Update and critical appraisal of the use of topical azithromycin ophthalmic 1% (AzaSite®) solution in the treatment of ocular infections

Clinical Ophthalmology

Volumn 5, Issue 1, 2011, Pages 801-809

  Utine, Canan Asli ^a,b  

^a YEDITEPE UNIVERSITY   (Turkey)

^b JOHNS HOPKINS UNIVERSITY   (United States)

Author keywords

AzaSite; Azithromycin; Durasite

Indexed keywords

AZASITE XTRA; AZITHROMYCIN; AZYTER; DEXAMETHASONE; DOXYCYCLINE; MOXIFLOXACIN; PLACEBO; TOBRAMYCIN; UNCLASSIFIED DRUG;

ANTIINFLAMMATORY ACTIVITY; ANTIMICROBIAL ACTIVITY; AREA UNDER THE CURVE; ARRHYTHMOGENESIS; BEDTIME DOSAGE; BLEPHARITIS; BLURRED VISION; CHEMOSIS; CONJUNCTIVAL HYPEREMIA; CONJUNCTIVITIS; CONTACT DERMATITIS; CORNEA EROSION; DRUG BIOAVAILABILITY; DRUG BLOOD LEVEL; DRUG DISTRIBUTION; DRUG DOSAGE FORM COMPARISON; DRUG ELIMINATION; DRUG HALF LIFE; DRUG SAFETY; DRUG STRUCTURE; DRUG TOLERABILITY; DRY EYE; DYSGEUSIA; EYE BURNING; EYE DISCHARGE; EYE INFECTION; EYE IRRITATION; HUMAN; MAXIMUM PLASMA CONCENTRATION; NONHUMAN; NOSE CONGESTION; OCULAR PRURITUS; PEER REVIEW; PUNCTATE KERATITIS; QT PROLONGATION; REVIEW; SCIENTIFIC LITERATURE; SEBACEOUS GLAND DISEASE; SIDE EFFECT; SINUSITIS; TRACHOMA;

EID: 79959819436     PISSN: 11775467     EISSN: 11775483     Source Type: Journal    
DOI: 10.2147/OPTH.S13785     Document Type: Review

References (59)

1. Amsden GW. Advanced-generation macrolides: tissue directed antibiotics. Int J Antimicrob Agents. 2001;18(Suppl 1):S11-S15.
2. Akpek EK, Vittitow J, Verhoeven RS, et al. Ocular surface distribution and pharmacokinetics of a novel ophthalmic 1% azithromycin formulation. J Ocul Pharmacol Ther. 2009;25(5):433-439.
3. Abelson MB, Heller W, Shapiro AM, et al. Clinical cure of bacterial conjunctivitis with azithromycin 1%: vehicle-controlled, doublemasked clinical trial. Am J Ophthalmol. 2008;145(6):959-965.
4. Retsema J, Girard A, Schelkly W, et al. Spectrum and mode of action of azithromycin (CP-62,993), a new 15-membered-ring-macrolide with improved potency against gram-negative organisms. Antimicrob Agents Chemother. 1987;31(12):1939-1947.
5. West SK. Azithromycin for control of trachoma. Community Eye Health. 1999;12(32):55-56.
6. Ianaro A, Ialenti A, Maffia P, et al. Anti-inflammatory activity of macrolide antibiotics. J Pharmacol Exp Ther. 2000;292(1):156-163.
7. Piacentini GL, Peroni DG, Bodini A, et al. Azithromycin reduces bronchial hyperresponsiveness and neutrophilic airway inflammation in asthmatic children: a preliminary report. Allergy Asthma Proc. 2007;28(2):194-198.
8. Howe RA, Spencer RC. Macrolides for the treatment of Pseudomonas aeruginosa infections? J Antimicrob Chemother. 1997;40(2):153-155.
9. Hoffmann N, Lee B, Hentzer M, et al. Azithromycin blocks quorum sensing and alginate polymer formation and increases the sensitivity to serum and stationary-growth-phase killing of Pseudomonas aeruginosa and attenuates chronic P. aeruginosa lung infection in Cftr(-/-) mice. Antimicrob Agents Chemother. 2007;51(10):3677-3687.
10. Amsden GW. Anti-inflammatory effects of macrolides - an underappreciated benefit in the treatment of community-acquired respiratory tract infections and chronic inflammatory pulmonary conditions? J Antimicrob Chemother. 2005;55(1):10-21.
11. Jacot JL, Jacot TA, Sheppard JD, et al. Evaluation of MMP 2/9 modulation by AzaSite and DuraSite in human corneal epithelial cells and bovine corneal endothelial cells in vitro. Poster presented at The Association for Research in Vision and Ophthalmology (ARVO) 2008 Annual Meeting. 2008 Apr 28; Fort Lauderdale, FL, 49: abstract 1985.
12. Sadrai Z, Hajrasouliha AR, Chauhan S, Saban DR, Dastjerdi MH, Dana R. Effect of topical azithromycin on corneal innate immune response. Invest Ophthalmol Vis Sci. 2011;52(5):2525-2531.
13. Bowman L, Si E, Pang J, Archibad R, Friedlaender M. Development of a topical polymeric mucoadhesive ocular delivery system for azithromycin. J Ocul Pharmacol Ther. 2009;25(2):133-139.
14. Bowman LM, Si E, Pang J, Friedlaender M. Development of a commercial eye drop formulation of azithromycin. Poster presented at The Association for Research in Vision and Ophthalmology (ARVO) 2007 Annual Meeting. 2007 May 6-10; Fort Lauderdale, FL, 48: e-Abstract 772.
15. Abelson M, Protzko E, Shapiro A, Garces-Soldana A, Bowman L; 1% Azithromycin in DuraSite Clinical Study Group. A randomized trial assessing the clinical efficacy and microbial eradication of 1% azithromycin ophthalmic solution vs tobramycin in adult and pediatric subjects with bacterial conjunctivitis. Clin Ophthalmol. 2007:1(2);177-182.
16. Wu EC, Kowalski RP, Romanowski EG, Mah FS, Gordon YJ, Shanks RM. AzaSite® inhibits Staphylococcus aureus and coagulasenegative Staphylococcus biofilm formation in vitro. J Ocul Pharmacol Ther. 2010 Dec;26(6):557-562.
17. Harper DG, Chen CE, Friedlaender MH. Controlled comparison of two fluorometholone formulations in the antigen challenge model of allergic conjunctivitis. CLAO J. 1995;21(4):256-260.
18. Liu P, Allaudeen H, Chandra R, et al. Comparative pharmacokinetics of azithromycin in serum and white blood cells of healthy subjects receiving a single-dose extended-release regimen versus a 3-day immediate-release regimen. Antimicrob Agents Chemother. 2007;51(1):103-109.
19. Schentang JJ, Ballow CH. Tissue-directed pharmacokinetics. Am J Med 1991;91(3A):5S-11S.
20. Gladue RP, Snider ME. Intracellular accumulation of azithromycin by cultured human fi broblasts. Antimicrob Agents Chemother. 1999;34(6):1056-1060.
21. Gladue RP, Bright GM, Isaacson RE, Newborg MF. In vitro and in vivo uptake of azithromycin (CP-62,993) by phagocytic cells: possible mechanism of delivery and release at sites of infection. Antimicrob Agents Chemother. 1989;33(3):277-282.
22. Rapp RP. Pharmacokinetics and pharmacodynamics of intravenous and oral azithromycin: enhanced tissue activity and minimal drug interactions. Ann Pharmacother. 1998;32(7-8):785-793.
23. Karcioglu ZA, Ahmed WS, Raines D, El-Yazigi A. Pharmacokinetics of azithromycin rabbit lacrimal glands and conjunctiva. Ophthalmic Res. 1999;31(1):47-52.
24. O'Day DM, Head FS, Foulds G, Robinson RD, Williams TE, Ferraina RA. Ocular pharmacokinetics of orally administered azithromycin in rabbits. J Ocul Pharmacol. 1994;10(4):633-641.
25. Tabbara KF, Al-Kharashi SA, Al-Mansouri SM, et al. Ocular levels of azithromycin. Arch Ophthalmol. 1998;116(12):1625-1628.
26. Amar T, Caillaud T, Elena P. Ocular pharmacokinetic study following single and multiple azithromycin administrations in pigmented rabbits. Curr Eye Res. 2008;33(2):149-158.
27. Investigator's Brochure, Azithromycin Ophthalmic Solution 1%, ed 2.0, Inspire Pharmaceuticals, Inc, Raleigh, NC. November 12, 2009.
28. Stewart WC, Crean CS, Zink RC, Brubaker K, Haque R, Hwang DG. Pharmacokinetics of azithromycin and moxifloxacin in human conjunctiva and aqueous humor during and after the approved dosing regimens. Am J Ophthalmol. 2010;150:744-751.
29. Torkildsen G, O'Brien TP. Conjunctival tissue pharmacokinetic properties of topical azithromycin 1% and moxifloxacin 0.5% ophthalmic solutions: a single-dose, randomized, open-label, active-controlled trial in healthy adult volunteers. Clin Ther. 2008;30(11):2005-2014.
30. Si PC, Cheung PS, Bowman L, Hosseini K. Ocular pharmacokinetics of Azasite Xtra - 2% azithromycin formulated in a DuraSite delivery system. Curr Eye Res. 2009;34(6):485-491.
31. Amacher DE, Ellis JH, Joyce AJ, et al. Preclinical toxicology studies with azithromycin: genetic toxicology evaluation. Mutat Res. 1993;300:79-90.
32. Stadnicki SW, Kessedijan M, Stadler J, Tachibana M. Preclinical reproductive and teratology studies with azithromycin. Oyo Yakuri/ Pharmacometrics. 1996;51:85-95.
33. Granet D, Lichtenstein SJ, Onofney B, Katz JA. An assessment of the tolerability of moxifloxacin 0.5% compared to azithromycin 1.0% in DuraSite. Clin Ophthalmol. 2007;1(4):519-525.
34. Ohtani H, Taninaka C, Hanada E, et al. Comparative pharmacodynamic analysis of Q-T interval prolongation induced by the macrolides clarithromycin, roxithromycin, and azithromycin in rats. Antimicrob Agents Chemother. 2000;44(10):2630-2637.
35. Ness PJ, Mamalis N, Werner L, et al. An anterior chamber toxicity study evaluating Besivance, AzaSite, and Ciprofloxacin. Am J Ophthalmol. 2010;150(4):498-504.
36. Seal DV, Barrett SP, McGill JI. Aetiology and treatment of acute bacterial infection of the external eye. Br J Ophthalmol. 1982;66:357-360.
37. AzaSite [package insert]. Durham, NC: inspire Pharmaceuticals; 2008.
38. Abelson M, Heller W. Efficacy of azithromycin 1% eye drops vs vehicle as first line therapy for bacterial conjunctivitis. Unpublished study the Cochrane Register of Controlled Trials (CENTRAL). 2006;ID CN00634804.
39. Heller W, Abelson M, Group TAS. Safety and tolerabiltiy of azithromycin 1% eye drops as anti-infective therapy for bacterial conjunctivitis. Unpublished study for the Cochrane Register of Controlled Trials (CENTRAL). Study ID CN 00634521.
40. Protzko E, Bowman L, Abelson M, Shapiero A; Group TACS. Phase 3 safety comparisons for 1% azithromycin in polymeric mucoadhesive eye drops versus 0.3% tobramycin eye drops for bacterial conjunctivitis. Invest Ophthalmol Vis Sci. 2007;48(8):3425-3429.
41. Cochereau I, Meddeb-Ouertani A, Khairallah M, et al. 3-Day treatment with azithromycin 1.5% eye drops versus 7-day treatment with tobramycin 0.3% for purulent bacterial conjunctivitis: multicentre, randomised and controlled trial in adults and children. Br J Ophthalmol. 2007;91(4):465-469.
42. Bremond-Gignac D, Mariani-Kurkdjian P, Beresniak A, et al. Efficacy and safety of azithromycin 1.5% eye drops for purulent bacterial conjunctivitis in pediatric patients. Pediatr Infect Dis J. 2010;29(3):222-226.
43. Robert PY, Bourcier T, Meddeb-Ouertani A, et al. [Efficacy assessment of azithromycin 1.5% eye drops versus tobramycin 0.3% on clinical signs of purulent bacterial conjunctivitis]. J Fr Ophtalmol. 2010;33(4):241-248. French.
44. Seal DV, McGill JI, Jacobs P, Liakos GM, Goulding NJ. Microbial and immunological investigations of chronic non-ulcerative blepharitis and meibomianitis. Br J Ophthalmol. 1985;69(8):604-611.
45. Smith RE, Flowers CW. Chronic blepharitis: a review. CLAO J. 1995;21(3):200-207.
46. McDermott AM, Perez V, Huang AJ, et al. Pathways of corneal and ocular surface inflammation: a perspective from the cullen symposium. Ocul Surf. 2005;3(Suppl 4):S131-S138.
47. Luchs J. Azithromycin in DuraSite for the treatment of blepharitis. Clin Ophthalmol. 2010;4:681-688.
48. Foulks GN, Borchman D, Yappert M, Kim SH, McKay JW. Topical azithromycin therapy for meibomian gland dysfunction: clinical response and lipid alterations. Cornea. 2010;29(7):781-788.
49. Luchs J. Efficacy of topical azithromycin ophthalmic solution 1% in the treatment of posterior blepharitis. Adv Ther. 2008;25(9):858-870.
50. Trattler WB, Kuhn KL, Haque R, Zink RC, Sall KN, Luchs J. Topical azithromycin improves blepharitis signs and symptoms. Presented at: The American Society of Cataract and Refractive Surgery. 2009 Apr 3-8; San Francisco, CA.
51. Haque RM, Torkildsen GL, Brubaker K, et al. Multi-center, open-label study evaluating the efficacy of azithromycin ophthalmic solution 1% on the signs and symptoms of subjects with blepharitis. Cornea 2010;29(8):871-877.
52. Opitz DL, Tyler KF. Efficacy of azithromycin 1% ophthalmic solution for treatment of ocular surface disease from posterior blepharitis. Clin Exp Optom. 2011;94(2):200-206.
53. Torkildsen GL, Cockrum P, Meier E, Hammonds WM, Silverstein B, Silverstein S. Evaluation of clinical efficacy and safety of tobramycin/ dexamethasone ophthalmic suspension 0.3%/0.05% compared to azithromycin ophthalmic solution 1% in the treatment of moderate to severe acute blepharitis/blepharoconjunctivitis. Curr Med Res Opin. 2011;27(1):171-178.
54. Mariotti SP, Prüss A; World Health Organization. The safe strategy. Preventing trachoma. A guide for environmental sanitation and improved hygiene. WHO/PBD/GET/00.7/ Rev 1. 2001:1-36.
55. Resnikoff S, Pascolini D, Etya'ale D, et al. Global data on visual impairment in the year 2002. Bull World Health Organ. 2004;82: 844-851.
56. Tabbara KF, Abu-El-Asrar A, Al-Omar O, Choudhury AH, Al-Faisal Z. Single dose azithromycin in the treatment of trachoma. A randomized controlled study. Ophthalmology. 1996;103(5):842-846.
57. Cochereau I, Goldschmidt P, Goepogui A, et al. Efficacy and safety of short duration azithromycin eye drops versus azithromycin single oral dose for the treatment of trachoma in children: a randomised, controlled, doublemasked clinical trial. Br J Ophthalmol. 2007;91(5):667-672.
58. Amza A, Goldschmidt P, Einterz E, et al. Elimination of active trachoma after two topical mass treatments with azithromycin 1.5% eye drops. PLoS Negl Trop Dis. 2010;4(11):e895.
59. Huguet P, Bella L, Einterz EM, Goldschmidt P, Bensaid P. Mass treatment of trachoma with azithromycin 1.5% eye drops in the Republic of Cameroon: feasibility, tolerance and effectiveness. Br J Ophthalmol. 2010;94(2):157-160.