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Ok Pharmacology... Let's Do This... Be Gentle > Inhibitors of DNA Function > Flashcards

Inhibitors of DNA Function Flashcards

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1
Q

what are the 3 inhibitors of DNA function

A
  1. fluoroquinolones
  2. nitrofurantoin
  3. metronidazole
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2
Q

which fluoroquinolone has good pseudomonal coverage

A

cipro

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3
Q

which fluoroquinolone has good urinary and respiratory coverage

A

levo

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4
Q

what fluoroquinolone has good gram (+) coverage

A

moxi

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5
Q

what part of bacteria do fluoroquinolones target

A

bacterial DNA gyrase and topoisomerase IV

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6
Q

what is the fxn of bacterial DNA gyrase

A

required for normal DNA replication → transcription and some aspects of DNA repair and recombination

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7
Q

DNA inhibitors inhibit DNA __

A

precursors

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8
Q

what is fluoroquinolones MOA

A

bactericidal → rapid w.in 2 hr

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9
Q

how does strep pneumo develop resistance against fluoroquinolones

A

point mutations in DNA gyrase/topoisomerase

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10
Q

strep pneumo resistance to fluoroquinolones is a __ process

A

step wise

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11
Q

strep pneumo prevents drug-target against fluoroquinolones via ___

and ___ gene

A

drug efflux

MDR

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12
Q

what is the holy trinity of URI infxn

A

strep pneumo

m. cat
h. flu

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13
Q

what are the respiratory quinolones

A

levo

moxi

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14
Q

which quinolone covers bacillus anthracis

A

cipro

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15
Q

quinolones should only be used in

A

very serious infxns

→ ex don’t use levo for m.cat for sinusitis or bronchitis

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16
Q

cipro and levo should be used for pseudo and e.coli only in

A

complicated UTIs

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17
Q

which quinolone has good coverage against atypical organisms (chlamydia, mycoplasma pneumoniae, rickettsia)

A

moxi

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18
Q

fluoroquinolones are well absorbed __

and also available __

A

orally

IV

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19
Q

fluoroquinolones have good penetration into most tissues, including high __

A

urinary levels

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20
Q

fluoroquinolones are primarily excreted by the __,

except for __

A

kidneys

moxi

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21
Q

renal dosing is needed for levo and cipro, but not for __

A

moxi

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22
Q

fluoroquinolones are generally well tolerated, the most two common adverse rxns are mild

A
  1. GI tract
  2. CNS (HA, dizzy, insomnia)
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23
Q

what are the 2 box warnings for quinolones

A
  1. 3-4 fold risk of tendon rupture → rare
  2. potential for athropathies → limits use in pregnancy and children <12 yo
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24
Q

what cardiac adverse effect do quinolones have

A

prolonged QT interval

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25
what are the 3 drug-drug interactions w. quinolones
1. antacids 2. theophylline and caffeine
26
which quinolone are drug-drug interactions most associated with
cipro
27
theophylline rxn w. cipro is of less importance now bc
theophylline is hardly ever used
28
nitrofurantoin is most commonly used for
urinary tract antiseptic
29
nitrofurantoin is not used for __ infxns bc __ can not be obtained w. safe doses
systemic effective Cp
30
nitrofurantoins are \_\_\_ by \_\_ to intermediates that \_\_\_
reduced bacterial enzymes damage bacterial DNA
31
nitrofurantoins are generally (cidal or static)
bactericidal
32
why is nitrofurantoin selectively toxic
bc mammalian enzymes don't reduce nitrofurantoin as rapidly
33
nitrofurantoin is used for what class of bacteria
gram negative rods
34
nitrofurantoin is used for what type of infxn
uncomplicated UTIs
35
nitrofurantoin works well against \_\_ but \_\_ and __ are resistant
e.coli pseudomonas and proteus
36
nitrofurantoin has rapid and complete __ absorption
oral
37
nitrofurantoin is excreted into the \_\_\_ and requires __ dosing
urine renal
38
use of nitrofurantoin is contraindicated in
renal insufficiency
39
mabrobid is
bid nitrofurantoin
40
macrodantin is
qid nitrofurantoin
41
most common adverse rxns of nitrofurantoin occur in the
GI tract
42
\_\_\_ forms of nitrofurantoin are better tolerated
macrocrystalline
43
what are 3 serious adverse rxns of nitrofurantoin
1. hemolytic anemia 2. neuropathies → chronic use 3. category B for pregnancy → but should NOT be given in 3rd trimester dt hemolytic anemia
44
metronidazole is a __ transformed to reactive radicale in organisms with \_\_
prodrug negative redox potential
45
metronidazole is effective against what 2 bacteria
1. anaerobic 2. protozoa
46
metronidazole kills via
DNA strand breaks inhibition of replication
47
metronidazole is (static or cidal)
cidal
48
resistance to metronidazole is via \_\_ which \_\_\_
expression of nitroimidazole reductase stops formation of nitroso-group
49
metronidazole has esecially good activity against which anaerobes
1. bacteroides 2. c.diff
50
the bioavailability of metronidazole is \_\_ and absorption is not \_\_
80% affected by food
51
metronidazole has good distribution, including \_\_ and \_\_
CSF bone
52
metronidazole is primarily metabolized via __ metabolism, and __ dosing is required
hepatic liver
53
what is a concern for nursing moms with metronidazole
it is excreted in breast milk
54
drug interactions w. metronidazole are possible w.
CYP450 inhibitors
55
the most common adverse rxns with metronidazole are (4)
nausea HA dry mouth metallic taste
56
metronidazole is contraindicated in pregnancy during the \_\_
1st trimester
57
metronidazole can have a drug-drug interaction w.
etoh
58
what are the 2 inhibitors of intermediary metabolism
1. sulfonamides 2. trimethroprim/sulfamethoxazole
59
resistance to sulfonamides is widespread and persistent in vivo in
meningococci gonococci b-hemolytic strep enteric gram-negative rods
60
what are the 2 mechanisms of acquired resistance to sulfonamides
1. increased production of PABA 2. altered DHPS
61
resistance to sulfonamides occurs in a __ fashion, not during \_\_
stepwise therapy
62
bacteria obtain DNA precursors from \_\_, which is why ___ is important
pus surgical drainage
63
organisms with no __ requirement are not susceptible to sulfonamides
folic acid
64
sulfonamides are synergistic w. \_\_\_
trimethoprim
65
sulfonamides are (cidal vs static)
cidal
66
is trimethoprim a sulfonamide
no!
67
trimethoprim is __ more potent than \_\_
5-20% sulfonamides
68
resistance to sulfonamides is via
altered DHFR
69
what is DHFR
dihydrofolate reductase
70
pyrimethamine inhibits __ DHFR which is \_\_
protozoal malaria
71
methotrexate inhibits ___ DHFR which is \_\_\_
mammalian neoplasms
72
the target of sulfonamides is
the enzyme that makes folic acid
73
trimethoprim targets
another step of folic acid formation
74
does TMP/SMX cover MRSA
yes
75
sulfonamides plus trimethoprim work well for what types of gram negative infxns
uncomplicated UTI → e. coli burn infxns → pseudomonas
76
sulfonamides are ___ that are well absorbed from the \_\_\_
weak acids GI tract
77
sulfacetamide is
topical sulfonamide + trimethoprim
78
sulfacetamide is used for
conjunctivitis
79
sulfonanides should be taken
on an empty stomach
80
sulfonamides have good distribution in body water, including (4)
1. pleural 2. ocular 3. synovial fluids 4. CSF
81
sulfonamides can cause displacement of \_\_\_ in \_\_\_, predisposing them to \_\_\_
bilirubin neonates kernicterus
82
what can be a source of drug-drug interactions with sulfonamides
displacement of protein-bound drugs
83
sulfonamides are not used in what pt population
neonates pregnant women
84
the major metabolic pathway for sulfonaides is \_\_, which may be toxic dt \_\_\_
n-acetylation low solubility in urine
85
do sulfonanides require renal dosing
yes
86
sulfonamides should be taken with
lots of fluids
87
sulfonamides are the worst drug for what type of rxn
hypersensitivity rxns
88
what is a severe adverse rxn with sulfonamides
stevens-johnson

Ok Pharmacology... Let's Do This... Be Gentle (6 decks)

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