PMID: 11338674May 8, 2001Paper

Non-protein bound dienogest in serum and salivary dienogest in women taking the oral contraceptives Certostat and Valette

Die Pharmazie
G KlingerG Hobe

Abstract

Dienogest (17 alpha-cyanomethyl-17-hydroxy-4,9-estradien-3-one) is the progestagen component of the oral contraceptives Certostat and Valette. In contrast to other 19-norsteroid progestagens like levonorgestrel, norethisterone, gestodene and 3-ketodesogestrel, dienogest does not bind to sexual hormone binding globulin (SHBG). The absent binding to SHBG results in a high portion of free, non-protein bound dienogest in serum. In female volunteers taking the oral contraceptives Certostat and Trisiston, the part of non-protein bound dienogest and levonorgestrel, respectively, in serum was determined by the method of centrifugal ultrafiltration. The portion of free dienogest was found to be 9.55 +/- 0.95% (m +/- SD, n = 13) of total serum dienogest. Free levonorgestrel constituted 0.97 +/- 0.14% (n = 12) of total serum levonorgestrel. In an investigation with 47 female volunteers taking Certostat, serum total dienogest was quantified by a specific radioimmunoassay and free dienogest in serum by centrifugal ultrafiltration. In the serum samples with dienogest concentrations in the range of 4.1-57.7 ng/ml, the part of free, non-protein bound dienogest was found to be 8.90 +/- 0.54% of serum total dienogest. There is a high correlation...Continue Reading

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