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alkylating agent- nitrogen mustard, attacks guanin N7 -CYP450 activation -Acrolein urotoxic metabolite->stop with aggressive hydration and/or MESNA (Na 2-mercaptoethane sulfonate) -CCNS -Non-hodgkin, ovarian, bread, neuroblastoma |
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alkylating agent- nitrosoureas lipophilic-cross BBB -Guanine residues position 6, cells can correct mismatch with AGT, also blocked with temozolamide (stronger) |
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alkylating agent- nitrosoureas lipophilic-cross BBB -Guanine residues position 6, cells can correct mismatch with AGT, also blocked with temozolamide (stronger) |
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alkylating agent -condition BM -CML therapy replaced by Imatinib -pulmonary fibrosis |
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alkylating agent -IV -used for hodgkins |
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alkylating agent -IV/PO -Hodgkins/brain tumors -disulfram like drug |
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alkylating agent- nitrosoureas lipophilic-cross BBB -P/O -Guanine residues position 6, cells can correct mismatch with AGT, also blocked with temozolamide (stronger) -Brain tumors |
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used for chonic alcoholism -stops acid aldehyde breakdown to acidic acid -gives hungover feeling (don't take with alcohol) |
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platinum complex -N7 of guanine -nephrotoxicity- dose limiting -ototoxicity (don't combine with hearing problems or aminoglyocolides) |
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-combined with cisplatin to prevent nephrotoxicity |
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platinum complex -myelosuppression-dose related |
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platinum complex -peripheral sensory neuropathy -dose dependent-pins and needles w/ cold, propioception (can't button shirt) -colon cancer |
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folic acid analog (B9) -blocks dihydrofolate reductase->no synthesis of adenine, guanine, or thymidine -weak acid-secreted with base -polyglutanated to active for and at high levels go to 7-OH methotrexate->crystalluria->hydration and alkalinization of urine to prevent -other drugs-trimethaprime (antimicrobial) and pyromethamine (anti-protozoa) -anticancer, immunosuppressant, and anti-inflammatory -leucovorin rescues normal cell from toxicity |
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purine analog -needs hypoxanthine-guanine phophoribosyl transferase (HSPRT) to activate-deficiency in Lesch-Nyan -allopurinol increase [] -ALL |
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purine analog -needs hypoxanthine-guanine phophoribosyl transferase (HSPRT) to activate-deficiency in Lesch-Nyan -allopurinol increase [] -AML |
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pyrimidine analog -must go active 5-FdUMP -binds with cofacter n5n10 methylene , thyidylate synthase to stop thymine synthesis -can be used topically for basal cell carcinoma -hand and foot syndrome |
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pyrimidine analog -cytosine arabinoside/ara-C |
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methotraxate rescue- replenishes N N methylene tetrahydrofolate -leucovorin=folinic acid which is converted to N5N10 methylent THF which bypasses DHF reducatase and be used to make nucleic acids |
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-turns to 5-FU with thymidine phosphorylase (primarily concentrated in tumors->more specific) |
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Camptothecin group topoisomerase I religation -s phase only -BMS and diarrhea |
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Camptothecin group topoisomerase I religation -s phase only -BMS and diarrhea |
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podophyllotoxin group -topoisomerase II religatino -S and G2 phase specific -BMS |
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-stops the polymerization of microtubules in spindles -M phase specific -no BMS, peripheral neuropathy, CNs, and autonomic CDS |
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-stops the polymerization of microtubules in spindles -M phase specific -BMS |
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-blocks the break down of microtuble spindles -M phase specific -BMS |
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-blocks the break down of microtuble spindles -M phase specific -BMS |
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-antinomycin D -anti-cancer antibiotics- derived from steptomyces -DNA intercalation, Topo II inhibition, and free radicals -BMS -no CCNS |
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anticancer antibiotics (larger group) -DNA intercalation, inhibition of topo II, and generation of free radicals -resistance-superoxide dismutase (usually in normal cells, but not in cardiac or tumor cells) -BMS and cardiac toxicity -"rubican" -reversible arrythmias->CHF -take dexrazoxane |
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anticancer antibiotics -DNA intercalation, inhibition of topo II, and generation of free radicals -resistance-superoxide dismutase (usually in normal cells, but not in cardiac or tumor cells) -BMS and cardiac toxicity -"rubican"- rubi red heart -reversible arrythmias->CHF -take dexrazoxane |
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-anticancer antibiotic -forms DNA-Fe-Bleomycin complex->develops radicals->DNA strand breaks -G2 phase specific (the only one) -bleomycin hydrolase in normal cells or in resistance -pulmonary and skin toxicity because of no hydrolase (pneumonitis, pulmonary fibrosis) -amiodaron (class III andti arrythmic) and busulfan can also cause pulmonary problems -more O2->more ROS->higher toxicity |
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-GnRH agonist -non-pulsatile stimulation of anterior pituitary-> desensitization->no LH and reduce testosterone production -stops prostate cancer growth |
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-estrogen antagonist -inactivates estrogen signal transduction -SERM-selective estrogen receptor modulator (acts as antagonist and agonist in different tissues) -breast-antagonist, bone and other tissue-agonist :) -used for breast cancer -doesn't work if no receptor in cancer and is resistance if from loss of recpetor -hot flashes, N and V |
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-aromatase inhibitor- stops the extraovarian conversion of androstenedione ->estrogen by aromatase in postmenopausal women -breast cancer in postmen. women -most be receptor positive -can be used with tamoxifen resistance |
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-corticosteroids-supresses mitosis in lymphocytes -leukemia/lymphoma -supresses hypersensitivity, edema, pain, and inflammation from other drugs or cancer -side effects-osteoporosis, psychosis, glucose intolerance |
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-GnRH agonist -non-pulsatile stimulation of anterior pituitary-> desensitization->no LH and reduce testosterone production -stops prostate cancer growth |
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-aromatase inhibitor- stops the extraovarian conversion of androstenedione ->estrogen by aromatase in postmenopausal women -breast cancer in postmen. women -most be receptor positive -can be used with tamoxifen resistance |
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-aromatase inhibitor- stops the extraovarian conversion of androstenedione ->estrogen by aromatase in postmenopausal women -breast cancer in postmen. women -most be receptor positive -can be used with tamoxifen resistance |
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-stops tumor cells producing asparagine-->turns all asparagine to aspartic acid and ammonia (which can also be used by normal cells to get asparagine -G1 phase specific -can cause hypersensitivity rxns -used for ALL |
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-stops ribonucleotide reductase (cannot form deoxyribonucleotides) -G1 and S phase specific -BMS - |
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cytarabine, 6-mercaptopurine, 6-thioguanine, methotrexate, hydroxyurea, etoposide, 5-FU |
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podophyllotoxin group -topoisomerase II religatino -S and G2 phase specific -BMS |
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bleomycin, busulfan, procarbazine |
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docorubicin, daunorubican |
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vincritine, cisplatin (oto) |
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cyclophosphamide, methotrexate |
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IL-2, increase lymphocyte differenttiaion and NK -use in renal cell cancer and metastatic melanoma |
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G-CSF -increase granulocytes-used in marrow recovery |
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GM-CSF -increase granulocytes and macrophages-used in marrow recovery |
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