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Anti-cancer drugs
Anti-cancer drugs
56
Medical
Professional
04/19/2011

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Term
cyclophosphamide
Definition
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
Term
carmustine
Definition
alkylating agent- nitrosoureas
lipophilic-cross BBB
-Guanine residues position 6, cells can correct mismatch with AGT, also blocked with temozolamide (stronger)
Term
lamustine
Definition
alkylating agent- nitrosoureas
lipophilic-cross BBB
-Guanine residues position 6, cells can correct mismatch with AGT, also blocked with temozolamide (stronger)
Term
busulfan
Definition
alkylating agent
-condition BM
-CML therapy replaced by Imatinib
-pulmonary fibrosis
Term
dacarbazine
Definition
alkylating agent
-IV
-used for hodgkins
Term
procarbazine
Definition
alkylating agent
-IV/PO
-Hodgkins/brain tumors
-disulfram like drug
Term
Temozolamide
Definition
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
Term
disulfram
Definition
used for chonic alcoholism
-stops acid aldehyde breakdown to acidic acid
-gives hungover feeling (don't take with alcohol)
Term
cisplatin
Definition
platinum complex
-N7 of guanine
-nephrotoxicity- dose limiting
-ototoxicity (don't combine with hearing problems or aminoglyocolides)
Term
amifostine
Definition
-combined with cisplatin to prevent nephrotoxicity
Term
carboplatin
Definition
platinum complex
-myelosuppression-dose related
Term
oxaliplatin
Definition
platinum complex
-peripheral sensory neuropathy -dose dependent-pins and needles w/ cold, propioception (can't button shirt)
-colon cancer
Term
methotrexate
Definition
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
Term
6-mercaptopurine
Definition
purine analog
-needs hypoxanthine-guanine phophoribosyl transferase (HSPRT) to activate-deficiency in Lesch-Nyan
-allopurinol increase []
-ALL
Term
6-thioguanine
Definition
purine analog
-needs hypoxanthine-guanine phophoribosyl transferase (HSPRT) to activate-deficiency in Lesch-Nyan
-allopurinol increase []
-AML
Term
5-fluorouracil
Definition
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
Term
cytarabine
Definition
pyrimidine analog
-cytosine arabinoside/ara-C
Term
leucovorin
Definition
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
Term
capecitabine
Definition
-turns to 5-FU with thymidine phosphorylase (primarily concentrated in tumors->more specific)
Term
irinotecan
Definition
Camptothecin group
topoisomerase I religation
-s phase only
-BMS and diarrhea
Term
topotecan
Definition
Camptothecin group
topoisomerase I religation
-s phase only
-BMS and diarrhea
Term
etoposide
Definition
podophyllotoxin group
-topoisomerase II religatino
-S and G2 phase specific
-BMS
Term
vincristine
Definition
-stops the polymerization of microtubules in spindles
-M phase specific
-no BMS, peripheral neuropathy, CNs, and autonomic CDS
Term
vinblastin
Definition
-stops the polymerization of microtubules in spindles
-M phase specific
-BMS
Term
paclitaxel
Definition
-blocks the break down of microtuble spindles
-M phase specific
-BMS
Term
docetaxel
Definition
-blocks the break down of microtuble spindles
-M phase specific
-BMS
Term
dactinomycin
Definition
-antinomycin D
-anti-cancer antibiotics- derived from steptomyces
-DNA intercalation, Topo II inhibition, and free radicals
-BMS
-no CCNS
Term
anthracycline
Definition
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
Term
doxorubican
Definition
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
Term
bleomycin
Definition
-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
Term
leuprolide
Definition
-GnRH agonist
-non-pulsatile stimulation of anterior pituitary-> desensitization->no LH and reduce testosterone production
-stops prostate cancer growth
Term
tamoxifen
Definition
-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
Term
anastrazole
Definition
-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
Term
prednisone
Definition
-corticosteroids-supresses mitosis in lymphocytes
-leukemia/lymphoma
-supresses hypersensitivity, edema, pain, and inflammation from other drugs or cancer
-side effects-osteoporosis, psychosis, glucose intolerance
Term
goserelin
Definition
-GnRH agonist
-non-pulsatile stimulation of anterior pituitary-> desensitization->no LH and reduce testosterone production
-stops prostate cancer growth
Term
letrozole
Definition
-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
Term
exemestare
Definition
-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
Term
L-asparaginase
Definition
-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
Term
hydroxyurea
Definition
-stops ribonucleotide reductase (cannot form deoxyribonucleotides)
-G1 and S phase specific
-BMS
-
Term
G2 specific
Definition
bleomycin
Term
S phase
Definition
cytarabine, 6-mercaptopurine, 6-thioguanine, methotrexate, hydroxyurea, etoposide, 5-FU
Term
teniposide
Definition
podophyllotoxin group
-topoisomerase II religatino
-S and G2 phase specific
-BMS
Term
G1 phase
Definition
L-asparaginase
Term
Renal toxicity
Definition
cisplatin, methotrexate
Term
pulmonary
Definition
bleomycin, busulfan, procarbazine
Term
cardiac toxicity
Definition
docorubicin, daunorubican
Term
neruologic toxicity
Definition
vincritine, cisplatin (oto)
Term
Immunosupressive
Definition
cyclophosphamide, methotrexate
Term
hemorrhagic cystitis
Definition
cycophosphamid
Term
causes leukemia
Definition
procarbazine
Term
causes pancreatitis
Definition
asparaginase
Term
aldesleukin
Definition
IL-2, increase lymphocyte differenttiaion and NK
-use in renal cell cancer and metastatic melanoma
Term
IL-11
Definition
increase platlets
Term
filgrastim
Definition
G-CSF
-increase granulocytes-used in marrow recovery
Term
sargramostim
Definition
GM-CSF
-increase granulocytes and macrophages-used in marrow recovery
Term
Dexrazoxane
Definition
cardiac protective
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