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18 Cards in this Set

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Methotrexate (MTX)

1)MOA
2)Use
3)Toxicity
1) Specific to S-phase. Analog to Folic Acid that inhibits Dihydrofolate Reductase (makes THF)--> lower dTMP--> lowers DNA synthesis

2) Leukemia, Lymphoma, choriocarcinoma,sarcoma, abortion, ectopic pregnancy, RA, psoriasis

3) Meylosuppression, which is overcome by leucovorin (folinic acid)
5-Fluorouracil (5-FU)

1)MOA
2)Use
3)Toxicity
1) S Phase specific. Acivated to 5F-dUMP which complexes Folic Acid, and inhibits Thymidylate Synthase. No thymidylate Synthase means no dTMP from Methyl-THF --> decrease DNA synthesis

2)Colon Cancer, solid tumors, basal cell (topical)
Acts in Synergy with MTX

3) Myelosuppression that is NOT reversible, and Photosensitivity
6-mercaptopurine (6-MP)

1)MOA
2)Use
3)Toxicity
1) Prevents de novo Purine snythesis after activation from HGPRTase

2) Leukemia, Lymphoma (not CLL or Hodgkin's)

3) Bone Marrow toxicity, GI problems, Liver. It is broken down by Xanthine Oxidase, so someone with gout taking Allopurinol can become toxic
Cytarabine (ara-C)

1)MOA
2)Use
3)Toxicity
1) Block DNA polymerase
2) AML
3)Leukopenia, Thrombocytopenia, Megaloblastic anemia
Cyclophosphamide, Isosfamide

1)MOA
2)Use
3)Toxicity
1)Alkylating agent that cross links DNA strands via Guanine residues after activation in liver

2)NHL, Breast, Ovarian, Wegener's Granulomatosis (C-ANCA)

3)Myelosuppression, hemorrhagic cystitis, Bladder cancer (trt with Mesna)
Nitrosureas (-stine ending, and streptozocin)
1)MOA
2)Uses
3)Toxicity
1)Alkylate DNA after bioactivation. Crosses BBB

2) Brain tumors --> Glioblastoma multiforme

3)CNS toxicity -->dizzy, ataxia
Cisplatin, Carboplatin

1)MOA
2)Use
3)Toxicity
1)Alkylating agents -->cross link DNA

2) Testicular, Bladd, Ovarian, Lung Cancer

3) Nephrotoxic, Acoustic Nerve Damage
Busulfan
1)MOA
2)Use
3)Toxicity
1) Alkyates DNA
2)CML
3)Pulmonary Fibrosis, Hyperpigmentation
Doxorubicin (Adriamycin), Daunorubicin

1)MOA
2)Uses
3)Toxicity
1)Generates free radicals to intercalate into DNA causing breaks in the chains

2)part of ABVD for Hodgkin's Lymphoma (Adriamycin, Bleomycin), Sarcomas, Solid Tumors

3) Cardiotoxic, alopecia, toxic extravasation (fluids leak out of vessels into tissue)
Dactinomycin (Actinomycin D)
1)MOA
2)Uses
3)Toxicity
1) Intercalates DNA to block replication

2)Wilm's tumor, Ewing Sarcoma, Rhabdomyosarcoma (children's tumors use Actinomycin D)

3) Myelosuppression
Bleomycin
1)MOA
2)Uses
3)Toxicity
1) Induces Free Radicals to break DNA

2) testicular cancer, lymphoma (Hodgkins),

3)Pulmonary Fibrosis, Skin Changes
Etoposide (VP-16)

1)MOA
2)Uses
3)Toxicity
1) g2 phase agent that inhibits Topoisomerase II --> increase DNA degradation

2)Small Cell Lung Cancer, Prostate, Testicular

3) GI irritation, alopecia, Myelosuppression
Prednisone

1)MOA
2)Uses
3)Toxicity
1) Apoptotic??
2) Used in Hodgkin's Lymphoma, CLL, and autoimmune diseases

3) Cushingoid, cataracts, acne, peptic ulcers, hyperglycemia
Tamoxifen, Raloxifene

1)MOA
2)Uses
3)Toxicity
1) Estrogen receptor mixed Agonist/Antagonist (SERMS) that prevent estrogen binding to its receptors

2)Breast Cancer, Osteoporosis

3) Tamoxifen can increase risk of endometrial cancer
Trastuzumab (Herceptin)
1)MOA
2)Uses
3)Toxicity
1) Monoclonal Ab to HER-2 (erb-2) receptor to kill cells overexpressing this receptor

2) Metastatic Breast Cancer

3)Cardiotoxic
Imitinib (Gleevac)

1)MOA
2)Uses
3)Toxicity
1)Myoclonal Ab to bcr-abl Tyrosine Kinase

2) CML, GI stromal tumors

3) Fluid Retention
Vincristine, Vinblastine

1)MOA
2)Uses
3)Toxicity
1)M-phase alkaloids that bind tubulin to prevent mitotic spindle formation

2) Treatment of Lymphoma (MOPP), Wilm's tumor, Choriocarcinoma

3) Vincristine - neurotoxic, ileus
VinBLASTine- BLASTS the marrow
Paclitaxel
1)MOA
2)Uses
3)Toxicity
1) M-phase specific agent that binds tubulin which locks cells in Metaphase (can't break mitotic spindle)

2) Ovarian and Breast Cancer

3) Myelosuppression, Hypersensitvity