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
Nitrosoureas (-ustines) / Streptozocin
alkylating agent cross-links DNA is bioactivated and crosses the BBB use in gliomablastoma multiforme and other brain tumors can cause CNS toxicity
Busulfan
alkylating agent cross-links DNA use in CML or to ablate BM before transplant SEVERE myelosuppression pulmonary fibrosis hyperpigmentation
Vincristine
microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
can cause neurotoxicity and paralytic ileus
Vinblastine
microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
causes bone marrow suppression
Paclitaxel (taxols)
hyperstabilize tubules --> spindles cannot break down --> cannot progress to anaphase use in ovarian and breast Ca causes myelosuppression alopecia hypersensitivity
Cisplatin
cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis
Carboplatin
cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis
Etoposide
inhib topoisomerase II –> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia
Teniposide
inhib topoisomerase II –> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia
