Summary: A synthetic glucocorticoid with anti-inflammatory properties.

Top Publications

  1. Bradshaw S, Shankar P, Maini R. Topical steroid and antibiotic combination therapy in red eye conditions. Br J Gen Pract. 2006;56:304 pubmed
  2. Wagner S, Apley M. Pharmacodynamics of isoflupredone acetate in an endotoxin-induced mastitis model. J Dairy Sci. 2003;86:792-8 pubmed
    ..When compared with untreated mastitic controls, cows treated with isoflupredone acetate did not exhibit statistically significant differences in milk production following endotoxin-induced mastitis. ..
  3. Picandet V, Leguillette R, Lavoie J. Comparison of efficacy and tolerability of isoflupredone and dexamethasone in the treatment of horses affected with recurrent airway obstruction ('heaves'). Equine Vet J. 2003;35:419-24 pubmed
    ..Even if clinical signs of hypokalaemia were not observed, this is a side effect that deserves further investigation. ..
  4. Cho H, Pillai P, Nicholson L, Sobrin L. Inflammatory Papillitis in Uveitis: Response to Treatment and Use of Optic Nerve Optical Coherence Tomography for Monitoring. Ocul Immunol Inflamm. 2016;24:194-206 pubmed publisher
    ..1 to 362.9 µm (p?=?0.01). Resolution of inflammatory papillitis can lag behind resolution of uveitis. SD-OCT assessment of papillitis is reproducible and correlates with presence vs. resolution of uveitis. ..
  5. Hewson J, Viel L, Caswell J, Shewen P, Buchanan Smith J. Impact of isoflupredone acetate treatment on clinical signs and weight gain in weanling heifers with experimentally induced Mannheimia haemolytica bronchopneumonia. Am J Vet Res. 2011;72:1613-21 pubmed publisher
    ..To characterize the impact of Mannheimia haemolytica infection on feed intake and weight gain in feedlot heifers and to evaluate the clinical efficacy of isoflupredone acetate administered in combination with oxytetracycline...
  6. Lauzurica R, Bonal J, Bonet J, Romero R, Teixido J, Serra A, et al. Rhabdomyolysis, oedema and arterial hypertension: different syndromes related to topical use of 9-alpha-fluoroprednisolone. J Hum Hypertens. 1988;2:183-6 pubmed
    ..Discontinuation of treatment and administration of potassium supplements produced a rapid recovery and all patients remain well six months later. ..
  7. Shulman D, Sargent J, Stewart R, Mester U. Comparative evaluation of the short-term bactericidal potential of a steroid-antibiotic combination versus steroid in the treatment of chronic bacterial blepharitis and conjunctivitis. Eur J Ophthalmol. 1996;6:361-7 pubmed
    ..However, in the long-term treatment of chronic blepharitis the well-known toxic problems of neomycin sulphate have to be taken into account. ..
  8. Liu D. A prospective randomized study of medications after silicone intubation. Ophthalmic Surg Lasers. 1996;27:434-7 pubmed
    ..Following silicone intubation, there appears to be no additional benefit of an antibiotic-steroid combination medication over an antibiotic alone. ..
  9. Nakano Goto S, Yamamoto T, Kirii E, Abe S, Yamashita H. Treatment of diffuse diabetic macular oedema using steroid eye drops. Acta Ophthalmol. 2012;90:628-32 pubmed publisher
    ..Eye drop therapy using difluprednate ophthalmic emulsion 0.05% is a useful and effective treatment modality without surgical intervention or severe side-effects. ..

More Information


  1. Martin M, Orgul S, Robertson A, Flammer J. [Traumatic lesion of the optic nerve head by flying fish: a case report]. Klin Monbl Augenheilkd. 2004;221:410-3 pubmed
    ..Severe traumatic lesions, even bone fractures induced by flying fish are not a seldom encounter in the Caribbean Sea. ..
  2. Ujiie H, Shimizu T, Shimizu H. Cutaneous reactions to imatinib mesylate treated by topical steroid. Am J Hematol. 2005;78:246 pubmed
  3. van Endt J, Veraart H, Kramer R, Janssen A, Sunder Raj P. A comparison of two ophthalmic steroid-antibiotic combinations after cataract surgery. Eur J Ophthalmol. 1997;7:144-8 pubmed
  4. Seifi H, LeBlanc S, Vernooy E, Leslie K, Duffield T. Effect of isoflupredone acetate with or without insulin on energy metabolism, reproduction, milk production, and health in dairy cows in early lactation. J Dairy Sci. 2007;90:4181-91 pubmed
    ..There were no treatment effects on test-day milk production, milk fat and protein percentages, or the intervals from calving to first insemination or pregnancy. ..
  5. Maresca M, Calconi G, Amici G, Teodori T, da Porto A. [Hypopotassemia and rhabdomyolysis. Description of 3 cases of different etiologies]. Minerva Med. 1988;79:55-60 pubmed
    ..The aetiology of each case is discussed with a description of the clinical course and laboratory tests and particular emphasis on variations in the renin-angiotensin-aldosterone system. ..
  6. Eustis H, Rhodes A. Suture contamination in strabismus surgery. J Pediatr Ophthalmol Strabismus. 2012;49:206-9 pubmed publisher
    ..Bacterial contamination of strabismus sutures is high (28%) and can be reduced significantly if sutures are soaked in antiseptic before use. ..
  7. Torboli P, Spagnolli W, Contu C, Ramponi C, Marzano A, Fedrizzi A, et al. [Arterial hypertension and hyporeninemic hypoaldosteronism. Description of a clinical case]. Minerva Med. 1991;82:147-50 pubmed
  8. Vanderijst J, Vandeleene B, De Plaen J, Kolanowski J. An unusual cause of factitious mineralocorticoid excess. Acta Clin Belg. 1992;47:408-13 pubmed
    ..This typical syndrome of apparent mineralocorticoid excess was secondary, in our patient, to prolonged administration of a mineralocorticoid-containing nasal spray. ..
  9. Cavina G, Valvo L, Gallinella B, Porra R, Savella A. The identification of related substances in 9 alpha-fluoroprednisolone-21 acetate by means of high-performance liquid chromatography with diode array detector and mass spectrometry. J Pharm Biomed Anal. 1992;10:437-46 pubmed
    ..The chromatographic, spectrophotometric and mass-spectrometric characteristics of the studied compounds are reported. ..
  10. Cho S, Park J, Zheng W, Abd El Aty A, Kim S, Choi J, et al. Quantification of bupivacaine hydrochloride and isoflupredone acetate residues in porcine muscle, beef, milk, egg, shrimp, flatfish, and eel using a simplified extraction method coupled with liquid chromatography-triple quadrupole tandem mass spectro. J Chromatogr B Analyt Technol Biomed Life Sci. 2017;1065-1066:29-34 pubmed publisher
    ..1% solution of acetic acid in acetonitrile and n-hexane followed by LC-MS/MS could effectively extract bupivacaine hydrochloride and isoflupredone acetate from porcine muscle, beef, milk, egg, shrimp, flatfish, and eel samples. ..
  11. Coffer N, Frank N, Elliott S, Young C, Van Amstel S. Effects of dexamethasone and isoflupredone acetate on plasma potassium concentrations and other biochemical measurements in dairy cows in early lactation. Am J Vet Res. 2006;67:1244-51 pubmed
    ..Both corticosteroids had glucocorticoid activity; however, only ISO had mineralocorticoid activity. Compared with saline solution, administration of 2 doses of ISO significantly increased the frequency of severe hypokalemia. ..
  12. Mulki L, Foster C. Difluprednate for inflammatory eye disorders. Drugs Today (Barc). 2011;47:327-33 pubmed publisher
    ..S. Furthermore, difluprednate proved to have a comparable safety profile. Here, we review difluprednate pharmacokinetics, ocular indications, animal studies, as well as the results of the clinical trials conducted to date in the U.S. ..
  13. Yamaguchi M, Yasueda S, Isowaki A, Yamamoto M, Kimura M, Inada K, et al. Formulation of an ophthalmic lipid emulsion containing an anti-inflammatory steroidal drug, difluprednate. Int J Pharm. 2005;301:121-8 pubmed
    ..Ophthalmic lipid emulsion enhances the intraocular penetration of drugs, and it is useful as a delivery system for the ophthalmic preparations of lipophilic drugs. ..
  14. Liu M, Hwang F, Dunn J, Stark W, Bower K. Hypopyon uveitis following LASIK in a patient with ulcerative colitis. J Refract Surg. 2012;28:589-91 pubmed publisher
    ..Early recognition and treatment can result in an excellent outcome. The exact relationship between hypopyon uveitis and LASIK is impossible to ascertain. ..
  15. Li J, Terry M, Goshe J, Shamie N, Davis Boozer D. Graft rejection after Descemet's stripping automated endothelial keratoplasty: graft survival and endothelial cell loss. Ophthalmology. 2012;119:90-4 pubmed publisher
    ..There is a trend toward a greater percentage of ECD loss with time in eyes experiencing graft rejection after DSAEK surgery. Proprietary or commercial disclosure may be found after the references. ..
  16. Donnenfeld E, Holland E, Solomon K, Fiore J, Gobbo A, Prince J, et al. A multicenter randomized controlled fellow eye trial of pulse-dosed difluprednate 0.05% versus prednisolone acetate 1% in cataract surgery. Am J Ophthalmol. 2011;152:609-617.e1 pubmed publisher
    ..Difluprednate was superior at protecting the cornea and reducing macular thickening after cataract surgery. ..
  17. Tajika T, Waki M, Tsuzuki M, Kida T, Sakaki H. Pharmacokinetic features of difluprednate ophthalmic emulsion in rabbits as determined by glucocorticoid receptor-binding bioassay. J Ocul Pharmacol Ther. 2011;27:29-34 pubmed publisher
    ..It is comparable, and possibly even superior, to the 0.1% BMP solution, and may be particularly useful in cases of severe disease where treatment with BMP solution alone is insufficient. ..
  18. Slabaugh M, Herlihy E, Ongchin S, Van Gelder R. Efficacy and potential complications of difluprednate use for pediatric uveitis. Am J Ophthalmol. 2012;153:932-8 pubmed publisher
    ..A high rate of steroid-induced IOP elevation and cataract formation is seen in this population. Close monitoring of pediatric patients receiving difluprednate is recommended. ..
  19. Tajika T, Takahashi H, Sakai Y, Fujii H, Isowaki A, Sakaki H. Metabolic profiles of difluprednate in rabbit ocular tissues after instillation of difluprednate ophthalmic emulsion. Xenobiotica. 2010;40:569-77 pubmed publisher
    ..The K(i) value of DF21C was 5.6 x 10(-7) mol/L, indicating very weak glucocorticoid receptor binding of DF21C (approximately 1000-fold less than that of DFBA and DFB). ..
  20. Sheppard J, Toyos M, Kempen J, Kaur P, Foster C. Difluprednate 0.05% versus prednisolone acetate 1% for endogenous anterior uveitis: a phase III, multicenter, randomized study. Invest Ophthalmol Vis Sci. 2014;55:2993-3002 pubmed publisher
    ..Difluprednate 0.05% four times daily is well tolerated and is noninferior to prednisolone acetate 1% eight times daily for the treatment of endogenous AU. (ClinicalTrials.gov number, NCT01201798.). ..
  21. Kawada K, Maeda N, Kobayashi S, Sowa J, Tsuruta D, Kawada N. Injection site with generalized rash caused by pegylated interferon alpha 2a injection. Dermatology. 2006;212:82-3 pubmed
  22. Ioannidis A, Rai P, Mulholland B. Conjunctival lymphoid hyperplasia presenting with bilateral panuveitis. Am J Ophthalmol. 2005;139:566-8 pubmed
    ..Furthermore, we advocate periodic follow-up examinations because of the small potential risk of developing ocular or systemic lymphoma in these patients. ..
  23. Yasueda S, Kimura M, Ohtori A, Kakehi K. Analysis of an anti-inflammatory steroidal drug, difluprednate, in aqueous humor by combination of semi-micro HPLC and column switching method. J Pharm Biomed Anal. 2003;30:1735-42 pubmed
    ..002% DFBA ophthalmic emulsion was not detected, but DFB was present at the concentration of 4.3+/-3.1 ng/ml. ..
  24. Foresti V, Parisio E, Ricci G. [Excess mineralocorticoid syndrome secondary to nasal sprays containing 9 alpha-fluoroprednisolone]. Minerva Med. 1987;78:1305-11 pubmed
    ..Since the factitious use of mineral corticoids is not taken into account, the need of an accurate collection of case history in the differential diagnosis of hyporeninemic hypoaldosteronism with hypokalemia is stressed. ..
  25. Korenfeld M, Silverstein S, Cooke D, Vogel R, Crockett R. Difluprednate ophthalmic emulsion 0.05% for postoperative inflammation and pain. J Cataract Refract Surg. 2009;35:26-34 pubmed publisher
    ..There were no serious ocular adverse events. Fewer adverse events were reported in the difluprednate-treated groups than in the placebo group. ..
  26. Foster C, Davanzo R, FLYNN T, McLeod K, Vogel R, Crockett R. Durezol (Difluprednate Ophthalmic Emulsion 0.05%) compared with Pred Forte 1% ophthalmic suspension in the treatment of endogenous anterior uveitis. J Ocul Pharmacol Ther. 2010;26:475-83 pubmed publisher
    ..Trial NCT00501579 was registered at the National Institutes of Health Registry in July 2007 ( http://clinicaltrials.gov/ct2/show/NCT00501579?term=sirion&rank=4 ). ..
  27. Knych H, Harrison L, White A, McKemie D. Disposition of isoflupredone acetate in plasma, urine and synovial fluid following intra-articular administration to exercised Thoroughbred horses. Drug Test Anal. 2016;8:141-7 pubmed publisher
    ..38 ± 5.21 and 2.38 ± 0.52 days, respectively. Results of this study provide information that can be used to regulate the use of intra-articular isoflupredone in the horse. ..
  28. Meehan K, Vollmer L, Sowka J. Intraocular pressure elevation from topical difluprednate use. Optometry. 2010;81:658-62 pubmed publisher
    ..However, clinicians need to be aware of the potential risk for significant and potentially rapid onset of IOP increase with this medication and manage patients accordingly. ..
  29. Tajika T, Isowaki A, Sakaki H. Ocular distribution of difluprednate ophthalmic emulsion 0.05% in rabbits. J Ocul Pharmacol Ther. 2011;27:43-9 pubmed publisher
    ..These results suggest that difluprednate delivered as a topical ophthalmic emulsion reached the anterior and posterior segments of the eye quickly and may be a potential treatment for ocular inflammation in these areas. ..
  30. Hernandez C, Lepoole C, Tessler H. Vogt-Koyanagi-Harada syndrome in a 6-year-old Hispanic boy. Pediatr Dermatol. 2012;29:191-4 pubmed publisher
    ..The patient was diagnosed with Vogt-Koyanagi-Harada syndrome (VKH). This article reviews the literature regarding the cutaneous presentation of VKH. ..
  31. Wagner S, Apley M. Effects of two anti-inflammatory drugs on physiologic variables and milk production in cows with endotoxin-induced mastitis. Am J Vet Res. 2004;65:64-8 pubmed
    ..Flunixin meglumine decreased rectal temperature, whereas isoflupredone did not; however, it has not been established that reduction of fever is beneficial to cows with naturally occurring mastitis. ..
  32. Marin F, Gonzalez Quintela A, Moya M, Suarez E, De Zarraga M. Pseudohyperaldosteronism due to application of an antihemorrhoid cream. Nephron. 1989;52:281-2 pubmed
    ..Two of the patients also exhibited slight arterial hypertension. This iatrogenic possibility must be ruled out in cases of hypermineralocorticoidism, thus avoiding unnecessary and costly examinations. ..
  33. Takahashi N, Aramaki Y, Tsuchiya S. Allergic rhinitis model with Brown Norway rat and evaluation of antiallergic drugs. J Pharmacobiodyn. 1990;13:414-20 pubmed
    ..The estimation of the released markers using allergic rhinitis brought about in BN rats was found to be a useful experimental system for evaluating the effect of drugs on allergic rhinitis. ..
  34. Wolf C, Maslchitzky E, Gregory R, Jobim M, Mattos R. Effect of corticotherapy on proteomics of endometrial fluid from mares susceptible to persistent postbreeding endometritis. Theriogenology. 2012;77:1351-9 pubmed publisher
    ..Short-term corticotherapy could be beneficial for treatment of uterine infectious processes in the mare. ..
  35. Kobayashi T, Yamasaki Y, Watanabe T, Onoda N. Extensive lichen amyloidosus refractory to DMSO. J Dermatol. 1995;22:755-8 pubmed
    ..The application of DMSO ointment had no clinical effect, and the amyloid deposits persisted in the histological specimens despite the treatment. The administration of a topical corticosteroid led to gradual clinical improvement. ..
  36. Kurz P, Chheda L, Kurz D. Effects of twice-daily topical difluprednate 0.05% emulsion in a child with pars planitis. Ocul Immunol Inflamm. 2011;19:84-5 pubmed publisher
    ..To report the effects of twice-daily difluprednate in a child with pars planitis (PP)...
  37. Lillich J, Bertone A, Schmall L, Ruggles A, Sams R. Plasma, urine, and synovial fluid disposition of methylprednisolone acetate and isoflupredone acetate after intra-articular administration in horses. Am J Vet Res. 1996;57:187-92 pubmed
    ..CONCLUSIONS--Both steroids appeared to be rapidly hydrolyzed to their respective ester forms, as detected by HPLC. The ELISA appeared to be a useful screening tool for detection of corticosteroids in this variety of body fluids. ..
  38. Gaines A, Carroll J, Allee G. Evaluation of exogenous glucocorticoid injection on preweaning growth performance of neonatal pigs under commercial conditions. J Anim Sci. 2004;82:1241-5 pubmed
    ..In contrast to our previous findings, Dex did not improve preweaning growth performance regardless of dose or supplemental milk. ..
  39. McLean H, Khalil M, Heiman A, Lee H. Novel fluorinated antiinflammatory steroid with reduced side effects: methyl 9 alpha-fluoroprednisolone-16-carboxylate. J Pharm Sci. 1994;83:476-80 pubmed
    ..This lack of adverse systemic effects is ostensibly due to the presence of the metabolically labile 16-carboxylate ester moiety. ..
  40. Reid A, Spence C, Coghlan J, Denton D, Whitworth J, Scoggins B. Steroid antagonism of the hypertensinogenic activity of adrenocortical steroids. J Steroid Biochem. 1987;27:977-83 pubmed
    ..These data support our concept of a "hypertensinogenic" class of steroid activity. ..
  41. Nakano S, Yamamoto T, Kirii E, Abe S, Yamashita H. Steroid eye drop treatment (difluprednate ophthalmic emulsion) is effective in reducing refractory diabetic macular edema. Graefes Arch Clin Exp Ophthalmol. 2010;248:805-10 pubmed publisher
    ..Instillation of difluprednate ophthalmic emulsion 0.05% is a safe and effective treatment that does not require surgical intervention and does not produce severe side-effects. ..
  42. Lohmann A, Van Best J, de Keizer R. Corneal metabolism and epithelial barrier function after cataract surgery and intraocular lens implantation: a fluorophotometric study. Int Ophthalmol. 1995;19:225-33 pubmed
    ..The interaction with the fellow eye indicates a consensual reaction which may attributed to damage to the neural system by the surgery. ..
  43. You Z, Heiman A, Hudson C, Lee H. Effect of chirality at C-20 of methyl 11beta,17alpha,20-trihydroxy-3-oxo-1,4-pregnadien-21-oate derivatives on antiinflammatory activity. Steroids. 2002;67:353-9 pubmed
    ..Metabolic inactivation during assessment of NO inhibition may play a role in the divergence noted between receptor affinity and the measured biologic activity resulting from the binding. ..