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Acarbose

ENDOCRINE SYSTEM

ORAL ANTIDIABETIC AGENTS - [ ENDOCRINE SYSTEM ]

Acarbose competitively and reversibly inhibits pancreatic α-amylase and intestinal brush border α-glucosidases, resulting in retardation of glucose absorption from hydrolysed complex carbohydrates and reduction of blood-glucose concentrations.(1,2,3)

Type 2 diabetes mellitus.(1,2,3)

Patients <18 yr; Diabetic ketoacidosis or cirrhosis; Malabsorption; inflammatory bowel disease; with or pre-disposed to intestinal obstruction; Intestinal diseases that affect digestion or absorption; Conditions that worsen as a result of increased gas formation e.g. Hernias; colonic ulcers; Hepatic impairment; crclr< 25 ml/min/1.73m2. Pregnancy, lactation.(1,2,3)

Flatulence, abdominal pain, distension, diarrhoea, nausea, vomiting. Elevation of transaminases, hepatitis, jaundice. Rarely, skin reactions. Potentially Fatal: Hepatotoxicity.(1,2)

Drugs that may increase blood glucose levels e.g. thiazides, steroids, chlorpromazine, atypical antipsychotics, may antagonise the action of acarbose. GI adsorbents and digestive enzyme preparations may reduce acarbose effects; avoid concomitant admin. Cholestyramine may enhance effects of acarbose. Effects of other hypoglycaemics may be potentiated by acarbose. Neomycin may enhance reduction of postprandial blood-glucose and intensify GI symptoms. Acarbose may reduce digoxin bioavailability. May interact with warfarin and affect INR. Increased risk of hypoglycaemia with disopyramide.(1,2,3)

Cautious administration should be advised in hypertension, renal and liver function impairment patients. Cautious administration should be advised in elderly. Should be avoided in children, pregnancy and lactation.(1,2,3)

Initially, 25 mg daily. May adjust dose at 4-8 wkly intervals based on tolerance and 1-hr post-prandial blood glucose levels. Maintenance dose: 50-100 mg tid. Max: ≤60 kg: 50 mg tid; >60 kg: 100 mg tid.(1,2,3)

1. Brunton LL, Chabner BA, Knollmann BC, editors. Goodman & Gilman’s The Pharmacological Basis of Therapeutics. 12th ed. China: McGraw Hill; 2011 2. Katzung BG, Masters SB, Trevor AJ, editors. Basic & Clinical Pharmacology. 12th ed. New York: McGraw Hill; 2012 3. Acarbose. (cited on 3rd november 2013) available online from website http://www.accessdata.fda.gov/drugsatfda_docs/label/2012/020482s025lbl.pdf.