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Pharmacology > Nucleic Acid Synthesis Inhibitors > Flashcards

Nucleic Acid Synthesis Inhibitors Flashcards

1
Q

Are NA synth drugs cidal/static? Concentration/time dependent?

A

Fluoroquinolones: cidal, concentration dep.
Metronidizole: cidal, dependent on anaerobic environment for antibacterial activity
Rifampin: cidal

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2
Q

How do fluroquinolones target NA synthesis?

A

Inhibits topoisomerase
(DNA gyrase)

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3
Q

How does Rifampin target NA synthesis?

A

Inhibits DNA-dependent RNA
Polymerase

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4
Q

How does metronidozole target NA synthesis?

A

Causes DNA breaks with free radicals and inhibits DNA repair of the breaks

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5
Q

How do bacteria develop resistance to fluoroquinolones?

A

Biggest concern is mutation of the Topo II enzyme (gyrase) that alters drug binding site

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6
Q

How do bacteria develop resistance to metronidozole?

A
  • Rare
  • Effects on ferredoxin, the protein that catalyzes reduction of metronidazole
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7
Q

How do bacteria develop resistance to Rifampin?

A

Resistance due to an alteration of the target:
mutation in the RNA polymerase enzyme
* Occurs very rapidly (within 2 days) when used alone
* MUST USE IN COMBINATION WITH OTHER DRUGS!!!

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8
Q

Which NA synth drug has resistance that is going from aimals to humans? How does this affect use regulations?

A

Fluoroquinilone esistance in human medicine increasing -> increased use in veterinary medicine transferring resistance to humans.
EXTRA-LABEL USE BANNED IN FOOD ANIMALS!

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9
Q

Which NA synthesis drugs are most important in treating resistant infections in humans? How does this affect use in veterinary species?

A

Fluoroquinolones
Off-label use in food animals is prohibited

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10
Q

What are the important side effects of Fluoroquinolones?

A
  • Cartilage/joints: DO NOT USE IN GROWING OR IMMATURE ANIMALS!!!
  • Eyes: ACUTE BLINDNESS IN CATS
  • GI upset
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11
Q

What are the important side effects of Metronidozole?

A
  • Rare
  • Carcinogenic and mutagenic in laboratory animal models
  • FOR THIS REASON, METRONIDAZOLE USE IS BANNED IN FOOD ANIMALS
  • CNS
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12
Q

What are the important side effects of Rifampin?

A
  • Rare
  • Liver
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13
Q

What factors must you consider when using Rifampin with other drugs?

A
  • Rifampin must NEVER be administered alone
  • POTENT HEPATIC ENZYME INDUCER- Increases rate of metabolism of other drugs
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14
Q

Which NA synthesis inhibitor drug type is banned in food animals and why?

A

Metronidazole because carcinogenic in lab animal studies

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15
Q

What is the spectrum of activity of the NA synthesis inhibitor drugs? Are some better than others for certain bacteria?

A
  • Fluoroquinolones: Excellent Gram (-), Poor Gram (+), No coverage of anaerobes
  • Metronidazole: Excellent anaerobes and protozoa
  • Rifampin: Excellent Gram (+), Mycobacteria
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16
Q

Which NA synthesis inhibitor can only be used in aerobic infections?

A

Fluoroquinolones

17
Q

Which NA synthesis inhibitor drug type is unique to anaerobic infections and why can’t it be used in aerobic infections?

A

Metronidazole must be reduced to be activated
* Reduction requires an anaerobic environment
* Reduction system of aerobic activity is insufficient

18
Q

What might you want to warn an owner about when giving Rifampin?

A

Drug may impart an orange-red color to urine, feces,
saliva, sputum, tears, and sweat and it STAINS

19
Q

Which nucleic acid synthesis inhibitor drug would you use to treat an in fection with an aerobic Gram (-) bacterium?

A

Fluoroquinolones

20
Q

Which nucleic acid synthesis inhibitor drug would you use to treat an in fection with an aerobic Gram (+) bacterium?

A

Rifampin

21
Q

Which nucleic acid synthesis inhibitor drug would you use to treat an in fection with mycobacterium?

A

Rifampin

22
Q

Which nucleic acid synthesis inhibitor drug would you use to treat an in fection with an anaerobic Gram (+) or Gram (-) bacterium?

A

Metronidazoles

23
Q

What NA synthesis inhibitor would you use to treat an abscess?

A

Rifampin loves pus!

Pharmacology (9 decks)

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