Neoplasm Drugs Flashcards
Cell cycle specific neoplasm drugs
Vinca alkaloids Anti-metabolites Taxanes Phodophyllotoxins Bleomycin Aspariginases
Hyperacute graft rejection
- Mechanism: Pre-formed antibodies and complimenting activation
- target: RBC antigens
- pathology: thrombosis and ischemia
- time course:
Non-cell cycle specific neoplasm drugs
Classic alkylating agents Dactinomycin Anthracyclins Nitroureases Mitomycin
Basics: Antimetabolites- methotrexate
- folate/folinate analog -> inhibits DHFR
- dose dependent toxicities (see immunopharm for list)
- can be given intrathecally for trt of carcinomatous meningitis
Antimetabolites: plant alkaloids
M-phase specific: e.g. Vincristine, Vineblastine, ninorebine
- microtubule polymerization inhibitor: inhibits assembly
- highly immunosuppressive
- neurotoxic
Taxanes: taxman, records, pennies
Paclitaxel, docetaxel
- MOA: interfere with mitotic spindle by preventing disassembly
- solid tumors
- neutropenias, tcytopenia, neuropathy
Rescue therapy
Levucorin: methotrexate
Mesna: traps acrolein byproduct of cyclophosphamide
Dexrazoxane: inhibits ROS in anthracyclins
Alkylators: (3)
Cyclophosphamide, chlorambucil, mechlorethamine
(Have chlorine/phosphate group)
- resistance is a result of trapping, decreasing drug permeability, and DNA repair
Mechloramine
Alkylating agent
- converts to reactive cytotoxic agent in the body
- hodgkins and non-hodgkins lymphoma
- vesicant
Platinum analogs
Cisplatin, carboplatin, oxaplatin
- testicular carcinomas, bladder, ovary and lung
- hematoxic, neurotoxic, nephrotoxic
Procarbazine
Forms H2O2
- orally active
- H/NH lymphomas
- inhibits MAO, and has a disulfiram like rxn. Nephro and neurotoxic as well
Mercaptopurine and thioguanine
Both inhibit HGPRTases -> stop purine synthesis
- high first pass metabolism
- marrow suppression is dose limited, it is hepatotoxic.
5-FU
Inhibition of thymadylate synthetase
- widely distributed including CSF
- lots of chemotherapeutic uses
- low toxicity: alopecia, GI distress and myelosupression
TRK inhibitors: Nibs
imatinib, Disatinib, Nilotinib - MOA: block BCR-ABL tyrosine Kinase activity - CML - Heart failure, myalgia, edema (In Philly they show off their nibs)
Gemcitabine
- mOA: Gemcitabine di and triphosphate inhibit ribonucleotide reductase
- non hodge/small cell lung cancer, bladder, pancreatic cancers
- normal 3 with some pulmonary toxicity
Vinca alkaloids
- MOA: anti-microtubule, Blocks mitotic spindle formation
- blastine and cristine: lymphomas and neuroblastomas.
~ blastine: kaposis sarcoma
~ cristine: Wilms tumor - neurotoxic
Etoposide and teniposide
- MOA: inhibits topoisomerase II (active in late S phase early G2)
- lymphoma, lung and germ cell cancers
- normal toxicities
Topotecan and Irinotecan
- MOA: campothectins that inhibit topoisomerase I
- topo: Second line for advanced ovarian cancer Small cell lung cancer
- Irin: Metastatic colorectal cancer
- myelosupression and GI distress
Anthracyclins
Rubicins and mitxanatrone
- MOA: inhibits topoisomerase II and creates ROS
- lots. If you get time come back and learn them
- Cardiotoxicity including arrythmias and AHF
Bleomycin
- MOA: causes production of Free rads which degrade DNA
- hodgkins and testicular cancer
- pulmonary toxicity, HSN and mucocutaneous rxns
Tratzuzumab
- MOA: MoAb growth factor receptor inhibitor (her-2/neu receptor)
- used in breast cancer
- cytokine syndrome effect, potential CHF
Ritixumab
- CD20 inhibitor Mab
- used in cocktail with other anti cancer drugs
- non-hodgkins lymphomas
- HSN, myelosupression
Mitomycin
- CCNS DNA cross linker
- hypoxia tumor cell trt
- myelosupression, HLLK toxicity
Asparaginases
- MOA: depletes serum aspargine
- leukemias and lymphomas
- HSN, bleeding
Red urine; normal Hct
Doxorubicin
Red urine; low hematocrit
Hemorrhagic cystitis due to cyclophosphamide use
Hypoxic tumor treatment
Mitomycin
- HLLK tox
Stines
Nitroureases (except lumostine)
- cell cycle Non-specific
- crosses BBB: brain tumors
Phodophylotoxins (2)
Etoposide, tenoposide
- topoisomerase II inhibitors
Bine/ate
Antimetabolite
ide/ine
Alkylating agents