Dosing and uses of Precose (acarbose)
Adult dosage forms and strengths
tablet
- 25mg
- 50mg
- 100mg
Type 2 Diabetes Mellitus
Initially 25 mg PO q8hr, at meals (with first bite)
Can increase to 50 or 100 mg PO q8hr at 4- to 8-wk intervals based on 1 hour postprandial glucose or glycosylated hemoglobin levels, and on tolerance
Maximum Dose
<60 kg: 50 mg q8hr
>60 kg: 100 mg q8hr
Other Indications & Uses
Type 2 DM, mono treatment or with sulfonylurea
Pediatric dosage forms and strengths
Safety & efficacy not established
Precose (acarbose) adverse (side) effects
>10%
abdominal pain (19%)
diarrhea (31%)
elevated serum transaminases
flatulence (74%)
Postmarketing Reports
Gastrointestinal: Fulminant hepatitis with fatal outcome, ileus/subileus, jaundice and/or hepatitis and associated liver damage
Hypersensitive skin reactions: rash, erythema, exanthema and urticaria
Edema
Thrombocytopenia
Pneumatosis cystoides intestinalis
Warnings
Contraindications
Documented hypersensitivity to acarbose
Diabetic ketoacidosis, cirrhosis, inflammatory bowel disease, colonic ulceration, partial intestinal obstruction or predisposed to intestinal obstruction, known marked absorptive impairment of GI
Conditions that may deteriorate as result of increased gas formation in GI tract
Cautions
No clinical studies exist establishing conclusive evidence of macrovascular risk reduction with acarbose or any other anti-diabetic drug
Concurrent use with sulfonylureas or insulin may result in hypoglycemia; treat hypoglycemia with oral glucose (dextrose), not sucrose (cane sugar)
Monitoring glycemic control with 1,5-AG assay is not recommended; measurements of 1,5-AG are unreliable in assessing glycemic control in patients taking acarbose; use alternate methods to monitor for glycemic controL
Patients that are exposed to stress such as fever, trauma, infection, or surgery, may result in temporary loss of control of blood glucose; temporary insulin therapy may be necessary
Pregnancy and lactation
Pregnancy category: B
Lactation: not known if crosses into breast milk, avoid using in nursing women
Pregnancy categories
A: Generally acceptable. Controlled studies in pregnant women show no evidence of fetal risk.
B: May be acceptable. Either animal studies show no risk but human studies not available or animal studies showed minor risks and human studies done and showed no risk.
C: Use with caution if benefits outweigh risks. Animal studies show risk and human studies not available or neither animal nor human studies done.
D: Use in LIFE-THREATENING emergencies when no safer drug available. Positive evidence of human fetal risk.
X: Do not use in pregnancy. Risks involved outweigh potential benefits. Safer alternatives exist.
NA: Information not available.
Pharmacology of Precose (acarbose)
Half-Life: 2 hr
Onset: 1 hr
Peak Plasma Time: 1 hr
Bioavailability: <2 %
Metabolism: extensively degraded in the intestine by bacterial and digestive enzymes, glucose units are removed from acarbose molecule
Metabolites: 4-methylpyrogallol derivatives (major inactive mets) and other inactive mets
Excretion
Urine: 34 % as inactive metabolites
Feces: 51% as unabsorbed drug
Mechanism of action
Oral pancreatic alpha-amylase and intestinal brush border alph-glucosidases. This results in delayed hydrolysis of ingested complex carbohydrates and disaccharides and absorption of glucose. Inhibits metabolism of sucrose to glucose and fructose.
