Term
Inhibition of cell wall synthesis |
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Definition
Penicillins, cephalosporins, imipenem/meropenem, aztreonam, vancomycin |
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Term
Inhibition of bacterial protein synthesis |
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Definition
Aminoglycosides, chloramphenicol, macrolides, tetracyclines, streptogramins, linezolid |
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Term
Inhibtion of nucleic synthesis |
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Definition
Fluoroquinolones, rifampin |
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Term
Inhibition of folic acid synthesis |
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Definition
Sulfonamindes, trimethoprim, pyrimethamine |
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Term
Penicillin & cephalosporins resistance mechanisms |
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Definition
produces beta-lactamases that cleave the beta lactam ring structure, change the PCN-binding proteins, change in porins |
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Term
Aminoglycosides resistance |
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Definition
Drugs that bacteria develop resistance to (gentamicin, streptomycin, amikacin) Forms enzymes that inactivate drugs via conjugation rxns that trasfer acetyl, phosphoryl etc. groups |
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Term
Macrolides and clindamycin resistance |
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Definition
Drugs erythromycin, azithromycin, clarithromycin etc. Forms methyltransferases that alter drug binding sites on the 50S ribosomal subunit, or active transport of the drug out of cells |
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Term
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Definition
Increased activity of transport systems that "pump" drugs out of the cell |
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Term
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Definition
Change in sensitivity to inhibition of target enzyme, increased formation of of PABA, use of exogenous folic acid |
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Term
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Definition
Change in sensitivity to inhibition of target enzymes (topioisomerase II); increased activity of transport systems that promote drug efflux |
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Term
Chloramphenicol resistance |
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Definition
Formation of inactivating acetyltransferases |
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Term
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Definition
MOA: interact w/ cytoplasmic membrane binding proteins to inhibit transpeptidation rxns involving the bacterial cell wall synthesis Elimination: most via active tubular secretion in kidney, nafcillin, oxacillin eliminated via bile, benzathine pcn G eliminated via repository form SE: hypersensitivity can be any of the type I-IV rxns |
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Term
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Definition
Penicillin G and V Spectrum: gram (+) cocci (strep/penumo/meningo) + Treponema pallidum (G is DOC for syphilis) |
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Term
Very narrow spectrum PCN's |
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Definition
nafcillin, methicillin, oxacillin Spectrum: known or suspected staphylococci (NOT MRSA) |
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Term
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Definition
beta-lactamase sensitive Ampicillin & Amoxicillin Spectrum: gram + cocci (not staph), E.coli, H, influenzae, Listeria monocytogenes (DOC ampicillin) Borrelia burgdorferi, H.pylori (amoxicillin) Activity enhaced if used w/ clavulanic acid which are inhibitors of beta lactamase Synergy w/ aminoglycosides (gentamicin) against enterococcal species |
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Term
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Definition
Ticarcillin, piperacillin, azlocillin Spectrum: everything plus gram (-) rods like Pseudomonas aeruginosa Enhanced activity if used w/ beta-lactamase inhibitors like clavulanic acid and sulbactam Synergy w/ aminoglycosides against Pseudomonas |
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Term
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Definition
Pseudomonas Listeria Enterococcus |
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Term
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Definition
MOA: interact w/ cytoplasmic membrane-binding proteins to inhibit transpeptidation rxns w/in bacterial cell walls Elimination: via active tubular secretion blocked by probenecid, ceftriaxone is eliminated via bile SE: hypersensitivity (rashes/drug fever), disulfiram-like rxn (cefotetan, cefoperazone, cefamandole) hypoprothrombinemia (def. of factor II) |
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Term
Organisms not covered by cephalosporins |
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Definition
Listeria monocytogenes (amp + gent) Atypicals (chlamydia, mycoplasma) MRSA (vancomycin) Enterococci (amp +gent) |
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Term
Narrow spectrum cephalosporins (1st gen.) |
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Definition
cefazolin, cephalexin Spectrum: gram + cocci, Proteus, E.coli, Klebsiella pneumoniae Common in surgical prophylaxis, DO NOT enter CNS |
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Term
Broad spectrum cephalosprorins (2nd gen.) |
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Definition
cefotetan, cefaclor, cefuroxime Spectrum: increasing gram (-) coverage, some anaerobes (Actinomyces, bacteriodes, clostridium) |
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Term
Very broad spectrum cephalosporins (3rd gen.) |
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Definition
Ceftriaxone, Cefotaxime, Cefdinir, Cefixime Spectrum: Less gram (+) more gram (-) cocci & rods Most enter the CNS Empiric management of meningitis and sepsis |
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Term
very broad spectrum cephalosporins (4th gen.) |
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Definition
Cefepime Widest spectrum for mostly gram (-) cocci/rods Resistant to most beta-lactamases Enters the CNS |
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Term
Imipenem, Meropenem, Ertapenem |
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Definition
MOA: interact w/ cytoplasmic membrane-binding proteins to inhibit transpeptidation rxns w/in the bacterial cell wall (resistant to beta-lactamases) Spectrum: broadest we have! use for empiric tx Imipenem is given w/ cilastatin which inhibits its rapid metabolism by renal dehydropeptidase SE: GI distress, drug fever, CNS effects |
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Term
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Definition
MOA: interact w/ cytoplasmic mebrane-binding proteins to inhibit transpeptidation of bacterial cell wall synthesis (resistant to beta-lactamases) Spectrum: IV drug mainly active against gram (-) rods, doesn't kill any gram (+) |
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Term
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Definition
MOA: binds to the D-ala-D-ala muramyl pentapeptide to sterically hinder the transglycosylation rxns involved in peptidoglycan chains Spectrum: only gram +'s, Enterococci DOC: for nosocomial MRSA used as a backup drug for C. difficile Enterococcal resistance involves change in the muramyl pentapeptide target via changing the D-ala to a D-lactate Given IV and orally (not absorbed so good for colitis) SE: "red man syndrome" from histamine release, otoxicity, nephrotoxicity |
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Term
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Definition
30s Inhibits formation of initiation complex, via blocking associaiton of 50s ribosomal subunit w/ mRNA-30s, causes misreading of code, may even incorporate wrong amino acid (if so = bacteriocidal) |
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Term
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Definition
50s Inhibits the formation of the initiation complex by blocking the association of 50s ribosomal subunit w/ mRNA-30s |
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Term
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Definition
30s Block the attachment of aminoacyl tRNA to the acceptor site = tRNA specific for each AA is not allowed to enter site |
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Term
Dalfopristin/quinupristin (MOA) |
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Definition
50s block the attachment of aminoacyl tRNA to acceptor site |
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Term
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Definition
50s, bacteriostatic Inhibits the activity of peptidyltransferase (can't form peptide bond w/ elongating chain) |
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Term
Macrolides & clindamycin (MOA) |
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Definition
50s, bacteriostatic Inhibits translocation of peptidyl-tRNA from acceptor to donor site |
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Term
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Definition
gentamicin, tobramycin, amikacin, streptomycin Accumulated intracellularly via an O2-dependent uptake (so anaerobes are innately resistant), spectrum = gram (-) rods only Streptomycin: used in TB and is DOC for bubonic plague & tularemia Renal elimination so adjust dose in renal dysfunction SE: nephrotoxicity (usu reversible but enhanced by vancomycin, amphotericin B, cisplatin, and cyclosporine), ototoxicity (enhanced by loop diuretics) |
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Term
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Definition
doxycycline, minocycline, demeclocycline 30s, bacteriostatic Spectrum: "broad" including chlamydial, mycoplasmal species, H.pylori, Rickettsia, Borrelia burgdorferi, Brucella, Vibrio doxycyline: more activity overall, good for prostatitis b/c reaches high levels there minocycline: concentrates in saliva/tears demeclocycline: used in SIADH blocks ADH receptor function in collecting ducts (receptors aka V2) Elimination: kidney except doxy via liver chelators: bind divalent cations (Ca2+, Mg2+, Fe2+, Al3+) which decrease their absorption so becareful w/ antacids SE: Tooth enamel discoloration & dec. bone growth in children (DON'T use) Phototoxicity |
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Term
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Definition
50s, bacteriostatic Spectrum: wide, used as back up drug for Salmonella typhi, B. fragilis, Rickettsia Metabolized by hepatic glucuronidation so dec. dose in liver failure/neonates, also inhibits CYP450 SE: dose-dependent bone marrow supression, "gray baby syndrome" in neonates (b/c can't glucuronidate) |
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Term
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Definition
erythromycin, azithromycin, clarithromycin 50s, broad spectrum, often used in community acquired pneumonia erythromycin: gram + cocci, atypicals (chlamydia, mycloplasma), legionella, Campylobacter jejuni) liver metabolism, CYP450 inhibitor azithromycin: above + more active in respiratory infxns Mycobacterium avium Excreted by kidney, safer in pregnancy clarithromycin: greater activity against M. avium and H. pylori liver metabolism, CYP450 inhibitor SE: stimulate motilin receptor & cause GI distress, reversible deafness a high doses, erythromycin estolate causes cholestasis, jaundice |
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Term
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Definition
50s, not a macrolide Spectrum: "narrow" gram + cocci (no MRSA), anaerobes including B. fragilis, toxoplasmosis Concentrates in bone so has value in osteomyelitis 1st known drug to cause pseudomembranous colitis (caused by C. difficile) |
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Term
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Definition
50s, inhibits the formation of the initiation complex in bacterial translation systems by preventing formation of the complex Spectrum: tx of vancomycin resistant Staph & Enterococci, and drug-resistant pneumococci SE: bone marrow supression (thrombocytopenia- dec. platelets) |
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Term
Quinupristin-Dalfopristin |
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Definition
MOA: streptogramins that act in concert via several mechanisms (prevent interaction of amino-acyl-tRNA w/ acceptor site and stimulate dissociation from ternary complex & block the extrusion of a completed polypeptide) Spectrum: parenteral for VRSA & VRE, and other drug-resistant gram + cocci |
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Term
Sulfonamides, trimethoprim & pyrimethamine |
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Definition
MOA: folic acid synthesis inhibitors sulfonamides inhibit the bacterial enzyme dihydropteroate synthetase and trimethoprim & pyrimethamine inhibit the human & bacterial enzyme dihydrofolate reductase Sulfonamindes alone =limited use Sulfasalazine = prodrug in UC and RA Ag sulfadiazine = used topically in burns TMP-SMX = DOC in nocarida, mycobacteria, gram (-) infxns (E.coli, salmonella, shigella, H.flu) gram (+), fungus (pneumocystis jiroveci), protozoa (toxoplasma gondii - use sulfadiazine + pyrimethamine) Elimination: sulfonamides are hepatically acetylated, highly protein bound causes kernicterus in neonates (don't use in 3rd trimester) SE: Sulfonamides = hypersensitivity (SJS), phototoxicity, hemolysis in G6PD deficiency Trimethoprim or Pyrimethamine = bone marrow supression (anemias anti-folate) |
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Term
Drugs that have sulfonamides w/in watch for allergies |
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Definition
1. carbonic anhydrase inhibitors 2. thiazides 3. loops 4. sulfonylureas 5. celecoxib, valdecoxib |
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Term
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Definition
1. erythema multiforme 2. hemorrhagic crusts of lips and oral mucosa 3. MC in kids |
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Term
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Definition
Norfloxacin, ciprofloxacin, ofloxacin, other oxacins MOA: inhibit topoisomerase II (DNA gyrase) responsible for separation of replicated DNA during cell division (ie: inhibits DNA synthesis) Spectrum: great gram (-) coverage but not 1st line Fe2+, Ca2+ limit their absorption (chelators), eliminated via kiney SE: Phototoxicity, tendonitis/tendon rupture w/ long term use, increase the QT interval (so risk of torsades) |
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Term
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Definition
unclassified ATBX, may produce free radicals? GET BaC on the Metro Spectrum: giardia, entamoeba, trichomonas (protozoal), bacteroides, clostridium (bacterial) DOC for pseudomembranous colitis SE: metallic taste, stomatitis, cystitis, disulfram-like effect |
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Term
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Definition
"BMT" regimin = bismuth, metronidazole, and tetracycline OR Clarithromycin, amoxicillin, omeprazole |
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Term
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Definition
one of the drugs used for TB, & prophylaxis MOA: inhibits mycolic acid synthesis, but is a prodrug Resistance: comes via deletions in the katG gene that encodes the catalase needed for INH bioactivation SE: Hepatitis, peripheral neuritis, sideroblastic anemia, hemolysis in G6PD def., SLE in slow acetylators |
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Term
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Definition
used in TB tx MOA: inhibits DNA-dependent RNA polymerase (nucleic acid synthesis inhibitor) SE: hepatitis, induction of CYP450, red-orange metabolites in sweat, urine, tears |
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Term
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Definition
TB tx. regimin MOA: inhibits synthesis of arabingalactan (cell wall component) SE: dose-dependent retrobulbar neuritis --> dec. visual acuity and red-green discrimination |
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Term
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Definition
TB tx regimin MOA: unkown SE: hepatitis, polyarthralgia, myalgia, rash, hyperuricemia (GOUT!!!), phototoxicity, inc. porphyrin synthesis |
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