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99 Cards in this Set
- Front
- Back
cell cycle activity of chemo Rx
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Mechanism of CA Rx
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CA Chemo
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451 of Katzung
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6 mechanism of CA resistance to rx?
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DNA repair, trapping agents, enzyme morphs, dec activation, inactivation, dec drug accumulation
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What is MDR1 inv in?
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gene for P-gp for accelerated efflux
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Appearance of Sx when tumor gets to what # cells
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10 ^9-10
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Repetitive Tx of same method kills equal
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Fraction of cells; not number
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tumors exhibit what type of growth pattern?
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Gompertzian
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Tx during uppermost part of curve improves?
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Survival, but Sx recur b/t therapy
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In middle part of curve, relationship of tumor kill to growth?
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kill > regrowth -> cure results
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most effective approach at which part of curve?
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bottom
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when is surgery feasible?
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bottom
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chemo is used as
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adjuvant for small mets
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Antimetabolites - list: 5
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5-FU, MTX, cytarabine, mercaptopurine, thioguanine
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Which inh dNTP?
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5-FU, MTX
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Substitute for dNTP (DNA polymerization)?
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cytarabine
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Inh purine synth?
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thioguanine, mercaptopurine
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affect RNA processing, fxn?
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5-FU, MTX, cytarabine
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Antimitotics - list: 4
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Vincristine, vinblastine, paclitaxel, docetazel
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Which drug potentiates 5-FU?
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Leucovorin
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M/A of 5-FU?
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inh thymidylate synthase
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5-FU is the primary chemo agents for
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colon CA
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What's 5-FU prodrug?
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Capecitabine
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What toxicity is in the prodrug and not in 5-FU?
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Hand-foot syndrome (numbess, blistering of palms & soles)
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What's the advantage of the prodrug?
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Less myelosuppression
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M/A of MTX?
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Inh dihydrofolate reductase
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Indications for MTX? 4
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ALL, AML, choriocarcinoma, lung CA
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Difference in indication for 6MP v 6TG?
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MP for children, TG for adults
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What supportive therapy MUST you give with these Rx?
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Allopurinol
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What S-specific drug competitively inh dCTP?
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cytarabine
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Indications for cytarabine?
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AML, AMML
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Most severe toxicity?
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severe myelosuppression
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Difference b/t vin- drugs and -taxel drugs?
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Vin disrupt cytoskeletal structure; Taxel enhance tubulin polymerization
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Vinblastine indication? 1
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Systemic Hodgkin's
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Vincristine's indication?
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Acute leukemia in children
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Palcitaxel's indication? 2
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ovarian CA, advance breast CA
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Docetaxel's indication? 3
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breast, ovary, non-small cell
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Which 2 have acute fx?
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vinblastine, palcitaxel
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Which 2 have delayed fx?
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vincristine, docetaxel
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Categories of alkylating agents? 3
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Nitrogen mustards, nitrosureas, alkylsulfonates
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Which 2 categories act in part like alkylators?
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platinum analagos, carbazines
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Major site of alkylation?
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N7
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2 results of alkylation?
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miscoding by thymine; depurination by guanine excision
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Toxicities of all alkylating agents: 6
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vesicant, acute N/V, myelosuppresion, alopecia, teratogen, carcinogen
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What drug is often admin w/ these drugs b/c of their acute fx?
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Ondansetron b/c of N/V
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Nitrogenous mustards: 3
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cyclophosphamide, chlorambucil, mechlorethamine
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What does cyclophosphamide req for activity?
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P450
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What is the other main use for cyclophosphamide?
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Immune d/o
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3 advantages of cyclophosphamide to mechlorethamine?
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less thrombocytopenia, not vesicant, can be po
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What endocrine d/o is associated w/ cyclophosphamide?
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SIADH
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Which nitrogenous mustard has SLOW fx, and SLOW tox?
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chlorambucil
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Which mustard is given for MM?
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melphalan
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Nitrosureas: 3
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BCNU (carmustine), CCNU (lomustine), methyl-CCNU (semustine)
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Because of their lipophilicity, these Rx are used for?
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Brain tumors
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These alkylate at which position?
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O6
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The only alkyl sulfonate?
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Busulfan
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Primarily used for?
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CML
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Most significant tox?
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Nephrotox from build up of urate (GIVE ALLOPURINOL)
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Why does procarbazine SUCK?
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Strand breaks, Undermines immunity, Carcinogenic, Kills fetus
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Platin drugs (in order of generation): 3
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Cisplatin, carboplatin, oxaliplatin
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Which platin is not cross-resistant to other platins?
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oxaliplatin
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What drugs is ALWAYS given with these?
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Mannitol for renal tox
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What's a unique tox?
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Ototoxicity - tinnitis, hearing loss
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Anthracyclines: 2
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Daunorubicin, doxorubicin
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Main difference b/t the two?
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doxorubicin can also be used for solid tumors
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2 indications for daunorubicin?
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ALL, AML
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Other CA Abx: 4
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dactinomycin, bleomycin, mitoxantrone, mitomycin
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Main drug for pediatric tumors?
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DACTINOMYCIN!!!
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Unusual tox of bleomycin? 2
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pulm, mucocutaneous
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Which is cardiotox?
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Mitoxantrone
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What is weird tox of mitoxantrone?
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Blue discoloration of fingernails, sclera, urine
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Which is used with radiation against hypoxic tumor cells?
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Mitomycin
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2 mechanisms of tamoxifen?
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Blocks binding of ERE, decr IGF-1
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Toxicities? 3
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hot flashes, endometriosis, blood-clotting weirdness
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Mechanism of flutamide?
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Inh androgen-R translocation to nuc
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Toxicities? 4
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dec sex fxn, hot flashes, gynecomastia/mastodynia
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Leuprolide and Goserelin mech?
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Desensitize pit to GnRH -> dec FSH & LH
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This makes them great for treating which 2 CA?
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Prostate, breast
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What do you worry about? 3
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low sex steroid fx: hot flashes, osteoporosis, low muscle mass
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What drug inh aromatase?
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aminoglutethimide
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So what do you think this drug is good for?
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Adrenocarcinomas!
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Aspariginase takes advantage of what?
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Tumors can't make L-asparagine!
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Imatinib is specifically for?
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9;22 bcr-abl CML tyr kinase
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Camptothecins: 2
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Tropotecan, irinotecan
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Mech?
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Inh topoisomerase
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Difference b/t the 2?
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Tropotecan needs good renal; irino needs good liver
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ATRA is CURE for?
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5;17 APL
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Mech?
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Induce maturation
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What works similarly?
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As2O3
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What is the cardiotox with this drug?
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QT prolongation
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Let's name some mabs:
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Cetuximab, trastuzamb, rituximab, bevacizumab
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What well tolerated drug may cause acneiform rash?
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Cetuximab
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Mech?
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EGFR-mab
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What makes this good for?
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Preventing CA 2o to radiation therapy (esp H&N)
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What works similarly?
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Gefitinib, erlotinib
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What also works on EGFR but is used for breast CA?
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Trastuzumab to HER2 (type 2 EGFR)
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Mech of bevacizumab?
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mab to VEGF
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Mech of rituximab?
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mab to CD20
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What drug is a rescuer of norm cells from ROS and superoxide?
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AmifOStine
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