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Details Title: Pharma of MaleSexAndrogens Description: 4.20.07 Total Flash Cards: 36 Created: 04/25/2007 15:43:26	To study from this set of flash cards, or to create your own your own study flash cards, register HERE. If you are already a registered user, CLICK HERE.
Cards Term what are the 2 male sex horomones? Definition test, and 5alpha-DHT Term what are 2 enzymes you should know in steroidogenesis in leydig cells? Definition SCC (cholesterol to pegnenolone) and 3beta-HSD/KSI Term what are 2 major sources of adnrogens in adults? Definition Leydig cells produce test and 5alpha-DHT. Adrenals produce androstenedione and dehydroepiandrosterone Term Is 5Alpha-DHT or T more potent? Definition 5alpha DHT Term can androgens be antagonists or agonists? Definition antagonists at high doses and agonists ad physiological doses Term what does LH do to T? Definition LH stimulates steriodogenesis in Leydig cells which stimulates T. Term FSH in sertolli cells do what to steroids? Definition FSH stimulated spermatogenesis in seminif tubules--and this stimulates Estrogen testosterone and inbinin... Term what does T do? Definition Testosterone Induced -Male sex drive, performance -Muscle mass increase -Penis enlargement -Vocal cord enlargement -Spermatogenesis Term what does 5alpha DHT do? Definition 5a-Dihydrotestosterone induced -Increased facial and body hair -Acne -Scalp hair recession -Prostate enlargement Term Do T and 5 alpha DHT do the exactly the same thing? Definition No, Evidence in support of different actions of T and 5a-DHT come from patients with 5a-reductase deficiency (pseudo-hermaphrodites) Term What do T and 5alpha DHT bind to? Definition They both bind to androgen receptors Term where is 5 alpha reductase 1 expressed? Definition it's expressed high in the scalp and skin Term where is 5 alpha reductase 2 expressed? Definition in the prostate Term which type is more easily inhibited by finasteride? Definition #2 Term How will steriods act as full agonists? Definition Ag binds to R, Complex binds to HRE, Recruits co-activator, Amplified gene transcription Term How do you become a mixed agonist/antagonist (as a steroid)? Definition Ligand binds to R, Complex binds to HRE, Differential recruitment of co-activator/co-repressor, Abrogated gene transcription Term How do you become a pure antagonist? Definition Ligand binds to R; Complex binds to HRE; Recruits co-repressor; No gene transcription Term what's another way you can become a pure antagonist (no co-repressor required)? Definition Ligand binds to R; Complex does not bind to HRE; No gene transcription Term Describe the androgen receptor and its coactivator ARA70 Definition For complete activity the AR-Ligand complex must bind ARA70; AR-Testosterone and AR-5a-DHT complexes both bind ARA70; ARA70 is not bound in the presence of the anti-androgen 4-hydroxyflutamide; Concept exists that ligands with a spectrum of agonist/antagonist activity may be dependent upon tissue specific co-activators and co-repressors Term what are Type iii 17Beta-HSD and 5alpha reductase? Definition they are synthesis blockers of antiandrogen therapy Term what do you use androgen therapy for? Definition Hypogonadism; Hypopituitarism; Androgen replacement Term what are examples of androgen therapy agents? Definition Synthetic androgens; Testosterone derivatives; 17b-esters and 17a-alkyl analogs Term what do you use anti-androgens for? Definition Precocious puberty; Female virilization; Male-pattern baldness; Benign prostatic hyperplasia; Prostate cancer; Term what are examples of antiandrogens for pecocous puberty? Definition receptor antagonists Term what;s an example of anti-androgens? Definition Receptor antagonists; 5a-reductase inhibitors Term what are the most commonly used synthetic androgens? Definition t-cypionate and t-acetate. these are 17b-esters-complete androgens Term What are Therapeutic Use of Synthetic Androgens ? Definition A. Hypogonadism: -Adult males with testicular damage -Adult males with hypothalamic disorders -Young adults with failure of onset of puberty B. Androgen Replacement Therapy (andropause) C. Anemia D. Anabolic effects Term How do you treat benign prostatic hyperplasia? Definition (this is a disease of the inner gland): surgically remove or use 5-alpha-reductase inhibitors Term How do you tx prostatic cancer? Definition (this is a disease of the outer gland which will metastisize to the pelvic bone). Use hormone ablative therapy-and castration, adrenalectomy, DES, antriandroges (Flutamide/nilutamide; Cyproterone acetate; 5a-reductase inhibitors ), and use LH-RH agonists; Zoladex; Leuprolide Term How do you do Treatment of Benign Prostatic Hyperplasia? Definition Development / enlargement of the prostate gland is dependent on DHT; Type II 5a -reductase converts testosterone to DHT in prostate gland In man, a single 5-mg oral dose produces a rapid reduction in serum DHT concentration (maximum effect at 8 hours). Suppression is maintained throughout 24-hr dosing interval. Daily dosing reduces serum DHT concentration by ~70% Circulating level of testosterone increased by ~10-20% but remained within the physiologic range Term what is Development / enlargement of the prostate gland dependent on? Definition DHT Term What converts testosterone to DHT in prostate gland? Definition Type II 5alpha reductase Term What is Hormonal Treatment of Prostatic Cancer? Definition Low tumor staging, when txd with DES is associated with high incidence of CVD and gynecomastia ; Delay hormone therapy to late stage disease; Castration is more effective than DES treatment; Anti-androgens are tumoristatic not tumoricidal; Need to show tumor is androgen receptor positive; Androgen receptor can be mutated in prostate cancer; LH-RH receptor agonists: Zoladex and Leuprolide Concept of triple therapy: LH-RH receptor agonists, 5a-reductase type 2 inhibitor, and AR antagonist (flutamide or nilutamide) Term What is Finasteride Treatment of Male-Pattern Baldness? Definition In MPB the scalp contains miniaturized hair follicles and increased amounts of DHT compared with hairy scalp; High activity of type II 5a-reductase in hair follicles type 1 predominates in sebaceous glands of scalp; Finasteride is a competitive specific inhibitor of Type II 5a-reductase; Finasteride produces a rapid reduction in serum DHT concentration, reaching 65% suppression within 24 hours of oral dosing with a 1-mg tablet; Finasteride decreased scalp and serum DHT concentrations and increased hair counts in studies of 1-2 year duration Term What are 3 main methods of male contraception? Definition 1. Inhibition of LH secretion -LH-RH agonists - leuprolide/zoladex -Silastic implants (estrogen plus progesterone) -Long-acting progestins (6-medroxyprogesterone acetate) 2. Inhibition of spermatogenesis -Inhibin 3. Inhibition of sperm motility Glossypol Term what are the main points of this lecture? Definition Leydig cells are the site of testosterone biosynthesis; A more potent androgen, 5a-dihydrotestosterone is produced in select androgen target tissues; The effects of testosterone and 5a-DHT are tissue specific; Androgen tx consists of administering synthetic androgens (receptor agonists) to tx of hypogonadism or hypopituatarism; Approaches to anti-androgen therapy are receptor antagonism, synthesis inhibition; Use of LHRH agonists provides another approach