Cancer Drugs Flashcards
Inhibits DHF reductase of pyrimidine synthesis
Methotrexate
Three uses for MTX
1) Anti-cancer: leukemias (ALL), lymphomas, sarcomas
2) Uterine pathology: Hydatidiform mole, choriocarcinoma
3) Immunosuppression: RA and psoriasis
What rescues MTX and from what?
Leucovorin allows for the myelosuppresion of MTX to be reversible
Derivative of THF which bypasses the inhibited DHF reductase
Bone marrow suppression
Pulmonary toxicity
Tetratogenic
MTX
Inhibits thymidylate synthase
5-Fluorouracil
Used for colon cancer, pancreatic cancer, basal cell carcinoma and actinic keratosis
5-Fluorouracil
What rescues 5-FU and from what?
Uridine rescues F-FU from bone marrow suppression
Photosensitivity
5-FU
What other drugs act at the same spot as MTX?
TMP
Inhibits DNA polymerase as a pyrimidine analog
Cytarabine
Inhibits PRPP amidotransferase portion of purine synthesis
6-Mercaptopurine
6-Thioguanine
Azathioprine
This will increase 6-Mercaptopurine toxicity
Name the drug, the enzyme and the toxicity
6-MP is metabolized by xanthine oxidase
Allopurinol (gout drug) inhibits xanthine oxidase and will increase myelosuppression
What drug is metabolized by xanthine oxidase and what drug in the same class isn’t?
6-MP metabolized by xanthine oxidase
6-thioguanine is not! (can be coadmistered with allopurinol)
Induces free radical formation causing breaks in DNA strands
Bleomycin
Pulmonary fibrosis
MTX (pulm tox)
Bleomycin
Busulfan
Dactinomycin MOA
Intercalates DNA
Used to tx rhabdomyosarcoma, Wilm’s tumor and Ewing sarcoma
Dactinomycin
“kids ACT out give them dACTinomycin”
Generate free radicals
Intercalate into DNA
Doxorubicin
Daunorubicin
(Anthracyclines)
Cardiotoxicity
Anthracyclines (Doxorubicin Daunorubicin)
What saves Anthracyclines and from what
Using Dexrazoxane with doxorubicin/daunarubicin acts to decrease free radical formation and thus cardiotoxicity
Why is the mechanism of cardiotoxicity?
doxorubicin/daunarubicin create oxygen free radical sad the heart is suspceptible to free radical damage due to decreased superoxide dismutase
Alkylating agents (4)
Busulfan
Cyclophosphamide
Nitrosureas (Carmustine)
Cisplatin
What drug requires liver bioactivation?
Cyclophosphamide
What cancer drug is also used in immunosuppression in lupus nephritis and polyarteritis nodosa?
Cyclophosphamide
Increased risk of transitional cell cancer of bladder
Cyclophosphamide
What rescues cyclophosphamide and from what
MESNA recues cyclophosphamide from hemorrhagic cystitis due to acrolein (metabolite accumulation)
What causes hemorrhagic cystitis and in what drug is this seen?
Acrolein
Cyclophosphamide
What is sodium 2-mercaptoethan sulfonate
Mesna which rescues cyclophosphamide from producing hemorrhagic cystitis
Used to tx brain tumors
Nitrosureas
Carmustine
Lomustine
Semustine
Crosses BBB causing CNS toxicity
Nitrosoureas
Carmustine
Lomustine
Semustine
General side effects of cancer drugs
Alopecia
GI upset
Myelosuppresion
(All rapidly dividing cells)
Causes hypersensitivity reactions
Paclitaxel
Hyperstabalizes microtubules
Paclitaxel
Tx ovarian and breast cancer
Paclitaxel
Tx ALL NH lymphomas, Hodgkin lymphomas, Wilms tumors Ewing sarcoma and Choriocarcinoma
Vincristine/Vinblastine
SE peripheral neuropathy neurotoxicity and bone marrow suppressions
Vincristine/Vinblastine
Tx GU tumors (testicular, ovarian, bladder)
Cisplatin
Causes ototoxicity/nephrotoxicity
Cisplatin
Inhibits topoisomerase 2
Etoposide
Teniposide
Tx small cell lung cancer and testicular cancer
Etoposide
Inhibits topoisomerase 1
Irinotecan
Topotecan
Inhibits ribonucleotide reductase
Hydroxyurea
Also tx sickle cell disease
Hydroxyurea
Testicular Cancer Tx
“Eradicate Ball Cancer”
Etoposide
Bleomycin (Ifosfamide)
Cisplatin
Triggers apoptosis of lymphoid cells
Prednisone
SE Cushingoid Sx
Prednisone
Monoclonal Ab against VEGF
Bevacizumab
“Bev bleeds monthly”
SE hemorrhage and impaired wound healing
Bevacizumab
“Bev bleeds monthly”
Tyrosine kinase inhibitor of BRC-ABL
Imatinib
Tx CML
Imatinib
inhibitor of BRC-ABL
Monoclonab Ab to CD20
Rituximab
Increased risk of endometrial cancer
Tamoxifen
Used to tx osteoporosis
Raloxifene
Doesn’t increase risk of endometrial cancer
Ralofxifene
Estrogen receptor antagonist used to tx breast cancer
Tamoxifen
SE Cardiotoxicity
Doxorubicin
Trastuzumab
“Herceptin hurts the heart”
Monoclonal Ab against HER-2
Trastuzumab
Herceptin
Myelosuppresion
5-FU
6-MP
MTX