anticancer1 Flashcards
Mechlorethamine [MustargenR]
Nitrogen Mustard, Alkylating Agent
NCCS
Cyclophosphamide [CytoxanR]
important requirement
Nitrogen Mustard, Alkylating Agent
*Requires metabolic activation by cytochrome P-450 oxidation system in the liver
-immunosuppressive agent
NCCS
Carmustine [BiCNUR]
important biochemical structure factor
Nitrosourea, (acts like) Alkylating Agent
-highly lipid soluble
NCCS
Cisplatin [PlatinolR-AQ]
important SEs
Platinum Complex, Alkylating Agent
SEs: nephrotoxicity and ototoxicity
NCCS
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)
Mercaptopurine [PurinetholR]
Purine Analog, Antimetabolite
-inhibits a number of enzymes of purine interconversion–>
inhibition of purine nucleotide synthesis and metabolism
CCS: S Phase
Fluorouracil (5-FU)[AdrucilR]
Pyrimidine Analog, antimetabolite
-Binds to thymidylate synthetase covalently
CCS: S Phase
less GI SEs
Cytarabine [CytosarR]
Pyrimidine Analog, antimetabolite
-Converted to cytarabine triphosphate inhibiting DNA polymerase by competing with physiologic substrate; deoxycitidine triphosphate
CCS: S Phase
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
alkylating agent toxicity
-direct vesicant (vesicle producing), damaging tissues at site of injection
Acute: GI: N/V
Delayed: BM depression
what to know for anticancer drugs
name, what type, MOA, and unique toxicity
if different from acute: GI and delayed: BM suppression
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!
Daunorubicin hydrochloride [CerubidineR]
Anthracycline Antibiotic
CCNS
Doxorubicin hydrochloride [AdriamycinR]
Anthracycline Antibiotic
CCNS
