Anticancer 1 Flashcards
Common toxicity associated with Anticancer drugs.
Severe vomiting
• Stomatitis
• Bone marrow suppression
• Alopecia
Anticancer drugs with high relative myelosuppression
Cytarabine Alkylating agents Doxorubicin Daunorubicin Vinblastine
Anticancer drugs with medium relative myelosuppression
Carboplatin
Methotrexate
5-FU
Anticancer drugs with low relative myelosuppression
Bleomycin
Vincristine
Asparaginase
AE of Doxorubicin?
Cardiotoxicitiy
Ae of Cyclophosphamide
hemorrhagic
cystitis
Ae of Bleomycin
pulmonary fibrosis.
Ae of Vincristine and paclitaxel
peripheral
neuropathy
What types of drugs are used to minimize chemotherapy induced emesis?
5HT3 receptor blockers and NK-1 inhibitors
What areused in prevention
and treatment of chemotherapy-induced neutropenia.
Filgrastim and sargramostim
Rescues bone marrow from methotrexate?
Leucovorin
Reduces hemorrhagic cystitis caused by
cyclophosphamide.
Mesna
Reduces anthracycline-induced
cardiotoxicity.
Dexrazoxane
Reduces renal toxicity caused by cisplatin.
Amifostine
AE of Methotrexate?
Common: Stomatitis, mucositis,
myelosuppression, alopecia, nausea, vomiting.
• Renal Damage: Uncommon. Complication of
high-dose methotrexate.
• Hepatic fibrosis and cirrhosis.
• Pneumonitis.
• Neurologic Toxicities. With IT administration.
MOA of Methotrexate?
Inhibits dihydrofolate reductase
• The cell is deprived of folate
• The synthesis of dTMP and purine
nucleotides decrease; consequently, synthesis
of DNA, RNA, and protein decreases, leads to cell
death.
What and how is methotrexate metabolized?
Methotrexate undergoes conversion to a series
of polyglutamates (MTX-PGs).
• The process is catalyzed by the enzyme
folylpolyglutamate synthase (FPGS).
Describe Leucovorin
Leucovorin is N5
-formyl-THF.
• Antidote to drugs that decrease levels of folic
acid, such as methotrexate, to rescue the bone
marrow.
• Leucovorin provides the normal tissues with the
reduced folate, thus circumventing the inhibition
of DHFR.
P glycoprotein confers multidrug resistance to which drugs?
Doxorubicin Daunorubicin Vincristine vinblastine etoposide tenoposide
General MOA of antimetabolites?
Target pathways related to nucleotide and nucleic acid synthesis.
Cycle specific
Main cytotoxic effects are in the S phase.
CELL CYCLE-SPECIFIC AGENTS?
Antimetabolites Bleomycin Microtubule inhibitors Epipodophyllotoxins Camptothecins
CELL CYCLE-NONSPECIFIC AGENTS
Alkylating agents
Platinum coordination complexes
Antitumor Antibiotics
Which types of rapidly proliferating tissues affected with chemotherapy?
buccal mucosa, bone marrow, GI
mucosa, and hair cells.
