asacol
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Synonyms
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Asacol, known generically as mesalamine, represents one of the foundational treatments in managing inflammatory bowel disease, specifically ulcerative colitis. It’s a 5-aminosalicylic acid (5-ASA) compound delivered via a pH-dependent, delayed-release coating designed to target the distal ileum and colon, where UC inflammation is typically localized. Unlike systemic corticosteroids, its topical action within the intestinal lumen minimizes systemic absorption and associated side effects, making it a first-line maintenance therapy. The development of this delivery system was a significant advancement over older sulfasalazine, which carried a higher burden of intolerance due to its sulfapyridine moiety.
Asacol: Targeted Mucosal Healing for Ulcerative Colitis - Evidence-Based Review
1. Introduction: What is Asacol? Its Role in Modern Medicine
Asacol is an oral, delayed-release formulation of mesalamine, a well-established anti-inflammatory agent. It belongs to the 5-aminosalicylate drug class and is specifically indicated for the treatment of mildly to moderately active ulcerative colitis and for the maintenance of remission. Its role in modern gastroenterology is pivotal; it serves as a cornerstone therapy due to its favorable safety profile and proven efficacy. For patients and clinicians asking “what is Asacol used for,” the answer centers on its ability to control intestinal inflammation with minimal systemic interference, a significant benefit over older alternatives.
2. Key Components and Bioavailability of Asacol
The core active component is mesalamine (5-aminosalicylic acid or 5-ASA). The critical innovation of Asacol is not the drug itself, but its delivery system. Each tablet is coated with a pH-sensitive acrylic-based resin (Eudragit S). This coating remains intact in the acidic environment of the stomach and proximal small intestine, only dissolving at a pH of 7.0 or higher, which is typically reached in the terminal ileum and colon. This ensures targeted release directly at the site of disease. The bioavailability of the mesalamine from Asacol is primarily local, with only about 20-30% of the dose absorbed systemically and rapidly acetylated to the inactive N-acetyl-5-ASA metabolite, which is then renally excreted. This targeted approach maximizes mucosal exposure while minimizing systemic drug levels.
3. Mechanism of Action of Asacol: Scientific Substantiation
So, how does Asacol work at a molecular level? Its mechanism is multifactorial, acting topically on the inflamed colonic mucosa. Mesalamine is a direct inhibitor of the cyclooxygenase and lipoxygenase pathways, reducing the production of pro-inflammatory prostaglandins and leukotrienes. More significantly, it functions as a potent scavenger of reactive oxygen species, which are elevated in the inflamed gut and contribute to tissue damage. It also inhibits the activation of nuclear factor-kappa B (NF-κB), a master transcription factor that regulates the expression of numerous cytokines like TNF-α, IL-1, and IL-6. Think of it as a local firefighter, dousing the cellular signals that perpetuate the cycle of inflammation, neutrophil chemotaxis, and mucosal injury characteristic of UC.
4. Indications for Use: What is Asacol Effective For?
The primary indications for Asacol are well-defined by robust clinical data.
Asacol for Active Ulcerative Colitis
For patients experiencing a flare of mild to moderate UC, Asacol is effective at inducing clinical and endoscopic remission. Doses typically range from 2.4 grams to 4.8 grams per day, divided.
Asacol for Maintenance of Remission
Once remission is achieved, a lower daily dose (e.g., 1.6 grams to 2.4 grams) is highly effective at preventing relapse. This long-term use is a cornerstone of UC management.
Asacol for Proctosigmoiditis and Left-Sided Colitis
Due to its targeted release profile, Asacol is particularly well-suited for conditions affecting the distal colon. It can be used in conjunction with topical mesalamine enemas for enhanced effect in these specific distributions.
5. Instructions for Use: Dosage and Course of Administration
Dosing is critical and must be individualized. It’s not a “one-size-fits-all” situation.
| Indication | Typical Dosage | Frequency | Administration |
|---|---|---|---|
| Active UC | 2.4 - 4.8 g/day | 2-3 divided doses | With or without food; swallow whole |
| Maintenance of Remission | 1.6 - 2.4 g/day | 2 divided doses | With or without food; swallow whole |
The course of administration is typically long-term for maintenance. For active disease, patients may see symptomatic improvement within a few weeks, but the full course to achieve remission can take up to 8 weeks. Adherence is a massive factor—missing doses is a common reason for treatment failure.
6. Contraindications and Drug Interactions with Asacol
Asacol is contraindicated in patients with a known hypersensitivity to mesalamine, salicylates, or any component of the formulation. It should be used with extreme caution in patients with active peptic ulcer disease or severe renal impairment (creatinine clearance <30 mL/min), as rare cases of interstitial nephritis have been reported. From a drug interaction perspective, it’s relatively clean. However, since it is a salicylate, there is a theoretical potential for increased nephrotoxicity when combined with other nephrotoxic agents like NSAIDs. Concerning pregnancy, mesalamine is generally considered low risk and is often continued, but this requires a careful risk-benefit discussion. The most common side effects are headache, nausea, diarrhea, and abdominal pain, which can sometimes be difficult to distinguish from active disease symptoms.
7. Clinical Studies and Evidence Base for Asacol
The scientific evidence for Asacol is extensive. The ASCEND I, II, and III trials were pivotal in establishing its efficacy for active UC. ASCEND II, for instance, demonstrated that 6-week treatment with Asacol 4.8 g/day resulted in treatment success in 72% of patients with moderate disease, compared to 59% on 2.4 g/day. For maintenance, a meta-analysis published in Clinical Gastroenterology and Hepatology confirmed that mesalamine reduces the relapse rate by approximately 70% compared to placebo. The evidence base is what solidifies its position in guidelines worldwide; it’s not just tradition, it’s data-driven.
8. Comparing Asacol with Similar Products and Choosing a Quality Product
When comparing Asacol to other mesalamines like Lialda (MMX mesalamine) or Pentasa, the key difference lies in the delivery system. Pentasa releases mesalamine throughout the GI tract, which may be preferable for Crohn’s disease, while Asacol’s pH-dependent release is more specific for the colon. Lialda uses a Multi-Matrix System designed for once-daily dosing, which can aid adherence. There’s no definitive “better,” it’s about matching the drug’s release profile to the patient’s disease distribution. When choosing, look for FDA-approved generic versions from reputable manufacturers to ensure consistent coating integrity and bioavailability. The cheap, non-approved generics can be a gamble with inconsistent dissolution.
9. Frequently Asked Questions (FAQ) about Asacol
What is the recommended course of Asacol to achieve results for active UC?
For active disease, a minimum of 3 to 8 weeks at a dose of 2.4g to 4.8g per day is standard. Response should be assessed at 4-6 weeks.
Can Asacol be combined with other UC medications like biologics?
Yes, it is commonly used in combination with therapies like azathioprine or biologics (e.g., anti-TNF agents) as part of a treat-to-target strategy, especially in moderate to severe cases.
Is it safe to take Asacol long-term?
For most patients, yes. The long-term safety profile is excellent with routine monitoring, including periodic renal function tests.
Why are my symptoms not improving on Asacol?
This could be due to several factors: inadequate dosing, non-adherence, more severe disease requiring a different drug class (e.g., steroids, biologics), or an incorrect diagnosis (e.g., Crohn’s disease).
10. Conclusion: Validity of Asacol Use in Clinical Practice
In conclusion, the risk-benefit profile of Asacol firmly supports its validity as a first-line therapy for ulcerative colitis. Its targeted mechanism, strong evidence base for both induction and maintenance of remission, and generally favorable safety profile make it an indispensable tool. For patients with mild to moderate UC, it remains a foundational treatment that effectively controls disease activity and improves quality of life with a low burden of side effects.
I remember when we first started using the newer pH-dependent formulations like Asacol back in the late 90s, there was a lot of skepticism in our department. The old guard was still wedded to sulfasalazine, despite the nausea and headaches. I had this one patient, Sarah, a 28-year-old law student with terrible left-sided colitis. She’d failed sulfa and was miserable on prednisone—moon face, insomnia, the whole bit. We started her on Asacol 2.4g daily, and honestly, the first two weeks were underwhelming. She called the office twice, frustrated. My senior partner at the time, Dr. Evans, was ready to switch her to something else, arguing the delivery system was a gimmick and we should just push the prednisone taper faster. I pushed back, insisted we give it the full 4 weeks. It was a bit of a tense disagreement in the clinic.
But then, around week 3, she reported her bleeding had practically stopped. By her 8-week sigmoidoscopy, the mucosa was nearly normal. It was a turning point for me, seeing that targeted delivery actually work as advertised. We’ve since used it in hundreds of patients. Another case that sticks with me is an elderly gentleman, Mr. Davies, 78, with chronic proctosigmoiditis and stage 3 CKD. We were very cautious, monitored his creatinine monthly. He’s been on a maintenance dose of 1.6g daily for five years now, no relapses, and his renal function has remained perfectly stable. That’s the real-world evidence you don’t always see in the trials—the long-term safety in a vulnerable population. You learn that while the drug is the tool, knowing which patient to use it on, and having the patience to let it work, is the real art. Sarah, by the way, sent a thank you card a year later; she’d graduated and was in remission. Those are the outcomes that validate the clinical guidelines.