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Aromatase inhibitors (AIs) are a class of drugs used in the treatment of breast cancer in postmenopausal women and in men, [1] [2] and gynecomastia in men. They may also be used off-label to reduce estrogen conversion when supplementing testosterone exogenously. They may also be used for chemoprevention in women at high risk for breast cancer.
Side effects of antihormone therapy are generally minimal, but can produce similar feelings to menopause in women. [4] Common symptoms of all antihormone therapies include irregular menstrual cycles, hot flashes, weight gain, vaginal dryness, headaches, mood swings and hair thinning. [ 4 ]
The main source of estrogen is the ovaries in premenopausal women, while in post-menopausal women most of the body's estrogen is produced via the conversion of androgens into estrogen by the aromatase enzyme in the peripheral tissues (i.e. adipose tissue like that of the breast) and a number of sites in the brain. Estrogen is produced locally ...
[11] [4] In addition, it is described as a much more potent aromatase inhibitor than adrenal steroidogenesis inhibitor. [17] AG can inhibit aromatase by 74 to 92% and decrease circulating estradiol levels by 58 to 76% in men and postmenopausal women. [1] [7] AG is not an effective ovarian steroidogenesis inhibitor in premenopausal women. [17]
Aromatase inhibitors, which stop the production of estrogen in postmenopausal women, have become useful in the management of patients with breast cancer whose lesion was found to be estrogen receptor positive. [33] Inhibitors that are in current clinical use include anastrozole, exemestane, and letrozole.
[3] [2] As such, 1 mg/day is considered to be the minimal dosage required to achieve maximal suppression of aromatase with anastrozole. [3] This decrease in aromatase activity results in an at least 85% decrease in estradiol levels in postmenopausal women. [3] Levels of corticosteroids and other adrenal steroids are unaffected by anastrozole. [3
Among all aromatase inhibitors, Letrozole is commonly used for improving female fertility. It works by inhibiting aromatase which is an enzyme that catalyses the conversion of androstenedione and testosterone to estrogen by hydroxylation. Hence, Letrozole inhibits the synthesis of estrogen. [18]
Letrozole, sold under the brand name Femara among others, is an aromatase inhibitor medication that is used in the treatment of breast cancer for post-menopausal women. [1]It was patented in 1986 and approved for medical use in 1996. [4]