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43 Cards in this Set
- Front
- Back
what are the origins of antibiotics?
Give examples; |
Antibiotics are common metabolic products of aerobic bacteria and fungi
Bacteria: Streptomyces and Bacillus Molds: Penicillium and Cephalosporium |
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Drugs should be ______ ______they kill or inhibit microbial cells without damaging host tissues
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selectively toxic
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what does the spectrum of an antibiotic mean?
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Range of different bacteria affected by Ab
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describe:
broad spectrum narrow spectrum limited spectrum |
BROAD SPECTRUM: kill/inhibit wide range of gram+/-NARROW SPECTRUM: kill/inhibit mainly gram+ or gram-LIMITED SPECTRUM: effective against single species
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what are the 5 fundamental mechanism of antibiotic action?
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Inhibition of cell wall synthesis
2: Inhibition of nucleic acid structure and function 3: Inhibition of folic acid synthesis (really this is a type NA inhibition) 4: Inhibition of protein synthesis 5: Interference with cell membrane structure or function |
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What is the anagram for the 5 fundamental mechs of antibiotic actioN?
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Pro (protein synthesis)
Members (cell membrane) Follow (folic acid) New (nucleic acid) Wallets (cell wall) |
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name two antibiotic classes that react to disrupt cell wall synthesis. How?
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penicillins and cephalosporins
Block some aspect of peptidoglycan synthesis |
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what is a "r"-lactam?
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penicillins and cephalosporins - Named for their four membered ring structure
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"r"-lactams cause _____ _____ ______
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cell wall destruction
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what is the spectrum of "r"-lactams?
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Some: against gram+/-, others: against either/or
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how does vancomycin work?
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Natural product. Blocks NAM cross-linking. Effective against Gram +. Made by a class of M.O. know as Actinobacteria (make some of our most useful antibiotics)
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what drug could you use against TB? Why?
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Isoniazid
Frontline TB drug. Inhibits mycolic acid production crucial for Mycobacterial sp. cell wall construction |
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Why does Vancomycin primarily target Gram +?
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because it is such a huge molecule, Gram - outer membrane prohibit it from entering.
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what does Bacitracin do?
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Block peptidoglycan synthesis at early stages
blocksrecycling of bactoprenol |
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what are the drugs that target the cell wall?
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"r"-lactams
bacitracin isoniazid vancomycin |
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give an example of a class of drugs that target nucleic acid synthesis. Do they have a broad, narrow, or limited spectrum?
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fluoroquinolones
Broad |
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how do drugs disrupt nucleic acid synthesis
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Block synthesis of nucleotides
Inhibit replication Stop transcription Inhibit DNA synthesis |
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Give an example of a drug that disrupts nucleic acid synthesis. What would you use it for treating?
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ciprofloxacin
Penetrates Macrophages (good for intracellular parasites) Has been used to treat Anthrax |
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what nucleic acid targeting drug would you use to treat anaerobes which are resistant to many Ab's
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metronidazole - blocks passage of DNA polymerases, must be activated by flavodoxin, which is not found in eukarotic cells, onlin in anaerobes.
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what are some micro-orgs that you would use metronidazole to treat?
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helicobacter pylori
trichomatis vaginalis giardia inestinalis |
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what two classes of drugs target folic acid synthesis?
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sulfonamides and trimethoprim
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describe sulfonamides and what they're good for
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Sulfa drugs
Very first modern antimicrobial drug Synthetic Shigellosis, acute urinary tract infections, certain protozoan infections |
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describe trimethoprim and what it's good for
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Inhibits the enzymatic step immediately following the step inhibited by solfonamides in the synthesis of folic acid
Often given in combination with sulfamethoxazole One of the primary treatments for Pneumocystis (carinii) jiroveci pneumonia (PCP) in AIDS patients |
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how do drugs that inhibit protein synthesis work?
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Inhibit translation by reacting with the ribosome-mRNA complex
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what is a class of drugs that target protein synthesis?
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Aminoglycoside Drugs (Streptomycin
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what could you use streptomycin for?
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Streptomycin: Bubonic plague and tularemia and good antituberculosis agent
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How does streptomycin work?
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interferes with protein synthesis
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how do aminoglycoside drugs work?
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cause mRNA to misread, protein is incorrect
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how do tetracycline drugs work?
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bind to ribosomes and block tRNA and protein synthesis
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how do chloroamphenical drugs work?
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Blocks peptide bond formation and protein synthesis
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how does erythromycin work?
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Blocks protein synthesis by attaching to the 50s ribosome prevents it from moving down the mRNA
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Name a protein synthesis blocker that can be given in 1-2 doses.
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azithromycin (Zithromax)
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what are the protein synthesis inhibiting drugs?
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aminoglycosides, tetracycline
chloramphenicol, erythromycin clindamycin, Azithromycin, and streptogramins |
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what is an example of something that will disrupt the cell membrane function?
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surfactants such as soap
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what are some drugs that disrupt cell membrane function?
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polymyxins
triclosan |
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Describe the 5 steps of traditional antibiotic development
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Hypersensitive strain of bacterial plated on agar
Spot soil isolate on plate Allow lawn of bacteria to develop Identify zone of inhibition of growth Isolate strain producing Ab, ID Ab structurally |
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Describe combinatorial chemistry
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Start with core structure
Chemically modify core to make derivatives Test derivatives against known pathogens |
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Describe rational drug design
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Use known structure of target to design drugs
Apply combinatorial chemistry Test efficacy of new combinatorial compounds |
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For every Ab introduced, resistance has occurred in ______
The driving force in Ab discovery and development is _________ The 2002 Ab market was estimated at US$________! |
1-10 yrs
economic 25 billion |
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Microbes become newly resistant to a drug after
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Spontaneous mutations in critical chromosomal genes
Acquisition of entire new genes or sets of genes via transfer from another species (plasmids called resistance (R) factors) |
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what are some ways microbes can become resistant.
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drug inactivation-enzyme deactivates the drug
decreased permeability-microbe receptor to the drug is changed Activation of drug pumps-pumps drug out of cell Change in drug binding site Use of alternate metabolic pathway. |
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