Antineoplastics Flashcards
Toxicity of Immunosuppressives (5)
- Bone marrow
- GI tract
- Alopecia
- Renal
- Teratogenesis
- Hyperuricemia
Alkylating Agents (3)
- Mechlorethamine
- Cyclophosphamide
- Cisplatin
Nitrosoureas (2)
- Carmustine
- Lomustine
- Alkylate DNA
- Cause miscoding, breakage, crosslinking
- NOT cell-cycle phase specific
Alkylating Agents MOA
Alkylating Agents SE (6)
- Vesicant
- Affects rapidly proliferating cells
- N/V
- Bone marrow depression
- Immunosuppression
- Teratogenesis
Hodgkin’s dz
Mechlorethamine
Alkylating Agent that is NOT a vesicant
Cyclophosphamide
- Hemorrhagic cystitis (tx: MESNA)
- Inappropriate ADH
Cyclophosphamide SE (2)
Curative testicular CA
Cisplatin
- Acoustic nerve damage
- Anaphylaxis
Cisplatin
- Kill in all phases
- Bifunctional alkylators
- Inhibit DNA/RNA synthesis
Nitrosoureas
- Brain tumors
- Oral CA and GI
Nitrosoureas
Antimetabolites (Purine Analogues)
- Methotrexate
- 6 Mercaptopurine
- 5-fluorouracil
- Inhibits dihydrofolate reductase
- No thymidylate
- Blocks DNA, RNA, protein synthesis
Methotrexate
What drug acts as a rescue of Methotrexate (bypass blockade)
- Leucovorin
Methotrexate SE (3)
- Hepatotoxicity (more with immunosuppressant)
- Precipitates in renal tubules (kidney problems when used in CA tx)
- Pulmonary dz
- Converted by HGPRT to nucleotide
- Inhibit synthesis of purine nucleotides: DNA, RNA
- Not cell cycle specific
Antimetabolites (Purine Analogues)
- Metabolized by xanthine oxidase
- Allopurinol sometimes needed for hyperuricemia, but increases toxicity
6-Mercaptopurine
Drug used to tx Leukemias
6-Mercaptopurine
Drug that causes Jaundice
6-Mercaptopurine
- Inhibits thymidylate synthase - block DNA synthase
- Cell-cycle specific - G1 and S phases
5-Fluorouracil
Leucovorin increases response of what drug?
5-Fluorouracil
- Solid tumors
- Topical BCC
5-Fluorouracil Tx
- Intercalates into DNA
Doxorubicin MOA
Iron increases effect of ______
Doxorubicin
Antibiotics (3)
- Doxorubicin
- Bleomycin
- Mitomycin
- Cardiotoxic, esp with herceptin
Doxorubicin
- Intercalates into DNA
- Generates free radicals, effect increased by iron
Doxorubicin
- Directly damage DNA
- Cell cycle specific - G2 and M
Bleomycin
Bleomycin SE
- LITTLE myelosuppression
- PULMONARY FIBROSIS
- Anaphylactoid symptoms
Plant Alkaloids (3)
- Vincristine
- Vinblastine
- Paclitaxel
Vincristine & Vinblastine MOA
- Bind to tubulin - M phase
- Axonal transport affected
Vincristine SE
- Neurotoxicity
- Low myelosupression
Vinblastine SE
- More myelosupression
- Less neurotoxicity
Paclitaxel MOA
- Binds tubulin/microtubulin
- Arrests mitosis
- Disrupts axonal transport
Tyrosine Kinase Inhibitors
- Imatinib
- Erlotinib
Inhibitor of Bcr-AbI fusion protein
Imatinib (Gleevec)
- CML
- Gastrointestinal Stromal tumor
Imatinib (Gleevec) Tx (2)
Imatinib (Gleevec) SE
- Immunosuppressive (avoid if recently immunized for polio)
Epidermal Growth Factor Inhibitors
- Cetuximab
- Erlotinib
Angiogenesis Inhibitors
- Bevacizumab
- EGF receptor, blocks cell growth
- Monoclonal antibody
Cetuximab
- Blocks ATP binding to HER1/EGFR tyrosine kinase
Erlotinib
- VEGF needed for angiogenesis, over expressed in tumor
- Decreases blood supply and slows tumor growth
Bevacizumab
- Solid tumors (renal and glioblastoma)
- Injected in eye for Macular degeneration (ranibizumab)
Bevacizumab
Bevacizumab SE
- Bleeding and thromboembolism risk increased with systemic use
- Sunitinib (renal CA) and Sorafenib (hepatocellular CA) similar, SE similar
Hormones and Antagonists (4)
- Prednisone
- Tamoxifen
- Trastuxumab
- Flutamide
- Lymphomas and leukemias
Prednisone
- Block estrogen receptor in breast
- Hot flashes, uterine hyperplasia
Tamoxifen
- Antibody to HER2 receptor
- Cardiac toxicity, esp doxorubicin
Trastuzumab
- Anti-androgen for prostate CA
Flutamide