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Table 1 Pharmacokinetics of intravitreal antibiotics - recommended dosing and frequency of administration

From: Pharmacokinetics of intravitreal antibiotics in endophthalmitis

Serial number Drug Model Recommended dose (?g/0.1 ml) Route of clearance Half-life (t1/2) in vitreous Frequency of repeat injections (h) Susceptible microorganisms
Non-inflamed phakic eyes Inflamed eyes Aphakic vitrectomized eyes
1. Amikacin [16],[33]-[35] Human 400 Anterior NA NA NA 24 to 48 Aerobic GNBs, Pseudomonas aeruginosa
Rabbit 400 25.5 h <24 h 7 h 24 to 48
2. Ampicillin [36] Human 5,000 Posterior NA NA NA 48 GPC, enterobacteria, therapeutic option for infections caused by MDR pathogens
3. Amphotericin-B [37] Human 5 to 10 Posterior 8.9 days NA 1.8 h NA Yeasts, filamentous fungi (resistance reported for various species of Aspergillus)
Rabbit 10 4.7 days NA NA NA
4. Aztreonam [38] Rabbit 100 Posterior 7.5 h NA NA 12 Excellent activity against family Enterobacteriaceae; moderate activity against Pseudomonas
5. Carbenicillin [24] Rabbit 2,000 Anterior 5 h NA NA 15 to 24 Pseudomonas, therapeutic option for infections caused by MDR pathogens
Monkey 1,000 10 h NA NA NA
6. Cephazolin [24],[39] Human 2,250 Posterior 6.5 h 10.5 h NA 24 GPC, GPB, E. coli, Proteus, H. influenza
Rabbit 2,250 6.5 h 10.4 h 6 h NA
7. Ceftazidime [16],[40] Human 2,250 Both posterior and anterior NA NA NA 48 to 72 Aerobic GNBs, GPBs including Pseudomonas
Rabbit 2,250 13.8 h 10.1 h 4.7 h 72
8. Ceftriaxone [21],[29] Rabbit 2,000 Both posterior and anterior NA NA NA 48 to 72 Aerobic GNBs
9. Cefuroxime [21],[29] Human eyes 1,000 Posterior NA NA NA 48 to 72 GPC, GPB, GNC, GNB including Pseudomonas aeruginosa, penicillinase-producing N. gonorrhoeae, ampicillin-resistant H. influenzae
10. Ciprofloxacin [26],[28] Human 100 Both anterior and posterior 3.5 to 5.5 h NA 1.2 h 12 Broad-spectrum activity against aerobic Gram-positive and Gram-negative bacteria, Actinomyces, Nocardia spp.
Rabbit 100 2.2 h NA NA NA
11. Clarithromycin [41] Rabbit <1,000 Posterior 2 h NA NA NA GPC, GPB, Chlamydia, Toxoplasma gondii
12. Clindamycin [42] Human 1,000 Posterior 40 h NA NA 72 GPCs - staphylococci, pneumococci; GPBs - Bacillus; GNBs - Bacteroides, Fusobacterium; resistance - enterococci, Enterobacteriaceae, Clostridium, Toxoplasma gondii
13. Chloramphenicol [43] Human 2,000 Posterior NA NA NA 24 Gram-negative bacteria, Rickettsia, Borellia recurrentis; moderately active against Gram-positive bacteria and Mycobacterium tuberculosis
14. Daptomycin [44] Rabbit 200 Posterior 42 h NA NA Single dose Gram-positive organisms, MRSA, VRSA, pneumococci, enterococci
15. Dalfopristine/quinopristine [45] Rabbit 400 Posterior NA NA NA 48 Active against VRSA
16. Doxycycline [46] Rabbit 125 NA NA NA NA NA Broad-spectrum - Gram-positive and Gram-negative bacteria, Spirochaetes, Rickettsia, Chlamydiae, Mycoplasma, Actinomyces, Entamoeba histolytica, atypical mycobacteria
17. Fluconazole [47] Rabbit 200 Posterior 3.08 h NA NA NA Yeasts
18. Gentamicin [48],[49] Human 200 Anterior 40 to 60 h 20 to 40 h <40 h 72 to 96 Aerobic GNBs
Rabbit 40 to 70 32 h 19 h 12 h NA
19. Imipenem [50] Rabbit 50 to 100 Posterior NA NA NA NA MDR GPB, GNBs including Psedomonas aeruginosa, therapeutic option for infections caused by MDR pathogens
20. Linezolid [5],[51] Rabbit 400 NA 2 h NA NA NA Aerobic GPC including MRSA and vancomycin-resistant enterococci
21. Moxifloxacin [52] Rabbit 200 Both anterior and posterior 1.72 h Prolonged NA 12 Broad-spectrum activity against Gram-positive and Gram-negative organisms
22. Ofloxacin [27] Rabbit 200 to 500 Both anterior and posterior 5.6 h 9.7 h NA 24 Broad-spectrum activity against Gram-positive and Gram-negative organisms
23. Penicillin [11] Human 2 to 4,000 units Posterior NA NA NA 48 Broad-spectrum activity against Gram-positive organisms, Spirochaetes
24. Piperacillin/tazobactam [17]-[19] Human 225 Posterior NA NA NA NA Effective GNBs, Staphylococcus epidermidis and Pseudomonas aeruginosa; therapeutic option for infections caused by MDR pathogens
Rabbit <250 NA NA NA NA
25. Sulfamethoxazole/trimethoprim [52] Rabbit 1,600 trimethoprim Anterior NA NA NA NA Broad-spectrum antibacterial activity; Toxoplasma gondii
26. Tobramycin [53] Human 200 to 400 Anterior NA NA NA NA Aerobic Gram-negative organisms
Rabbit 750 NA NA NA 72 to 96
27. Trovafloxacin [54] Rabbit 25 Both anterior and posterior NA NA NA 24 to 48 Expanded spectrum against Gram-positive and Gram-negative bacteria
28. Vancomycin [25],[55]-[57] Human 1,000 Anterior 25.5 to 56 h 48 h 9.8 h 72 Active against GPCs - MRSA and MDR Staphylococcus epidermidis
Rabbit   25.1 h NA 8.9 h NA
29. Voriconazole [58] Human 50 to 200 Posterior 2.5 to 6.5 h NA NA NA Broad-spectrum activity against moulds and yeasts
Rabbit 25 2.5 h NA NA NA
30. Meropenem [73] Human   Posterior 2.6 h NA NA NA Pseudomonas, Bacteroides, Clostridia, Listeria, Enterobacteriaceae
Rabbit 0.5
  1. GPC, Gram-positive cocci; GPB, Gram-positive bacilli; GNB, Gram-negative bacilli, GNC, Gram-negative cocci; MDR, multidrug-resistant; MRSA, methicillin-resistant Staphylococcus aureus; VRSA, vancomycin-resistant Staphylococcus aureus; NA, not available.