Asacol

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Asacol

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Medically reviewed

Laura Arias

Last updated on 22/12/2025

This page provides general, reference-level information compiled from official medical sources. It is not a substitute for professional medical advice, diagnosis, or treatment. For decisions about your health, please consult a qualified healthcare professional.

Overview of Asacol

Quick Facts about Asacol (Mesalazine)

Property Description
Active Ingredient Mesalazine (5-aminosalicylic acid, 5-ASA)
Form Delayed-release tablets, extended-release tablets, suppositories, enemas
Pharmacological Class Aminosalicylate (Topical Anti-inflammatory)
General Purpose Managing and suppressing chronic intestinal inflammation
Origin Synthetic Compound

What Type of Medicine is Asacol?

Asacol is a prescription-only medication whose active component is Mesalazine, which is chemically identified as 5-aminosalicylic acid or 5-ASA. It is a synthetic compound classified within the aminosalicylate pharmacological group, operating primarily as a topical anti-inflammatory agent. Mesalazine is used as a foundational treatment approach for managing chronic irritation in the bowel. Asacol is a single-component product, utilizing Mesalazine, which is the therapeutically active part derived from older aminosalicylate therapies, providing a focused anti-inflammatory component.

Composition and Specialized Delivery System

The unique composition of Mesalazine products is engineered for site-specific delivery to the lower gastrointestinal tract. Formulations include oral delayed-release tablets and extended-release tablets, as well as rectal formulations, such as suppositories and enemas. The oral dosage forms of Asacol are specifically protected by an enteric-coated matrix designed to release the active ingredient only when it reaches the terminal ileum and colon. This mechanism ensures that drug concentrations are maximized at the site of inflammation. This targeted release capability is a defining characteristic of Mesalazine formulations.

General Purpose of Mesalazine

The general purpose of this medicine is to suppress and manage the chronic, localized inflammation within the lining of the large intestine. Mesalazine achieves this by executing a direct localized anti-inflammatory action, believed to interfere with the chemical pathways that generate inflammatory mediators like prostaglandins and leukotrienes. By modulating this biological response, the core benefit of the drug is to control the underlying inflammatory process, which is necessary for promoting mucosal healing and maintaining the long-term health of the affected intestinal tissue. This general therapeutic use involves maintaining disease stability.

Regulatory References

  1. MedlinePlus Drug Information

What side effects are possible with Asacol?

Official Safety Profile of Mesalazine

The possible side effects and safety characteristics of Mesalazine (Asacol) are classified and documented by government regulatory agencies based on data from clinical studies and post-marketing experience. Adverse reactions are grouped by the affected system or their estimated frequency of occurrence.

Frequency Classification of Adverse Reactions

The most frequently reported adverse reactions, classified as Common (affecting up to 1 in 10 patients), generally include headache, nausea, abdominal pain, and diarrhea. Adverse events such as myocarditis, pericarditis, and peripheral neuropathy are officially classified as Rare (affecting up to 1 in 1,000 patients).

Reactions categorized as Very Rare or Frequency Not Known (based on post-marketing reports) include serious blood disorders like aplastic anemia, as well as severe hepatic failure and acute pancreatitis.

Systemic Safety Considerations

The official labeling notes the potential for serious adverse reactions, particularly those involving internal organ hypersensitivity. These include the risk of renal impairment (such as interstitial nephritis and, rarely, renal failure) and hepatic impairment (hepatitis or hepatic failure). The potential for Mesalazine-Induced Acute Intolerance Syndrome is also noted; this condition presents with symptoms that can mimic a severe exacerbation of ulcerative colitis.

Use is contraindicated in individuals with a known or suspected hypersensitivity to salicylates or any component of the formulation. Specific caution is advised for patients with pre-existing renal or hepatic impairment, and monitoring of renal function is recommended prior to and periodically during treatment.

Overdose and Emergency Response

The official regulatory profile for mesalazine (Asacol) overdose indicates that human experience is rare and limited, leading to guidance that management must be symptomatic and supportive. There is no specific antidote available. In the event of acute high exposure, clinical manifestations may include symptoms associated with the aminosalicylate structure, such as nausea, vomiting, headache, confusion, or seizures, though these are often an exaggeration of known adverse effects.

Regulatory documentation mandates that immediate medical help must be sought for signs of severe or life-threatening systemic reactions that require urgent intervention. This includes any indication of cardiac hypersensitivity (myocarditis or pericarditis), rapid deterioration of renal function (nephritis or renal failure), blood dyscrasias, or the appearance of Severe Cutaneous Adverse Reactions (SCARs). Regulators require patients to discontinue the drug immediately and seek medical attention upon the suspicion of these serious manifestations. Due to the finding that the kidney is a principal target organ for toxicity in preclinical studies, continuous monitoring of renal function and blood counts is essential. This monitoring is particularly critical for elderly patients or those with pre-existing renal or hepatic impairment.

Therapeutic Uses of Asacol

What Asacol Treats

Asacol is a medication primarily prescribed for the management of inflammatory bowel disease (IBD). Its active ingredient, mesalamine (also known as 5-aminosalicylic acid or 5-ASA), acts locally on the lining of the gastrointestinal tract to reduce inflammation.

Main Uses

Asacol is specifically indicated for the following conditions:

  • Ulcerative Colitis: It is used to treat mildly to moderately active ulcerative colitis, a condition characterized by inflammation and sores (ulcers) in the lining of the large intestine (colon) and rectum.
  • Maintenance of Remission: Beyond treating active flare-ups, Asacol is used as a long-term maintenance therapy to help patients stay in remission. This means it helps prevent the symptoms of ulcerative colitis from returning after they have been controlled.

How it Works

The medication is designed with a delayed-release coating that allows the active ingredient to pass through the stomach and small intestine. It begins to release once it reaches the terminal ileum and the colon. By concentrating the medication at the site of the inflammation, it inhibits the production of substances that cause tissue damage and swelling in the intestinal wall.

Expected Benefits

When used as part of a comprehensive treatment plan, the primary goals of therapy include:

  • Reduction of Symptoms: Patients may experience a decrease in common symptoms such as rectal bleeding, abdominal pain, and frequent bowel movements.
  • Mucosal Healing: The anti-inflammatory effect encourages the healing of the intestinal lining.
  • Improved Quality of Life: By maintaining remission and preventing relapses, the medication helps individuals sustain more consistent daily routines and overall well-being.

Eligibility and Restrictions for Use

Eligibility for Asacol (Mesalazine)

Eligibility to use Asacol is determined by regulatory bodies and focuses on documented age restrictions, known allergies, and organ function status.

Absolute Contraindications

Asacol is strictly contraindicated for use in certain patient groups due to formal, documented risks:

  • Hypersensitivity: Individuals with a known or suspected allergy to salicylates (which include mesalazine) or to any other ingredients in the product.
  • Severe Organ Impairment: Patients with severe hepatic impairment (liver failure) or severe renal impairment (kidney failure).
  • Age: Certain formulations are contraindicated in children under 2 years of age.

Conditional Use and Limitations

Use is restricted or conditional for several populations, requiring medical caution and monitoring:

  • Adults: Approved for treating and maintaining remission of Ulcerative Colitis.
  • Pediatric Patients: Approved for treating active UC in children 5 years of age and older. Efficacy for maintenance of remission in those under 18 is not established.
  • Known Impairment: Patients with known, non-severe renal or hepatic impairment require caution and mandatory monitoring of kidney function before and during therapy.
  • Pregnancy and Lactation: Use is conditional; it is only permitted if the potential benefit justifies the potential risk, as determined by a healthcare provider. Specific advice exists for monitoring infants for diarrhea while breastfeeding.
  • Older Adults: Should be used with caution, generally only if they have normal or non-severely impaired kidney and liver function.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Official regulatory documents define the interaction profile of mesalazine (Asacol) based on risks of additive organ system toxicity, potential changes to anticoagulant activity, and compromise to the drug's specialized delivery system.

Documented Interaction Patterns

Category Interacting Substance/Class Official Interaction Outcome
Additive Toxicity Thiopurines (Azathioprine or 6-Mercaptopurine) Increased risk of myelotoxicity (severe blood disorders).
Nephrotoxic Agents (including NSAIDs) Increased risk of nephrotoxicity (kidney damage).
Anticoagulation Warfarin (Oral Anticoagulants) May potentiate or diminish anticoagulant effects, requiring monitoring of INR.
Drug Delivery Antacids or Proton Pump Inhibitors (PPIs) Risk of premature release of the active ingredient due to disruption of the enteric coating, potentially reducing therapeutic effect.

Official Constraints and Monitoring

Co-administration with Thiopurines necessitates monitoring of blood cell counts. When used alongside Warfarin, the regulatory documents require close monitoring of the International Normalized Ratio (INR). Due to the risk of additive kidney damage, renal function must be monitored when mesalazine is administered with other nephrotoxic agents. There are no mandatory timing rules for separation between mesalazine and other medicines. Furthermore, mesalazine use has been documented to interfere with specific laboratory tests, leading to spuriously elevated urinary normetanephrine test results.

Mechanism of Action

The active ingredient, Mesalazine (5-ASA), acts primarily via a localized mechanism that modulates inflammatory pathways within the colon and terminal ileum. This action involves direct intervention in the inflammatory signaling at the cellular level within the gut lining, a process dependent on high local concentration.

Regulating Inflammatory Gene Activation

Mesalazine's fundamental action involves intervening in the nuclear signaling pathways that drive inflammation. It acts as an inhibitor of Nuclear Factor-kappa B (NF-kB), a key protein that initiates the production of inflammatory molecules, while simultaneously acting as an agonist for PPAR-gamma, a nuclear receptor that actively suppresses these same inflammatory genes. This dual-action modulation of transcription factors results in the suppression of the molecular signals that sustain localized inflammation.

Suppressing Local Chemical Mediators

The drug further suppresses inflammation by interfering with key destructive substances in the mucosa. Mesalazine inhibits enzymes like Cyclooxygenase (COX) and Lipoxygenase (LOX), thereby reducing the synthesis of inflammatory messengers such as Leukotriene B4 (LTB4). Additionally, it functions as an antioxidant, chemically scavenging Reactive Oxygen Species (ROS). This multi-target suppression of mediators attenuates tissue degradation and reduces the chemoattraction of immune cells.

Mechanism Constrained to the Mucosal Surface

The mechanism is physiologically constrained, relying on achieving high local concentrations of 5-ASA in direct contact with the inflamed mucosal surface. This topical requirement means the mechanism's action is constrained to superficial inflammation in the colon and is physiologically limited in its influence on inflammation extending deep into the bowel wall (transmural).

Dosage and Administration Information

How to use Asacol (Mesalamine) — Administration Guidelines

Asacol is an oral, delayed-release tablet containing mesalamine (5-aminosalicylic acid), and its administration must strictly follow the instructions to ensure the drug reaches the colon. Due to formulation differences, specific rules apply based on the product prescribed.


Administration Scope

Feature Delayed-Release Tablet (e.g., Asacol 400 mg) Delayed-Release Tablet (e.g., Asacol HD 800 mg)
Route of Administration Oral Oral
Preparation Swallow whole. Do not cut, crush, break, or chew the tablets. Swallow whole. Do not cut, crush, break, or chew the tablets.
Timing in relation to meals Can be taken with or without food. Must be taken on an empty stomach (at least one hour before or two hours after a meal).
Dosing (Adults) 2.4 g to 4.8 g per day for acute disease; 1.6 g per day for maintenance, typically in divided doses. 4.8 g total daily dose (1600 mg three times daily) for moderately active ulcerative colitis, for a duration of 6 weeks.
Age-Group Rules Indicated for mildly to moderately active UC in children 5 years and older (weight-based dosage, max 2.4 g/day); not recommended in some jurisdictions. Approved for use in adults only.
Missed Dose Take the next dose as usual; do not take a double dose to make up for the missed one.
Special Conditions Evaluate renal function before and periodically during therapy; ensure adequate fluid intake. Evaluate renal function before and periodically during therapy; one 800 mg tablet is not substitutable for two 400 mg tablets.

Resulting Procedural Structure

The required sequence involves evaluating renal function prior to initiation, then swallowing the correct delayed-release tablet whole as prescribed, either with or without food for the 400 mg product or specifically on an empty stomach for the 800 mg product (Asacol HD). Doses must be taken regularly, in divided doses or once daily as directed by the condition being treated, and adequate fluid intake must be maintained.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Asacol (Mesalazine)

Evidence for Inducing Remission in Active Ulcerative Colitis

Research examined Asacol (Mesalazine) in numerous short-term, randomized controlled trials (RCTs) to explore how it was evaluated in periods of heightened symptom activity in adults with mild to moderate Ulcerative Colitis (UC). These studies focused on outcomes related to physical discomfort. Researchers mainly studied standardized measurements of Clinical Remission, which included assessing changes in rectal bleeding and stool frequency, as well as monitoring signs of mucosal healing in the colon lining.

Short-term trials reported measurements that differed between the groups using Mesalazine and those using placebo. Studies reported how symptoms evolved in the observed populations over the defined time interval of the trial. These reported outcomes supported the evidence base of Mesalazine for this clinical situation.

Evidence for Maintaining Remission in Ulcerative Colitis

Longer-term research, including multi-year randomized trials, was evaluated in adults whose Ulcerative Colitis was already in a stable state of remission. These studies explored the ongoing use of Mesalazine to see how it was associated with non-recurrence of active symptoms and monitored time to relapse—the return of acute or disruptive episodes.

Studies monitored time to relapse and reported that those continuing Mesalazine treatments had different patterns of symptom recurrence compared to those on placebo. Research also examined simplified approaches to using the medication, with some non-inferiority trials observing how once-daily dosing regimens compared to taking the drug multiple times a day. Findings indicate that these more convenient regimens showed similar patterns of maintaining remission in the observed populations.

Long-Term Research and Extended Follow-up Outcomes

Research has explored the potential extended-term outcomes of Mesalazine use beyond the prevention of immediate relapse. Large-scale observational and cohort studies were necessary to study how use of the medication over many years was associated with long-term complications, such as tracking the incidence of colorectal cancer (CRC) and the need for colectomy (surgical removal of the colon).

Studies focusing on these long-term outcomes reported varied findings across different patient cohorts regarding the association between Mesalazine use and CRC incidence. Some meta-analyses described observed associations with lower incidence rates when Mesalazine was used continuously for long periods. The long-term effects are not fully established because these studies cannot definitively prove cause and effect; they can only describe observed associations over time.

Key Studies & References

  1. Long-Term Mesalamine Maintenance in Ulcerative Colitis: Which is More Important? Adherence or Daily Dose (Veterans Affairs Data)

Frequently Asked Questions (FAQ)

Common questions about Asacol (FAQ)


Q: Is Asacol used to treat all forms of inflammatory bowel disease (IBD)?

A: Official regulatory approval for Asacol is specifically for the treatment of ulcerative colitis (UC). While the active ingredient, mesalamine, may sometimes be discussed in the context of other inflammatory bowel diseases, it is not formally approved for the treatment of Crohn's disease.

Q: What is the difference between Asacol and other mesalamine brands like Lialda or Pentasa?

A: Different oral mesalamine products utilize unique delivery mechanisms, such as specialized enteric coatings or multi-matrix systems, to ensure the medicine reaches the correct part of the digestive tract. These differences in release technology are associated with the variation in official recommendations for use, such as the timing relative to food, which may differ between products.

Q: How quickly should I expect to see an improvement in my symptoms after starting Asacol?

A: Regulatory documents detailing clinical trials often reference a defined period of assessment, which, in many studies for mesalamine, spans several weeks for evaluating the induction of remission (achieving symptom control). Official documents generally describe the overall timeframe for achieving clinical outcomes rather than specifying the exact day-to-day onset of symptom relief.

Q: What should I do if my ulcerative colitis symptoms seem to get worse after starting Asacol?

A: Official labeling notes the potential for a rare reaction called Mesalamine-Induced Acute Intolerance Syndrome. Since the symptoms of this condition, such as cramping, fever, and bloody diarrhea, can closely mimic a severe flare-up of ulcerative colitis, official regulatory documents indicate that the prescribed product is often discontinued if this syndrome is suspected, followed by appropriate medical re-evaluation.

Q: Is the empty shell or casing of the Asacol tablet appearing in my stool normal?

A: Yes, regulatory labeling for this type of delayed-release mesalamine tablet reports that the tablet shell or casing has been observed in the stool. This is a possibility due to the enteric coating designed for release in the lower bowel. However, if this occurs repeatedly, official consumer information generally recommends that this observation be discussed with a healthcare provider.

Q: Is 'mesalamine-induced acute intolerance syndrome' the same as an ulcerative colitis flare-up?

A: No, this syndrome is a drug-induced reaction, not an exacerbation of the disease itself. Regulatory information states that the condition can be difficult to distinguish from a true flare-up because it presents with very similar symptoms, including cramping and bloody diarrhea. It is critical to differentiate the two because the treatment pathway differs.

Q: What are the signs of a serious allergic reaction to Asacol?

A: Mesalamine-induced hypersensitivity reactions have been reported, sometimes involving serious internal organ inflammation like myocarditis (inflammation of the heart muscle) or nephritis (inflammation of the kidney). Official product information emphasizes that signs or symptoms consistent with a hypersensitivity reaction necessitate prompt medical evaluation and may lead to the discontinuation of the prescribed product.

Q: Why is it described that Asacol may cause the urine to change color?

A: Official European product documents describe that mesalamine may cause a harmless red-brown discoloration of the urine. This color change is a result of a common chemical reaction that occurs when the mesalamine metabolites in the urine come into contact with sodium hypochlorite bleach, which is often found in toilet water.

Q: Does Asacol make a person more sensitive to sun exposure (photosensitivity)?

A: According to official consumer safety information, increased sensitivity of the skin to sunlight (known as photosensitivity) has been reported as an uncommon side effect of mesalamine. Some official consumer information materials note that minimizing or avoiding exposure to direct sunlight and tanning devices has been recommended during the use of this medication.

Q: How long does the drug stay in my system after I stop taking it?

A: The time it takes for a drug to be eliminated is described by its half-life, which is the time required for the drug concentration to be reduced by half. Regulatory documents state that the average elimination half-life for mesalamine and its primary metabolite is approximately 12 hours, though this can be variable, depending on individual factors.

Q: Is there a generic version of Asacol available, and is it the same as the brand name?

A: Yes, generic versions of mesalamine delayed-release tablets are formally approved and available. For a generic version to receive official approval, regulatory bodies require it to meet strict bioequivalence standards, meaning they are expected to perform similarly to the brand name reference product in the body.

Q: Does Asacol cause weight gain as a side effect?

A: While not listed among the most common adverse reactions, weight gain has been reported in post-marketing or rare side effect listings for mesalamine. When reported, it is often associated with other symptoms, such as the retention of fluid (edema).

Q: If I have a history of heart issues like myocarditis or pericarditis, can I still use Asacol?

A: Official product information advises that caution should be taken when prescribing mesalamine to patients with pre-existing conditions that might predispose them to developing heart inflammation, such as myocarditis or pericarditis. Official documents also indicate that if previous heart issues were suspected to be drug-induced by mesalamine, the product may be contraindicated.

Q: Is there a link between Asacol and hair loss?

A: Official drug documentation, including European summaries of product characteristics, lists alopecia (hair loss) in the side effect profile for mesalamine. It is generally classified as a very rare or less common side effect.

Q: Can taking Asacol cause joint or muscle pain?

A: Official regulatory sources document that arthralgia (joint pain) and myalgia (muscle pain) are known side effects associated with mesalamine. These are typically classified as less common or very rare adverse events.

Q: Is it possible to develop a severe skin reaction, like Stevens-Johnson syndrome, from taking Asacol?

A: Official sources confirm that the use of mesalamine has been associated with very rare, serious skin reactions, including Stevens-Johnson syndrome (SJS) and toxic epidermal necrolysis (TEN). Regulatory documents state that if signs of a severe skin reaction appear, discontinuation of the product and prompt medical attention are indicated.

Q: Can Asacol be taken if a person has a known sulfur allergy?

A: Asacol's active ingredient, mesalamine, is a salicylate and does not contain sulfa. However, official labeling advises caution for individuals with a history of hypersensitivity to sulfasalazine, a related drug that does contain sulfa, because they may have a similar reaction to mesalamine.

Q: Will Asacol affect my ability to drive or operate machinery?

A: Official product information states that mesalamine has a negligible influence on a person's ability to drive or use heavy machinery. However, if an individual experiences potential side effects such as dizziness or headache, official regulatory advice suggests that driving or operating machinery should be avoided.

Q: What is the connection between Asacol and Reye's syndrome in children?

A: Asacol belongs to the drug class known as salicylates. Official health advisories associated with the salicylate drug class generally caution against their use in children and teenagers who have symptoms of influenza or chickenpox, due to a documented association with the rare, serious condition known as Reye's syndrome.

Q: Can taking Asacol cause new or worsening cough or shortness of breath?

A: Official regulatory summaries list allergic and fibrotic lung reactions as very rare side effects of mesalamine. These reactions may include symptoms such as a cough, shortness of breath (dyspnoea), or tightening of the airways (bronchospasm).

Q: What if I have kidney stones? Can I still take Asacol?

A: Regulatory documents report that the formation of kidney stones has been associated with the use of mesalamine. Official patient information emphasizes the need to ensure sufficient liquid intake during treatment, particularly for individuals with a history of kidney stones.

Q: How long after stopping Asacol might symptoms return?

A: Research studies have indicated that a relapse of the disease (a return of active symptoms) can be anticipated in approximately half of the patients who discontinue mesalamine monotherapy. The official product label does not specify an exact timeframe, but studies describe a potential risk of recurrence following withdrawal.

Q: Do other ingredients in the Asacol tablet cause side effects?

A: Official drug labeling specifies that the medication is contraindicated if a person has an allergy to the active ingredient (mesalamine/salicylates) or to any other ingredient in the product. While the non-active ingredients are not typically listed as causes of common side effects, an allergic reaction to any component of the tablet is a formal possibility.

Q: What is the difference in how Asacol tablets work compared to the discontinued Asacol HD?

A: The two formulations contain different amounts of mesalamine and have different administration requirements: Asacol (400 mg) can be taken with or without food, while Asacol HD (800 mg) was generally required to be taken on an empty stomach. These differing rules are linked to the specific enteric coating technology designed to ensure drug release only occurs in the colon.

How should Asacol be stored and disposed of?

Storage and Disposal of Asacol Tablets

Asacol tablets must be stored according to regulatory requirements to ensure product quality and stability. The medicine must be kept at controlled room temperature, specifically between 68 F and 77 F (20 C and 25 C). Temporary excursions are permitted up to 86 F.

Container and Protection

Storage requires protection from moisture; therefore, the container must be closed tightly, and any desiccant pouches inside the bottle must be left in place. For child safety, the medication must be stored out of the reach of children at all times.

Disposal Instructions

When disposing of unused or expired Asacol, it is mandated that disposal procedures align with local regulations for pharmaceutical waste. The product should not be discarded via wastewater or standard household trash.

Attention! Always consult to a doctor or pharmacist before using pills or medicines.

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