Term
| antifolates are what kind of class |
|
Definition
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|
Term
| specificity for cell phases means max effect on _ phase and none on- |
|
Definition
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|
Term
| advtg of cell cycle specific drugs-3 |
|
Definition
inhibiton of DNA/RNA at clincal dose
plateua cell sruvial wiht increase dose
minimal leukogeneisis/carincogenesis |
|
|
Term
| disadvtg of cell pahse specific drugs-2 |
|
Definition
fewer targets
little effect on slow grow/stem cells |
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Term
| what are the antimetabolits of the CCS group-3 |
|
Definition
antifolates
purines
pyrimidines |
|
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Term
|
Definition
|
|
Term
| antimetabolites work bc they are struct similar to- |
|
Definition
| DNA/RNA synth intermediates |
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Term
| antimetabolites affect _ synth, and tumor cells are more suscpetible bc |
|
Definition
nucleic acid
they are dividing more |
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|
Term
| folic acid is which vitamin |
|
Definition
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|
Term
| folic acid is used in what base conversion |
|
Definition
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|
Term
| folic acid is struct similar to |
|
Definition
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|
Term
| MTX and aminopterin inhibit |
|
Definition
|
|
Term
| what does methotrexate inhibit-3 |
|
Definition
purine synth (RNA/DNA)
thymidine (tMP) synth
methionine, serine, f-met (proteins_ |
|
|
Term
| MTX binds to- so it inhibits synth of |
|
Definition
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|
Term
| cancers not sensitive to MTX-3 |
|
Definition
acute myelo leukemia
colon
renal |
|
|
Term
| cancers sensitive to MTX-4 |
|
Definition
acute lymph leukemia
nurkitts
choriocarcin
diffuse lympohma |
|
|
Term
| cytotoxic effect of MTX is mediated by- |
|
Definition
|
|
Term
| what metab MTX into cytotoxic form |
|
Definition
| folypolygutamyl synthetase |
|
|
Term
polyglutamation is _ depenednet (2)
it occurs in tumor and less in nromal cells |
|
Definition
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|
Term
| the MTX ->plyglut probbaly account for selective activity of the drug as this is 80% in tumors |
|
Definition
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|
Term
| MTX eliminated primary in |
|
Definition
|
|
Term
|
Definition
| IM, oral, IV, intrathecal |
|
|
Term
|
Definition
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|
Term
| when giving dose of MTX >1000, pt needs to:3 |
|
Definition
hydrate
void with specific grav <1.01
alkaline urin Ph> 7.5 |
|
|
Term
| nephortox of MTX increases with UO<100 and pH<6.5* |
|
Definition
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|
Term
| counseling for MTX and NSAID within 36 hrs: -3 |
|
Definition
| will cause renal, meylo suppres, mucositis |
|
|
Term
| what drug slow MTX elmin and prolongs leucovorin-3 |
|
Definition
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|
Term
ADEs of MTX-4
what is a reversible on? |
|
Definition
stomatitis
nepho, headache, meylo
hepatox |
|
|
Term
| MTX plasma levels monitored until <0.05 and kidney funct why? |
|
Definition
| bc PK have high variability |
|
|
Term
| systemic tox of MTX correlates with |
|
Definition
|
|
Term
Leucovorin rescue dose adjusted to-
when is it stoppedd? |
|
Definition
|
|
Term
time after dose MTX:
24 hrs, desired level?
48?
72? |
|
Definition
|
|
Term
| resistance methods for MTX-4 |
|
Definition
transport
DHFR expression
altered DHFR
polyglut sythn |
|
|
Term
| DHFR amplificaiton is common tumor resistance * |
|
Definition
|
|
Term
| toxicity of MTX can be reversed by admin- how? |
|
Definition
reduced folate
doesnt need DHFR activation |
|
|
Term
| leuvocorin is converted to _ which bypasses the inhibited MTX reductase |
|
Definition
|
|
Term
Leuvocorin is used when-
how mnay hrs afterr MTX dose? |
|
Definition
MTX dose exceed 10-100 x conventional dose
24-36 hr |
|
|
Term
|
Definition
able to use high MTX dose
reduced toxic effects
folate cofactors |
|
|
Term
what is the multi target antifolate drug?
what are its 3 enzymes it inhibits? |
|
Definition
pemetrexed
thymidylate synthase
dihydrofolate reductase
GARFT (glycin ribo formyltransferase) |
|
|
Term
| pemetrexed prevents formaiton of |
|
Definition
|
|
Term
|
Definition
mesothelioma
non small cell lung cancer |
|
|
Term
| toxicity most common wiht antimetab-3 |
|
Definition
| nausea, mucositis, myelosupp |
|
|
Term
toxicty with chronic methotrexate
tox with high dose methotex |
|
Definition
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