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Module 9 > Antimicrobial use in Lung Infection 2 > Flashcards

Antimicrobial use in Lung Infection 2 Flashcards

1
Q

what are examples of aminoglycosides

A

streptomycin

neomycin

kanamycin

gentamicin

tobramycon

amikacin

netilmicin

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2
Q

what is the shape of aminoglycosides

A

highly cationic polar molecule

highly ionized at physiological pH –> doesn’t distribute very well

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3
Q

how do streptomycin enter bacteria

A

oxygen dependent polyamine carrier to enter –> more efficient with B-lactams (like getimicin, work together –> B-lactams interfere with cell wall so aminoglycosides can get into the cell)

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4
Q

what is the mechanism of action of aminoglycosides

A
  1. bind to 30S subunit of bacterial ribosome
  2. use anticodones and codones that mismatch and cause them to bind in incorrect place
  3. protein will be truncated and non-functional
  4. cell won’t work
  5. destroys itself
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5
Q

list 6 pharmacokinetic features of aminoglycosides

A
  1. highly polar with low lipid solubility
  2. very poor absorption from GI tract –> give another route IM, SC
  3. therapeutic concentrations in joints and pleural and pericardial fluids
  4. don’t cross BBB or penetrate vitreous humour of eye or prostate
  5. not metabolized, excreted unchanged by kidney (glomerular filtration) (high accumulation in kidney cortex and can cause damage)
  6. selective binding to certain tissues esp kidney cortex (not used in patients with renal impairement)
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6
Q

what is ototoxicity of aminoglycosides

A

damage to vestibular apparatus cells –> disturbed balance, ataxia, vertigo, nysatgmus

cochlear: damages sensory cells of cochlea, causing deafness

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7
Q

what is the neprotoxicity of aminoglycosides

A

usually following prolonged therapy or persistent high plasma through concentrations

urine contains protein and tubular cast

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8
Q

what are examples of fluoroquinolones (6)

A

norfloxaxin

enrofloxacin (batril)

danofloxacin (advocin)

marbofloxacin (marbocyl, aurizon0

orbifoxacin (prosatex ear drops)

pradofloxacin (veraflox)

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9
Q

what are fluoroquinolones

A

fluorinated quinolones with mostly broad spectrum of activity

bactericidal

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10
Q

what is the mechanism of action of fluoroquinolones

A

rapid concentration-dependant killing (bactericidal)

enter bacteria through porins –> reduction in permeability of porins to quinolones may confer resistance

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11
Q

what is the spectrum of activity of fluoroquinolones

A

broad

highly active against gram - (aerobes)

gram positive (aerobes)

intracellular bacteria (chlamydia, legionella, brucella spp)

mycoplasma

relatively ineffective against obligate anaerobes

bactericidal

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12
Q

what is the metabolism of fluoroquinolones

A

some unchanged (ofloxacin)

some metabolized in liver (cipro-, enrofloxacin)

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13
Q

what is the excretion of fluoroquinolones

A

parent drug and metabolies excreted in urine, bile

renal excretion: glomerular filtration & tubular secretion –> high urinary conc of parent drug

in milk

enterohepatic recycling may occur

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14
Q

what is the half life of fluoroquinolines

A

half life varries with species and drug variations (3-14 h)

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15
Q

what is the clinical use of fluoroquinolines

A
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16
Q

what is the absorption and bioavailability of fluoroquinolones

A

highly orally bioavailable

rapid absorption (80-90%)

17
Q

what is the IM and SC absorption of fluoroquinolones

A

100%

18
Q

what is the distribution of fluroquinolones

A

low protein binding and extensive distribution

enters phagocytes

19
Q

what are the fluoroqiunolone concentrations in tissues

A

liver, kidney, urinary tract, lung, prostate, bone, skin

in fluids, interstitial, bronchial secretions, bile

most do not cross BBB

20
Q

what interferes with fluoroquinolone absorption

A

aluminium and magnesium antacids

21
Q

what indications would fluoroquinolones be the drug of first choice in dogs and cats (6)

A
  1. UTI with pseudomonas aeruginosa
  2. prostate infection in dogs
  3. skin, soft tissue and wound infection
  4. serious G-negative systemic infection
  5. serious resp infections
  6. osteomyelitis caused by G-negative aerobes
22
Q

what are the indications of fluoroquinolones in small mammals

A

rabbits, mice, rats and exocits for skin and visceral infection

do not cause GI disturbance as with beta-lactams or macrolides

23
Q

what are the indications of fluoroquinolones in birds

A

drinking water or injection

dose is higher than in mammals because of faster clearance rates

24
Q

what are the indications of fluoroquinolones in large mammals

A

good safety profile in adult horse but none currently licenced

cattle and sheep (marbofloxacin, enrofloxacin, danofloxacin) for BRD (excreted in milk)

pigs: marbofloxacin, enrofloxacin, danofloxacin

25
Q

what is the toxicity of fluoroquinolones

A

considered relatively safe

erosion of weight bearing cartilage –> dogs most susceptible, contraindicated in young growing cats and dogs

some CNS problems may occur and associated with CNS pathology (GABA)

ocular problems in cats (enrofloxacin)

26
Q

what is the spectrum of enrofloxacin

A

broad spectrum

wide variety of species including birds and reptiles

27
Q

what is the mechanism of enrofloxacin

A

rapid killing of bacteria

28
Q

what is the absorption and bioavailability

A

highly bioavailable

rapid absorption

29
Q

what are the tissue concentrations of enrofloxacin

A

tissue concentrations frequently exceed plasma concentrations

crosses placenta into aqueous humour and CSF

low plasma protein binding

30
Q

how is enrofloxacin excreted

A

renal

31
Q

what are the trade names of enrofloxacin

A

baytril

bayer

xeden

alstoe

32
Q

what is the activity of marbofloxacin

A

enterobacteriaciae, pasteurella

33
Q

what is the absorption of marbofloxacin and excretion

A

adequate plasma levels maintained for 24 hours after SC injection (40%) parent drug excreted (67% uring, feces 33%)

34
Q

what are the trade names of marbofloxacin

A

marbocyl, aurizon, vetoquinol

35
Q

what is marbofloxacin used for

A

resp infection in cattle and pig

Module 9 (43 decks)

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