Pharm
Alpha-glucosidase Inhibitor
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Alpha-glucosidase Inhibitor
, Acarbose, Precose, Miglitol, Glyset
See Also
Oral Hypoglycemic
Agents
Indications
Type II Diabetes Mellitus
Close to target (
Hemoglobin A1C
<8% as monotherapy)
Contraindications
Creatinine Clearance
<25 ml/min (or
Serum Creatinine
>2.0 mg/dl)
Diabetic Ketoacidosis
(DKA)
Cirrhosis
(Acarbose)
Intestinal disorder
Inflammatory Bowel Disease
Colonic ulceration
Small bowl obstruction history
Partial
Intestinal Obstruction
Mechanism
Structurally similar to
Glucose
Reversible inhibitor of the enzyme alpha glucosidase
Present in brush border of
Small Intestine
Alpha glucosidase catalyzes complex
Carbohydrate
s
Interferes with hydrolysis of
Carbohydrate
s
Complex
Carbohydrate
s
Dietary
Disaccharide
s
Delays absorption of
Glucose
and other
Monosaccharide
s
Decreases postprandial
Hyperglycemia
Benefits rely on food within the
Intestine
at the time of medication dosing
Dosing
Acarbose (Precose)
Start dose: 25 mg orally three times daily at start of meal
Maintenance: 50-100 mg orally three times daily ($45/month)
Miglitol (Glyset)
Start dose: 25 mg orally three times daily at start of meal
Maintenance: 50-100 mg orally three times daily ($52/month)
Pharmacokinetics
Acarbose is not absorbed from
Gastrointestinal Tract
Miglitol is absorbed from
Gastrointestinal Tract
Not metabolized
Excreted in urine
Elimination Half-Life
: 2 hours
Excreted in
Breast Milk
in small amounts
Adverse Effects
Poorly tolerated
Decreased GI effects when taken with a high fiber, starchy diet
Gastrointestinal side effects (unabsorbed
Carbohydrate
)
Abdominal Pain
Abdominal Bloating
Diarrhea
Flatulence
Hepatotoxicity (Acarbose)
Serum
Transaminitis
Hypoglycemia
If used with other
Oral Hypoglycemic
agent or
Insulin
Use oral
Glucose
(not sucrose) to treat
Hypoglycemia
Efficacy
Acarbose associated with cardiovascular benefits
Reduced cardiovascular events
Reduced
Hypertension
risk
Significant weight loss
Chiasson (2003) JAMA 290:486-94 [PubMed]
References
(1999) Med Lett Drugs Ther, 41(1053):49-50 [PubMed]
Chiasson (1994) Ann Intern Med 121:928-35 [PubMed]
Vaughan (2024) Am Fam Physician 109(4): 333-42 [PubMed]
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