Antineoplastics

Question 1

Cyclophosphamide

Answer 1

A nitrogen mustard alkylating agent. Acts by binding to DNA covalently. Not cell cycle specific but requires proliferation to work. Can cause hemorrhagic cystitis but is prevented with meson.

Question 2

Cisplatin

Answer 2

Alkylating agent (platinum compound). Cross links DNA. Causes acoustic nerve damage.

Question 3

Methotrexate

Answer 3

DHF reductase inhibitor. Folate analog. Decreases dTMP creation. Give leukovorin to replenish folate in non-cancer cells. Side effects include myelosuppression and stomatitis/diarrhea. Drug of choice in RA and similar conditions

Question 4

5FU

Answer 4

Pyrimidine analog which covalently complexes folic acid. Inhibits thymidylate synthase, decreases dTMP, decreases DNA and protein synthesis. Causes myelosuppression not rescuable with leukovorin. But can give uridine to rescue.

Question 5

Mercaptopurine

Answer 5

Purine analog that decreases denote purine synthesis. Bone marrow suppression. Increased toxicity with allopurinol.

Question 6

Vincristine

Answer 6

Blocks microtubule polymerization. Incorporates in S phase and prevents M phase from proceeding by blocking assembly of the spindle. Bone marrow suppression and peripheral neuropathy

Question 7

Bleomycin

Answer 7

Induces free radical formation which causes breaks in DNA. Toxicity includes pulmonary fibrosis.

Question 8

Doxorubicin

Answer 8

Intercalates DNA and inhibits topoisomerases. Cardiotoxic, stomatitis, myelosuppression. q

Question 9

Paclitaxel

Answer 9

Promotes stability of MT so causes M phase arrest. Spindle can’t break down. Myelosuppression and neuropathy.

Question 10

Rituximab

Answer 10

Anti CD-20 chimeric antibody used for B cell lymphomas. q

Question 11

Imatinib

Answer 11

TKI blocks activity of BCR ABL by binding to DNA binding domain. also works for c-kit common in GI stromal tumors.

Question 12

Bevacizumab

Answer 12

Monoclonal antibody against VEGF, inhibits angiogenesis.