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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

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

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

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?

Isoniazid
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
blocksrecycling of bactoprenol

what are the drugs that target the cell wall?

"r"-lactams

bacitracin
isoniazid
vancomycin

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

fluoroquinolones

Broad

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?

ciprofloxacin

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
Synthetic
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?

polymyxins
triclosan

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

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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
economic
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.

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