Term
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Definition
Cyclophosphamide
- Alkylating agent, newer
- Oral or IV
- Activated by P450 system in liver
- Adverse events: acute ns/vm, delayed BM depression, alopecia
- SIGNATURE EVENT - hemorrhagic cystitis (urinary tract irritation) from acrolein (toxic metabolite), give Mesna to react with acrolein in urine. |
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Term
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Definition
| Mechloroethamine
- Alkylating agent (1st), nitrogen mustard, "unguided missle"
- IV only, caustic, short half life
- Adverse affects: acute ns/vm, delayed |
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Term
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Definition
Cis-Platin
- Alkylating agent, cross links, blocks DNA synthesis
- IV, cleared in urine
- Adverse Events: severe ns/vm
- Less BM Depression, dose limiting Renal toxicity (ensure hydration) |
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Term
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Definition
Methotrexate
- Antimetabolite: Folate analog, DHFR substrate and inhibitor (can't "renew" folate for another round)
- Blocks production of DNA bases
- IV or intrathecally, excreted in urine
- Sometimes given in high dose, with folinic acid "rescue"
- Adverse affects: BM and GI
- Chronic use: hepatotoxicity |
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Term
| 6-mercaptopurine/6-thiogaunine |
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Definition
6-Mercaptopurine/6-thiogaunine
- Antimetabolites: Purine analogs
- Oral admin, well tolerated
- Blocks DNA/RNA synthesis
- 6-MP inhibits AMP/GMP formation
- 6-TG incorporated, alters function
- Adverse: BM depression only at high doses
- decreased hprt activity leads to resistance |
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Term
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Definition
5-fluorouracil/Cytarabine
- Antimetabolites: pyrimidine analogs
- 5-FU inhibits thmidylate synthase ("thymineless death"), enhanced by folinic acid
- Cytarabine - C analog, chain termination
- Adverse: more toxic than purines, BM depression, GI |
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Term
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Definition
Vinblastine
- Plant Vinca alkaloids: no tubulin polymerization, disrupts MT spindle, casuses metaphase arrest
- IV admin, biliary excretion
- Adverse: n/v, alopecia, Bone marrow depression |
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Term
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Definition
Vincristine
- Plant Vinca alkaloids: no tubulin polymerization, disrupts MT spindle, casuses metaphase arrest
- IV admin, biliary excretion
- Adverse: less BM toxic than vinblastine, no ns/vm, limited by peripheral neuropathy (think MT transport) |
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Term
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Definition
Paclitaxel/Docetaxel
- Plant alkaloids, Taxanes
- IV in Cremophor (nasty detergent), big greasy molecules
- Stabilizes MTs, blocks mitotic progress
- Adverse: hypersensitivity, nausea (from cremophor), delayed BM supression, neuropathy |
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Term
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Definition
Etoposide (VP-16)
- Plant alkyloid Podophyllotoxins - topoisomerase inhibitor, causes DS breaks, degredation
- CCS - arrest cells in S-G2 stage
- Oral or IV
- Adverse: NS/VM, alopecia, BM suppression |
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Term
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Definition
Doxorubicin/Daunorubicin (rubicin = red)
- Antitumor antibiotics anthracyclines: intercalate flat structure into DNA, don't alkylate
- Block topoisomerase, inhibit synthesis, DS breaks
- Generate free radicals
- IV, metabolized in liver
- Adverse: BM suppression, GI, severe alopecia
- Cardiotoxicity is dose limiting, lifetime dose. Caused my mitochondrial death |
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Term
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Definition
Bleomycin
- Antitumor antibiotic, mixture of glycopeptides
- Binds DNA, generate ROS, DS breaks
- CCS - G2
- IV
- Adverse: hypersensitivity, dose limiting pulmonary toxicity, fibrosis |
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Term
| Hydrocortisone/prednisone |
|
Definition
Hydrocortisone/prednisone
- Hormonal, adrenocorticosteroids, suppress immune cell proliferation - leukemia/lymphoma
- Oral
- Adverse: fluid retention, immunosuppression, diabetes |
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Term
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Definition
Anastrazole/Letrozole
- Hormone aromatase inhibitor (blocks estrogen production)
- Similar to antifungal drugs, for ER+ BRCA
- Adverse: mild nausea, headache, delayed fatigue, hot flashes, menopause like symptoms |
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Term
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Definition
Tamoxifen
- Hormome SERM (receptor antagonist), best in post-menopausal women. Antagonist in breast, agonist in endometrium.
- Can be used for prevention, about 5 yrs
- Treatment of ER+ BRCA
- Oral
- Adverse: menopause like, nausea, hot flashes, vaginal bleeding |
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Term
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Definition
Flutamide
- Androgen receptor antagonist, diminish androgen effects
- Used w/ radiation for prostate CA
- Oral admin
- Adverse: mild nausea, hot flushes, transient hepatic effects |
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Term
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Definition
Interferon-alpha
- Biologic agent, cytokine from WBCs
- Alters gene expression, antiviral
- Used for blood cancers, met melanoma, renal cell carcinoma
- Parenteral Admin - other than oral
- Adverse: fever/chills, anorexia, weakness |
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Term
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Definition
Trastuzumab (herceptin)
- Biological, antibody to HER2 oncogene product
- Very effective against HER2+ tumors, when it can get there, can't cross blood/brain barrier
- IV admin
- Adverse: infusion rxns, hypersensitivity, cardiomyopathy |
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Term
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Definition
Imatinib (STI-571)
- Signal trans inhibitor, blocks BCR-ABL kinase, blocks GF signaling in chronic myelogenous leukemia
- Blocks kit kinase in GI stromal tumors
- CA management, not cure
- Adverse: BM suppression, edema/fluid retention, hepatotoxicity |
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Term
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Definition
Gefitinib
- STI, inhibits EGF-R tyrosine Kinase for lung CA,
- IV admin
- Adverse: fever, dyspnea
- CA management, not cure |
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Term
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Definition
Cyclophosphamide, mechlorethamine, cis-platin
NCSS |
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Term
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Definition
Cytarabine, 5-FU, 6-mercaptopurine, methotrexate, thioguanine
ALL ARE CCS |
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Term
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Definition
| Bleomycin, daunorubicin, doxorubicin |
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Term
|
Definition
| anastrazole, flutamide, hydrocortisone, letrozole, prednisone, tamoxifen |
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Term
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Definition
Docetaxel, paclitaxel, Vinblastine, Vincristine
ALL ARE CCS |
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Term
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Definition
| Interferon-a2, trastuzamab |
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Term
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Definition
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Term
| tyrosine kinase inhibitors |
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Definition
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Term
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Definition
| EPO, GM-CSF, Mesna, Ondasetron |
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