Androgens Flashcards
Methyltestosterone
Androgen
17-alkylated testosterone
Route: oral / sublingual
SE: ↑ liver toxicity / ↓ spermatogenesis / ↓ testis size
Testosterone enanthate
Androgen
Route: IM
SE: ↓ spermatogenesis / ↓ testis size / change in lipid metabolism
Testosterone
Androgen
Route: transdermal / topical gel
SE: ↓ spermatogenesis / ↓ testis size / change in lipid metabolism
Low bioavailability b/c of 1st pass
Flutamide
Antiandrogen
MOA: androgen receptor antagonist
Rx: prostate CA
SE: gynecomastia / reversible liver toxicity
administered prior to GnRH analog Tx to prevent effects of initial testosterone surge
Bicalutamide
Antiandrogen
MOA: androgen receptor antagonist
Rx: prostate CA
SE: gynecomastia / reversible liver toxicity
administered prior to GnRH analog Tx to prevent effects of initial testosterone surge
Enzalutamide
Antiandrogen
MOA: androgen receptor antagonist / prevents nuclear translocation of AR / blocks DNA binding / blocks coactivator recrutitment
Rx: prostate cancer
Leuprolide
Antiandrogen
GnRH receptor agonist
Rx: prostate cancer
MOA: initial LH and testosterone surge -> desensitization and downregulation of GnRH receptors on pituitary
SE: sexual dysfunction / ↓ BM density / anemia / fatigue
must be used w/ AR receptor antagonist to prevent prostate CA growth
Goserelin
Antiandrogen
GnRH receptor agonist
Rx: prostate cancer
MOA: initial LH and testosterone surge -> desensitization and downregulation of GnRH receptors on pituitary
SE: sexual dysfunction / ↓ BM density / anemia / fatigue
must be used w/ AR receptor antagonist to prevent prostate CA growth
Degarelix
Antiandrogen
GnRH receptor antagonist
Rx: prostate cancer
more quickly reduces testosterone and no LH/testosterone surge (as seen w/ leuprolide and gosrelin)
Abiraterone
Antiandrogen
Synthesis Inhibitor
Rx: metastatic prostate CA
MOA: inhibits 17A-hydroxylase
SE: adrenal insufficiency (17A-hydroxylase used in cortisol production) -> HTN, hypokalemia, fluid retention / hepatic toxicity
used in combo w/ prednisone
Finasteride
5Alpha-reductase inhibitor
Rx: BPH
MOA: inhibits transformation from testosterone -> dihydrotestosterone
SE: impotence / gynecomastia / ↓ PSA levels
Dutasteride
5Alpha-reductase inhibitor
Rx: BPH
MOA: inhibits transformation from testosterone -> dihydrotestosterone
SE: impotence / gynecomastia / ↓ PSA levels
Sildenafil
PDE5 Inhibitor
Rx: ED
SE: cardiac events / low BP w/ nitrates / priapism
The phosphodiesterase type 5 (PDE5) enzyme decreases levels of cGMP levels by converting cGMP to GMP. This causes an increase in Ca2+ levels and a subsequent constriction of the smooth muscles.
Vardenafil
PDE5 Inhibitor
Rx: ED
SE: cardiac events / low BP w/ nitrates / priapism
The phosphodiesterase type 5 (PDE5) enzyme decreases levels of cGMP levels by converting cGMP to GMP. This causes an increase in Ca2+ levels and a subsequent constriction of the smooth muscles.
Tadalafil
PDE5 Inhibitor
Rx: ED
SE: cardiac events / low BP w/ nitrates / priapism
18 hour half life
The phosphodiesterase type 5 (PDE5) enzyme decreases levels of cGMP levels by converting cGMP to GMP. This causes an increase in Ca2+ levels and a subsequent constriction of the smooth muscles.
