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50 Cards in this Set
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drugs that target cell wall synthesis
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cycloserine
bacitracin vancomycin b lactams |
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cycloserine
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target cell wall synthesis;
interferes with production of D-alanine and its coupling |
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bacitracin
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target cell wall synthesis;
interfers with cycling lipid carrier that transfer PG subunits |
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vancomycin
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target cell wall synthesis;
prevents crosslinking/elongation of repeating disaccharide (NAG-NAM) subunits |
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B lactams: penicillin
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blocks crosslinking of PGs
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folate antagonists
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trimethoprim (bacteria), pyrimethamine (malarial parasite), methotrexate (ALL cancer cells)
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5-FU
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blocks thymidine biosynthesis and is a pyrimidine analog
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Ara-c
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mercaptopurine
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pyrimidine analog, inhibitor of DNA replication and repair polymerases
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cell membranes targets; anti fungals
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polymixin, amphotericin B, nystatin
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protein synthesis inhibitors
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chloramphenicol, tetracyclines, erythromycin, streptogramins, linezolid
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translational miscoding
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aminoglycosides
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Clavulanic acid
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mimic of b-lactams, helps circumvents resistance. This drug doesn’t interfere with crosslinking though and needs to be added with penicillin.
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Cephalosporins
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B-lactam like. They differ in side chain from penicillin, and if something is resistant to penicillin, it might not be to cephalosporins
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50S subunit inhibitors
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macrolides
chloramphenicol lincosamides streptogramins oxazolidinones |
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30S subunit
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aminoglycosides
spectinomycin tetracyclines |
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aminoglycoside
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bind rRNA in 30S subunit and binds incorrect tRNA. nephrotocity and ototoxicity ex: gentamicin and streptomycin
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tetracycline
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blocks a.a tRNA binding to A site; bacteriostatic, pGI problems, chelates Ca and is not rec for children and pregnant women
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chloramphenicol and lincosamides
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inhibit peptidyl transferase; chlorampenicol = bacteriostatic. side effects = bone marrow depression, grey baby
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streptinomycin, macrolides, streptogramins
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inhibit peptide translocation.
macrolides= bacteriocidal/static. can cause jaundice lincosamides = can cause pseudomembranous colitis streptogramins = synergistic (with quinupristin which binds 50s), active against drug resistance |
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fusidic acid
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narrow spectrum Ab, inhibits protein syn; bone infections; side effects: gi
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oxalazidonones
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inhibit fMet-tRNA binding to large subunit, active against drug resistance
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Topo II inhibitors
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quinolones, ciprofloxacin
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topo I inhibitor
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camptothecin
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folic acid competitve inhibitors
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sulfanilamide, sulfadiazine
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DHFR inhibitors
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trimethoprim
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transduction
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bacterial gene spreads through bacteriophage
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transformation
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bacteria takes up DNA from its environment
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antiviral--inhibitors of gp41 fusion in HIV
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maraviroc--CCR5 inhbitor
enfuvirtide--HR2 mimic that hides fusion protein and prevents membrane fusion |
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antiviral--inhibit M2 channel to prevent flu virus uncoating
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amantadine
rimantadine |
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acyclovir
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purine analog. chain terminator in DNA
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non-nu antiviral
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inhibit base pair checking in DNA polymerase
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anthracycline antibiotics
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DNA intercalating agents and inhibitors of topo II
daunorubicin, doxorubicin, mitoxantrone |
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camptothecins
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topo I poisons (stabilized topo I-DNA adduct)
other -tecans. TDP1 hydrolyzes the bond, form of resistance. |
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DNA alkylating agents
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reacts to form covalent adduct with DNA bases
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nitrosoureas
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alkylating agent for CNS tumors
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cisplatin/carboplatin
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DNA crosslinking agents for treating testicular and ovarian cancers
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6-thiopurines
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mercapto-, thioguanine.
-loss of HGPRT -> resistance allopurinol blocks oxidation of drugs |
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2-deoxycoformycin (pentostatin)
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inhibits adenosine deaminase -> adenosine buildup; used for leukemia.
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hydroxy urea
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inhibits pulrine salvage, deplete dNTP pools
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vinca alkyloids (vinblastine, vincristine)
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bind to b-tubulin, interfere with spindle apparatus
vinblastine = metastitic testicular cancer vincristine = childhood leukemia |
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taxanes
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bind MTs, prevent disassembly and remodeling
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cetuximab
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monoclonal ab. interferes with EGFR signaling, treats metastatic colorectal cancer
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bevacizumab
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monoconal ab against VEGF, VEGFR-2
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gemtuzumab
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monoclonal Ab agonist that targets AML cells, linked to an antibiotic that causes DNA fragmentation
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glucocorticoids
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suppress mitosis in lyphocytes
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SERM
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selective estrogen R modulators
ie: tamoxifen--competitve antagonist |
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SERD
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selective estrogen R downregulator; "pure anti-estrogens"
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fulvestrant
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anti-estrogen that prevents estrogen R dimerization and R degredation
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aromatase inhibitors
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type 1: irreversibly inactivate aromatase, bind substrate site
type 2: reversibly binds to heme group |
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P-glycoprotein
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P-gp pumps drugs out of Gi, CNS, cancer cells.
Substrates: digoxin, fexofenadine, cyclosporine, tacrolimus, loperamide |
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