| Medication: Mesalamine | Medication Information and Guidelines |
|---|---|
| Recommended Dose and Dosage Regimen | The recommended dose of mesalamine varies depending on the formulation, severity of the condition, and individual patient response. For the induction of remission in mild to moderate ulcerative colitis, the typical oral dose of mesalamine is 2.4 to 4.8 grams per day, divided into multiple doses. For maintenance of remission, the usual oral dose ranges from 1.2 to 2.4 grams per day, administered once daily or in divided doses. Mesalamine formulations may include delayed-release tablets, extended-release capsules, rectal suppositories, and enemas, each with specific dosing instructions. Follow your healthcare provider’s instructions regarding dosing and administration. |
| Frequency of Administration | The frequency of mesalamine administration depends on the formulation and indication. Oral mesalamine is typically administered once daily or in divided doses, with or without food, as directed by your healthcare provider. Rectal mesalamine formulations (suppositories, enemas) may be used nightly or as directed by a physician for localized treatment of distal ulcerative colitis. Follow the prescribed dosing regimen for optimal therapeutic effects. |
| Route of Administration | Mesalamine is available for oral and rectal administration in various formulations, including tablets, capsules, suppositories, and enemas. Oral mesalamine formulations are swallowed whole with a glass of water, while rectal mesalamine formulations are inserted into the rectum using the provided applicator. The choice of route and formulation depends on the location and severity of inflammation in inflammatory bowel disease (IBD) and the patient’s preference and tolerability. |
| Mechanism of Action (MOA) | Mesalamine is an aminosalicylate anti-inflammatory agent that exerts its pharmacological effects locally in the gastrointestinal tract. Although the exact mechanism of action is not fully elucidated, mesalamine is thought to inhibit the production of inflammatory mediators, including prostaglandins and leukotrienes, and modulate immune responses in the intestinal mucosa. Mesalamine may also scavenge free radicals, stabilize lysosomal membranes, and promote tissue repair and mucosal healing in inflammatory bowel disease (IBD). |
| Pharmacokinetics (PK) | Mesalamine is poorly absorbed after oral administration, with limited systemic bioavailability due to rapid metabolism and excretion in the gastrointestinal tract. Delayed-release and extended-release mesalamine formulations are designed to deliver the active drug to the distal ileum and colon, where it exerts its therapeutic effects locally. Rectal mesalamine formulations provide targeted delivery of the drug to the rectum and distal colon, minimizing systemic absorption and maximizing local concentrations at the site of inflammation. The elimination half-life of mesalamine is relatively short, ranging from 0.5 to 1.5 hours, with rapid clearance from the circulation. Dosage adjustments are generally not required based on renal function, but caution should be exercised in patients with impaired renal or hepatic function. |
| Pharmacodynamics (PD) | Mesalamine exerts its pharmacodynamic effects by inhibiting inflammatory pathways and modulating immune responses in the intestinal mucosa. By reducing the production of pro-inflammatory mediators, such as prostaglandins, leukotrienes, and cytokines, mesalamine helps suppress inflammation, alleviate symptoms, and promote mucosal healing in inflammatory bowel disease (IBD). Mesalamine’s anti-inflammatory properties are predominantly localized to the gastrointestinal tract, where it acts topically on inflamed tissues without significant systemic absorption or adverse effects. |
| Pathophysiology | Mesalamine is indicated for the induction and maintenance of remission in patients with mild to moderate ulcerative colitis, a chronic inflammatory condition characterized by diffuse mucosal inflammation and ulceration in the colon and rectum. Ulcerative colitis is associated with a dysregulated immune response, resulting in the release of pro-inflammatory cytokines, recruitment of inflammatory cells, and disruption of mucosal barrier function, leading to symptoms such as diarrhea, rectal bleeding, abdominal pain, and urgency. Mesalamine therapy aims to reduce inflammation, control symptoms, and prevent disease flares in affected individuals. |
| Primary Indications | Induction and maintenance of remission in mild to moderate ulcerative colitis. |
| Contraindications | Contraindications to mesalamine use include hypersensitivity to mesalamine or any component of the formulation, salicylate allergy, and severe renal impairment (creatinine clearance < 30 mL/min) or renal failure. Use caution when prescribing mesalamine in patients with hepatic impairment, coagulation disorders, or a history of gastrointestinal strictures, as they may be at increased risk of adverse effects or complications. Mesalamine is not recommended for use during pregnancy or lactation unless the potential benefits outweigh the risks to the fetus or infant. |
| Purpose of Taking Medication | The purpose of mesalamine therapy is to induce and maintain remission in patients with mild to moderate ulcerative colitis by reducing inflammation, controlling symptoms, and promoting mucosal healing in the colon and rectum. Mesalamine is used as a first-line treatment option to manage acute flares of ulcerative colitis and prevent disease recurrence in affected individuals, either as monotherapy or in combination with other agents such as corticosteroids or immunomodulators. |
| Usage Instructions | Take mesalamine orally as directed by your healthcare provider, usually once daily or in divided doses, with or without food. Swallow the tablets or capsules whole with a glass of water; do not crush, chew, or break them unless instructed otherwise. If using rectal mesalamine formulations (suppositories, enemas), follow the package instructions for proper administration and use as directed by a physician. |
| Precautions and Care | Patients taking mesalamine should be monitored for signs of gastrointestinal intolerance, exacerbation of symptoms, and adverse effects throughout the course of treatment. Use caution when prescribing mesalamine in elderly patients or those with impaired renal function, as they may be at increased risk of adverse reactions or complications. Discontinue mesalamine and seek medical attention if signs of hypersensitivity, worsening colitis, or severe adverse effects occur during therapy. |
| Dietary Considerations | There are no specific dietary restrictions associated with mesalamine use. Maintain a balanced diet and adequate hydration to support overall health and well-being. Avoid excessive consumption of alcohol or other substances that may exacerbate gastrointestinal symptoms or interact with mesalamine. |
| Missed Dose | If a dose of mesalamine is missed, take it as soon as remembered, unless it is almost time for the next scheduled dose. Do not double the dose to make up for a missed one. Resume the regular dosing schedule and continue taking mesalamine as prescribed by your healthcare provider. |
| Possible Side Effects | Common side effects of mesalamine may include headache, nausea, abdominal pain, diarrhea, and flatulence. Less common side effects may include rash, pruritus, dyspepsia, and elevated liver enzymes. Rare but serious adverse effects may include pancreatitis, interstitial nephritis, and hypersensitivity reactions. Contact your healthcare provider if you experience severe or persistent side effects while taking mesalamine. |
| Storage and Disposal | Store mesalamine tablets and capsules at room temperature away from moisture, heat, and light. Keep the medication out of reach of children and pets. Unused or expired medication should be disposed of properly according to local regulations or guidelines for pharmaceutical waste disposal. |
| Overdose or Emergency | In case of mesalamine overdose or emergency, seek immediate medical attention or contact a poison control center. Overdose may lead to excessive gastrointestinal symptoms such as nausea, vomiting, diarrhea, and abdominal pain. Treatment of mesalamine overdose is supportive and symptomatic, with monitoring of fluid and electrolyte balance as needed. |
| Monitoring and Laboratory Tests | Patients receiving mesalamine therapy require regular monitoring of clinical symptoms, disease activity, and adverse effects throughout the course of treatment. Monitor for changes in bowel habits, abdominal pain, rectal bleeding, and other symptoms of ulcerative colitis, as well as signs of medication intolerance or toxicity. Additional monitoring may include renal function tests, liver function tests, and complete blood counts as clinically indicated. |
Important Note: Always consult with a healthcare professional for personalized medical advice and guidance regarding the use of given drug, especially regarding dosing, administration, and potential side effects. Your healthcare provider can provide tailored recommendations based on your individual medical history, current medications, and specific treatment needs. Never self-adjust your given drug regimen or discontinue treatment without first consulting your healthcare provider. If you have any questions or concerns about given drug or its use, talk to your doctor or pharmacist for further information and assistance.