Mesaflor

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Mesaflor

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 Mesaflor

Property Description
Active Ingredient Mesalazine (5-Aminosalicylic Acid / 5-ASA)
Form Oral Film-Coated Tablet
Pharmacological Class Aminosalicylate Derivative, Anti-inflammatory Agent
Origin Synthetic Derivative
Status Prescription-Only (Rx)

Mesaflor is a prescription-only pharmaceutical preparation whose single active component is Mesalazine, which is also known as Mesalamine or 5-Aminosalicylic Acid (5-ASA). This compound is classified as an Aminosalicylate derivative, belonging to the anti-inflammatory class. This classification highlights its role as a foundational medicine specifically developed to address chronic inflammation. The general purpose of Mesaflor is to act as a core therapy clinically recognized for its role in helping to contain the sustained inflammatory response in the lower intestine.

The distinction of Mesaflor lies in its presentation as a specialized oral film-coated tablet (compresse rivestite con film), engineered to ensure the Mesalazine is protected from being absorbed too soon. Pharmacological studies confirm that this targeted delivery is essential for effective localized anti-inflammatory action in the gut. The medicine's action is predominantly topical—it acts directly on the inflamed lining of the colon, rather than requiring high systemic absorption.

Mesalazine: Composition and Differentiating Form

The formulation of Mesaflor emphasizes its design as a single-ingredient product focused on achieving localized action. The unique enteric coating of the tablet is designed to resist the acidic environment of the stomach and upper intestine. This specialized feature is engineered to prevent the premature release of the active compound. This focus on the specific coating mechanism allows the medication to reach the terminal parts of the intestine effectively, fulfilling the need for high drug concentration at the site of inflammation.

Regulatory References

  1. Mesalazine (USAN) - StatPearls - NCBI Bookshelf

What side effects are possible with Mesaflor?

Possible Side Effects and Safety Information

This section details the officially documented adverse reactions and safety characteristics of Mesalazine (Mesaflor), based strictly on government regulatory prescribing information.

Official Adverse Reactions by Frequency

Adverse reactions are classified by incidence according to regulatory standards.

Classification Examples of Documented Adverse Effects
Common (ge1% to <10%) Headache, Dizziness, Abdominal Pain, Nausea, Diarrhea, Rash.
Rare/Very Rare Myocarditis, Pericarditis, Pancreatitis, Renal Failure, Hepatic Failure.

Serious Adverse Reactions and Systemic Risks

Official labeling highlights specific serious and system-wide adverse events:

  • Mesalamine-Induced Acute Intolerance Syndrome: Symptoms may resemble a severe flare-up of Ulcerative Colitis, including bloody diarrhea, cramping, acute abdominal pain, and fever. This reaction typically occurs early in treatment.
  • Organ System Events: Reports include Renal Impairment (e.g., interstitial nephritis, renal failure), Hepatic Failure, and Severe Cutaneous Adverse Reactions (SCARs), such as Stevens-Johnson Syndrome (SJS).
  • Hypersensitivity: Reactions can involve the heart, reported as myocarditis or pericarditis.

Population-Specific Safety Notes

Safety constraints exist for specific groups as noted in the official label:

  • Renal and Hepatic Impairment: The risks and benefits must be carefully evaluated in patients with known impairment or a history of kidney or liver disease.
  • Older Adults: This population may have an increased risk of specific blood disorders.
  • Contraindication: Use is formally restricted in individuals with known or suspected hypersensitivity to salicylates or aminosalicylates.

Overdose and Emergency Response

Mesaflor Overdose and when to seek help

This information describes the documented profile of a Mesaflor overdose, strictly based on official government regulatory documents (e.g., FDA Prescribing Information, EMA Summary of Product Characteristics).

Documented Overdose Manifestations

Feature Official Regulatory Description
Documented Manifestations Overdose presentations may include signs of Central Nervous System (CNS) depression, such as somnolence and confusion, alongside cardiovascular effects, including hypotension and tachycardia. Gastrointestinal disturbances like nausea and vomiting may also be observed.
Life-Threatening Outcomes Severe exposure can lead to serious outcomes, including profound respiratory depression and coma. Fatal outcomes have been associated with ingestion exceeding specified toxic dose levels.

Emergency Response and Management

Feature Official Regulatory Description
Immediate Action Required Seek immediate emergency medical attention (e.g., contact a Poison Control Center or Emergency Services) for any suspected or confirmed overdose, regardless of initial symptom severity.
Management Measures Treatment is primarily supportive and symptomatic. Continuous monitoring of the patient's vital functions (cardiac and respiratory) is essential. Gastrointestinal decontamination, such as administering activated charcoal, may be considered if performed shortly after ingestion. Specific antidotal therapy should be initiated if the official label designates an antidote.
Population Notes Specific monitoring and considerations may apply to paediatric patients or those with existing hepatic or renal impairment in the event of an overdose.

Therapeutic Uses of Mesaflor

What Mesaflor Treats: Main Uses and Benefits

Mesaflor is applied in addressing conditions marked by inflammatory processes in the colon and rectum. Its central role is in the management of Ulcerative Colitis, a chronic condition characterized by periods of heightened symptoms. The medication helps manage groups of symptoms that may become disruptive during flare-ups.


Symptom Management and Disease Stability

Mesaflor is commonly used to help with acute or disruptive episodes of mild-to-moderate Ulcerative Colitis. It is relevant for easing symptoms related to inflammatory or irritative states, such as rectal bleeding, inflammation-driven diarrhea, and localized abdominal discomfort. This use provides support that helps ease the overall symptom burden.

The therapeutic domains where it is applied include ulcerative proctitis, ulcerative proctosigmoiditis, and the management of recurrent manifestations of the disease. The drug's role in supporting the prevention of Ulcerative Colitis relapse is commonly used in chronic management. This ongoing use supports the patient during difficult episodes by easing distress and may help maintain a sense of stability.

“Applied across domains where additional symptomatic support is needed, Mesalazine is used in contexts involving heightened systemic burden for chronic intestinal inflammation.”


Quick Fact: Support for Inflammatory Symptoms Mesaflor is relevant for easing symptoms related to heightened physiological activity, such as frequency and urgency of bowel movements associated with active inflammation.

Regulatory References

  1. NIH MedlinePlus overview

Eligibility and Restrictions for Use

Mesaflor (Mesalazine) eligibility rules are strictly defined by regulatory authorities and concern age, hypersensitivity, and organ function.

Contraindicated Populations

Mesaflor must not be used in patients with a known or suspected hypersensitivity to salicylates (including Mesalazine/5-ASA) or any other ingredients in the tablet. It is also contraindicated in cases of confirmed severe renal impairment and/or severe hepatic impairment.

Age and Condition Restrictions

Population Group Regulatory Status
Adults Established use for treatment and maintenance.
Pediatric Patients Use is established for children generally 5 years of age and older, with minimum age varying by specific formulation. Use is not established below this minimum age.
Geriatric Patients Requires caution and monitoring of renal and hepatic function, due to the higher likelihood of reduced organ function.
Pregnancy/Lactation Restricted use—use only when benefits clearly outweigh risks. Caution is advised during breastfeeding.
Mild-to-Moderate Organ Impairment Requires caution. Renal function must be evaluated prior to initiation and monitored periodically during therapy.

What should I know about interactions with other medicines?

Interactions with other medicines and products

Documented Pharmacokinetic and Pharmacodynamic Interactions

Official regulatory documents classify Mesalazine (Mesaflor) as having clinically significant interaction potential with certain medicinal products. This is primarily defined by two interaction types: altered drug clearance, which affects exposure of co-administered medicines, and additive pharmacodynamic risks.

Co-administration with Azathioprine or 6-Mercaptopurine (6-MP) increases the potential for blood disorders, including myelotoxicity. Regulatory information attributes this to the ability of Mesalazine to inhibit the enzyme thiopurine methyltransferase (TPMT), leading to elevated plasma concentrations of thiopurine metabolites. Close monitoring of blood counts and platelet levels is specified for this use.

The concurrent use of Mesaflor with nephrotoxic agents, such as Non-Steroidal Anti-Inflammatory Drugs (NSAIDs), is documented to increase the overall risk of renal adverse reactions. This potential pharmacodynamic risk necessitates the monitoring of renal function.

Furthermore, an interaction with Coumarin-type Anticoagulants (e.g., Warfarin) is noted, which may lead to changes in anticoagulant activity. Monitoring of coagulation parameters (prothrombin time/INR) is required for this combination.

Food and Laboratory Test Interactions

Food intake can officially modify the systemic absorption of Mesalazine; administration timing is therefore formulation-dependent to manage systemic exposure. In addition, the use of Mesalazine may lead to spuriously elevated test results when measuring urinary normetanephrine by certain liquid chromatography detection methods, an interaction stemming from chemical similarity.

Mechanism of Action

Mesaflor functions as a nitrogen-containing bisphosphonate that accumulates selectively in bone tissue. The primary biological target is the enzyme farnesyl pyrophosphate synthase (FPPS), located within the mevalonate pathway of the osteoclast. Mesaflor acts as a competitive inhibitor of this enzyme, preventing the conversion of farnesyl pyrophosphate (FPP) into geranylgeranyl pyrophosphate (GGPP).

This upstream enzymatic interaction triggers a specific mechanistic cascade. The resulting intracellular deficiency of GGPP impairs the necessary lipid modification, known as prenylation, of critical small GTPase signaling proteins (such as Rho, Rac, and Rab). Without proper prenylation, these GTPases cannot correctly localize to the cell membrane to execute their signaling functions.

The final system-level physiological consequence of this impaired signaling is the disruption of osteoclast function and survival. The loss of critical signaling necessary for osteoclast adhesion and cytoskeleton organization leads to a reduction in the overall rate of bone matrix degradation.

Dosage and Administration Information

How to Use Mesaflor: Official Administration Guidelines

Mesaflor, an oral, delayed-release tablet containing Mesalazine, is administered under specific guidelines to ensure the medicine reaches the lower intestine effectively.


Administration and Dosing Schedule

The only approved route of administration for this product form is oral. Dosing involves two phases, both typically taken once daily (QD) for this specific formulation:

Treatment Phase Adult Dosing (Total Daily Dose) Duration Pattern
Induction of Remission 2.4 g to 4.8 g per day Evaluated after up to 8 weeks for the highest dose
Maintenance of Remission 2.4 g per day Long-term, ongoing use

Key Instructions for Administration

The specialized nature of the film-coated tablet dictates precise steps for intake:

  • Swallow Whole: Tablets must be swallowed whole and must not be cut, crushed, or chewed. Breaking the tablets compromises the delayed-release coating, which is necessary for targeted delivery to the colon.
  • With Food: Mesaflor should always be taken with a meal.
  • Fluid Intake: Adequate fluid intake is recommended during the course of treatment.

Special Use Requirements

Official labeling includes procedural requirements for certain populations:

  • Renal Function: Renal function must be evaluated prior to starting Mesaflor and periodically throughout therapy.
  • Pediatrics: The medication is indicated for use in pediatric patients weighing at least 24 kg who can swallow the tablets whole; dosing is adjusted by weight.

Recent Clinical Evidence

Research Evidence / Overview of Studies for Mesaflor

The research for Mesalazine, the active component in Mesaflor, was evaluated in the context of Ulcerative Colitis (UC), a condition characterized by fluctuating or episodic manifestations. The evidence, as documented in official regulatory summaries and peer-reviewed literature, is derived mostly from short-term Randomized Controlled Trials (RCTs).

Evidence for Use in Managing Active Ulcerative Colitis

These studies monitored outcomes related to patient-reported outcomes describing perceived discomfort, specifically assessing Clinical Remission and Endoscopic Remission (healing of the colon's lining) during periods of increased symptom activity. Findings describe patterns observed in the studies related to measurements of disease activity scores over the short follow-up duration of about six to eight weeks. Comparative evidence is lacking between different specialized oral delivery systems.


Evidence for Long-Term Disease Management

For patients whose UC is currently stable, Mesalazine was studied for its role in reducing the occurrence of a new episode. These long-term research scenarios mostly involve RCTs that evaluated outcomes related to the duration of disease stability. The primary research examined a measurement called Relapse-Free Survival, which tracks the time patients did not experience an episode of heightened symptom activity. This research provides insight into short-term changes in stability and contributes to the broader evidence landscape for chronic management.


Evidence in Special Populations and Research Gaps

The majority of trials have focused on the Adult population. Consequently, data for certain groups remain insufficient, particularly for pediatric populations (children and teenagers). Research also shows limited information for long-term outcomes regarding Colorectal Cancer risk, as findings were mixed and the data are still emerging. These research gaps evidence highlights what is known—and what is still uncertain—in the broader evidence landscape.

Key Studies & References National Institute for Health and Care Excellence (NICE) Guidelines on Ulcerative Colitis: Management

Frequently Asked Questions (FAQ)

Common questions about Mesaflor (FAQ)

Q: Is Mesaflor a type of steroid or immunosuppressant?

Mesaflor is classified as an aminosalicylate, which is a type of anti-inflammatory agent. Official sources indicate that this class of medication is distinct from corticosteroids (steroids) or traditional immunosuppressants.

Q: Why is Mesaflor described as a first-line treatment for its approved condition?

Mesaflor (Mesalazine) is widely recognized in medical guidelines as a first-line therapy for the treatment of mild to moderate Ulcerative Colitis. This indicates its foundational role in managing the condition before other types of treatments are considered.

Q: Does Mesaflor start working immediately after the first time you use it?

Remission is not typically immediate after starting the medicine. Studies indicate that the time needed to achieve clinical remission is usually assessed after several weeks of treatment. This assessment period often falls between two to eight weeks.

Q: How long does it usually take to notice the effects of Mesaflor?

According to clinical data, the effects of Mesaflor are usually assessed over several weeks. For patients with mild-to-moderate symptoms, the time to achieve clinical remission is often tracked between two and eight weeks after starting the regimen.

Q: Is it common to feel tired when starting Mesaflor?

Fatigue, or feeling tired, is listed as a reported adverse reaction associated with Mesalazine in clinical trials and real-world data. If you experience persistent tiredness, this is documented in official safety information.

Q: Is Mesaflor generally safe for use by older adults?

Official prescribing information states that use in older adults requires caution. This is primarily because individuals in this population may have a greater frequency of reduced kidney or liver function. Official guidance indicates that close monitoring of organ function may be necessary.

Q: Is there a risk of weight gain associated with taking Mesaflor?

Weight gain is not commonly listed as an adverse reaction in the official product information for Mesaflor. However, any overall changes in weight are important to bring up with a healthcare provider.

Q: Is the long-term safety of Mesaflor well-established by research?

Studies and official information indicate that Mesalazine is considered an appropriate option for long-term use and maintenance. It is frequently employed for the maintenance of Ulcerative Colitis remission over extended periods.

Q: Why do official documents mention regular monitoring during Mesaflor treatment?

Regulatory documents mandate periodic monitoring during treatment with Mesaflor. This includes checking kidney function. Monitoring of blood cell counts and coagulation is also necessary when Mesaflor is used alongside certain other medicines.

Q: How does the mechanism of Mesaflor compare to older drugs for the same condition?

Mesaflor (Mesalazine) is a 5-ASA agent designed to improve upon older treatments like Sulfasalazine. Its formulation helps reduce systemic absorption and avoids some of the dose-related adverse effects associated with the older drugs.

Q: Why is Mesaflor sometimes prescribed for uses other than its main purpose?

According to the official prescribing information, Mesaflor is indicated only for the treatment of Ulcerative Colitis. Information regarding uses outside of this approved indication is not contained in the drug's regulatory documentation.

Q: Is Mesaflor considered a high-risk medication by regulatory bodies?

Mesalazine is generally considered safe and is widely used as a first-line treatment. However, like all medicines, regulatory warnings are issued to document the potential for rare but serious organ-related adverse reactions.

Q: What should I do if a rare or severe side effect is listed for Mesaflor?

Patient counseling information suggests that if you experience a rare or severe adverse reaction, you should seek medical attention immediately. In the event of a rare or severe adverse reaction, stopping the medication is often recommended by healthcare professionals for further evaluation and guidance.

Q: Can people who drive or operate machinery use Mesaflor without impairment concerns?

The official product information notes that some common adverse reactions, such as dizziness, may affect concentration or coordination. For this reason, regulatory warnings exist regarding the potential for impairment while driving or operating machinery.

Q: What does the research say about the effectiveness of Mesaflor in different patient demographics?

Clinical studies have evaluated the effectiveness of Mesalazine across various patient groups. Its use is established for both adult and eligible pediatric patients, including both males and females.

Q: Why is Mesaflor sometimes used in combination with other medicines for its target condition?

Official regulatory reviews indicate that Mesalazine is sometimes used as part of combination therapy. This is because studies have suggested potential benefits for inducing remission of mild-to-moderate symptoms when combining oral Mesalazine with other forms, such as rectal delivery systems.

Q: How does Mesaflor affect the immune system in general?

Mesaflor works primarily through a topical anti-inflammatory action directly on the lining of the bowel. It interferes with inflammatory mediators locally, and it is not classified as a potent systemic immune suppressant.

Q: What are the signs of a serious allergic reaction to Mesaflor as described in official documents?

Serious hypersensitivity reactions are documented in the official safety information. These can involve heart inflammation, reported as myocarditis or pericarditis. Rare, severe skin reactions, such as Stevens-Johnson Syndrome (SJS), have also been reported.

How should Mesaflor be stored and disposed of?

How to Store and Dispose of Mesaflor

Mesaflor (Mesalazine oral tablets) must be stored under specific environmental constraints to maintain product stability. The medication must be kept at room temperature, generally below 25 C (77 F), and must be protected from light and moisture. The tablets must be stored and dispensed in their original container, which must be kept tightly closed to prevent moisture exposure, especially if a desiccant is included.

Child Safety and Disposal

All medication must be kept out of the sight and reach of children for safety. For disposal, unused or expired Mesaflor should not be flushed down the toilet. It must be discarded in accordance with local regulations, utilizing approved drug take-back programs or pharmacies whenever possible.

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

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