Chemotherapeutic Agents EC

Question 1

What drugs act on the S phase of the cell cycle?

Answer 1

Etoposide

Antimetabolites (MTX, 5FU, Cytarabine, Azathioprine, 6-MP, 6-TG)

Question 2

What drugs act on phase G2 of the cell cycle?

Answer 2

Etoposide

Bleomycin

Question 3

What drugs act on the M phase of the cell cycle?

Answer 3

Vinca alkaloids (inhibit microtubule formation)
Taxols (ie. paclitaxel - inhibit microtubule disassembly)

Question 4

Methotrexate (MOA, Use, Tox)

Answer 4

Folic acid analog (inhibits DIHYDROFOLATE REDUCTASE)
(decreased dTMP, decreased DNA synthesis)

Leukemias, Lymphomas, Choriocarcinoma, Sarcoma
Abortion, Ectopic pregnancy, RA, Psoriasis

Myelosuppression (reversible with leucovorin)
Fatty change in liver
Mucositis
Teratogenic

Question 5

5-Fluorouracil (MOA, Use, Tox)

Answer 5

Pyrimidine analog (inhibits THYMIDYLATE SYNTHASE)
(decerase dTMP, decreased DNA synthesis)

Colon cancer, Basal cell carcinoma

Myelosuppression (not reversible)
Photosensitivity

Question 6

Cytarabine (MOA, Use, Tox)

Answer 6

Pyrimidine analog (inhibits DNA POLYMERASE)

Leukemias, Lymphomas

Leukopenia, Thrombocytopenia, megaloblastic anemia

Question 7

Azathioprine, 6MP, 6TG (MOA, Use, Tox)

Answer 7

Purine analog (decrease de novo synthesis)

Leukemias

Bone marrow, GI, liver
Met. by xanthine oxidase (toxic with allopurinol-xanthine oxidase inhibitor )

Question 8

Dactinomycin [actinomycin D] (MOA, Use, Tox)

Answer 8

Antitumor antibiotic
Intercalates in DNA

Wilm’s tumor, Ewing’s sarcoma, rhabdomyosarcoma,
Used for childhood tumors
“Children ACT out”

Question 9

Doxorubicin [Adriamycin] (MOA, Use, Tox)

Answer 9

Antitumor antibiotic
Generate free radicals
Intercalates in DNA

Solid tumors, Leukemias, Lymphomas

Dilated cardiomyopathy, Myelosuppression, Alopecia,
Dexrazoxane (Fe chelator) prevents cardiotoxicity

Question 10

Bleomycin (MOA, Use, Tox)

Answer 10

Antitumor antibiotic
Generates free radicals

Testicular cancer
Hodgkin’s lymphoma

Pulmonary fibrosis, Skin changes

Question 11

Cyclophosphamide (MOA, Use, Tox)

Answer 11

Alkylating agent
Covalently X-link DNA at guanine N-7

Solid tumors, Leukemia, Lymphoma, some brain cancers

Myelosuppression
Hemorrhagic cystitis (prevented with Mesna-binds Acrolein)

Question 12

Nitrosoureas [-mustine] (MOA, Use, Tox)

Answer 12

Alkylating agent
(requires bioactivation)

Brain tumors (crosses BBB)

CNS toxicity

Question 13

Busulfan (MOA, Use, Tox)

Answer 13

Alkylating agent

CML, bone marrow ablation prior to transplantation

Pulmonary fibrosis
Hyperpigmentation

Question 14

Vincristine/Vinblastine (MOA, Use, Tox)

Answer 14

Bind tubulin and block formation of mitotic spindle

Solid tumors, Leukemias, Lymphomas

Vincristine- Neurotoxicity and paralytic ileus
VinBLASTine-BLASTS Bone marrow

Question 15

Paclitaxel (MOA, Use, Tox)

Answer 15

Hyperpolymerize microtubules (inhibit microtubule breakdown)

Ovarian and breast carcinomas

Myelosuppression and hypersensitivity

Question 16

Cisplatin/Carboplatin (MOA, Use, Tox)

Answer 16

Cross-link DNA

Testicular, bladder, ovary, and lung carcinomas

Nephrotoxicity and acoustic nerve damage
(prevent nephrotox. w/ Amifostine (free radical scavenger)

Question 17

Etoposide (MOA, Use, Tox)

Answer 17

Inhibit topoisomerase II (DNA degradation)

Solid tumors, leukemias, lymphomas

Myelosuppression, GI irritation, Alopecia

Question 18

Hydroxyurea (MOA, Use, Tox)

Answer 18

Inhibits RIBONUCLEOTIDE REDUCTASE (decrease DNA synthesis)

Melanoma, CML, sickle cell disease (increases HbF)

Bone marrow suppression, GI upset

Question 19

Prednisone/Prednisolone (MOA, Use, Tox)

Answer 19

May trigger apoptosis (even in undividing cells)

CLL, non-Hodgkin’s lymphomas, (immunosuppressant)

Cushing-like, immunosuppression, cataracts, acne, hypertension, peptic ulcers, hyperglycemia, phychosis

Question 20

Tamoxifen/Raloxifene (MOA, Use, Tox)

Answer 20

SERMs (antagonist in breast, agonist in bone)

Breast cancer treatment and prevention, Prevent osteoporosis

Tamoxifen-increase risk of endometrial cancer, hot flashes

Question 21

Trastuzumab (MOA, Use, Tox)

Answer 21

HER-2 (TK) MAB

HER-2 + breast cancer

Cardiotoxicity

Question 22

Imatinib (MOA, Use, Tox)

Answer 22

Philidelphia chromosome bcr-abl TK inhibitor

CML, GI stromal tumors

Fluid retention

Question 23

Rituximab (MOA, Use, Tox)

Answer 23

MAB against CD20 (B-cells)

non-Hodgkin’s, RA (w/ MTX)

Question 24

Vemurafenib (MOA, Use, Tox)

Answer 24

Small molecule inhibitor of forms of the B-Raf kinase with the V600E mutation

Metastatic melanoma

Question 25

Bevacizumab (MOA, Use, Tox)

Answer 25

MAB against VEGF (inhibits angiogenesis)

Solid tumors

Question 26

Cisplatin/Carboplatin classic toxicity

Answer 26

Acoustic nerve damage

Nephrotoxicity

Question 27

Vincristine classic toxicity

Answer 27

Peripheral neuropathy

Question 28

Bleomycin/Busulfan classic toxicity

Answer 28

Pulmonary fibrosis

Question 29

Doxorubicin classic toxicity

Answer 29

Cardiotoxicity

Question 30

Trastuzumab classic toxicity

Answer 30

Cardiotoxicity

Question 31

Cyclophosphamide classic toxicity

Answer 31

Hemorrhagic cystitis

Question 32

5-FU classic toxicity

Answer 32

Myelosuppression

Question 33

6-MP classic toxicity

Answer 33

Myelosuppression

Question 34

Methotrexate classic toxicity

Answer 34

Myelosuppression