Acarboz

Uses

Acarboz is used for an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.

Acarboz is also used to associated treatment for these conditions: Type 2 Diabetes Mellitus

How Acarboz works

Alpha-glucosidase enzymes are located in the brush-border of the intestinal mucosa and serve to metabolize oligo-, tri-, and disaccharides (e.g. sucrose) into smaller monosaccharides (e.g. glucose, fructose) which are more readily absorbed. These work in conjunction with pancreatic alpha-amylase, an enzyme found in the intestinal lumen that hydrolyzes complex starches to oligosaccharides.

Acarboz is a complex oligosaccharide that competitively and reversibly inhibits both pancreatic alpha-amylase and membrane-bound alpha-glucosidases - of the alpha-glucosidases, inhibitory potency appears to follow a rank order of glucoamylase > sucrase > maltase > isomaltase. By preventing the metabolism and subsequent absorption of dietary carbohydrates, acarbose reduces postprandial blood glucose and insulin levels.

Dosage

Acarboz dosage

Since acarbose prevents the digestion of complex carbohydrates, the drug should be taken at the start of main meals (taken with first bite of meal). Moreover, the amount of complex carbohydrates in the meal will determine the effectiveness of acarbose in decreasing postprandial hyperglycemia. Adults may take doses of 25 mg 3 times daily, increasing to 100 mg 3 times a day.

Side Effects

Diarrhea, gas, upset stomach, constipation, or stomach pain may occur in the first few weeks of treatment as your body adjusts to this medication but usually improve with time. Follow your prescribed diet to help lessen these side effects. If any of these effects persist or worsen, tell your doctor or pharmacist promptly.

Toxicity

The symptoms of acarbose overdose are likely to be consistent with its adverse effect profile and may therefore include significant gastrointestinal (GI) symptoms (flatulence, distension, etc), although an overdose on an empty stomach (i.e. when not co-administered with food) is less likely to result in these GI symptoms. In the event of an overdose, patients should be instructed to avoid carbohydrate-containing foods for 4-6 hours following administration as these can precipitate the aforementioned GI symptoms.

Precaution

Patient exposed to stress (e.g. fever, trauma, infection, surgery). Mild to moderate hepatic and renal impairment. Pregnancy and lactation.

Interaction

May enhance effects of other antidiabetics including insulin. Diminished effects with GI adsorbents (e.g. charcoal) and digestive enzyme preparations containing carbohydrate splitting enzymes (e.g. amylase, pancreatin). Neomycin and colestyramine may enhance effects of acarbose. May inhibit absorption of digoxin.

Food Interaction

• Take with food. Each dose should be taken with the first bite of a main meal.

[Moderate] GENERALLY AVOID: Alcohol may cause hypoglycemia or hyperglycemia in patients with diabetes.

Hypoglycemia most frequently occurs during acute consumption of alcohol.

Even modest amounts can lower blood sugar significantly, especially when the alcohol is ingested on an empty stomach or following exercise.

The mechanism involves inhibition of both gluconeogenesis as well as the counter-regulatory response to hypoglycemia.

Episodes of hypoglycemia may last for 8 to 12 hours after ethanol ingestion.

By contrast, chronic alcohol abuse can cause impaired glucose tolerance and hyperglycemia.

Moderate alcohol consumption generally does not affect blood glucose levels in patients with well controlled diabetes.

A disulfiram-like reaction (e.g., flushing, headache, and nausea) to alcohol has been reported frequently with the use of chlorpropamide and very rarely with other sulfonylureas.

MANAGEMENT: Patients with diabetes should avoid consuming alcohol if their blood glucose is not well controlled, or if they have hypertriglyceridemia, neuropathy, or pancreatitis.

Patients with well controlled diabetes should limit their alcohol intake to one drink daily for women and two drinks daily for men (1 drink = 5 oz wine, 12 oz beer, or 1.5 oz distilled spirits) in conjunction with their normal meal plan.

Alcohol should not be consumed on an empty stomach or following exercise.

Acarboz Drug Interaction

Unknown: aspirin, aspirin, rosuvastatin, rosuvastatin, sitagliptin, sitagliptin, insulin glargine, insulin glargine, metoprolol, metoprolol, metoprolol, metoprolol, acetaminophen, acetaminophen, cyanocobalamin, cyanocobalamin, ergocalciferol, ergocalciferol, cholecalciferol, cholecalciferol

Acarboz Disease Interaction

Major: cirrhosis, renal dysfunction, diabetic ketoacidosis, intestinal diseaseModerate: liver disease

Elimination Route

The oral bioavailability of acarbose is extremely minimal, with less than 1-2% of orally administered parent drug reaching the systemic circulation. Despite this, approximately 35% of the total radioactivity from a radiolabeled and orally administered dose of acarbose reaches the systemic circulation, with peak plasma radioactivity occurring 14-24 hours after dosing - this delay is likely reflective of metabolite absorption rather than absorption of the parent drug. As acarbose is intended to work within the gut, its minimal degree of oral bioavailability is therapeutically desirable.

Half Life

In healthy volunteers, the plasma elimination half-life of acarbose is approximately 2 hours.

Elimination Route

Roughly half of an orally administered dose is excreted in the feces within 96 hours of administration. What little drug material is absorbed into the systemic circulation (approximately 34% of an orally administered dose) is excreted primarily by the kidneys, suggesting renal excretion would be a significant route of elimination if the parent drug was more readily absorbed - this is further supported by data in which approximately 89% of an intravenously administered dose of acarbose was excreted in the urine as active drug (in comparison to 7

Pregnancy & Breastfeeding use

Pregnancy category B. Either animal-reproduction studies have not demonstrated a foetal risk but there are no controlled studies in pregnant women or animal-reproduction studies have shown an adverse effect (other than a decrease in fertility) that was not confirmed in controlled studies in women in the 1st trimester (and there is no evidence of a risk in later trimesters).

Contraindication

Patient with inflammatory bowel disease, diabetic ketoacidosis or cirrhosis, colonic ulceration, partial intestinal obstruction or predisposition to this condition, chronic intestinal diseases associated with marked disorders of digestion or absorption and state/s which may deteriorate as a result of increased gas formation in the intestine (e.g. larger hernias). Severe hepatic and renal impairment (CrCl <25 mL/min).

Storage Condition

Store below 25° C. Protect from moisture.

Innovators Monograph

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