Pharmacology-Cancer drugs Flashcards
What is azathioprine metabolized into?
6-MP
What is azathioprine activated by?
HGPRT
What is the mechanism of 6-MP/Azathioprine?
Decreases de novo purine synthesis
Indications for azathioprine/6-MP
Prevent organ rejection
RA, IBD, SLE
What enzyme metabolizes azathioprine/6-MP
Xanthine oxidase
What drugs increase toxicity of azathioprine/6-MP
Allopurinol and febuxostat
What are side effects of azathioprine/6-MP?
Myelosuppression, GI, liver
Drug that is a purine analog which inhibits DNA polymerase and causes DNA strand breaks
Cladribine
What is the indication for the purine analog Cladribine?
Hairy cell leukemia
What are the side effects of purine analog Cladribine?
Myelosuppression, nephrotoxicity, and neurotoxicity
Pyrimidine analog that inhibits DNA polymerase and indicated for AML and lymphomas
Cytarabine
Side effects of Cytarabine
Myelosuppression with megaloblastic anemia and pancytopenia
Antimetabolite used topically for treatment of basal cell carcinoma; also used for colon cancer and pancreatic cancer
5-FU
What is the mechanism of 5-FU
Converted to 5-FdUMP which inhibits thymidylate synthase
What is the effect of 5-FU converting to 5-FdUMP and inhibiting thymidylate synthase?
Decreases dTMP causing decreased DNA synthesis
What drug is used to enhance the effects of 5-FU?
Leucovorin
What is the mechanism of methotrexate?
Folic acid analog that inhibits dihydrofolate reductase
What is the effect of methotrexate inhibiting dihydrofolate reductase?
Decreases dTMP causing decreased DNA synthesis
What are side effects of 5-FU?
Myelosuppression and redness, swelling and desquamation of soles and palms
Non-neoplastic indications for methotrexate
Ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis
What drug is used with methotrexate to induce abortions?
Misoprostol
Myelosuppression caused by methotrexate can be reversed with what drug?
Leucovorin
Side effects of methotrexate
Myelosuppression, hepatotoxicity, mouth ulcers, and pulmonary fibrosis
What are the antitumor medications?
Bleomycin, Dactinomycin, and doxorubicin
What antitumor drug induces free radical formation causing DNA strand breaks?
Bleomycin
Which antitumor drug is indicated for testicular cancer and Hodgkin lymphoma?
Bleomycin
What are the side effects of Bleomycin?
Pulmonary fibrosis and skin hyperpigmentation
Antitumor agent indicated for testicular agent that causes minimal myelosuppression
Bleomycin
Antitumor drug that intercalates DNA and causes myelosuppression
Dactinomycin
Antitumor drug indicated for Wilms tumor, Ewing sarcoma, rhabdomyosarcoma and used in childhood tumors
Dactinomycin
Antitumor drug that generates free radicals and intercalates into DNA causing double stranded breaks
Doxorubicin and Daunorubicin
Antitumor drug indicated for solid tumors, leukemias and lymphomas
Doxorubicin and Daunorubicin
Antitumor drug that causes dilate cardiomyopathy
Doxorubicin
Iron chelating agent that is used to prevent cardiotoxicity when using doxorubicin
Dexrazoxane
What are the alkylating agents?
Busulfan, Cyclophosphamide, Nitrosoureas
Alkylating agent used to treat CML and bone marrow ablation which cross-links DNA
Busulfan
Alkylating agent that almost always causes severe myelosuppression, pulmonary fibrosis, and hyperpigmentation
Busulfan
Alkylating agent used for solid tumors, leukemias and lymphomas that cross-links DNA at guanine N-7
Cyclophosphamide
What is used to prevent hemorrhagic cystitis when using cyclophosphamide?
Mesna or N-acetylcysteine
What does cyclophosphamide need before it can have an effect?
Bioactivation by the liver
Side effects of cyclophosphamide
Myelosuppression and hemorrhagic cystitis
Alkylating agent used for brain tumors since the are able to cross the BBB
Nitrosoureas
CNS toxicity resulting in seizures, dizziness and ataxia is seen with which alkylating agent?
Nitrosoureas
What are the microtubule inhibitors?
Paclitaxel, Vincristine and Vinblastine
Microtubule inhibitor used for ovarian and breast carcinomas?
Paclitaxel
What phase in mitosis is stopped by paclitaxel?
Anaphase - stabilizes microtubules so mitotic spindle cannot break down
Side effects of paclitaxel
Myelosuppression, neuropathy, hypersensitivities
Anticancer drug that binds B-tubulin and inhibits polymerization of microtubules preventing mitotic spindle formation
Vincristine or Vinblastine
Anticancer drug indicated for solid tumors and leukemias that binds B-tubulin
Vincristine or Vinblastine
Anticancer drug with neurotoxicity and used for treatment of non-Hodgkin lymphoma that binds B-tubulin
Vincristine
Anticancer drug with used for treatment of Hodgkin lymphoma that binds B-tubulin
Vinblastine
Used to prevent nephrotoxicity when using cisplatin
Amifostine and chloride
Anticancer drug for treatment of testicular, bladder, ovary and lung carcinomas that cross-links DNA
Cisplatin or carboplatin
Cisplatin or carboplatin side effects
Nephrotoxicity, peripheral neuropathy, ototoxicity
Anticancer drug that inhibits topoisomerase II causing DNA degradation
Etoposide and Teniposide
Etoposide and Teniposide side effects
Myelosuppression and alopecia
Anticancer drug that inhibits topoisomerase I preventing unwinding and replication of DNA
Irinotecan, Topotecan
Topoisomerase I inhibitor used for colon cancer
Irinotecan
Topoisomerase I inhibitor used for ovarian and small cell cancers
Topotecan
Anticancer drug that inhibits ribonucleotide reductase decreasing DNA synthesis and is S-phase specific
Hydroxyurea
Anticancer drug that causes severe myelosuppression and used fro myeloproliferative disorders, sickle cell, and melanoma that is S-phase specific
Hydroxyurea
Monoclonal antibody against VEGF which inhibits angiogenesis used for solid tumors
Bevacizumab
Monoclonal antibody used for treatment of colorectal cancer and renal cell carcinoma that causes hemorrhage, blood clots and impaired wound healing
Bevacizumab
EGFR tyrosine kinase inhibitor used for non-small cell lung carcinoma that causes a rash
Erlotinib
Monoclonal antibody against EGFR used for stage IV colorectal cancer and head and neck cancer that causes rash, elevated LFTs and diarrhea
Cetuximab
Tyrosine kinase inhibitor of Bcr-Abl and c-kit use for treatment of CML and GI stromal tumors that cause fluid retention
Imatinib
Monoclonal antibody against CD20 used for non-Hodgkin lymphoma, CLL, TIP, and RA that increases risk of progressive multifocal leukoencephalopathy
Rituximab
Proteosome inhibitors that induce arrest at G2-M phase and apoptosis used in MM and mantle cell lymphoma that cause peripheral neuropathy and herpes zoster reactivation
Bortezomib and Carfilzomib
Selective estrogen receptor blocker used in the treatment of breast cancer that block binding of estrogen to ER positive cells
Tamoxifen
Selective estrogen receptor modulator used for treatment of osteoporosis
Raloxifene
Selective estrogen receptor blocker that is a partial agonist in endometrium which increases the risk of endometrial cancer
Tamoxifen
Estrogen receptor antagonist that is safe to use since it does not increase risk of endometrial cancer and used for treatment of osteoporosis
Raloxifene
What drug is a monoclonal antibody against HER-2 used for the treatment of breast and gastric cancer that causes cardiotoxicity?
Trastuzumab
Small molecule inhibitor of BRAF oncogene positive melanoma used for V600E metastatic melanoma
Vemurafenib
Oncologic emergency triggered by massive tumor lysis
Tumor lysis syndrome
Treatment for Tumor lysis syndrome
Aggressive hydration, allopurinol and rasburicase
Recombinant uricase that catalyzes metabolism of uric acid and used for prevention and treatment of tumor lysis syndrome
Rasburicase