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AROMATASE INHIBITORS
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AROMATIZATION
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INDRODUCTION Aromatization: Aromatase is a enzyme
It converts androgens into estrogen Aromatase Inhibitors: Block the production of E
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CLASSIFICATION OF AIs 2 TYPES 1- IRREVERSIBLE STEROIDAL INHIBITORS:
Exemestane It forms a permanent and deactivating bond with the aromatase enzyme 2- REVERSIBLE NON-STEROIDAL INHIBITORS: Anastrozole Letrozole Inhibit the synthesis of E via reversible competition for the aromatase enzyme
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MECHANISM OF ACTION SOURCE OF ESTROGEN: In premenopausal women:
Main source is ovaries In post-menopausal women: E is produced in peripheral tissues
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AROMATASE & GYNECOMASTIA
Excess aromatization in the presence of high testosterone levels in males: GYNECOMASTIA CLINICAL RELEVANCE: So AIs can be used for the treatment of
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SIDE EFFECTS OF AIs BONE: Osteoporosis, arthritis, joint & bone pain
Hot flushes Endometrial cancer: No increased risk Thromboembolism:
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USES OF AIs Treatment of breast & ovarian cancer in postmenopausal women Tamoxifen resistant breast carcinoma Gynecomastia in men
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