Oncology Flashcards
Interferes with S phase (2)
Antimetabolites
Etoposide
Interferes with G2 phase (2)
Bleomycin
Etoposide
Interferes with M phase (2)
Vinca alkaloids
Taxols
Folic acid analog
Inhibits dihydrofolate reductase
Reduces dTMP, DNA and protein synthesis
Leukemia, lymphoma, choriocarcinoma, sarcomas
Abortion, ectopic pregancy, rheumatoid arthritis, psoriasis
Myelosuppression, macrovesicular fatty change in liver, mucositis, teratogen
Methotrexate
Myelosuppression reversible with leucovorin
Pyrimidine analog
Metabolite 5F-dUMP complexes to folic acid
Inhibits thymidylate synthase
Decreases dTMP, DNA, protein synthesis
Colon cancer, basal cell carcinoma (topical)
Myelosuppression, photosensitivity
5-Fluorouracil (5-FU)
Myelosuppression reversed by thymidine
Pyrimidine analog
Inhibits DNA Pol
Leukemias, lymphomas
SE: leukopenia, thrombocytopenia, megaloblastic anemia
Cytarabine
(arabinofuranosyl cytidine)
Purine analogs (3)
Decreases purine synth
Activated by HGPRT
Leukemias
SE: bone marrow, GI, liver
Metabolized by xanthine oxidase
(What increases toxicity?)
Azathioprine
6-mercaptopurine (6-MP)
6-thioguanine (6-TG)
Allopurinol increases toxicity
Intercalates in DNA
Wilm’s tumor, Ewing’s sarcoma, rhabdomyosarcoma, childhood tumors
SE: myelosuppression
Dactinomycin
(actinomycin D)
Noncovalent interacalation in DNA
Causes breaks in DNA
Generates free radicals
Solid tumors, leukemias, lymphomas
SE: cardiotoxicity (dilated cardiomyopathy), myelosuppression, alopecia, toxic to tissues after extravasation
(What prevents cardiotoxicity?)
Doxorubicin
(Adriamycin)
Daunorubicin
Dexrazoxane prevents cardiotoxicity
(iron chelating agent)
Induces free radical formation
Which causes breaks in DNA
Testicular cancer, Hodgkin’s lymphoma
Pulmonary fibrosis, skin changes
Minimal myelosuppression
Bleomycin
Covalent interstrand crosslinks with DNA
at guanine N-7
Alkylating agent- requires bioactivation
Solid tumors, leukemia, lymphoma, some brain cancers
Myelosuppression, hemorrhagic cystitis
(How to treat hemorrhagic cystitis?)
Cyclophosphamide, ifosfamide
Mesna
(binds toxic metabolites)
Alkylating agent- requires bioactivation
Cross BBB
Brain tumors (inc. GBM)
CNS toxicity (dizziness, ataxia)
Nitrosoureas
Carmustine, lomustine, semustine, streptozocin
Alkylates DNA
CML, bone marrow ablation before transplant
SE: pulmonary fibrosis, hyperpigmentation
Busulfan
Bind tubulin in M phase
Block polymerization, mitotic spindles
Solid tumors, leukemias, lymphomas
(1) areflexia, peripheral neuritis, paralytic ileus
(1) bone marrow suppression
Vincristine
(areflexia, peripheral neuritis, paralytic ileus)
Vinblastine
(bone marrow suppression)
Stabilizes polymerized tubules in M phase
No mitotic spindle breakdown
Ovarian, breast carcinomas
Myelosuppression, hypersensitivity
Paclitaxel
Cross-links DNA
Testicular, bladder, ovary, lung carcinoma
Nephrotoxic, acoustic nerve damage
(How to prevent nephrotoxicity?)
Cisplatin, carboplatin
Amifostine, chloride diuresis
(Prevents nephrotoxicity)
Inhibits topoisomerase II
DNA degradation ensues
Solid tumors, leukemias, lymphomas
Myelosuppression, GI irritation, alopecia
Etoposide, teniposide
Inhibits ribonucleotide reductase
Decreases DNA synthesis (S phase)
Melanoma, CML, sickle cell disease (increase HbF)
Bone marrow suppression, GI upset
Hydroxyurea
Glucocorticoid
May trigger apoptosis
CLL, non-Hodgkin’s lymphoma, immunosuppressant
SE: Cushing’s, immunosuppression, catraracts, acne, osteoporosis, hypertension, peptic ulcers, hyperglycemia, psychosis
Prednisone, prednisolone
Blocks estrogen binding to receptor-positive cells
Antagonist in breast, agonist in bone
Breast cancer treatment/prevention,
osteoporosis prevention
(2) Which increases risk of endometrial cancer?
Tamoxifen, raloxifene
Tamoxifen increases risk of endometrial cancer, can give hot flashes
Raloxifene is endometrial antagonist
Monoclonal antibody against HER2
(a tyrosine kinase)
HER-2 positive breast cancer
SE: cardiotoxicity
Trastuzumab
(Herceptin)
bcr-abl tyrosine kinase inhibitor
(Philadelphia chromosome)
CML, GI stromal tumors
SE: fluid retention
Imatinib
(Gleevec)
Monoclonal antibody to CD20
Non-Hodgkin’s lymphoma, rheumatoid arthritis
Rituximab
(w/ methotrexate for RA)
Inhibits B-Raf kinase w/V600E mutation
Metastatic melanoma
Vemurafenib
Monoclonal antibody to VEGF
(inhibits angiogenesis)
Solid tumors
Bevacizumab
Acoustic nerve damage
Cisplatin, carboplatin
Peripheral neuropathy
Vincristine
Pulmonary fibrosis (2)
Bleomycin, busulfan
Cardiotoxicity (2)
Doxorubicin
Trastuzumab
Nephrotoxicity
Cisplatin, carboplatin
Hemorrhagic cystitis
Cyclophosphamide
Myelosuppression
(3 antimetabolites)
5-FU
6-MP
Methotrexate
