Estradiol for Female
Estradiol cypionate , or estradiol cipionate, is a synthetic ester, specifically the 3-cyclopentylpropanoyl ester, of the natural estrogen, estradiol. It was first introduced in 1952 by Upjohn in the United States, and has been in widespread use since. Estradiol cypionate is absorbed more slowly than estradiol itself, and for that reason, it can be administered less often.Compared to other commonly used estradiol esters, via the intramuscular route, estradiol cypionate was found to have the longest duration of action with a duration of ~11 days, while estradiol benzoate and estradiol valerate were found to last for 4-5 days and 7-8 days, respectively.
1. Sexual development
The development of secondary sex characteristics in women is driven by estrogens, to be specific, estradiol. These changes are initiated at the time of puberty, most are enhanced during the reproductive years, and become less pronounced with declining estradiol support after the menopause. Thus, estradiol produces breast development, and is responsible for changes in the body shape, affecting bones, joints, and fat deposition. Fat structure and skin composition are modified by estradiol.
2. Female reproduction
In the female, estradiol acts as a growth hormone for tissue of the reproductive organs, supporting the lining of the vagina, the cervical glands, the endometrium, and the lining of the fallopian tubes. Estradiol enhances growth of the myometrium. Estradiol appears necessary to maintain oocytes in the ovary.
During the menstrual cycle, estradiol produced by the growing follicle triggers, via a positive feedback system, the hypothalamic-pituitary events that lead to the luteinizing hormone surge, inducing ovulation. In the luteal phase, estradiol, in conjunction with progesterone, prepares the endometrium for implantation.
3. Male reproduction
The effect of estradiol (and estrogens in general) upon male reproduction is complex. Estradiol is produced by action of aromatase mainly in the Leydig cells of the mammalian testis, but also by some germ cells and the Sertoli cells of immature mammals.
Estradiol functions (in vitro) to prevent apoptosis of male sperm cells. While some studies in the early 1990s claimed a connection between globally declining sperm counts and estrogen exposure in the environment, later studies found no such connection, nor evidence of a general decline in sperm counts. Suppression of estradiol production in a subpopulation of subfertile men may improve the semen analysis.
Males with certain sex chromosome genetic conditions, such as Klinefelter's syndrome, will have a higher level of estradiol.
Estradiol has a profound effect on bone. Individuals without it (or other estrogens) will become tall and eunuchoid, as epiphyseal closure is delayed or may not take place. Bone structure is affected also, resulting in early osteopenia and osteoporosis.
Also, women past menopause experience an accelerated loss of bone mass due to a relative estrogen deficiency.
Estrogens can be produced in the brain from steroid precursors. As antioxidants, they have been found to have neuroprotective function.
The positive and negative feedback loops of the menstrual cycle involve ovarian estradiol as the link to the hypothalamic-pituitary system to regulate gonadotropins.
6. Gynecological cancers
Estradiol has been tied to the development and progression of cancers such as breast cancer, ovarian cancer and endometrial cancer.
Estradiol has complex effects on the liver. In high amounts, it can lead to cholestasis. Estradiol affects the production of multiple proteins, including lipoproteins, binding proteins, and proteins responsible for blood clotting.
Estrogen affects certain blood vessels. Improvement in arterial blood flow has been demonstrated in coronary arteries.
Several benign gynecologic conditions are dependent on estrogen, such as endometriosis, leiomyomata uteri, and uterine bleeding.
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