Chemo Pharmacology

Question 1

What are the classes of chemotherapy drugs?

Answer 1

Antimetabolites
"Natural Products" Antibiotics
Alkylating Agents
Microtublule Inhibitors
Enzymes
Kinase Inhibitors
Antibodies
Biological Response Modifiers

Question 2

Name the antimetabolites and their mechanism.

Answer 2

Methotrexate: Folic acid analog, inhibits dihydrofolate reductase
5-Fluorouracil: Pyrimidine analog, inhibits thymidylate synthase
6-Mercaptopurine: Purine analog, decreases denovo purine synthesis
6-Thioguanine: Purine analog, decreases denovo purine synthesis
Cytarabine: Pyrimidine analog, inhibits DNA polymerase

Question 3

What are the categories of alkylating agents?

Answer 3

1) nitrogen mustards
2) ethylenimines
3) alkylsulfonates
4) nitrosoureas
5) triazenes.

Question 4

How do alkylating agents function?

Answer 4

cause DNA damage

Question 5

What are some alkylating agents?

Answer 5

Cyclophosphamide, ifosfamide
Carmustine, lomustine, semustine, streptozocin
Busulfan

Question 6

What are some microtubule inhibitors?

Answer 6

Vincristine, vinblastine: block polymerization

Paclitaxel, -taxols: prevent depolymerization

Question 7

What are some anti tumor antibiotics?

Answer 7

Dactinomycin - Intercalates in DNA
Doxorubicin - Generates free radicals, intercalates/breaks DNA
Bleomycin - Induces free radical formation, breaks DNA strands
Etoposide (VP-16)- inhibits topoisomerase II, increases DNA degradation

Question 8

Cisplatin: Mechanism, Clinical Use, Toxicity

Answer 8

Cross-link DNA
Testicular, bladder, ovary, lung
Nephrotoxic and acoustic nerve damage

Question 9

Hydroxyurea: Mechanism, Clinical Use, Toxicity

Answer 9

Inhibits ribionucleotide reductase
Melanoma, CML, SSD
BM supression, GI upset

Question 10

Prednisone: Mechanism, Clinical Use, Toxicity

Answer 10

May trigger apoptosis, even in non-dividing cells
CLL, Hodgkin’s (glucocorticoid immunosuppressant)
Cushing-like sx, immunosuppression, cataracts, acne, osteoporosis, HTN, peptic ulcers, hyperglycemia, psychosis

Question 11

Tamoxifen, raloxifine: Mechanism, Clinical Use, Toxicity

Answer 11

SERMs- block estrogen binding to receptors
Breast cancer (and prevents osteoporosis)
Tam- increase in endometrial carcinoma

Question 12

What are some antibodies used to treat cancer?

Answer 12

Trastuzumab (herceptin)
Imatinib (Gleevec)
Rituximab

Question 13

Trastuzumab (herceptin): Mechanism, Clinical Use, Toxicity

Answer 13

Monoclonal Ab against HER-2 tyrosine kinase
Metastatic breast cancer
Cardiotoxicity

Question 14

Imatinib: Mechanism, Clinical Use, Toxicity

Answer 14

Philadelphia chromosome bcr-abl tyrosine kinase inhibitor
CML, GI stromal tumors
Fluid Retention

Question 15

Rituximab: Mechanism, Clinical Use, Toxicity

Answer 15

Monoclonal Ab against CD20

B-cell neoplasms, NH lymphoma, RA.