Chemotherapeutics: Hormonal Agents and miscellaneous compounds Flashcards
Aromatase inhibitors MOA
aromatase responsible for extra adrenal synthesis of estrogen; inhibition results in decreased estrogen production
aromatase inhibitors side effects
nausea, fatigue and hot flashes
aromatase inhibitor drugs
Aminoglutethimide, Anastrozole, Exemestane, Letrozole
Aminogluethimide treats
breast cancer
aromatase inhibitor drugs unique properteis
side effects less severe than tamoxifen
Anastrozole additional MOA
imidazole inhibitor
Anastrozole treats
breast cancer
Exemestane additional MOA
steroidal, irreversible inhibtor
exemestane treats
breast cancer
letrozole treats
breast cancer in post menopause
letrozole additional MOA
imidazole inhibitor
Non steroidal antiandrogens
Bicalutamide, Flutamide, Nilutamide
Non steroidal anti-androgens MOA
competitive antagonist to androgen receptor
Non steroidal anti-androgens treats
prostate cancer
Non steroidal anti-androgens side effects
Gynecomastia, n/v/d, visual problems, hepatotoxicity
Goserelin MOA
desensitize GnRH receptor and inhibit release of FSH and LH; decrease androgen and estrogen release
goserelin treats
prostate cancer and breast cancer post menopause
goserelin side effects
impotence, hot flashes, tumor flare
Leuprolide (Lupron) MOA
desensitize GnRH receptor and inhibit release of FSH and LH; decrease androgen and estrogen release
Leuprolide (Lupron) treats
prostate cancer and breast cancer post menopause
Leuprolide (Lupron) side effects
impotence, hot flashes, tumor flare
Prednisone treats
leukemia/lymphomas
prednisone side effects
immunosuppression, ulcers, hyperglycemia, osteoporosis, glaucoma and cataracts
Tamoxifen MOA
partial agonist inhibitor of the estrogen receptor; blocks nuclear translocation of estrogen receptor and lowers estrogen responsive genes
Tamoxifen treats
high risk recurrent breast cancer
tamoxifen side effects
hot flashes, n/v, menstrual complications, hypercalcemia, thromboembolism, vision complications
Toremifene MOA
partial agonist inhibitor of the estrogen receptor; blocks nuclear translocation of estrogen receptor and lowers estrogen responsive genes
Toremifene treats
breast cancer
Toremifene side effects
hot flashes, n/v, menstrual complications, hypercalcemia, thromboembolism, vision complications
Megestrol acetate MOA
synthethic progestin; progesterone receptor agonist; MOA not fully understood
megestrol acetate treats
breast cancer and endometrial cancer
Asparaginase MOA
hydrolyzes circulating L-arginine to aspartic acid+ammonia
asparaginase treats
childhood leukemia specifically ALL
asparaginase side effects
hypersensitivity reaction (fever/chills), n/v, skin rash(uticaria), ammonia toxicity
interferon MOA
exact MOA unknown, finding IFN receptors results in suppression of cell proliferation
interferon treats
leukemias and kaposi sarcoma
interferon side effects
flu like symptoms that can be severe
procarbazine MOA
oxidized/metabolized into a form that binds DNA and inhibits DNA, RNA and protein synth
procarbazine treats
Hodgkin
procarbazine side effects
myelosuppression, n/v/d, neurotoxicity, mutagen, teratogen,
procarbazine unique properties
inhibits monoamine oxidase; food drug interactions leading to HTN crisis
Arsenic trioxide MOA
believed to induce apoptosis in cancer cells by release of cyt C from mito and caspase activation
arsenic trioxide treats
drug resistant AML
arsensic trioxide side effects
fatigue, prolonged QT, heavy metal toxicity
arsensic trioxide is used in combo with
all-trans retinoic acid (ATRA)
Bortezomib MOA
proteasome inhibitor; intercellular build up of unfolded proteins leads to cell death
Bortezomib treats
multiple myeloma
bortezemib side effects
peripheral neuropathy, myelosuppression, GI upset