Pharmacology-Cancer drugs

Question 1

Which drugs target nucleotide sequence?

Answer 1

MTX, 5-FU: decrease thymidine synthesis
6-MP: decreases de novo purine synthesis
Hydroxyurea: inhibits ribonucleotide reductase

Question 2

Which drugs target DNA?

Answer 2

Alkylating agents, Pt agents: cross-link DNA
Bleomycin: DNA strand breaks
Dactinomycin, Doxorubicin: DNA intercalators
Etoposide/Teniposide: inhibit topoisomerase II
Irinotecan/Topotecan: inhibit topoisomerase I

Question 3

Which drugs target cellular division?

Answer 3

Vinca alkaloids: inhibit microtubule assembly

Paclitaxel: inhibits microtubule assembly

Question 4

What is azathioprine metabolized into?

Answer 4

6-MP

Question 5

What is azathioprine activated by?

Answer 5

HGPRT

Question 6

What is the mechanism of 6-MP/Azathioprine?

Answer 6

Decreases de novo purine synthesis

Question 7

Indications for azathioprine/6-MP

Answer 7

Prevent organ rejection

RA, IBD, SLE

Question 8

Antimetabolite used to wean patients off steroids in chronic disease and to treat steroid refractory chronic disease

Answer 8

Azathioprine/6-MP

Question 9

What enzyme metabolizes azathioprine/6-MP

Answer 9

Xanthine oxidase

Question 10

What drugs increase toxicity of azathioprine/6-MP

Answer 10

Allopurinol and febuxostat

Question 11

What are side effects of azathioprine/6-MP?

Answer 11

Myelosuppression, GI, liver

Question 12

Drug that is a purine analog which inhibits DNA polymerase and causes DNA strand breaks

Answer 12

Cladribine

Question 13

What is the indication for the purine analog Cladribine?

Answer 13

Hairy cell leukemia

Question 14

What are the side effects of purine analog Cladribine?

Answer 14

Myelosuppression, nephrotoxicity, and neurotoxicity

Question 15

Pyrimidine analog that inhibits DNA polymerase and indicated for AML and lymphomas

Answer 15

Cytarabine

Question 16

Side effects of Cytarabine

Answer 16

Myelosuppression with megaloblastic anemia and pancytopenia

Question 17

Antimetabolite used topically for treatment of basal cell carcinoma; also used for colon cancer and pancreatic cancer

Answer 17

5-FU

Question 18

What is the mechanism of 5-FU

Answer 18

Converted to 5-FdUMP which inhibits thymidylate synthase

Question 19

What is the effect of 5-FU converting to 5-FdUMP and inhibiting thymidylate synthase?

Answer 19

Decreases dTMP causing decreased DNA synthesis

Question 20

What drug is used to enhance the effects of 5-FU?

Answer 20

Leucovorin

Question 21

What is the mechanism of methotrexate?

Answer 21

Folic acid analog that inhibits dihydrofolate reductase

Question 22

What is the effect of methotrexate inhibiting dihydrofolate reductase?

Answer 22

Decreases dTMP causing decreased DNA synthesis

Question 23

What are side effects of 5-FU?

Answer 23

Myelosuppression and redness, swelling and desquamation of soles and palms

Question 24

Cancers treated by methotrexate

Answer 24

Leukemias (ALL), lymphomas, carcinomas, and sarcomas

Question 25

Non-neoplastic indications for methotrexate

Answer 25

Ectopic pregnancy, medical abortion, RA, psoriasis, IBD, vasculitis

Question 26

What drug is used with methotrexate to induce abortions?

Answer 26

Misoprostol

Question 27

Myelosuppression caused by methotrexate can be reversed with what drug?

Answer 27

Leucovorin

Question 28

Side effects of methotrexate

Answer 28

Myelosuppression, hepatotoxicity, mouth ulcers, and pulmonary fibrosis

Question 29

What are the antitumor medications?

Answer 29

Bleomycin, Dactinomycin, and doxorubicin

Question 30

What antitumor drug induces free radical formation causing DNA strand breaks?

Answer 30

Bleomycin

Question 31

Which antitumor drug is indicated for testicular cancer and Hodgkin lymphoma?

Answer 31

Bleomycin

Question 32

What are the side effects of Bleomycin?

Answer 32

Pulmonary fibrosis and skin hyperpigmentation

Question 33

Antitumor agent indicated for testicular agent that causes minimal myelosuppression

Answer 33

Bleomycin

Question 34

Antitumor drug that intercalates DNA and causes myelosuppression

Answer 34

Dactinomycin

Question 35

Antitumor drug indicated for Wilms tumor, Ewing sarcoma, rhabdomyosarcoma and used in childhood tumors

Answer 35

Dactinomycin

Question 36

Antitumor drug that generates free radicals and intercalates into DNA causing double stranded breaks

Answer 36

Doxorubicin and Daunorubicin

Question 37

Antitumor drug indicated for solid tumors, leukemias and lymphomas

Answer 37

Doxorubicin and Daunorubicin

Question 38

Antitumor drug that causes dilate cardiomyopathy

Answer 38

Doxorubicin

Question 39

Iron chelating agent that is used to prevent cardiotoxicity when using doxorubicin

Answer 39

Dexrazoxane

Question 40

What are the alkylating agents?

Answer 40

Busulfan, Cyclophosphamide, Nitrosoureas

Question 41

Alkylating agent used to treat CML and bone marrow ablation which cross-links DNA

Answer 41

Busulfan

Question 42

Alkylating agent that almost always causes severe myelosuppression, pulmonary fibrosis, and hyperpigmentation

Answer 42

Busulfan

Question 43

Alkylating agent used for solid tumors, leukemias and lymphomas that cross-links DNA at guanine N-7

Answer 43

Cyclophosphamide

Question 44

What is used to prevent hemorrhagic cystitis when using cyclophosphamide?

Answer 44

Mesna or N-acetylcysteine

Question 45

What does cyclophosphamide need before it can have an effect?

Answer 45

Bioactivation by the liver

Question 46

Side effects of cyclophosphamide

Answer 46

Myelosuppression and hemorrhagic cystitis

Question 47

Alkylating agent used for brain tumors since the are able to cross the BBB

Answer 47

Nitrosoureas

Question 48

CNS toxicity resulting in seizures, dizziness and ataxia is seen with which alkylating agent?

Answer 48

Nitrosoureas

Question 49

What are the microtubule inhibitors?

Answer 49

Paclitaxel, Vincristine and Vinblastine

Question 50

Microtubule inhibitor used for ovarian and breast carcinomas?

Answer 50

Paclitaxel

Question 51

What phase in mitosis is stopped by paclitaxel?

Answer 51

Anaphase - stabilizes microtubules so mitotic spindle cannot break down

Question 52

Side effects of paclitaxel

Answer 52

Myelosuppression, neuropathy, hypersensitivities

Question 53

Anticancer drug that binds B-tubulin and inhibits polymerization of microtubules preventing mitotic spindle formation

Answer 53

Vincristine or Vinblastine

Question 54

Anticancer drug indicated for solid tumors and leukemias that binds B-tubulin

Answer 54

Vincristine or Vinblastine

Question 55

Anticancer drug with neurotoxicity and used for treatment of non-Hodgkin lymphoma that binds B-tubulin

Answer 55

Vincristine

Question 56

Anticancer drug with used for treatment of Hodgkin lymphoma that binds B-tubulin

Answer 56

Vinblastine

Question 57

Used to prevent nephrotoxicity when using cisplatin

Answer 57

Amifostine and chloride

Question 58

Anticancer drug for treatment of testicular, bladder, ovary and lung carcinomas that cross-links DNA

Answer 58

Cisplatin or carboplatin

Question 59

Cisplatin or carboplatin side effects

Answer 59

Nephrotoxicity, peripheral neuropathy, ototoxicity

Question 60

Anticancer drug that inhibits topoisomerase II causing DNA degradation

Answer 60

Etoposide and Teniposide

Question 61

Etoposide and Teniposide side effects

Answer 61

Myelosuppression and alopecia

Question 62

Anticancer drug that inhibits topoisomerase I preventing unwinding and replication of DNA

Answer 62

Irinotecan, Topotecan

Question 63

Topoisomerase I inhibitor used for colon cancer

Answer 63

Irinotecan

Question 64

Topoisomerase I inhibitor used for ovarian and small cell cancers

Answer 64

Topotecan

Question 65

Anticancer drug that inhibits ribonucleotide reductase decreasing DNA synthesis and is S-phase specific

Answer 65

Hydroxyurea

Question 66

Anticancer drug that causes severe myelosuppression and used fro myeloproliferative disorders, sickle cell, and melanoma that is S-phase specific

Answer 66

Hydroxyurea

Question 67

Monoclonal antibody against VEGF which inhibits angiogenesis used for solid tumors

Answer 67

Bevacizumab

Question 68

Monoclonal antibody used for treatment of colorectal cancer and renal cell carcinoma that causes hemorrhage, blood clots and impaired wound healing

Answer 68

Bevacizumab

Question 69

EGFR tyrosine kinase inhibitor used for non-small cell lung carcinoma that causes a rash

Answer 69

Erlotinib

Question 70

Monoclonal antibody against EGFR used for stage IV colorectal cancer and head and neck cancer that causes rash, elevated LFTs and diarrhea

Answer 70

Cetuximab

Question 71

Tyrosine kinase inhibitor of Bcr-Abl and c-kit use for treatment of CML and GI stromal tumors that cause fluid retention

Answer 71

Imatinib

Question 72

Monoclonal antibody against CD20 used for non-Hodgkin lymphoma, CLL, TIP, and RA that increases risk of progressive multifocal leukoencephalopathy

Answer 72

Rituximab

Question 73

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

Answer 73

Bortezomib and Carfilzomib

Question 74

Selective estrogen receptor blocker used in the treatment of breast cancer that block binding of estrogen to ER positive cells

Answer 74

Tamoxifen

Question 75

Selective estrogen receptor modulator used for treatment of osteoporosis

Answer 75

Raloxifene

Question 76

Selective estrogen receptor blocker that is a partial agonist in endometrium which increases the risk of endometrial cancer

Answer 76

Tamoxifen

Question 77

Estrogen receptor antagonist that is safe to use since it does not increase risk of endometrial cancer and used for treatment of osteoporosis

Answer 77

Raloxifene

Question 78

What drug is a monoclonal antibody against HER-2 used for the treatment of breast and gastric cancer that causes cardiotoxicity?

Answer 78

Trastuzumab

Question 79

Small molecule inhibitor of BRAF oncogene positive melanoma used for V600E metastatic melanoma

Answer 79

Vemurafenib

Question 80

Oncologic emergency triggered by massive tumor lysis

Answer 80

Tumor lysis syndrome

Question 81

Treatment for Tumor lysis syndrome

Answer 81

Aggressive hydration, allopurinol and rasburicase

Question 82

Recombinant uricase that catalyzes metabolism of uric acid and used for prevention and treatment of tumor lysis syndrome

Answer 82

Rasburicase