Acarbose (Glucobay), an alpha-glucosidase inhibitor, is used in the treatment of Type 2 Diabetes Mellitus.

It reduces the gastrointestinal absorption of glucose by inhibiting disaccharidases in the intestinal mucosa.

Thus, it prevents glucose absorption and reduces the post-meal spikes in blood glucose.

Acarbose use is associated with weight loss. The "STOP-NIDDM" Trial demonstrated the efficacy of acarbose in delaying the progression from prediabetes to diabetes.

Acarbose use in Prediabetes:

• Prediabetes and Diabetes are risk factors for cardiovascular diseases.
• Diet, exercise, and lifestyle change are the main methods for lowering diabetes incidence.
• In the two important investigations, the Finnish Diabetes Prevention Study and the US Diabetes Prevention Program (DPP), there was a 58% decrease in the incidence of diabetes (DPS).
• Lifestyle modification and exercise may not maintain long term glycemic control.
• Drugs that are used to reduce the incidence of diabetes include metformin, acarbose, pioglitazone, SGLT2 inhibitors (dapagliflozin, empagliflozin, and canagliflozin).
• Comparing metformin and acarbose, the incidence of diabetes was reduced by 36% with acarbose and 31% with metformin in the STOP-NIDDM trial (The Study to Prevent Non-Insulin Dependent Diabetes Mellitus).

Can Acarbose cause weight loss?

• Acarbose inhibits the absorption of glucose in the intestines. This results in the loss of calories in the stools.
• A study published in the Journal of Diabetes and its complications concluded that acarbose causes weight loss irrespective of glycemic control in diabetic individuals.
• Other studies have also shown that acarbose causes a modest weight loss in diabetic individuals.

Acarbose use in non-diabetic obese individuals:

• Acarbose has also been studied in non-diabetic obese individuals for its effects on body weight.
• It was found that acarbose significantly reduces weight compared to placebo.
• The weight-losing effects are more marked in communities and individuals with a high carbohydrates intake (such as the Persian diet).

Contraindications to Glucobay:

• Intolerance to acarbose and any other ingredients in the formula
  patients with cirrhosis and diabetic ketoacidosis.
• Patients with intestinal obstruction risk factors, such as those with inflammatory bowel disease, colonic ulcers, or partial or total obstruction.
• Patients with long-term intestinal illnesses, such as those that significantly impair digestion or absorption or those whose symptoms could get worse as a result of increasing gas production.

Starting Dose of Glucobay:

• With the first bite of each main meal, take 25 mg three times day.
• In some patients, it may be advisable to take acarbose once daily in the start.

Maintenance dose:

• Until the maximum acceptable dose is reached, it should be modified in accordance with the postprandial blood sugar readings at 4- to 8-week intervals.

Maximum dose of Glucobay:

Patients weighing less than 60 kgs:

• 50 mg 3 times/day

Patients weighing more than 60 kgs:

• 100 mg 3 times/day

Glucobay use in Children:

• The dosage for youngsters up to the age of 17 has not been determined.

Glucobay dose in renal disease:

Cl cr ≥25 mL/minute:

• No dosage adjustment necessary.

Cl cr <25 mL/minute or Serum creatinine greater than 2 mg/dL:

• Use not recommended (not adequately studied).

Glucobay dose in liver disease:

• No dosage adjustment has been provided in the manufacturers labeling.

How and when to take Glucobay?

• It should be taken orally along with each meal's first bolus. 

Pregnancy Risk Factor: B

• Studies on animal reproduction have not shown any adverse events. 
• Acarbose is therefore assigned pregnancy category B. Glucobay was studied to determine if it could be used in the treatment of Gestational Diabetes Mellitus. 
• Unfortunately, there is not much information available about the pregnancy outcomes.
• It shouldn't be used as a first-line diabetic medication during pregnancy due to its insufficient efficacy and data.

Use during lactation

• It's not known if the drug will get into breastmilk.

Acarbose side effects:

• Diarrhea,
• abdominal pain, and
• flatulence
• Liver injury

Rare side effects:

• Edema,
• erythema,
• exanthema,
• hepatitis,
• ileus,
• jaundice,
• liver damage,
• pneumatosis cystoids intestinalis,
• rash,
• thrombocytopenia and
• urticaria.

Acarbose mechanism of action (MOA):

• It competitively inhibits the a-glucosidase and pancreatic amylase present at the intestinal brush border.
• This causes delayed hydrolysis and absorption of complex carbohydrates and disaccharides.
• This causes a dose-dependent decrease in serum insulin levels and peak glucose levels postprandially.

 It also inhibits sucrose-to-glucose and fructose metabolism.

Half-life elimination is about 2 hours.

The time to peak action of the active drug is around 1 hour. 

International Brand Names of Acarbose:

• Glucobay
• Precose

Acarbose brands in Pakistan:

Acabose (Raazee theraputics PVT LTD)

Tablets:50 mg: 30 tablets pack : Rs.120

Tablets:100 mg: 30 tablets pack: Rs.220

Glucobay(Bayer schering pharma)

Tablets: 50 mg (30 tablets pack): Rs.149.44

Tablets:100 mg (30 tablets pack): Rs.281.29

Diabetes treatment - an overview of the Drugs

Insulin types and principles of insulin therapy

Empagliflozin - Treat Diabetes and heart failure