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48 Cards in this Set
- Front
- Back
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
|
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Doxorubicin
main tox |
cardiomyopathy
|
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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
|