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Flashcards in Chemotherapy And Cytotoxic Drugs Deck (28):
1

Cancer prevalence in m/f

M: prostate > lung > colon
F: breast > lung > colon

2

Cancer deaths M/F

M: lung > colon > prostate
F: lung > breast > colon

3

What kinds of tumors are most sensitive to cell cycle specific drugs?

Rapidly growing with growth fraction >70%, acute leukemia and high grade lymphomas

4

What kinds of tumors are more affected by cell-cycle nonspecific drugs?

Cancer cells that are cycling or in the resting state (G0)
Abx (except bleomycin), alkylating agents, camptothecins at high concentrations

5

Phases of Chemo tx of disseminated cancer

Induction: initial high dose
Consolidation: high dose for months
Maintenance: low dose for months/yrs

6

Examples of alkylating agents

Cyclophosphamide
Cisplatin

7

Alkylating agents MOA and resistance

Cyclophosphamide, Cisplatin
MOA: alkylate DNA at Guanine -> cross link of DNA -> can't repair -> apoptosis
Resistance: inc DNA repair, dec transport

8

Cyclophosphamide AE, dose limiting

Nitrogen mustard
AE: hemorrhagic cystitis
DL: myelosuppression

9

Cisplatin AE, DL

Platinum analog
AE: ototoxic
DL: nephrotoxicity (hydration, mannitol preventioN)

10

Examples of anti-metabolite drugs

MTX
5FU
6MP

11

MOAs as analogs of antimetabolites

MTX - folic acid analog
6MP - purine analog
5FU - pyrmidine analog

12

What is the most commonly used cytotoxic anti cancer agent

MTX

13

MTX MOA, AE

MOA: prevents THF formation leading to interruption of DNA, RNA, protein synth
AE: myelosuppresion, GI,renal
Give with leucovorin to rescue normal cells

14

6MP MOA, AE

MOA: metab by HGPRT -> TIMP replaces endogenous IMP, converted to t-dGMP and damages DNA
AE: myelosuppression that is worse with allopurinol

15

5FU MOA, AE

MOA: 5-FUTP -> inhibits TS
AE: myelosuppresion

16

Examples of vinca alkaloids, MOA

VinBlastine
VinCristine
MOA: binds to B tubular, blocks spindle formation, arrest at metaphase interferes with chromosome segregation -> death

17

VinBlastine use and tox

Vinca alkaloid
Use: Breast, testicular
Tox: bone marrow suppression

18

VinCristine use, tox

Use: childhood leukemia and tumors
Tox: neuritis, neuropathy, muscle weakness
Marrow sparing effect*

19

Which drug is a taxane?

Paclitaxel

20

Paclitaxel MOA, AE

MOA: binds to B tubule and prevents microtubule depolymerization
AE: myelosuppression and peripheral neuropathy

21

Example of a epipodophyllotoxin

Etoposide

22

Etoposide MOA, AE

MOA: blocks topoisomerase II
AE: myelosuppresion, alopecia

23

Example of camptothecins

Irinotecan

24

Irinotecan MOA, AE

MOA: inhibits topoisomerase I
AE: myelosuppression and diarrhea

25

How does tumor resistance develop against vinca alkaloids, taxanes, epipodophyllotoxins, and camptothecins?

inc MDR1 gene expression

26

Cytotoxic ABX and MOA

Doxorubicin
Bleomycin
MOA: intercalation insertion between base pairs

27

Doxorubicin MOA, AE

MOA: intercalation, inhib topo II, generation of free radicals
AE: irreversible cardiomyopathy, also acute arrhythmias

28

Bleomycin MOA, AE

MOA: intercalation, oxidation via bleomycin Fe II complex
DL: pulmonary fibrosis