Oncology Drugs I Flashcards
Alkylating Agent: interculates into DNA prevents transcription. Metabolized to pro–drug in liver and causes nasia+vomitting, alopecia, and BMS
Cyclophosphamide
Antimetabolite: Blocks the production of Thymidine. Excreted through Kidneys. Causes inflammation of mucous membranes
Methotrexate
Incorporates into DNA and causes strand termination. Metabolized in liver. Side effects GI, and BMS
Cytosine arabinoside
Antimetabolite: Blocks the production of thymidine. Metabolized by liver by DPD which some people lack. Side Effects are GI and BMS
5–flourouracil
Inhibits many enxymes including DNA polymerase. Turned into metabolites in plasma and cleared by kidneys. Side effects are GI and BMS
Fludarabine
Blocks DNA synthesis. Excreted in urine. Side Effects are GI and BMS
Gemcitabine
Anti–mitotic alkaloid: Prevents microtubule dimers from forming microtubules. Hepatic metabolism through CYP3A4. Side effects are neurotoxicity
Vincristine
Platinum complex: Complex binds to guanine in DNA and crosslinks strands promoting apoptosis. Cisplatin is on–enzymatically inactivated in tissue and blood and excreted in urine. Side Effects are GI, nephrotoxicity, impaired electrolyte metabolism, neur
Cisplaten
Anthracycline: Intercalates into DNA inhibit transcription, inhibits topisomerase II, and generates free oxygen radicals. Metabolized in liver, and side effects are GI, BMS, Alopecia, and CARDIAC toxicity
Doxorubicin
Taxine: Inhibits microtubule disassembly. Metabolized by CYP2C8. Side Effects are GI, alopecia, BMS and peripheral neuropathy.
Paclitaxel
Topoisomerase I inhibitor: Prevents topoisomerase I from religating DNA strand breaks. Undergoes activation in liver. Side effects are BMS, Diarrhea (can be fatal)
Irinotecan
Topoisomerase II inhibitor: Prevents topoisomerase I from religating DNA strand breaks. Side effects are GI, BMS, Alopecia
Etoposide
Anibiotic antineoplastic: Induces DNA strand breaks. Metabolized by many tissues. Side effects are pulmanary toxicity
Bleomycin
Proteasome inhibitor: Inhibits the proteasome leading to cell death. Metabolized by liver. Side effects are peripheral neruopathy, GI, BMS
Bortexomib
Thalidomide derivative: Works through many mechanism.. Excreted unchanged in Kidnay. Side effects are GI, BMS, Terratogen
Lenalidomide
Monoclonal antibody: Antibody against CD20. Metabolized throught reticuloendothelial system. Side effects are infusion reactions and reactiviation of hepatitis B virus if patient has hepB
Rituximab
Monoclonal antibody: Antibody to extracellular doamin of Her2. Metabolism is unknown. Side effects are CARDIOMYOPATHY infusion reaction.
Trastuzamab
Monoclonal antibody: Antibody to the VEGF and prevents its integration with receptor, necessary for angiogenisis. Metabolism unknown. Side effects are bleeding and clotting problems, wound heeling, and infusion reaction. May worsen HTN.
Bevacizumab
Chimeric antibody: Competative antagonist of EGFR receptor. Metabolism unknown. Side effects include rash, but more rash better survival, and infusion reaction.
Cetuximab
Small molecule inhibitor: Inhibits the Bcr–Abl fusion protein, and C–kit. Metabolized by P450 and side effects are GI, and BMS.
Imatinib
Small molecule inhibitor: inhibitor of tyrosine protein kinase at VEGFR and Raf kinase. Dose reduced if taken on high fat meal, and metabolized by live. Side effects are skin and GI.
Sorafenib
Small molecule inhibitor: reversible tyrosine kinase inhibitor of EGFR with hight affinity for mutated form of EGFR. Metabolized by liver in P450 and side effects are Rash and GI.
Erlotinib
Small molecule inhibitor: inhibits the BRAF kinase enzyme (downstream of RAS). Metabolism is that it is excreted in poop. Side effects are cutaneous squamous cell carcinomas.
Vemurfenib
Binds irreversibly agonize Pit GnRH receptor and makes testosterone drop below castrate levels. (though first testy levels go up). Drug is metabolized by many tissues and excreted in urine. Side effects are decreased libido and ED, and loss of bone dens
Leuprolide
