acarbose (Precose)
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Introduction
Tradename: Precose.
Indications
- type 2 diabetes with poor glycemic control (HgbA1c > 8.5%)
- especially for use in type II diabetics with post-prandial hyperglycemia
- may be useful as monotherapy
- useful as adjunctive agent to sulfonylurea
- may be useful in patients who fail sulfonylurea therapy & in whom metformin is contraindicated
Contraindications
- diabetic ketoacidosis (DKA)
- hepatic cirrhosis
- inflammatory bowel disease
- colonic ulceration
- partial intestinal obstruction
- chronic intestinal disease associated with marked disorder of digestion or absorption
- 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
- start: 25 mg PO TID (25 mg QD[4])
- max: 100 mg PO TID (> 60 kg); 50 mg TID (< 60 kg)
- with first bite
- discontinue if not effective at max dose for 3 months
Tabs: 50 & 100 mg.
Pharmacokinetics
- not absorbed
- may decrease fasting blood sugar by 20 mg/dL
- may decrease 2 hours post-prandial blood sugar by 40 mg/dL
- may decrease HgbA1c by 0.8% or more
elimination via feces
Monitor
- post-prandial glucose
- hemoglobin A1c (HgbA1c)
- serum transaminases every 3 months for 1st year, then periodically thereafter[7]
Adverse effects
- GI effects (30-60%) related to undigested sugars reaching the colon - does NOT interfere with lactase
- flatulence
- bloating & diarrhea
- reduce intake of carbohydrate to minimize GI side effects
- common (> 10%)
- may elevate liver enzymes at highest doses
- abdominal pain
- 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
- carbohydrate analog
- inhibits alpha glucosidase
- slows digestion of complex carbohydrates
- major effect is on post-prandial hyperglycemia
More general terms
References
- ↑ Bayer Corporation
- ↑ Kaiser Permanente Northern California Regional Drug Formulary, 1998
- ↑ Prescriber's Letter 9(8):45 2002
- ↑ 4.0 4.1 Prescriber's Letter 10(9):51 2003
- ↑ Caiasson J-L et al, JAMA 390:486, 2003
- ↑ Department of Veterans Affairs, VA National Formulary
non formulary drug request - ↑ 7.0 7.1 Prescriber's Letter 17(7): 2010 Recommended Lab Monitoring for Common Medications Detail-Document#: http://prescribersletter.com/(5bhgn1a4ni4cyp2tvybwfh55)/pl/ArticleDD.aspx?li=1&st=1&cs=&s=PRL&pt=3&fpt=25&dd=260704&pb=PRL (subscription needed) http://www.prescribersletter.com
Database
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=441184
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=41774
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=445421
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=444254
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=508375
- PubChem: http://pubchem.ncbi.nlm.nih.gov/summary/summary.cgi?cid=1976