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Drug Mechanisms > Inhibitors of Nucleic Acid Synthesis > Flashcards

Inhibitors of Nucleic Acid Synthesis Flashcards

1
Q

What are the two classes of antibiotics that are inhibitors of nucleic acid synthesis?

A

Rifamycins and Quinolones

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2
Q

What drugs are first-generation quinolones?

A

Nalidixic acid and cinoxacin

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3
Q

How do rifamycins inhibit nucleic acid synthesis?

A

They inhibit DNA-dependent RNA polymerase

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4
Q

What are the second-generation quinolones?

A

Fluoroquinolones

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5
Q

What is the activity of the Quinolones?

A

Bactericidal

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6
Q

What is the activity of the rifamycins?

A

Intermediate bactericidal

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7
Q

What do the first and second generation quinolones inhibit in gram-positive bacteria?

A

Topoisomerase IV

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8
Q

What do the first and second generation quinolones inhibit in gram-negative bacteria?

A

DNA gyrase

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9
Q

What is cross-resistant with rifamycins?

A

Other rifamycins

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10
Q

How can bacteria resist the quinolones?

A

Active efflux and by altering DNA gyrase or topoisomerase IV

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11
Q

What can happen to body secretions when taking rifamycins?

A

they can be discolored orange or red

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12
Q

What causes the discoloration of rifamycins?

A

They are highly conjugated and colored red/orange

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13
Q

What caution is there in patients taking rifamycins besides discoloration?

A

Hepatotoxicity in patients with pre-existing liver conditions

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14
Q

What do rifamycins do to cytochrome P450?

A

They are inducers of the P450 enzyme which lowers concentrations of drugs in the plasma

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15
Q

What other infection are rifamycins used to treat besides atypical mycobacterial infections?

A

Tuberculosis

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16
Q

What effect do quinolones have on the P450 enzyme?

A

They are inhibitors of the P450 enzyme

17
Q

Which one is more efficacious, fluoroquinolones or 1st generation quinolones?

A

fluoroquinolones exhibit enhanced potency, extended spectrum of activity, and improved distribution properties

18
Q

What two toxicities are caused by fluoroquinolones?

A

Serious liver injury and phototoxicity

19
Q

What effect do fluoroquinolones have on collagen?

A

They can lead to collagen degradation and malformation

20
Q

What disease can be caused by quinolones?

A

Arthropathy

21
Q

What population are quinolones contraindicated in?

A

Pregnant women and children under 16

22
Q

What effect do fluoroquinolones have on the heart?

A

They can lead to a prolonged QT interval and arrhythmias

23
Q

What can lead to a decrease in the oral bioavailability of quinolones?

A

polyvalent cations

24
Q

Fluoroquinolones can cause ______ which can last for months after the treatment.

A

peripheral neuropathy

Drug Mechanisms (9 decks)

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