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Flashcards in Chemotherapies Deck (34):
1

Cyclophosphamide

alkylating agent

hemorrhagic cystitis
cardiotox

2

Cisplatin

alkylating agent

neprotox (hydrate prior to dose), ototox, electrolyte wasting

3

Alkylating agents
-MOA
-Toxicities
-cell cycle specific?

-crosslinks DNA strands, causing strand breakage
-NOT cell cycle specific
-myelosuppression, infertility

4

Anti-metabolites
-cell cycle specific?

-substitutes for normal nucleotides or folate, causing strand breakage
-S phase specific
-prolonged/severe neutropenia

5

Mercaptopurine

anti-metabolite/purine analog
-hepatotox, immunosuppression, secondary malignancies

6

Methotrexate
-MOA
-antidote
-rescue normal cells with ____

-anti-metabolite/folate analog
-leucovoricin rescues normal cells from MTX
-antidote = glucarpidase

7

Topoisomerase inhibitor
MOA?
toxicity?

-interferes w/ topoisomerase causing strand breakage
-myelosuppression

8

Doxyrubicin (anthracycline)
-dose limiting toxicity?
-antidote?

-Topo II inhibitor
-cardiotoxicity is dose-limiting
-vesicant - apply cold
-dexrazoxane is cardioprotectant, antidote for extravasation

9

Etoposide
-cell cycle specific?

-Topo II inhibitor
-S and G2 specific
-mucositis, alopecia

10

Topotecan (camptothecin)
-cell cycle specific?

-Topo I inhibitor
-S phase specific
-diarrhea, interstitial lung disease, typhilitis

11

paclitaxel

-inhibits microtubule disassembly
-M phase specific (M for Microtubule)
-myelosuppression esp neutropenia

12

vincristine

-inhibits microtubule assembly
-M phase specific (M for Microtubule)
-myelosuppression esp neutropenia

13

Leuoprolide

GnRH agonist
-binds and stimulates GnRH receptors in hypothalamus leading to increased release of LH/FSH which eventually causes downregulation of receptors due to negative feedback --> decreased estrogen/testosterone production
-initial tumor flare, CV disease, hyperglycemia, decr bone mineral density

14

Degarelix

GnRH antagonist
-binds and blocks GnRH receptors in pituitary --> decr LH/FSH release --> decr testosterone production

15

Flutamide

Antiandrogen
-binds and blocks testosterone receptor or inhibit nuclear receptor translocation
-hepatic failure, CV disease

16

Tamoxifen

Antiestrogen
-binds and blocks estrogen receptors

17

Anastrozole

Aromatase inhibitor
-blocks conversion of androstenedione to estradiol in peripheral tissues --> decr estrogen production
-postmenopausal women only (b/c premenopausal still can make estrogen in ovaries)
-hypercholesterolemia, decr bone mineral density

18

Flurouracil

also - what drug enhances its cytotoxicity?antidote?

anti-metabolite/Pyrimidine analog
-leucovorin enhances cytotox by stabilizing FdUMP/TS binding
-uridine antidote

19

Thalidomide

Immunomodulator
inhibits proliferation and induces apoptosis of tumor cells
enhances T-cell and NK-cell
hypocalcemia

20

Vorinostat

HDAC inhibitor
binds histone deacetylase to limit removal of acetyl groups

A for Active

21

Bortezomib

Proteasome inhibitor
binds 26S proteasome, inhibits it from degrading IkB, prevents NFkB activation (a TF that activates growth, angiogenesis, anti-apoptotic factors)

22

Imatinib

BCR/ABL Tyrosine Kinase Inhibitor

headache, rash, hepatotoxicity

Drug-drug interactions:
-acid reducers
-other CYP3A4 substrates

23

Rituximab

Anti-CD20 antibody
binds CD20 on surface of B-cells --> cell death

avoid live vaccinations, hep B reactivation, infusion-related reactions

24

Erlotinib

EGFR inhibitor

binds EGFR, preventing kinase phosphorylation and activation --> inhibits downstream signaling for cell proliferation

Dermatologic toxicity
interstitial lung disease

25

Trastuzumab

HER2 inhibitor

binds and inhibits HER2 receptor --> reduced proliferation of cells overexpressing HER2

26

Crizotinib

ALK inhibitor --> reduced proliferation of cells expressing ALK oncogenic fusion protein

hepatotoxicity, bradycardia

27

Bevacizumab

VEGF inhibitor - inhibits angiogenesis
hemorrhage, GI perf, impaired wound healing

28

Nivolumab

Checkpoint inhibitor

upregulates T-cell action by blocking immune suppressive ligand (PD-1, CTLA-4, or PD-L1)

29

Vemurafanib

BRAF inhibitor - inhibits mutated forms of the tyrosine kinase BRAF in the MAPK pathway

new primary cutaneous malignancy

30

Trametinib

MEK inhibitor

inhibits the tyrosine kinases MEK1 and MEK2 downstream of BRAF

risk of new primary malignancy is decreased when used together with BRAG inhibitor

31

Everolimus

mTOR inhibitor

32

Vismodegib

Hedgehog pathway inhibitor

binds to membrane protein smoothend within Hedgehod pathway --> prevents forward signaling, suppresses tumor growth

33

Olaparib

PARP inhibitor - prevents cell from fixing double strand DNA breaks --> cell death

34

Palbociclib

cyclin-dependent kinase inhibitor

prevents phosphorylation of retinoblastoma --> cell cycle arrest in G1