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Pathology 5050 Antibiotics
Mulvey's antibiotics sections - Chapter 15/16
44
Pathology
Graduate
02/23/2012

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Term
Disinfectant
Definition
Applied to nonliving objects/surfaces
Term
Antiseptic
Definition
Applied to living tissue/skin
Term
Antibiotic
Definition
Administered inside or outside body
Term
bactericidal
Definition
Kills bacteria
Term
bacteriostatic
Definition
Slows/stops growth of bacteria
Term
Beta lactams - mechanism
Definition
Inhibits transpeptidation step in peptidoglycan synthesis; binds penecillin-binding proteins; stimulates autolysins
Term
Glycopeptides - mechanism
Definition
Inhibits transglycosylation and transpeptidation steps in peptidoglycan sysnthesis by binding D-Ala-D-ala
Term
Aminoglycosides - mechanism
Definition
Binds 16s rRNA in 30S subunit of bacterial ribosome - stops 50S subunit from joining to activate the ribosome
Term
Tetracyclines - mechanism
Definition
Binds 16s rRNA in 30S subunit of bacterial ribosome; disrupts bacterial membrane - distorts A site so tRNA cannot match mRNA codon
Term
Macrolides/lincosamides - mechanism
Definition
Bind 23S rRNA in 50S subunit of bacterial ribosome - blocks the nascent peptides exit tunnel
Term
Streptogramins - mechanism
Definition
Binds 23S rRNA in 50S subunit of bacterial ribosome
Term
Fluoroquinolones - mechanism
Definition
Bind DNA gyrase to inhibit DNA replication
Term
Rifampin - mechanism
Definition
Binds beta subunit of RNA polymerase to block the exit tunnel for nascent RNA, thereby inhibiting transcription
Term
Trimethoprim/sulfonamides - mechanism
Definition
Inhibits enzymes responsible for THF production
Term
Metronidazole - mechanism
Definition
Nicks bacterial DNA and interferes with DNA replication when activated by bacterial flavodoxin protein
Term
Oxazolidinones - mechanism
Definition
Binds 50S ribosomal subunit in the peptidyltransferase site, blocking the first peptide bond from forming in translation.
Term
mupirocin - mechanism
Definition
Inhibits bacterial isoleucine aminoacyl-tRNA synthetase, thereby blocking translation
Term
Beta-lactams - common drug names
Definition
Penicillin, ampicillin, Cefobid, Augmentin
Term
Glycopeptides - common drug names
Definition
Vancomycin, teichoplanin, daptomycin
Term
Aminoglycosides - common drug names
Definition
Kanamycin, gentamycin, streptomycin
Term
Tetracyclines - common drug names
Definition
Tetracycline, doxycycline
Term
Macrolides/lincosamides - common drug names
Definition
Erythromycin (macrolide), lincomycin, clindamycin (lincosamides)
Term
Streptogramins - common drug names
Definition
Synercid
Term
Fluoroquinolones - common drug names
Definition
Ciproflaxcin, norfloxacin
Term
Tripmethoprim/sulfonamides - common drug names
Definition
Bactrim, Septra
Term
Metronidazole - common drug names
Definition
Flagyl
Term
Oxazolidinones - common drug names
Definition
Zyvox
Term
What are the four main categories for bacterial resistance mechanisms?
Definition
1) Restricted access of antibiotic to its target 2) Enzymatic inactivation of the antibiotic 3) Modification/protection of the antibiotic target 4) Failure to activate antibiotic
Term
Beta-lactams - resistance mechanisms
Definition
Gram-negative outer membrane, porin mutations, beta lactamase, modify penicillin-binding protein
Term
Glycopeptides - resistance mechanisms
Definition
Gram-negative outer membrane, substitute D-ala-D-lactate for D-ala-D-ala
Term
aminoglycosides - resistance mechanisms
Definition
Aminoglycoside-modifying enzymes that inactivate by adding chemical groups to the antibiotic
Term
Tetracyclines - resistance mechanisms
Definition
Ribosome protection, Tet efflux pump system
Term
Macrolides/lincosamides - resistance mechanism
Definition
Methylation of 23S rRNA on A2058 by RNA methylases (Erm), efflux pumps
Term
Streptogramins - resistance mechanisms
Definition
Methylation of 23S rRNA on A2058 by RNA methylases (Erm), inactivation of antibiotic via acetyltransferases, which weakens antibiotic binding to the 23S rRNA
Term
Fluoroquinolones - resistance mechanisms
Definition
Efflux, reduced uptake, mutation in DNA gyrase (target)
Term
Rifampin - resistance mechanisms
Definition
Mutation in RNA polymerase (target)
Term
Trimethoprim/sulfonamides - resistance mechanisms
Definition
Mutations in folate pathway biosynthetic enzymes so they no longer bind antibiotic
Term
Metronidazole - resistance mechanisms
Definition
Decreased production of flavodoxin gene
Term
Oxazolidinones - resistance mechanisms
Definition
Mutation in 23S rRNA genes
Term
Explain regulation of antibiotic resistance using the Tet pump.
Definition
With no tetracycline, TetR (repressor) binds operator to block transcription of tetB efflux pump. With tetracycline, tetR binds tetracycline drug causing release from the tetB operator, allowing tetB efflux pump to be expressed.
Term
Explain regulation of antibiotic resistance using the beta-lactamase BlaZ.
Definition
With no beta-lactam, BlaI inhibits transcription of blaZ (beta lactamase). With beta lactam, the antibiotic binds BlaR1, which releases BlaR2. BlaR2 can then cleave BlaI, and the blaZ beta lactamase is transcribed.
Term
Explain regulation of antibiotic resistance using the erm RNA methylase.
Definition
With no macrolide, ribosomes translate leader peptide and mRNA forms 2 stem loops so erm AUG is inaccessible. With macrolide, the ribosome stalls, leader peptide is not translated, and the RNA forms only one stem-loop. The erm gene start site is exposed allowing erm RNA methylase to be translated.
Term
Explain regulation of antibiotic resistance using the VanS histidine kinase.
Definition
Vancomycin-caused cell wall damage is sensed by VanS when fragments bind VanS. VanS then phosphorylates VanR to activate it; VanR binds and activates promoters of vanRS and vanHAX operons.
Term
Explain regulation of antibiotic resistance using the ampC beta-lactamase.
Definition
Peptidoglycan fragments are transported into the cytoplasm by AmpG and AmpD removes a sugar group from the fragment. This fragment can then bind AmpR, which activated binds and activates transcription of ampC. AmpC is then exported to periplasm to degrade beta lactams.
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