Antimetabolite Oncology Pharm Flashcards
MoA of Azathioprine and 6-Mercaptopurine?
Purine (thiol) analogs -> decreased de novo purine synthesis
Azathioprine and 6-MP must be activated by what?
HGPRT
Azathioprine is metabolized to what?
6-Mercaptopurine
Azathioprine and 6-MP have increased toxicity with what drug and why?
Allopurinol and Febuxostat
Azathioprine and 6-MP are normally metabolized by Xanthine Oxidase
MoA of Cladribine
Purine analog
inhibits DNA polymerase
Clinical use of Cladribine?
Hairy Cell Leukemia
ADR of Cladribine
Myelosuppression
Nephrotoxicity
Neurotoxicity
MoA of Cytarabine
Pyrimidine Analog -> inhibits DNA Polymerase
Clinical Use of Cytarabine
AML
ADR of CYTarabine
Myelosuppression
Megaloblastic Anemia
PanCYTopenia
MoA of 5-Fluorouracil
Pyrimidine analog which covalently complexes folic acid.
inhibits thymidylate synthase -> decreased DNA synthesis
5-FU must be bioactivated to what metabolite?
5-FdUMP
What drug can be used topically to treat basal cell carcinoma?
5-FU
Clinical Use of 5-FU? (3)
Colon Cancer
Pancreatic Cancer
Basal Cell Carcinoma (topical)
ADR of 5-FU?
Myelosuppression
What drug interacts with 5-FU to enhance its clinical use and worsen its side effects?
Leucovorin (folinic acid)
MoA of Methotrexate?
Folic Acid analog that competitively inhibits dihydrofolate reductase -> decreased dTMP -> decreased DNA synthesis
What cancers can Methotrexate treat?
ALL and choriocarcinoma
What OB/GYN uses are there for Methotrexate?
ectopic pregnancy and medical abortion (with misoprostol)
What non-neoplastic uses are there for Methotrexate?
Immunosuppressant: RA, Psoriasis, IBD, Vasculitis
What can be given with MTX to avoid toxicity?
Leucovorin Rescue to reverse Myelosuppression
What are the toxicities of MTX? (4)
Myelosuppression
Hepatotoxicity
Mucositis (mouth ulcers)
Pulmonary Fibrosis
