Chemotherapeutics: Hormonal Agents and miscellaneous compounds Flashcards by Reginald Johnson

Aromatase inhibitors MOA

aromatase responsible for extra adrenal synthesis of estrogen; inhibition results in decreased estrogen production

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aromatase inhibitors side effects

nausea, fatigue and hot flashes

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aromatase inhibitor drugs

Aminoglutethimide, Anastrozole, Exemestane, Letrozole

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Aminogluethimide treats

breast cancer

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aromatase inhibitor drugs unique properteis

side effects less severe than tamoxifen

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Anastrozole additional MOA

imidazole inhibitor

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Anastrozole treats

breast cancer

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Exemestane additional MOA

steroidal, irreversible inhibtor

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exemestane treats

breast cancer

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letrozole treats

breast cancer in post menopause

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letrozole additional MOA

imidazole inhibitor

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Non steroidal antiandrogens

Bicalutamide, Flutamide, Nilutamide

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Non steroidal anti-androgens MOA

competitive antagonist to androgen receptor

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Non steroidal anti-androgens treats

prostate cancer

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Non steroidal anti-androgens side effects

Gynecomastia, n/v/d, visual problems, hepatotoxicity

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Goserelin MOA

desensitize GnRH receptor and inhibit release of FSH and LH; decrease androgen and estrogen release

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goserelin treats

prostate cancer and breast cancer post menopause

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goserelin side effects

impotence, hot flashes, tumor flare

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Leuprolide (Lupron) MOA

desensitize GnRH receptor and inhibit release of FSH and LH; decrease androgen and estrogen release

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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