Motegrity 1mg Tablets
It is used to treat constipation.
Drug Class
Prokinetic agent
Pharmacologic Class
Selective serotonin-4 (5-HT4) receptor agonist
Pregnancy Category
Not available
FDA Approved
Dec 2018
DEA Schedule
Not Controlled
Overview
What is this medicine?
Motegrity (prucalopride) is a medication used to treat chronic constipation, especially when other laxatives haven't worked. It works by helping your colon move stool through your intestines more effectively, making it easier to have a bowel movement.
How to Use This Medicine
Taking Your Medication
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom. Keep all medications in a safe location, out of the reach of children and pets.
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 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 make up for the missed one.
To use this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication as directed, with or without food. It's essential to continue taking this medication as prescribed by your doctor or healthcare provider, even if you're feeling well.
Storing and Disposing of Your Medication
Store your medication in its original container at room temperature, in a dry place. Avoid storing it in a bathroom. Keep all medications in a safe location, out of the reach of children and pets.
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 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 make up for the missed one.
Lifestyle & Tips
- Maintain adequate hydration by drinking plenty of fluids.
- Increase dietary fiber intake through fruits, vegetables, and whole grains, unless medically contraindicated.
- Engage in regular physical activity to promote bowel regularity.
- Do not take more than the prescribed dose, as this will not increase effectiveness but may increase side effects.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
2 mg orally once daily
Dose Range:
1 - 2 mg
Condition-Specific Dosing:
chronic_idiopathic_constipation:
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 dose adjustment needed (CrCl 50-79 mL/min)
Moderate:
1 mg orally once daily (CrCl 30-49 mL/min)
Severe:
1 mg orally once daily (CrCl <30 mL/min)
Dialysis:
Not recommended in patients with end-stage renal disease requiring dialysis due to lack of data.
Hepatic Impairment:
Mild:
No dose adjustment needed (Child-Pugh A)
Moderate:
No dose adjustment needed (Child-Pugh B)
Severe:
Not recommended (Child-Pugh C) due to lack of data and potential for increased exposure.
Pharmacology
Mechanism of Action
Prucalopride is a selective, high-affinity serotonin-4 (5-HT4) receptor agonist. By activating 5-HT4 receptors, it stimulates colonic motility, leading to increased bowel movements and improved stool consistency. It enhances propulsive gastrointestinal motility, particularly in the colon, without affecting gastric emptying or small bowel transit in healthy subjects.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 90%
Tmax:
2-3 hours
FoodEffect:
Food does not affect the extent of absorption.
Distribution:
Vd:
Approximately 480 L
ProteinBinding:
Approximately 30%
CnssPenetration:
Limited
Elimination:
HalfLife:
Approximately 24-28 hours
Clearance:
Approximately 31.7 L/hour (renal clearance is 24.1 L/hour)
ExcretionRoute:
Renal (approximately 60-65% unchanged), fecal (approximately 20% unchanged)
Unchanged:
Approximately 60-65% (urine), 20% (feces)
Pharmacodynamics
OnsetOfAction:
Within 24 hours for some patients, but full effect may take several days to weeks.
PeakEffect:
Not precisely defined for clinical effect, but steady-state plasma concentrations are reached within 3-4 days.
DurationOfAction:
Due to long half-life, effects persist for at least 24 hours, allowing once-daily dosing.
Safety & Warnings
Side Effects
Important Side Effects to Report to Your Doctor Immediately
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, seek medical attention 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
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
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:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Bloating
Gas
Feeling dizzy, tired, or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other 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. Your doctor can provide medical advice about side effects.
Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, seek medical attention 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
New or worsening behavioral or mood changes, including:
+ Depression
+ Thoughts of suicide
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:
Headache
Upset stomach or vomiting
Stomach pain or diarrhea
Bloating
Gas
Feeling dizzy, tired, or weak
Reporting Side Effects
This list is not exhaustive, and you may experience other 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. Your doctor can provide medical advice about side effects.
Seek Immediate Medical Attention If You Experience:
- Severe or persistent abdominal pain
- Persistent or severe diarrhea
- New or worsening depression, anxiety, or unusual mood changes
- Thoughts of harming yourself or others
- Allergic reactions such as rash, itching, swelling, severe dizziness, or 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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bowel problems, such as bowel blockage, Crohn's disease, a hole in the gastrointestinal (GI) tract, or ulcerative colitis.
+ Kidney disease.
+ Difficulty digesting certain sugars, including lactose, glucose, or galactose, as your body may have trouble processing them.
This list is not exhaustive, and it is crucial to discuss all your medications, health problems, and concerns with your doctor.
To ensure your safety, please inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking.
Any natural products or vitamins you are using.
* All your health problems, including those not listed here.
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so, given your unique health situation and medication regimen.
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 allergic reaction you experienced, including any symptoms that occurred.
Certain health conditions, including:
+ Bowel problems, such as bowel blockage, Crohn's disease, a hole in the gastrointestinal (GI) tract, or ulcerative colitis.
+ Kidney disease.
+ Difficulty digesting certain sugars, including lactose, glucose, or galactose, as your body may have trouble processing them.
This list is not exhaustive, and it is crucial to discuss all your medications, health problems, and concerns with your doctor.
To ensure your safety, please inform your doctor and pharmacist about:
All prescription and over-the-counter (OTC) medications you are taking.
Any natural products or vitamins you are using.
* All your health problems, including those not listed here.
Before starting, stopping, or changing the dose of any medication, including this one, consult with your doctor to confirm it is safe for you to do so, given your unique health situation and medication regimen.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. If you are pregnant, planning to become pregnant, or are breast-feeding, be sure to discuss this with your doctor. You and your doctor will need to carefully weigh the benefits and risks of using this medication to ensure the best possible outcome for both you and your baby.
Overdose Information
Overdose Symptoms:
- Headache
- Nausea
- Diarrhea
- Abdominal pain
What to Do:
In case of overdose, contact a poison control center immediately. Call 1-800-222-1222. Treatment should be symptomatic and supportive. There is no specific antidote for prucalopride.
Drug Interactions
Moderate Interactions
- Drugs that prolong QT interval (e.g., Class IA and III antiarrhythmics, antipsychotics, macrolide antibiotics, fluoroquinolones, tricyclic antidepressants): Theoretical risk of additive QT prolongation, though prucalopride itself has not shown significant QT prolongation at therapeutic doses.
- P-glycoprotein (P-gp) inhibitors (e.g., cyclosporine, quinidine, verapamil, amiodarone, ritonavir): May increase prucalopride exposure. Consider dose reduction of prucalopride to 1 mg daily if co-administered with potent P-gp inhibitors.
Monitoring
Baseline Monitoring
Renal function (CrCl)
Rationale: To determine appropriate starting dose and identify need for dose adjustment.
Timing: Prior to initiation of therapy.
Hepatic function (Child-Pugh score)
Rationale: To determine appropriate starting dose and identify need for dose adjustment, especially in severe impairment.
Timing: Prior to initiation of therapy if hepatic impairment is suspected or known.
Routine Monitoring
Bowel movement frequency and consistency
Frequency: Daily or as needed
Target: Improved bowel habits (e.g., 3 or more complete spontaneous bowel movements per week)
Action Threshold: Lack of improvement after 4 weeks may warrant re-evaluation of therapy.
Adverse effects (e.g., headache, nausea, abdominal pain, diarrhea)
Frequency: Regularly, especially during initial treatment
Target: Tolerable or absent
Action Threshold: Persistent or severe adverse effects may require dose reduction or discontinuation.
Mood changes, suicidal ideation
Frequency: Periodically, especially in patients with history of psychiatric disorders
Target: Stable mood, absence of suicidal thoughts
Action Threshold: New or worsening depression, anxiety, or suicidal thoughts require immediate medical attention and discontinuation.
Symptom Monitoring
- Constipation relief (frequency, consistency, straining)
- Abdominal pain or discomfort
- Nausea
- Diarrhea
- Headache
- Dizziness
- Fatigue
- Mood changes (depression, anxiety, suicidal thoughts)
Special Patient Groups
Pregnancy
Use during pregnancy is not recommended unless the potential benefit justifies the potential risk to the fetus. There are no adequate and well-controlled studies in pregnant women. Animal studies have shown some evidence of developmental toxicity at high doses.
Trimester-Specific Risks:
First Trimester:
Limited human data; animal studies suggest potential for developmental toxicity at high doses.
Second Trimester:
Limited human data.
Third Trimester:
Limited human data.
Lactation
Prucalopride is excreted into human milk. A decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of the drug to the mother and the potential adverse effects on the breastfed infant. Monitor infants for diarrhea.
Infant Risk:
L3 (Moderate risk - limited human data, potential for non-serious adverse effects like diarrhea in infant).
Pediatric Use
Safety and effectiveness in pediatric patients (under 18 years of age) have not been established. Use is not recommended.
Geriatric Use
No overall differences in safety or effectiveness were observed between elderly and younger patients, but greater sensitivity of some older individuals cannot be ruled out. No dose adjustment is generally needed based on age alone, but renal function should be assessed.
Clinical Information
Clinical Pearls
- Prucalopride is a highly selective 5-HT4 agonist, which differentiates it from older prokinetics like cisapride that had broader receptor activity and associated cardiac risks.
- It is indicated for chronic idiopathic constipation (CIC) in adults when other laxatives have failed.
- Patients should be advised that while some may experience relief within 24 hours, the full therapeutic effect may take several days to weeks.
- Dose adjustment is crucial for patients with moderate to severe renal impairment (1 mg daily).
- Patients should be monitored for new or worsening psychiatric symptoms, including depression and suicidal ideation, especially those with a history of such conditions.
Alternative Therapies
- Osmotic laxatives (e.g., polyethylene glycol, lactulose, magnesium hydroxide)
- Stimulant laxatives (e.g., bisacodyl, senna)
- Chloride channel activators (e.g., lubiprostone)
- Guanylate cyclase-C agonists (e.g., linaclotide, plecanatide)
- Peripherally acting mu-opioid receptor antagonists (PAMORAs) for opioid-induced constipation (e.g., methylnaltrexone, naloxegol, naldemedine)
- Fiber supplements (e.g., psyllium, methylcellulose)
Cost & Coverage
Average Cost:
Varies, typically $400-$600 per 30 tablets
Insurance Coverage:
Tier 2 or Tier 3 (preferred or non-preferred brand), may require prior authorization.
General Drug Facts
If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek emergency medical attention. When seeking help, be prepared to provide details about the overdose, including the medication taken, the amount, and the time it occurred.