Cell-Cycle Dependent Drugs Flashcards
What is the MOA of Azathioprine and 6-mercaptopurine?
Purine analog → Inhibition in S-phase.
What are the HY indications for Azathioprine and 6-mercaptopurine?
Renal transplant rejection, autoimmune diseases, leukemia.
How are Azathioprine and 6-mercaptopurine metabolized to exert cytotoxic effects?
Metabolized by HGPRT.
What is the MOA of Cladribine and Fludarabine?
Purine analogs → Various mechanisms, non-specific.
What are the HY indications for Cladribine and Fludarabine?
Chronic lymphocytic leukemia (CLL), hairy cell leukemia (Cladribine).
What are the adverse effects of Cladribine and Fludarabine?
Nephrotoxic, neurotoxic, cardiotoxic.
What is the MOA of Cytarabine and Gemcitabine?
Pyrimidine analog → Inhibition in S-phase.
What cancers are treated with Cytarabine and Gemcitabine?
Acute myeloid leukemia (AML) (Cytarabine), pancreatic cancer, non-small cell lung cancer (Gemcitabine).
What is the MOA of 5-Fluorouracil (5-FU) and Capecitabine?
Inhibition of thymidylate synthase → ↓ dTMP → Inhibition in S-phase.
What cancers are treated with 5-FU and Capecitabine?
Colorectal cancer, breast cancer, pancreatic cancer, skin cancers (topical 5-FU).
What enhances the effect of 5-FU?
Leucovorin.
What is the MOA of Hydroxyurea?
Inhibition of ribonucleotide reductase → Inhibition in S-phase.
What cancers and conditions are treated with Hydroxyurea?
Chronic myelogenous leukemia (CML), polycythemia vera, sickle cell disease (to increase HbF).
What are the adverse effects of Hydroxyurea?
Teratogenicity, megaloblastic anemia.
What is the MOA of Methotrexate?
Inhibition of dihydrofolate reductase → ↓ dTMP, ↑ Adenosine → Inhibition in S-phase.
What cancers are treated with Methotrexate?
Acute lymphoblastic leukemia (ALL), breast cancer, choriocarcinoma, lymphomas.
How is Methotrexate toxicity reversed?
Leucovorin.
What is the MOA of Irinotecan and Topotecan?
Inhibition of topoisomerase I → DNA unwinding.
What cancers are treated with Irinotecan and Topotecan?
Colorectal cancer (Irinotecan), ovarian cancer, small cell lung cancer (Topotecan).
What is the MOA of Etoposide and Teniposide?
Inhibition of topoisomerase II → DNA unwinding.
What cancers are treated with Etoposide and Teniposide?
Small cell lung cancer, testicular cancer, lymphomas, leukemias.
What is the MOA of Bleomycin?
Free radical DNA damage → Inhibition in G₂ and M phase.
What cancers are treated with Bleomycin?
Testicular cancer, Hodgkin lymphoma.
What is the MOA of Paclitaxel?
Impaired degradation of polymerized microtubules → Mitotic arrest.
