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Anti-neoplastics
Pharmacology
41
Medical
Professional
10/01/2011

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Term
what are the three classes of alkylating agents?
Definition
Nitrogen Mustards
alkyl sulfonates
nitrosureas
Term
5 nitrogen mustards
Definition
mechlorethamine, cyclophosphamide, ifosfamide, melphalan, chlorambucil
Term
alkyl sulfonate
Definition
busulfan
Term
nitrosurease
Definition
BCNU, CCNU, MeCCNU
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
mechlroethamine
Term
This alkylating agent needs to activated by hepatic P450
Definition
cyclophosamide
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
4 antrhacyclines
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
mitoxantrone
Term
Anthracycline isolated from Strep veicillus
Definition
Bleomycin
Term
Bleomycin mech of action
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
Mitomycin C
Term
Side effects of anthracyclines
Definition
Cardiotoxicity (D in middle of chest)
Term
Drug with side effect of pulmonary fibrosis
Definition
bleomycin
Term
Side effect of Dactinomycin
Definition
myelosuppression
Term
Side effects of Mitomycin C
Definition
Late myelosuppression
Term
What are the 3 classes of antimetabolites
Definition
Folic acid analogs
Pyrimidine analogs
Purine analogs
Term
What's the folic acid analog
Definition
methotrexate
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
5FU
Term
This pyrimidine analog can interfere w/DNA replication
Definition
Ara-C
Term
5 Purine analogs
Definition
6-TG
6-MP
Fludarbine
2' deoxycoformycin
2' chlorodeoxyadenosine
Term
Purine analogs that help convert to thioinosine to inhibit A-G
Definition
6-TG and MP
Term
This purine analong inhibits DNA poymerase, primase, and reductase
Definition
Fludarabine
Term
This purine analog blocks adenosine deaminase and inhibits ribonucleotide
Definition
2-deoxycoformycin
Term
antimetabolite that induces hemorrhagic cysitis
Definition
methotrexate
Term
side effect of 5-FU
Definition
mucositis, diarrhea
Term
Fludarabine side effects
Definition
CD4 T cell depletion, peripheral neuropathy
Term
side effect of 2' chlorodeoxyadenosine
Definition
thrombocytopenia
Term
This stabilizes 5FU
Definition
Lecuvorin
Term
Side effect of methotrexate
Definition
hemorrhagic cystitis
Term
side effect of araC
Definition
cerebellar dysfunction
Term
DOC Hairy cell leukemia + Thrombocytopenia
Definition
2' chlordeoxyadenosine
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