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40 Cards in this Set
- Front
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In general, Alkylating agents
MOA: uses: S/E: |
MOA: bind to ds DNA
uses: slow growing cancer S/E: n/v |
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clue for slow growing cancer
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did not appear til >40 y/o
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How can we treat the n/v these pts will inevitibly get?
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Ondansetron
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Cyclophosphamide
MOA: uses: S/E: reverse: |
MOA: require bioactivation by liver (pro-drug); covalently link DNA interstrand (x-link) at guanine N-7.
uses: Non-Hodgkins, Ovaries, Breast, Wegner's, Polyarterits Nodosa "NOB" tox: hemorrhagic cystitis reverse tox with Mesna |
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Nitrosoureas
examples: MOA: uses: S/E: |
examples: -mustines, streptozocin
MOA: require bioactivation by liver (pro-drug); alkylate DNA; crosses BBB uses: brain tumors (esp. glioblastoma multiforme), Hodgkins tox: neurotox |
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Cisplatin, Carboplatic
MOA: uses: S/E: |
MOA: cross-link DNA
uses: bladder, ovary, lung, testicles "BOLT" tox: nephrotox, ototox |
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Busulfan
MOA: uses: S/E: |
MOA: alkylates DNA
uses: CML, transplant of hemopoetic cells S/E: pulmonary fibrosis, hyperpigmentation |
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Adriamycin/ Doxorubacin/ Daunorubacin
MOA: uses: S/E: |
MOA: generate free rads and squeeze into (intercalte in) DNA; create breaks in DNA strand to dec replication
uses: Myeloma, Hodgkins, Sarcoma, Solid tumors "My heart so sick" tox: cardiotoxic (dilated cardiomyopathy), alopecia |
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Dactinomycin/ Actinomycin D
MOA: uses: tox: |
MOA: intercalates in DNA
uses: Ewings, Wilm's, Rhabdomyosarcoma tox: BM suppression |
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Bleomycin
MOA: uses: tox |
MOA: generate free rads and squeeze into (intercalte in) DNA; create breaks in DNA strand to dec replication
uses: Hodgkins, Testicular Tox: Pulm fibrosis, skin changes, minimal BM suppression |
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Alkylating agents that cause
1) pulm fibrosis 2) skin changes (i.e. darker) |
bleomycin, busulphan
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Alkylating agents that cause
cardiomyopathy |
1) adriamycin (Doxyrubacin/ Donarubacin)
2) Transtuzimab |
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Alkylating agents that cause
damage to renal PCT |
Cisplatin
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Alkylating agents that cause
hemorrhagic cystitis |
cyclophosphamide, isophosphomide
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Alkylating agents that block ETC
(antimitochondria) |
Antimycin
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Alkylating agent used for Multiple Myeloma
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Melphalan
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Alkylating agents used for Hodgkins
2 treatment regimens |
1st line:Mechlorethamine, Procarbazine, Dacarbazine,
other: Vinblastine, Vincristine, Adriamycin, Transtuzamab, Bleomycin, Prednisone regimen: Mustine, Oncovin (vincristine), Procarbazine, Prednisone "MOPP" regimen: Adriamycin, Bleomycin, Vinblastin, Decarbazine "ABVD" |
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MC used alkylating agent
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Chlorambucil
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Toxicity of chlorambucil
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Neuro (seizures, tremors, hallucinations, confusion)
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Rescue for
1) adriamycin 2) cyclophosphomide 3) cisplatin |
1) Desroxzasane
2) mesna 3) amifastine |
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Hydroxyurea
MOA: uses: S/E: |
MOA: S phase; inh ribonucleotide reductase (thus dec DNA synth)
uses: Sickle cell (inc HbF), melanoma, CML S/E: BM suppression, GI upset |
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Etoposide (VP-16)
MOA: uses: S/E: |
MOA: late S phase, early G2 phase; inh topoisomerase II; inc DNA degredation
uses: small cell CA of lung, prostate, testicular S/E: allopecia |
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Raloxifene, Tamoxifene
MOA: (in general) 3 sites cells with estrogen rec; at which sites is it agonist, partial agonist, antagonist uses: S/E: |
MOA: binds estrogen receptors found in breast, bone, uterus
agonist: -Ralox & Tamox: bone antagonist: -Ralox & Tamox: breast -Ralox- endometrium partial agonist: -Tamox- endometrium uses: breast cancer, prevent osteoporosis S/E: hot flashes, Tamox may increase risk of endometrial cancer. |
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Transtuzumab
MOA: uses: tox: |
MOA: monoclonal Ab against HER-2 (erb-2); kills cancer via Ab dependent cytotoxicity (type 2 HPY)
uses: METASTATIC breast cancer, Myeloma, Hodgkins, Sarcoma, Solid tumors "my heart so sick" Tox: cardiomyopathy |
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Vincristine/Vinblastine
MOA: uses: tox: |
MOA: M phase; block formation (polymerization) of microtubules
uses: ChorioCA, Hodgkins, Wilm's tumor "CHW" tox: -Vincristine: neurotoxic, paralytic ileus -Vinblastin: *BLASTS BM |
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Imatinib (Gleevac)
MOA: uses: tox: |
MOA: inh corrupt tyrosine kinase activity of bcr-abl
uses: CML, GI stroma tumors tox: fluid retention |
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Paclitaxel, -taxol
MOA: uses: tox: |
MOA: M phase; hyperstabilize microtubles that have already been formed (polymerized); ANAphase cannot occur.
uses: ovarian, breast tox: BM supp, hypersensitivity |
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Prednisone:
MOA: uses: tox: |
MOA: triggers apoptosis (anti-neoplastic); also in phospholipase A breakdown (immunosupprent)
uses: 1) anti-neoplastic quality used in CLL, Hodgkins (not treated by 6MP) 2) immunosupp quality used in autoimmune dz's tox: 1) high cortisol/stress effects: Cushing's-like symps, immunosuppress, acne, PUD, hyperglycemia, demargination (inc WBC), K low (has aldosterone effects) HTN= "PICK'D HAG" 2) other: cataracts, osteoporosis, psychosis= "COP" "COP PICK'D HAG" |
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L-asparaginase
MOA: S/E: |
MOA: knocks out asparigine (takes cells source of nutrition away, to try to kill them)
S/E: ***anaphylaxis |
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Which drug treats CLL?
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Prednisone
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Which two drugs are pro-drugs (need activation by liver?
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1) cyclophosphamide needs oxidation by CYP450 to be activated
2) nitrosureas (mustines) "must" be activated by ????? |
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Which drugs treat CML?
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Busulfan
Hydroxyurea Imatinib |
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Which drugs are S phase specific?
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Antimetabolites (esp 5FU and 6MP)
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Which drugs are G2 phase specific?
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Etoposide (late S, early G2)
Bleomycin Vincristin Vinblastin |
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Which drugs are M phase specific?
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Paclitaxel
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Which drugs treat NonHodgkins?
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Cytarabine (antimetabolite)
Cyclophosphomide (alkylating agent) |
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Which drugs treat Choriocarcinoma?
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Vincristin/Vinblastin (alkylating agents)
Methotrexate (antimetabolite) |
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1st and 2nd sign of doxyrubicin assoc cardiomyopathy
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1st: swelling of sarco retic
2nd: loss of cardiomyocytes ("myofibrillar dropout") |
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Dexrazoxane
MOA: uses: |
MOA: Fe-chelating agent; decreases formation of oxygen free rads
uses: antidote for doxorubicin |
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Aromatase inh
ex: MOA: uses: |
ex: anastrozole, letrozole, exmestane
MOA: inh the synthesis of Estrogen from from androgens uses: *** equivalent or SUPERIOR to Tamoxifen in treatment of breast cancer |