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Overview

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This medicine contains an important and useful components, as it consists of
Ornithine aspartateis available in the market in concentration

Name

Acarbose

Precaution

Acarbose is an oral antihyperglycemic medication used to manage type 2 diabetes. It works by inhibiting enzymes involved in the digestion of carbohydrates, thus slowing the absorption of glucose and lowering postprandial blood sugar levels. Several precautions are important to consider before starting acarbose therapy: - **Gastrointestinal (GI) symptoms**: Acarbose frequently causes GI side effects, including flatulence, diarrhea, and abdominal pain, particularly during the initial stages of treatment. These effects are related to its mechanism of action, which alters carbohydrate metabolism in the intestines. To minimize these effects, patients should start at a low dose and gradually increase it. If severe gastrointestinal symptoms occur, dose reduction or discontinuation may be necessary. - **Renal impairment**: Acarbose is contraindicated in patients with severe renal impairment (creatinine clearance <25 mL/min). For those with mild to moderate renal impairment, dose adjustments may be necessary, and close monitoring of kidney function is recommended during treatment. - **Hepatic impairment**: Acarbose should be used with caution in patients with liver disease, particularly if there is a history of liver dysfunction, as it can worsen hepatic conditions. Liver function tests should be monitored regularly. - **Pregnancy and breastfeeding**: Acarbose is classified as a Category B drug during pregnancy, indicating that animal studies have not demonstrated a risk to the fetus, but adequate human studies are lacking. It should only be used during pregnancy if clearly needed. Acarbose is excreted in breast milk, so its use while breastfeeding is not recommended unless the benefits outweigh the potential risks. - **Hypoglycemia**: Although acarbose itself does not directly cause hypoglycemia, it can contribute to low blood sugar when used in combination with other antidiabetic agents like sulfonylureas or insulin. In the event of hypoglycemia, it is important to treat the condition with glucose (not sucrose), as acarbose delays the absorption of sucrose. - **Drug interactions**: Acarbose can interact with other medications, including digestive enzyme supplements (which may reduce its effectiveness), and oral contraceptives (which may be less effective).

Indication

Acarbose is primarily used to manage **type 2 diabetes mellitus**, especially in patients whose blood sugar is inadequately controlled by diet and exercise alone. It is used to lower postprandial blood glucose levels by inhibiting the breakdown of carbohydrates in the intestine, reducing the amount of glucose absorbed into the bloodstream after meals. The primary indications for acarbose are: - **Monotherapy**: It can be used alone in patients with type 2 diabetes who are not achieving adequate glycemic control with diet and exercise. - **Combination therapy**: Acarbose is often used in combination with other antidiabetic drugs, such as metformin or sulfonylureas, when blood sugar control is suboptimal with monotherapy. - **Off-label uses**: Acarbose has occasionally been used for treating metabolic syndrome, as well as preventing the development of diabetes in individuals at high risk (pre-diabetic patients). However, its use in these settings is less common and less well-established in clinical guidelines.

Contra indication

There are several contraindications to acarbose therapy, including: - **Severe renal impairment**: Acarbose is contraindicated in patients with severe renal impairment (creatinine clearance <25 mL/min) because the drug is primarily excreted through the kidneys, and impaired renal function increases the risk of drug accumulation and potential toxicity. - **Severe liver disease**: Patients with active liver disease or cirrhosis should not use acarbose due to the increased risk of liver dysfunction, as the drug may worsen hepatic conditions. - **Intestinal disorders**: Acarbose is contraindicated in patients with chronic intestinal disorders such as inflammatory bowel disease (IBD), colonic ulceration, or partial intestinal obstruction. The drug’s action on the gut can exacerbate these conditions and worsen symptoms like bloating, cramping, and diarrhea. - **Hypersensitivity**: Acarbose should not be used in patients who have a known hypersensitivity to the drug or any of its components. - **Pregnancy**: Acarbose is not recommended for use during pregnancy, as there are limited studies on its safety in pregnant women. If treatment is necessary, it should only be prescribed if the benefits clearly outweigh the potential risks.

Side Effect

Common and serious side effects of acarbose are primarily gastrointestinal, given the drug's mechanism of action. These side effects are typically dose-dependent and can improve over time as the body adjusts: - **Common side effects**: - **Flatulence**: The most frequent side effect, occurring in a significant number of patients. It results from the fermentation of undigested carbohydrates in the colon. - **Diarrhea**: Some patients experience diarrhea, especially when acarbose is first introduced. This can be managed by starting with a low dose and gradually increasing it. - **Abdominal pain**: Bloating and discomfort are commonly reported, especially with higher doses of the medication. - **Nausea and indigestion**: These can occur, especially when the medication is taken with large amounts of carbohydrate-containing meals. - **Serious side effects**: - **Liver dysfunction**: While rare, acarbose can lead to elevated liver enzymes and potential liver toxicity. Regular monitoring of liver function is advised during long-term use. - **Hypoglycemia**: Although acarbose does not directly cause hypoglycemia, it can contribute to low blood sugar when used in combination with other hypoglycemic agents, especially sulfonylureas or insulin. If hypoglycemia occurs, it must be treated with glucose, not sucrose, as acarbose inhibits the absorption of sucrose. - **Management**: Gastrointestinal side effects may be minimized by starting with a low dose and gradually increasing it. If severe GI symptoms persist, dose reduction or discontinuation may be necessary. Regular liver function tests should be performed, especially for patients on long-term therapy.

Pregnancy Category ID

2

Mode of Action

Acarbose works by inhibiting the enzymes responsible for breaking down carbohydrates in the small intestine, particularly **alpha-glucosidase**. This enzyme normally breaks down complex carbohydrates into simple sugars, which are then absorbed into the bloodstream. By inhibiting this enzyme, acarbose reduces the amount of glucose that is absorbed after meals, leading to a decrease in postprandial blood sugar levels. - **Pharmacodynamics**: Acarbose does not directly affect insulin secretion or sensitivity, but by slowing the absorption of glucose, it helps maintain more stable blood sugar levels throughout the day. This reduces the peak blood glucose levels following meals, which is particularly beneficial for people with type 2 diabetes who struggle to control postprandial hyperglycemia. - **Pharmacokinetics**: Acarbose is not absorbed significantly into the bloodstream; it acts locally in the gut. After oral administration, it remains in the gastrointestinal tract where it exerts its effect on carbohydrate digestion. Because it is minimally absorbed, acarbose generally does not cause systemic side effects but may still have local GI side effects.

Interaction

Acarbose interacts with several medications, and these interactions can affect its efficacy or safety: - **Oral hypoglycemic agents**: When used with sulfonylureas or insulin, acarbose may increase the risk of hypoglycemia due to the additive effects on lowering blood sugar. If hypoglycemia occurs, glucose (not sucrose) should be administered for treatment, as acarbose inhibits the absorption of sucrose. - **Digestive enzyme supplements**: Medications such as amylase and pancreatin can reduce the effectiveness of acarbose by assisting in the digestion of carbohydrates, thus counteracting its therapeutic effects. Co-administration should be avoided or carefully monitored. - **Metformin**: When used together with metformin, acarbose can provide complementary blood glucose control, as metformin works on hepatic glucose production and acarbose inhibits carbohydrate absorption. This combination can help improve glycemic control in patients who do not respond to monotherapy. - **Cimetidine**: Cimetidine, a drug used for acid reflux, may inhibit the absorption of acarbose slightly, though this interaction is generally not considered significant. However, monitoring is advised if used concurrently. - **Digoxin**: There is some evidence suggesting that acarbose may increase the absorption of digoxin, a drug used for heart failure and arrhythmias, though this interaction is not well-documented. Monitoring of digoxin levels is recommended when both drugs are used together. - **Other antidiabetic agents**: Acarbose may interact with other antidiabetic drugs, including thiazolidinediones, and may enhance the effects of these drugs. Careful monitoring of blood glucose levels is recommended when these medications are used in combination.

Pregnancy Category Note

Information not available

Adult Dose

The recommended starting dose for adults is typically **25 mg** three times daily, taken with the first bite of each meal. The dose can be gradually increased depending on tolerance and blood glucose levels, with a maximum recommended dose of **100 mg** three times daily. - **Adjustments**: If gastrointestinal side effects occur, starting with a lower dose and gradually increasing it can help improve tolerance. For patients with renal or hepatic impairment, dose adjustments may be necessary.

Child Dose

Acarbose is generally not recommended for children under 18 years of age due to the lack of sufficient safety and efficacy data. If used off-label, pediatric doses would typically be lower than adult doses, but careful monitoring for side effects, especially gastrointestinal issues, would be necessary. Pediatric use should be under close medical supervision.

Renal Dose

In patients with renal impairment, the dose of acarbose should be reduced or adjusted based on the severity of kidney dysfunction: - **Mild to moderate renal impairment (creatinine clearance ≥25 mL/min)**: No dose adjustment is necessary, but regular monitoring is recommended. - **Severe renal impairment (creatinine clearance <25 mL/min)**: Acarbose is contraindicated in severe renal impairment, and an alternative treatment option should be considered.

Administration

Information not available