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71 Cards in this Set

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Three types of antimetabolites?
1. Folic acid analogs
2. Pyrimidine analogs
3. Purine analogs
Folic Acid Analogs?
Methotrexate
Trimetrexate (PCP)
Pyrimidine analogs?
5-Flurouracil
Capecitabine
Cytarabine
Purine Analogs?
Mercaptopurine
Fludarabine
Cladribine
Thioguanine
Pentostatin (Hairy cell leukemia)
General notes on antimetabolites
Structural analogs of naturally occurring bases to inhibit enzymes or substitute

Cytotoxic effects during S phase and impaired synthesis in G1 phase
Antimetabolites resistance formed via?
Gene amplification of inhibited enzymes

Making enzymes that have less affinity for drug
Methotrexate works by? Also used in?
folic acid analog with high affinity for dihydrofolate reductase

Also used in rheumatoid arthritis, lupus, transplants
How does MTX get into cells?
actively transported into cells (moreso into cancer cells) and then polyglutamate synthetase adds glutamyl residues to trap MTX into cells

Leucovorin is given to be taken into healthy cells so that they can make folic acid normally
MTX used in?
Oral and IV for

Acute lymphoblastic leukemia, bladder, breast, CNS lymphomas

Inhibits cell-mediated immune reactions
MTX toxcity?
Ulceration
Marrow suppression
N/V
Alopecia
Hepaotox
Teratogenic
*Actively secreted into proximul tubule so can interact with other things that are secreted

BBW: preg, hepatic disease, pulmonary disease, infections
Pemetrexed MOA? used in? Special tox?
MOA: converted to poly-glutamated form, rapidly transported to inhibit Thymidylate synthetase and Dihydrofolate synthetase

For: mesothelioma, lung cancer, better for colon cancer than MTX

S/E: pruritic rash, severe marrow suppression, neuropathy
Pyrimidine analogs:
5-Fluorouracil
Cytarabine
MOA of 5-FU
5-FU attached to ribose to make fdUMP which can displace dUMP to inhibit thymidine for DNA synthesis and RNA synthesis
Leucovorin use in MTX vs 5-FU
In MTX Leucovorin is used to save the non-cancer cells and help them make folic acid

With 5-FU leucovorin is used to potentiate the toxicity
Describe how 5-FU is given, Why?
5-FU is used both intraarterially and topically
Infused over 5 days to get cells into S phase

*Cell cycle specific
5-FU most used for?
Slow growing solid tumors
Floxuridine is?
FU + deoxyribose (FUdR)
Floxuridine used for? given via?
Used for metastatic carcinoma in liver, given via hepatic artery
Capecitabine is?
Prodrug of FUdR

for nonresponsive metastatic breast cancer
5-FU specific S/E? (along with common)
Hand-foot syndrome - pain and sensitivity of palms and soles
Cytarabine is what?
Cytosine plus D-arabinose sugar (OH in the wrong orientation so blocks next base pair)
Cytarabine MOA?
inhibits DNA polymerase leading to unbalanced growth

Incorporated into DNA to inhibit elongation
Cytarabine given how?
IV over 5 - 7 days to phase cell cycle (get into S phase)
Cytarabine used for?
AML, CML, CLL (i.e. Leukemia)
Cytarabine tox?
Potent myelosuppression
Ulceration
Gemcitabine MOA?
is a Difluroanalogue of cytidine incorporated into DNA to terminate strand
Gemcitabine used for?
metastatic cancers

given every 7 days
Gemcitabine tox?
Flu-Like syndrome, potent radiation sensitizer, dyspnea
Purine Analogs for what?
Adenine and Guanine
Name Purine Analogs
6-Mercaptopurine
Thioguanine
Fludarabine
Cladribine
6-Mercaptopurine MOA
6-MP is phosphorylated and added to sugar to form thio-IMP which will inhibit Hypoxanthine-guanine phosphoribosyl transferase to inhibit xanthine and adenosine

Prevents DNA and RNA synthesis
6-Mercaptopurine used for?
Oral and IV for

Leukemias
6-MP metabolized by?
Two pathways:
P-450
Xanthine oxidase
what consequence with 6-MP?
hyperuricemia so give Allopurinol given to increase 6-MP levels and decrease uric acid levels
6-MP Tox?
Long term hepatotox
OIs
hematological suppression
Thioguanine used in? Tox?
Used in leukemias

S/E: hematological suppression
Fludarabine used in? Tox?
Used in leukemias and lymphomas

S/E: N/V bone marrow suppression
Cladribine used in?
hair cell leukemia, CML, ALL
Antibiotics used in cancer therapy
Dactinomycin
Daunorubicin
Doxorubicin
Bleomycin
Daunorubicin and Doxorubicin used in?
Hematological and solid tumors
Bleomycin used in?
Testicular, head, neck, cervical, Hodgkin's lymphomas, sarcoma's
General MOA of ATBs in chemo?
MOA: Directly bind DNA or intercalate between DNA base pairs preventing replication

Physically prevent replication
Dactinomycin used in?
Ewings
Wilm's
Dactinomycin MOA? notes?
intercalates DNA causing ss breaks

One of the most potent tumor agents
Dactino used in?
rhabdomyosarcoma
Wilm's tumor
Dactino tox?
Pancytopenia, GI effects
Dauno and Doxo MOA?
Intercalate into DNA,
preventing uncoiling,
inhibiting Topoisomerase II
Possible MOA of cardiotox of Dauno and Doxo
Will also bind to cell membranes to alter IP3 activation

Cardiac tissue is low in superoxide dismutase and catalase so are affected by radicals
Dauno and Doxo form a ____ intermediate that may?
Semiquinolone intermediate that forms free radicals that can cause DNA damage and breaks
Dauno used in?
AML
Doxo used in?
many things, wider range

breast, bladder, lung, ovarian, testicular, thyroid, ALL, lymphomas..
Dauno and Doxo tox?
usual +
Cardiac toxocity! -- there is a life dose (Doxo is 550)
Discoloration of urine! (red)
Severe vesiant properties
Secondary leukemias
Can give what to decrease superoxide?
Dexarzoxane to prevents free radicals
Lipid complexes which aren't taken into the cell
Idarubicin used in?
leukemias
Idarubicin tox?
less cardiotox
red urine
Epirubicin used in?
multiple; bladder, breast, head and neck, lung ovarian
Epirubicin tox?
cardiac tox
red urine
Valrubicin used in?
bladder tumors
Resistant bladder tumors
Valrubicin tox?
teratogenic (as all are)
red urine
Mitoxantrone analog of?
Doxorubicin
Mitoxantrone used in?
AML, CLL, breast, ovarian
Mitoxantrone tox?
less cardio tox, less bone marrow suppression
sexual dysfunction
blue-green urine and nails
not as much vesicant
Mitoxantrone also used in?
Progressing MS
Bleomycin MOA?
can intercalate into DNA and the metal binding core will complex with Fe and Cu, will also form free radicals
Bleomycin cell cycle specific?
Yes; for G2 phase
Bleomycin used in?
multiple: cervical, pancrativ, Hodgkin's, sarcoma

ABVD for Hodgkin's
Bleomycin tox?
low myelosuppression
Dry cough==> pulmonary fibrosis
flu-like
skin reactions
Bleomycin also used third line in?
topically for wart removal
Mitomycin MOA?
alkylation, free radicals
Mitomycin used in?
many: head and neck, soft tissue sarcoma, metastatic bone, stomach
Mitomycin tox?
SEVERE bone marrow tox (wait 8 weeks between treatments)
pulmonary tox
secondary leukemias