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75 Cards in this Set
- Front
- Back
androgenic hormones?
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produce masculine characteristics
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anabolic hormones?
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promoting synthesis, growth
(opposite of catabolism) |
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most potent androgen?
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testosterone
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site of production of androgenic/anabolic hormones in males and females?
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males: testes (95%), adrenal cortex (5%);
females: adrenal cortex and ovaries (40-65%), peripheral conversion of DHEA (35-60%) |
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what hormone stimulates testosterone production at puberty?
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LH
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DHT vs T
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T serves predominantly as prohormone;
DHT is active moiety in many tissues; cytosolic receptor has 10x affinity for DHT and is more readilyt transported to nucleus |
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deficiency of DHT is associated with?
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lack of development of male genitalia
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enzyme that converts T to DHT?
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5α reductase
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where is T the active hormone rather than DHT?
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hypothalamus
pituitary (negative feedback) |
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testosterone effect on liver?
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stimulation or suppression of protein synthesis
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testosterone effect on kidney?
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stimulation of erythropoietin
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testosterone effect on hematopoietic system?
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direct stimulation of growth of stem cells
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testosterone effect on CNS?
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facilitation of libido and sexual function;
aggressive behavior |
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testosterone effect on muscle?
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development of muscle mass and strength
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testosterone effect on skin, sebaceous gland, hair?
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stimulation of beard, axillary, and pubic hair growth;
increase in temporal hair recession and balding; increase in sebum secretion |
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testosterone effect on bone/cartilage?
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promotion of epiphyseal fusion
maintenance of bone mass |
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testosterone effect on larynx and vocal cords?
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enlargement of larynx and thickening of vocal cords
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testosterone effect on mammary glands?
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development of gynecomastia
affected by androgen:estrogen ratio |
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why is testosterone a poor drug?
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high first pass effect
rapidly absorbed and metabolized mixed anabolic and androgenic effects |
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type B testosterone alteration?
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17α substitution
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testosterone effect on kidney?
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stimulation of erythropoietin
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testosterone effect on hematopoietic system?
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direct stimulation of growth of stem cells
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testosterone effect on CNS?
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facilitation of libido and sexual function;
aggressive behavior |
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testosterone effect on muscle?
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development of muscle mass and strength
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testosterone effect on skin, sebaceous gland, hair?
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stimulation of beard, axillary, and pubic hair growth;
increase in temporal hair recession and balding; increase in sebum secretion |
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testosterone effect on bone/cartilage?
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promotion of epiphyseal fusion
maintenance of bone mass |
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testosterone effect on larynx and vocal cords?
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enlargement of larynx and thickening of vocal cords
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testosterone effect on mammary glands?
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development of gynecomastia
affected by androgen:estrogen ratio |
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why is testosterone a poor drug?
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high first pass effect
rapidly absorbed and metabolized mixed anabolic and androgenic effects |
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type B testosterone alteration?
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17α substitution
methyltestosterone |
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type C testosterone modification?
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ring alteration
mesterolone orally active not metabolized to T can cause liver toxicity and cancer |
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type A testosterone modification?
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17β esterification
enanthate cypionate injected sc - absorption greatly delayed metabolized to T |
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methyltestosterone?
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type B
1:1 (androgen:anabolic activity) |
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fluoxymesterone?
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type BC
1:1-2 (androgen:anabolic activity) |
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methandrostenolone?
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type BC
1:3 (androgen:anabolic activity) |
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oxymetholone?
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1:3 (androgen:anabolic activity)
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stanozolol?
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1:3-5 (androgen:anabolic activity)
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oxandrolone?
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1:3-13 (androgen:anabolic activity)
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mesterolone?
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type C
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enanthate?
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type A
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cypionate?
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type A
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true of all oral and parenteral preparations of testosterone derivatives?
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exhibit both androgenic and anabolic effects
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causes of hypogonadism/primary testicular failure?
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genetic/chromosomal causes;
direct damage to Leydig cells or seminiferous tubules |
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hormone levels in primary testicular failure?
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testosterone low but gonadotropin levels high
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drug of choice for primary testicular failure?
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testosterone ester: enanthate or cypionate;
testosterone measure and titrated to normal range; normal event occur if done correctly |
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causes of secondary testicular failure?
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lack of gonadotropins (prader-willi)
lack of LH/FSH (hypopit.) lack of GnRH (hypothalamus) |
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hormone levels in secondary testicular failure?
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testosterone and gonadotropin levels low
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treatment of secondary testicular failure?
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treat underlying hypogonadism
gonadotropins have been used androgens added at puberty slow increase to mimic surge |
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anabolic/androgenic steroids for use in treating anemias?
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large required dose causes androgenic side effects;
contraindicated for aplastic anemia |
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which anemia are anabolic/androgenic steroids contraindicated and what is the alternative treatment?
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aplastic anemia: causes HCC;
colony-stimulating factors should be used instead |
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hereditary angioneurotic edema?
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lack of an active inhibitor of the first component of compliment resulting in complement cascade always 'on' with increased blood vessel permeability causing painful submucosal swelling
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androgens in treatment of hereditary angioneurotic edema?
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increase hepatic synthesis of the active inhibitor;
danazol: 17α alkylated |
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use of androgens in treatment of delayed growth?
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do produce growth spurt
cause epiphyseal calcification so generally spurt is limited and treatment is questionable |
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use of androgens to counter muscle wasting?
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typically that seen with antiinflammatory steroid use;
positive nitrogen balance in hypogonadal individuals |
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use of androgens with aging?
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combat male menopause (drop off at 55 yo) which results in decrease in muscle mass, strength, and libido;
low doses shown to have some beneficial effects |
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side effects of high androgen levels?
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virilizing effects (adolescent males and females);
inhibition of spermatogenesis; feminizing side effect; hepatic abnormalities; changes in lipoprotein profiles; increase in aggressive behavior |
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how is spermatogenesis inhibited by high androgen levels?
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decreased LH and FSH resulting in decreased sperm production;
may persist for long periods |
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feminizing side effect seen with high androgen levels?
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T converted to an estrogen;
gynecomastia is most common; estradiol is 7x higher in athletes abusing androgens |
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hepatic abnormalities seen with high androgen levels?
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cholestatic hepatitis
hepatic adenocarcinoma |
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changes in lipoprotein profiles seen with high androgen levels?
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decreased HDL
increased LDL |
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situations where androgen suppression or antiandrogens would be useful?
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male pattern baldness
virilizing syndromes in women acne prostate hyperplasia, carcinoma male contraception |
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long-acting GnRH analogs?
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continuous level has inhibitory effects
leuprolide acetate goserelin |
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effects of long-acting GnRH analogs?
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testosterone levels fall to 10% of normal;
initial flare but can be countered by antagonist |
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leuprolide acetate?
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long-acting GnRH analog
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goserelin?
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long-acting GnRH analog
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GnRH antagonists?
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inhibitory effect without initial flare
further research required |
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ketoconazole?
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inhibit steroid synthesis P450s;
requires high doses; cause gynecomastia; not promising for prostate cancer |
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finasteride?
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5α reductase inhibitor
effective in BPH blocks hirsutism in women (not approved) by local administration |
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androgen receptor antagonists?
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cyproterone acetate
flutamide block effect on target tissue effective for excess androgen in women effective for advanced prostate carcinoma often coupled with GnRH agonist |
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cyproterone acetate?
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androgen receptor antagonist
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flutamide?
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androgen receptor antagonist
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gossypol?
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phenolic extract of cottonseed
destroys elements of seminiferous tubules does not effect endocrine function reversible with discontinuation directly decreases sperm motility |
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male contraception?
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testosterone alone
GnRH suppression + testosterone gossypol |
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why isn't testosterone alone an effect form of male contraception?
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too many side effects
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tried as intravaginal contraceptive?
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gossypol
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