Tissue penetration of antimicrobials: Difference between revisions

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|[[piperacillin-tazobactam]]
  
|[[piperacillin-tazobactam]]
 
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|-
  
|-
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| rowspan="5" |[[Cephalosporins]]
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| rowspan="6" |[[Cephalosporins]]
 
|first-generation cephalosporins
  
|first-generation cephalosporins
 
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| style="text-align:center" | +†
  
| style="text-align:center" | +†
 
| style="text-align:center" |
  
| style="text-align:center" |
  +
|-
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|[[ceftriaxone]]
  +
|
  +
| +
  +
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  +
|
  +
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|
 
|-
  
|-
 
|[[cefepime]]
  
|[[cefepime]]
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==Specific Tissues==
  
==Specific Tissues==
   
  +
=== Central Nervous System ===
  +
  +
* Reviewed in [[CiteRef::nau2010pe]]
  +
  +
{| class="wikitable"
  +
!Class
  +
!Antimicrobial
  +
!CSF Penetration (AUC)
  +
!With Meningeal Inflammation
  +
|-
  +
! colspan="4" |Antibiotics
  +
|-
  +
| rowspan="5" |[[penicillins]]
  +
|overall
  +
|2%
  +
|2%
  +
|-
  +
|[[ampicillin]]
  +
|
  +
|
  +
|-
  +
|[[amoxicillin]]
  +
|
  +
|6%
  +
|-
  +
|[[cloxacillin]]
  +
|0.87%
  +
|
  +
|-
  +
|[[piperacillin]]
  +
|3%
  +
|32%
  +
|-
  +
| rowspan="3" |beta lactamase inhibitors
  +
|overall
  +
|7%
  +
|10%
  +
|-
  +
|[[clavulanate]]
  +
|4%
  +
|8%
  +
|-
  +
|[[tazobactam]]
  +
|11%
  +
|
  +
|-
  +
| rowspan="4" |[[cephalosporins]]
  +
|overall
  +
|0.7 to 10%
  +
|15%
  +
|-
  +
|[[cefotaxime]]
  +
|12%
  +
|4 to 17%
  +
|-
  +
|[[ceftriaxone]]
  +
|0.7%
  +
|
  +
|-
  +
|[[ceftazidime]]
  +
|0.6%
  +
|
  +
|-
  +
| rowspan="3" |[[carbapenems]]
  +
|overall
  +
|20%
  +
|30%
  +
|-
  +
|imipenem
  +
|
  +
|14%
  +
|-
  +
|meropenem
  +
|5 to 25%
  +
|39%
  +
|-
  +
|[[aminoglycosides]]
  +
|overall
  +
|20%
  +
|
  +
|-
  +
| rowspan="4" |[[fluoroquinolones]]
  +
|overall
  +
|30 to 70%
  +
|70 to 90%
  +
|-
  +
|[[ciprofloxacin]]
  +
|24 to 43%
  +
|92%
  +
|-
  +
|[[levofloxacin]]
  +
|71%
  +
|
  +
|-
  +
|[[moxifloxacin]]
  +
|46%
  +
|79%
  +
|-
  +
|[[chloramphenicol]]
  +
|
  +
|60 to 70%
  +
|60 to 70%
  +
|-
  +
|[[macrolides]]
  +
|[[clarithromycin]]
  +
|
  +
|18%
  +
|-
  +
|[[tetracyclines]]
  +
|[[doxycycline]]
  +
|20%
  +
|20%
  +
|-
  +
|[[fosfomycin]]
  +
|
  +
|18%
  +
|
  +
|-
  +
|[[linezolid]]
  +
|90%
  +
|
  +
|
  +
|-
  +
|[[metronidazole]]
  +
|
  +
|
  +
|87%
  +
|-
  +
|[[rifamycins]]
  +
|[[rifampin]]
  +
|22%
  +
|
  +
|-
  +
|[[trimethoprim-sulfamethoxazole]]
  +
|[[trimethoprim]]
  +
|18%
  +
|42 to 51%
  +
|-
  +
|
  +
|[[sulfamethoxazole]]
  +
|12%
  +
|24 to 30%
  +
|-
  +
|[[glycopeptides]]
  +
|[[vancomycin]]
  +
|14 to 18%
  +
|30%
  +
|-
  +
|antituberculosis medications
  +
|[[isoniazid]]
  +
|
  +
|86%
  +
|-
  +
! colspan="4" |Antivirls
  +
|-
  +
| rowspan="2" |anti-herpes nucleoside analogues
  +
|[[acyclovir]]
  +
|31%
  +
|
  +
|-
  +
|[[valacyclovir]]
  +
|19%
  +
|
  +
|-
  +
|[[foscarnet]]
  +
|
  +
|27 to 43%
  +
|23 to 66%
  +
|-
  +
| rowspan="4" |HIV antiretrovirals
  +
|[[abacavir]]
  +
|35%
  +
|
  +
|-
  +
|[[zidovudine]]
  +
|75%
  +
|
  +
|-
  +
|[[indinavir]]
  +
|6 to 15%
  +
|
  +
|-
  +
|[[lopinavir]]
  +
|29%
  +
|
  +
|-
  +
! colspan="4" |Antifungals
  +
|-
  +
|
  +
|[[flucytosine]]
  +
|
  +
|74%
  +
|-
  +
| rowspan="2" |[[azoles]]
  +
|[[fluconazole]]
  +
|
  +
|86%
  +
|-
  +
|[[voriconazole]]
  +
|
  +
|46%
  +
|-
  +
|[[polyenes]]
  +
|[[amphotericin B]]
  +
|
  +
|low
  +
|-
  +
! colspan="4" |Antiparasitics
  +
|-
  +
|
  +
|[[albendazole]]
  +
|38 to 43%
  +
|
  +
|-
  +
|
  +
|[[praziquantel]]
  +
|24%
  +
|
  +
|-
  +
|
  +
|[[sulfadiazine]]
  +
|27 to 33%
  +
|
  +
|}
 
===Prostate===
  
===Prostate===
   

Revision as of 10:21, 8 November 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 ± +†
ceftriaxone +
cefepime +
ceftazidime + ± +
Cephamycins cephamycins –
cefoxitin –
Carbapenems imipenem +
meropenem + + +
Antibiotics: Non-β-Lactams
Aminoglycosides –
Chloramphenicol chloramphenicol +
Fluoroquinolones –? + +
Fosfomycin fosfomycin +
Lincosamides clindamycin – +
Lipopeptides daptomycin + – +
Macrolides macrolides – +
Nitrofurans nitrofurantoin – – – + – –
Nitroimidazoles metronidazole +
Oxazolidinones linezolid + + + ±‡
Rifamycins rifampin +
Sulfonamides trimethoprim-sulfamethoxazole +
Tetracyclines tetracyclines – +
doxycycline – + +
Antivirals
acyclovir / valacyclovir +
ganciclovir +
foscarnet
Antifungals
Azoles fluconazole + +
Echinocandins + – –
Polyenes liposomal amphotericin B – ±†
Class Antimicrobial Blood CNS Vitreous Urine Prostate Necrotic
  • † if inflammation present
  • ‡ very low levels, but likely enough for Enterococcus

Specific Tissues

Central Nervous System

  • Reviewed in 1
Class Antimicrobial CSF Penetration (AUC) With Meningeal Inflammation
Antibiotics
penicillins overall 2% 2%
ampicillin
amoxicillin 6%
cloxacillin 0.87%
piperacillin 3% 32%
beta lactamase inhibitors overall 7% 10%
clavulanate 4% 8%
tazobactam 11%
cephalosporins overall 0.7 to 10% 15%
cefotaxime 12% 4 to 17%
ceftriaxone 0.7%
ceftazidime 0.6%
carbapenems overall 20% 30%
imipenem 14%
meropenem 5 to 25% 39%
aminoglycosides overall 20%
fluoroquinolones overall 30 to 70% 70 to 90%
ciprofloxacin 24 to 43% 92%
levofloxacin 71%
moxifloxacin 46% 79%
chloramphenicol 60 to 70% 60 to 70%
macrolides clarithromycin 18%
tetracyclines doxycycline 20% 20%
fosfomycin 18%
linezolid 90%
metronidazole 87%
rifamycins rifampin 22%
trimethoprim-sulfamethoxazole trimethoprim 18% 42 to 51%
sulfamethoxazole 12% 24 to 30%
glycopeptides vancomycin 14 to 18% 30%
antituberculosis medications isoniazid 86%
Antivirls
anti-herpes nucleoside analogues acyclovir 31%
valacyclovir 19%
foscarnet 27 to 43% 23 to 66%
HIV antiretrovirals abacavir 35%
zidovudine 75%
indinavir 6 to 15%
lopinavir 29%
Antifungals
flucytosine 74%
azoles fluconazole 86%
voriconazole 46%
polyenes amphotericin B low
Antiparasitics
albendazole 38 to 43%
praziquantel 24%
sulfadiazine 27 to 33%

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 outcomes2

Eye

Class Antimicrobial Retinal Penetration Vitreal Penetration Ref
Antibiotics
penicillins ampicillin below MIC in non-inflamed rabbit eyes 3
amoxicillin 2% (below MIC) in non-inflamed rabbit eyes 3
piperacillin undetectable in inflamed human eyes 3
cephalosporins cefazolin above MIC in inflamed rabbit eyes 3
ceftriaxone 4% in non-inflamed human eyes 3
ceftazidime 30% in inflamed rabbit eyes 3
cefipime 8% in non-inflamed human eyes 3
carbapenems imipenem 8 to 10% in non-inflamed human eyes 3
meropenem 30% in non-inflamed human eyes 3
oxazolidinones linezolid 30 to 80% in non-inflamed human eyes 3
vancomycin above MIC in inflamed rabbit eyes 3
daptomycin 30% in inflamed human eyes 3
aminoglycosides amikacin below MIC in inflamed rabbit eyes 3
gentamicin below MIC in inflamed rabbit eyes 3
fluoroquinolones ciprofloxacin below MIC in non-inflamed human eyes 3
levofloxacin 30% but below MIC in non-inflamed human eyes 3
moxifloxacin 10 to 40% and above MIC in non-inflamed human eyes 3
Antifungals
azoles fluconazole 40 to 50% 40 to 50% 45
itraconazole 10% in inflamed eyes 5
posaconazole 20% in inflamed eyes 5
voriconazole 40 to 100% 5
flucytosine 40 to 100% 5
polyenes liposomal amphotericin B only detectable in inflamed eyes 5
echinocandins echinocandins very low penetration 5
micafungin excellent undetectable 45
Antivirals
acyclovir above IC
valacyclovir 20 to 30%, above IC in non-inflamed human eyes 6
ganciclovir close to IC
foscarnet 100% 10%, close to IC 7

References

  1. ^ nau2010pe 
  2. ^  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.
  3. a b c d e f g h i j k l m n o p q r  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.
  4. a b  Takashi Suzuki, Toshihiko Uno, Guangming Chen, Yuichi Ohashi. Ocular distribution of intravenously administered micafungin in rabbits. Journal of Infection and Chemotherapy. 2008;14(3):204-207. doi:10.1007/s10156-008-0612-5.
  5. a b c d e f g h  T. Felton, P. F. Troke, W. W. Hope. Tissue Penetration of Antifungal Agents. Clinical Microbiology Reviews. 2014;27(1):68-88. doi:10.1128/cmr.00046-13.
  6. ^  Tony H. Huynh, Mark W. Johnson, Grant M. Comer, Douglas N. Fish. Vitreous Penetration of Orally Administered Valacyclovir. American Journal of Ophthalmology. 2008;145(4):682-686. doi:10.1016/j.ajo.2007.11.016.
  7. ^  Luis F. López-Cortés, R. Ruiz-Valderas, M. J. Lucero-Muñoz, E. Cordero, M. T. Pastor-Ramos, J. Marquez. Intravitreal, Retinal, and Central Nervous System Foscarnet Concentrations after Rapid Intravenous Administration to Rabbits. Antimicrobial Agents and Chemotherapy. 2000;44(3):756-759. doi:10.1128/aac.44.3.756-759.2000.

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