Tissue penetration of antimicrobials: Difference between revisions

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!Blood
!Blood
!CNS
!CNS
!Vitreous
!Urine
!Urine
!Prostate
!Prostate
!Necrotic
!Necrotic
|-
|-
! colspan="7" |Antibiotics: β-Lactams
! colspan="8" |Antibiotics: β-Lactams
|-
|-
| rowspan="3" |[[Penicillins]]
| rowspan="3" |[[Penicillins]]
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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|[[piperacillin-tazobactam]]
|[[piperacillin-tazobactam]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +†
| style="text-align:center" | +†
| style="text-align:center" |
| style="text-align:center" |
|-
|-
| rowspan="5" |[[Cephalosporins]]
| rowspan="6" |[[Cephalosporins]]
|first-generation cephalosporins
|first-generation cephalosporins
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +†
| style="text-align:center" | +†
| style="text-align:center" |
| style="text-align:center" |
|-
|[[ceftriaxone]]
|
| +
|
|
|
|
|-
|-
|[[cefepime]]
|[[cefepime]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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|-
|-
|[[cefoxitin]]
|[[cefoxitin]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |–
| style="text-align:center" |–
|-
|-
|[[Carbapenems]]
| rowspan="2" |[[Carbapenems]]
|[[imipenem]]
|[[imipenem]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" | +
| style="text-align:center" | +
|-
|-
|[[meropenem]]
! colspan="7" |Antibiotics: Non-β-Lactams
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
|-
! colspan="8" |Antibiotics: Non-β-Lactams
|-
|-
|[[Aminoglycosides]]
|[[Aminoglycosides]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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|[[Chloramphenicol]]
|[[Chloramphenicol]]
|[[chloramphenicol]]
|[[chloramphenicol]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" | +
| style="text-align:center" | +
|-
|-
|[[Fluoroquinolones]]
| rowspan="2" |[[Fluoroquinolones]]
|all
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–?
| style="text-align:center" |–?
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
|-
|[[moxifloxacin]]
|
|
|
|–
|
|
|-
|-
|[[Fosfomycin]]
|[[Fosfomycin]]
|[[fosfomycin]]
|[[fosfomycin]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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|[[Lipopeptides]]
|[[Lipopeptides]]
|[[daptomycin]]
|[[daptomycin]]
| style="text-align:center" | +
| +
| style="text-align:center" |–
|–
| style="text-align:center" |
| +
| style="text-align:center" | +
|
| style="text-align:center" |
|
| style="text-align:center" |
|-
|-
|[[Macrolides]]
|[[Macrolides]]
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
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|[[Nitrofurans]]
|[[Nitrofurans]]
|[[nitrofurantoin]]
|[[nitrofurantoin]]
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |–
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|[[Nitroimidazoles]]
|[[Nitroimidazoles]]
|[[metronidazole]]
|[[metronidazole]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
|-
|[[Oxazolidinones]]
|[[linezolid]]
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |±‡
| style="text-align:center" |
| style="text-align:center" |
|-
|-
|[[Rifamycins]]
|[[Rifamycins]]
|[[rifampin]]
|[[rifampin]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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|[[Sulfonamides]]
|[[Sulfonamides]]
|[[trimethoprim-sulfamethoxazole]]
|[[trimethoprim-sulfamethoxazole]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
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| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |±[[CiteRef::jodlowski2020do]]
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
|-
|-
! colspan="7" |Antifungals
! colspan="8" |Antivirals
|-
|-
|
|[[Azoles]]
|[[acyclovir]] / [[valacyclovir]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
|-
|
|[[ganciclovir]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
|-
|
|[[foscarnet]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
|-
! colspan="8" |Antifungals[[CiteRef::felton2014ti]]
|-
| rowspan="3" |[[Azoles]]
|[[fluconazole]]
|[[fluconazole]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |±
| style="text-align:center" | +
|-
|[[itraconazole]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |±
| style="text-align:center" |–
| style="text-align:center" | +
| style="text-align:center" |–
| style="text-align:center" |
| style="text-align:center" |
|-
|[[voriconazole]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |±
| style="text-align:center" |±
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
|-
| rowspan="3" |[[Echinocandins]]
|[[anidulafungin]]
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |±
| style="text-align:center" |–
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
|-
|-
|[[Echinocandins]]
|[[caspofungin]]
| style="text-align:center" | +
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
|-
|[[micafungin]]
| style="text-align:center" |
| style="text-align:center" |±
| style="text-align:center" |–
| style="text-align:center" |±
| style="text-align:center" |
| style="text-align:center" |
|-
| rowspan="2" |[[Polyenes]]
|deoxycholate [[amphotericin B]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" | +
| style="text-align:center" | +
| style="text-align:center" |
| style="text-align:center" |
|-
|liposomal [[amphotericin B]]
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |–
| style="text-align:center" |–
| style="text-align:center" |±†
| style="text-align:center" | +
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
| style="text-align:center" |
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!Blood
!Blood
!CNS
!CNS
!Vitreous
!Urine
!Urine
!Prostate
!Prostate
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*† if inflammation present
*† if inflammation present
*‡ very low levels, but likely enough for [[Enterococcus]]


==Specific Tissues==
==Prostate==

=== 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===


*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]]


===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 inflammation[[CiteRef::brockhaus2019re]]
**Preferred agents for vitreal penetration include [[meropenem]], [[linezolid]], and [[moxifloxacin]]
**Agents that are likely effective, especially when inflammation is present, include [[vancomycin]], [[cefazolin]], [[ceftriaxone]], [[ceftazidime]], [[imipenem]], and [[trimethoprim-sulfamethoxazole]], and possible [[daptomycin]] and [[rifampin]]
**Agents that do not reach adequate levels include [[ciprofloxacin]], [[levofloxacin]], [[aminoglycosides]], [[aminopenicillins]], [[piperacillin]], [[cefepime]], and [[clarithromycin]]

{| class="wikitable"
!Class
!Antimicrobial
!Retinal Penetration
!Vitreal Penetration
!Ref
|-
! colspan="5" |Antibiotics
|-
| rowspan="3" |[[penicillins]]
|[[ampicillin]]
|
|below MIC in non-inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[amoxicillin]]
|
|2% (below MIC) in non-inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[piperacillin]]
|
|undetectable in inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
| rowspan="4" |[[cephalosporins]]
|[[cefazolin]]
|
|above MIC in inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[ceftriaxone]]
|
|4% in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[ceftazidime]]
|
|30% in inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[cefipime]]
|
|8% in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
| rowspan="2" |[[carbapenems]]
|[[imipenem]]
|
|8 to 10% in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[meropenem]]
|
|30% in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[oxazolidinones]]
|[[linezolid]]
|
|30 to 80% in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|
|[[vancomycin]]
|
|above MIC in inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|
|[[daptomycin]]
|
|30% in inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
| rowspan="2" |[[aminoglycosides]]
|[[amikacin]]
|
|below MIC in inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[gentamicin]]
|
|below MIC in inflamed rabbit eyes
|[[CiteRef::brockhaus2019re]]
|-
| rowspan="3" |[[fluoroquinolones]]
|[[ciprofloxacin]]
|
|below MIC in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[levofloxacin]]
|
|30% but below MIC in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
|[[moxifloxacin]]
|
|10 to 40% and above MIC in non-inflamed human eyes
|[[CiteRef::brockhaus2019re]]
|-
! colspan="5" |Antifungals
|-
| rowspan="4" |[[azoles]]
|[[fluconazole]]
|40 to 50%
|40 to 50%
|[[CiteRef::suzuki2008oc]][[CiteRef::felton2014ti]]
|-
|[[itraconazole]]
|
|10% in inflamed eyes
|[[CiteRef::felton2014ti]]
|-
|[[posaconazole]]
|
|20% in inflamed eyes
|[[CiteRef::felton2014ti]]
|-
|[[voriconazole]]
|
|40 to 100%
|[[CiteRef::felton2014ti]]
|-
|
|[[flucytosine]]
|
|40 to 100%
|[[CiteRef::felton2014ti]]
|-
|[[polyenes]]
|liposomal amphotericin B
|
|only detectable in inflamed eyes
|[[CiteRef::felton2014ti]]
|-
| rowspan="2" |[[echinocandins]]
|echinocandins
|
|very low penetration
|[[CiteRef::felton2014ti]]
|-
|[[micafungin]]
|excellent
|undetectable
|[[CiteRef::suzuki2008oc]][[CiteRef::felton2014ti]]
|-
! colspan="5" |Antivirals
|-
|
|[[acyclovir]]
|
|above IC
|
|-
|
|[[valacyclovir]]
|
|20 to 30%, above IC in non-inflamed human eyes
|[[CiteRef::huynh2008vi]]
|-
|
|[[ganciclovir]]
|
|close to IC
|
|-
|
|[[foscarnet]]
|100%
|10%, close to IC
|[[CiteRef::lópez-cortés2000in]]
|}
[[Category:Antimicrobials]]
[[Category:Antimicrobials]]

Latest revision as of 17:51, 19 September 2024

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 all –? + +
moxifloxacin –
Fosfomycin fosfomycin +
Lincosamides clindamycin – +
Lipopeptides daptomycin + – +
Macrolides macrolides – +
Nitrofurans nitrofurantoin – – – + – –
Nitroimidazoles metronidazole +
Oxazolidinones linezolid + + + ±‡
Rifamycins rifampin +
Sulfonamides trimethoprim-sulfamethoxazole +
Tetracyclines tetracyclines – +
doxycycline ±1 + +
Antivirals
acyclovir / valacyclovir +
ganciclovir +
foscarnet
Antifungals2
Azoles fluconazole + + + ± +
itraconazole ± – + –
voriconazole ± ± ±
Echinocandins anidulafungin + ± – ±
caspofungin + – – ±
micafungin ± – ±
Polyenes deoxycholate amphotericin B – +
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 3
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 outcomes4

Eye

Class Antimicrobial Retinal Penetration Vitreal Penetration Ref
Antibiotics
penicillins ampicillin below MIC in non-inflamed rabbit eyes 5
amoxicillin 2% (below MIC) in non-inflamed rabbit eyes 5
piperacillin undetectable in inflamed human eyes 5
cephalosporins cefazolin above MIC in inflamed rabbit eyes 5
ceftriaxone 4% in non-inflamed human eyes 5
ceftazidime 30% in inflamed rabbit eyes 5
cefipime 8% in non-inflamed human eyes 5
carbapenems imipenem 8 to 10% in non-inflamed human eyes 5
meropenem 30% in non-inflamed human eyes 5
oxazolidinones linezolid 30 to 80% in non-inflamed human eyes 5
vancomycin above MIC in inflamed rabbit eyes 5
daptomycin 30% in inflamed human eyes 5
aminoglycosides amikacin below MIC in inflamed rabbit eyes 5
gentamicin below MIC in inflamed rabbit eyes 5
fluoroquinolones ciprofloxacin below MIC in non-inflamed human eyes 5
levofloxacin 30% but below MIC in non-inflamed human eyes 5
moxifloxacin 10 to 40% and above MIC in non-inflamed human eyes 5
Antifungals
azoles fluconazole 40 to 50% 40 to 50% 62
itraconazole 10% in inflamed eyes 2
posaconazole 20% in inflamed eyes 2
voriconazole 40 to 100% 2
flucytosine 40 to 100% 2
polyenes liposomal amphotericin B only detectable in inflamed eyes 2
echinocandins echinocandins very low penetration 2
micafungin excellent undetectable 62
Antivirals
acyclovir above IC
valacyclovir 20 to 30%, above IC in non-inflamed human eyes 7
ganciclovir close to IC
foscarnet 100% 10%, close to IC 8

References

  1. ^  Tomasz Jodlowski, Charles R Ashby, Sarath G Nath. Doxycycline for ESBL-E Cystitis. Clinical Infectious Diseases. 2020. doi:10.1093/cid/ciaa1898.
  2. a b c d e f g h i  Timothy Felton, Peter F. Troke, William W. Hope. Tissue Penetration of Antifungal Agents. Clinical Microbiology Reviews. 2014;27(1):68-88. doi:10.1128/cmr.00046-13.
  3. ^ nau2010pe 
  4. ^  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.
  5. 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.
  6. 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.
  7. ^  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.
  8. ^  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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