Chemotherapy 1

Question 1

Alkylating agents

Answer 1

Nitrogen mustards: Cyclophosphamide
Nitrosoureas: Carmustine 
Methylhydrazines: Procarbazine
Triazenes: Temozolomide
Platinum coordination complexes: Cisplatin

Question 2

Antimetabolites

Answer 2

Folate antagonists: Methotrexate
Pyrimidine analogs: 5-Fluorouracil
Purine analogs: 6-Mercaptopurine

Question 3

Vincristine, Paclitaxel, Doxorubicin

Answer 3

Natural products

Question 4

Flutamide

Answer 4

Hormone

Question 5

Aldesleukin

Answer 5

Immunomodulators

Question 6

Rituximab

Answer 6

Monoclonal antibodies

Question 7

Imatinib

Answer 7

Protein-tyrosine kinase inhibitors:

Question 8

Cell Cycle Specific Drugs (CCS)

Answer 8

5-Fluorouracil, 6-Mercaptopurine, Methotrexate, Bleomycin, Etoposide, Paclitaxel, Vincristine

Question 9

Cell Cycle Nonspecific Drugs (CCNS)

Answer 9

Carmustine, Cyclophosphamide, Doxorubicin, Cisplatin

Question 10

Cell Cycle Specific Drugs Effective in

Answer 10

high-growth-fraction tumors

Question 11

Cell Cycle Nonspecific Drugs Effective in

Answer 11

high/low-growth-fraction tumors

Question 12

Acquired resistance

Answer 12

Develops in a number of drug-sensitive tumor types
Multidrug resistance
170 KDa P-glycoprotein (MDR)
190 KDa Multidrug resistance protein (MRP)

Question 13

Ondansetron, Dexamethasone

Answer 13

emesis treatment

Question 14

Chemoreceptor trigger zone for emesis

Answer 14

Area postrema, Near the caudal end of the 4th ventricle: 5-HT3, D2, M1
Vomiting center of the medulla oblongata

Question 15

Use: Colorectal cancer

Answer 15

F-CL
Fluorouracil
Leucovorin
Note: Fluorouracil is given after starting Leucovorin

Question 16

Use: Breast cancer, NSCLC

Answer 16

ICE-T
Ifosfamide (with Mesna)
Carboplatin
Etoposide
Paclitaxel (Taxol®)

Question 17

Nitrogen Mustards MOA

Answer 17

DNA alkylation:
Mispairing: G = C → G = T
Scission: Depurination, Imidazole ring opening, DNA strand
Inter/intrastrand cross-linking

Question 18

Nitrogen Mustards Therapeutic Uses

Answer 18

hematologic and solid tumors

Question 19

Cyclophosphamide need to be

Answer 19

bioactivated to work

Question 20

Nitrogen Mustards Side Effects

Answer 20

Myelosuppression: Nadir of peripheral blood granulocytes at 6 to 10 days & recovery in 14 to 21 days
Hepatic venooclusive disease: Vasculitis → ↑ fibrin → ↓ portal circulation
Neurotoxicity (Ifosfamide → chloracetaldehyde)
Alopecia (hair loss)
Pulmonary fibrosis

Question 21

Nitrosoureas Therapeutic Uses:

Answer 21

Brain (C, L), HD (C), NHL (C), Melanoma (C)

Question 22

Nitrosoureas Side Effects

Answer 22

Leukemogenic (secondary cancer)

Question 23

Nitrosoureas mech of resistance

Answer 23

Alkyl guanine transferase

Question 24

Degradation of carmustine generates

Answer 24

carbamoylating and alkylating intermediates

Question 25

Methylhydrazine MOA (procarbazine)

Answer 25

Methylates DNA & free radical production which causes chromosomal damage & inhibition of DNA, RNA & protein synthesis

Question 26

Methylhydrazine (procarbazine) therapeutic uses

Answer 26

HD, NSCLC, Brain (astrocytoma)

Question 27

Methylhydrazine (procarbazine) side effects

Answer 27

Weak MAO Inhibitor, Disulfirum effect (makes you sick when you have alcohol)