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58 Cards in this Set

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First microbiologist to search for what we now know as antibiotics? What was he searching for?

Paul Ehrlich


Searched for a "magic bullet", or selective toxicity

Selective toxicity

A characteristic that causes the death of microbes while leaving host tissue unharmed

What term did Paul Ehrlich coin?

Chemotherapy

Chemotherapy

Using chemicals to treat a disease

Who invented penicillin?

Alexander Fleming

How was Penicillin invented?

A plate of Staphylococcus aureus was left out and grew mold, specifically the genus Penicillium. It was found that this mold inhibited the growth of the bacteria

Antibiotics

Substances produced by microorganisms that inhibit the growth of other microorganisms

Sulfa Drugs

Developed by three Germans during WWII to combat Streptococcal infections


Technically not an antibiotic because it was derived from a chemical, not microbe

What is the source of more than half of antibiotics?

Streptomyces

What are some other sources of antibiotics?

- Bacillus subtilis produces Bacitracin


- Molds such as Penicillium and Cephalosporium

Spectrum classifications of antimicrobial activity

1. Narrow spectrum


2. Broad spectrum

2

Narrow spectrum

Antibiotics only affect a few organisms

Broad spectrum

Large range of organisms is affected


Overused


Damage normal flora

Example of broad spectrum activity

Some drugs that combat both gram + and gram- bacteria

What are some limitations in antimicrobial activity against organisms other than bacteria? What is the significance?

- protozoans, fungi, and helminths are more closely related to humans


- viruses aren't cellular and only reproduce inside cells using our cellular machinery


- antibiotics tend to be more effective against bacteria

What is the purpose of bacteriostatic agents against infection?

The inhibited growth allows the immune system to catch up and destroy the organisms

How does penicillin act against microbes?

Inhibits cell wall synthesis by blocking peptidoglycan synthesis


This leads to cell lysis

Drugs that inhibit cell wall synthesis

1. Natural penicillins


2. Semisynthetic Penicillins


3. Cephalosporins


4. Polypeptide antibiotics

4

Semisynthetic penicillins

Amoxicillin


Ampicillin


Carbapenems


Monobactams

4

Cephalosporins

Resemble Penicillin, but beta-lactam ring is slightly different

Polypeptide antibiotics

Bacitracin


Vancomycin

Bacitracin

Topical antibiotic derived from B. subtilis

Vancomycin

Used to combat MRSA

How have certain bacteria built a resistance to penicillins and cephalosporins?

They have developed the ability to cut up beta-lactam rings, making these classes ineffective

Ways that drugs target microbes

1. Inhibition of cell wall synthesis


2. Inhibition of protein synthesis


3. Injury to the plasma membrane


4. Inhibition of nucleic acid synthesis


5. Inhibition of the synthesis of essential metabolites

5

Drugs that act as inhibitors of protein synthesis

1. Aminoglycosides


2. Tetracyclines


3. Macrolides

How do drugs inhibit protein synthesis?

Bacterial ribosome differs from what is found in eukaryotic ribosomes, so drugs can be made to target them and prevent protein synthesis

Macrolides

Erythromycin


Azithromycin

Aminoglycosides

Streptomycin


Gentamicin

2

How do antibiotics injure plasma membranes?

By binding to the cell membrane and changing its permeability, leading to lysis

How do some antifungal bind to the cell membrane of fungi?

They bind to sterols in the phospholipid bilayer

What drugs cause injury to the plasma membranes of microbes?

1. Polymyxin B


2. Lipopeptides

2

What is an example of a Lipopeptide?

Daptomycin

What is a common use for daptomycin

Used against MRSA

How do some antibiotics inhibit nucleic acid synthesis?

By interfering with DNA replication or transcription by targeting DNA gyrase and RNA polymerase

What is the affect of antibiotics targeting DNA gyrase?

Bacteria can't uncoil DNQ

Antibiotics that inhibit Nucleic acid synthesis

- Rifampin


- Quinolones


- Fluoroquinolones

Fluoroquinolones

Ciprofloxacin


Levofloxacin

How do drugs inhibit the synthesis of essential metabolites?

Some drugs block the synthesis of folic acid, which is synthesized by bacteria but not humans

What are common drugs that inhibit the synthesis of essential metabolites and how do they do it?

Sulfa drugs, by mimicking PABA, which is a precursor to folic acid

Types of antiviral drugs

1. Nucleotide analogs


2. Enzyme inhibitors


3. Interferons

3

Nucleotide analogs

Drugs that mimic nucleotides, preventing viral replication

What is an example of a common Nucleotide analog?

Acyclovir

Enzyme inhibitors

Block viral enzymes

What is an example of a common enzyme inhibitor and how does it work?

Tamiflu


Blocks neuraminidase in influenza

Interferons

Proteins that are produced by cells infected with a virus


Cause uninfected cells to produce antiviral proteins

How do we test the effectiveness of antibiotics?

Disk diffusion method

Disk diffusion method

Adding discs laden with antibiotics to a spread plate and looking for zones of inhibition

How do we determine the necessary strength of an antibiotic?

We find the Minimal Inhibitory Concentration (MIC) by using a broth dilution test to find the lowest concentration of an antibiotic that will still prevent bacterial growth

Mechanisms of resistance to antimicrobial drugs

1. Enzymatic destruction or inactivation of the drug


2. Blocking entry/ prevention of penetration to target site


3. Alteration of the target molecule


4. Rapid efflux of the antibiotic

Enzymatic destruction or inactivation of the drug

B-Lactamases target the B-lactam ring shared by penicillins and cephalosporins

Blocking the entry/ prevention of penetration to the target site

Some bacteria alter the structure of porins, which no longer allow entry of the antibiotic

Alteration of the target molecule

Minor changes in the structure of bacterial proteins can prevent the antibiotic from binding to them

Rapid efflux of the antibiotic

The bacteria have molecular pumps that spit the antibiotics out of the cell before they can have an effect

Effects of combining drugs

1. Synergism


2. Antagonism

2

Synergism

When 2 or more antibiotics are more effective when taken together

Antagonism

Antibiotics taken in tandem are less effective than when taken alone

Microdilution plate

Used in broth dilution test to determine MIC using many different wells with varying concentrations of antibiotics