Tissue penetration of antimicrobials: Difference between revisions

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*† if inflammation present
  
*† if inflammation present
   
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== Specific Tissues ==
⚫
==Prostate==
  
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  ⚫
===Prostate===
   
 
*Poorly penetrated by most antibiotics
  
*Poorly penetrated by most antibiotics
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*[[Piperacillin]], [[aztreonam]], [[imipenem]], and some [[aminoglycosides]] are likely useful
  
*[[Piperacillin]], [[aztreonam]], [[imipenem]], and some [[aminoglycosides]] are likely useful
   
−
==Bone==
 +
===Bone===
   
 
*Essentially all antibiotics achieve similar bone-to-serum levels, with the exception of oral β-lactams which nevertheless have no worse outcomes[[CiteRef::landersdorfer2009pe]]
  
*Essentially all antibiotics achieve similar bone-to-serum levels, with the exception of oral β-lactams which nevertheless have no worse outcomes[[CiteRef::landersdorfer2009pe]]
   
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=== Eye ===
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* Ocular compartments include anterior and posterior
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** Anterior includes aqeous humour, and is best accessed using topical medications
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** Posterior includes vitreous humour, retina, and choroid, and is best accessed using intravitreal or systemic medications
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* Penetration of systemic antimicrobials into retina and vitreous is poor (~0 to 2%), but is better with inflammation[[CiteRef::brockhaus2019re]]
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{| class="wikitable"
  +
!Class
  +
!Antimicrobial
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!Vitreal Penetration
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|-
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| rowspan="3" |penicillins
  +
|[[ampicillin]]
  +
|below MIC in non-inflamed rabbit eyes
  +
|-
  +
|[[amoxicillin]]
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|2% (below MIC) in non-inflamed rabbit eyes
  +
|-
  +
|[[piperacillin]]
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|undetectable in inflamed human eyes
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|-
  +
| rowspan="4" |cephalosporins
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|[[cefazolin]]
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|above MIC in inflamed rabbit eyes
  +
|-
  +
|[[ceftriaxone]]
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|4% in non-inflamed human eyes
  +
|-
  +
|[[ceftazidime]]
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|30% in inflamed rabbit eyes
  +
|-
  +
|[[cefipime]]
  +
|8% in non-inflamed human eyes
  +
|-
  +
| rowspan="2" |carbapenems
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|[[imipenem]]
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|8 to 10% in non-inflamed human eyes
  +
|-
  +
|[[meropenem]]
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|30% in non-inflamed human eyes
  +
|-
  +
|oxazolidinones
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|[[linezolid]]
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|30 to 80% in non-inflamed human eyes
  +
|-
  +
|
  +
|[[vancomycin]]
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|above MIC in inflamed rabbit eyes
  +
|-
  +
|
  +
|[[daptomycin]]
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|30% in inflamed human eyes
  +
|-
  +
| rowspan="2" |aminoglycosides
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|[[amikacin]]
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|below MIC in inflamed rabbit eyes
  +
|-
  +
|[[gentamicin]]
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|below MIC in inflamed rabbit eyes
  +
|-
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| rowspan="3" |fluoroquinolones
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|[[ciprofloxacin]]
  +
|below MIC in non-inflamed human eyes
  +
|-
  +
|[[levofloxacin]]
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|30% but below MIC in non-inflamed human eyes
  +
|-
  +
|[[moxifloxacin]]
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|10 to 40% and above MIC in non-inflamed human eyes
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|}
 
[[Category:Antimicrobials]]
  
[[Category:Antimicrobials]]

Revision as of 10:58, 6 March 2021

Summary

Class Antimicrobial Blood CNS Vitreous Urine Prostate Necrotic
Antibiotics: β-Lactams
Penicillins β-lactamase inhibitors –
ampicillin + –
piperacillin-tazobactam +†
Cephalosporins first-generation cephalosporins – –
second-generation cephalosporins –
third-generation cephalosporins +†
cefepime +
ceftazidime + +
Cephamycins cephamycins –
cefoxitin –
Carbapenems imipenem +
Antibiotics: Non-β-Lactams
Aminoglycosides –
Chloramphenicol chloramphenicol +
Fluoroquinolones –? + +
Fosfomycin fosfomycin +
Lincosamides clindamycin – +
Lipopeptides daptomycin + – +
Macrolides macrolides – +
Nitrofurans nitrofurantoin – – + – –
Nitroimidazoles metronidazole +
Rifamycins rifampin +
Sulfonamides trimethoprim-sulfamethoxazole +
Tetracyclines tetracyclines – +
doxycycline + +
Antivirals
acyclovir / valacyclovir +
ganciclovir +
foscarnet
Antifungals
Azoles fluconazole +
Echinocandins + –
Class Antimicrobial Blood CNS Urine Prostate Necrotic
  • † if inflammation present

Specific Tissues

Prostate

  • Poorly penetrated by most antibiotics
  • Penetration is higher with a high concentration gradient, high lipid solubility, low degree of ionization, high dissociation constant, low protein binding, and small molecular size
  • Fluoroquinolones are the mainstay of therapy, though there is increasing resistance
  • TMP-SMX often used, though conflicting data about its penetration into the prostate
  • Minocycline, doxycycline, and macrolides achieve high levels in the prostate but are rarely indicated for the causative organisms
  • Third-generation cephalosporins and carbapenems can be used
  • Piperacillin, aztreonam, imipenem, and some aminoglycosides are likely useful

Bone

  • Essentially all antibiotics achieve similar bone-to-serum levels, with the exception of oral β-lactams which nevertheless have no worse outcomes1

Eye

  • Ocular compartments include anterior and posterior
    • Anterior includes aqeous humour, and is best accessed using topical medications
    • Posterior includes vitreous humour, retina, and choroid, and is best accessed using intravitreal or systemic medications
  • Penetration of systemic antimicrobials into retina and vitreous is poor (~0 to 2%), but is better with inflammation2
Class Antimicrobial Vitreal Penetration
penicillins ampicillin below MIC in non-inflamed rabbit eyes
amoxicillin 2% (below MIC) in non-inflamed rabbit eyes
piperacillin undetectable in inflamed human eyes
cephalosporins cefazolin above MIC in inflamed rabbit eyes
ceftriaxone 4% in non-inflamed human eyes
ceftazidime 30% in inflamed rabbit eyes
cefipime 8% in non-inflamed human eyes
carbapenems imipenem 8 to 10% in non-inflamed human eyes
meropenem 30% in non-inflamed human eyes
oxazolidinones linezolid 30 to 80% in non-inflamed human eyes
vancomycin above MIC in inflamed rabbit eyes
daptomycin 30% in inflamed human eyes
aminoglycosides amikacin below MIC in inflamed rabbit eyes
gentamicin below MIC in inflamed rabbit eyes
fluoroquinolones ciprofloxacin below MIC in non-inflamed human eyes
levofloxacin 30% but below MIC in non-inflamed human eyes
moxifloxacin 10 to 40% and above MIC in non-inflamed human eyes

References

  1. ^  Cornelia B. Landersdorfer, Jürgen B. Bulitta, Martina Kinzig, Ulrike Holzgrabe, Fritz Sörgel. Penetration of Antibacterials into Bone. Clinical Pharmacokinetics. 2009;48(2):89-124. doi:10.2165/00003088-200948020-00002.
  2. ^  L. Brockhaus, D. Goldblum, L. Eggenschwiler, S. Zimmerli, C. Marzolini. Revisiting systemic treatment of bacterial endophthalmitis: a review of intravitreal penetration of systemic antibiotics. Clinical Microbiology and Infection. 2019;25(11):1364-1369. doi:10.1016/j.cmi.2019.01.017.

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