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57 Cards in this Set

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  • Back
What is the mechanism of action of methotrexate?
inhibits dihydrofolate reductase, decreased dTMP and decreased DNA
What drugs are cell cycle specific?
Antimetabs (MTX, 5-FU, 6-MP
etoposide
bleomycin
vinca alkaloids
paclitaxel
What drugs are cell cycle nonspecific?
alkylating agents
Abtics
What phase of the cell cycle do the vinca alkaloids and taxols work on?
M
What part of the cell cycle do the antimetabolites work on?
S
What part of the cell cycle does etoposide work on?
S and G2
What part of the cycle does Bleomycin work on?
G2
What is MTX used for clinically?
Leukemias
lymphomas
choriocarcinoma
sarcomas
abortion
ectopic preggs
RA
psoriasis
What is the mechanism of action of 5-FU?
Pyrimidine analog activated to 5F-dUMP- covalently complexes folic acid.
Inhibs thymidylate synthase. decreased dTMP
What are the SEs of MTX?
myelosuppression- reversible with leucovorin
Macrovesicular fatty change in liver
What is the role of leucovorin?
reverses MTX myelosuppression
When is 5FU used clinically?
colon cancer, other solid tumors
basal cell carcinoma- topical
Synergy w/ MTX
What are the SEs of 5FU?
Myelosuppression- not reversible
photosensitivity
What is the mechanism of action of 6-mercaptopurine?
blocks de novo purine synthesis. Activated by HGPRTase
What is 6-MP clinically used for?
Leukemias, lymphomas (not CLL or hodgkins)
What are the SEs of 6-MP?
BM, GI, Liver
metabed by xanthine oxidase
increased tox with allopurinol
What is the mechanism of action of Cytarabine?
inhibs DNA polymerase
What is cytarabine used for?
AML
What is the tox of Cytarabine?
Leukopenia, Tpenia, Megaloblastic anemia
What is the mechanism of action of alkylating agents?
covalently x-link DNA at N-7
require bioactivation by the liver
What are the two major alkylating agents?
Cyclophosphamide
Ifosfamide
What is the clinical use of Cyclophosphamide and Ifosfamide?
Non-Hodgkin's lymphoma, breast and ovarian carcinomas. Immunosuppression
What are the SEs of cyclophosphamide and ifosfamide?
Myelosuppression; hemorrhagic cystitis, prevented with mesna
What is the mechanism of action of the Nitrosureas?
alkylate DNA, require bioactivation, cross BBB
What is the clinical use for Nitrosureas?
brain tumors (including glioblastoma multiforme)
crosses BBB
what are the SEs of Nitrosureas?
CNS tox- dizzy, ataxia
What are the Nitrosureas?
carmustine
lomustine
semustine
streptozocin
What is the mechansim of action of Cisplatin and Carboplatin?
alkylate DNA
What is Cisplatin used for?
Testicular, bladder, ovary and lung carcinoma
What are the SEs of Cisplatin?
Nephrotox, acoustic nerve damage
What is the mechanism of action of Busulfan?
alkylates DNA
What is Busulfan clinically used for?
CML
What is the tox of Bulsulfan?
Pulm fibrosis, hyperpigmentation.
What is the mech of action of Doxorubicin (adriamycin) and daunorubicin?
generates free radicals and noncovalently intercalates in DNA Creating breaks
What is Adriamycin used for clinically?
ABVD of Hodgkins
myelomas, sarcomas and solit tumors
breast, ovary, lung
What are the SEs of adriamycin
Cardiotox
myelosuppression
marked alopecia
toxic extravaasaion.
What is the mechanism of action of Dactinomycin (actinomycin D)?
Intercalates in DNA.
What is actinomycin used for clinically?
ACTinomycin ACTS out, just like kids. Kids tumors
Wilm's
Ewing's
Rhabdomyosarcoma
What is the tox of actinomycin?
Myelosuppression
What is the mechanism of action of Bleomycin?
Free radicals
What is bleomycin used for clinically?
testes
ABVD in hodgkins
What are the SEs of Bleomycin?
plm fibrosis, skin changes
minimal myelosuppression
What is the mechanism of action of Etoposide?
G2-phase-specific- inhibs topo II and increases DNA degredation
What is Etoposide used for clinically?
small cell carcinoma of lung and prostate, teste carcinoma
What is prednisone used for in cancer treatment?
CLL, Hodgkins
can trigger apoptosis
What is the mechanism of action of Tamoxifen?
SERM
What are the SEs of Tamoxifen?
may increase risk of endometrial carcinoma
What is the mechanism of action of trastuzumab?
Herceptin
Monoclonal Ab against HER-2 (erb-B2)
breast cancer
What are the SEs to Trastuzumab?
Herceptin
Cardiotoxicity
What are the SEs of Imatinib?
Fluid retention
What is the mechanism of vincristine/vinblastine?
M phase alkaloid that bind to tubulin and block polymerization of microtubules so that mitotic spindle cannot form
What is vincristine used for clinically?
mOpp for lymphoma
wilm's tumor
choriocarcinoma
What are the SEs of vincristine?
neurotox (areflexia, peripheral neuritis)
paralytic ileus
What are the SEs of vinblastine?
BLAST's Bone Marrow
What is the mechanism of action of Paclitaxel?
M-phase specific agents that bind to tubulin and hyperstabalize it. No anaphase
What is the clinical use of Paclitaxel?
Ovarian and breast cancer
What are the SEs of Paclitaxel
myelosuppression
hypersensitivity