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45 Cards in this Set
- Front
- Back
Cell Cycle Specific Drugs:
-name them (5) |
1. antimetabolites (MTX, 5-FU, 6-MP)
2. etoposide 3. bleomycin 4. vinca alkaloids 5. paclitaxel |
|
Cell Cycle Nonspecific Drugs:
-name them (2) |
1. alkylating agents
2. antibiotics (dactinomycin, doxorubicin, bleomycin) |
|
Site of action - name cancer drug:
1. nucleotide synthesis 2. DNA 3. mRNA 4. protein |
1a. MTX + 5-FU - decrease thymidine synth
1b. 6-MP - decrease purine synth 1c. Cytarabine 2a. Alkylating agents + cisplatin - DNA cross-linkage 2b. Dactinomycin + doxorubicin - DNA intercalation 2c. Bleomycin - strand breakage + DNA intercalation 2d. Etoposide - strand breakage 3. Steroids 4a. Tamoxifen 4b. Vinca alkaloids - inhibit MT formation 4c. Paclitaxel - inhib MT disassembly |
|
Which drugs block...
1. S phase 2. G2 phase 3. M phase |
1. antimetabolites, etoposide
2. bleomycin, etoposide 3. vinca alkaloids, taxols |
|
Methotrexate (MTX)
-mech |
-S-phase specific antimetabolite
-folic acid analog that inhibits DIHYDROFOLATE REDUCTASE (decreases dTMP -> decr DNA and prot synth) |
|
MTX
-clin use |
-leukemias, lymphomas
-choriocarcinoma, sarcomas -abortion, ectopic pregnancy -rheumatoid arthritis, psoriasis |
|
MTX
-toxicity? -reversible with? |
-MYELOSUPPRESSION reversible with LEUCOVORIN (folinic acid) rescue
-Macrovesicular fatty change in liver |
|
5-Fluorouracil (5-FU)
-mechanism |
-S-phase specific antimetabolite
-pyrimidine analog bioactivated to 5F-dUMP (covalently complexes folic acid)- inhibits THYMIDYLATE SYNTHASE) -results in decreased dTMP and same effects as MTX |
|
5-FU
-clin use |
-colon CA, other solid tumors
-BCC (topical) *SYNERGY with MTX |
|
5-FU
-toxicity? rescue? |
-Myelosuppresion *NOT reversible with leucovorin
-PHOTOSENSITIVITY -can "rescue" with THYMIDINE |
|
6-mercaptopurine (6-mp)
-mech -clin use |
-blocks de novo purine synthesis
-activated by HGPRTase -for leukemias, lymphomas (not CLL or Hodgkins') |
|
6-MP
-toxicity -metabolized by? what drug increases 6-MP toxicity |
-bone marrow, GI, liver
*Metabolized by XANTHINE OXIDASE (thus increased toxicity with ALLOPURINOL) |
|
Cytarabine (ara-C)
-mech -clin use -tox |
-Inhibits DNA polymerase
-AML -tox: leukopenia, thrombocytopenia, megaloblastic anemia |
|
Cyclophosphamide, ifosfamide
-mechanism -need bioactivation? |
Alkylating agents
-covalently x-link (interstrand) DNA at guanine N-7 *Require bioactivation by liver |
|
Cyclophophamide, ifosfamide
-clin use |
Non-hodkin's lymphoma
Breast and Ovarian CA Immunosuppressants |
|
Cyclophosphamide, ifosfamide
-toxicity? prevention? |
-Myelosuppression
-HEMORRHAGIC SYSTITIS (partially prevented tih MESNA) |
|
Mesna - mechanism
-neutralize which metabolits? -what moieties -increase urinary excretion of? |
In vivo, cyclophos/ifosfamide may be converted to urotoxic metabolites such as acrolein. Mesna assists to neutralise these metabolites by binding through its sulfhydryl-moieties, and also increases urinary excretion of cysteine.
|
|
Nitrosureas
-name them (4) "CLSS" |
Carmustine
Lomustine Semustine Streptozocin |
|
Nitrosureas
-mech -req bioactivation? |
Alkylate DNA
Require bioactivatio Cross BBB - CNS |
|
Nitrosureas
-clin use -toxicity |
-for brain tumors (including glioblastoma multiforme)
-tox: CNS toxicity (dizzy, ataxia) |
|
What drugs used for glioblastoma multiforme?
|
Nitrosureas?
-carmustine -lomustine -semusteim -streptozocin |
|
Cisplatin, carboplatin
-mech -clin use -toxicity |
-act like alkylating agents
-for Testicular, Bladder, Ovary, and Lung CAs -tox: NEPHROTOXIC, ACOUSTIC NERVE DAMAGE |
|
Busulfan
-mech -clin use -toxicity |
-alkylates DNA
*for CML tox: PULMONARY FIBROSIS, HYPERPIGMENTATION |
|
Doxorubicin (Adriamycin), daunorubicin
-mechanism |
-generates free radicals
-non covalently intercalate in DNA (create DNA strand breaks, decreasing replication) |
|
Doxorubicin (Adriamycin), daunorubicin
-clin use |
*part of ABVD combination regimen for Hodgkin's and for myelomas, sarcomas, and solid tumors (breast, ovary, lung)
|
|
Doxorubicin (adriamycin), daunorubisin
-toxicity |
CARDIOTOXICITY
MYELOSUPPRESSION *MARKED ALOPECIA Toxic extravasation |
|
Dactinomycin (actinomycin D)
-mech -clin use -toxicity Hint: "children ACT out" |
-intercalates in DNA
-clin use: WILMS's tumor, EWING's sarcoma, RHABDOmyosarcoma -tox: myelosuppression |
|
Bleomycin
-mech -clin use -tox |
-induces formation of free radicals - causes breaks in DNA strands
-for Testicular CA, lymphomas (part of ABVD regimen for Hodgkins') -tox: PULMONARY FIBROSIS, skin changes *minimal myelosuppression* |
|
Etoposide (VP-16)
-mech |
-G2-phase specific agent that inhibits TOPOISOMERASE II and increases DNA degradation
|
|
Etoposide (VP-16)
-clinical use -tox |
Small cell CA of LUNG and PROSTATE; TESTICULAR CA
tox: myelosuppression, GI irritaiton, alopecia |
|
Prednisone
-mech |
-may trigger apoptosis
-may even work on nondividing cells |
|
Prednisone
-clin use |
-most commonly used glucocorticoid in CA chemotherapy
-CLL -Hodgkin's lympohomas (part of MOPP regiment) -also immunosuppressant in autoimmune dz |
|
Prednisone
-tox |
Cushing-like sxs
immunosuppression CATARACTS acne osteoporosis HTN peptic ulcers hyperglycemia psychosis |
|
Tamoxifen, raloxifene
-mech |
-receptor antagonist in breat
-agonist in bone -blocks binding of E to E-receptor+ cells |
|
Tamoxifen, raloxifene
-clin use |
-breast cancer
-prevent osteoporosis |
|
Tamoxifen, raloxifene
-Toxicity (tamox vs. ralox) |
Tamoxifene: may increase risk of endometrial CA via partial agonist effects, hot flashes
Raloxifene - does not cause endometrial CA b/c it's an endometrial ANTAGoNIST |
|
Trastuzumab (herceptin)
-mechanism |
-monoclonal ab vs HER-2 (erb-B2)
-helps kill breast CA cells that overexpress HER-2, possibly through antibody-dependent cytotoxicity |
|
Trastuzumab - other name?
|
Herceptin
|
|
Trastuzumab
-clin use -tox |
-for METASTATIC breast CA
-may cause cardiotoxicity |
|
Imatinib (gleevec)
-mech -clin use -toxicity |
Philadelphia chromosome brc-able tyrosine kinase inhibitor
-for CML and GI stromal tumors tox: fluid retention |
|
Vincristine, Vinblastine
-mechanism |
-M-phase sepcific alkaloids that bind to tubulin and block polymerization of MTs so that mitotic spindle cannot form
|
|
Vincristine, Vinblastine
-clin use |
part of MOPP (Oncovin [vincristine]) regimen for lymphoma, Wilm's tumor, choriocarcinoma
|
|
Vincristine vs. Vinblastine
-toxicity |
Vincristine: NEUROTOXICITY (areflexia, peripheral neuritis) + PARALYTIC ILEUS
VinBLASTine BLASTS Bone marrow (suppression) |
|
Paclitaxel, other taxols
-mech |
M-phase specific agents that bin to tubulin and hyperstabilize polymerized MTs so that mitotic spindle cannot break down (anaphase cannot occur)
|
|
Paclitaxel, other taxols,
-clin use -tox |
-for OVARIAN and BREAST CAs
-tox: Myelosuppression and Hypersenstivity |