Difluprednate: clinical pharmacological analysis of experience and prospects of its application in eye disease pharmacotherapy
DOI: 10.32364/2311-7729-2025-25-1-6
E.V. Shikh, A.A. Makhova
I.M. Sechenov First Moscow State Medical University (Sechenov University), Moscow, Russian Federation
Difluprednate (DFP), a synthetic difluorinated prednisolone derivative, is the first corticosteroid approved by Food and Drug Administration for medical use to relieve postoperative pain and to treat inflammation in ophthalmology. As compared with other active substances of the class, its distinctive feature is unique ophthalmic bioavailability. DFP is a prodrug that is rapidly metabolized by deacetylation to 6(α), 9 -difluoroprednisolone acetate butyrate, a metabolite with a pronounced corticosteroid receptor agonist activity, in the eye tissues. Limited systemic absorption is a significant advantage of DFP. As a lipid emulsion, DFP ensures high efficiency combined with a lower dosage frequency and minimal side effects. The anti-inflammatory and anginal efficiency of DFP is comparable to that of dexamethasone. However, a longer half-life of dexamethasone is associated with a higher risk of side effects such as increased intraocular pressure and impaired corneal barrier function (especially, in case of prolonged use). As fluorometholone is less lipophilic than DFP, this leads to lower penetration through the cornea and a lower risk of increased intraocular pressure than in the latter case. The former has a shorter period of action, and more frequent dosage is required. Although DFP is dosed twice as often as prednisolone acetate (4 times a day vs. 8 times a day, respectively), the former and the latter have comparable efficiency and safety profiles.
Keywords: difluprednate, bioavailability, cataract surgery, inflammatory eye diseases, safety.
For citation: Shikh E.V., Makhova A.A. Difluprednate: clinical pharmacological analysis of experience and prospects of its application in eye disease pharmacotherapy. Russian Journal of Clinical Ophthalmology. 2025;25(1):42–48 (in Russ.). DOI: 10.32364/2311-7729-2025-25-1-6
About the authors:
Evgeniya V. Shikh — Dr. Sc. (Med.), Professor, Head of the Department of Clinical Pharmacology and Propaedeutics of Internal Diseases, N.V. Sklifosovskiy Institute of Clinical Medicine, I.M. Sechenov First Moscow State Medical University (Sechenov University); 8, building 2, Trubetskaya str., Moscow, 119991, Russian Federation; ORCID iD 0000-0001-6589-7654
Anna A. Makhova — Dr. Sc. (Med.), Professor, Department of Clinical Pharmacology and Propaedeutics of Internal Diseases, N.V. Sklifosovskiy Institute of Clinical Medicine, I.M. Sechenov First Moscow State Medical University (Sechenov University); 8, building 2, Trubetskaya str., Moscow, 119991, Russian Federation; ORCID iD 0000-0001-9817-9886
Contact information: Anna A. Makhova, e-mail: makhova_a_a@staff.sechenov.ru
Financial Disclosure: no authors have a financial or property interest in any material or method mentioned.
There is no conflict of interest.
Received 01.10.2024.
Revised 22.10.2024.
Accepted 18.11.2024
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