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Chemo drugs 3

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britt611's version from 2017-01-19 17:28

Section 1

Question Answer
What is the structure of antimetabolites similar to?similar to metabolist but they cant be used by the cell
What do antimetabolites interfer with?production of the nucleic acids, RNA and DNA
How do antimetabolites enter the cell?via specific active transporters (nucleosides or faciliated)
What phase to antimetabolites predominantly effect?S phase
What are 3 groups of anitmetabolites?folate antagonist, purine analogs, pyrimidine analogs
What are 3 examples of antimetabolities?Cystosin Arabinoside (cytarabine), 5-Fluorouracil, Gemcitabine
What do antimicrotubule agents interfer with?interfer with polymerization or depolymrization of the microtubules (M phase)
What are 2 examples of antimicrotubule agents?vincristine, vinblastin
What is an example of a miscellaneous drug?L-asparaginase
What is an example of targeted therapies?tyrosine kinase inhibitors
What are 2 examples of tyrosine kinase inhibitors?1. toceranib (palladia) 2. Masitinib (kinavet)
What vaccine is used for iummunotherapy?melanoma vaccine
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Section 2

Question Answer
What does cytosine Arabinoside (cytarabine) act as an analog for?deoxycytidine
After phosphorylation in the cell what does cytosine Arabinoside (cytarabine) act as?DNA polymerase alpha inhibitor
What is cytosine Arabinoside (cytarabine) main mechanisms of toxicity?Incorporate to DNA
How does cytosine Arabinoside (cytarabine) get into cells?active transport via a nucleoside transporter
how is cytosine Arabinoside (cytarabine) given?IV or SQ
Does cytosine Arabinoside (cytarabine) cross the BBB? YES
Describe cytosine Arabinoside (cytarabine) half lifevery short half life- need to be given as a CRI- longer its infused the better the therapeutic effect and higher the toxicity
What is the dose limiting toxicty of cytosine Arabinoside (cytarabine) myelosupression and GI (not common)
What is the clinical use of cytosine Arabinoside (cytarabine) Lymphoma, leukemia, menigoencephalities
5-Fluorouracil is an analog of what?uracil
how does 5-Fluorouracil enter the cell?co-facilitated transported (adenine)
What does activation of 5-Fluorouracil cause?thymidines and deoxy uridine depletion which interfers with DNA and RNA synthesis and integrity
how is 5-Fluorouracil given?IV - mostly metabolites by liver
Which 2 drugs should you never give to cats5-Fluorouracil (causes fatal CNS toxicity) and cisplatin!!
What does 5-Fluorouracil cause to cats?fatal CNS toxicty- NEVER GIVE TO CATS
What is the dose limiting toxicity of 5-Fluorouracilmyelosupprsion, GI, neurotoxicity (dogs)
what is the clinical use of 5-Fluorouracilcarcinoma (also bladder cancer)
How does Gemcitabine get into cells? actively transported by nucleoside transporters
What is Gemcitabine function?inhibition of DNA polymerase, depletion of deoxyribonucleotide pools
What is the function of Gemcitabine active moleculedFdCDP is incroporated into DNA leading to strand termination
How is Gemcitabine given?IV- longer infusion increase cellular uptake
What is the dose limiting toxicity of Gemcitabinebone marrow suppression
What is the clinical use of Gemcitabinecarcinomas
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Section 3

Question Answer
How does vincristin and vinblastin work?disruption of mitotic spinds
how does vincristin and vinblastin enter cells?by passive diffusion
how is vincristin and vinblastin given?IV- IRRITANT! can cause extravastion
where is vincristin and vinblastin metabolised and exreted?liver and 90% excretion
what is the dose limiting toxicity of vincristin and vinblastinGI influding ileus and peripheral neurotoxicity
What is the clinical use of vincristine?Lymphoma (CHOP), immune mediated, thrombocytopenia
What is the clinical use of vinblastine?mast cell tumor
what are the drug resistances seen in vincristin and vinblastin?MDR1 (PgP) up regulation and mutation o microtubule targets
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Section 4

Question Answer
What does hydrolysis of L asparagine to L aspartic acid reduce?availability of L-asparagine in circulation and as result protein synthesis
What can malignant lymphoblast not produce?L-asparagine- so they are most sensitive to enzymatic effect
does L-asparaginease induce bone marrow suppression?NO!
How is L- asparaginease given?IV or SQ
What is the dose limiting toxicity of L-asparaginase?hypersensitivity
how do you prevent hypersensitive reaction when using L-asparaginase?give antihistamine and dexamethasone
What is the clinical use of L-asparaginase?lymphoma rescue
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Section 5

Question Answer
philadelphia chormosome is expressed on what?95% of patients with chronic myeloid leukemia, which activates BCR-ABL tyrosine kinase
Why was imatinib (Gleevec) developed?to prevent the continues activation of BCR-ABL
What is the function of tyrosine kinase inhibitor?binds to the ATP activation cassette at the BCL kinase and prevent phosphorylation
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Section 6

Question Answer
Toceranib (Palladia) targets which receptor?C-kit receptor
where is C-kit receptor expressed?Marrow stem cells, melanocytes, cell of Cajal in gut
How is C-kit receptor normally activated?by initiation of stem cell factor (SCF)
what type of inhibitor is Toceranib (Palladia)tyrosine kinase inhibitor
High grade MST may have a mutation at ___, which results in ___Exon 11, results in a constant activation of C-kit receptors at the juxtamembrane region
Toceranib (Palladia) is FDA approved drug for what?Mast cell tumor
how is Toceranib (Palladia) given?oral - 3x a week
What does Toceranib (Palladia) target?C-kit, PDGFR, VEGFR-II
What is the dose limiting toxicity of Toceranib (Palladia)GI, Bone marrow suppresion, proteinuria
What is the clinical use of Toceranib (Palladia)?MST, Gastro intestinal stromal tumor (GIST), metronomic,
How does the cancer become resistant to Toceranib (Palladia)?second mutation at target
Masitinib (kinavet) is what type of inhibitor?tyrosine kinase inhibitor
how is Masitinib (kinavet) given?oral- 5x a wekk
What does Masitinib (kinavet) target?same mutation as palladia - C-kit mutation
What is the dose limiting toxicyt of Masitinib (kinavet)?GI, myelosuprresion, proteinuria
What is the clinical use of Masitinib (kinavet)?MST
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Section 7

Question Answer
What type of vaccine is melanoma vaccine?Xenogenic DNA vaccine
What is the antigen of interest of melanoma vaccineit is cloned into a bacterial plasmid with a constiutively active promotor
how is the plasmid of Melanoma vaccine introduced?to the skin or muscle and induces an immune response
What does the Melanoma vaccine in canines target?target gene is human tyrosinase which is a glycoprotein essential for melanin synthesis
What does the prognosis of melanoma dependent on?on the proliferative markers, not the vaccine treatment
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