Active Substance: Opipramol 2HCl.
Overview
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This medicine contains an important and useful components, as it consists of
Opipramol 2HClis available in the market in concentration
5 Aminosalicylic Acid (Mesalamine)
Mesalamine (5-aminosalicylic acid, or 5-ASA) is primarily used to treat inflammatory bowel diseases, such as ulcerative colitis and Crohn's disease. However, several precautions must be taken into account before its use: - **Pregnancy and breastfeeding**: Mesalamine is classified as a category B drug during pregnancy, indicating that it is generally considered safe, but it should only be used when the potential benefits outweigh the risks. It is excreted in breast milk in small amounts, so breastfeeding mothers should use caution, though it is generally considered safe to use during breastfeeding. - **Renal function**: Mesalamine is known to potentially cause renal toxicity. Patients with pre-existing renal conditions, particularly those with a history of renal disease, should be closely monitored for signs of renal impairment. Kidney function should be assessed before starting treatment and periodically throughout therapy, especially if the patient is on long-term mesalamine therapy. - **Liver function**: Mesalamine may also cause liver enzyme elevations, particularly during prolonged use. Liver function tests should be conducted before starting therapy and periodically monitored during treatment. - **Gastrointestinal issues**: In some cases, mesalamine may exacerbate gastrointestinal symptoms, such as abdominal pain, nausea, or diarrhea. This is particularly concerning in patients with a history of gastrointestinal ulcers or other significant GI disorders. - **Hypersensitivity**: Patients with a known allergy to mesalamine or other aminosalicylates should avoid this medication. Hypersensitivity reactions can include skin rashes, fever, and blood dyscrasias. - **Monitoring parameters**: Regular monitoring of renal and liver function is essential, particularly for patients receiving long-term therapy. Complete blood counts (CBC) should be done periodically to monitor for signs of blood dyscrasias such as leukopenia or thrombocytopenia.
Mesalamine is indicated for the treatment of several inflammatory bowel diseases and other conditions: - **Ulcerative colitis**: Mesalamine is commonly used to treat mild-to-moderate ulcerative colitis by reducing inflammation in the colon and rectum, thereby improving symptoms such as diarrhea, bleeding, and abdominal pain. It is effective in both acute flares and maintenance therapy. - **Crohn's disease**: Although less commonly used for Crohn’s disease, mesalamine can be effective in treating mild-to-moderate cases, particularly when the disease is localized to the colon. - **Off-label uses**: Mesalamine may be used off-label for other inflammatory gastrointestinal conditions, including microscopic colitis or indeterminate colitis. Some studies suggest it may help reduce inflammation in the ileum or other areas affected by chronic inflammation. - **Post-surgical prevention**: Mesalamine is sometimes used to reduce the risk of recurrence of inflammatory bowel disease following surgery, especially in ulcerative colitis patients who have undergone colectomy.
Mesalamine is contraindicated in certain conditions or populations due to the potential for severe reactions or ineffectiveness: - **Hypersensitivity**: Mesalamine is contraindicated in patients who have a known hypersensitivity to it or other aminosalicylates, such as sulfasalazine. Hypersensitivity reactions can include severe skin rashes, anaphylaxis, or blood dyscrasias. - **Renal impairment**: Mesalamine is contraindicated in patients with significant renal impairment (e.g., those with creatinine clearance less than 30 mL/min). It can further compromise kidney function and lead to acute renal failure. - **Liver dysfunction**: Mesalamine should be used with caution or avoided in patients with severe liver dysfunction, as it can lead to liver enzyme elevations or, in rare cases, liver injury. - **Intestinal or gastric obstruction**: Mesalamine is contraindicated in patients with a history of severe intestinal or gastric obstruction, as its use can exacerbate these conditions. - **Pregnancy (third trimester)**: While mesalamine is generally considered safe during pregnancy, it should be avoided in the third trimester unless absolutely necessary, as the effects on fetal development are not fully understood.
Side effects associated with mesalamine therapy can vary in frequency and severity. While many patients tolerate mesalamine well, some may experience mild or more serious reactions: - **Common side effects**: - **Gastrointestinal issues**: Abdominal pain, bloating, nausea, and diarrhea are common, particularly during the initiation of therapy. These symptoms usually improve as the body adjusts. - **Headache**: Mild headaches may occur, especially during the early stages of treatment. - **Rash**: Skin rashes are relatively common but are usually mild and resolve after discontinuation of the drug. - **Serious side effects**: - **Renal toxicity**: Mesalamine can cause acute kidney injury or interstitial nephritis, especially with long-term use. Signs of kidney issues include decreased urine output, fluid retention, or elevated creatinine levels. - **Liver toxicity**: Although rare, mesalamine can cause liver enzyme elevations, jaundice, or hepatitis. Liver function tests should be performed regularly during long-term therapy. - **Blood disorders**: Severe blood dyscrasias, such as leukopenia, thrombocytopenia, or agranulocytosis, can occur. Patients should be monitored for signs of infection, unexplained bruising, or unusual bleeding. - **Hypersensitivity reactions**: Severe allergic reactions, including anaphylaxis, have been reported in some patients. Symptoms include difficulty breathing, swelling, and severe skin rashes. - **Management of side effects**: - Mild gastrointestinal side effects can often be managed by taking mesalamine with food. - Kidney and liver functions should be closely monitored during treatment, especially for patients with pre-existing conditions. - Severe allergic reactions or blood dyscrasias require immediate discontinuation of the drug and medical attention.
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Mesalamine exerts its therapeutic effects by reducing inflammation in the intestines, particularly the colon. It is thought to work through the following mechanisms: - **Inhibition of cyclooxygenase (COX)**: Mesalamine inhibits COX enzymes, which are responsible for producing prostaglandins, compounds that play a key role in the inflammatory process. By reducing prostaglandin production, mesalamine helps to decrease inflammation and associated symptoms in the intestines. - **Modulation of immune responses**: Mesalamine also has immunomodulatory effects, inhibiting the activation of inflammatory cells such as T-lymphocytes and macrophages. This reduces the overall immune response and helps control the chronic inflammation seen in inflammatory bowel diseases. - **Antioxidant effects**: Mesalamine has been shown to possess antioxidant properties, which may contribute to its ability to reduce oxidative stress in the colon, further helping to control inflammation. - **Topical effect**: The drug’s primary effect is local, as it is delivered directly to the affected area of the gastrointestinal tract. This makes mesalamine particularly effective in treating localized inflammation associated with ulcerative colitis and Crohn's disease.
Mesalamine may interact with other drugs and substances, potentially altering its effectiveness or increasing the risk of side effects: - **Azathioprine and mercaptopurine**: These immunosuppressive medications can increase the risk of bone marrow suppression when used with mesalamine. Regular monitoring of blood counts is recommended for patients taking both drugs. - **Other immunosuppressive agents**: Combining mesalamine with other immunosuppressive drugs (e.g., methotrexate, corticosteroids) can increase the risk of infections, liver damage, or bone marrow suppression. Careful monitoring is necessary. - **Warfarin**: Mesalamine may enhance the effects of warfarin, increasing the risk of bleeding. INR levels should be closely monitored in patients receiving both medications. - **Probenecid**: Probenecid may increase mesalamine levels by inhibiting its renal clearance. This can increase the risk of mesalamine-related side effects, particularly renal toxicity. - **Antacids**: Antacids or proton pump inhibitors (PPIs) can alter the absorption of mesalamine, particularly in delayed-release formulations. Mesalamine should be taken on an empty stomach for optimal absorption, and antacids should be avoided immediately before or after administration. - **Alcohol**: Alcohol consumption should be limited during mesalamine therapy, as it can irritate the gastrointestinal tract and potentially exacerbate symptoms of inflammatory bowel diseases.
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The recommended dose of mesalamine varies depending on the specific condition being treated: - **Ulcerative colitis (active disease)**: The typical starting dose is 4.8 g per day, usually divided into two or three doses. Depending on the severity, the dose may be adjusted up to 6 g per day for more severe cases. - **Ulcerative colitis (maintenance therapy)**: A maintenance dose of 2.4 g to 4.8 g per day is commonly used after achieving remission. - **Crohn's disease**: Dosing for Crohn’s disease is similar to that for ulcerative colitis, with a starting dose of 4.8 g per day and a maintenance dose of 2.4 g to 4.8 g per day. - **Other indications**: Dosing may vary depending on the condition being treated, and the medication should always be tailored to the patient's response and tolerance.
- **Ulcerative colitis (pediatric use)**: Mesalamine is sometimes used in children, typically starting at 40-60 mg/kg per day, divided into two or three doses. The dose should not exceed 4.8 g per day. - **Crohn's disease (pediatric use)**: In pediatric patients, the dose is typically 40 mg/kg per day, divided into two or three doses.
In patients with mild-to-moderate renal impairment (e.g., creatinine clearance between 30-60 mL/min), the dose of mesalamine should be reduced or used with caution. For patients with severe renal impairment (creatinine clearance <30 mL/min), mesalamine should generally be avoided, as it may worsen kidney function.
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