Acarbose

Pharmacokinetics

 

Given orally less than 2% is
absorbed as the oral drug. It is metabolized in the GI tract primarily
by intestinal bacteria and to a lesser degree by digestive enzymes.
Urine contains 2% drug and its metabolites. As a result, accumulation of
the drug does not occur when given thrice daily.

 

Indication
and Dosage



First line therapy in NIDDM
inadequately controlled by diet; adjunct to existing conventional oral
hypoglycaemic agents where hypoglycaemic control is inadequate.

Dosage: 50mg initially increased to 50mg
thrice daily; if required may be increased after 6-8 weeks to 100mg
thrice daily. Max 200mg thrice daily.

 

An
oligosaccharide obtained from a fermentation process using the
microorganism Actinoplans utahensis. Causes a competitive, reversible
inhibition of pancreatic alpha-amylase and membrane-bound intestinal
alpha-glucosidase hydrolase enzymes. This causes delayed glucose
absorption resulting in a smaller increase in blood glucose following
meals. Glycosylated hemoglobin levels are decreased in those with
non-insulin-dependent diabetes mellitus. Because the mechanism of action
is different from sulfonylureas (i.e., enhance insulin secretion),
acarbose is additive to the effect of sulfonylureas. Approximately 65%
of an oral dose of acarbose remains in the GI tract, which is the site
of action. Metabolized in the GI tract by both intestinal bacteria and
intestinal enzymes. The acarbose and metabolites that are absorbed are
excreted in the urine.

Charcoal /
Effect of acarbose

Digestive enzymes /
Effect of acarbose

Digoxin / Serum digoxin
levels

Insulin /
Hypoglycemia which may cause severe hypoglycemia

Sulfonylureas /
Hypoglycemia which may cause severe hypoglycemia

 

Adverse
Effect & Precautions

 

Flatulence, soft stools,
diarrhea, abdominal distention and pain, rarely abnormal liver function
tests and skin reaction.

Precaution: Monitor hepatic function tests
specially with higher doses. May enhance hyprglycaemic effects of
sulphonylureas (if it occurs give glucose and not sucrose).

Pregnancy: Contraindicated

Breast Feeding: Contraindicated.

Man: May be used.