Progesterone effects

P8. Fesch, L. A., Segal, S., and Topper, Y. J., Progesterone effects on galactose metabolism in prepubertal patients with congenital galactosemia and in rats main-tamed on high galactose diets. J. Clin. Invest. 39, 178-184 (1960). 

Andreen L, Bixo M, Nyberg S, Sundstrom-Poromaa I, Backstrom T. Progesterone effects during sequential hormone replacement therapy. Eur J Endocrinol 2003 148 571-7. 

Cuchacovich M, Tchernitchin A, Gatica H, Wurgaft R, Valenzuela C, Cornejo E. Intraarticular progesterone effects of a local treatment for rheumatoid arthritis. J Rheumatol 1988 15(4) 561-5. 

Extracts of corpora lutea were known ia the early tweatieth ceatury to inhibit ovulatioa ia animals. Pure progesterone (3), the active component of the extracts, was isolated ia 1934 and its stmcture reported (15). Several problems limited its use and drove efforts to develop progesterone analogues, ie, it was available only ia small quantities from animal sources, was not orally active, and was discovered to cause androgenic side effects. 

Preparation of Ba-Methyi-17-Hydroxy progesterone 17-Acetate 1 g of 6a-methyl-17a-hy-droxyprogesterone was dissolved in a mixture of 10 ml of acetic acid and 2 ml of acetic anhydride by heating. After solution was effected the mixture was cooled to 15°C, and 0.3 g of p-toluenesulfonic acid was added. After allowing the mixture to stand for a period of 2 /a hours at room temperature, the pink solution was poured into ice water to give an amorphous solid which was recovered by filtration. 

FIGURE 8.3 Examples of chemical modification of active drags that have either unwanted effects (cocaine, norepinephrine) or suboptimal effects (penicillin, progesterone) to molecules with useful therapeutic profiles. 

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