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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.
Chemical structure of the endogenous androstenedione. In the human body, the enzyme aromatase converts androstenedione to estrogen. Aromatase is an enzyme that belongs to the cytochrome P450 family located on chromosome 15. In the human body, the aromatase consists of 10 β-strands (1 major sheet and 3 minor sheets) and 12 α-helixes.
[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]
The medication has been found to achieve 96.7% to 97.3% inhibition of aromatase at a dosage of 1 mg/day and 98.1% inhibition of aromatase at a dosage of 10 mg/day in humans. [3] [2] As such, 1 mg/day is considered to be the minimal dosage required to achieve maximal suppression of aromatase with anastrozole. [3]
Heart palpitations and arrhythmias, hypotension, nausea, vomiting, abdominal pain, respiratory system paralysis, death [4] [5] Aloe vera juice medicinal aloe Aloe vera "abdominal pain, diarrhea, potentially carcinogenic, with others can potentiate cardiac glycosides and antiarrhythmic agents" [3] Anthranoid laxatives
Exemestane is known chemically as 6-methylideneandrosta-1,4-diene-3,17-dione. Like the aromatase inhibitors formestane and atamestane, exemestane is a steroid that is structurally similar to 4-androstenedione, the natural substrate of aromatase. It is distinguished from the natural substance only by the methylidene group in position 6 and an ...
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