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Flashcards in Chemotherapy Deck (35):
1

MTX

S-specific
folic acid analog --> inhib DHFR
dec dTMP --> dec DNA and protein synthesis
SE: myelosuppression --> leucovorin rescue
liver macrovesicular fatty changes
mucositis
teratogenic

2

Neoplastic uses of MTX

leukemias
lymphomas
choriocarcinoma
sarcoma

3

Non-neoplastic uses of MTX

abortion
ectopic prego
RA
psoriasis
IBD

4

5-FU

S-specific
pyrimidine analog --> activates to 5F-dUMP --> complexes folic acid
complex inhibits thymidylate synthase (dec dTMP)
SE: myelosuppression --> not revers by leucovorin
overdose: rescue with uridine
photosensitivity

5

Uses of 5-FU

colone cancer
pancreatic cancer
basal cell Ca (topical)

6

Cytarabine

S-specific
Pyrimidine analog --> inhib DNA pol
SE: leukopenia
thrombocytopenia
megaloblastic anemia
use for leukemias and lymphomas

7

Azathioprine, 6-mercaptopurine

S-specific
purine analog --> activated by HGPRT --> dec de novo purine synthesis
use in preventing organ rejection
RA
SLE (azathioprine)
leukemia
IBD (6-MP)
metal by XO --> inc toxicity with allopurinol
also has bone marrow, liver, and GI toxicity

8

6-thioguanine (6-TG)

S-specific
purine analog --> activated by HGPRT --> dec de novo purine synthesis
use in IBD and leukemia

9

Actinomycin D

intercalates DNA
use in Wilms tumor
Ewing sarcoma
rhabdomyosarcoma
(basically childhood tumors)
can cause myelosuppression

10

Doxorubicin

generates free radicals
intercalates DNA --> causes breaks --> dec replication
use in solid tumors, leukemias and lymphomas

11

Doxorubicin SE

CARDIOTOXIC --> dilated cardiomyopathy
use DEXRAZOXANE (iron chelator) to prevent myopathy
myelosuppression
alopecia

12

Bleomycin

induces free radical formation --> DNA strand breaks
use in testicular cancer and Hodgkin lymphoma
can cause PULMONARY FIBROSIS
skin changes
mucositis
MINIMAL myelosuppression

13

Cyclosphosphamide

alkylating agent --> X-link DNA at guanine n-7
requires hepatic bioactivation
use in solid tumors
lymphomas
some brain cancers

14

Cyclophosphamide SE

myelosuppression
hemorrhagic cystitis
can be partially prevented by MENSA
same for ifosfamide

15

Ifosfamide

alkylating agent --> X-link DNA at guanine n-7
requires hepatic bioactivation
use in solid tumors
lymphomas
some brain cancers

16

Nitrosoureas (-ustines) / Streptozocin

alkylating agent
cross-links DNA
is bioactivated and crosses the BBB
use in gliomablastoma multiforme and other brain tumors
can cause CNS toxicity

17

Busulfan

alkylating agent
cross-links DNA
use in CML or to ablate BM before transplant
SEVERE myelosuppression
pulmonary fibrosis
hyperpigmentation

18

Vincristine

microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
can cause neurotoxicity and paralytic ileus

19

Vinblastine

microtubule inhibitor
bind beta-tubulin and inhibit its polymerization
prevents spindle formation and M-phase
use in solid tumors, leukemias, and lymphomas
causes bone marrow suppression

20

Paclitaxel (taxols)

hyperstabilize tubules --> spindles cannot break down --> cannot progress to anaphase
use in ovarian and breast Ca
causes myelosuppression
alopecia
hypersensitivity

21

Cisplatin

cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis

22

Carboplatin

cross-links DNA
use in testicular / bladder / ovarian / lung Ca
can cause nephrotoxicity and acoustic nerve damage
prevent nephro with AMIFOSTINE (free radical scavenger)
and Cl- diuresis

23

Etoposide

inhib topoisomerase II --> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia

24

Teniposide

inhib topoisomerase II --> inc DNA degradation
testicular and small cell lung cancer / leukemias / lymphomas
SE: GI irritation / myelosuppression / alopecia

25

Irinotecan

inhib tobopisomerase I --> prevents DNA unwinding and replication
used in colon cancer / ovarian cancer
can cause severe myelosuppression and diarrhea

26

Topotecan

inhib tobopisomerase I --> prevents DNA unwinding and replication
used in small cell lung cancer / ovarian cancer
can cause severe myelosuppression and diarrhea

27

Hydroxyurea

inhib ribonucleotide reductase --> inhib DNA synthesis
use for melanoma, CML and sickle cell (inc HbF)
SE: BM suppression and GI upset

28

Prendisone / Prednisolone

may trigger apoptosis
use in CLL, non-Hodgkin lymphomas
also used as immunosuppressants
SE: Cushing-like Sx

29

Tamoxifen

selective estrogen receptor modulator (SERMs)
blocks binding of estrogen to ER+ cells
use for breast cancer
SE: endometrium partial agonist --> inc risk of endometrial cancer
hot flashes

30

Raloxifene

selective estrogen receptor modulator (SERMs)
blocks binding of estrogen to ER+ cells
use to prevent osteoporosis
not an endometrial antagonist

31

Trastu(2)zumab

Ab against HER-2 --> tyrosine kinase receptor
use for HER-2 + breast cancer and gastric cancer
can cause CARDIOTOXICITY

32

Imatinib

tyrosine kinase inhib of bcr-able and c-Kit
use in CML and GI stromal tumors
can cause fluid retention

33

Rituximab

Ab against CD20 (B-cell neoplasms)
non-Hodgkin lymphoma
RA (in combo with MTX)
ITP
SE: inc risk of multifocal leukoencephalopathy

34

Vemurafenib

small molec inhib of B-Raf kinase with the V600E mutation
use for metastatic melanoma

35

Bevacizumab

Ab against VEGF --> inhib angiogenesis
use with colorectal and renal cell Ca
risk of hemorrhage and impaired wound healing