Anticancer - Antimetabolites Flashcards
What is the Folate antagonist
MTX
What are the Purine Antagonists
6-MP
6-thioguanine
What are the Pyrimadine antagonists
5-FU
Capecitabine
Gemcitabine
Cytarabine
What can you give with MTX to minimize side effects
Leucovorin
What does MTX do
Inhibit DHF reductase
What are the main MTX AE
Renal damage (crystals in tubules)
What happens when you add Leucorvin to 5-FU
Increases 5-FU cytotoxicity
What is the main Gemcitabine AE
Elevated liver enzymes (AST/ALT)
What is the main Cytarabine AE
Ataxia
What is the main use for Gemcitabine
Pancreatic Cancer
How do we administer MTX in cancer
Short term, High dose
How do we administer MTX in RA
Long term, Low dose
What does MTX inhibit in RA
AICAR transformylase
When do we give MTX
Choriocarcinoma ALL Burkitt's Osteosarcoma Breast CA
What are the other MTX AE
BM/Immuno suppression Mucositis Alopecia Pulm tox (Children) Heptatic fibrosis (long term)
What metabolizes 6-MP
Xanthine Oxidase
What is 6-MP given for
ALL
How does 6-MP work
Converted to TIMP inhibiting de novo purine synth
Block formation of AMP & GMP
What are the 6-MP AE
BM suppression
Hepatotoxicity
N/V
What is useful about 6-thioguanine over 6-MP
No interaction with Allopurinol
How does 6-thioguanine work
Decrease GMP
Inhibit DNA/RNA synth
What is 6-thioguanine used for
ALL
What are the 6-thioguanine AE
BM suppression
Hepatotoxicity
N/V
How do 5-FU and Capecitabine work
Inhibit Thymidylate Synthase
Incorporation into RNA
