Medications> Glucose-lowering>

INDICATIONS

• Type 2 diabetes mellitus

MECHANISM

• Competitively and reversibly inhibit the enzymes (alpha glucoside hydrolases) which break down complex sugars in the small intestinal brush border.
• Cause delayed absorption of simple sugars from the gut, thus reducing post prandial hyperglycemia.
• Inhibit lactase only minimally, therefore do not cause lactose intolerance

USUAL ADULT DOSING

• Before alpha glucosidase inhibtor (AGI) initiation, check baseline liver enzymes, then every 3 months for the first year of use, and periodically thereafter.
• AGIs must be always be taken with the first bite of a meal. This applies to the dosing information listed below.
• Acarbose initiation: 25 mg orally once daily; titrate up to 25 mg three times per day.
• Acarbose maintenance: 50-100 mg three times per day; maximum dose 50 mg three times per day (if body weight < 60 kg) or 100 mg three times per day (if body weight > 60 kg).
• Miglitol initiation: 25 mg orally three times per day.
• Miglitol maintenance: 50 mg three times per day (maximum dose 100 mg three times per day).

FORMS

*Prices represent cost per unit specified and are representative of "Average Wholesale Price" (AWP). AWP Prices were obtained and gathered by Lakshmi Vasist Pharm D using the Red Book, manufacturer's information, and the McKesson database.

^Dosage is indicated in mg unless otherwise noted.

DOSING IN SPECIAL POPULATIONS

• Do not use if GFR < 25 mL/min or if serum creatinine > 2 mg/dL

• Acarbose is absolutely contraindicated in cirrhosis of the liver

• FDA Category B

• Thomson Lactation Ratings: infant risk cannot be ruled out

ADVERSE DRUG REACTIONS

• Not for use in renal failure (GFR < 25 mL/min or serum creatinine > 2 mg/dL).
• Contraindicated in GI conditions such as inflammatory bowel disease, intestinal obstruction/ileus, conditions potentially exacerbated by increased intestinal gas, conditions associated with decreased digestion or absorption, or colonic ulcerations.
• If used with an insulin secretagogue (sulfonylureas or meglitinides), can result in hypoglycemia. This hypoglycemia must be corrected with oral glucose (monosaccharide), not with sucrose (table sugar; a disaccharide whose breakdown will be inhibited).
• Acarbose is absolutely contraindicated in cirrhosis of the liver.
• Not for use in diabetic ketoacidosis.

• Many patients (up to 74%) will experience GI disturbances (flatulence, diarrhea, bloating, abdominal pain)

• Miglitol can cause a transient skin rash
• Miglitol can decrease serum iron levels

• Dose-dependent hepatotoxicity. Therefore, check liver enzymes every 3 months for the first year of use, then periodically thereafter.

DRUG INTERACTIONS

• Somatropin may decrease the efficacy of oral antidiabetic agents such as acarbose and miglitol

PHARMACOKINETIC

COMMENTS

• Expected HbA1c reduction is 0.5 to 0.7%
• Weight neutral
• No hypoglycemia when used as monotherapy
• Multiple daily dosing regimen can create compliance issues
• GI disturbances (flatulence, diarrhea, bloating, abdominal pain) are the main reason why these medications have never become popular in the U.S.
• Acarbose may be useful in the prevention of diabetes and cardiovascular complications among individuals with impaired glucose tolerance.

REFERENCES

RELATED MODULES

• Cardiovascular Disease Screening and Management
• Elderly and Diabetes
• Nutrition for Type 2 Diabetes