Penetration of Topically Administered Prednisolone Acetate Into the Human Aqueous Humor

Leibowitz, Howard M.; Berrospi, Amado R.; Kupferman, Allan; Restropo, Guillermo Velez; Galvis, Virgilio; Alvarez, Juan Arango

doi:10.1016/0002-9394(77)90740-1

Cited by 21 publications

(10 citation statements)

References 4 publications

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“…This conclusion seems also to be true for pilocarpine from a comparison of its penetration into human and rabbit eyes under similar conditions (KROHN 1978). On the other hand, the penetration of prednisolone acetate into the anterior chamber of the two species was not found to be significantly different by LEIBOWITZ et al (1977), but the epithelium is not an effective barrier to this substance.…”

Section: Epithelial Permeability Valuesmentioning

confidence: 45%

Ocular Pharmacokinetics

Maurice¹,

Mishima²

1984

Handbook of Experimental Pharmacology

224

169

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Section: Epithelial Permeability Valuesmentioning

confidence: 45%

Ocular Pharmacokinetics

Maurice¹,

Mishima²

1984

Handbook of Experimental Pharmacology

224

169

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“…The peak of prednisolone acetate concentration in the aqueous humor occurred 30-45 min after topical instillation in humans and rabbits [6]. After topical instillation of indomethacin 0.5%, 1.34 Ìg/ml of the agent was found in the rabbit aqueous humor [7].…”

Section: Discussionmentioning

confidence: 99%

Effects of Topical Corticosteroids and Nonsteroidal Anti-Inflammatory Drugs on Prostaglandin E<sub>2</sub>-Induced Aqueous Flare Elevation in Pigmented Rabbits

Hayasaka

Zhang

et al. 2003

Ophthalmic Res

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We evaluated the effects of anti-inflammatory potency of corticosteroids and nonsteroidal anti-inflammatory drugs on prostaglandin E₂ (PGE₂)-induced aqueous flare elevation in pigmented rabbits. Transcorneal diffusion of PGE₂, 25 µg/ml (7.09 × 10^–2 mmol/l), with the use of a glass cylinder was achieved to produce aqueous flare elevation. Anti-inflammatory drugs were topically administered once before PGE₂ application. Aqueous flare was measured with a laser flare-cell meter. Topical single instillation of dexamethasone sodium metasulfobenzoate 0.1%, dexamethasone sodium phosphate 0.1%, and fluorometholone 0.1% 6 h before PGE₂ application inhibited 56, 59, and 43% of flare elevation, respectively. Topical single instillation of bromfenac sodium 0.1% and pranoprofen 0.1% 1 h before PGE₂ application inhibited 33 and 15% of flare elevation, respectively. Indomethacin 0.5% did not inhibit flare elevation. Corticosteroid eyedrops needed several hours from topical instillation to exhibit inhibition of flare elevation. Most nonsteroidal anti-inflammatory drug eyedrops inhibited aqueous flare elevation when instilled 1 h before PGE₂ application.

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“…The peak ofprednisoloneacetateconcentrationoccurred30to45minutes after topical instillation in humans and rabbits. 15 Corticosteroids might need several hours after administration to show action by inhibitory effects on expression of the messenger RNA-encoding cyclooxygenase-related protein. 10 Diclofenac and pranoprofen instilled 1 and 0.5 hour before PGE 2 application inhibited flare elevation.…”

Section: Commentmentioning

confidence: 99%

Effects of Topical Anti-inflammatory and Antiallergic Eyedrops on Prostaglandin E2–Induced Aqueous Flare Elevation in Pigmented Rabbits

Hayasaka

Hayasaka²,

Zhang³

et al. 2002

Arch Ophthalmol

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To evaluate the role of topical instillation of anti-inflammatory or antiallergic agents on experimental elevation of aqueous flare induced by prostaglandin E 2 (PGE 2) in pigmented rabbits. Methods: Transcorneal diffusion of PGE 2 , 25 µg/mL (7.09ϫ10 −2 mmol/L), by means of a glass cylinder produced aqueous flare elevation. Anti-inflammatory or antiallergic agents were topically administered once or twice before PGE 2 application. Aqueous flare was measured with a laser flare-cell meter. Results are given as mean±SD. Results: Double instillations of 0.1% betamethasone sodium phosphate and 0.1% fluorometholone acetate at 4 and 2 hours before PGE 2 application inhibited 61%±11% and 46%±14%, respectively, of flare elevation. Double instillations of 0.1% diclofenac sodium and 0.1% pranoprofen at 4 and 2 hours before PGE 2 application did not inhibit flare elevation. Double instillations of 0.1% betamethasone, 0.1% fluorometholone, 0.1% diclofenac, and 0.1% pranoprofen at 1 and 0.5 hour before PGE 2 application inhibited 16% ± 10%, 16% ± 6%, 24% ± 9%, and 23%±10%, respectively, of flare elevation. Double instillations of 2% cromolyn sodium, 0.5% tranilast, 0.025% levocabastine hydrochloride, 0.1% pemirolast potassium, and 0.01% ibudilast at 1 and 0.5 hour before PGE 2 application did not inhibit flare elevation. Single instillation of 0.1% betamethasone 6 hours before PGE 2 application inhibited 88% of PGE 2-induced aqueous flare elevation. Single instillation of 0.1% diclofenac 1 hour before PGE 2 application inhibited 23% of PGE 2induced aqueous flare elevation.

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Penetration of Topically Administered Prednisolone Acetate Into the Human Aqueous Humor

Cited by 21 publications

References 4 publications

Ocular Pharmacokinetics

Ocular Pharmacokinetics

Effects of Topical Corticosteroids and Nonsteroidal Anti-Inflammatory Drugs on Prostaglandin E<sub>2</sub>-Induced Aqueous Flare Elevation in Pigmented Rabbits

Effects of Topical Anti-inflammatory and Antiallergic Eyedrops on Prostaglandin E2–Induced Aqueous Flare Elevation in Pigmented Rabbits

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