Pharmaceuticals for contraception/hormone substitution containin

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai

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514841, 514843, A61K 3156

Patent

active

056332424

ABSTRACT:
This invention relates to a compound preparation for contraception and hormone replacement that consists of three steps totalling 28 daily doses. The pharmaceutical is characterized in that
step 1 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component,
step 2 consists of 20 to 22 daily doses, each containing a preparation in which the active ingredients are at least one biogenous estrogen and one gestagen component from the group of C.sub.21 -gestagens including progesterone, as well as dienogest, desogestrel, 3-keto desogestrel, gestodene, levonorgestrel, norgestimate, norethisterone, norethisterone acetate and dydrogesterone, and
step 3 consists of 3 or 4 daily doses, each containing a preparation in which the active ingredient is at least one biogenous estrogen component.

REFERENCES:
patent: 3639600 (1972-02-01), Hendrix
patent: 4921843 (1990-05-01), Pasquale
patent: 5010070 (1991-04-01), Boissonneault
Zhu et al., "The Carcinogenic Activity of Ethinyl Estrogen Is Determined by Both Their Hormonal Characteristics and Their Conversion to Catechol Metabolites", Endocrinology, vol. 132, No. 2, pp. 577-583 (1993).
Jiang et al., "Effect of 17.beta.-oestradiol on contraction, Ca.sup.2+ current and intracellular free Ca.sup.2+ in guinea-pig isolated cardiac myocytes", Pharmacol (1992), 106, pp. 739-745.
Mooradian, "Antioxidant Properties of Steroids", J. Steroid Biochem, Molec. Biol., vol. 45, No. 6, pp. 509-511, 1993.
Jiang et al., "Acute effect of 17.beta.-estradiol on rabbit coronary artery contractile responses to endothelin-1", Am. J. Physiol., 263 pp. H271-275, 1992.
Clarkson, "Experimental effects of progesterone versus progestins on arterial wall", Gynecol. Endocrinal., 6 Suppl. 1:15, 1992.

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