Anti-Neoplastic Drugs

Question 1

Cyclophosphamide

Answer 1

Alkylating, Class III (specific, non phase)
pro-drug w wide spectrum
(-) GI
limited myelosup
alopecia
bladder toxicity (acrolein)

Question 2

Mechlorethamine

Answer 2

alkylating, Class I (non-specif)
(X) Hodkin's, Non-Hodgkin's
(X) Breast, ovarian,lung
(-) GI
myelosupp
mild alopecia

Question 3

Carmustine

Answer 3

alkylating 
*cross BBB
(X) brain tumor, multiple myeloma, melanoma
(-) GI
delayed myelosupp

Question 4

Procarbazine

Answer 4

atypical alkylating (G1, S)
methylation of DNA
(X) Hodgkin's lymphoma
(-) GI
myelosupp
**2o malignancy

Question 5

Methotrexate

Answer 5

Anti-metabolite: anti-folate
bind DHFR--/THF production
(!) rescue with leucovorin (folinic acid) 
(X) acute lymphocytic leukemia
(X) choriocarcinoma
(-) intestinal epi damage
bone marrow supp
renal tube necrosis
displaced drugs from Albumin

Question 6

Fluorouracil

Answer 6

anti-metabolite: pyrimidine analog
FUTP--/RNA
FdUMP--/thymidylate synthase--/DNA
(X) GI CA
(X) bladder
(X) ovary, breast, neck
(-) GI + anorexia
myelosupp

Question 7

Cytarabine

Answer 7

anti-metabolite: pyrimidine analog 
cytidine competition- chain termination
(X) acute leukemia -AML
(-) myelosuppression
neurotoxicity

Question 8

Mercaptopurine

Answer 8

anti-metabolite: purine analog
--/RNA and DNA synth
(!) TPMT polymorphism- reduced metabolism= ^ toxic
(X) acute leukemia
(-) BM suppression

Question 9

Hydroxyurea

Answer 9

Misc. Anti-neo: G1/S interface
block r-NT> dNTP==/DNA synth
\+ radiation
(X) granulocytic leukemia
(-) GI sxs
hemato depr

Question 10

Vincristine

Answer 10

Natural agents- M phase
bind tubulin--/microtub and mitotic spindle formation
(X) acute lymphocytic anemia
(X) lymphoma
(X) neuroblastoma
(-) alopecia
NMJ abn- periph neurop

Question 11

Vinblastine

Answer 11

natural agent- M phase
bind tubulin--/microtub and mitotic spindle formation
(X) lymphoma
(X) breast CA 
(-) myelosuppressive (dose-limiting)

Question 12

Paclitaxel

Answer 12

Natural agent- G2/M phase
bind B-tubulin- ^^ assembly and stability
(X) radiosensitizer- refraf ovarian cancer
+ cisplatin- breast CA
(-) leukopenia
periph neuropathy
myalgia/arthralgia

Question 13

Etoposide

Answer 13

Natural agent- G2/M phase
DNA topoisom II--/dsDNA break repair
(X) Lymphoma, acute leukemia
small lung
testis
(-) GI sxs
leukopenia
alopecia

Question 14

Doxorubicin

Answer 14

Natural- Abx- non-phase specif
anti-angiogenic 
1. distort DNA helix
2. lipid peroxidation, ROS
3. bind DNA + topo-II
(X) lymphoma
(X) breast, ovary CA
(X) small cell lung 
(-) cardiomyopathy
BM depr, alopecia
GI sxs

Question 15

Bleomycin

Answer 15

Natural Product Abx- G2/M
iron-chelating glycopeptide
oxidative 
(X) germ cell tumors (testes, ovary)
(X) head, neck, lung lymphoma
(-) pulmonary toxicity
skin 
hyper-pigmentation 
(lung, skin have little bleomycin hydrolase)

Question 16

Trastuzumab

Answer 16

Natural product-monoAb-
--/HER2+-R= block prolif of cells
(X) metastatic breast CA 
\+ Paclitaxel 
(-) cardiomyopathy
hypersensitivity

Question 17

Filgrastim

Answer 17

Natural product- BRM
(X) limit chemotx-induced neutropenia
-promote progen of neutrophils = ^ pop of neutrophils
(-) bone pain

Question 18

Cisplatin

Answer 18

Natural Product- Class III
platinum DNA crossplinks 
--/ thioredoxin reductase (TrxR) 
^ apoptosis
(X) testicular CA
cisplatin + etoposide + bleomycin
(X) ovarian cancer
cisplatin + paclitaxel 
(-) nephrotoxicity
ototoxicity
peripheral neuropathy 
electrolyte disturbances

Question 19

Prednisone

Answer 19

Hormone-Steroid
bind steroid R–/growth genes
–>*nuclease> cell lysis
(X) leukemia, lymphoma
(+) anti-emetic, appetite stim, anti-inflamm
(-) immuno/myelosupp, wt gain, fluid retention, psych effect

Question 20

Tamoxifen

Answer 20

Hormone- anti-estrogen
CYP2D6> TAM*= ^ sex hormone binding globulin
(X) adv post-men BC
metastatic pre-men BC
BC prophylaxis
(-) CYP2D6 ultrametab= & SE
hot flash, fatigue, 
bone, musc-sk pain
^ risk of uterine/endometrial CA

Question 21

Letrozole

Answer 21

Hormone- anti-estrogen
Aromatase(CYP19) inhibitor 
(X) metastatic post-men BC
(+) oral, rapid onset w NO androgenic SE
(-) hot flash, fatigue
bone, musc-sk pain
loss of bone, mineral density

Question 22

Leuprolide

Answer 22

Hormone- anti-testosterone
GnRH analog= ^ LH, FSH, then sudden drop!
(X) 1st line prostate CA
--monthly subQ inject/implant
(-) hot flashes, impotence

Question 23

Flutamide

Answer 23

Hormone- anti-testosterone 
Ar-R blocker
(X) 2nd line metastatic prostate CA
\+ GnRH agonist (Leuprolide) 
(-) gynecomastia, diarrhea
hepatotoxic