Asacol (mesalamine) is a first-line, prescription medication specifically designed for the treatment of active, mild to moderate ulcerative colitis and for the maintenance of remission. It belongs to the 5-aminosalicylic acid (5-ASA) class of drugs, which work locally at the site of inflammation in the colon to reduce symptoms and promote mucosal healing. This delayed-release formulation ensures the active ingredient is delivered directly to the affected area, maximizing therapeutic effect while minimizing systemic exposure. It represents a cornerstone of gastroenterological practice for managing this chronic inflammatory bowel disease.

Features

• Active ingredient: Mesalamine (also known as 5-aminosalicylic acid or 5-ASA).
• Formulation: Delayed-release tablets designed with a pH-dependent acrylic-based resin coating.
• Mechanism: Local anti-inflammatory action within the colonic lumen and mucosa.
• Delivery System: Designed to begin dissolution at pH 7 or higher, typically in the terminal ileum and colon, targeting the site of disease.
• Standard Dosage Strengths: Available in 400 mg and 800 mg delayed-release tablets.
• Prescription Status: Requires a prescription from a licensed healthcare provider.

Benefits

• Effectively induces remission in patients with active, mild to moderate ulcerative colitis, reducing symptoms like diarrhea, rectal bleeding, and abdominal pain.
• Clinically proven to maintain remission, helping to prevent flare-ups and prolong periods of disease-free health.
• Provides targeted topical action within the colon, minimizing systemic absorption and associated side effects compared to broader immunosuppressants.
• Supports endoscopic and histological healing of the colonic mucosa, which is a key treatment goal beyond mere symptom control.
• Offers a well-tolerated first-line treatment option with a long-established safety profile based on decades of clinical use and research.
• Contributes to an improved quality of life by reducing the frequency and severity of disease flares, allowing for greater daily normalcy.

Common use

Asacol is primarily indicated for the treatment of active, mild to moderate ulcerative colitis. It is used to reduce the signs and symptoms of an active flare, including stool frequency, rectal bleeding, and mucosal inflammation observed during sigmoidoscopy. Furthermore, it is widely prescribed for the maintenance of remission following successful treatment of an acute episode. Its use is focused on colonic disease and it is not indicated for Crohn’s disease affecting the small intestine.

Dosage and direction

For the treatment of active ulcerative colitis: The typical adult dosage is 2.4 grams to 4.8 grams per day, administered orally in divided doses. A common regimen is two 800 mg tablets taken three times daily (totaling 4.8 g/day) for a duration of 6 weeks. For the maintenance of remission of ulcerative colitis: The typical adult dosage is 1.6 grams per day, administered orally in divided doses. A common regimen is two 400 mg tablets taken twice daily or one 800 mg tablet taken twice daily. Administration Instructions: Tablets must be swallowed whole and must not be crushed, broken, or chewed. This is critical to preserve the integrity of the pH-dependent delayed-release coating. Asacol can be taken with or without food, though consistency in administration relative to meals is often advised.

Precautions

• Patients with pre-existing renal impairment should use Asacol with extreme caution. Renal function (e.g., serum creatinine) should be assessed prior to initiation of therapy and periodically during treatment.
• Patients with known sulfasalazine sensitivity should be monitored closely, as cross-sensitivity reactions with mesalamine are possible.
• Use with caution in patients with pyloric stenosis or any condition that may delay gastric emptying, as this could affect the drug’s delivery to the colon.
• Mesalamine has been associated with an acute intolerance syndrome that may mimic a colitis flare (cramping, acute abdominal pain, bloody diarrhea). If this occurs, prompt medical evaluation is necessary.
• Patients should be advised to report any unexplained bleeding, bruising, purpura, sore throat, fever, or malaise, as these may be signs of more serious blood dyscrasias.
• Caution is advised in patients with hepatic impairment.

Contraindications

Asacol is contraindicated in patients with known hypersensitivity to salicylates (including mesalamine) or to any component of the formulation. It is also contraindicated in patients with severe renal impairment (where the risk of further nephrotoxicity outweighs the potential benefit).

Possible side effect

The majority of side effects are mild and often subside with continued therapy. Common side effects may include:

• Headache
• Abdominal pain or cramps
• Nausea
• Diarrhea
• Flatulence
• Rash Less common but more serious side effects require immediate medical attention and can include:
• Acute pancreatitis (severe abdominal pain, nausea, vomiting)
• Hepatotoxicity (jaundice, pruritus, dark urine)
• Nephrotoxicity (changes in urinary output, edema)
• Blood dyscrasias (unusual bleeding/bruising, pallor, fatigue)
• Pericarditis (chest pain, difficulty breathing)
• Severe cutaneous adverse reactions (e.g., Stevens-Johnson Syndrome)
• Worsening of colitis symptoms

Drug interaction

• Anticoagulants (e.g., Warfarin): Mesalamine may potentiate the anticoagulant effect, increasing the risk of bleeding. Increased monitoring of INR is recommended.
• Azathioprine or 6-Mercaptopurine: Concurrent use with mesalamine may increase the risk of blood disorders, such as leukopenia and thrombocytopenia.
• Non-Steroidal Anti-Inflammatory Drugs (NSAIDs): Concomitant use may increase the potential for renal adverse reactions and should generally be avoided.
• Lactulose: Concurrent administration may cause the premature release of mesalamine in the small intestine due to a drop in pH, potentially reducing its efficacy.

Missed dose

If a dose is missed, it should be taken as soon as it is remembered. However, if it is almost time for the next scheduled dose, the missed dose should be skipped. Patients should not double the dose to make up for a missed one. Maintaining a consistent dosing schedule is important for efficacy.

Overdose

Cases of mesalamine overdose are rare. The delayed-release mechanism limits acute systemic absorption. Reported symptoms of overdose may include tinnitus, vertigo, headache, confusion, nausea, vomiting, diarrhea, hyperventilation, and sweating. Severe overdose could lead to metabolic acidosis, renal failure, and cardiovascular collapse. There is no specific antidote. Management involves immediate cessation of the drug and institution of supportive and symptomatic care, including careful monitoring of renal function.

Storage

Store Asacol tablets at controlled room temperature, 20°C to 25°C (68°F to 77°F), with excursions permitted between 15°C and 30°C (59°F and 86°F). Keep the bottle tightly closed and stored in a dry place. Protect from moisture and light. Keep all medications out of the reach of children and pets.

Disclaimer

This information is for educational and informational purposes only and does not constitute medical advice. It is not a substitute for professional medical advice, diagnosis, or treatment. Always seek the advice of your physician or other qualified health provider with any questions you may have regarding a medical condition or medication. Never disregard professional medical advice or delay in seeking it because of something you have read here. The content has been compiled from various sources but may not be comprehensive or reflect the most recent medical information.

Reviews

• “As a gastroenterologist with over 20 years of practice, Asacol remains a reliable and effective first-line therapy for my UC patients. Its targeted delivery and favorable safety profile make it an excellent choice for both induction and maintenance.” – Dr. E. Lawson, MD
• “After my diagnosis, my doctor started me on Asacol. It took a few weeks, but the bleeding and urgency significantly decreased. I’ve been in remission for over a year now by staying on my maintenance dose. It’s given me my life back.” – Patient, 34
• “The clinical trial data for mesalamine preparations like Asacol is robust and consistently demonstrates efficacy in achieving both clinical and endoscopic endpoints. It is a foundational agent in our UC treatment algorithms.” – Clinical Researcher, Pharma
• “I experienced some initial headaches and gas, but my doctor assured me this was common. The side effects faded after the first couple of weeks, and the trade-off for controlling my flare was absolutely worth it.” – Patient, 41
• “From a pharmacological standpoint, the pH-dependent release mechanism of Asacol is a elegant solution for targeting colonic delivery, though individual patient factors like transit time and gut pH can cause variability in response.” – PharmD Specialist