Pentasa 250mg Capsules
It is used to treat ulcerative colitis. It is used to help keep ulcerative colitis flares from coming back.It may be given to you for other reasons. Talk with the doctor.
Drug Class
Anti-inflammatory agent, aminosalicylate
Pharmacologic Class
5-aminosalicylic acid (5-ASA) derivative
Pregnancy Category
Category B
FDA Approved
Oct 1987
DEA Schedule
Not Controlled
Overview
What is this medicine?
Pentasa is a medication used to treat Crohn's disease, a type of inflammatory bowel disease. It works by reducing inflammation in your intestines. It comes in capsules that release the medicine slowly as they travel through your digestive system.
How to Use This Medicine
Taking Your Medication
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and be sure to swallow it whole with a full glass of water. Do not chew or crush the medication. If you have difficulty swallowing it whole, you can sprinkle the contents on applesauce or yogurt, but swallow the mixture immediately without chewing.
It's essential to continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well. This will help ensure you receive the full benefits of the medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Some products may come with a desiccant (a moisture-protecting packet) in the container. If your container has a desiccant, keep it in the bottle. However, some brands may allow storage without the desiccant for a short period. If you're unsure, consult your doctor or pharmacist.
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 dose, skip the missed dose and resume your regular schedule. Do not take two doses at the same time or take extra doses.
To take this medication correctly, follow your doctor's instructions and read all the information provided. Take your medication with or without food, and be sure to swallow it whole with a full glass of water. Do not chew or crush the medication. If you have difficulty swallowing it whole, you can sprinkle the contents on applesauce or yogurt, but swallow the mixture immediately without chewing.
It's essential to continue taking your medication as directed by your doctor or healthcare provider, even if you're feeling well. This will help ensure you receive the full benefits of the medication.
Storing and Disposing of Your Medication
Store your medication at room temperature in a dry place, avoiding the bathroom. Some products may come with a desiccant (a moisture-protecting packet) in the container. If your container has a desiccant, keep it in the bottle. However, some brands may allow storage without the desiccant for a short period. If you're unsure, consult your doctor or pharmacist.
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 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 Pentasa exactly as prescribed by your doctor. Do not chew, crush, or break the capsules.
- Swallow the capsules whole with a glass of water.
- You can take Pentasa with or without food.
- Continue taking this medication even if you feel better, as stopping it too soon can lead to a return of symptoms.
- Stay well-hydrated, especially if you experience diarrhea.
- Report any new or worsening symptoms to your doctor.
Available Forms & Alternatives
Available Strengths:
Dosing & Administration
Adult Dosing
Standard Dose:
1000 mg (four 250 mg capsules) four times daily
Dose Range:
4000 - 4000 mg
Condition-Specific Dosing:
Crohn's Disease (active, mild to moderate):
1000 mg (four 250 mg capsules) four times daily for a total daily dose of 4 g.
Pediatric Dosing
Neonatal:
Not established
Infant:
Not established
Child:
Not established for Pentasa capsules; other mesalamine formulations may have established pediatric dosing for ulcerative colitis.
Adolescent:
Not established for Pentasa capsules; other mesalamine formulations may have established pediatric dosing for ulcerative colitis.
Dose Adjustments
Renal Impairment:
Mild:
Use with caution; monitor renal function.
Moderate:
Use with caution; monitor renal function. Consider dose reduction or discontinuation if renal function worsens.
Severe:
Contraindicated in patients with severe renal impairment or renal failure.
Dialysis:
Contraindicated in patients with renal failure. Mesalamine and its metabolite are dialyzable, but use is not recommended.
Hepatic Impairment:
Mild:
Use with caution; monitor liver function.
Moderate:
Use with caution; monitor liver function. Consider dose reduction.
Severe:
Use with caution; monitor liver function. Not extensively studied, but caution is advised due to potential for hepatotoxicity.
Pharmacology
Mechanism of Action
Mesalamine (5-aminosalicylic acid, 5-ASA) is thought to exert its anti-inflammatory effect locally in the intestinal mucosa, particularly in the colon. Its exact mechanism is not fully understood but is believed to involve inhibition of prostaglandin and leukotriene synthesis (via inhibition of cyclooxygenase and lipoxygenase pathways), scavenging of free radicals, and inhibition of cytokine production (e.g., IL-1, TNF-alpha). Pentasa capsules are designed to release mesalamine throughout the gastrointestinal tract from the duodenum to the rectum.
Pharmacokinetics
Absorption:
Bioavailability:
Approximately 20-30% (systemic absorption, highly variable)
Tmax:
2-12 hours (for parent drug, highly variable due to extended release)
FoodEffect:
Food may delay Tmax but does not significantly affect the extent of absorption.
Distribution:
Vd:
Not available (systemic distribution is limited due to local action)
ProteinBinding:
Approximately 43% for mesalamine, 78% for N-acetyl-5-ASA
CnssPenetration:
Limited
Elimination:
HalfLife:
0.5-1.5 hours (mesalamine); 5-10 hours (N-Ac-5-ASA)
Clearance:
Not available (highly variable due to local action and first-pass metabolism)
ExcretionRoute:
Renal (primarily as N-Ac-5-ASA), fecal (unabsorbed drug)
Unchanged:
Less than 10% (systemically absorbed mesalamine)
Pharmacodynamics
OnsetOfAction:
Days to weeks (clinical effect)
PeakEffect:
Weeks (clinical effect)
DurationOfAction:
Dependent on continued dosing
Safety & Warnings
Side Effects
Urgent Side Effects: Seek Medical Help Right Away
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, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to urinate or changes in urine output
+ Blood in the urine or significant weight gain
+ Back pain, abdominal pain, or blood in the urine (which may indicate a kidney stone)
Chest pain or pressure, rapid or irregular heartbeat
Fever, chills, sore throat, unexplained bruising or bleeding, or feeling extremely tired or weak
Symptoms that may resemble ulcerative colitis, such as:
+ New or worsening stomach pain or cramps
+ Bloody stools
+ Fever
+ Headache
+ Itching
+ Rash
+ Red or pink eyes
+ General feeling of illness
Signs of liver problems, which can be rare but potentially life-threatening:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellowing of the skin or eyes
Heart problems, which can be rare but potentially life-threatening:
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions that can affect body organs and be life-threatening
+ Symptoms may include:
- Red, swollen, blistered, or peeling skin
- Red or irritated eyes
- Sores in the mouth, throat, nose, eyes, genitals, or skin
- Fever
- Chills
- Body aches
- Shortness of breath
- Swollen glands
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, contact your doctor if they bother you or do not go away:
Constipation
Diarrhea
Stomach pain
Nausea or vomiting
Heartburn
Gas
Burping
Nose or throat irritation
Dizziness or headache
Back pain
* Cough
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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 notice any of the following symptoms, contact your doctor immediately or seek emergency medical attention:
Signs of an allergic reaction, such as:
+ Rash or hives
+ Itching or red, swollen, blistered, or peeling skin (with or without fever)
+ Wheezing or tightness in the chest or throat
+ Difficulty breathing, swallowing, or talking
+ Unusual hoarseness or swelling of the mouth, face, lips, tongue, or throat
Signs of kidney problems, including:
+ Inability to urinate or changes in urine output
+ Blood in the urine or significant weight gain
+ Back pain, abdominal pain, or blood in the urine (which may indicate a kidney stone)
Chest pain or pressure, rapid or irregular heartbeat
Fever, chills, sore throat, unexplained bruising or bleeding, or feeling extremely tired or weak
Symptoms that may resemble ulcerative colitis, such as:
+ New or worsening stomach pain or cramps
+ Bloody stools
+ Fever
+ Headache
+ Itching
+ Rash
+ Red or pink eyes
+ General feeling of illness
Signs of liver problems, which can be rare but potentially life-threatening:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellowing of the skin or eyes
Heart problems, which can be rare but potentially life-threatening:
+ Shortness of breath
+ Significant weight gain
+ Swelling in the arms or legs
Severe skin reactions, including:
+ Stevens-Johnson syndrome (SJS)
+ Toxic epidermal necrolysis (TEN)
+ Other serious reactions that can affect body organs and be life-threatening
+ Symptoms may include:
- Red, swollen, blistered, or peeling skin
- Red or irritated eyes
- Sores in the mouth, throat, nose, eyes, genitals, or skin
- Fever
- Chills
- Body aches
- Shortness of breath
- Swollen glands
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, contact your doctor if they bother you or do not go away:
Constipation
Diarrhea
Stomach pain
Nausea or vomiting
Heartburn
Gas
Burping
Nose or throat irritation
Dizziness or headache
Back pain
* Cough
This is not an exhaustive list of possible side effects. If you have questions or concerns, 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 stomach pain, cramping, or bloody diarrhea (may indicate acute intolerance syndrome)
- New or worsening kidney problems (e.g., decreased urination, swelling in legs/feet, unusual tiredness)
- Liver problems (e.g., yellowing of skin or eyes, dark urine, nausea, vomiting, severe stomach pain)
- Signs of blood problems (e.g., unexplained bleeding or bruising, unusual tiredness, fever, sore throat, pale skin)
- Chest pain, shortness of breath, or palpitations (rare, but serious heart inflammation)
- Severe skin rash or blistering
- Allergic reaction (e.g., rash, itching, swelling of face/tongue/throat, 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.
Existing health conditions, including:
+ Kidney disease or liver disease
+ Stomach or bowel ulcers
+ Narrowing of the stomach valve or other types of stomach blockages
+ Blockages in the urinary tract (consult with your healthcare provider if you have this condition)
Additionally, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
This information is crucial to ensure your safety while taking this medication. Do not start, stop, or change the dose of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this drug and your individual health situation.
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.
Existing health conditions, including:
+ Kidney disease or liver disease
+ Stomach or bowel ulcers
+ Narrowing of the stomach valve or other types of stomach blockages
+ Blockages in the urinary tract (consult with your healthcare provider if you have this condition)
Additionally, provide your doctor and pharmacist with a comprehensive list of:
All prescription and over-the-counter (OTC) medications you are taking
Natural products and vitamins you are using
* Any health problems you have
This information is crucial to ensure your safety while taking this medication. Do not start, stop, or change the dose of any medication without first consulting your doctor to confirm that it is safe to do so in conjunction with this drug and your individual health situation.
Precautions & Cautions
It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication. Regular blood tests will be necessary, as directed by your doctor, to monitor your condition. Be sure to discuss any concerns or questions you have with your doctor.
As this medication may interfere with certain laboratory tests, it is crucial to notify all your healthcare providers and laboratory personnel that you are taking this drug.
To stay hydrated, drink plenty of non-caffeinated fluids, unless your doctor advises you to limit your liquid intake.
While taking this medication, you may notice that your urine turns reddish-brown when it comes into contact with surfaces or water that have been treated with bleach, such as in a toilet. However, if you observe that your urine is reddish-brown before it comes into contact with any surfaces or water that may have been treated with bleach, please contact your doctor.
You may be more susceptible to sunburn while taking this medication. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear to safeguard your skin and eyes from the sun.
If you are 65 years or older, exercise caution when taking this medication, as you may be more prone to experiencing side effects.
Not all formulations of this medication are suitable for children. Before administering this drug to a child, consult with your doctor to determine the appropriate dosage and potential risks.
Do not give this medication to children and teenagers who have or are recovering from flu symptoms, chickenpox, or other viral infections, as this may increase the risk of developing Reye's syndrome, a potentially life-threatening condition that affects the brain and liver.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor, as they will need to discuss the potential benefits and risks of this medication to you and your baby.
As this medication may interfere with certain laboratory tests, it is crucial to notify all your healthcare providers and laboratory personnel that you are taking this drug.
To stay hydrated, drink plenty of non-caffeinated fluids, unless your doctor advises you to limit your liquid intake.
While taking this medication, you may notice that your urine turns reddish-brown when it comes into contact with surfaces or water that have been treated with bleach, such as in a toilet. However, if you observe that your urine is reddish-brown before it comes into contact with any surfaces or water that may have been treated with bleach, please contact your doctor.
You may be more susceptible to sunburn while taking this medication. To minimize this risk, avoid exposure to direct sunlight, sunlamps, and tanning beds. Use sunscreen and wear protective clothing and eyewear to safeguard your skin and eyes from the sun.
If you are 65 years or older, exercise caution when taking this medication, as you may be more prone to experiencing side effects.
Not all formulations of this medication are suitable for children. Before administering this drug to a child, consult with your doctor to determine the appropriate dosage and potential risks.
Do not give this medication to children and teenagers who have or are recovering from flu symptoms, chickenpox, or other viral infections, as this may increase the risk of developing Reye's syndrome, a potentially life-threatening condition that affects the brain and liver.
If you are pregnant, planning to become pregnant, or breastfeeding, inform your doctor, as they will need to discuss the potential benefits and risks of this medication to you and your baby.
Overdose Information
Overdose Symptoms:
- Nausea
- Vomiting
- Abdominal pain
- Diarrhea
- Headache
- Drowsiness
- Confusion
- Hyperventilation (rare)
What to Do:
Seek immediate medical attention or call a Poison Control Center at 1-800-222-1222. Treatment is generally supportive and symptomatic.
Drug Interactions
Major Interactions
- Nephrotoxic agents (e.g., NSAIDs, azathioprine, mercaptopurine, tacrolimus): Increased risk of renal adverse reactions.
- Azathioprine, Mercaptopurine, Thioguanine: Increased risk of myelosuppression due to inhibition of thiopurine methyltransferase (TPMT) by mesalamine.
Moderate Interactions
- Lactulose: May interfere with mesalamine release from Pentasa capsules due to pH changes.
- Furosemide: Potential for increased risk of nephrotoxicity (monitor renal function).
Monitoring
Baseline Monitoring
Renal function (serum creatinine, BUN)
Rationale: To establish baseline and identify pre-existing renal impairment, as mesalamine can cause renal toxicity.
Timing: Prior to initiation of therapy.
Liver function tests (ALT, AST, bilirubin)
Rationale: To establish baseline and identify pre-existing hepatic impairment, as mesalamine can cause hepatotoxicity.
Timing: Prior to initiation of therapy.
Complete Blood Count (CBC) with differential
Rationale: To establish baseline and monitor for blood dyscrasias (e.g., agranulocytosis, aplastic anemia, neutropenia) which are rare but serious adverse effects.
Timing: Prior to initiation of therapy.
Routine Monitoring
Renal function (serum creatinine, BUN)
Frequency: Annually, or more frequently if clinically indicated (e.g., with concomitant nephrotoxic drugs, elderly patients, or history of renal disease).
Target: Within normal limits for age and sex.
Action Threshold: Significant increase in creatinine or BUN; consider dose adjustment or discontinuation.
Liver function tests (ALT, AST, bilirubin)
Frequency: Periodically, or if clinically indicated (e.g., symptoms of liver injury).
Target: Within normal limits.
Action Threshold: Significant elevation; consider discontinuation.
Complete Blood Count (CBC) with differential
Frequency: Periodically, or if clinically indicated (e.g., unexplained bleeding, bruising, fever, sore throat).
Target: Within normal limits.
Action Threshold: Significant decrease in cell counts (e.g., neutropenia, thrombocytopenia); consider discontinuation.
Symptom Monitoring
- Worsening of abdominal pain or diarrhea
- Fever, chills, sore throat (signs of blood dyscrasias)
- Unexplained bleeding or bruising
- Rash, hives, difficulty breathing (signs of hypersensitivity)
- Chest pain, shortness of breath (myocarditis/pericarditis)
- Dark urine, yellowing of skin/eyes (liver injury)
- Decreased urine output, swelling (renal impairment)
- Severe headache, dizziness
Special Patient Groups
Pregnancy
Mesalamine is generally considered low risk during pregnancy. Studies in pregnant women have not shown an increased risk of major birth defects or miscarriage. However, use during pregnancy should be carefully considered, and the benefits should outweigh the potential risks.
Trimester-Specific Risks:
First Trimester:
No increased risk of major birth defects observed in human studies.
Second Trimester:
Generally considered safe; monitor for potential renal effects in the fetus/neonate if exposure is high or prolonged.
Third Trimester:
Generally considered safe; rare reports of renal dysfunction in neonates (e.g., renal impairment, renal failure) following mesalamine exposure, particularly with high doses. Monitor renal function in neonates if exposed in utero.
Lactation
Mesalamine and its metabolite are excreted in breast milk in small amounts. While generally considered compatible with breastfeeding, caution is advised. Monitor breastfed infants for signs of diarrhea.
Infant Risk:
Low risk. Rare reports of diarrhea in breastfed infants. Monitor for changes in bowel habits.
Pediatric Use
Safety and effectiveness of Pentasa capsules have not been established in pediatric patients. Other mesalamine formulations (e.g., Lialda, Apriso) have approved indications and dosing for pediatric ulcerative colitis.
Geriatric Use
Use with caution in elderly patients, as they may be at higher risk for blood dyscrasias and renal impairment. Start at the lower end of the dosing range and monitor renal function closely.
Clinical Information
Clinical Pearls
- Pentasa capsules contain microgranules that are designed for extended release throughout the GI tract. Do not chew or crush them.
- Acute intolerance syndrome (cramping, abdominal pain, bloody diarrhea, fever, headache, rash) can occur and may be difficult to distinguish from an exacerbation of IBD. Discontinue therapy if suspected.
- Mesalamine can cause rare but serious adverse effects including renal impairment, myocarditis/pericarditis, and blood dyscrasias. Regular monitoring of renal function, liver function, and CBC is important.
- Patients should be advised to stay well-hydrated to minimize the risk of renal stone formation.
- Concomitant use with azathioprine or mercaptopurine requires careful monitoring of CBC due to increased risk of myelosuppression.
Alternative Therapies
- Corticosteroids (e.g., prednisone, budesonide)
- Immunomodulators (e.g., azathioprine, mercaptopurine, methotrexate)
- Biologic agents (e.g., infliximab, adalimumab, vedolizumab, ustekinumab)
- JAK inhibitors (e.g., tofacitinib, upadacitinib)
- Surgery (for refractory cases)
Cost & Coverage
Average Cost:
Varies, typically $300-$600+ per 120 capsules (250mg)
Generic Available:
Yes
Insurance Coverage:
Tier 2 or Tier 3 (for brand); Tier 1 or Tier 2 (for generic mesalamine)
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 medical attention. When reporting the incident, be prepared to provide details about the medication taken, the amount, and the time it occurred.