Active Substance: Acarbose.
Overview
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This medicine contains an important and useful components, as it consists of
Acarboseis available in the market in concentration
Acarbose
- **Gastrointestinal Issues**: Acarbose may cause gastrointestinal side effects such as bloating, flatulence, and diarrhea. It should be used with caution in individuals with gastrointestinal disorders like inflammatory bowel disease or intestinal obstruction. - **Renal Impairment**: Caution is required in patients with renal impairment. Acarbose is primarily excreted through the urine, so its use may need to be adjusted in patients with moderate or severe kidney dysfunction. Regular renal function monitoring is recommended. - **Liver Function**: Although rare, liver enzyme elevations have been reported with acarbose use. Liver function should be monitored, particularly in patients who develop symptoms of hepatotoxicity (e.g., jaundice, fatigue). - **Hypoglycemia Risk**: Acarbose can cause mild hypoglycemia when used in combination with other anti-diabetic agents (e.g., sulfonylureas or insulin). In the case of hypoglycemia, only glucose (not sucrose) should be used to treat it, as acarbose inhibits the digestion of sucrose. - **Pregnancy and Breastfeeding**: Acarbose should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. Its safety during breastfeeding has not been well established, so caution is advised. - **Elderly Patients**: Older adults may be more susceptible to the gastrointestinal side effects of acarbose. Dose adjustments may be necessary to minimize discomfort and improve tolerability. - **Allergic Reactions**: While rare, hypersensitivity reactions such as rash or anaphylaxis may occur. Discontinue use and seek medical attention if these reactions develop.
- **Type 2 Diabetes Mellitus**: Acarbose is primarily indicated as an adjunct to diet and exercise in the management of type 2 diabetes. It helps control blood sugar levels by inhibiting the enzyme alpha-glucosidase, which slows the breakdown of carbohydrates in the intestine, thus reducing postprandial blood glucose spikes. - **Monotherapy**: It can be used alone when other medications are not suitable or when blood sugar levels cannot be adequately controlled by diet alone. - **Combination Therapy**: Acarbose is often used in combination with other oral anti-diabetic medications like metformin, sulfonylureas, or insulin to help improve glycemic control in patients who cannot achieve target blood glucose levels with a single drug. - **Off-Label Use**: Acarbose may also be used off-label for managing prediabetes or in patients at high risk for developing type 2 diabetes to delay or prevent the onset of the disease.
- **Hypersensitivity to Acarbose**: Acarbose is contraindicated in individuals with a known hypersensitivity to the drug or any of its components. - **Severe Renal Impairment**: It should not be used in patients with severe renal impairment (creatinine clearance <25 mL/min), as renal dysfunction can increase the risk of adverse effects due to accumulation of the drug. - **Chronic Intestinal Disorders**: Acarbose is contraindicated in patients with chronic intestinal conditions such as inflammatory bowel disease, colonic ulcers, or intestinal obstruction, as it may exacerbate gastrointestinal symptoms. - **Hepatic Impairment**: Acarbose should be avoided in patients with significant liver dysfunction (e.g., cirrhosis or liver failure), as it can increase the risk of liver enzyme abnormalities. - **Pregnancy**: It is contraindicated in pregnancy due to the lack of sufficient safety data. The potential benefit should be weighed against potential risks. - **Breastfeeding**: Since acarbose is not well studied in lactating women, it is contraindicated for use during breastfeeding unless deemed absolutely necessary by a healthcare provider.
- **Common Side Effects**: - Flatulence and bloating, which are the most frequently reported side effects. - Diarrhea and abdominal discomfort. - Nausea and vomiting. - **Serious Side Effects**: - **Liver Damage**: Rare instances of liver enzyme elevations, hepatitis, and hepatotoxicity have been reported, requiring monitoring of liver function. - **Hypoglycemia**: If used with sulfonylureas or insulin, there is a risk of hypoglycemia, especially in combination therapy. - **Lactic Acidosis**: While more common with other anti-diabetic agents, acarbose can contribute to lactic acidosis, particularly in combination with metformin or other lactic acid-producing drugs. - **Allergic Reactions**: Rarely, acarbose can cause allergic reactions such as skin rash, pruritus, or anaphylaxis. - **Acute Intestinal Obstruction**: Although extremely rare, some patients may experience a risk of acute intestinal obstruction, particularly when acarbose is used in patients with pre-existing gastrointestinal conditions. - **Long-term Use**: Prolonged use of acarbose can lead to chronic gastrointestinal issues, including persistent bloating and flatulence, which may affect a patient's quality of life.
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- **Alpha-Glucosidase Inhibition**: Acarbose is an alpha-glucosidase inhibitor that works by blocking the action of enzymes (alpha-glucosidases) in the small intestine, which are responsible for breaking down complex carbohydrates into simple sugars (like glucose). - **Delayed Carbohydrate Absorption**: By inhibiting these enzymes, acarbose delays the absorption of glucose and other carbohydrates from the digestive tract. This reduces the postprandial rise in blood glucose levels, leading to better control of blood sugar. - **No Effect on Insulin Secretion**: Unlike other oral anti-diabetic agents, acarbose does not affect insulin secretion or insulin sensitivity. Instead, it specifically targets the digestive process to improve glucose metabolism. - **Slow Effect on Blood Glucose**: The effect of acarbose is primarily seen in reducing the post-meal spike in blood glucose, making it most effective when used in combination with other agents that control basal glucose levels. - **Minimal Systemic Absorption**: Acarbose is minimally absorbed into the bloodstream, ensuring that its effects are localized in the intestines, which helps reduce the risk of systemic side effects.
- **Other Antidiabetic Medications**: When combined with sulfonylureas or insulin, acarbose can increase the risk of hypoglycemia. In these cases, blood glucose monitoring is essential. - **Metformin**: Acarbose can be used with metformin as part of a combination therapy for diabetes, as they work through different mechanisms. No significant adverse interactions have been reported. - **Digestive Enzyme Supplements**: Digestive enzyme supplements may interfere with the effectiveness of acarbose by breaking down carbohydrates more rapidly, potentially reducing its efficacy. - **Corticosteroids**: Corticosteroids may increase blood glucose levels and reduce the effectiveness of acarbose. Close monitoring of blood glucose levels is advised during corticosteroid therapy. - **Acid-Suppressing Medications**: Proton pump inhibitors (PPIs) or H2 blockers may reduce the absorption of acarbose, leading to a decrease in its effectiveness. - **Antibiotics**: Antibiotics that affect gut flora (e.g., broad-spectrum antibiotics) may reduce the effectiveness of acarbose, as they may alter the carbohydrate digestion process. - **Charcoal and Other Absorbents**: Activated charcoal and similar substances may absorb acarbose, potentially decreasing its therapeutic effect if used together.
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- **Starting Dose**: The usual starting dose of acarbose is 25 mg taken orally with the first bite of each main meal. This can help minimize gastrointestinal side effects. - **Dose Adjustment**: If tolerated, the dose can be gradually increased to 50 mg or 100 mg per meal, depending on the patient’s response and tolerance. - **Maximum Dose**: The maximum recommended dose is 100 mg three times a day (total of 300 mg/day). - **Monitoring**: It is important to monitor blood glucose regularly to ensure adequate glycemic control and adjust the dose as needed. - **Renal Impairment**: In patients with renal impairment (creatinine clearance 25-50 mL/min), the starting dose should be reduced, and doses should not exceed 50 mg per meal. - **With Other Antidiabetics**: When used in combination with other anti-diabetic agents, acarbose may lower postprandial blood glucose levels further, requiring careful monitoring for hypoglycemia.
- **Pediatric Use**: The safety and efficacy of acarbose in children under 18 years of age have not been established. - **Not Recommended for Children**: Acarbose is generally not recommended for pediatric use due to the lack of specific dosing guidelines and limited safety data in children. - **Special Circumstances**: If a healthcare provider prescribes acarbose in children, doses would be based on weight, and close monitoring would be necessary.
- **Mild to Moderate Renal Impairment**: In patients with creatinine clearance between 25-50 mL/min, acarbose can still be used, but the starting dose should be reduced, and the dose should not exceed 50 mg per meal. - **Severe Renal Impairment**: Acarbose is contraindicated in patients with severe renal impairment (creatinine clearance <25 mL/min) due to the risk of accumulation and increased toxicity. - **Dialysis**: The drug is not significantly removed by dialysis, so dialysis patients may still require adjusted doses or alternative treatment options.
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