Clinical Experience With Chlorpropamide in the Management of Diabetes Mellitus

Hills, A. Gorman; Abelove, William A.

doi:10.1111/j.1749-6632.1959.tb39613.x

Cited by 5 publications

(1 citation statement)

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“…Results are in general agreement with those of many previous studies." 5,11,12,21,29 Drug absorption proceeds at a variable rate from subject to subject, but that it is complete is evidenced by essentially total recovery of dose from urine as unchanged drug and metabolites. Several investigators 9 , 14, 16, 25 have reported serum CPA half-life values from 30 to 40 hours by use of the Toolan-Wagner assay procedure.…”

Section: Discussionmentioning

confidence: 99%

Pharmacokinetics and biotransformation of chlorpropamide in man

Taylor

1972

Clin Pharma and Therapeutics

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Chlorpropamide (CPA) pharmacokinetics were determined in 6 normal adult volunteers after a single oral 250 mg. dose. Drug absorption half-lifes varied from 0.1 to 1.5 hours with a calculated mean of 0.5 hour. Half-life for drug in plasma ranged from 25 to 42 hours with a calculated mean of 33 hours while the half-life estimated from urinary excretion data averaged 36 hours. In addition to drug, p-chlorobenzenesulfonylurea (CBSU),2-hydroxy-CPA (2-0H-CPA), and 3-hydroxy-CPA (3-0H-CPA) were recovered from urine of 4 diabetic subjects receiving 250 to 500 mg. of CPA daily. Approximately 2 per cent of daily dose was recovered from urine as p-chlorobenzenesulfonamide (CBSA), a degradation product of CBSU, and a similar amount was excreted as 3-0H-CPA. Drug, CBSU, and 2-0H-CPA excretion quantitated in 24 hour urine samples of these diabetic subjects by high-pressure liquid chromatography, averaged 18,21, and 55 per cent of dose, respectively. Two hours after CPA administration, unchanged drug accounted for 95 per cent of total drug and metabolite concentrations in plasma indicating that CBSU and 2-0H-CPA have significantly shorter elimination half-lifes than unchanged drug.

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