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D&D Infectious Disease Midterm > Quinolones - Pharm > Flashcards

Quinolones - Pharm Flashcards

1
Q

what are the DNA gyrase inhibitors

A

quinolones

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2
Q

MOA of quinolones

A

inhibit topoisomerase II (AKA DNA gyrase) and topoisomerase IV

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3
Q

what does topoisomerase II/DNA gyrase do

A

relaxes the positive supercoils ahead of the replication fork by negative supercoiling DNA

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4
Q

by quinolones inhibiting topoisomerase IV, what is this doing?

A

interferes with the separation of replicated DNA into daughter cells

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5
Q

which drug is in the 1st group of the quinolones?

the 1st group is largely limited to what kind of bacteria??

A

gram negative, aerobic bacteria

nalidixic acid

not used anymore

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6
Q

what drugs (4) are in the 2nd group of the quinolones?

these are largely active against which bacteria?

A

aerobic gram negative - like the 1st group

levofloxacin
ciprofloxacin
norfloxacin
ofloxacin

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7
Q

which drug is the most active in the 2nd group of the quinolones

A

cipro

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8
Q

within the 2nd group, which drug is best for streptococcus pneumoniae?

A

levofloxacin - it’s sometimes in group 3 for respiratory!

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9
Q

can the 2nd group of quinolones cover gram positive bacteria?

A

gram positive coverage is limited

can cover MSSA, but NOT all MRSA

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10
Q

which group of quinolones is actually good for gram positive bacteria?

A

third group

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11
Q

name 3 drugs in the 3rd group of the quinolones

A

moxifloxacin
gatifloxacin
gemifloxacin

could also consider levofloxacin here - all good for resp infections

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12
Q

what is a newer quinolone

A

delafloxacin

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13
Q

which group of quinolones is mainly for respiratory infection

A

3

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14
Q

which group 3 quinolone has good activity for anaerobes

A

moxifloxacin

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15
Q

compare the activity of cipro vs group 3 for gram negative bacteria, like pseudomonas

A

group 3 is same or inferior to cipro for gram negative, including pseudomonas

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16
Q

which group of quinolones is active for atypical bacteria like mycobacteria and legionella, and for anaerobes

A

2

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17
Q

MAJOR resistance mechanism to quinolones

A

1 or more point mutations in quinolone binding region of the target enzyme (topo 2 or 4), or change in permeability of the organism

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18
Q

name 2 plasmid mediated mechanism of fluoroquinolone resistance

A

-Qnr proteins protect DNA gyrase (topoisomerase II) from the fluoroquinolones

-modifying cipro by aminoglycoside acetyltransferase

QNR = plasmid mediated quinolone resistance

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19
Q

fluoroquinolones generally have HIGH bioavailability with the exception of…..

A

norfloxacin

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20
Q

true or false

fluroquinolones have low tissue penetration

A

FALSE - high

this is partly why so toxic

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21
Q

fluoroquinolones undergo _________ excretion with the exception of ________

A

renal - adjust dose!!!

moxifloxacin

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22
Q

important consideration of something that can impair fluoroquinolone absorption

A

divalent and trivalent cations

therefore, have them 2 hours b4 or 4 hours after the fluoroquinolone

23
Q

which fluoroquinolone is used with caution in HEPATIC failure

A

moxifloxacin

24
Q

____________ is a drug of choice for the prophylaxis and treatment of anthrax

A

cipro

25
Q

name the 4 respiratory fluoroquinolones

A

levofloxacin
gatifloxacin
gemifloxacin
moxifloxacin

used for upper and lower Resp tract infections

26
Q

are fluoroquinolones effective against UTI

A

yes - including when cause by pseudomonas

27
Q

true or false

fluoroquinolones can be used for bacterial diarrhea

A

true

28
Q

name 4 bacteria that cause bacterial diarrhea that fluoroquinolones can treat

A

shigella
salmonella
toxigenic e. coli
campylobacter

29
Q

can fluoroquinolones be used in skin and soft tissue infections

A

yes

30
Q

do fluoroquinolones have pseudomonas aeruginosa coverage

A

YES

31
Q

AE’s of fluoroquinolones

A

GI - NVD, anorexia, abdominal pain

CNS - headache, dizzy, drowsy, insomnia, seizure (rare)

derm - rash, itching, edema, hives

PHOTOTOXICITY - few hours after exposure

musculoskeletal

32
Q

as mentioned, fluoroquinolones have musculoskeletal adverse effects.
thus, who are they used in caution/not used in

A

caution - children
avoided in pregnancy

33
Q

true or false

quinolones are bactericidal

A

TRUE

bactericidal, conc dependent

34
Q

nitrofurantoin is a urinary _____

A

antiseptic

35
Q

is nitrofurantoin bactericidal or static

A

cidal

36
Q

nitrofurantoin is used for treatment of……..

A

lower UTIs ONLY
simple and uncomplicated

37
Q

does macrobid have systemic antibacterial action? explain

A

NO

it is metabolized and excreted so rapidly

38
Q

explain the MOA of nitrofurantoin

A

activated inside bacteria by reduction of nitro via reduction by FLAVOPROTEIN NITROFURANTOIN REDUCTASE into unstable metabolites (radicals)

these unstable metabolites disrupt the ribosomal RNA, DNA, and other intracellular components of bacteria

39
Q

agent of choice in uncomplicated lower UTI

A

nitrofurantoin

40
Q

how does resistance to nitrofurantoin happen

A

RARE - but by mutations in the reductase that reduces nitrofurantoin into unstable metabolites

41
Q

AE nitrofurantoin

A

*pulmonary toxicity
*hemolytic anemia in G6PDH deficiency – bc produces reactive species - have no NADPH to reduce

GI issues
neuropathy

42
Q

long acting formulation of nitrofurantoin

how often is it taken?

A

macrobid

twice daily

43
Q

What is usually at position 6 in fluoroquinolones
what is exception

A

FLUORINE

exception is nalidixic acid, which is H

44
Q

in general, topo 2 and 4 are important for bacteria in….

A

replicating DNA

45
Q

all fluoroquinolones have what common feature

A

activity against all gram NEGATIVE AEROBIC bacteria

46
Q

true or false

all fluoroquinolones inhibit MRSA

A

false -

some active against MRSA, but not all

all active against MSSA

47
Q

true or false

all fluoroquinolones inhibit DHFR

A

no

48
Q

name 2 specific things that cannot be taken with fluoroquinolones

A

milk and antacids

bivalent and trivalent cations

impairs absorption

49
Q

true or false

moxifloxacin is not renally eliminated

A

true - hepatic

50
Q

if taking milk/antacids how long to wait before/after fluoroquinolones

A

2 hours before or 4 hours after

51
Q

WHY is nitrofurantoin only for lower UTIs

A

gets matabolized and excreted so fast that no systemic antibacterial reaction achieved

52
Q

WHY is resistance to nitrofurantoin rare

A

major resistance mechanism in general is changing the target site. however, the reactive species can target anything - RNA, DNA, and other component s—- resistance is rare

53
Q

nitrofurantoin has ____- toxicity

A

pulmonary

54
Q
A

D&D Infectious Disease Midterm (26 decks)

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