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Flashcards in anticancer1 Deck (14):
1

Mechlorethamine [MustargenR]

Nitrogen Mustard, Alkylating Agent
NCCS

2

Cyclophosphamide [CytoxanR]
*important requirement*

Nitrogen Mustard, Alkylating Agent
*Requires metabolic activation by cytochrome P-450 oxidation system in the liver
-immunosuppressive agent
NCCS

3

Carmustine [BiCNUR]
*important biochemical structure factor*

Nitrosourea, (acts like) Alkylating Agent
-*highly lipid soluble*
NCCS

4

Cisplatin [PlatinolR-AQ]
*important SEs*

Platinum Complex, Alkylating Agent
*SEs: nephrotoxicity and ototoxicity*
NCCS

5

Methotrexate [RheumatrexR ]
*important protector compound*

Folic Acid Analog, Antimetabolite
CCS: S Phase
-inhibitor of dihydrofolate reductase (inhibits folic acid-->THF: inhibits DNA synthesis)
*Leucovorin (folinic acid) bypasses metabolic block by MTX: PROTECTS NORMAL CELLS* (bypasses enzyme so some normal DNA synthesis)

6

Mercaptopurine [PurinetholR]

Purine Analog, Antimetabolite
-inhibits a number of enzymes of purine interconversion-->
inhibition of purine nucleotide synthesis and metabolism
CCS: S Phase

7

Fluorouracil (5-FU)[AdrucilR]

Pyrimidine Analog, antimetabolite
-Binds to thymidylate synthetase covalently
CCS: S Phase
less GI SEs

8

Cytarabine [CytosarR]

Pyrimidine Analog, antimetabolite
-Converted to cytarabine triphosphate inhibiting DNA polymerase by competing with physiologic substrate; deoxycitidine triphosphate
CCS: S Phase

9

alkylating agents :

NCCS, but cells damaged/killed when proliferating (as enter S phase: late G1 and S phase)
transfer a reactive alkyl group to the DNA molecule-->death of cell via
-miscoding of DNA strands
-incomplete repair of alkylated segment (topoisomerase can't seal breaks)
-excessive crosslinking of DNA and inability for strand separation (with polyfunctional alkylators)

*7-Nitrogen atom of guanine (purine) appears most sensitive to alkylation

10

alkylating agent toxicity

-direct vesicant (vesicle producing), damaging tissues at site of injection
Acute: GI: N/V
Delayed: BM depression

11

what to know for anticancer drugs

name, what type, MOA, and unique toxicity
(if different from acute: GI and delayed: BM suppression)

12

Antracycline Antibiotics:
Daunorubicin, Doxorubicin
*important SE!!*

from soil fungus Streptomyces
-bind to DNA through intercalation between specific bases and block the synthesis of new RNA or DNA (or both), cause DNA strand scission, and interfere with cell replication
CCNS

*important SE: cardiomyopathy!*

13

Daunorubicin hydrochloride [CerubidineR]

Anthracycline Antibiotic
CCNS

14

Doxorubicin hydrochloride [AdriamycinR]

Anthracycline Antibiotic
CCNS