Term
| Mechlorethamine (Mustargen®) |
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Definition
Anti-CA; Alkylating Agent
Use: Hodgkin's disease
Mechanism: Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells
Major Side Effects: ARF; vesicant (tissue damage at injection site) hyperuricema, hematologic tox., other rapidly proliferating cells i.e. BM, GI, sperm, hair; nausea/vomiting (CTZ and local); BM suppression, immuno suppression, teratogenesis, reproduction |
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Term
| Cyclophosphamide (Cytoxan®), Ifosfamide (Ifex®) |
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Definition
Anti-CA; Alkylating Agent; KNOW THIS GUY!!!
Use: Broad spectrum; breast, lung, ovarian, endometrial, cervical carinomas; for immunosuppression in RA, organ transplant, lupus nephritis; leukemia, lymphomas, Hodgkin's disease, testicular cancer
Mechanism: Pro-drug (CYP450 activates); Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells
Major Side Effects: Acrolein is breakdown product -> hemorrhagic cystitis (MESNA sulhydryl donor blocks); alopecia, hematogic, SIADH
Other Drugs: Chlorambucil (Leukeran®) - CLL, given for months/years, low tox
Thiotepa - Bladder cancer
Bendamustine (Treanda)- CLL, non-hodgkins lymphoma
Busulfan (Busulfex®) - CML, hyperuricema side effect
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Term
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Definition
Anti-CA drug: Alkylating Agent (Nitrosurea)
Uses: brain tumor
Mechanism: Enters CNS (highly lipid soluble)Alkylates DNA, casuing miscoding, breakage and cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells
Major Side Effects: PROFOUND MYELOSUPPRESSION
Other Drugs: Lomustine (CCNU) - PROFOUND MYELOSUPPRESSION (also brain tumors)
Streptozocin (Zanosar®) - pancreatic cancer
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Definition
Anti-CA drug; Alkylating agent
Mechanism: Alkylates DNA, causing cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells
Major Side Effects:
Other Drugs: Procarbazine (Matulane®)
Temozolamide (Temodar®) |
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Definition
Anti-CA drug: Alkylating Agent
Uses: testicular cancer
Mechanism: bifunctional alkylating agents, most effective in S phase; Alkylates DNA, casuing cross linking; Not cell-cycle phase specific; Most effect on rapidly proliferating cells i.e. tumor cells
Major Side Effects: renal (amifostin antagonises tox), acoustic nerve damage (HEARING LOSS)
Other Drugs: Carboplatin (Paraplatin®)
Oxaliplatin (Eloxatin®) |
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Term
| Methotrexate (Methotrexate®) |
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Definition
Antimetabolite
Uses: Leukemia, chriocarcinoma, immunosuppression (RA, psoriasis); burkitt's, non-hodgkins lymphoma, breast carcinoma, head and neck squamous cell carcinoma
Mechanism: inhibits dihydrofolate reductase, blocks synth of tetrahydrofolate from folic acid; blocks DNA, RNA and protein synthesis (as a result); chemotherpeutic effect DECREASED by folinic acid
Side effects: Leucovorin rescues from toxicity of methotrexate, must hydrate (decreased precipitations in renal tubules), hepatotoxicity (long term), pulmonary infiltrates; Apthos ulcer and pancytopenia
Other Drugs: Pemetrexed (Alimta®) |
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Term
| 6-Mercaptopurine (Purinethol®) |
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Definition
Antimetabolite: BIG drug
Uses: Leukemias
Mechanism: Purine analogue; converted by Hypoxanthine guanine phosphoribosyl transferase (HGPRT), interferes with DNA and RNA synthesis
Resistance develops through HGPRT
Metabolized by xanthine oxidase, allopurinol blocks breakdown
Side effects: BM depression, cholestatic jaundice, hyperuricemia (may need allopurinol)
Other Drugs: Thiogaunine - unaffected by allopurinol (not metabolized by xanthine oxidase; causes myelosuppression
Fludarabine (Fludara)
Cladribine (Leustatin®) |
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Term
| 5-Fluorouracil (Adrucil®) |
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Definition
Antimetabolite; BIG drug
Uses: Solid tumors (breast, stomach, esophagus, pancrease); hepatomas, ovarian cancer, cervical cancer, bladder and prostate; topical creame for premalignant keratoses and basal cell carcinomas; Colorectal cancer (combo with leucovorin)
Mechanism: G1 and S phase specific; a Pyrimidine that binds thymidylate synthase (rate limiting step in DNA synth) inhibiting it, blocking DNA synthesis; chemotherapeutic effect ENHANCED by folinic acid
Side effects: GI ulcers, BM depression
Other Drugs: Capecitabine (Xeloda®) - 5 fluorouracil pro-drug;
Cytarabine
Gemcitabine (Gemzar®)
Hydroxyurea (Hydrea®) - radiation recall (if you give this to a person who had radiation before, will get pigmentation at the site of radiation)
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Term
| Daunorubicin (Cerubidine®) |
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Definition
Abx
Rationale: Bind DNA base pairs, causing DNA strand scission; interferes with cell replication
Side effects: red urine, cardiomyopathy (dexrazoxane for iron chelation), radiation recall |
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Term
Doxorubicin (Adriamycin®
KNOW |
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Definition
Abx; BIG drug
Use: Lymphoma, leukemia, Hodgkin's disease; solid tumors (breast); sarcomas, thyroid carcinoma
Rationale: Bind DNA base pairs, causing DNA strand scission; interferes with cell replication
Side effects: forms free radicals/CARDIOTOXICITY!! (iron makes worse i.e. fenton)
Dexrazoxane chelates iron, decreases toxicity
Other Drugs: Idarubicin (Idamycin®)
Epirubicin (Ellence®)
Valrubicin (Valstar®)
Mitoxantrone (Novantrone®) |
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Term
Bleomycin Sulfate (Blenoxane®)
KNOW |
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Definition
Abx
Doesn't suppress BM very much (advantage)
Uses: testicular carcinoma, ovarian carcinoma
Rationale: Directly damages DNA (breaks up DNA) fragmentation; most toxic in late G2 and early M phase
Side effects: PULMONARY FIBROSIS (lance armstrong refused it); anaphylactoid reactions
Other drugs: Dactinomycin (Cosmegen®) - wilm's tumor and rhagdomyosarcoma, choriocarcinoma; vesicant; radiation recall
Mitomycin (Mutamycin®) - has to be activated by CYP 450 |
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Term
Vinblastine Sulfate (Velban®)
KNOW |
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Definition
Microtubule Agent
Use: Widely used; hodgkin's disase, leukemia in children, non-hodgkin's lymphoma
Mechanism: binds tubulin disrupting mitotic spindle apparatus/prevents segregation of chromosome lined up in metphase/metaphase arrest; M phase specific
Side effect profile: less neurotoxicity but MORE BM depression (blasts bone marrow) |
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Vincristine Sulfate (Oncovin®)
KNOW |
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Definition
Microtubule Agent
Use: Testicular carcinoma (bleomycin and cisplatin combo)
Mechanism: binds tubulin disrupting mitotic spindle apparatus/prevents segregation of chromosome lined up in metphase/metaphase arrest; M phase specific
Side effect profile: WORSE for neurotoxicity, peripheral neuropathy (crisps nerves) but little myelosuppression |
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Term
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Definition
Microtubule Agent
Use: breast/ovary carcinoma, lung head and neck carcinomas; kaposi's sarcoma
Mechanism: binds AND STABILIZES tubulin and microtubulin - arresting mitosis; G2 and M phase specific (mitosis!); axonal transport disruption
Side effect profile: Peripheral neuropathy, highly myelosuppressive, myalgias, severe hypersensitivity
Other Drugs: Docetaxel (Taxotere) - MORE TOXIC |
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Definition
Anti-CA drug; Topoisomerase Inhibitor
Use: Testicular cancer
Mechanism: forms comples with topoisomerase II resulting in strand breakage of DNA and cell death
Tox: leukopenia, BM suppression
Other Drug: Tenoposide (Vumon®) |
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Definition
Anti-CA drug: Topoisomerase Inhibitor
Use: Ovarian cancer
Mechanism: topoisomerase I inhibitor
Toxicity: BM myelosuppression, anemia, leukopenia, thrombocytopenia and neutropenia
Other Drugs: Irinotecan (Camptosar®)
Asparaginase (Elspar®) - ALL, asparagine only used by neoplastic cells, hydrolysis asparagine, leading to hypersensitivity
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Term
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Definition
Tyrosine Kinase Inhibitor
PROTOTYPE
Use: CML
Mechanism: Inhibits Bcr-Abl tyrosine kinase (CML causing)
metabolized by CYP3A4
Side effects: GI, Diarrhea
Other Drugs: Dasatanib
Erlotinib
Gefinitib |
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Definition
Growth Factor Receptor Inhibitor
Mechanism: Binds to epidermal growth factor receptor (EGFR), blocking signals for cell growth and survival
Other Drugs: Panitimumab (Vectibix®) |
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Term
Bevacizumab (Avastin)
KNOW |
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Definition
Growth Factor Receptor Inhibitor
Use: clear cell renal carcinoma, blioblastoma; injected in eye for macular degeneration
Mechanism: inhibits angiogenesis by blocking vascular endothelial growth factor (VEGF)
Side effect: HTN, proteinuria, thromboembolism; vessel injury and bleeding, delay Sx in pts on this drug
Other Drugs: Sorafenib
Sunitinib - kidney
Pazopanib |
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Term
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Definition
Hormone or antagonist
Use (which CA): Leukemia and lympoma
Mechanism: suppresses mitosis in lymphocytes
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Term
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Definition
Hormone or Antagonist
Use (which CA): prevention of breast CA (prior Hx); therapy of breast cancer
Mechanism: estrogen antagonist in breast
Activated by CYP2D6 |
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Definition
Hormone or Antagonist
Use (which CA): Metastatic breast cancer
Mechanism: Ab against HER2 protein; only used in pts with HER2 overexpression
Side effect: Cardiomyopathy (DON'T COMBINE WITH DOXIRUBICIN) |
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Definition
Hormone or antagonist
Use (which CA): Metastatic prostate carcinoma
Mechanism: blocks androgen receptor of androgen sensitive tissue or tumors |
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