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Medical Disclaimer: This information is for educational purposes only and is not a substitute for professional medical advice.
Brand Name
Pentasa
Generic Name
Mesalamine
Active Ingredient
MesalamineCategory
Aminosalicylate [EPC]
Variants
2
This page is for informational purposes only and does not replace medical advice. Before using any prescription or over-the-counter medication for Pentasa, you must consult a qualified healthcare professional.
Detailed information about Pentasa
Mesalamine is an aminosalicylate anti-inflammatory medication primarily used to induce and maintain remission in patients with ulcerative colitis. It works locally in the gastrointestinal tract to reduce inflammation and associated symptoms.
Dosage for mesalamine varies significantly based on the brand, the severity of the condition, and whether the goal is to treat an active flare or maintain remission. According to clinical guidelines:
Mesalamine is approved for use in pediatric patients for specific indications, but the age and weight requirements vary by brand. For instance:
Mesalamine is known to be nephrotoxic (toxic to the kidneys). Patients with known renal impairment should use this medication with extreme caution. Healthcare providers typically avoid prescribing mesalamine if the estimated glomerular filtration rate (eGFR) is significantly reduced. Regular monitoring of serum creatinine is mandatory.
While mesalamine is primarily cleared renally, it is metabolized in the liver. Caution is advised in patients with known liver failure, as there have been reports of hepatic failure in patients with pre-existing liver disease taking mesalamine.
Clinical trials have not identified major differences in safety between elderly and younger patients. However, since older adults are more likely to have decreased renal function, dose selection should be cautious, usually starting at the lower end of the dosing range.
If you miss a dose, take it as soon as you remember. However, if it is almost time for your next scheduled dose, skip the missed dose and return to your regular schedule. Do not double the dose to catch up.
Signs of mesalamine overdose are similar to salicylate (aspirin) poisoning and may include:
In the event of a suspected overdose, contact your local poison control center or seek emergency medical attention immediately. Treatment typically involves gastric lavage and intravenous fluids to maintain electrolyte balance.
> Important: Follow your healthcare provider's dosing instructions. Do not adjust your dose without medical guidance.
Most patients tolerate mesalamine well, but some may experience mild to moderate side effects as the body adjusts to the medication. Common side effects include:
Mesalamine is a salicylate, related to aspirin. Patients with a known allergy to aspirin or other salicylates should not take mesalamine. It is crucial to inform your doctor if you have ever had a reaction to sulfasalazine (Azulfidine), as many patients who cannot tolerate sulfasalazine may also react to mesalamine.
No FDA black box warnings for Mesalamine.
There are few absolute contraindications for drug combinations with mesalamine, but the following should be avoided due to the high risk of toxicity:
Mesalamine must NEVER be used in the following circumstances:
Mesalamine is generally considered one of the safer options for managing ulcerative colitis during pregnancy. It was formerly classified as FDA Pregnancy Category B. Data from published observational studies and case reports have not identified a clear drug-associated risk of major birth defects or miscarriage. However, it is known that mesalamine crosses the placental barrier.
Untreated ulcerative colitis poses a significant risk to both the mother and the fetus, including preterm birth and low birth weight. Therefore, most gastroenterologists recommend continuing mesalamine during pregnancy to maintain remission. Some formulations (like Asacol HD) previously contained dibutyl phthalate (DBP), which raised concerns in animal studies, but many newer formulations have removed this ingredient.
Mesalamine and its metabolite, N-acetyl-5-ASA, are excreted in human milk in small amounts. While most infants do not experience adverse effects, there have been reports of diarrhea in breastfed infants. If you are breastfeeding, monitor your baby for changes in bowel habits. The decision to breastfeed should be made in consultation with your doctor, weighing the benefits of breastfeeding against the potential risk of infant exposure.
Mesalamine (5-aminosalicylic acid) is an anti-inflammatory drug that acts locally on the intestinal mucosa. Its molecular mechanism involves several pathways:
Common questions about Pentasa
Mesalamine is primarily used to treat and manage ulcerative colitis, a chronic inflammatory bowel disease that affects the lining of the large intestine and rectum. It is used both to treat active 'flares' (induction of remission) and to prevent symptoms from returning (maintenance of remission). By acting locally on the gut lining, it reduces inflammation, which helps stop rectal bleeding, diarrhea, and abdominal pain. Some doctors may also use it off-label for certain types of Crohn's disease, though it is most effective for ulcerative colitis. It is available in various oral and rectal forms to target different areas of the colon.
The most frequently reported side effects of mesalamine include headache, flatulence (gas), nausea, and mild abdominal pain. Many patients also report burping or a sore throat shortly after starting the medication. These symptoms are often mild and may resolve as your body adjusts to the drug. However, if you experience severe cramping, bloody diarrhea, or a fever, you should contact your doctor immediately, as these can be signs of a rare intolerance syndrome. Most people find mesalamine much easier to tolerate than older medications like sulfasalazine.
There is no known direct chemical interaction between alcohol and mesalamine that would make the drug dangerous. However, alcohol is a known gastrointestinal irritant and can trigger or worsen the symptoms of ulcerative colitis, such as diarrhea and cramping. For this reason, many healthcare providers suggest limiting alcohol consumption to help keep your disease in remission. If you do choose to drink, it is best to do so in moderation and observe how your body reacts. Always discuss your lifestyle habits with your gastroenterologist.
Mesalamine is generally considered a low-risk medication during pregnancy and is often continued to ensure the mother's disease remains stable. Clinical data suggests that it does not significantly increase the risk of birth defects or miscarriage. Because an active flare-up of ulcerative colitis poses a greater risk to the pregnancy than the medication itself, most doctors advise staying on the drug. However, you should inform your obstetrician and gastroenterologist as soon as you become pregnant. They will help you weigh the benefits and ensure you are on a formulation that is appropriate for pregnancy.
Mesalamine is not a fast-acting medication; it takes time to reduce the inflammation in the gut wall. Most patients begin to notice an improvement in their symptoms, such as reduced frequency of bowel movements and less bleeding, within 2 to 4 weeks of starting treatment. However, it can take up to 6 to 12 weeks to achieve full clinical remission or for the intestinal lining to heal completely. It is important to continue taking the medication exactly as prescribed, even if you do not feel an immediate difference. Consistency is key to the drug's success.
You should not stop taking mesalamine suddenly without first consulting your healthcare provider. Ulcerative colitis is a lifelong condition, and mesalamine is often used as a 'maintenance' therapy to keep the disease from flaring up again. Stopping the medication abruptly can lead to a return of painful symptoms and inflammation within a few weeks or months. While there is no 'withdrawal' effect like you might see with some other drugs, the risk of a disease relapse is very high. If you are concerned about side effects or the cost of the drug, talk to your doctor about alternatives.
If you miss a dose of mesalamine, you should take it as soon as you remember. If it is almost time for your next scheduled dose, skip the missed dose and continue with your regular dosing schedule. You should never take two doses at the same time to make up for a missed one, as this could increase the risk of side effects like stomach upset or headache. Setting a daily alarm or using a pillbox can help you stay consistent with your treatment. If you miss multiple doses in a row, contact your doctor for further instructions.
Weight gain is not a common side effect of mesalamine according to clinical trial data. Unlike corticosteroids (such as prednisone), which are also used for ulcerative colitis and frequently cause weight gain and increased appetite, mesalamine acts locally and has minimal systemic hormonal effects. If you experience weight gain while taking mesalamine, it may be because your disease is better controlled, allowing you to eat a more varied diet and absorb nutrients more effectively. If you have concerns about sudden or unusual weight changes, discuss them with your healthcare provider.
Mesalamine can be taken with many other medications, but there are some important exceptions. You should be particularly cautious with NSAIDs like ibuprofen or naproxen, as these can increase the risk of kidney damage when combined with mesalamine. It also interacts with certain immune-suppressing drugs like azathioprine, potentially increasing the risk of low blood cell counts. Always provide your doctor with a full list of your current medications, including over-the-counter supplements. Your doctor may need to perform more frequent blood tests if you are taking interacting drugs.
Yes, mesalamine is available in several generic versions, which can significantly reduce the cost of treatment. However, it is important to note that different brands and their generic equivalents use different delivery systems (such as pH-dependent coatings). Because of this, a generic for one brand (like Lialda) is not the same as a generic for another brand (like Asacol HD). You should ensure that your pharmacist provides the specific generic that matches the brand your doctor prescribed. Do not switch between different generic versions without your doctor's approval.
Other drugs with the same active ingredient (Mesalamine)
> Warning: Stop taking Mesalamine and call your doctor immediately if you experience any of these.
No FDA black box warnings for Mesalamine. However, the lack of a black box warning does not imply the drug is without significant risks; the warnings regarding renal impairment and acute intolerance syndrome are considered the most critical safety issues.
Report any unusual symptoms to your healthcare provider. Monitoring through regular blood tests is the best way to detect serious side effects before they become symptomatic.
To ensure the safe use of mesalamine, the following monitoring is typically recommended by healthcare providers:
Mesalamine is generally not expected to affect your ability to drive or operate machinery. However, if you experience dizziness or significant headaches, you should avoid these activities until you know how the medication affects you.
There is no direct contraindication between alcohol and mesalamine. However, alcohol can irritate the gastrointestinal tract and may worsen the symptoms of ulcerative colitis (such as diarrhea and cramping). It is generally advised to limit alcohol consumption to avoid exacerbating your underlying condition.
Do not stop taking mesalamine suddenly without consulting your doctor, even if you feel better. Ulcerative colitis is a chronic condition, and stopping maintenance therapy often leads to a relapse of symptoms. There is no known withdrawal syndrome associated with mesalamine, but the risk of a disease flare is high upon discontinuation.
> Important: Discuss all your medical conditions with your healthcare provider before starting Mesalamine.
For each major interaction, the management strategy usually involves either avoiding the combination or increasing the frequency of laboratory monitoring to detect early signs of toxicity or reduced efficacy.
> Important: Tell your doctor about ALL medications, supplements, and herbal products you are taking.
> Important: Your healthcare provider will evaluate your complete medical history before prescribing Mesalamine.
As discussed in the dosage section, mesalamine is approved for children as young as 5 years old for certain brands (like Delzicol). It is not typically used in infants. In pediatric patients, the primary concern is ensuring the child can swallow the tablets or capsules whole, as crushing them destroys the therapeutic delivery mechanism. Growth parameters should be monitored in children with IBD, though mesalamine itself does not typically affect growth negatively.
In patients over 65, the primary concern is age-related decline in renal function. Clinical studies have shown that the risk of adverse reactions is slightly higher in the elderly, particularly blood dyscrasias (like leucopenia). Healthcare providers should perform baseline renal function tests and monitor more frequently than in younger adults.
For patients with a GFR between 30 and 60 mL/min/1.73m², mesalamine should be used with caution and at the lowest effective dose. It is generally avoided if the GFR is below 30 mL/min/1.73m². There is no specific data on the clearance of mesalamine by hemodialysis, but given its protein binding, it is unlikely to be significantly removed.
No specific dose adjustment guidelines exist for hepatic impairment, but because the liver is the primary site of acetylation (metabolism), patients with Child-Pugh Class B or C cirrhosis should be monitored for signs of drug accumulation and toxicity.
> Important: Special populations require individualized medical assessment.
The therapeutic effect of mesalamine is concentration-dependent at the site of inflammation. Because it acts topically, the 'dose-response' relationship is more closely tied to the amount of drug reaching the colon than the amount in the bloodstream. The onset of action is typically slow, with symptomatic improvement often taking 2 to 4 weeks, and full mucosal healing taking 6 to 12 weeks.
| Parameter | Value |
|---|---|
| Bioavailability | 20% to 30% (systemic) |
| Protein Binding | 40% to 50% |
| Half-life | 0.5 to 1.5 hours (Mesalamine); 5-10 hours (N-acetyl metabolite) |
| Tmax | 4 to 12 hours (varies by formulation) |
| Metabolism | N-acetyltransferase-1 (NAT-1) in liver and gut wall |
| Excretion | Renal (absorbed portion); Fecal (unabsorbed portion) |
Mesalamine is the gold-standard 'Aminosalicylate.' Related medications in the same class include sulfasalazine (a prodrug), balsalazide, and olsalazine. Unlike sulfasalazine, mesalamine does not contain a sulfa moiety, which makes it much better tolerated by most patients.