Antimetabolites Flashcards
Folic acid analog
Binds with DHFR —> results inhibition of THF
FPGS: add 5-7 glutamate residues
Methotrexate (MTX)
Drug x when taken with:
Aspirin
NSADs
Penicillin
Cephalosporins
D/D I
MTX
biologic effects of MTX can be reversed by administration of the oxidised folate
leucovorin ? (True/false)
False
Nooot oxidised. Reduced folate leucovorin
biologic effects of MTX can be reversed by administration of:
the reduced folate leucovorin
or
by L-leucovorin, which is the active enantiomer.
inhibition of thymidylate synthase (TS)
Inhibition of DHFR
This drug is?
A) MTX
B) 5-FU
C) pemetrexed
C) pemetrexed
S.E: skin rash & hand-foot syndrome
Toxicity can be reduced by vitamin supplements with folic acid and vitamin b12
This drug is?
A) MTX
B) 5-FU
C) pemetrexed
C) pemetrexed
hand-foot syndrome (is a viral infection manifested by painful erythema and swelling
of the hands and feet, and treatment with dexrazoxane?
Noooo! dexrazoxane (for anthracycline)
dexamethasone (same as Paclitaxel)
given (IV) onnnnly
- inhibits TS
- inhibits 5-MTHF
A) capecitabine
B) trifluridine
C) 5-flurouracil
C) 5-flurouracil
5-FU has long half life and not catabolized by DPD enzyme (true/ false)?
false
Has short half-life (10-15 mins)
Catabolised by DPD enzyme
Capecitabine - > 5-FU
Via enzyme called?
TP
Thymidine phosphorylase
Capox is the first-line treatment of CRC
What is it?
Capecitabine + oxaliplatin
While Folfox is second- line therapy for CRC
(oxaliplatin + 5-FU + leucovorin)
Made up of two components
Trifluridine: Inhibits TS Leading to I DNA synthesis
Tipiracil : inhibits TP
A) Cytarabine
B) Gemcitabine
C) Capecitabine
D) Trifluridine (TAS-102)
D) Trifluridine (TAS-102)
Trifluridine TTT Means TP TS
competitively inhibits DNA polymerase-α and DNA polymerase-β,
Ara-CDP ?
Ara-CTP ?
Ara-CMP ?
Ara-CDP ?
Ara-CTP ? Yeeees
Ara-CMP ?
This agent has absolutely ((( no ))) activity in solid tumors.
Cytarabine or gemicitane
Cytarabine
has broad-spectrum activity against both solid tumors and hematologic malignancie.
In contrast to cytarabine, which has no activity on solid tumor
Gemicitabine
(جم و ست)
ستر بدون
جم مع
Nausea and vomiting occur in 20% of patients, and a flu-like syndrome also has been
observed in gemicitabine (true/false)
70%
Not 20%
Inhibition of ribonucleotide reductase by gemcitabine diphosphate
IMP!
Not triphosphate
Diiiii phosphate
Flu-like syndrome is S.E of drug?
A)cytarabine
B) 5-FU
C) MTX
D) trifluridine
E) capecitabine
E) gemcitabine
F) two answers are correct
E) gemcitabine
