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27 Cards in this Set
- Front
- Back
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What are the anabolic effects of androgen?
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increased muscle mass, bone density red blood cell mass
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What is produced by Leydig cells under influence of LH?
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testosterone
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What is formed by by 5 alpha reductase in target tissues?
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dihydrotestosterone
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What short acting testosterone ester needs to be administered 2-3 times weekly?
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testosterone proprionate
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What long acting preps can be dosed every 2-4 weeks and used an oil based vehicle for slow absorption?
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testosterone enanthate, cypionate
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Most commonly presribed 17 alpha alkylated analogs
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methyltesterosterone and oxymetholone
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Which preparation is used orally in anemia?
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Oxymetholone
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What is methyltestosterone used and administered?
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Buccal or oral for hypogonadism, palliative for breast cancer, delayed puberty
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popular oral androgens with athletes because of anabolic actions
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oxandrolone, fluoxymesterone, stanozolol
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How is testosterone metabolized and how long is its half life?
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first pass effect by liver; very short
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What testosterone delivery system could you use to bypass the first pass hepatic effect?
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transdermal testosterone
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What is the primary cause of use for androgen replacement therapy?
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primary hypogonadism or secondary to defect in hypothalamus or pituitary
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What area has 5 alpha reductase rich tissue for patch location?
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scrotum
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What other uses is androgen therapy used for?
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anemia, short stature (increased linear growth prior to epiphyseal closure), athletic performance
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What are some side effects of androgens?
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acne, muscle dvlpmt, impotence, decreased spermatogenesis, liver abnorms, psychosis, closure of epiphyseal plates
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Two anti androgens and competitive antagonists of cholesterol esterase
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ketoconazole (antifungal) and spironolactone (diuretic and aldosterone antagonist)
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What is spironolactone and ketoconazole also used for?
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hirsutism; prostate cancer
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What 5 alpha reductase inhibitor is used for benign prostatic hypertrophy?
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oral finasteride
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What does finasteride biologically do and manifest?
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blocks conversion of testosterone to DHT, no change in testosterone or LH
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What else can finasteride be used for?
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stimulate hair growth in male pattern baldness
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What is an androgen receptor antagonist that competes with DHT and also has progesterone like activity in suppressing gonadotropin activity?
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Cyproterone acetate
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What pure competitive antagonist of DHT binding to androgen receptor also blocks inhibitory feedback loop resulting in increased levels of LH and testosterone?
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Flutamide
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What else is flutamide used in conjunction with to treat prostatic cancer?
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Leuprolide (GnRh blockade)
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Most effective inhibitors of testosterone synthesis?
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GnRH and analogs like Leuprolide
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What male contraceptive is an extract from the cotton plant?
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Gossypol
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How does Gossypol work?
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causes vacuolization and breakdown of Sertoli cells and sperm density reduction
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What were side effects of Gossypol?
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diarrhea edema, dyspnea, neuritis, paralysis at high doses
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