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46 Cards in this Set
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Penicillin G
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1st B-lactam abx, 1st gen (narrow spectrum); acid labile, penicillinase-sensitive
activity: G+, G- cocci |
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Penicillin V
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B-lactam, 1st gen (narrow spectrum); acid STABLE (1st oral), penicillinase-sensitive
Activity: G+, G- cocci |
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Ampicillin
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B-lactam, 2nd gen (broader spectrum); acid stable, penicillinase-sensitive
Activity: G+, G- enteric bacilli |
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Amoxicillin
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B-lactam, 2nd gen (broader spectrum); acid stable, 2x more serum levels, penicillinase-sensitive
Activity: G+, G- enteric bacilli |
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Carbenicillin
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B-lactam, 2nd gen (broader spectum); 1st B-lactam active against Pseudomonas aeruginosa
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Ticarcillin
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B-lactam, 2nd gen (broader spectrum); like carbenicillin, active against Pseudomonas aeruginosa, but 2x as active
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Methicillin
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B-lactam, 3rd gen (narrow-spec/pen-ase resistant); acid labile, 1st antistaph penicillin, no longer used (Staph aureus is B-lactamase +)
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Oxacillin, cloxacillin, dicloxacillin, nafcillin
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B-lactam, 3rd gen (narrow-spec/pen-ase resistant);
like Methicillin |
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Piperacillin
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B-lactam, 4th gen (extended-spec/anti-pseudomonas penicillin); active against a wide variety of G- bacilli, incl. pseudomonas aeruginosa, less active against G+ cocci
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B-lactam antibiotics
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D-ala:D-ala analogue, bind to PBP, inhibits the transpeptidase activity, preventing cross-linking, and thereby preventing cell wall maintenance
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Cephalosporins
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Similar in activity to B-lactams (prevent cell wall maintenance via inhibition of transpeptidase activity); more acid stable, penicillinase resistant, cephalosporinase-sensitive; 5-15% cross-reactivity w/ penicillin
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cefazolin, cephalexin
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1st gen cephalosporins (resistant to S. aureus B-lactamase, but sensitive to normal cephalosporinases); most active against G+, active vs some G-, not pseudomonas aeruginosa
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cefoxition, cefotetan
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2nd gen cephalosporin; improved resistance to normal cephalosporinases, still resistant to B-lactamase; more effective against Bacteroides, anaerobes, G- enterics, but still not towards Pseudomonas aeruginosa
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ceftriaxone, ceftazidime, cefoperazone, cefotaxime
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3rd gen cephalosporin; improved B-lactamase resistance, broader G- spectrum, effective against P. aeruginosa
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Cefepime (maxipime)
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4th gen cephalosporin, active against those G- resistant to ceftriaxone & cefotaxime, also active against Enterobacter & Citrobacter resistant to ceftazidime; superior to ceftazidime in coverage of G+
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Aztreonam
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Monobactam (activity similar to B-lactam abx); activity limited to aerobic G- bacilli, resistant to most B-lactamases, minimal cross-reactivity w/ other B-lactams
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Imipenem (& meropenem & ertapenem)
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Carbapenem - resistant to B-lactamases (and have similar action mechanism to other B-lactamases), perhaps the broadest antimicrobial spectrum of any abx
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Clavulanic acid
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anti-B-lactamase drug, not an abx! Taken with other abx (amoxicillin + clavulinate = augmentin)
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augmentin
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amoxicillin _ clavulinate
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Unasyn
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ampicillin + sulbactam
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Zosyn
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piperacillin + tazobactam
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Vancomycin (also, teichoplanin)
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glycoprotein, activity restricted to G+ organisms; prevents transfer of the lipid-attached peptidoglycan precursors to the growing cell wall. The drug of choice for MRSA
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Bacitracin
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prevents transfer of peptidoglycan precursor across cell membrane by inhibiting the phosphatase that "resets" the carrier phospholipid. TOXIC, restricted to topical use
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Cycloserine
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2nd-line anti-TB medicine. a D-ala analogue, that inhibits the L-ala --> D-ala step and D-ala + D-ala -> D-ala-D-ala step in peptidoglycan synthesis
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Polymyxin B
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+ly charged polypeptides, damaging against G- rods; damaging against cell membrane (topical only, due to TOXIC organ effects)
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Neomycin, gentamycin, amikacin,
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aminoglycoside abx (which all work against the 30S subunit of bacterial ribosomes)-not effective against intracellular bacteria or anaerobes - VIII nerve damage, kidney damage
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tetracycline, doxacycline, minocycline
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Tetracyclines (active against 30S subunit by blocking aminoacyl-tRNA binding), bind to growing bones & teeth (discoloration of teeth), so don't give before 8 yrs of age
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erythromycin
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macrolide abx (active against 50S subunit of bacterial ribosome, dislodges amino-acyl-tRNA, terminates peptides) - spectrum similar to Pen G (G+, G-cocci), as well as mycoplasma & chlamydia
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azithromycin & clarithromycin
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macrolide (inhibits 50S subunit by dislodging aminoacyl-tRNA, terminates polypeptides), longer half life (70 hours)
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telithromycin (Ketek)
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ketolide abx (related to macrolide, but more active & works against macrolide-resistant species) - inhibits 50S subunit same as macrolides; active against most respiratory tract pathogens
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clindamycin
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spectrum of activity like macrolides, plus activity against anaerobes in general; bacteriostatic (prevents peptide transfer) - causes pseudomembranous colitis, from overgrowth of clostridium difficile
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chloramphenicol
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broad spectrum, bacteriostatic, mainly inhibits peptidyl transfer; can penetrate human mitochondria, causing bone-marrow depression, aplastic anemia!!!
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quinupristin/dalfopristin (aka, Synercid)
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synergistic combination of two streptogramin agents; blocks ribosome channel through which new proteins are extruded. Wide-spread G+ activity, active against MRSA, possibly against VRSA
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Linezolid (Zyvox)
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novel class of agents (oxazolidones)-highly active against G+ organisms (bacteriostatic); another VRSA agent candidate, but better tolerated than Synercid; blocks interaction of 50S subunit with fMet-tRNA
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Rifampin
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blocks initiation of transcription by RNA polymerase (thereby inhibiting RNA synthesis) - broad-spectrum bacteriocidal, but resistance quickly develops - a 1st line abx against TB, along w/ other abx
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ciprofloxacin, norfloxacin
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fluroquinolone - broad spectrum, bacteriocidal, inhibits DNA gyrase (thereby preventing DNA replication & synthesis) & topoisomerase IV; resistance rapidly develops due to point mutation in DNA gyrase A
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Metronidazole
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once activated (its a pro-drug), it binds to and breaks up DNA; useful against protozoa, broad spectrum of anaerobic & microaerophilic bacteria (bactericidal)
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nitrofurantoin
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Nitrofuran drug - binds covalently to proteins - active against G+ & G-, protozoa & fungi - mainly bacteriostatic - a pro-drug, restricted to UTIs
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Mupirocin
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binds reversibly & specifically to leucyl-tRNA synthetase; used topically to tx S. aureus in nares, and impetigo in children
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list the anti-mycobacterium agents
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isoniazid
pyrazinamide ethionamide ethambutol cycloserine all 5 work to inhibit the mycobacterium's cell wall from forming |
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amphotericin B & nystatin
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polyene antibiotics - are important ANTIFUNGALS, not effective against bacteria - used topically, they bind ergosterols (found in fungal & plant membranes only), damaging the cell membrane
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Ketoconazole
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systemic antifungal agent (member of the "azole" derivatives) - blocks CYP-dependent demethylation of lanosterol (precursor to ergosterol), disturbing the fungal cell membrane properties; inhibits hyphae synthesis, enabling easy phagocytosis by PMNs and macrophages - the Azoles have higher affinity for fungal CYP than human CYP
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Fluconazole & Itraconazole
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triazoles, similar action to azoles (CYP inhibition), but less specific for fungal CYP, therefore more side effects
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Voriconazole
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azole agent, higher activity against aspergillus
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Caspofungin
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echinocandin (a new class of antifungal), inhibits synthesis of 1-3-beta-D-glucan, used in fungal cell wall - fungicidal for candida & active against aspergillus
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Griseofulvin
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FUNGISTATIC against dermatophytes; oral route, delivered to skin bound to keratin; inhibits microtubule formation, blocking mitosis & cell wall synthesis
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