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Assessment 03
Micro - Antibiotics
55
Microbiology
Professional
05/11/2010

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Term
Sulfonamide
Definition
Blocks Dihydropteroate Synthase to Inhibit Folic Acid Synthesis;
G+/-, not anaerobes;
IV/oral
Term
Trimethoprim
Definition
Blocks Dihydrofolate Reductase to Inhibit Folic Acid Synthesis;
G+/-, not anaerobes;
IV/oral
Term
Pencillin G
Definition
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
Term
Pencillin V
Definition
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
Term
Ampicillin
Definition
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
Term
Amoxicillin
Definition
Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
G+ and G- enteric bacilli (E.coli);
Oral
Term
Carbenicillin
Definition
Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
1st B-lactam effective against P. aeruginosa;
IV
Term
Ticarcillin
Definition
Broad spectrum B-lactam;
Binds to and inactivate PBP's to Block Peptidoglycan/Cell Wall Synthesis;
effective against P. aeruginosa;
IV
Term
Pipercillin
Definition
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
Term
Methicillin
Definition
narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant (MRSA);
IV
Term
Oxacillin
Definition
narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
IV/oral
Term
Nafcillin
Definition
narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
IV/oral
Term
Cloxacillin
Definition
narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
Oral
Term
Dicloxacillin
Definition
narrow spectrum B-lactam;
Anti-Staphylococcal, not E.coli (lower activity than Pen G, but resistant to penicillinase;
Resistant;
Oral
Term
Cephalosporins
general
Definition
Cephalosporins differ from penicillins in having greater acid stability; being penicillinase resistant; and being antigenically dissimilar (5-15% cross reactivity in penicillin-allergic patients)
Term
Cephalexin
Definition
1st gen. cephalosporin;
G+, G- enterics, not P. aeruginosa; Sensitive to cephalosporinases;
IV/Oral
Term
Cefazolin
Definition
1st gen. cephalosporin;
G+, G- enterics, not P. aeruginosa; Sensitive to cephalosporinases;
IV/Oral
Term
Cefoxitin
Definition
2nd gen cephalosporin;
Improved anaerobic activity; resistant to cephalosporinases, but sensitive to ESBL's
IV/Oral
Term
Cefotetan
Definition
2nd gen cephalosporin;
Improved anaerobic activity; resistant to cephalosporinases, but sensitive to ESBL's
IV/Oral
Term
Ceftriaxone
Definition
3rd gen cephalosporin;
Improved G- activity;
resistant to cephalosporinases, but sensitive to ESBL's;
IV/Oral
Term
Cefepime
Definition
4th gen cephalosporin;
Anti-Psuedomonal and preserved activity for Streptococci;
Resistant to both cephalosporinases and ESBL's; IV/Oral
Term
Aztreonam
Definition
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
Term
Imipenem-cilastatin
Definition
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
Term
Meropenem
Definition
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
Term
Ertapenem
Definition
carbapenem;
same activity as penecillins/cephalosporins etc.;
Low Pseudomonas and Acinetobacter activity;
Sensitive to carbanpenemases; also bacteria can alter porin channels decreasing permeability;
IV
Term
Vancomycin
Definition
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
Term
Bacitracin
Definition
Blocks phosphatase to inhibit carrier lipid in peptidoglycan synthesis; Topical therapy for G+
Term
Polymyxins;
{Polymyxin B, Polymyxin E (Colistin)}
Definition
Cationic detergent-damaging cell membrane;
Topical therapy for G- rods
Term
Daptomycin
Definition
bactericidal;
Irreversibily binds cell membrane; depolarizes and causes cell death; Aerobic G+ (note that binding to pulmonary surfactant causes inactivation)
Term
Cycloserine
Definition
Disrupts proper pentapeptide formation in peptidoglycan precursors;
Anti-Tuberculosis
Term
Streptomycin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
Term
Kanamycin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
Term
Neomycin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Broad spectrum, not anaerobes, not intracellular bacteria;
IV
Term
Gentamycin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
Term
Tobramycin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
Term
Amikacin
Definition
Specific binding to a 30S ribosomal protein , distorts the acceptor site and causes misreading;
Extended spectrum, including activity against Pseudomonas;
IV
Term
Spectinomycin
Definition
Binds to 30S subunit to inhibit protein syn.;
Neisseria gonorrhoeae;
neither-IM
Term
Tetracycline
Definition
Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
Term
Minocycline
Definition
Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
Term
Doxycycline
Definition
Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding;
broad spectrum, mycoplasma, rickettsia, chlamydia;
IV/oral
Term
Tigecycline
Definition
a glycylcycline; Blocks acceptor-site on 30S subunit to inhibit aminoacyl-tRNA binding; broad spectrum, tetracycline resistant strains; IV/oral
Term
Erythromycin
Definition
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
Term
Azithromycin
Definition
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
Term
Clairithromycin
Definition
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
Term
Telithromycin
Definition
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
Term
Clindamycin
Definition
Binds to 50S to inhibit peptidyl transfer;
similar to erythromycin plus highly effective against anaerobes in general;
IV/oral
Term
Chloramphenicol
Definition

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.

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