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43 Cards in this Set

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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
Drugs should be ______ ______they kill or inhibit microbial cells without damaging host tissues
selectively toxic
what does the spectrum of an antibiotic mean?
Range of different bacteria affected by Ab
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
what are the 5 fundamental mechanism of antibiotic action?
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
What is the anagram for the 5 fundamental mechs of antibiotic actioN?
Pro (protein synthesis)
Members (cell membrane)
Follow (folic acid)
New (nucleic acid)
Wallets (cell wall)
name two antibiotic classes that react to disrupt cell wall synthesis. How?
penicillins and cephalosporins

Block some aspect of peptidoglycan synthesis
what is a "r"-lactam?
penicillins and cephalosporins - Named for their four membered ring structure
"r"-lactams cause _____ _____ ______
cell wall destruction
what is the spectrum of "r"-lactams?
Some: against gram+/-, others: against either/or
how does vancomycin work?
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)
what drug could you use against TB? Why?
Frontline TB drug. Inhibits mycolic acid production crucial for Mycobacterial sp. cell wall construction
Why does Vancomycin primarily target Gram +?
because it is such a huge molecule, Gram - outer membrane prohibit it from entering.
what does Bacitracin do?
Block peptidoglycan synthesis at early stages
blocks recycling of bactoprenol
what are the drugs that target the cell wall?

give an example of a class of drugs that target nucleic acid synthesis. Do they have a broad, narrow, or limited spectrum?

how do drugs disrupt nucleic acid synthesis
Block synthesis of nucleotides
Inhibit replication
Stop transcription
Inhibit DNA synthesis
Give an example of a drug that disrupts nucleic acid synthesis. What would you use it for treating?

Penetrates Macrophages (good for intracellular parasites)
Has been used to treat Anthrax
what nucleic acid targeting drug would you use to treat anaerobes which are resistant to many Ab's
metronidazole - blocks passage of DNA polymerases, must be activated by flavodoxin, which is not found in eukarotic cells, onlin in anaerobes.
what are some micro-orgs that you would use metronidazole to treat?
helicobacter pylori
trichomatis vaginalis
giardia inestinalis
what two classes of drugs target folic acid synthesis?
sulfonamides and trimethoprim
describe sulfonamides and what they're good for
Sulfa drugs
Very first modern antimicrobial drug
Shigellosis, acute urinary tract infections, certain protozoan infections
describe trimethoprim and what it's good for
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
how do drugs that inhibit protein synthesis work?
Inhibit translation by reacting with the ribosome-mRNA complex
what is a class of drugs that target protein synthesis?
Aminoglycoside Drugs (Streptomycin
what could you use streptomycin for?
Streptomycin: Bubonic plague and tularemia and good antituberculosis agent
How does streptomycin work?
interferes with protein synthesis
how do aminoglycoside drugs work?
cause mRNA to misread, protein is incorrect
how do tetracycline drugs work?
bind to ribosomes and block tRNA and protein synthesis
how do chloroamphenical drugs work?
Blocks peptide bond formation and protein synthesis
how does erythromycin work?
Blocks protein synthesis by attaching to the 50s ribosome prevents it from moving down the mRNA
Name a protein synthesis blocker that can be given in 1-2 doses.
azithromycin (Zithromax)
what are the protein synthesis inhibiting drugs?
aminoglycosides, tetracycline
chloramphenicol, erythromycin
clindamycin, Azithromycin, and streptogramins
what is an example of something that will disrupt the cell membrane function?
surfactants such as soap
what are some drugs that disrupt cell membrane function?
Describe the 5 steps of traditional antibiotic development
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
Describe combinatorial chemistry
Start with core structure
Chemically modify core to make derivatives
Test derivatives against known pathogens
Describe rational drug design
Use known structure of target to design drugs
Apply combinatorial chemistry
Test efficacy of new combinatorial compounds
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
25 billion
Microbes become newly resistant to a drug after
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)
what are some ways microbes can become resistant.
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.