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What's the characteristic of Class 1 Chemo Agents?
Kill cells regardless of state of proliferation
What's the characteristic of Class 2 chemo agents?
Kill cells in a specific phase of cell cycle; plateau proportional to fraction not at stage
What's the characteristic of Class 3 chemo drugs?
Non-cycle specific
More effective against proliferating cells
What are chemo drugs' effectiveness dependent on?
Concentration and time of exposure
What chemo class are Alkylating agents?
Class III (no specific phase)
What's the mechanism of alkylating agents?
Induce DNA damage or p53 mediated apoptosis
What's the specific mechanism of action of Nitrogen Mustards?
Alkylation of DNA at N-7 position of guanine
Misreading of DNA replication
What is Mechlorethamine?
Nitrogen Mustard Alkylating Agent
What is Melphalan?
Nitrogen Mustart Alylating agent
Oral stable
What's Chlorambucil?
Nitrogen Mustard Alkylating Agent
What's Cyclophosphamide?
Nitrogen Mustard Alkylating Agent
CYP450 Activation
What SE come from Cyclophosphamide?
Hepatotoxicity
Pulmonary Fibrosis
What's Busulfran? (MoA & SE)
Alkylsulfonate Alkylating Agent
Granulocytopenia
What's Carmustine? (MoA & SE)
Nitrosourea Alkylating Agent
Lipid soluble -> CNS & delayed/severe BM&pulmonary fibrosis
What's Cisplatin? (MoA & SE)
Platinum Complex Alkylating Agent
MoA
: Covalent bonds to plasma proteins
SE
: Nephrotoxicity
What's Oxaliplatin? (MoA & SE)
Cisplatin analogue (AA)
SE
: not cross resistant
What's Carboplatin? (MoA & SE)
Cisplatin Analogue (AA)
Less renal toxicity
What's vincristine?
Vinca Alkaloid
MoA
: inhibit spindle fiber mitosis/cytoskeletal movement
SE
: Neurotoxicity
What's vinblastine?
Vinca Alkaloid
MoA
: inhibit spindle fiber mitosis/cytoskeletal movement
SE
: less neurotoxicity; granulocytopenia
What's Paclitaxel?
Taxane
MoA
: inhibits dissasembly of microtubules during mitosis
SE
: cardiotoxic
What's Docetaxel?
Paclitaxel Analogue
MoA
: inhibits dissasembly of microtubules during mitosis
SE
: cardiotoxic
What's etoposide?
Epipodophyllotoxin
Inhibition of topoisomerase II
What's teniposide?
Epipodophyllotoxin
Inhibition of topoisomerase II
What's Irinotecan?
Inhibition of Topoisomerase I
What's topotecan?
Inhibition of Topoisomerase I
What's Dactinomycin? (MoA & SE)
Antibiotic
Intercalates between G:C
Low conc
: inhibit RNA synthesis
High conc
: inhibit RNA & DNA synthesis
SE
: radiation sensitization
What's Daunorubicin?
MoA
: DNA intercalation & single stratnded breaks
SE
: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
What's Dexrazoxane?
Inhibits ROS to reduce cardiotoxicity from Daunorubicin/doxorubicin
What's doxorubicin?
MoA
: DNA intercalation & single stratnded breaks
SE
: Cumulative cardiotoxicity (lack of superoxide dismutase to fix ROS)
What's Bleomycin? (MoA/SE)
MoA
: DNA/Fe binding => single/double stranded breaks
SE
: pneumonitis with oxygen reaction
What's the mechanism of resistance for Bleomycin?
Bleomycin hydrolase -> inactivation of drug
What's Methotrexate (MoA)
Folic Acid analogue -> competative inhibition of DHFR
Block dUMP-> dTMP DNA synthesis
Block FH
4
co-factor rxns
What's the mechanism of resistance for Methotrexate?
Increased DHFR activity
What's the toxicity of Methotrexate?
Low
: Myelosuppression
High
: Mylosuppression, renal & liver toxicity
What's Leucovorin?
Abort MTX tocity by supplying already reduced folate to cells (bypass DHFR)
What's 5-Fluorouracil?
Metabolized to 5-FdUMP in cell
Suicide inhibitor of thymidylate synthase
Defective RNA synthesis
What's the mechanism of resistance to 5-Fluorouracil?
Overexpression of TS
What's capecitabine?
5-FU prodrug selectively activated in target cell
What's azacitidine?
Pyrimidine Analogue
Inhibit DNA methyltransferase; inhibited RNA
What's 6-mercaptopurine? (MoA/Resistance)
MoA
: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
Resistance
: HPRT mutations
What's 6-thioguanine?
MoA
: inhibit de novo purine synthesis -> inhibit biosynthetic reactions
Resistance
: HPRT mutations
What's asparaginase?
MoA
: Deprivation of asparagine (-> aspartate)
SE
: reduction on concentration of proteins (albumin, clotting, insulin); HS, hepatotoxicity
What's imatinib mesylate? (MoA/SE)
Competatively blocks ATP binding site of c-abl kinase
SE
: CHF
What's erlotinib/gefitinib? (MoA/SE)
Inhibitors of EGF receptor associated tyrosine kinase
SE
: CHF
What's Cetuximab?
Antibody against EGF receptor
What's trantuzumab?
Ab against VGEF
Anti-angiogenesis
SE
: increased Thromboembolic events
What's rituximab?
anti CD-20 against B-cells
What's gemtuzumab/ozogamin?
Ab against CD33
What's vorinostat?
histone deacetylase inhibitor
What's bortezomib?
proteasome inhibitor
What's all-trans-retinoic acid?
Vitamin a
Author
eschott
ID
82256
Card Set
Chemo Drugs
Description
stuff
Updated
2011-04-27T15:18:55Z
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