Antimicrobrial Drugs

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The use of drugs to treat a disease

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Chemotherapy

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Interfere with the growth of microbes within a host

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Antimicrobial drugs

Front 3

Substance produced by a microbe that, in small amounts, inhibits another microbe

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Antibiotic

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A drug that kills harmful microbes without damaging the host

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Selective toxicity

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Year when Flemming discovered penicillin

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1928

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What was discovered by Flemming?

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Penicillin

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What produces penicillin?

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Penicillum

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Performed the first clinical trials of penicillum

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Howard Florey and Ernst Chain

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Year when Howard Florey and Ernst Chain performed the first clinical trials of penicillum

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1940

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Range of microbes the agent acts against

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Spectrum of activity

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Gram positive and negative; used for unidentified microbe

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Broad

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Small number of microbes; Used when microbe identified; Prevents destruction of normal flora

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Narrow

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2 Gram-Positive Rods antibiotics

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1. Bacitracin (Bacillus subtilis)

2. Polymyxin (Bacillus polymyxa)

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8 Actinomycetes antibiotics

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1. Amphotericin B (Streptomyces nodosus)

2. Chloramphenicol (Streptomyces venezuelae)

3. Chlortetracycline (Streptomyces aureofaciens)

4. Tetracycline (Streptomyces aureofaciens)

5. Erythromycin (Streptomyces erythraeus)

6. Neomycin (Streptomyces fradiae)

7. Streptomycin ( Streptomyces griseus)

8. Gentamicin (Micromonospara purpureae)

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3 Fungi antibiotics

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1. Cephalothin (Cephalosporium spp.)

2. Griseofulvin (Penicillum griseofulvum)

3. Penicillin (Penicillum notatum)

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Penicillinase-resistant penicillins

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Penicillin

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Extended-spectrum penicillins

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Penicillin

Front 18

6 Antibacterial antibiotics inhibitors of cell wall synthesis

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1. Penicillin

2. Cephalosporins

3. Bacitracin

4. Vancomycin

5. Isoniazid (INH)

6. Ethambutol

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2nd, 3rd and 4th generations more effective against gram-negatives

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Cephalosporins

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Topical application; against gram-positives

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Bacitracin

Front 21

Glycopeptide; Important "last line" against antibiotic resistant S. aureus

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Vancomycin

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2 Polypeptide antibiotics

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1. Bacitracin

2. Vancomycin

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2 antimycobacterium antibiotics

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1. Isoniazid (INH)

2. Ethambutol

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Inhibits mycolic acid synthesis

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Isoniazid (INH)

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Inhibits incorporation of mycolic acid

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Ethambutol

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5 Antibacterial Antibiotics Inhibitors of Protein synthesis

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1. Chloramphenicol

2. Aminoglycosides

3. Tetracyclines

4. Macrolides

5. Erythromycin

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Broad spectrum; Binds 50S subunit, inhibits peptide bond formation

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Chloramphenicol

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3 Aminoglycosides

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1. Streptomycin

2. Neomycin

3. Gentamycin

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Broad spectrum; Changes shape of 30S subunit

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Aminoglycosides

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Broad spectrum; Interferes with tRNA attachment

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Tetracyclines

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Gram-positives; Binds 50S, prevents translocation

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Macrolides and Erythromycin

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1 Antibacterial Antibiotic Inhibitor of Plasma membrane

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Polymyxin B

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Topical; Combined with bacitracin and neomycin in over-the-counter preparation

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Polymyxin B

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2 Antibacterial Antibiotics Inhibitors of Nucleic Acid Synthesis

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1. Rifamycin

2. Quinolones and fluoroquinolones

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Inhibits RNA synthesis; Antituberculosis

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Rifamycin

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1 Quinolones and fluoroquinolones

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Ciprofloxacin

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Inhibits DNA gyrase; UTI

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Quinolones and fluoroquinolones

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1 Antibacterial Antibiotics Competitive Inhibitors

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Sulfonamides (Sulfa drugs)

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Inhibit folic acid synthesis; Broad spectrum

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Sulfonamides (Sulfa drugs)

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The ability of a microorganism to withstand the effects of an antibiotic

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Antibiotic resistance

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2 types of drug resistance

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1. Natural resistance

2. Acquired resistance

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Antibiotics favor resistant strains but do not cause genetic changes

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Acquired resistance

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4 mechanisms

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1. Alteration of target of drug action

2. Alteration of membrane permeability

3. Efflux or pumps out the drug

4. Development of enzymes

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Mutation alters protein produced or target is modified

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Alteration of target of drug action

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-Change alters nature of proteins in membrane

-Membrane transport system

-Pores in membrane prevent entry

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Alteration of membrane permeability

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Mutation that increases expression of efflux gene

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Efflux or pumps out the drug

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-Destroy or inactivate drug

-B-lactamase-several

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Development of enzymes