Medicines Estradiol

Brain delivery of steroid hormones is also of interest to medicinal chemists. Again, most data available on CDSs of steroids pertain to rates of oxidation of the dihydropyridine carrier, to blood and brain concentrations, and to pharmacological activities. The latter can then be taken as proof of efficient cerebral hydrolysis of the pyridinium metabolite. Thus, the dihydrotrigonelline carrier allowed good brain delivery of estradiol and some other estrogens [181][182],... 

Kaliwal, B. B. Efficacy of carrot seed Daucus carota) extract in inhibiting implantation and its reversal as compared with estradiol-17-beta in albino rats. J Curr Biosci 1989 6(3) 77—82. Lokar, L. C., and L. Poldini. Herbal remedies in the traditional medicine of the Venezia Giulia region (north east Italy). J Ethnopharmacol 1988 22(3) 231-239. 

For therapeutic purposes and under the control of a responsible veterinarian, the administration to farm animals of 17/3-estradiol, testosterone, and progesterone and derivatives that readily yield the parent compound on hydrolysis after absorption at the site of application may be authorized by the individual EU member states. Also, for therapeutic purposes, the administration of authorized veterinary medicinal products containing (i) allyl trenbolone, administered orally, or beta-agonists to equidae and pets, provided they are used in accordance with the manufacturer s instructions, (ii) beta-agonists, in the form of an injection to induce tocolysis in cows when calving may be authorized. Again, these veterinary medicinal products must be administered by a veterinarian under his direct responsibility. 

P-Estradiol (=17p-Oestradiol 17 p-Estradiol) (sterol) isolated by Edward Doisy (USA) (Nobel Prize, Medicine, 1943, with Henrik Dam, Vitamin K)... 

Viscoli et al 2001 New England Journal of Medicine 345 1243-1249. Women received estradiol 1 mg or placebo. There were 99 strokes or deaths in the estradiol group vs 93 in controls. Twelve of the strokes in the estradiol group were fatal compared to four in controls. 

Spironolactone is antiandrogenic and increases the peripheral metabohsm of testosterone to estradiol (13). It often causes g)mecomastia in men and breast enlargement and soreness in women. Five cases of mammary carcinoma have been reported. Potential human metabohc products of spironolactone are carcinogenic in rodents, and the UK Committee on Safety of Medicines in 1988 restricted the approved indications for the drug, removing the indications of essential hypertension and idiopathic edema (14). 

Ethynyl estradiol Oral contraceptive and reproductive medicine therapy 100-200... 

Two human hormones that have received considerable attention are 17p-estradiol (a natural estrogen) and 17a-ethynyl estradiol (a synthetic hormone used in contraceptive medicines) both of which have been found in wastewater treatment plant effluents. 

Testosterone, the testicular hormone, is identified as a male hormone. Estradiol (17/3), which differs from testosterone only by loss of a methyl group and aromatization of ring A, is the ovarian hormone. Progesterone is the progestational hormone and is essential for fertilization and maintenance of pregnancy. Once again medicinal chemists, by further alteration of structures, have made more potent oral and more useful progestins. 

Bachmann, G., Estradiol-releasing vaginal ring delivery system for urogenital atrophy—experience over the past decade. Journal of Reproductive Medicine, 1998, 43(11), 991-998. 

SAR of DES. One may consider DES as another form of estradiol wherein the two 6-membered rings B and C open up and a 6-membered aromatic ring D introduced in place of the cyclopentane ring. It was further suggested that the aetual distance prevailing between the two DES phenol OH moieties was virtually the same as the C-3 OH to C-17 OH distance existing in estradiol and, hence, these two entities may prove to be a perfect fit to the same receptor site. Recently, with the advent of latest computer softwares the medicinal chemist has established the distance between the two OH moieties in DES to be 12.lA and in estradiol 10.9A. 

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