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Review Question - QID 320

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QID 320 (Type "320" in App Search)
Rifampin is highly effective against phagocytized intracellular Staphylococcus aureus especially in combination with other antibiotics because of its:

Hydrophilic activity

6%

101/1761

High cell penetration

82%

1442/1761

Structural similarity to penicillin

2%

34/1761

Structural similarity to vancomycin

1%

22/1761

Beta-lactamase activity

9%

157/1761

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Based on the choices above, rifampin works well synergistically with other antibiotics because of its high cell penetration.

Rifampin is a bactericidal antibiotic that blocks the function of RNA polymerase and subsequent RNA transcription. It is used to treat both staphylococcus and mycobacterium infections. Because of the high rate of cellular penetration, it is effective against intracellular phagocytized staphylococcus.

Darouiche et al. investigated the cellular penetration of seven antibiotics in cultured human umbilical vein endothelial cells. Lipophilic drugs such as minocycline, ciprofloxacin and rifampin had better cell penetration. Although rifampin was found to have limited killing activity, it potentiated the bactericidal activity of other antibiotics when used in combination.

Illustration A shows a schematic detailing the mechanism of rifampin’s bactericidal action.

Incorrect Answers
Answer 1, 3, 4, 5: Rifampin is lipophilic, rendering its ability to cross the cell wall/membrane and exert its actions against RNA polymerase.

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