Anti-Microbial Agents Ii

Front 1

What are the two main classes of Abio?

Back 1

1. Cell Wall Agents

2. Ribosomal Agents

Front 2

Subclasses of Ribosomal Agents?

Back 2

1. Macrolides

2. Lincosamides

3. Tetracylines

4. Amphenicols

5. Aminoglycosides

(there are more)

Front 3

MOA of Ribosomal Agents?

Back 3

Agent binds to rRNA (30s, 50s or 70s) --> bc rRNA is involved in protein synthesis --> Incomplete protein, Incorrect protein or Nonsense protein.

--> cell has reduced ability to carry out normal functions --> apoptosis

They disrupt bacterial protein synthesis.

Front 4

30s ribosomal agents

Back 4

1. Aminoglycocides

2. Tetracyclines

3. Nitrofuranes

Front 5

Aminoglycosides

Back 5

1. Irreversible 30s agent

2. Narrow spectrum = G(-)

3. Bactericidal

4. Poorly absorbed in GI tract (∴ admin IV)

5. Strongly basic, hydrophilic

6. Poor penetration of CSF

7. Ex. Gentamycin

Front 6

Bacterial resistance of Aminoglycocides via?

Back 6

Metabolism.

Acetylation, Phosphorylation and Adenylation.

Front 7

What Aminoglycocide drug lowers bacterial

resistance?

Back 7

Amikacin

(α-hydroxy-γ-aminobutyl grp blocks metabolism)

Front 8

Aminoglycocide ADR

Back 8

Ototoxicity (irreversible)

Nephrotoxcity

Front 9

Tetracycline

Back 9

1. 30s agent. Prevents tRNA binding.

2. Broad spectrum

3. Bacteriostatic

4. Potent chelator of metals

5. Ex. Tetracycline, Doxycline

Front 10

What should you warn the pt about when taking Tetracyclines?

Back 10

Because they chelate metals, separate iron

supplements and milk/dairy 2-4 hours from dose.

Otherwise, decrease Abs.

Front 11

Nitrofurans

Back 11

1. 30s agent

2. Spectrum?

3. Ex. Nitrofurantoin

Front 12

Macrolides

Back 12

1. 50s agent

2. Narrow spectrum = G(+)

3. Also mycoplasma, legionella, chlamydia.

4. Bacteriostatic

5. Ex. Erythromycin, Azithromycin

6. Used for CAP, otitis media and bronchitis

Front 13

Why does Telithromycin have an advantage over other macrolides?

Back 13

Removal of Cladinose

Increase domain II binding

Decrease domain V binding

Front 14

Lincosamides

Back 14

1. 50s agent (cross over with macrolides)

2. Narrow spectrum = G(+)

3. Bacteriostatic

4. Ex. Clindamycin

Front 15

Biggest side effect of Lincosamides?

Back 15

Severe diarrhea associated with pseudomembranous colitis. Over growth of intestinal C. difficile.

Front 16

Amphenicols

Back 16

1. 50s agent

2. Broad spectrum

3. Bacteriostatic

4.Ex. Chloramphenicol

Front 17

Streptogramins

Back 17

1. 50s agent

2. Narrow Spectrum = G(+)

3. Inhibits CYP3A4 ∴ drug-drug possible (unique)

4. Ex. Quinupristin, Dalfopristin

5. Bacteriostatic alone, Bactericidal together.

(Synercide®)

Front 18

Oxazolidinone

Linezolid

Back 18

1. 70s agent

2. Last line of treatment for MRSA

3. Narrow Spectrum = G(+)

4. Bactericidal

Front 19

Glycopolypeptides

Back 19

1. Prevent cell wall synthesis by binding to the D-ala/ala tail of the peptidoglycan layer

2. Narrow Spectrum = G(+)

3. Active against resistant S. aureus.

4. Bactericidal

5. Ex. Vancomycin (IV), Teicoplanin (IM)

Front 20

Cyclic Peptides

Bacitracin A

Back 20

1. Induces cell death by disrupting cell wall permeability --> apoptosis

2. Narrow Spectrum = G(+)

3. Bactericidal

Front 21

Cyclic Peptides

Daptomycin

Back 21

1. Induces cell death by causing depolarization of cell membrane

2. Narrow spectrum = G(+)

3. Bactericidal

Front 22

Sulfonamide

Back 22

1. Competitive inhibitor of PABA in bacterial THF synthesis (tetrahydrofoliate)

2. Broad Spectrum

3. Bacteriostatic

4. Ex. Sulfmethoxazole (Bactrim)

5. The first two steps of this rxn are bacteria

specific.

Front 23

Trimethoprim

Back 23

1. Competitive inhibitor of dihydrofolate reductase in the production of THF

2. Broad Spectrum

3. Bacteriostatic

4. Opposed to sulfonamides, this acts at a

human target ∴ potential for toxicity

Front 24

4-Quinolones (Fluoroquinolones)

MOA, examples.

Back 24

1. Inhibitor of DNA gyrase ∴ can't make mRNA.

2.Broad Spectrum

3. Bactericidal

4. Ex. Ciprofloxacin (2nd), Levofloxacin (3rd) and Moxifloxacin (4th)

Front 25

4-Quinolones (Fluoroquinolones)

Side effects

Back 25

N/V, diarrhea

Drug interaction though inhibition of CYP1A2

Prolongation of QTc interval

Phototoxcity

Achilles Tendon rupture

Front 26

Narrow Spectrum = G(+)

Back 26

Penicillin class, Methicillin class, Some 1st Generation Cephalosporins, Macrolides predominantly Lincosamides, Linezolid, Glycopolypeptides, Cyclic polypeptides (Bacitracin and Daptomycin), Streptogramins

Front 27

Narrow Spectrum G(-)

Back 27

Monobactam class

Aminoglycosides

Front 28

Broad Spectrum

Back 28

Ampicillin class, Carbenicillin class, Mezlocillin class, Carbapenems, many 2nd-4th generation cephalosporins, Tetracyclines, Amphenicols, Sulfonamides, Trimethoprim, Fluoroquinolones

Front 29

4-Quinolones (Fluoroquinolones)

Generational trends

Back 29

2nd-4th generation...no real trend except a little more gram(-) in earlier generations

1st generation are not fluorinated mostly and are virtually non-existent in clinical use

Front 30

We're ECSTaTiC about bacteriostatic

Back 30

Erythromycin, Clindamycin, Sulfonamides, Tetracyclines, Trimethoprim, Chloramphenicol

Front 31

Very Finely Proficient At Cell Murder

Back 31

Vancomycin, Fluoroquinolones, Penicillins, Aminoglycosides, Cephalosporins, Metronidazole