Chemotherapy Flashcards
MTX
S-specific
folic acid analog –> inhib DHFR
dec dTMP –> dec DNA and protein synthesis
SE: myelosuppression –> leucovorin rescue
liver macrovesicular fatty changes
mucositis
teratogenic
Neoplastic uses of MTX
leukemias
lymphomas
choriocarcinoma
sarcoma
Non-neoplastic uses of MTX
abortion ectopic prego RA psoriasis IBD
5-FU
S-specific
pyrimidine analog –> activates to 5F-dUMP –> complexes folic acid
complex inhibits thymidylate synthase (dec dTMP)
SE: myelosuppression –> not revers by leucovorin
overdose: rescue with uridine
photosensitivity
Uses of 5-FU
colone cancer
pancreatic cancer
basal cell Ca (topical)
Cytarabine
S-specific Pyrimidine analog --> inhib DNA pol SE: leukopenia thrombocytopenia megaloblastic anemia use for leukemias and lymphomas
Azathioprine, 6-mercaptopurine
S-specific
purine analog –> activated by HGPRT –> dec de novo purine synthesis
use in preventing organ rejection
RA
SLE (azathioprine)
leukemia
IBD (6-MP)
metal by XO –> inc toxicity with allopurinol
also has bone marrow, liver, and GI toxicity
6-thioguanine (6-TG)
S-specific
purine analog –> activated by HGPRT –> dec de novo purine synthesis
use in IBD and leukemia
Actinomycin D
intercalates DNA use in Wilms tumor Ewing sarcoma rhabdomyosarcoma (basically childhood tumors) can cause myelosuppression
Doxorubicin
generates free radicals
intercalates DNA –> causes breaks –> dec replication
use in solid tumors, leukemias and lymphomas
Doxorubicin SE
CARDIOTOXIC –> dilated cardiomyopathy
use DEXRAZOXANE (iron chelator) to prevent myopathy
myelosuppression
alopecia
Bleomycin
induces free radical formation –> DNA strand breaks
use in testicular cancer and Hodgkin lymphoma
can cause PULMONARY FIBROSIS
skin changes
mucositis
MINIMAL myelosuppression
Cyclosphosphamide
alkylating agent --> X-link DNA at guanine n-7 requires hepatic bioactivation use in solid tumors lymphomas some brain cancers
Cyclophosphamide SE
myelosuppression
hemorrhagic cystitis
can be partially prevented by MENSA
same for ifosfamide
Ifosfamide
alkylating agent --> X-link DNA at guanine n-7 requires hepatic bioactivation use in solid tumors lymphomas some brain cancers