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Monographs of Topical Drugs that Have Caused Contact Allergy/Allergic Contact Dermatitis
Published in Anton C. de Groot, Monographs in Contact Allergy, 2021
Estrogens, conjugated, is a pharmaceutical preparation containing a mixture of water-soluble, conjugated estrogens derived wholly or in part from urine of pregnant mares or synthetically from estrone and equilin. It contains a sodium-salt mixture of estrone sulfate (52-62%) and equilin sulfate (22-30%) with a total of the two between 80 and 88 per cent. Other concomitant conjugates include 17α-dihydroequilin, 17α-estradiol, and 17β-dihydroequilin. The product is indicated for use as treatment of vasomotor symptoms or vulvar and vaginal atrophy due to menopause, hypoestrogenism due to hypogonadism, castration or primary ovarian failure, as palliative treatment of breast cancer with metastatic disease, as palliative treatment of androgen-dependent carcinoma of the prostate, and as preventive therapy for postmenopausal osteoporosis (1).
Alternate Pathways of Steroid Biosynthesis and the Origin, Metabolism, and Biological Effects of Ring B Unsaturated Estrogens
Published in Ronald Hobkirk, Steroid Biochemistry, 1979
B. R. Bhavnani, C. A. Woolever
The data from these studies are very much in agreement with the findings from the earlier animal experiments Equilin and 17β-dihydroequilin are potent estrogens.Equilenin and 17α-dihydroequilenin have little activity.The sulfate esters are more potent than the parent compounds when given by the oral route.Equilin and equilin sulfate are more potent than estrone and estrone sulfate.Equilin sulfate given alone is more potent than an equal weight of the conjugated equine estrogens.
Primary choice of estrogen and progestogen as components for HRT: a clinical pharmacological view
Published in Climacteric, 2022
Remarkably, the content of 17β-estradiol is only about 1%. It is produced by the metabolism of estrone, the amount of which, however, is dependent on the activity of 17β-reductases differing in the target tissues such as the brain, bone, urogenital tract and vasculature. Likewise, other components can also function as prodrugs for active metabolites. Equilin can be metabolized to 17β-dihydroequilin (and vice versa) or to equilenin [13], both with strong biological activities, as presented in Table 4 [14]. This table summarizes several experimental studies in ovariectomized rats, showing the mean percentages of the CEE components used in these studies and the biological activity with respect to the potency in the vagina and uterus. The strong efficacy of these equine estrogens has been also shown in a variety of clinical studies with different results according to different endpoints. For example, equilenin increased the hepatic proteins high density lipoprotein-cholesterol, SHBG, CBG and angiotensinogen to a six or seven-times higher extent than the use of 17β-estradiol [14]. These effects are not dependent on the binding affinity to these proteins, which is about 30% lower for equilenin compared to 17β-estradiol [14].