Acarbose
Indications
Acarbose is indicated as an adjunct to diet and exercise to improve glycemic control in adults with type 2 diabetes mellitus.
Pharmacology
In contrast to sulfonylureas, Acarbose does
not enhance insulin secretion. The antihyperglycemic action of acarbose
results from a competitive, reversible inhibition of pancreatic
alpha-amylase and membrane-bound intestinal alpha-glucoside hydrolase
enzymes. Pancreatic alpha-amylase hydrolyzes complex starches to
oligosaccharides in the lumen of the small intestine, while the
membrane-bound intestinal alpha-glucosidases hydrolyze oligosaccharides,
trisaccharides, and disaccharides to glucose and other monosaccharides
in the brush border of the small intestine. In diabetic patients, this
enzyme inhibition results in a delayed glucose absorption and a lowering
of postprandial hyperglycemia. Because its mechanism of action is
different, the effect of Acarbose to enhance glycemic control is
additive to that of sulfonylureas, insulin or metformin when used in
combination. In addition, Acarbose diminishes the insulinotropic and
weight-increasing effects of sulfonylureas. Acarbose has no inhibitory
activity against lactase and consequently would not be expected to
induce lactose intolerance.
Dosage & Administration
The recommended starting dosage of
Acarbose is 25 mg given orally three times daily at the start (with the
first bite) of each main meal. However, some patients may benefit from
more gradual dose titration to minimize gastrointestinal side effects.
This may be achieved by initiating treatment at 25 mg once per day and
subsequently increasing the frequency of administration to achieve 25 mg
t.i.d. Maintenance Dosage Once a 25 mg t.i.d. dosage regimen is
reached, dosage of Acarbose should be adjusted at 4–8 week intervals
based on one-hour postprandial glucose or glycosylated hemoglobin
levels, and on tolerance. The dosage can be increased from 25 mg t.i.d.
to 50 mg t.i.d. Some patients may benefit from further increasing the
dosage to 100 mg t.i.d. The maintenance dose ranges from 50 mg t.i.d. to
100 mg t.i.d.
Interaction
Certain drugs tend to produce hyperglycemia
and may lead to loss of blood glucose control. These drugs include the
thiazides and other diuretics, corticosteroids, phenothiazines, thyroid
products, estrogens, oral contraceptives, phenytoin, nicotinic acid,
sympathomimetics, calcium channel-blocking drugs, and isoniazid. When
such drugs are administered to a patient receiving Acarbose, the patient
should be closely observed for loss of blood glucose control. When such
drugs are withdrawn from patients receiving Acarbose in combination
with sulfonylureas or insulin, patients should be observed closely for
any evidence of hypoglycemia.
Patients Receiving Sulfonylureas or Insulin: Sulfonylurea agents or insulin may cause hypoglycemia. Acarbose given in combination with a sulfonylurea or insulin may cause a further lowering of blood glucose and may increase the potential for hypoglycemia. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made. Very rarely, individual cases of hypoglycemic shock have been reported in patients receiving Acarbose therapy in combination with sulfonylureas and/or insulin.
Patients Receiving Sulfonylureas or Insulin: Sulfonylurea agents or insulin may cause hypoglycemia. Acarbose given in combination with a sulfonylurea or insulin may cause a further lowering of blood glucose and may increase the potential for hypoglycemia. If hypoglycemia occurs, appropriate adjustments in the dosage of these agents should be made. Very rarely, individual cases of hypoglycemic shock have been reported in patients receiving Acarbose therapy in combination with sulfonylureas and/or insulin.
Contraindications
Acarbose is contraindicated in patients
with known hypersensitivity to the drug. Precose is contraindicated in
patients with diabetic ketoacidosis or cirrhosis. Acarbose is also
contraindicated in patients with inflammatory bowel disease, colonic
ulceration, partial intestinal obstruction or in patients predisposed to
intestinal obstruction. In addition, Acarbose is contraindicated in
patients who have chronic intestinal diseases associated with marked
disorders of digestion or absorption and in patients who have conditions
that may deteriorate as a result of increased gas formation in the
intestine.
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.
Pregnancy & Lactation
Pregnancy Category B. The safety of
Acarbose in pregnant women has not been established. A small amount of
radioactivity has been found in the milk of lactating rats after
administration of radiolabeled acarbose. It is not known whether this
drug is excreted in human milk. Because many drugs are excreted in human
milk, Acarbose should not be administered to a nursing woman.
Precautions & Warnings
Because of its mechanism of action,
Acarbose when administered alone should not cause hypoglycemia in the
fasted or postprandial state. Sulfonylurea agents or insulin may cause
hypoglycemia. Because Acarbose given in combination with a sulfonylurea
or insulin will cause a further lowering of blood glucose, it may
increase the potential for hypoglycemia. Hypoglycemia does not occur in
patients receiving metformin alone under usual circumstances of use, and
no increased incidence of hypoglycemia was observed in patients when
Acarbose was added to metformin therapy.
Oral glucose (dextrose), whose absorption is not inhibited by Acarbose, should be used instead of sucrose (cane sugar) in the treatment of mild to moderate hypoglycemia. Sucrose, whose hydrolysis to glucose and fructose is inhibited by Acarbose, is unsuitable for the rapid correction of hypoglycemia. Severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Oral glucose (dextrose), whose absorption is not inhibited by Acarbose, should be used instead of sucrose (cane sugar) in the treatment of mild to moderate hypoglycemia. Sucrose, whose hydrolysis to glucose and fructose is inhibited by Acarbose, is unsuitable for the rapid correction of hypoglycemia. Severe hypoglycemia may require the use of either intravenous glucose infusion or glucagon injection.
Use in Special Populations
Pediatric Use: safety and effectiveness of Acarbose in pediatric patients have not been established.
Geriatric Use: of the total number of subjects in clinical studies of Acarbose in the United States, 27% were 65 and over, while 4% were 75 and over. No overall differences in safety and effectiveness were observed between these subjects and younger subjects.
Geriatric Use: of the total number of subjects in clinical studies of Acarbose in the United States, 27% were 65 and over, while 4% were 75 and over. No overall differences in safety and effectiveness were observed between these subjects and younger subjects.
Overdose Effects
Unlike sulfonylureas or insulin, an
overdose of Acarbose will not result in hypoglycemia. An overdose may
result in transient increases in flatulence, diarrhea, and abdominal
discomfort which shortly subside. In cases of overdosage the patient
should not be given drinks or meals containing carbohydrates
(polysaccharides, oligosaccharides and disaccharides) for the next 4–6
hours.
Therapeutic Class
Alpha-Glucosidase inhibitor
Storage Conditions
Store below 25° C. Protect from moisture.
Showing 1 to 4 of 4 (1 Pages)