Femara is a specific nonsteroidal aromatase inhibitor. It inhibits the aromatase enzyme by competitively binding to the haem of the cytochrome P450 subunit of the enzyme, resulting in a reduction of estrogen biosynthesis in all tissues.
Breast cancer
Femara online exerts its antitumour effect by depriving estrogen dependent breast cancer cells of their growth stimulus. In postmenopausal women, estrogens are derived mainly from the action of the aromatase enzyme, which converts adrenal androgens-primarily androstenedione and testosterone-to-estrone (E). The suppression of estrogen biosynthesis in the peripheral tissues and the malignant tissues can be achieved by specifically inhibiting the aromatase enzyme. Impairment of adrenal steroidogenesis has not been observed.
Induction of ovulation in Infertility
Estrogen exerts a negative feedback on the hypothalamic-pituitary axis and decreases the release of FSH from the pituitary gland. Letrozole acts by blocking the synthesis of estrogen. Administration of letrozole in the early part of the menstrual cycle results in release of FSH from the pituitary gland. Femara acts by blocking the feedback, thereby increasing gonadotropin secretion and resulting in stimulation of ovarian follicle. Letrozole leads to induction of ovulation in women with anovoluatory infertility. Femara does not deplete estrogen receptor or produce a negative effect on the endometrium. Addition of letrozole to gonadotropins decreases gonadotropin requirements, increases the number of preovulatory follicles, and decreases endometrial thickness without a negative effect on pregnancy rates.
Induction of ovulation in anovulatory infertility
Patient selection for the treatment of infertility should be done with care and pelvic examination should be performed prior to letrozole administration and before each subsequent course. The patient should be instructed to inform the doctor of any abdominal or pelvic pain, weight gain or discomfort. Endometrial biopsy should always be performed prior to letrozole therapy in this population. Caution should be exercised when using letrozole in patients with uterine fibroids due to the potential for further enlargement of the fibroids.
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