Acarbose

Acarbose is indicated for:

• Type 2 Diabetes Mellitus (Non-Insulin Dependent Diabetes Mellitus)
  As an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
  It may be used:
• As monotherapy in patients inadequately controlled by diet and exercise alone.
• In combination with other oral antidiabetic agents (such as metformin, sulfonylureas) or insulin, particularly in cases where control of postprandial (after-meal) blood glucose levels is required.

• Initial Dose:
• 25 mg orally, three times daily, taken with the first bite of each main meal.
• Titration:
• The dose may be gradually increased based on tolerance and blood glucose response.
• Typical maintenance dose ranges from 50 mg to 100 mg three times daily.
• Maximum Dose (based on body weight):
• Patients <60 kg: 50 mg three times daily
• Patients ≥60 kg: 100 mg three times daily
• Administration:
• Must be taken with the first bite of food to inhibit carbohydrate absorption effectively.
• If a dose is missed, skip it and take the next dose with the next meal—do not double the dose.
• Dietary Compliance:
• Efficacy depends on adherence to diabetic diet; improper diet may reduce effectiveness and increase GI side effects.

Acarbose is an alpha-glucosidase inhibitor that works in the small intestine to delay the digestion and absorption of complex carbohydrates. It inhibits enzymes such as alpha-glucosidase and pancreatic alpha-amylase, which are responsible for breaking down starches and disaccharides into glucose. By slowing carbohydrate breakdown, Acarbose reduces postprandial (after-meal) blood glucose spikes without causing insulin release or hypoglycemia when used alone.

• Absorption:
  Acarbose is minimally absorbed from the gastrointestinal tract in its active form. A small portion is absorbed as inactive metabolites after bacterial fermentation in the colon.
• Distribution:
  Due to its poor systemic absorption, plasma levels are typically very low or undetectable after oral administration.
• Metabolism:
  Acarbose is extensively metabolized by intestinal bacteria. Approximately 34% of the absorbed portion is metabolized systemically.
• Elimination:
  Unabsorbed drug is excreted in feces. The absorbed fraction is eliminated primarily via the kidneys.
• Half-life:
  The elimination half-life of the absorbed, systemically active component is approximately 2 hours.

Acarbose can interact with other medications that affect blood sugar levels. When taken with insulin or other antidiabetic drugs like sulfonylureas, it may increase the risk of hypoglycemia, so blood sugar levels should be monitored closely. Digestive enzyme products such as amylase or pancreatin can reduce the effectiveness of Acarbose and should be avoided. Similarly, intestinal adsorbents like activated charcoal and certain antacids may interfere with Acarbose’s action. Other drugs such as diuretics, corticosteroids, thyroid hormones, and estrogens may raise blood sugar levels, potentially reducing Acarbose's benefit. In all cases, adjustments to therapy and regular glucose monitoring may be necessary.

Acarbose commonly causes gastrointestinal side effects due to its action in the gut. The most frequent side effects include flatulence, abdominal discomfort, diarrhea, and bloating, especially during the initial weeks of therapy. These symptoms are usually mild and may lessen over time or with dietary adjustments. Less commonly, it can cause elevated liver enzymes, particularly at higher doses or with prolonged use, so liver function should be monitored periodically. Rare but serious side effects include intestinal obstruction, ileus, or hypoglycemia, especially when used with other antidiabetic medications. Most side effects are manageable and improve with continued use or dose adjustments.

Acarbose is contraindicated in patients with hypersensitivity to acarbose or any of its components. It should not be used in individuals with inflammatory bowel disease, colonic ulceration, partial intestinal obstruction, or patients at risk of intestinal obstruction. It is also contraindicated in patients with chronic intestinal diseases associated with marked digestion or absorption disorders, as these conditions may be worsened by acarbose. Additionally, it should not be used in patients with cirrhosis or severe renal impairment (creatinine clearance <25 mL/min or serum creatinine >2 mg/dL).

Acarbose is classified as Pregnancy Category B, meaning animal studies have not shown harm to the fetus, but adequate studies in pregnant women are lacking. It should be used during pregnancy only if clearly needed, and under medical supervision. There is no adequate data on the excretion of acarbose into human breast milk; however, studies in animals have shown low levels in milk. Caution is advised if used during breastfeeding, and infants should be monitored for gastrointestinal symptoms. If possible, alternative treatments with more established safety profiles in pregnancy and lactation may be preferred.

Alpha-Glucosidase Inhibitors.

Store Acarbose at room temperature between 15°C to 25°C (59°F to 77°F), in a tightly closed container, away from moisture, heat, and light. Keep out of reach of children and do not store in the bathroom or near sinks.