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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.