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Chemo Drugs/GN Wk 2
chemo drugs
29
Medical
Graduate
10/12/2008

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Cards

Term
Cyclophosphamide
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.
Term
Mechloroethamine
Definition
Mechloroethamine - Alkylating agent (1st), nitrogen mustard, "unguided missle" - IV only, caustic, short half life - Adverse affects: acute ns/vm, delayed
Term
Cis-Platin
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)
Term
Methotrexate
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
Term
6-mercaptopurine/6-thiogaunine
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
Term
5-Flurouracil/Cytarabine
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
Term
Vinblastine
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
Term
Vincristine
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)
Term
Paclitaxel/Docetaxel
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
Term
Etoposide
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
Term
Doxorubicin/Daunorubicin
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
Term
Bleomycin
Definition
Bleomycin
- Antitumor antibiotic, mixture of glycopeptides
- Binds DNA, generate ROS, DS breaks
- CCS - G2
- IV
- Adverse: hypersensitivity, dose limiting pulmonary toxicity, fibrosis
Term
Hydrocortisone/prednisone
Definition
Hydrocortisone/prednisone
- Hormonal, adrenocorticosteroids, suppress immune cell proliferation - leukemia/lymphoma
- Oral
- Adverse: fluid retention, immunosuppression, diabetes
Term
Anastrazole/Letrozole
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
Term
Tamoxifen
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
Term
Flutamide
Definition
Flutamide
- Androgen receptor antagonist, diminish androgen effects
- Used w/ radiation for prostate CA
- Oral admin
- Adverse: mild nausea, hot flushes, transient hepatic effects
Term
Interferon-alpha
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
Term
Trastuzumab
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
Term
Imatinib
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
Term
Gefitinib
Definition
Gefitinib
- STI, inhibits EGF-R tyrosine Kinase for lung CA,
- IV admin
- Adverse: fever, dyspnea
- CA management, not cure
Term
alkylating agents
Definition
Cyclophosphamide, mechlorethamine, cis-platin
NCSS
Term
Antimetabolites
Definition
Cytarabine, 5-FU, 6-mercaptopurine, methotrexate, thioguanine
ALL ARE CCS
Term
Anti-tumor antibiotics
Definition
Bleomycin, daunorubicin, doxorubicin
Term
Hormonal agents
Definition
anastrazole, flutamide, hydrocortisone, letrozole, prednisone, tamoxifen
Term
MT poisons
Definition
Docetaxel, paclitaxel, Vinblastine, Vincristine
ALL ARE CCS
Term
Biologicals
Definition
Interferon-a2, trastuzamab
Term
topoisomerase inhibitors
Definition
etoposide (VP-16) CCS
Term
tyrosine kinase inhibitors
Definition
gefitinib, imatinib
Term
Ancillary Agents
Definition
EPO, GM-CSF, Mesna, Ondasetron
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