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acarbose (Precose)

Tradename: Precose. Indications: 1) type 2 diabetes with poor glycemic control (HgbA1c > 8.5%) 2) especially for use in type II diabetics with post-prandial hyperglycemia 3) may be useful as monotherapy 4) useful as adjunctive agent to sulfonylurea 5) may be useful in patients who fail sulfonylurea therapy & in whom metformin is contraindicated Contraindications: 1) diabetic ketoacidosis (DKA) 2) hepatic cirrhosis 3) inflammatory bowel disease 4) colonic ulceration 5) partial intestinal obstruction 6) chronic intestinal disease associated with marked disorder of digestion or absorption 7) a condition that deteriorate as a result of increased gas formation within the intestine Cautions: -> avoid using in patients with serum creatinine > 2.0 mg/dL Dosage: 1) start: 25 mg PO TID (25 mg QD [4]) 2) max: 100 mg PO TID (> 60 kg); 50 mg TID (< 60 kg) 3) with first bite 4) discontinue if not effective at max dose for 3 months Tabs: 50 & 100 mg. Pharmacokinetics: 1) not absorbed 2) may decrease fasting blood sugar by 20 mg/dL 3) may decrease 2 hours post-prandial blood sugar by 40 mg/dL 4) may decrease HgbA1c by 0.8% or more Monitor: 1) post-prandial glucose 2) hemoglobin A1c (HgbA1c) 3) serum transaminases every 3 months for 1st year, then periodically thereafter [7] Adverse effects: 1) GI effects (30-60%) related to undigested sugars reaching the colon - does NOT interfere with lactase a) flatulence b) bloating & diarrhea c) reduce intake of carbohydrate to minimize GI side effects 2) common (> 10%) a) may elevate liver enzymes at highest doses b) abdominal pain 3) uncommon (< 1%) - sleepiness, weakness, headache, vertigo, erythema, urticaria, severe gastrointestinal distress Give glucose rather than sucrose, fructose etc. for hypoglycemia Drug interactions: - additive effects with sulfonylureas on plasma glucose Mechanism of action: 1) carbohydrate analog 2) inhibits alpha glucosidase 3) slows digestion of complex carbohydrates 4) major effect is on post-prandial hyperglycemia

Interactions

drug interactions drug adverse effects of hypoglycemic agents

General

alpha glucosidase inhibitor

Properties

INHIBITS: maltase MISC-INFO: elimination route FECES pregnancy-category B safety in lactation -

Database Correlations

PUBCHEM correlations

References

  1. Bayer Corporation
  2. Kaiser Permanente Northern California Regional Drug Formulary, 1998
  3. Prescriber's Letter 9(8):45 2002
  4. Prescriber's Letter 10(9):51 2003
  5. Caiasson J-L et al, JAMA 390:486, 2003
  6. Department of Veterans Affairs, VA National Formulary - non formulary drug request
  7. Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Detail-Document#: 260704 (subscription needed) http://www.prescribersletter.com