Term
what are the three classes of alkylating agents? |
|
Definition
Nitrogen Mustards alkyl sulfonates nitrosureas |
|
|
Term
|
Definition
mechlorethamine, cyclophosphamide, ifosfamide, melphalan, chlorambucil |
|
|
Term
|
Definition
|
|
Term
|
Definition
|
|
Term
2 properties of alkylating agents |
|
Definition
mispairing of DNA bases (G binds with T) causing point mutation.
cross-linking (covalent link b/t DNA and proteins) |
|
|
Term
what is the effect of alkylating agents? |
|
Definition
proliferating cells. (not cytotoxic per se) |
|
|
Term
This alkylating agent is the least stable, rapidly metabolized |
|
Definition
|
|
Term
This alkylating agent needs to activated by hepatic P450 |
|
Definition
|
|
Term
method of activation of cyclophosphamide |
|
Definition
cyclo-->OHcyclo-->aldophos-->phosphoramide + acrolein |
|
|
Term
side effects of alkylating agents |
|
Definition
myelosuppression hemorrhagic cystitis sterility secondary leukemia |
|
|
Term
|
Definition
daunorubicine, doxorubicin, idarubicin, mitoxantrone |
|
|
Term
Mech of Action for Anthracyclines |
|
Definition
react with P450 to generate free radicals (requres presence of Iron) intercalate into DNA (TOPO II inhibitors!) |
|
|
Term
This anthracycline produces fewer free radicals |
|
Definition
|
|
Term
Anthracycline isolated from Strep veicillus |
|
Definition
|
|
Term
|
Definition
free radical formation inducing DNA strand breaks |
|
|
Term
Dactinomycin mech of action |
|
Definition
intercalates b/t G-C pairs, blocking RNA polymerase |
|
|
Term
This drug alkylates DNA at the N6 of adenine and the N7 of guanine |
|
Definition
|
|
Term
Side effects of anthracyclines |
|
Definition
Cardiotoxicity (D in middle of chest) |
|
|
Term
Drug with side effect of pulmonary fibrosis |
|
Definition
|
|
Term
Side effect of Dactinomycin |
|
Definition
|
|
Term
Side effects of Mitomycin C |
|
Definition
|
|
Term
What are the 3 classes of antimetabolites |
|
Definition
Folic acid analogs Pyrimidine analogs Purine analogs |
|
|
Term
What's the folic acid analog |
|
Definition
|
|
Term
what does methotrexate require for cytotoxic activity |
|
Definition
FPGS leading to depletion of critical folates |
|
|
Term
Mech of Act. for methotrexate |
|
Definition
inhibits DHFR and DNA and protein synthesis
thymidylate and purine synthesis |
|
|
Term
These are the pyrimidine analogs |
|
Definition
5-FU ara-C 2,2-difluorodeoxycytidine |
|
|
Term
Pyrimidine analog mech of action |
|
Definition
inhibit conversion of orotic acid to UMP can be incorporated in either DNA or RNA |
|
|
Term
This pyrimidine analog causes inhibition of thymidine synthesis |
|
Definition
|
|
Term
This pyrimidine analog can interfere w/DNA replication |
|
Definition
|
|
Term
|
Definition
6-TG 6-MP Fludarbine 2' deoxycoformycin 2' chlorodeoxyadenosine |
|
|
Term
Purine analogs that help convert to thioinosine to inhibit A-G |
|
Definition
|
|
Term
This purine analong inhibits DNA poymerase, primase, and reductase |
|
Definition
|
|
Term
This purine analog blocks adenosine deaminase and inhibits ribonucleotide |
|
Definition
|
|
Term
antimetabolite that induces hemorrhagic cysitis |
|
Definition
|
|
Term
|
Definition
|
|
Term
|
Definition
CD4 T cell depletion, peripheral neuropathy |
|
|
Term
side effect of 2' chlorodeoxyadenosine |
|
Definition
|
|
Term
|
Definition
|
|
Term
Side effect of methotrexate |
|
Definition
|
|
Term
|
Definition
|
|
Term
DOC Hairy cell leukemia + Thrombocytopenia |
|
Definition
|
|