adrenal pharm Flashcards
(17 cards)
name conditions of xs androgens
prostate cancer bph androgenetic alopecia precocious puberty hirsituism
what are the 5a reductase inhibitors? which ones are used for prostate ca?
finasteride -prostate
dutasteride - prostate
propecia
finasteride
inhibits type II 5a-reductase
blocks conversion of T –> DHT
use: prostate cancer
propecia
5a-reductase inhibitor
use: hair loss
dutasteride
type I/II 5a-reductase inhibitor
use: prostate cancer
what are conditions of androgen deficiency
hypogonadism
osteoporosis
muscle wasting in AIDS
HRT in aging men
Whats the mech of testosterone?
diffuses across the membrane –> cytosolic receptor –> dimerization/binding to DRE –>alteration of target gene transcription –> growth/differentation/ synthesis of enzymes and functional proteins
where testosterone synthesized?
95% synthesized in testes
5% synthesized in adrenal (mostly adrenal for women)
converted to DHT by 5a-reductase
converted to estradiol by aromatase
who gets testosterone?
men with subnormal T (<200-300 ng/dL) with sx:
- *low libido
- *decreased morning boners
- *low bone mineral density
- *gynecomastia
- *small testes
- fatigue
- depression
- anemia-reduced muscle strength
why is testosterone NOT indicated for impaired spermatogenesis?
T would suppress GnRH and further impair spermatogenesis
testosterone formulations
- IM
- transdermal gel
- transdermal patch
- SubQ
- buccal
- nasal
- oral
what are advantages of the transdermal formulations?
maintain a stable T level throughout the dosing period
adverse effects of testosterone
- decreased spermatogenesis (will return to nl function after discontinuation)
- reversible cholestatic jaundice
- weight gain (edema)
- arterial thrombosis (dec HDL with inc LDL)
- prostate enlargement
bicalutamide/flutamide
- androgen receptor antagonist
- use: prostate ca, hirsutism from PCOS
- PO qid
- can have androgen deprivation effects
leuprolide
- GnRH analog
- SC or IM
- antagonist when continuous admin –> prostate ca, precocious puberty in boys
- agonist when used pulsatile
- can cause hypogonadism with prolonged treatment
spironolactone
androgen receptor antagonist
- inhibits 17aOH-ase + 17,20 desmolase
- use: prostate ca, hirsutism in PCOS
- **causes hyperkalemia and gynocomastia
ketoconazole
17a-OH inhibitor –> inhibits testosterone synth
used as antiandrogen in PCOS