Ocular Tissue Distribution in Rabbit after Instillation of Bromfenac Sodium Ophthalmic Solution.

Isaka, Mitsuyoshi; Inada, Katsuhiro; Tsutsumi, Shuichiro; Fushimi, Megumi; Inaba, Atsuhiro; Karasawa, Yoshio; Esumi, Yoshio

doi:10.2133/dmpk.14.32

Cited by 8 publications

(12 citation statements)

References 2 publications

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“…For example, topical administration of 0.1% nepafenac inhibits the synthesis of PGs in the retina-choroid by 55% for 4 h. 48 Although, topical bromfenac has good ocular penetration and reaches a sufficient level in the retina and choroid, the inhibitory activity of bromfenac on either COX-1 or COX-2 was stronger than nepafenac or dicrofenac. 49,50 In our pilot study, we tested several different NSAIDs and found that topical bromfenac had a sufficient inhibitory effect on CNV in rat, as expected. Therefore, we chose bromfenac for the present study.…”

Section: Reduction Of Intraocular Vegf By Bromfenac Was Diminished Bysupporting

confidence: 57%

NSAIDs inhibit neovascularization of choroid through HO-1-dependent pathway

Yoshinaga

Arimura

Otsuka

et al. 2011

Laboratory Investigation

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Intraocular neovascularization is the leading cause of severe visual loss and anti-vascular endothelial growth factor (VEGF) therapy is currently performed for choroidal neovascularization (CNV). Despite its potent anti-angiogenic effect, there are concerns about its long-term safety. Non-steroidal anti-inflammatory drugs (NSAIDs) are common therapeutic agents used for treating inflammatory diseases, and their anti-stress effects are attracting attention now. We studied the effects of topical NSAIDs on CNV, focusing on anti-stress proteins. Cultured retinal pigment epithelium (RPE) cells were treated with NSAIDs: bromfenac, indomethacin, or vehicle control. Transcription factor NF-E2-related factor 2 (Nrf2) and its downstream anti-oxidant protein heme oxygenase (HO)-1 were assessed using western blot and immunohistochemistry. As a result, NSAIDs induced translocation of Nrf2 into the nucleus and the robust expression of HO-1 in a dose-and time-dependent manner. Flow cytometric analysis revealed that bromfenac inhibited H 2 O 2 -induced apoptosis in cultured RPE cells. Next, we studied the effects of topical bromfenac on laser-induced CNV model in rat. The expressions of Nrf2 and HO-1, infiltrations of ED-1-positive macrophages at CNV lesions and size were analyzed. VEGF in the ocular fluid of these rats was also measured using enzyme-linked immunosorbent assay. Rats administered an inhibitor of HO-1 stannic mesoporphyrin (SnMP) were also studied. The results showed that topical bromfenac led to translocation of Nrf2 and induction of HO-1 in CNV lesions and that the number of infiltrating macrophages at the CNV lesion decreased. The sizes of CNV lesions were significantly smaller in bromfenac-treated rats than control CNV, and the effects were diminished by SnMP. VEGF increased in the ocular fluid after laser treatment and was inhibited by bromfenac and SnMP canceling these effects. NSAIDs inhibit CNV through the novel anti-stress protein HO-1-dependent pathway, indicating its potential therapeutic value for various intraocular angiogenic diseases including CNV.

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Section: Reduction Of Intraocular Vegf By Bromfenac Was Diminished Bysupporting

confidence: 57%

NSAIDs inhibit neovascularization of choroid through HO-1-dependent pathway

Yoshinaga

Arimura

Otsuka

et al. 2011

Laboratory Investigation

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“…26,[38][39][40] Several groups have evaluated the ocular pharmacokinetics of bromfenac sodium ophthalmic solution in animal models. 9,10,19 The T max (2.0 h) of bromfenac in humans appears to be the same as 1.7 h in rabbits. 19 Though C max (78.7 Ϯ 68.1 ng/mL) in humans is lower than 86.5 ng/mL in rabbits, 19 this may simply be the result of species differences whose blink rate is greater in humans, and corneal and conjunctival surface area in rabbits are about twice the area as humans.…”

Section: Discussionmentioning

confidence: 86%

“…9,10,19 The T max (2.0 h) of bromfenac in humans appears to be the same as 1.7 h in rabbits. 19 Though C max (78.7 Ϯ 68.1 ng/mL) in humans is lower than 86.5 ng/mL in rabbits, 19 this may simply be the result of species differences whose blink rate is greater in humans, and corneal and conjunctival surface area in rabbits are about twice the area as humans. 42,43 Most recently, McNamara and colleagues replicated our study in albino rabbits.…”

Section: Discussionmentioning

confidence: 86%

“…The pharmacologic and chemical properties of bromfenac sodium ophthalmic solution suggests that it should be a potent inhibitor of ophthalmic inflammation 17,18 and penetrate ocular tissues efficiently. 9,10,19 Like all ophthalmic NSAIDs, bromfenac sodium acts primarily by blocking prostaglandin synthesis through the inhibition of the cyclo-oxygenase-2 (COX-2) enzyme. The chemical structure of bromfenac sodium is identical to amfenac, the active moiety of nepafenac, except for the addition of a bromine atom in the 4-position of the benzoyl ring.…”

Section: Introductionmentioning

confidence: 99%

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Ocular Pharmacokinetics of a Single Dose of Bromfenac Sodium Ophthalmic Solution 0.1% in Human Aqueous Humor

Miyake

Ogawa²,

Tajika³

et al. 2008

Journal of Ocular Pharmacology and Therapeutics

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Pharmacokinetic modeling, based upon samples collected over 240 min after a single dose of bromfenac sodium ophthalmic solution 0.1% suggests that aqueous-humor concentrations remain at clinically effective levels (above its IC(50) value for COX-2) for over 12 h. Based upon this rationale, these results supported clinical trials that demonstrated the efficacy of twice-daily dosing of bromfenac sodium ophthalmic solution 0.1% to manage patients with postoperative ocular pain and inflammation.

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“…After topical instillation of indomethacin 0.5%, 1.34 Ìg/ml of the agent was found in the rabbit aqueous humor [7]. After a single instillation of 14 C-bromfenac sodium, radioactivity levels in the iris and ciliary body reached their maximum at 30 min after administration in rabbits [8]. It is possible that corticosteroids and nonsteroidal anti-inflammatory drugs may enter the anterior chamber maximally within 1 h in rabbits.…”

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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Ocular Tissue Distribution in Rabbit after Instillation of Bromfenac Sodium Ophthalmic Solution.

Cited by 8 publications

References 2 publications

NSAIDs inhibit neovascularization of choroid through HO-1-dependent pathway

NSAIDs inhibit neovascularization of choroid through HO-1-dependent pathway

Ocular Pharmacokinetics of a Single Dose of Bromfenac Sodium Ophthalmic Solution 0.1% in Human Aqueous Humor

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

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