally, if you are taking methadone for pain management, discuss this with your doctor, as the combination of methadone and this drug may increase the risk of stomach problems, such as diarrhea and stomach pain, compared to other pain medications.
The effectiveness of this drug may be reduced in individuals who have been taking pain medications for less than 4 weeks. If you are pregnant or planning to become pregnant, consult with your doctor to weigh the benefits and risks of using this medication during pregnancy. If this drug is used during pregnancy, it 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:
- Severe abdominal pain
- Diarrhea
- Symptoms of opioid withdrawal (if central effects occur)
What to Do:
Seek immediate medical attention or call Poison Control at 1-800-222-1222. Treatment is supportive.
Drug Interactions
Contraindicated Interactions
- Strong CYP3A4 inhibitors (e.g., ketoconazole, itraconazole, clarithromycin, ritonavir, indinavir, saquinavir, telithromycin, nefazodone)
- Patients with known or suspected gastrointestinal obstruction or at increased risk of recurrent obstruction (e.g., advanced ovarian cancer, other abdominal malignancies)
Major Interactions
- Moderate CYP3A4 inhibitors (e.g., diltiazem, erythromycin, fluconazole, verapamil, grapefruit juice) - requires dose reduction of naloxegol
- P-glycoprotein (P-gp) inhibitors (e.g., cyclosporine, quinidine, verapamil, amiodarone, diltiazem, itraconazole, ketoconazole, ritonavir, clarithromycin, erythromycin, ticagrelor) - may increase naloxegol exposure
Moderate Interactions
- Opioid analgesics (potential for opioid withdrawal symptoms if naloxegol crosses blood-brain barrier, though limited)
- Other laxatives (may increase risk of diarrhea)
Confidence Interactions
Monitoring
Baseline Monitoring
Assessment of GI obstruction risk
Rationale: To rule out mechanical obstruction, which is a contraindication.
Timing: Prior to initiation
Current opioid regimen and duration
Rationale: To confirm opioid-induced constipation and assess chronic pain management.
Timing: Prior to initiation
Renal and hepatic function (CrCl, LFTs)
Rationale: To determine appropriate starting dose and monitor for dose adjustments.
Timing: Prior to initiation
Routine Monitoring
Bowel movement frequency and consistency
Frequency: Daily or as needed
Target: Regular, soft, spontaneous bowel movements
Action Threshold: Lack of response after 1-2 weeks, worsening constipation, or development of new GI symptoms
Symptoms of opioid withdrawal (e.g., abdominal pain, nausea, vomiting, diarrhea, sweating, chills, anxiety, irritability)
Frequency: Regularly, especially during initial treatment
Target: Absence of withdrawal symptoms
Action Threshold: Presence of withdrawal symptoms, indicating potential central opioid antagonism
Abdominal pain or discomfort
Frequency: Regularly
Target: Absence or reduction of pain
Action Threshold: Worsening or new severe abdominal pain, which could indicate GI perforation or other serious events
Symptom Monitoring
- Abdominal pain
- Diarrhea
- Nausea
- Vomiting
- Flatulence
- Headache
- Hyperhidrosis (sweating)
- Chills
- Anxiety
- Irritability
- Symptoms of opioid withdrawal
Special Patient Groups
Pregnancy
Use only if the potential benefit justifies the potential risk to the fetus. Animal studies showed adverse effects at high doses. Limited human data.
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 naloxegol crosses the placenta.
Lactation
Naloxegol is present in human milk. Monitor breastfed infants for signs of opioid withdrawal (e.g., irritability, poor feeding, vomiting, diarrhea) and for decreased analgesia in the mother. Consider the developmental and health benefits of breastfeeding along with the mother’s clinical need for Movantik and any potential adverse effects on the breastfed infant from Movantik or from the underlying maternal condition.
Infant Risk:
Moderate risk (L3). Potential for opioid withdrawal symptoms in the infant or interference with infant's opioid analgesia if the infant is receiving opioids.
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 and younger patients. No dosage adjustment is required based on age alone. However, greater sensitivity of some older individuals cannot be ruled out, and elderly patients are more likely to have decreased renal function, which may require dose adjustment.
Clinical Information
Clinical Pearls
- Movantik is specifically for opioid-induced constipation (OIC) in adults with chronic non-cancer pain. It is not indicated for other types of constipation.
- Ensure patients are not taking strong CYP3A4 inhibitors, as this is a contraindication due to significantly increased naloxegol exposure.
- Advise patients to take Movantik on an empty stomach to optimize absorption.
- Monitor for symptoms of opioid withdrawal, especially in patients with compromised blood-brain barrier integrity (e.g., severe head trauma, brain tumors, active CNS lesions, or conditions that may disrupt the BBB).
- Educate patients about the risk of GI perforation, particularly in those with underlying GI conditions (e.g., diverticulitis, inflammatory bowel disease, GI malignancies).
- If a patient experiences severe or persistent abdominal pain, discontinue Movantik and investigate for GI perforation.
Alternative Therapies
- Methylnaltrexone (Relistor)
- Naldemedine (Symproic)
- Lubiprostone (Amitiza)
- Linaclotide (Linzess)
- Prucalopride (Motegrity)
- Traditional laxatives (e.g., stool softeners, osmotic laxatives, stimulant laxatives)
Cost & Coverage
Average Cost:
Varies, typically $300-$500 per 30 tablets
Generic Available:
Yes
Insurance Coverage:
Tier 2 or 3 (Specialty/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, a patient fact sheet that provides crucial information. 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, a patient fact sheet that provides crucial information. 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.