Hellekant Antineoplastics Flashcards
What is goserelin?
GnRH receptor agonist
What is leuprolide?
GnRH agonist
What is Degarelix?
GnRH receptor antagonist
What tissues produce 5 alpha reductase?
Prostate, external genitalia, skin
What is the MOA of finasteride?
5 alpha reductase inhibitor; inhibits conversion of testosterone to DHT
What is the MOA of dutasteride?
5 alpha reductase inhibitor; prevents conversion of testosterone to DHT
What 5 alpha reductase inhibitor has a trophic effect on the prostate?
Dutasteride
What is abiraterone?
17 alpha hydroxylase and 17,20-lyase inhibitor; prevents testosterone synthesis
What tissues does testosterone target?
Muscle, seminal vesicle, epididymis, bone
What is the MOA of bicalutamide?
Blocks androgen receptors
What is the MOA of flutamide?
Blocks androgen receptors
In treatment of prostate cancer, leuprolide is administered with what for the first few weeks? Why?
Leuprolide (GnRH agonist) is administered with androgen receptor blocker (eg bicalutamide) to prevent early GnRH stimulation
What is aminoglutethimide?
Blocks pregnenolone synthesis
What drug blocks 17 alpha hydroxylase and is used in the treatment of prostate cancer?
Abiraterone
What is anastrazole?
Aromatase inhibitor
What is the MOA of anastrazole?
Inhibit aromatase, preventing the conversion of testosterone to estradiol 17 beta and androstendione to estrone
What is exemestane?
Irreversibly inhibitor of aromatase
What is fluvestrant?
Selective estrogen downregulator; inhibits all ER actions and causes ER degradation following SERD binding
What is tamoxifen?
SERM; antagonist at breast, agonist and uterus and bone
What is an AE due to tamoxifen use?
Endometrial cancer due to agonism at the uterus
What is Raloxifene?
SERM; antagonist at breast and uterus; agonist at bone
What is tormifene?
SERM; antagonist at breast; no effect on bone, ? On uterus
What SERM is an antagonist at the breast and uterus, but is an agonist at the bone?
Raloxifene
What is letrozole?
Aromatase inhibitor
