Term
resistant strains that spread rapidly
MRSA, VRE, FQRP and what percentage of resistance renders antibiotic essentially unusable for the common pathogen? |
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Definition
Methicilin Resistant Staphylococcus aureus
Vancomycin resistant enterococci
Fluoroquinolone resistant pseudomonas
30-40% level |
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Term
| Only ____ structurally new antibiotics have been approved since 1962. |
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Definition
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Term
| Reasons for little research and development of antibiotics |
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Definition
1. high cost of development
2. antibiotics have a low return rate
3. lack of guidance documents from the FDA |
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Term
| From 1962-2000 ______major classes of antibiotics were introduced |
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Definition
no major classes introduced
=> gap in novel antibiotic discovery for over 20 yrs.
most antibiotics are produced by bacteria or fungi originally (approximately 70% of antibacterials are natural products or have a natural product pharmacophore) |
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Term
| Mutilins developed from .... |
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Definition
| Fungi, originally developed in 50s but are re-emerging as potential treatment |
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Term
| Dificid treats? (fidaxomicin Difficid) |
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Definition
| Closridium difficile. approved april 2011. product of filamentous bacteria, pharm companies used natural product to derive |
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Term
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Definition
| molecules that stop microbes both bacteria and fungi from growing or kill them outright. |
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Term
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Definition
| antibiotics that stop bacteria from growing |
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Term
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Definition
| antibiotics that cause bacterial cell death |
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Term
| Classification of antibiotics is based on (3) |
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Definition
1. the class and spectrum of microorganism it kills
2. the biochemical pathway it interferes with
3. the chemical structure of the pharmacophore |
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Term
| Sulfonamides (synthetic) target what path? example? |
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Definition
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Term
|
Definition
|
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Term
|
Definition
Protein Synthesis
Tetracycline |
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Term
|
Definition
protein synthesis
chloramphicol |
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Term
|
Definition
|
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Term
|
Definition
DNA Replication
Ciprofloxacin |
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Term
|
Definition
Protein synthesis
Pristinamycin 1A |
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Term
|
Definition
|
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Term
| Rifampin is used in treatment of? |
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Definition
|
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Term
| Oxazolidinones (synthetic) |
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Definition
|
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Term
|
Definition
Bacterial Membrane
Daptomycin |
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Term
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Definition
|
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Term
| What is the approach used to create successive generations of antibiotic classes? |
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Definition
| Successive rounds of medchem using synthetic tailoring. you take a natural product and modify the structure to try to overcome the resistance by adding modifying side chain structure (penicillins) or functional groups so that enzymes can Chew that up and not the pharmacophore |
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Term
Validated Targets in bacteria for antibiotics and their resistance mechanism
CELL WALL
1. Beta Lactams
2. Vancomycin
3. Teicoplanin |
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Definition
1. transpeptidase/
2. Transglycosylases (PBPS)
3. D-Ala-DAla termini of peptidoglycan and of lipid II
1. Beta lactamases
2. PBP Mutants
3. Reprogramming of D-Ala-D-Ala to Dala-D-Lac or D-alaD-Ser |
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Term
PROTEIN SYNTHESIS (target and Resistance Mechanism)
1. erythromycins
2. Tetracyclines
3. Aminoglycosides
4. oxazolidinones |
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Definition
1. Peptidyle transferase/ribosome
2-4 Peptidyl transferase
1. rRNA methylation/Efflux
2. Drug efflux
3. Drug modification
4. Ribosome mutations |
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Term
DNA REPLICATION/REPAIR (target and R Mech)
1. Fluoroquinolones |
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Definition
DNA Gyrase
Gyrase Mutations |
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Term
RNA SYNTHESIS (target and R mech)
Rifampin |
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Definition
RNA Polymerase
Polymerase Mutations |
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Term
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Definition
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