Quinolones, Folic Acid antagonists and urinary antiseptics Flashcards

1
Q

Name the 6 Fluoroquinolones

A
ciprofloxacin
levofloxacin 
moxifloxacin 
nalidixic acid 
norfloxacin 
ofloxacin
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2
Q

What infection is fluoroquinolone closely tied to

A

CDAD

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3
Q

Fluoroquinolone antibiotics targets ______, primarily in gram-_____ bacteria and ______________ in gram_____ bacteria to inhibit DNA __________

A

DNA gyrase, negative, topoisomerase IV, positive, replication

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4
Q

Ingestion of fluoroquinolone with calcium or other divalent cations can ______ absorption

A

reduce

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5
Q

Fluoroquinolone should be taken on a full/empty stomach

A

empty

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6
Q

clearance of fluoroquinolone

A

renal

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7
Q

levels of fluoroquinolone are high in….

A

bones, urine, kidney, prostatic tissue and lungs

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8
Q

Moxifloxacin is mainly metabolised by

A

liver

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9
Q

Cipro is most active against gram-___ strains and ____________

A

neg, enteric coliform

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10
Q

Cipro is active against penicillin, cephalosporin and amino glycoside-resistant strains

A

yes

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11
Q

Cipro is highly active against _____ and is commonly used in ___________ patients

A

P. aeruginosa, cystic fibrosis

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12
Q

Cipro is used in what type of infections?

A

skin, bone, joint

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13
Q

Name 5 indications for cipro

A
cystic fibrosis 
travellers diarrhoea (e.coli) 
food poisoning (enterobacteriaceae and campylobacter jejune) 
typhoid fever (salmonella typhi) 
UTI
prostatitis
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14
Q

Is cipro the first line agent for simple UTI?

A

No

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15
Q

3rd gen fluoroquiinolones like levy and maxi have better coverage agains gram _____ organisms especially _________ and ________

A

positive, S.pneumoniae, atypical pathogens

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16
Q

3rd gen fluoroquinolone are useful against ________ infections

A

respiratory

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17
Q

common ADR of fluoroquinolone

A

nausea, vomiting, diarrhoea, phototoxicity

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18
Q

Serious ADR of fluoroquinolone

A

tendinitis or tondon rupture
prolong QTc interval (3rd gen) –> not in patients predisposed to arrhythmias or taking other medications cause QT
peripheral neuropathy

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19
Q

Fluoroquinolone in children?

A

no <18 yo

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20
Q

Fluoroquinolone in preggo and breastfeeding

A

no

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21
Q

Fluoroquinolone contraindication

A

myasthenia graves

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22
Q

co administration of a sulfonamide and trimethoprim introduces sequential blocks in the biosynthetic pathway for _______ –> synergistic effect –> bacteri____ effect

A

tetrahydrofolate, cidal

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23
Q

sulphonamides are competitive inhibitors of ___________

A

dihydropteroate synthase

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24
Q

Bacteriostasis induced by sulphonamides is counteracted by ____ competitively

A

PABA

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25
Q

Name the 2 intermediate acting sulfonamides

A

sulfamethoxazole

sulfadiazine

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26
Q

sulfonamides administration

A

oral (except sulfasalazine)

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27
Q

sulfonamides CSF?

A

yes even in the absence of inflammation

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28
Q

sulfonamides metabolism

A

acetylated and conjugated primarily in the liver. Acetylated product can precipitate at neutral or acidic pH and cause crystalluria –>damage kidneys

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29
Q

sulfonamides clinicsal indications

A

combined with trimethoprim for pneumocystis carinii
combined with pyrimethamine for drug resistant malaria
IBS
infected burns (topically)
resp infections (eg with Nocardia)

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30
Q

ADR of sulfonamides

A

Crystalluria
hypersensitivity with sulfa allergy
hematopoietic disturbances
kernicterus in newborns if mom takes in late preggo

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31
Q

sulfonamides preggo?

A

avoided in newborns and infants less than 2months of age and pregnant women at term

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32
Q

Trimethoprim is a potent inhibitor of __________

A

bacterial dihydrofolate reductase

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33
Q

Trimethoprim leads to a decreased availability of tetrahydrofolate cofactors required for ___, ______ and ______ synthesis

A

purine, pyrimidine and AA

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34
Q

Trimethoprim may be used alone in the treatment of __ and ________________

A

UTI and bacterial prostatitis

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35
Q

modes of resistance in Trimethoprim

A

resistance in gram nag bacteria
presence of altered dihydrofolate reductase –> lower affinity for trimethoprim
efflux pumps and decreased perm to the drug

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36
Q

Trimethoprim administration

A

oral

37
Q

Higher concentrations of Trimethoprim are achieved in the

A

vagina and prostate

38
Q

Trimethoprim CSF?

A

yes

39
Q

Trimethoprim Excretion

A

renal

40
Q

Trimethoprim ADR

A

folic acid deficiency

- megaloblastic anemia, leukopenia, granulocytopenia

41
Q

Trimethoprim preggo?

A

cat c

42
Q

how to manage folic acid deficiency with Trimethoprim

A

simultaneous administration folinic acid

43
Q

Trimethoprim is most often compounded with ____ producing the combination _________

A

sulfamethoxazole, cotrimoxazole

44
Q

cotrimoxazole inhibits 2 sequential steps in the ________

A

synthesis of tetrahydrofolic acid

45
Q

cotrimoxazole administration

A

oral (full cup of water)

IV for patients with severe pneumonia

46
Q

cotrimoxazole CSF?

A

yes

47
Q

cotrimoxazole clearance?

A

renal

48
Q

cotrimoxazole indications? 5 indications

A

URI, E.coli
resp infections caused by haemophilia sp, mortadella catarrhal is and Klebsiella pneumonia
Toxoplasmosis
MRSA and community acquired skin and soft tissue infections
pneumocystis pneumonia caused by pneumocystis jiroveci

49
Q

cotrimoxazole MRSA?

A

yes

50
Q

Trimethoprim MRSA?

A

no

51
Q

Name 3 ADR of cotrimoxazole

A
rashes 
photosensitivity 
GI 
haemolytic anemia inpatients with G6PD deficiency 
folic acid deficiency
52
Q

Nitrofurantoin MOA?

A

bacteria reduce the drug to an active intermediate that inhibits various enzymes and disrupt the synthesis of proteins, DNA, RNA and metabolic processes

53
Q

Nitrofurantoin active against many strains of….

A

E.coli and enterococci

54
Q

what species are resistant to Nitrofurantoin

A

proteus and pseudomonas and many species of enterobacter and Klebsiella

55
Q

Nitrofurantoin administration

A

oral

56
Q

Nitrofurantoin distribution

A

high urinary concentrations while limiting systemic exposure due to rapid clearance (good for UTIs)

57
Q

Name 4 Nitrofurantoin ADR

A

N/V
hypersensitivity
G6PD deficiency
elderly patients susceptible to pulmonary toxicity of nitrofurantoin
peripheral neuropathies for renal patients

58
Q

Nitrofurantoin contraindications

A

impaired Bernal function (CrCl < 40mL/min)
late preggo, labour and delivery
infants < 1m

59
Q

Polymyxins is active against most gram ___ bacteria

A

neg

60
Q

Types of polymyxins?

A

colistin and polymyxin B

61
Q

polymyxin B is administered as a prodrug

A

false

62
Q

Colistin is administered as an inactive prodrug

A

True

63
Q

polymyxins are bacteriostatic

A

false

64
Q

gram neg bacteria are more sensitive than gram positive bacteria to polymyxins

A

True

65
Q

Polymyxins are mostly used against gram ___ bacteria

A

neg

66
Q

polymyxins are not active against….

A
proteus spp.
legionella
campylobacter
vibrio cholera 
gram neg cocci
gram positive bacteria 
anaerobic
67
Q

2 clinical uses of polymyxins

A

inhaled CMS for pseudomonas resp infections
polymyxin B: acute infections due to MDR gram neg microbes with no alternatives
- UTI and blood stream infections due to P.aeruginosa

68
Q

Polymyxin B administration

A

IV

69
Q

CMS administration

A

inhalation or IV

70
Q

polymyxins ADR (name 3)

A

nephrotoxicity
neurotoxicity
aerosolised reactions (chest tightness, sore throat etc)

71
Q

Fosfomycin is bacteriostatic

A

False

72
Q

Fosfomycin has activity against gram positive only

A

False (pos and neg)

73
Q

Fosfomycin MOA

A

interferes with cell wall synthesis by inhibiting the initial step involving phosphoenolpyrivate synthesise

74
Q

Fosfomycin highly active against which gram positive pathogens?

A

S.aureus and enterococcus

75
Q

Fosfomycin highly active against which gram positive pathogens?

A

P. aeruginosa and Klesiella pneumoniae

76
Q

Fosfomycin mainly used in the treatment of ___

A

UTI

77
Q

Fosfomycin has synergistic effect with _____

A

betalactams

78
Q

Fosfomycin administration

A

Fosfomycin tromethamine: oral

best taken on empty stomach

79
Q

Fosfomycin CSF?

A

yes

80
Q

Fosfomycin enters breast milk?

A

yes

81
Q

Fosfomycin 3 ADRs?

A

GI
headache
vaginitis

82
Q

Fosfomycin clearance

A

renal

83
Q

Anti-protozoal agent (metronidazole) administration

A

completely and rapidly absorbed after oral administration

84
Q

metronidazole CSF?

A

yes

85
Q

metronidazole breast milk?

A

yes

86
Q

metronidazole metabolism?

A

hepatic

87
Q

metronidazole elimination?

A

renal

88
Q

Name 4 ADR of metronidazole

A

GI
metallic taste
oral moniliasis
CNS (seizures, optic anad peripheral neuropathy)

89
Q

metronidazole preggo?

A

cat b but avoid in 1st trimester