Tissue penetration of antimicrobials: Difference between revisions

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! colspan="7" |Antibiotics: Ξ²-Lactams
! colspan="7" |Antibiotics: Ξ²-Lactams
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| rowspan="3" |Penicillins
| rowspan="3" |[[Penicillins]]
|Ξ²-lactamase inhibitors
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| rowspan="5" |Cephalosporins
| rowspan="5" |[[Cephalosporins]]
|first-generation cephalosporins
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| rowspan="2" |Cephamycins
| rowspan="2" |[[Cephamycins]]
|[[cephamycins]]
|[[cephamycins]]
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|Carbapenems
|[[Carbapenems]]
|[[imipenem]]
|[[imipenem]]
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! colspan="7" |Antibiotics: Non-Ξ²-Lactams
! colspan="7" |Antibiotics: Non-Ξ²-Lactams
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|Aminoglycosides
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|Fosfomycin
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|[[fosfomycin]]
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|[[clindamycin]]
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|Macrolides
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|Nitroimidazoles
|[[Nitroimidazoles]]
|[[metronidazole]]
|[[metronidazole]]
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| rowspan="2" |Tetracyclines
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! colspan="7" |Antifungals
! colspan="7" |Antifungals
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|Azoles
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!Class
!Class

Revision as of 18:46, 16 September 2020

Summary

Class Antimicrobial Blood CNS Urine Prostate Necrotic
Antibiotics: Ξ²-Lactams
Penicillins Ξ²-lactamase inhibitors –
ampicillin + –
piperacillin-tazobactam +†
Cephalosporins first-generation cephalosporins – –
second-generation cephalosporins –
third-generation cephalosporins +†
cefepime +
ceftazidime + +
Cephamycins cephamycins –
cefoxitin –
Carbapenems imipenem +
Antibiotics: Non-Ξ²-Lactams
Aminoglycosides –
Chloramphenicol chloramphenicol +
Fluoroquinolones –? + +
Fosfomycin fosfomycin +
Lincosamides clindamycin – +
Macrolides macrolides – +
Nitrofurans nitrofurantoin – – + – –
Nitroimidazoles metronidazole +
Rifamycins rifampin +
Sulfonamides trimethoprim-sulfamethoxazole +
Tetracyclines tetracyclines – +
doxycycline + +
Antifungals
Azoles fluconazole +
Echinocandins + –
Class Antimicrobial Blood CNS Urine Prostate Necrotic
  • † if inflammation present

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

References

  1. ^  Cornelia B. Landersdorfer, JΓΌrgen B. Bulitta, Martina Kinzig, Ulrike Holzgrabe, Fritz SΓΆrgel. Penetration of Antibacterials into Bone. Clinical Pharmacokinetics. 2009;48(2):89-124. doi:10.2165/00003088-200948020-00002.
  2. 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.
  3. 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.
  4. a b c d e f g h  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.
  5. ^  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.
  6. ^  Luis F. LΓ³pez-CortΓ©s, R. Ruiz-Valderas, M. J. Lucero-MuΓ±oz, 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.