Assessment 03 – Flashcards

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Sulfonamide
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Blocks Dihydropteroate Synthase to Inhibit Folic Acid Synthesis;
G+/-, not anaerobes;
IV/oral
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Trimethoprim
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Blocks Dihydrofolate Reductase to Inhibit Folic Acid Synthesis;
G+/-, not anaerobes;
IV/oral
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Pencillin G
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narrow spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
Highest activity against G+ bacteria and G- cocci, not G- enterics;
Sensitive to penicillinase (aka B-lactamase) breaks B-lactam ring IV
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Pencillin V
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narrow spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
Highest activity against G+ bacteria and G- cocci, not G- enterics;
Sensitive to penicillinase (aka B-lactamase) breaks B-lactam ring;
ORAL
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Ampicillin
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Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
G+ and G- enteric bacilli (E.coli);
IV/Oral
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Amoxicillin
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Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
G+ and G- enteric bacilli (E.coli);
Oral
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Carbenicillin
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Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
1st B-lactam effective against P. aeruginosa;
IV
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Ticarcillin
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Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
effective against P. aeruginosa;
IV
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Pipercillin
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extended spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
Most active penicillin against G- enterics, P. aeruginosa, and G- anaerobes (less active against G+ cocci;
IV
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Methicillin
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narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant (MRSA);
IV
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Oxacillin
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narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
IV/oral
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Nafcillin
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narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
IV/oral
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Cloxacillin
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narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
Oral
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Dicloxacillin
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narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
Oral
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Cephalosporins
general
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Cephalosporins differ from penicillins in having greater acid stability; being penicillinase resistant; and being antigenically dissimilar (5-15% cross reactivity in penicillin-allergic patients)
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Cephalexin
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1st gen. cephalosporin;
G+, G- enterics, not P. aeruginosa; Sensitive to cephalosporinases;
IV/Oral
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Cefazolin
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1st gen. cephalosporin;
G+, G- enterics, not P. aeruginosa; Sensitive to cephalosporinases;
IV/Oral
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Cefoxitin
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2nd gen cephalosporin;
Improved anaerobic activity; resistant to cephalosporinases, but sensitive to ESBL's
IV/Oral
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Cefotetan
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2nd gen cephalosporin;
Improved anaerobic activity; resistant to cephalosporinases, but sensitive to ESBL's
IV/Oral
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Ceftriaxone
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3rd gen cephalosporin;
Improved G- activity;
resistant to cephalosporinases, but sensitive to ESBL's;
IV/Oral
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Cefepime
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4th gen cephalosporin;
Anti-Psuedomonal and preserved activity for Streptococci;
Resistant to both cephalosporinases and ESBL's; IV/Oral
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Aztreonam
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monobactam;
same activity as penecillins/cephalosporins;
G- activity equal to 3rd gen. cephs; no anaerobic or G+ activity
****can be used in pen-allergic patients.;
IV
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Imipenem-cilastatin
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carbapenem;
same activity as penecillins/cephalosporins etc.;
Very broad Spectrum;
G+/-, Anti-Psuedomonal, anaerobes, Strep. Pneumo;
Sensitive to carbanpenemases; also bacteria can alter porin channels decreasing permeability;
IV
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Meropenem
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carbapenem;
same activity as penecillins/cephalosporins etc.;
Very broad Spectrum;
G+/-, Anti-Psuedomonal, anaerobes, Strep. Pneumo;
Sensitive to carbanpenemases; also bacteria can alter porin channels decreasing permeability;
IV
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Ertapenem
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carbapenem;
same activity as penecillins/cephalosporins etc.;
Low Pseudomonas and Acinetobacter activity;
Sensitive to carbanpenemases; also bacteria can alter porin channels decreasing permeability;
IV
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Vancomycin
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Binds to peptidoglycan precursors to inhibit transfer of precursors to growing cell wall;
Activity restricted to G+, drug of choice for MRSA;
Resistance already occurs in Enterococcus species (source of resistance for the 1st VRSA);
IV/Oral
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Bacitracin
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Blocks phosphatase to inhibit carrier lipid in peptidoglycan synthesis; Topical therapy for G+
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Polymyxins;
{Polymyxin B, Polymyxin E (Colistin)}
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Cationic detergent-damaging cell membrane;
Topical therapy for G- rods
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Daptomycin
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bactericidal;
Irreversibily binds cell membrane; depolarizes and causes cell death; Aerobic G+ (note that binding to pulmonary surfactant causes inactivation)
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Cycloserine
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Disrupts proper pentapeptide formation in peptidoglycan precursors;
Anti-Tuberculosis
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Streptomycin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
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Kanamycin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
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Neomycin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
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Gentamycin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
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Tobramycin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
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Amikacin
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Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
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Spectinomycin
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Binds to 30S subunit to inhibit protein syn.;
Neisseria gonorrhoeae;
neither-IM
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Tetracycline
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Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
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Minocycline
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Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
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Doxycycline
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Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
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Tigecycline
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a glycylcycline; Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding; broad spectrum, tetracycline resistant strains; IV/oral
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Erythromycin
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Bind to 50S subunit to cause dissociation of tRNA and termination of peptide linking;
similar to Pen G, but includes mycoplasma and chlamydia; IV/oral
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Azithromycin
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Bind to 50S subunit to cause dissociation of tRNA and termination of peptide linking;
similar to Pen G, but includes mycoplasma and chlamydia;
IV/oral
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Clairithromycin
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Bind to 50S subunit to cause dissociation of tRNA and termination of peptide linking;
similar to Pen G, but includes mycoplasma and chlamydia;
IV/oral
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Telithromycin
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a ketolide;
Bind to 50S subunit to cause dissociation of tRNA and termination of peptide linking;
Resp. tract pathogens (common and atypical), Strep. pneumo., effective against B-lactam and macrolide-resistant strains;
Unable to induce MLSB resistance;
IV/oral
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Clindamycin
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Binds to 50S to inhibit peptidyl transfer;
similar to erythromycin plus highly effective against anaerobes in general;
IV/oral
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Chloramphenicol
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Binds to 50S to inhibit peptidyl transfer + affects human mitochondria; broad spectrum; IV/oral

;

SI: Causes bone marrow depression due to effects on human mitochondria.

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Retapamulin
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inhibition of proteins synthesis by binding to 50S ribosome
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Quinupristin & Dalfopristin
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Blocks channel in ribosome where nascent peptides exit;
G+, VRSA, VR enterococci, MRSA
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Linezolid
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Blocks interaction of 50S with fMet-tRNA;
G+, MRSA, VSRA, VRE, Strep. pneumo.
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Mupirocin
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Topical antibiotic that inhibits bacterial RNA and protein synthesis
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Imidazoles (Ketoconazole,miconazole, otrimazole)
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Blocks CytP-450 dependent metabolism of a precursor of ergosterol- inc. opsonization;
Less specific and have higher side effects
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Triazoles (Fluconazole, Itraconazole)
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Blocks CytP-450 dependent metabolism of a precursor of ergosterol- inc. opsonization;
important in patients w/ recurrent fungal infections, broader spectrum, fewer side effects; less active @ human P450
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Echinocandins (Caspofungin)
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Inhibits synthesis of 1,3-beta-D-glucan which is essential for fungal cell wall Candida, aspergillus
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Polyene Antibiotics (Amphotericin B, Nystatin)
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Bind to sterols (esp. ergosterol) in cell membrane-damaging it Thrush (oral candidiasis)
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