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. | 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. | 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. | 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. | Rabbit | 2,000 | Both posterior and anterior | NA | NA | NA | 48 to 72 | Aerobic GNBs | |
9. | 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. | 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. | 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. | 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. | 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. | Human | 1,000 | Anterior | 25.5 to 56 h | 48 h | 9.8 h | 72 | Active against GPCs - MRSA and MDR Staphylococcus epidermidis | |
Rabbit | Â | 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 | Â | Posterior | 2.6 h | NA | NA | NA | Pseudomonas, Bacteroides, Clostridia, Listeria, Enterobacteriaceae |
Rabbit | 0.5 |