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48 Cards in this Set

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Alkylating agents MoA
formation of imonium or carbonium ion intermediate, reacts with nucleophiles leading to alkylated tissue molecules
alkylation of DNA interferes w nucleic acid synthesis and function
Alkylating agents general toxicities
BM suppression, GI (emesis), reproductive effects
Cyclophosphamide
(class of drugs & major SE)
alkylating agent,
hemorrhagic cystitis (treat w/ hydration, frequent voiding, mensa)
Procarbazine
(class of drugs & major SEs)
non-classical alkylating agent, CNS depression, disulfiram-like effect, MAOI activity
Cisplatin toxicities
nephrotoxicity, ototoxicity, periph neuropathy, electrolyte disturbance, emetogenic, anaphylaxis
Doxorubicin
main tox
cardiomyopathy
Methotrexate
(MoA, tox)
inhibits DHF reductase (therefore, synthesis of thymidylate & purines)
myelosuppression, stomatitis, hepatic
Leucovorin rescue
antidote for excessive methotrexate
Mechlorethamine
(class)
alkylating agent
Melphalan
(class)
alkylating agent
Cyclophosphamide
(class)
alkylating agent

(remember: hemorrhagic cystitis!)
Carmustine, Lomustine
(class)
alkylating agent
Streptozocin
(class)
alkylating agent
Busulfan
(class)
alkylating agent
Procarbazine
(class)
nonclassical alkylating agent

(remember: disulfiram effect, MAOI effects)
Cisplatin, Carboplatin, Oxaliplatin
(class & mech)
platinum compounds, inhibit DNA synthesis
Methotrexate
(class)
folic acid analog
inhibits DHFR
Pemetrexed
(class)
folic acid analog
inhibits thymidylate synthase
6-MP
(class)
purine analog
Fludarabine phosphate
(class)
purine analog
Cladribine
(class)
purine analog
5-FU
(class)
purine analog, inhibits thymidylate synthase
Cytarabine
(class)
purine analog
S phase specific
Gemcitabine
(class)
purine analog
inhibits ribonucleotide reductase
effect of TPMT
TMPT metabolizes 6-MP & 6-TG
low activity increases toxicity
Dactinomycin
(class & MoA)
antitumor antibiotic
binds DNA, interferes w RNA synth
Doxorubicin & Daunorubicin
(class & MoA)
antitumor antibiotic
intercalate between DNA bases, inhibit DNA synth
inhibit topoisomerase II --> DNA strand breaks
forms free radicals
Bleomycin
(class & MoA)
antitumor antibiotic
binds to DNA --> strand breaks
generates free radicals
Bleomycin toxicities
pulmonary (age)
cutaneous
allergic
NOT BONE MARROW SUPPRESSION!!
Mitomycin
(class & MoA)
antitumor antibiotic
reduced to alkylating agent
Vincristine & Vinblastine
(class and MoA)
vinca alkaloids
mitotic inhibitors
bind tubulin, inhibit MT polymerization
Vincristine tox vs. Vinblastine tox
Vincristine: mild myelosuppression, neurotoxicity
Vinblastine: more severe myelosuppression
Paclitaxel
(class & MoA)
mitotic inhibitor
binds MTs, promotes polymerization
Etoposide
(MoA)
inhibits topoisomerase II --> DNA strand breaks
Topotecan & Irinotecan
(MoA)
inhibits topoisomerase I --> DNA damage
Asparaginase
(MoA)
catalyzes hydrolysis of asparagine to aspartic acid, depleting asparagine pool in leukemic cells
Imantinib
(MoA & SEs)
inhibits Bcr-Abl TK in CML
(binds ATP binding site to prevent phosphorylation)
SE: GI, edema, cramps, neutropenia, hepatotoxicity
Cetuximab
(MoA and SEs)
binds EGFR on cell surface
acneiform rash, low Mg2+, ILD
NO BONE MARROW SUPPRESSION!!!
Gefitinib & Erlotinib
(MoA and SEs)
inhibit TK domain of EGFR intracellularly
acneiform rash, ILD
Bavacizumab
(MoA)
binds VEGF
Sorafenib & Sunitinib
(MoA)
inhibits many TK receptors
all trans retinoic acid
induces differentiation
retinoic acid syndrome
arsenic trioxide
induces differentiation
QT prolongation, arrhythmias
Bortezomib (MoA)
proteasome inhibitor
Hydroxyurea (MoA)
inhibits ribonucleotide reductase (decreased DNA synth)
Flutamide
blocks androgen receptor
Rituximab
binds CD20
Trastuzumab
Herceptin