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32 Cards in this Set
- Front
- Back
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Mechanism of Alkylating Agents
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Cause DNA crosslinking such that strands will not separate for replication
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Mechlorethamine
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Alkylating Agent
Most reactive Nitrogen mustard but is very unstable Cyclophosphamide is a more stable version |
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Cyclophosphamide
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An alkylating agent that is a prodrug metabolized by Cyt P450
Cardiac and Renal toxicity: Give MESNA to block acrolein |
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Ifosfamide
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Alkylating Agent
Like cyclophosphamide but more active Also give with MESNA Toxicity: Renal, CNS |
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Carmustine/Lomustine
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Alkylating Agents
Carmustine (IV) Lomustine (Oral) Toxicity: Lungs, Bone marrow |
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Busulfan
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Alkylating Agent
Oral Toxicity to Bone Marrow (esp. stem cells) |
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Cisplatin
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Alkylating Agent
Toxicity: Renal Damage (reduced with hydration) and ototoxicity |
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Carboplatin
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Alkylating Agent
Less toxic than cisplatin Myelosuppression is dose limiting |
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Mechanism of Antimetabolites
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Block the formation of DNA by forming abnormal DNA
Cell cycle dependent |
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Methotrexate
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Folic acid analog
Inhibits Dihydrofolate Reductase Toxicity: Hepatic necrosis and bone marrow depression |
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Rescues methotrexate toxicity
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Leucovorin
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Flourouracil
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Antimetabolite of Thymine
Converted to fraudulent FdUMP that complexes with thymidylate synthase Leucovorin potentiates action |
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Capecitabine
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Antimetabolite
Prodrug of 5 FU |
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6-Mercaptopurine
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Antimetabolite
Inhibits guanine synthesis Used for leukemia in children Metabolized in liver by TPMT and XO |
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TMPT mutations
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Affect the metabolism of 6-Mercaptopurine
Drug accumulates and destroys bone marrow |
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Azathioprine
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Prodrug of 6-MP
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Cytarabine
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Antimetabolite
Cytosine analog Inhibits chain elongation |
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Doxorubicin
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Antibiotic
Inhibits resealing of nicked DNA Toxicity:Cardio when drug complexes with iron to generate radicals Lifetime max 550mg/m |
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Dexrazoxane
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Protects from cardiotoxicity due to Doxorubicin
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Epirubicin
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Doxorubicin analog
Chronic cardiac toxicity (lifemax 900) Interaction with cimetidine |
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Dactinomycin
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Interferes with topoisomerase
Leaves nicks in DNA |
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Bleomycin
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Forms complex with DNA and Fe that interacts with oxygen to form radicals
Toxicity: pulmonary *No significant bone marrow tox |
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Mechanism of Vinca alkaloids
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Binds to tubulin and inhibits polymerization to microtubules causing metaphase arrest
Peripheral Sensory Neuropathy |
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Vincristine
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Vinca alkaloids
Mild bone marrow depression Can be used in combination with other therapeutics Assoc. with Peripheral Sensory Neuropathy |
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Paclitaxel, Docetaxel
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From plants
Stabilizes polymerized microtubules Blocks m phase Peripheral Sensory Neuropathy |
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Etoposide
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From plants
Blocks resealing action of topo II Sensory neuropathy |
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Differentiating Agents
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Causes cells to further differentiate
Treatment for Acute Promyelocytic Leukemia Arsenic and ATRA |
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Tamoxifen
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Binds estrogen receptor to target Estrogen-dependent breast cancer
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Imatinib (Gleevec)
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Blocks the ATP binding site on BCR-ABL tyrosine kinase
Treats CML |
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Transtuzumab
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Recognizes and blocks HER2 receptor in metastatic breast cancer
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Cetuximab
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Recognizes and blocks HER1/EGFR
Side effect of skin rash |
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Bevacizumab
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Recognizes VEGF to inhibit angiogenesis
Effective in metastatic colorectal cancer |
