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Acarbose (Glucobay) - Uses, Dosage, Side effects, MOA

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.