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Dental Bacteriology Exam 1
Chemotherapeutic Agents
55
Biology
Graduate
08/25/2009

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Term
Beta-lactam antibiotics:
Definition

destroy cell wall or prevent the synthesis of wall polymers in growing cells

**penicillins and cephalosporins, carbapenems, monobactams, Beta-lactamase inhibitors

Term
Agents that affect the cell wall:
Definition
Beta-lactams, vacomycin, and bacitracin
Term
Mechanism of action of penicillins:
Definition
Penicillins inhibit the last step of cell wall synthesis, in which a transpeptidation reaction results in a cross-linking of adjacent peptidoglycan strands (polymerization). The Beta-lactam portion of penicillin binds to the protein, preventing polymerization. When binding occurs, lysins are released which degrade previously formed peptidoglycan.
Term
Beta-lactamase:
Definition
"suicide inhibitors"-- They open the Beta-lactam ring hydrolytically
Term
Examples of Antistaphylococcal Penicillins resistant to Beta-lactamase:
Definition
oxacillin, methicillin, dicloxacillin, nafcillin
Term
Examples of Aminopenicillins:
Definition
ampicillin and amoxicillin-- have a broad spectrum, but are Beta-lactamase sensitive
Term
Antipseudomonas penicillins:
Definition

**extended spectrum, but Beta-lactamase sensitive

*ex: mezlocillin and piperacillin

Term
Cephalosporins mechanism of action:
Definition
cephalosporins also have a Beta-lactam ring like the penicillins-- same mode of action as penicillins, but have a broader antibacterial spectrum than penicillins. Their basic (6-member dihydrothiazine ring) structure allows moderate resistance to Beta-Lactamases, but not others (cephalosporinases)
Term
Examples of cephalosporins:
Definition

1. cefazolin

2. cephlathin

3. cefaclor

4. cefoxitin

5. cefotaxime

6. moxalactam

7. ceftriaxome

8. cefepime

Term
Carbapenems:
Definition

Beta-lactams with a carbon substituted for the sulfur on the thiazolidine right of penicillins.

***Broadest spectrum of all Beta Lactams

Example: imipenem

Term
Monobactams:
Definition

Mode of action is similar to other Beta-Lactams

example: aztreonam

Term
Beta-lactamase inhibitors:
Definition

Beta-lactams that bind to and inactivate Beta-lactamase enzymes.

*ex: clavulanic acid, sulbactam

**Clavulanate + amoxicillin = augmentin

**Clavulanate + ticarcillin = timentin

Term
glycopeptide antibiotics are not effective for gram _____ bacteria
Definition
gram negative-- won't pass through the outer membrane
Term
Glycopeptide antibiotics method of action:
Definition

inhibit the use of lipid-linked cell wall intermediates in the assembly of the linear peptidoglycan molecule.

***Used for multiresistant gram positive bacteria.

*example: vancomycin

Term
Bacitracin is used for gram ______ bacteria
Definition
Gram (+)
Term
Bacitracin method of action:
Definition

*topically applied

*targets a lipid carrier responsible for moving peptidoglycan precursors through the cytoplasmic membrane to the cell wall

*It is a Polypeptide

Term
Polymyxins are used for Gram _____ bacteria
Definition
Gram (-)
Term
Method of action for the polymyxins:
Definition

**Primarily used for external treatment of local infections (eye and skin)

fatty acid portion penetrates into the hydrophobic portion of the outer membrane of gram (-) bacteria. The ring portion interacts LPS and phospholipids. Distortion of the membrane results in increased cell permeability and lysis.

Term
Problems with polymyxins:
Definition
Causes severe nephrotoxicity
Term
Cell wall agents used for mycobacteria:
Definition

1. Isoniazid

2. ethionamide

3. ethambutol

4. cycloserine

Term
How to isoniazid and ethionamide work?
Definition
interfere with synthesis of mycolic acids (cell wall constituents) in mycobacteria
Term
Ethambutol and cycloserine method of action:
Definition
inhibit cell wall constituents in mycobacteria
Term
Agents that interfere with nucleic acid synthesis:
Definition

1. quinolones,

2. novobiocin,

3. rifamycins,

4. metronidazole

Term
Quinolones mechanism of action:
Definition
inhibit DNA replication--- inhibit the supercoiling DNA by binding to DNA gyrases (topoisomerases), which are enzymes that introduce negative superhelical turns into covalently circular DNA
Term
Examples of Quinolones:
Definition

Ciprofloxacin, levofloxacin, gatifloxacin and moxifloxacin

**(anything that ends with --floxacin)

Term
Novobiocin mechanism of action:
Definition
same as quinolones--inhibits DNA replication by binding to DNA gyrases, which introduce negative superhelical turns into covalently circular DNA
Term
examples of Rifamycins:
Definition

rifampin and rifabutin.

 

Term
Rifampin is used for what kind of bacteria?
Definition
Mycobacterium tuberculosis
Term
Rifabutin is used for what kind of bacteria?
Definition
Mycobacterium avium--causes tuberculosis like symptoms
Term
Rifamycins method of action:
Definition
prevents RNA synthesis by binding to DNA-dependent RNA polymerase
Term
Metronidazole has no significant activity against:
Definition
aerobic bacteria or facultatively anaerobic bacteria
Term
Metronidazole method of action:
Definition
Anaerobic bacteria reduce the compound when they take it up.  The reduced form acts as a free radical that damages bacterial DNA
Term
Agents that inhibit protein synthesis:
Definition

1. aminoglycosides

2. tetracyclines

3. macrolides

4. chloramthenicol

5. oxazolidinones

6. clindamycin

7. streptogramins

Term
Examples of aminoglycosides:
Definition

1. streptomycin

2. neomycin

3. kanamycin

4. gentamycin

5. tobramycin

6. amikacin

7. spectinomycin

Term
Are Aminoglycosides bacteriocidal or bacteriostatic?
Definition
aminoglycosides are bacteriocidal
Term
Aminoglycosides can treat Gram ______ bacteria
Definition
Gram (+) AND Gram (-)
Term
What kind of bacteria are resistant to aminoglycosides?
Definition
Anaerobes--do not take up the drugs
Term
examples of Tetracyclines:
Definition
tetracycline, doxycycline, minocycline
Term
Tetracyclines are bacteriostatic or bacteriocidal?
Definition
Bacteriostatic
Term
Examples of macrolides:
Definition

1. erythromycin

2. azithromycin

3. clarithromycin

Term
Macrolides are used for Gram ______ bacteria
Definition
Gram (+) AND Gram (-)
Term
Macrolides are bacteriostatic or bacteriocidal?
Definition
Bacteriostatic
Term
Chloramphenicol is used for what disease?
Definition
typhoid fever
Term
Oxazolidinones used for what kind of bacteria?
Definition

Staphylococcus, streptococcus, enterococcus

***used for strains of these bacteria resistant to penicillins, vancomycin, and aminoglycosides

Term
Example of oxazolidinones:
Definition
linezolid
Term

clindamycin used for Gram ______ bacteria

what type of metabolism does the bacteria have?

Definition

used for Gram (-) bacteria

the bacteria are anaerobic

Term
example of Streptogramins:
Definition
quinupristin-dalfopristin (Synercid)
Term
Streptogramins are used for what kind of bacteria?
Definition
Vancomycin resisitant E. faecium
Term
How do metabolic antagonists work?
Definition
they are analogs of bacterial growth factors-- the enzymes essential in the synthesis of and utilization of these factors can be inhibited by antimetabolites structurally related to the metabolites
Term
Examples of metabolic antagonists:
Definition

1. sulfonamides

2. trimethoprim

Term
sulfonamides mechanism of action:
Definition
structural analogs of p-aminobenzoid acid (PABA). Competitively inhit incorporate PABA into folic acid which is a precursor for purines, pyrimidines, and amino acids
Term
Trimethoprim mechanism of action:
Definition
structural analog of dihydrofolic acid--inhibits the synthesis of folic acid
Term
Clofazimine mechanism of action:
Definition
binds to mycobacterial DNA and causes damage
Term
Types of bacteria clofazimine is used for:
Definition
Mycobacterium tuberculosis and M. leprae
Term
Pyrazinamide (PZA) is used for what kind of bacteria?
Definition
Mycobacteria tuberculosis
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