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Published in: International Ophthalmology 5/2012

Open Access 01-10-2012 | Review

Loteprednol etabonate ophthalmic suspension 0.5 %: efficacy and safety for postoperative anti-inflammatory use

Authors: Michael Amon, Massimo Busin

Published in: International Ophthalmology | Issue 5/2012

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Abstract

Topical corticosteroids are routinely used as postoperative ocular anti-inflammatory drugs; however, adverse effects such as increased intraocular pressure (IOP) are observed with their use. While older corticosteroids such as dexamethasone and prednisolone acetate offer good anti-inflammatory efficacy, clinically significant increases in IOP (≥10 mmHg) are often associated with their use. Loteprednol etabonate, a novel C-20 ester-based corticosteroid, was retrometabolically designed to offer potent anti-inflammatory efficacy but with decreased impact on IOP. After exerting its therapeutic effects on the site of action, loteprednol etabonate is rapidly converted to inactive metabolites, resulting in fewer adverse effects. Randomized controlled studies have demonstrated the clinical efficacy and safety of loteprednol etabonate ophthalmic suspension 0.5 % for the treatment of postoperative inflammation in post-cataract patients with few patients, if any, exhibiting clinically significant increases (≥10 mmHg) in IOP. Furthermore, safety studies demonstrated a minimal effect of loteprednol etabonate on IOP with long-term use or in steroid responders with a much lower propensity to increase IOP relative to prednisolone acetate or dexamethasone. The anti-inflammatory treatment effect of loteprednol etabonate appears to be similar to that of rimexolone and difluprednate with less impact on IOP compared to difluprednate, although confirmatory comparative studies are needed. The available clinical data suggest that loteprednol etabonate is an efficacious and safe corticosteroid for the treatment of postoperative inflammation.
Literature
1.
go back to reference El-Harazi SM, Feldman RM (2001) Control of intra-ocular inflammation associated with cataract surgery. Curr Opin Ophthalmol 12:4–8PubMedCrossRef El-Harazi SM, Feldman RM (2001) Control of intra-ocular inflammation associated with cataract surgery. Curr Opin Ophthalmol 12:4–8PubMedCrossRef
2.
go back to reference The Loteprednol Etabonate Postoperative Inflammation Study Group 2 (1998) A double-masked, placebo-controlled evaluation of 0.5 % loteprednol etabonate in the treatment of postoperative inflammation. Ophthalmology 105:1780–1786CrossRef The Loteprednol Etabonate Postoperative Inflammation Study Group 2 (1998) A double-masked, placebo-controlled evaluation of 0.5 % loteprednol etabonate in the treatment of postoperative inflammation. Ophthalmology 105:1780–1786CrossRef
3.
go back to reference McColgin AZ, Heier JS (2000) Control of intraocular inflammation associated with cataract surgery. Curr Opin Ophthalmol 11:3–6PubMedCrossRef McColgin AZ, Heier JS (2000) Control of intraocular inflammation associated with cataract surgery. Curr Opin Ophthalmol 11:3–6PubMedCrossRef
4.
go back to reference Flach AJ (1998) The incidence, pathogenesis and treatment of cystoid macular edema following cataract surgery. Trans Am Ophthalmol Soc 96:557–634PubMed Flach AJ (1998) The incidence, pathogenesis and treatment of cystoid macular edema following cataract surgery. Trans Am Ophthalmol Soc 96:557–634PubMed
5.
go back to reference Guex-Crosier Y (1999) The pathogenesis and clinical presentation of macular edema in inflammatory diseases. Doc Ophthalmol 97:297–309PubMedCrossRef Guex-Crosier Y (1999) The pathogenesis and clinical presentation of macular edema in inflammatory diseases. Doc Ophthalmol 97:297–309PubMedCrossRef
6.
go back to reference Donnenfeld ED, Holland EJ, Solomon KD, Fiore J, Gobbo A, Prince J et al (2011) A multicenter randomized controlled fellow eye trial of pulse-dosed difluprednate 0.05 % versus prednisolone acetate 1 % in cataract surgery. Am J Ophthalmol 152(609–17):e1PubMed Donnenfeld ED, Holland EJ, Solomon KD, Fiore J, Gobbo A, Prince J et al (2011) A multicenter randomized controlled fellow eye trial of pulse-dosed difluprednate 0.05 % versus prednisolone acetate 1 % in cataract surgery. Am J Ophthalmol 152(609–17):e1PubMed
7.
go back to reference Assil KK, Massry G, Lehmann R, Fox K, Stewart R (1997) Control of ocular inflammation after cataract extraction with rimexolone 1 % ophthalmic suspension. J Cataract Refract Surg 23:750–757PubMed Assil KK, Massry G, Lehmann R, Fox K, Stewart R (1997) Control of ocular inflammation after cataract extraction with rimexolone 1 % ophthalmic suspension. J Cataract Refract Surg 23:750–757PubMed
8.
go back to reference Korenfeld MS, Silverstein SM, Cooke DL, Vogel R, Crockett RS (2009) Difluprednate ophthalmic emulsion 0.05 % for postoperative inflammation and pain. J Cataract Refract Surg 35:26–34PubMedCrossRef Korenfeld MS, Silverstein SM, Cooke DL, Vogel R, Crockett RS (2009) Difluprednate ophthalmic emulsion 0.05 % for postoperative inflammation and pain. J Cataract Refract Surg 35:26–34PubMedCrossRef
9.
go back to reference Henderson BA, Gayton JL, Chandler SP, Gow JA, Klier SM, McNamara TR (2011) Safety and efficacy of bromfenac ophthalmic solution (Bromday) dosed once daily for postoperative ocular inflammation and pain. Ophthalmology 118:2120–2127PubMedCrossRef Henderson BA, Gayton JL, Chandler SP, Gow JA, Klier SM, McNamara TR (2011) Safety and efficacy of bromfenac ophthalmic solution (Bromday) dosed once daily for postoperative ocular inflammation and pain. Ophthalmology 118:2120–2127PubMedCrossRef
11.
go back to reference Numaga J (2011) Phase II placebo-controlled study of nepafenac ophthalmic suspension 0.1 % for postoperative inflammation and ocular pain associated with cataract surgery in Japanese patients. J Ophthalmic Inflamm Infect 1:147–155PubMedCrossRef Numaga J (2011) Phase II placebo-controlled study of nepafenac ophthalmic suspension 0.1 % for postoperative inflammation and ocular pain associated with cataract surgery in Japanese patients. J Ophthalmic Inflamm Infect 1:147–155PubMedCrossRef
12.
go back to reference Kim SJ, Flach AJ, Jampol LM (2010) Nonsteroidal anti-inflammatory drugs in ophthalmology. Surv Ophthalmol 55:108–133PubMedCrossRef Kim SJ, Flach AJ, Jampol LM (2010) Nonsteroidal anti-inflammatory drugs in ophthalmology. Surv Ophthalmol 55:108–133PubMedCrossRef
13.
go back to reference Stewart R, Horwitz B, Howes J, Novack GD, Hart K (1998) Double-masked, placebo-controlled evaluation of loteprednol etabonate 0.5 % for postoperative inflammation. Loteprednol Etabonate Post-operative Inflammation Study Group 1. J Cataract Refract Surg 24:1480–1489PubMed Stewart R, Horwitz B, Howes J, Novack GD, Hart K (1998) Double-masked, placebo-controlled evaluation of loteprednol etabonate 0.5 % for postoperative inflammation. Loteprednol Etabonate Post-operative Inflammation Study Group 1. J Cataract Refract Surg 24:1480–1489PubMed
14.
go back to reference Pavesio CE, Decory HH (2008) Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol 92:455–459PubMedCrossRef Pavesio CE, Decory HH (2008) Treatment of ocular inflammatory conditions with loteprednol etabonate. Br J Ophthalmol 92:455–459PubMedCrossRef
15.
go back to reference Tripathi RC, Parapuram SK, Tripathi BJ, Zhong Y, Chalam KV (1999) Corticosteroids and glaucoma risk. Drugs Aging 15:439–450PubMedCrossRef Tripathi RC, Parapuram SK, Tripathi BJ, Zhong Y, Chalam KV (1999) Corticosteroids and glaucoma risk. Drugs Aging 15:439–450PubMedCrossRef
16.
go back to reference Doughty MJ (2001) Ophthalmic corticosteroids: management of the ocular inflammatory response. Ocular pharmacology & therapeutics. Butterworth-Heinemann, London, pp 92–102 Doughty MJ (2001) Ophthalmic corticosteroids: management of the ocular inflammatory response. Ocular pharmacology & therapeutics. Butterworth-Heinemann, London, pp 92–102
17.
go back to reference Ilyas H, Slonim CB, Braswell GR, Favetta JR, Schulman M (2004) Long-term safety of loteprednol etabonate 0.2 % in the treatment of seasonal and perennial allergic conjunctivitis. Eye Contact Lens 30:10–13PubMedCrossRef Ilyas H, Slonim CB, Braswell GR, Favetta JR, Schulman M (2004) Long-term safety of loteprednol etabonate 0.2 % in the treatment of seasonal and perennial allergic conjunctivitis. Eye Contact Lens 30:10–13PubMedCrossRef
18.
go back to reference Loteprednol Etabonate US Uveitis Study Group (1999) Controlled evaluation of loteprednol etabonate and prednisolone acetate in the treatment of acute anterior uveitis. Am J Ophthalmol 127:537–544CrossRef Loteprednol Etabonate US Uveitis Study Group (1999) Controlled evaluation of loteprednol etabonate and prednisolone acetate in the treatment of acute anterior uveitis. Am J Ophthalmol 127:537–544CrossRef
19.
go back to reference Yablonski ME, Burde RM, Kolker AE, Becker B (1978) Cataracts induced by topical dexamethasone in diabetics. Arch Ophthalmol 96:474–476PubMedCrossRef Yablonski ME, Burde RM, Kolker AE, Becker B (1978) Cataracts induced by topical dexamethasone in diabetics. Arch Ophthalmol 96:474–476PubMedCrossRef
20.
go back to reference McGhee CN, Dean S, Danesh-Meyer H (2002) Locally administered ocular corticosteroids: benefits and risks. Drug Saf 25:33–55PubMedCrossRef McGhee CN, Dean S, Danesh-Meyer H (2002) Locally administered ocular corticosteroids: benefits and risks. Drug Saf 25:33–55PubMedCrossRef
21.
go back to reference Clark AF (1995) Basic sciences in clinical glaucoma: steroids, ocular hypertension, and glaucoma. J Glaucoma 4:354–369PubMed Clark AF (1995) Basic sciences in clinical glaucoma: steroids, ocular hypertension, and glaucoma. J Glaucoma 4:354–369PubMed
22.
go back to reference Kersey JP, Broadway DC (2006) Corticosteroid-induced glaucoma: a review of the literature. Eye (Lond.) 20:407–416CrossRef Kersey JP, Broadway DC (2006) Corticosteroid-induced glaucoma: a review of the literature. Eye (Lond.) 20:407–416CrossRef
23.
go back to reference Jones R 3rd, Rhee DJ (2006) Corticosteroid-induced ocular hypertension and glaucoma: a brief review and update of the literature. Curr Opin Ophthalmol 17:163–167PubMed Jones R 3rd, Rhee DJ (2006) Corticosteroid-induced ocular hypertension and glaucoma: a brief review and update of the literature. Curr Opin Ophthalmol 17:163–167PubMed
24.
go back to reference Cantrill HL, Palmberg PF, Zink HA, Waltman SR, Podos SM, Becker B (1975) Comparison of in vitro potency of corticosteroids with ability to raise intraocular pressure. Am J Ophthalmol 79:1012–1017PubMed Cantrill HL, Palmberg PF, Zink HA, Waltman SR, Podos SM, Becker B (1975) Comparison of in vitro potency of corticosteroids with ability to raise intraocular pressure. Am J Ophthalmol 79:1012–1017PubMed
25.
go back to reference Macri A, Rosa R, Papadia M, Scotto R. Inflammation after modern cataract surgery: a comparison of different therapeutic regimen. Eur J Ophthalmol. doi:10.5301/EJO.2011.7589 Macri A, Rosa R, Papadia M, Scotto R. Inflammation after modern cataract surgery: a comparison of different therapeutic regimen. Eur J Ophthalmol. doi:10.​5301/​EJO.​2011.​7589
26.
go back to reference Bodor N (1993) Design of novel soft corticosteroids. Curr Probl Dermatol 21:11–19PubMed Bodor N (1993) Design of novel soft corticosteroids. Curr Probl Dermatol 21:11–19PubMed
27.
go back to reference Druzgala P, Hochhaus G, Bodor N (1991) Soft drugs—10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol 38:149–154PubMedCrossRef Druzgala P, Hochhaus G, Bodor N (1991) Soft drugs—10. Blanching activity and receptor binding affinity of a new type of glucocorticoid: loteprednol etabonate. J Steroid Biochem Mol Biol 38:149–154PubMedCrossRef
28.
go back to reference Alberth M, Wu WM, Winwood D, Bodor N (1991) Lipophilicity, solubility and permeability of loteprendnol etabonate: a novel, soft anti-inflammatory steroid. J Biopharm Sci 2:115–125 Alberth M, Wu WM, Winwood D, Bodor N (1991) Lipophilicity, solubility and permeability of loteprendnol etabonate: a novel, soft anti-inflammatory steroid. J Biopharm Sci 2:115–125
29.
go back to reference Comstock TL, Usner DW (2010) Effect of loteprednol etabonate ophthalmic suspension 0.5 % on post-operative pain and discomfort [E-abstract]. ASCRS symposium Comstock TL, Usner DW (2010) Effect of loteprednol etabonate ophthalmic suspension 0.5 % on post-operative pain and discomfort [E-abstract]. ASCRS symposium
30.
go back to reference Stewart RS (2004) Controlled evaluation of fluorometholone acetate and loteprednol etabonate in the treatment of postoperative inflammation following cataract surgery [abstract]. IOVS 45(Suppl 1):U159 Stewart RS (2004) Controlled evaluation of fluorometholone acetate and loteprednol etabonate in the treatment of postoperative inflammation following cataract surgery [abstract]. IOVS 45(Suppl 1):U159
31.
go back to reference Grigorian RA, Shah A, Guo A (2007) Comparison of loteprednol etabonate 0.5 % (Lotemax) to prednisolone acetate 1 % (Falcon) for inflammation treatment following cataract surgery [abstract]. IOVS Grigorian RA, Shah A, Guo A (2007) Comparison of loteprednol etabonate 0.5 % (Lotemax) to prednisolone acetate 1 % (Falcon) for inflammation treatment following cataract surgery [abstract]. IOVS
32.
go back to reference Çoban P, Kocak Altintas AG (2010) Comparison of the effect of loteprednol etabonate and prednisolone acetate on the intraocular pressure in uncomplicated phacoemulsification surgery [abstract]. Turk Klin J Ophthalmol 19:234–238 Çoban P, Kocak Altintas AG (2010) Comparison of the effect of loteprednol etabonate and prednisolone acetate on the intraocular pressure in uncomplicated phacoemulsification surgery [abstract]. Turk Klin J Ophthalmol 19:234–238
33.
go back to reference Howes J, Novack GD (1998) Failure to detect systemic levels, and effects of loteprednol etabonate and its metabolite, PJ-91, following chronic ocular administration. J Ocul Pharmacol Ther 14:153–158PubMedCrossRef Howes J, Novack GD (1998) Failure to detect systemic levels, and effects of loteprednol etabonate and its metabolite, PJ-91, following chronic ocular administration. J Ocul Pharmacol Ther 14:153–158PubMedCrossRef
34.
go back to reference Holland EJ, Bartlett JD, Paterno MR, Usner DW, Comstock TL (2008) Effects of loteprednol/tobramycin versus dexamethasone/tobramycin on intraocular pressure in healthy volunteers. Cornea 27:50–55PubMedCrossRef Holland EJ, Bartlett JD, Paterno MR, Usner DW, Comstock TL (2008) Effects of loteprednol/tobramycin versus dexamethasone/tobramycin on intraocular pressure in healthy volunteers. Cornea 27:50–55PubMedCrossRef
35.
go back to reference Novack GD, Howes J, Crockett RS, Sherwood MB (1998) Change in intraocular pressure during long-term use of loteprednol etabonate. J Glaucoma 7:266–269PubMed Novack GD, Howes J, Crockett RS, Sherwood MB (1998) Change in intraocular pressure during long-term use of loteprednol etabonate. J Glaucoma 7:266–269PubMed
36.
go back to reference Holland EJ, Djalilian AR, Sanderson JP (2009) Attenuation of ocular hypertension with the use of topical loteprednol etabonate 0.5 % in steroid responders after corneal transplantation. Cornea 28:1139–1143PubMedCrossRef Holland EJ, Djalilian AR, Sanderson JP (2009) Attenuation of ocular hypertension with the use of topical loteprednol etabonate 0.5 % in steroid responders after corneal transplantation. Cornea 28:1139–1143PubMedCrossRef
37.
go back to reference Bartlett JD, Horwitz B, Laibovitz R, Howes JF (1993) Intraocular pressure response to loteprednol etabonate in known steroid responders. J Ocul Pharmacol 9:157–165PubMedCrossRef Bartlett JD, Horwitz B, Laibovitz R, Howes JF (1993) Intraocular pressure response to loteprednol etabonate in known steroid responders. J Ocul Pharmacol 9:157–165PubMedCrossRef
38.
go back to reference Leibowitz HM, Bartlett JD, Rich R, McQuirter H, Stewart R, Assil K (1996) Intraocular pressure-raising potential of 1.0 % rimexolone in patients responding to corticosteroids. Arch Ophthalmol 114:933–937PubMedCrossRef Leibowitz HM, Bartlett JD, Rich R, McQuirter H, Stewart R, Assil K (1996) Intraocular pressure-raising potential of 1.0 % rimexolone in patients responding to corticosteroids. Arch Ophthalmol 114:933–937PubMedCrossRef
39.
go back to reference Bron A, Denis P, Hoang-Xuan TC, Boureau-Andrieux C, Crozafon P, Hachet E, Medhorn E, Akingbehin A (1998) The effects of rimexolone 1 % in postoperative inflammation after cataract extraction. A double-masked placebo-controlled study. Eur J Ophthalmol 8:16–21PubMed Bron A, Denis P, Hoang-Xuan TC, Boureau-Andrieux C, Crozafon P, Hachet E, Medhorn E, Akingbehin A (1998) The effects of rimexolone 1 % in postoperative inflammation after cataract extraction. A double-masked placebo-controlled study. Eur J Ophthalmol 8:16–21PubMed
40.
go back to reference Kavuncu S, Horoz H, Ardagil A, Erbil HH (2008) Rimexolone 1 % versus prednisolone acetate in preventing early postoperative inflammation after cataract surgery. Int Ophthalmol 28:281–285PubMedCrossRef Kavuncu S, Horoz H, Ardagil A, Erbil HH (2008) Rimexolone 1 % versus prednisolone acetate in preventing early postoperative inflammation after cataract surgery. Int Ophthalmol 28:281–285PubMedCrossRef
41.
go back to reference Yaylali V, Ozbay D, Tatlipinar S, Yildirim C, Ozden S (2004) Efficacy and safety of rimexolone 1 % versus prednisolone acetate 1 % in the control of postoperative inflammation following phacoemulsification cataract surgery. Int Ophthalmol 25:65–68PubMedCrossRef Yaylali V, Ozbay D, Tatlipinar S, Yildirim C, Ozden S (2004) Efficacy and safety of rimexolone 1 % versus prednisolone acetate 1 % in the control of postoperative inflammation following phacoemulsification cataract surgery. Int Ophthalmol 25:65–68PubMedCrossRef
42.
go back to reference Hirneiss C, Neubauer AS, Kampik A, Schonfeld CL (2005) Comparison of prednisolone 1 %, rimexolone 1 % and ketorolac tromethamine 0.5 % after cataract extraction: a prospective, randomized, double-masked study. Graefes Arch Clin Exp Ophthalmol 243:768–773PubMedCrossRef Hirneiss C, Neubauer AS, Kampik A, Schonfeld CL (2005) Comparison of prednisolone 1 %, rimexolone 1 % and ketorolac tromethamine 0.5 % after cataract extraction: a prospective, randomized, double-masked study. Graefes Arch Clin Exp Ophthalmol 243:768–773PubMedCrossRef
43.
go back to reference Donnenfeld ED (2011) Difluprednate for the prevention of ocular inflammation postsurgery: an update. Clin Ophthalmol 5:811–816PubMedCrossRef Donnenfeld ED (2011) Difluprednate for the prevention of ocular inflammation postsurgery: an update. Clin Ophthalmol 5:811–816PubMedCrossRef
44.
go back to reference Smith S, Lorenz D, Peace J, McLeod K, Crockett RS, Vogel R (2010) Difluprednate ophthalmic emulsion 0.05 % (Durezol) administered two times daily for managing ocular inflammation and pain following cataract surgery. Clin Ophthalmol 4:983–991PubMedCrossRef Smith S, Lorenz D, Peace J, McLeod K, Crockett RS, Vogel R (2010) Difluprednate ophthalmic emulsion 0.05 % (Durezol) administered two times daily for managing ocular inflammation and pain following cataract surgery. Clin Ophthalmol 4:983–991PubMedCrossRef
45.
go back to reference Cable MM (2010) Intraocular pressure spikes using difluprednate 0.05 % for postoperative cataract inflammation. ARVO (Meeting Abstracts) 2010(51):1981 Cable MM (2010) Intraocular pressure spikes using difluprednate 0.05 % for postoperative cataract inflammation. ARVO (Meeting Abstracts) 2010(51):1981
46.
go back to reference Spaeth GL, Monteiro de Barros DS, Fudemberg SJ (2009) Visual loss caused by corticosteroid-induced glaucoma: how to avoid it. Retina 29:1057–1061PubMedCrossRef Spaeth GL, Monteiro de Barros DS, Fudemberg SJ (2009) Visual loss caused by corticosteroid-induced glaucoma: how to avoid it. Retina 29:1057–1061PubMedCrossRef
Metadata
Title
Loteprednol etabonate ophthalmic suspension 0.5 %: efficacy and safety for postoperative anti-inflammatory use
Authors
Michael Amon
Massimo Busin
Publication date
01-10-2012
Publisher
Springer Netherlands
Published in
International Ophthalmology / Issue 5/2012
Print ISSN: 0165-5701
Electronic ISSN: 1573-2630
DOI
https://doi.org/10.1007/s10792-012-9589-2

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