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4 Cards in this Set
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Androgens |
Pharmacokinetics:good oral absorption,but marked first pass hepatic metabolism,so it isnt used orally.binds to sex hormone binding globulin in the plasma.Metabolised in the liver to 17-ketosteroid,then conjugated w/ glucoronate &sulfate & excreted in urine.T1/2:30min.In tissues it can be converted to HT & estradiol which are active metabolites.Alkylated androgens have good oral bioavailability. SE:causes,menstrual disorders &male sex characteristics in women,puberty precox &epiphyseal closure in puberty boys, infertiliiy+prostate hyperplasia in menas well as gynecomastia &in fetus it causes,dysgenesis of external genital organs in both sexes. Others unclude,acne,weight gain,hypertension due to erythrocytosis. Medical use:hypogonadism,improvement of muscle mass in elderly persons,protein loss due to trauma,immobilization.Hereditary angioneurotic edema,stimulation of longitudinal growth in boys w. delayed puberty,refractory anemias,osteoporosis, PHRT,paliative tx of hormone sensitive breast cancer. Contraindication:pregnancy,prostate hyperplasia & cancer,congestive heart failure |
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Androgen drugs |
1.endogenous testosterone:testosterone, dihydrotesterone(DHT),dehydroepiandosetrone, androstenedione:transdermal patch,gel, buccal(due to hih degree of 1st pass metabolism),the last two are weak androgen 2.Testosterone esters:testosterone enanthate,testosterone cypionate, estosterone undeccanoate:long acting testosterone esters--prodrugs releasing free testosterone in plasma,given in i.m & act for 1-4wks, testosterone undeccanoate is effective orally(predominantly absorbed in lymphatic capillaries) 3.17-alkylative derivatives: methyltestosterone, stanozolol, fluoxymesterone,nandrolone,danazol. Effective orally ,used for hereditary angioneurotic edema.SE:liver damage--intrahepatic cholestasis,elevation of plasma level of bilirubin,hepatic adenoma & carcinoma(rare). Danazol is also used for ovulation inhibition,endometriosis, menorrhagia,fibrocystic breast disease & hemophilia A |
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Anabolic steroids |
General:in therapeutic doses--increases muscle mass & physical perfomance in women,children & hypoonadal men, In higher doses--increases muscle mass & physical perfomance also in healthy athletic men. SE:same as androgens,but more severe 1.endogenous testosterone:testosterone, dehydroepiandrosterone,androstenedione,(hcG):usually for abusing. 2.17-alkylating derivatives:stanozolol, mandrolone,tetrahydrogesitrinone: classical anabolic steroids that are used illegally,has good oral bioavailability |
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Anti androgens |
Medical use:hirtuism in women,acne, seborrhea,androgen dependent alopecia in both sexes,prostate hyperplasia and carrier,pubertas precox in boys,tx of sexual offenders. 1.cyproterone acetate:has progestin activity--inhibits gonadotropin secretion,so less testosterone is formed. 2.flutamide,nilutamide:has no progestin effect,inhibits -ve feedback of testosterone, more testosterone is produced,so higher doses is needed. 3.finasteride:inhibitor of 5a-reductase converting testosterone to dihydrtestosterone in several tissues.Used mainly for alopecia |
