Acarbose administration

Kato K, Naruse S, Kondo T, Hayakawa T. Carbohydrate malabsorption following acarbose administration. Diabet Med 1998 15(5) 393-7. 

Maeda A, Yokoi S, Kunou T, Murata T. [A case of pneumatosis cystoides intestinalis assumed to be induced by acarbose administration for diabetes mellitus and pemphigus vulgaris.JNippon Shokakibyo Gakkai Zasshi 2002 99(ll) 1345-9. 

When acarbose is combined with insulin, the greatest effects are seen with regimens that involve only once- or twice-daily administration. The alpha-glucosidase inhibitors seem to be less effective when they are combined with intensive insulin therapy (35). In combination with insulin or oral hypoglycemic drugs the frequency of hypoglycemic episodes can increase sucrose or higher carbohydrates are reported to be less effective, which can be understood from the mechanism of action. 

Oba K, Kudo R, Yano M, Watanabe K, Ajiro Y, Okazaki K, Suzuki T, Nakano H, Metori S. Ileus after administration of cold remedy in an elderly diabetic patient treated with acarbose. J Nippon Med Sch 2001 68(l) 61-4. 

ANION EXCHANGE RESINS ACARBOSE t hypoglycaemic effect of acarbose Uncertain Monitor blood glucose during and co-administration and after discontinuation of concurrent therapy... 

However, in a formal study of the pharmacokinetics of a single dose of digoxin 0.75 mg before and after the administration of acarbose 50 mg tds for 12 days in healthy volunteers, apart from a small increase in Cmax, the pharmacokinetics of digoxin were unaffected by acarbose (219). It is not uncommon for anecdotal reports of a possible interaction to be unconfirmed by formal kinetic studies, and it is possible in such cases that there is a subset of patients who are susceptible to the interaction who have not been included in the formal study. In this case, for example, it may be that the interaction occurs in people with diabetes and not in healthy subjects. There may also be a difference in the effect of acarbose on a single dose of digoxin, compared with steady-state therapy. Advice that acarbose and digoxin should be administered 6 hours apart is still reasonable. 

Administration of a single dose of l4C-labelled acarbose (200 mg) to volunteers who had received the drug three times daily for 4 weeks revealed that, at steady state, mean Cmax was 18.4 fig/ and rmax 2.1 h (Muller and Hillebrand, 1986). The level of radioactivity in blood increased markedly after 6 h, because of the absorption of metabolites formed in the gut. 

After intravenous injection of 0.4mg/kg in healthy volunteers, plasma acarbose concentrations declined biexponentially and fitted the equation for an open two-compartment model. The volume of distribution of acarbose at steady state following intravenous administration was calculated to be about 0.321/kg while the apparent volume of the central compartment was 0.161/kg. The mean distribution half-life was found to be approximately 0.5 h after intravenous injection (Putter et al.. 1982) and 3.7 h following oral administration (Muller and Hillebrand, 1986). 

The faecal excretion of acarbose and component-II was almost complete within 24 h of administration of a single dose of 300 mg orally and amounted... 

Recently, a semisynthetic deoxynorjirimycin derivative Bay o 1248 (20), which is absorbed from the intestine and does not produce carbohydrate malabsorption, was reported as a potent glucosidase inhibitor exhibiting strong sucrase and maltase inhibitory activity and no amylase inhibition. Administration of which has a longer duration of action than acarbose, reduces food intake, body weight gain and epididymal fat pad weight in rats. ... 

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