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28 Cards in this Set
- Front
- Back
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Alkylating agents
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cyclophosphamide
carmustine procarbazine cisplatin carboplatin oxaliplatin |
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which alkylating agents are platinum complexes
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cisplatin
carboplatin oxaliplatin nephrotox |
|
Bis(chloroethyl)amine
Must be converted by P450. |
Cyclophosphamide
|
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Nitrosurea
non-resistant (w/ other alk’s) Lipid soluble Crosses BBB |
Carmustine
|
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Methylhyrdazine derivative
Inhibits synthesis of DNA, RNA and protein Asoprocarbazine & H2O2 generated |
Procarbazine
|
|
Inorganic platinum complex. Cross-links DNA (N7 guanine)
Nephrotoxicity – use IV hydration & diuretics!! ototox |
Cisplatin
|
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2nd gen platinum
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Carboplatin
less renal tox |
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3rd gen platinum
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Oxaliplatin
use when resistant |
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Antimetabolites: Folic acid antagonist
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Methotrexate
|
|
Methotrexate
drug resistance? |
↓transport
↓Polyglutamate formation ↑DHFR synthesis ↓Affinity of DHFR for MTX |
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Antimetabolites: Purine antagonists
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6-MP
Cladribine |
|
Metabolized by HGPRT
6-thioinosinic acid inh. purine pathway enzymes well tolerated!! Hyperuricemia assoiciated with tumor cell lysis – give allopurinol |
Mercaptopurine
(6-MP) |
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Mercaptopurine
(6-MP) resistance |
↓ HGPRT activity
|
|
Resistant to adenosine deaminase, thus reaches high intracellular concentrations
DNA strand breaks |
Cladribine
|
|
Antimetabolites: Pyrimidine antagonists
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5FU
Capecitabine Cytarabine (Ara C) |
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1. Inhibits thymidylate synthesis inhibits DNA synthesis
2. Incorporated into RNA interferes with RNA processing 3. Incorporated into DNA inhibits DNA synthesis |
5FU
|
|
5FU
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Colorectal cancer!
|
|
Fluoropyrimidine carbamate prodrug
Converted to 5-FU in tumor cells by thymidine phosphorylase |
Capecitabine
|
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Capecitabine
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Metastatic breast cancer!
Extensive liver metabolism |
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Ara CTP
S-phase-specific Inhibits DNA polymerase prevents chain elongation |
Cytarabine aka cytosine arabinoside of ara-C
|
|
Cytarabine aka cytosine arabinoside of ara-C
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Highly schedule dependent.
AML. |
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plant alkaloids that stop ASSEMBLY of microtubules
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Vinblastine
Vincristine |
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Hodgkins
non-hodgkins breast cancer |
Vinblastine
|
|
ALL
Hodgkins Non-hodgkins Pediatric tumors – ewing’s sarcoma and wilms’ tumor peripheral neurotoxicity usually well-tolerated |
ALL
Hodgkins Non-hodgkins Pediatric tumors – ewing’s sarcoma and wilms’ tumor |
|
Binds microtubules and enhances tubulin proliferation.
Blocks DISASSEMBLY of MTs – so you have a ton of MTs and nothing to do with them! plant alkaloid |
yew tree
Paclitaxel |
|
Inhibits topoisomerase II causing DNA strand breakage,
late S-G2 phase plant alkaloid |
Etoposide
Germ cell cancers Lung cancer Hematologic malignancy Germ cell cancer Gastric cancer |
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Inhibits topoisomerase I
plant alkaloid |
Topotecan
Advanced ovarian cancer when platinum based agents fail. Renal excretion. |
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Antibiotics
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Doxorubicin
Daunorubicin Dactinomycin Mitomycin Bleomycin |
