Plasma concentration of glibenclamide in routine clinical practice was determined
by a specific radioimmunoassay. In diabetic patients treated with glibenclamide for
a month or longer, the drug level in fasting morning plasma was variable but the mean
level paralleled the daily dose. After oral administration of 2.5 mg in healthy and
diabetic subjects, the drug level reached peaks in 1.5 hours and declined to the half
of the peak level in next 2-3 hours. The plasma glibenclamide profile after oral dose
did not differ significantly in patients with secondary failure to the drug. Comparison
of a single-dose and divided-dose schedules of 5 mg glibenclamide revealed that plasma
drug level increased each time after administration. Plasma glucose and insulin concentrations
did not differ significantly at most times of the day but there was a tendency that
increment of plasma glucose after meal was suppressed by a dose taken immediately
before a meal. The relationship of blood level of glibenclamide to clinical effectiveness
may be rather indirect and needs to be elucidated.
Radioimmunoassay of Glibenclamide
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Glibenclamide Level in Plasma
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Secondary Failure
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Plasma Insulin
