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

Miyake, Kensaku; Ogawa, Takahiro; Tajika, Tetsuya; Gow, J.A.; McNamara, T.R.

doi:10.1089/jop.2007.0132

Cited by 22 publications

(19 citation statements)

References 16 publications

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“…Also, in the placebo group, 21.6% (37/171) of the subjects discontinued the test agent due to lack of efficacy compared with only 3.1% (11/356) in the bromfenac group ( P <0.0001) (Table 2). Similar results were seen in the bromfenac 0.09% once-daily study,33 where early discontinuations from treatment occurred less frequently in the bromfenac group compared with the placebo group. Of the subjects in the placebo group, 16.2% (45/278) discontinued the test agent due to the occurrence of an AE compared with only 5.2% (29/559) in the bromfenac group ( P <0.0001).…”

Section: Bromfenac Compliance and Adherencesupporting

confidence: 78%

Bromfenac ophthalmic solution for the treatment of postoperative ocular pain and inflammation: safety, efficacy, and patient adherence

Rajpal¹,

Ross²,

Rajpal³

et al. 2014

PPA

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Ophthalmic nonsteroidal anti-inflammatory drugs (NSAIDs) are commonly used by clinicians to manage ocular inflammation and pain following cataract surgery. Over the past decade, the US Food and Drug Administration has approved multiple topical NSAIDs for these purposes, including several reformulated products. One of these medications, bromfenac ophthalmic solution, has a long and extensive history, with proven efficacy and safety in patients following cataract surgery. The evolution of bromfenac ophthalmic solution over the years has involved either lowering the concentration of the active ingredient or extending the dosing interval to improve patient adherence/compliance. This review will focus on the history and progression of bromfenac ophthalmic solution and report the available patient preference and adherence data regarding this ocular NSAID throughout its evolution.

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Section: Bromfenac Compliance and Adherencesupporting

confidence: 78%

Bromfenac ophthalmic solution for the treatment of postoperative ocular pain and inflammation: safety, efficacy, and patient adherence

Rajpal¹,

Ross²,

Rajpal³

et al. 2014

PPA

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“…Although bromfenac has very good intraocular penetration into the aqueous humor in human [19], detailed pharmacokinetics for retinochoroidal tissue has not been determined. In rabbits, Baklayan et al have reported on the pharmacokinetic profiles of ocular tissues by using topical radiolabeled bromfenac [20], however, the relationship of the pharmacokinetics and efficacy in the target tissues has not been determined.…”

Section: Introductionmentioning

confidence: 99%

Pharmacokinetics and Efficacy of Topically Applied Nonsteroidal Anti-Inflammatory Drugs in Retinochoroidal Tissues in Rabbits

et al. 2014

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PurposeTo evaluate the pharmacokinetics and efficacy of topically applied nonsteroidal anti-inflammatory drugs (NSAIDs) in the retinochoroidal tissues of rabbits.MethodsThe cyclooxygenase (COX) inhibitory activity of diclofenac, bromfenac, and amfenac, an active metabolite of nepafenac, were determined using human-derived COX-1 and COX-2. Each of the three NSAIDs was applied topically to rabbits, and after 0.5 to 8 hrs, the concentration of each drug in the aqueous humor and the retinochoroidal tissues was measured by liquid chromatography-tandem mass spectrometry. The pharmacokinetics of the drugs in the tissues after repeated doses as is done on patients was calculated by a simulation software. The inhibitory effect of each NSAID on the breakdown of the blood-retinal barrier was assessed by the vitreous protein concentration on concanavalin A-induced retinochoroidal inflammation in rabbits.ResultsThe half-maximal inhibitory concentration (IC50) of diclofenac, bromfenac, and amfenac was 55.5, 5.56, and 15.3 nM for human COX-1, and 30.7, 7.45, and 20.4 nM for human COX-2, respectively. The three NSAIDs were detected in the aqueous humor and the retinochoroidal tissue at all-time points. Simulated pharmacokinetics showed that the levels of the three NSAIDs were continuously higher than the IC50 of COX-2, as an index of efficacy, in the aqueous humor, whereas only the bromfenac concentration was continuously higher than the IC50 at its trough level in the retinochoroidal tissues. The intravitreous concentration of proteins was significantly reduced in rabbits that received topical bromfenac (P = 0.026) but not the other two NSAIDs.ConclusionsTopical bromfenac can penetrate into the retinochoroidal tissues in high enough concentrations to inhibit COX-2 and exerts its inhibitory effect on the blood-retinal barrier breakdown in an experimental retinochoroidal inflammation in rabbits. Topical bromfenac may have a better therapeutic benefit than diclofenac and nepafenac for retinochoroidal inflammatory diseases.

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“…In oral form, bromfenac has been shown to have superior potency when compared with other NSAIDs, with no systemic side effects 30,31. In its topical form, bromfenac has been shown to have enhanced intraocular penetration and distribution in the cornea, iris, ciliary body, retina, and choroids, along with a longer duration of action that may last for up to 24 hours at these sites 8,23,32–34. Bromfenac has been cited as being more selective toward COX-2, with ketorolac being more selective towards COX-1 35–37.…”

Section: Discussionmentioning

confidence: 99%

Evaluation of analgesic efficacy of bromfenac sodium ophthalmic solution 0.09% versus ketorolac tromethamine ophthalmic solution 0.5% following LASEK or Epi-LASIK

Chynn¹,

Wong²,

Wang³

2011

OPTH

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BackgroundTo evaluate the analgesic efficacy of bromfenac sodium ophthalmic solution 0.09% compared with ketorolac tromethamine ophthalmic solution 0.5% in laser epithelial keratomileusis (LASEK) or epithelial keratomileusis (epi-LASEK), sometimes referred to as epi-LASIK.MethodsEighty eyes (from 40 patients, 18 men and 22 women) undergoing bilateral simultaneous LASEK or epi-LASEK were randomized to receive ketorolac in one eye and bromfenac in the other. Mean age was 33.13 ± 9.34 years. One drop of bromfenac or ketorolac was instilled in each eye 15 minutes and one minute prior to surgery, and two and four hours following surgery. Patients were instructed to instill the medications on-label each day through postoperative day 4. The subjects completed pain and visual blurriness assessments from day of surgery to postoperative day 4. Uncorrected visual acuity was tested on postoperative days 1 and 6.ResultsFor each of the five days, pain scores for bromfenac-treated eyes were significantly less than that for ketorolac-treated eyes (P < 0.01). Of the 40 patients, 32 (80%) said bromfenac provided better postoperative analgesia than ketorolac. There was no statistically significant difference in visual blurriness scores between the two groups (P > 0.1). Uncorrected visual acuity did not vary significantly between the treatment groups (P > 0.1). No serious adverse events were noted.ConclusionBromfenac is subjectively superior to ketorolac in reducing postoperative pain following LASEK or epi-LASEK. The subjects tolerated the drugs well with no serious adverse outcomes and no difference in uncorrected visual acuity.

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

Cited by 22 publications

References 16 publications

Bromfenac ophthalmic solution for the treatment of postoperative ocular pain and inflammation: safety, efficacy, and patient adherence

Bromfenac ophthalmic solution for the treatment of postoperative ocular pain and inflammation: safety, efficacy, and patient adherence

Pharmacokinetics and Efficacy of Topically Applied Nonsteroidal Anti-Inflammatory Drugs in Retinochoroidal Tissues in Rabbits

Evaluation of analgesic efficacy of bromfenac sodium ophthalmic solution 0.09% versus ketorolac tromethamine ophthalmic solution 0.5% following LASEK or Epi-LASIK

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