Anti-Cancer Drugs

Question 1

Mechlorethamine

Answer 1

Action: Alkylation and cross-liinking of DNA.

Toxicity: BM suppression; male sterility; amenorrhea.

Question 2

Cyclophosphamide

Answer 2

Action: Alkylation and cross-liinking of DNA.

Toxicity: BM suppression; male sterility; amenorrhea.

Other: Requires activation by P450 in liver = no extravascular necrosis.

Question 3

Cisplatin

Answer 3

Action: Cross-linking of DNA.

Toxicity: BM suppression; renal tubular damage; neurotoxicity.

Question 4

Bleomycin

Answer 4

Action: Catalyzes free radical formation and DNA destruction.

Toxicity: Pulmonary fibrosis; skin changes.

Question 5

Actinomycin D

Answer 5

Action: Intercalates into DNA and blocks RNA and DNA synthesis.

Toxicity: BM suppression.

Question 6

Doxorubicin

Answer 6

Action: Topoisomerase II inhibitor.

Toxicity: BM suppression; cardiomyopathy.

Other drugs in class: Etoposide (drug list).

Picmonic: Dilated Cardiomyopathy.

Question 7

Irinotecan

Answer 7

Action: Topoisomerase I inhibitor.

Toxicity: BM suppression.

Question 8

Methotrexate

Answer 8

Action: DHFR inhibitor.

Toxicity: BM suppression.

Picmonic: Methotrexate.

Question 9

Fluorouracil (5-Fluorouracil)

Answer 9

Action: Inhibitor of thymidylate synthetase; misincorporated into RNA.

Toxicity: BM suppression.

Question 10

Cytosine arabinoside

Answer 10

Action: Inhibitor of DNA polymerase; misincorporated into DNA.

Toxicity: BM suppression.

Question 11

Hydroxyurea

Answer 11

Action: Inhibitor of ribonucleotide reductase.

Toxcity: BM suppression.

Question 12

6-Thioguanine

Answer 12

Action: Inhibitor of purine biosynthesis.

Toxicity: BM suppression.

Question 13

Tamoxifen

Answer 13

Action: Hormone therapy; estrogen receptor antagonist.

Uses: Breast cancer.

Toxicity: Hot flashes; risk increase for endometrial CA; thromboembolic events.

Picmonic: Tamoxifen.

Question 14

Leuprolide

Answer 14

Action: Hormone therapy; GnRH analog that causes GnRH receptor down regulation.

Uses: Prostate cancer; pre-menapausal breast cancer.

Toxicity: Hormone withdrawl.

Question 15

Anastrozole

Answer 15

Action: Hormone therapy; CYP19 aromatase inhibitor; inhibits estrogen produciton.

Uses: Breast cancer in post-menapausal women.

Toxicity: Estrogen deficiency.

Picmonic: Aromatase Inhibitors.

Question 16

Trastuzumab (Herceptin)

Answer 16

Action: Antibody therapy; binds to HER2 on cancer cells and stimulates antibody-dependent cellular cytotoxicity.

Toxicity: Cardiac toxicity.

Question 17

Bevacizumab

Answer 17

Action: Antibody therapy; inactivates VEGF; blocks angiogenesis.

Toxicity: Hypertension; GI perforation.

Question 18

Asparaginase (L-asparaginase)

Answer 18

Action: Degrades asparagine in the circulation and starves tumor cells for this amino acid.

Toxicity: Hypersensitivity reactions.

Question 19

Vinca alkaloids

Answer 19

Action: Interacts with tubulin and prevents microtubule polymerization.

Toxicity: BM suppression (vinblastine); peripheral neuropathy (vincristine).

Drugs in class: Vinblastine; vincristine.

Question 20

Imatinib (Gleevec)

Answer 20

Action: Tyrosine kinase inhibitor; inhibits ABL.

Uses: CML; GIST.

Toxicity: Fluid retention.

Picmonic: Chronic Myologenous Leukemia.

Question 21

Gefitnib

Answer 21

Action: Tyrosine kinase inhibitor; inhibits EGF-R.

Toxicity: Skin problems.

Question 22

Vemurafenib

Answer 22

Action: Tyrosine kinase inhibitor; inhibits BRAF.

Uses: Melanoma.

Toxicity: Skin problems.

Question 23

Allopurinol

Answer 23

Action: Xanthine oxidase inhibitor; prevents hyperuricemia.

Uses: Decrases toxicity of anti-cancer drugs.

Toxicity: Sensitivity reactions.

Picmonic: Gout Treatment.

Question 24

Leucovorin

Answer 24

Action: Vitamer for folic acid.

Uses: Rescue from methotrexate toxicity.

Picmonic: see Methotrexate.

Question 25

Filgrastim (G-CSF)

Answer 25

Action: Hematopoietic agent that stimulates neutrophil production.

Uses: Allows high dose chemotherapy with much less toxicity; reduced risk of infection.