DNA Function Inhibitors Flashcards

1
Q

Fluoroquinolones MOA

A

Targets bacterial DNA gyrase, which is needed for DNA unwinding and normal replication
Bactericidal

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2
Q

Fluoroquinolone Examples

A

Ciprofloxacin [Cipro] - urinary
Levofloxacin [Levoquin] - urinary/respiratory
Moxifloxacin [Alvelox] - respiratory

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3
Q

Fluoroquinolone Absorption

A

well absorbed orally

cipro and levo are availaible parenteral

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4
Q

Fluoroquinolone Distribution

A

Good penetration into most tissues, CNS if inflammed, highly concentrates in the urine

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5
Q

Fluoroquinolone metabolism/excretion

A

primarily renal excretion

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6
Q

“respiratory” quinolones

A

Levofloxacin

Moxifloxacin

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7
Q

Fluoroquinolone Use, gram + cocci

A

Strep. pneumoniae (pneumonia, bronchitis, acute sinusitis)
“respiratory quinolones”
MSSA (skin infections)

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8
Q

Fluoroquinolone use, gram - cocci

A
Moraxella catarrhalis (sinusitis, bronchitis) 
--> Levofloxacin
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9
Q

Fluoroquinolone use, gram - bacilli

A
Haemophilis Influenzae (lower respiratory tract infection, pneumonia)
Pseudomonas aeruginosa
E. Coli (UTI*)
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10
Q

Fluoroquinolone use, atypicals

A

[Moxifloxcin]
Chlamydia (trachoma, urethritis, CAP)
Mycoplasma pneumoniae (CAP)

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11
Q

Fluoroquinolone ADR

A

C. Diff Colitis - N/V/D
Possible tendon rupture, rare
Limited use in pregnancy and

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12
Q

Fluoroquinolone DDI

A

theophyline metabolism is reduced

antacids reduce ABX metabolism

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13
Q

Nitrofurantoin

A

Macrobid, Macrodantin
“urinary tract antiseptic” because concentrate highly in renal tubules. Plasma levels can’t get high enough safely to treat systemic infections

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14
Q

Nitrofurantoin MOA

A

Bacterial enzymes reduce the drug into intermediates that damage DNA. Humans dont reduce as quickly.
Bactericidal - concentration dependant

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15
Q

Nitrofurantoin pharmacokinetics

A

ABS by GI system very well
Excreted into urine, rate linearly related to renal function
Turns urine brown color

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16
Q

Nitrofurantoin uses in UTI

A

Second line - proteus and pseudomonas are resistant

Very effective against E. Coli though, can be used when patients are resistant to TMP/SMX

17
Q

Metronidazole

A

[Flagyl]

18
Q

Metronidazole MOA

A

Prodrug that is transformed into a highly reactive nitro radical by organisms, especially anaerobes and protozoa. The anion targets DNA and is bactericidal

19
Q

Metronidazole Pharmacokinetics

A

Absorbed well PO
Distribution is wide, including CSF and bone
Hepatic metabolism - adjust dose in liver dz
COntraindicated in breast feeding moms

20
Q

Metronidazole uses, anaerobes

A

Clostridium difficile
Bacteroides fragilis
Helicobacter pylori

21
Q

Metronidazole uses, protozoa

A

Trichomonas vaginalis

22
Q

Sulfonamides

A

Sulfamethoxazole

23
Q

Sulfonamide MOA

A

Inhibitors of folic acid production via inibiting the enzyme dihydropteroate synthetase organisms must use to create folic acid.
Bacteristatic, folic acid stores must be used up by the organism before the drug’s effects kick in

24
Q

Sulfonamide plus trimethoprim (TMP) MOA

A

Trimethoprim is a dihydrofolate reductase inhibitor. These together are synergistic, acting on two sequential steps of folinic acid synthesis. TMP is NOT a sulfonamide

25
Q

Sulfamethoxazole (SMX) plus trimethoprim (TMP)

A

Bactrim or Septra…. abbreviated TMP/SMX

26
Q

Sulfonamide ABS/distribution

A

Well absorbed on an empty stomach

Well distributed in body water. Displaces bilirubin bound to protein that can cause kernicterus in neonates

27
Q

Sulfonamide met/excr

A

Deactivated via acetylation, then excreted in kidneys

Need to change the dose in renal failure

28
Q

Sulfonamide uses - general

A

BROAD SPECTRUM ABX, seldom used in a single drug form due to resistance and the availability of less toxic drugs.
TMP/SMX used most commonly together

29
Q

TMP/SMX use, gram + cocci

A

MRSA (community acquired skin infection)

30
Q

TMP/SMX use, gram - bacilli

A

Klebsiella, proteus, enterobacter (uncomplicated UTI)

Pseudomonas

31
Q

TMP/SMX use, atypicals

A

Chlamydia - trachoma, CAP, urethritis