Bromfenac sodium hydrate
(Synonyms: (2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠,Bromfenac monosodium salt sesquihydrate) 目录号 : GC35556Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively.
Cas No.:120638-55-3
Sample solution is provided at 25 µL, 10mM.
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Bromfenac sodium hydrate (Bromsite, Bromday, Prolensa, Xibrom), a brominated nonsteroidal anti-inflammatory drugs (NSAID) with strong in vitro anti-inflammatory potency, is a potent and orally active inhibitor of COX with IC50 of 5.56 nM and 7.45 nM for COX-1 and COX-2, respectively.
[1] Barry A Schechter. Clin Ophthalmol. 2019 Aug 1;13:1439-1460.
Cas No. | 120638-55-3 | SDF | |
别名 | (2-氨基-3-(4-溴苯甲酰)苯基)乙酸钠,Bromfenac monosodium salt sesquihydrate | ||
Canonical SMILES | [O-]C(CC1=CC=CC(C(C2=CC=C(Br)C=C2)=O)=C1N)=O.[Na+].[1.5H2O] | ||
分子式 | C15H12BrNO3 . 3/2 H2O . Na | 分子量 | 383.17 |
溶解度 | DMSO: ≥ 100 mg/mL (260.98 mM); Water: ≥ 100 mg/mL (260.98 mM) | 储存条件 | Store at -20°C |
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1 mg | 5 mg | 10 mg | |
1 mM | 2.6098 mL | 13.049 mL | 26.0981 mL |
5 mM | 0.522 mL | 2.6098 mL | 5.2196 mL |
10 mM | 0.261 mL | 1.3049 mL | 2.6098 mL |
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2.
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[The clinical efficacy of 0.1% Bromfenac sodium hydrate ophthalmic solution after excimer laser in situ keratomileusis]
Zhonghua Yan Ke Za Zhi 2013 Apr;49(4):320-6.PMID:23900091doi
Objective: To investigate the clinical efficacy and safety of 0.1% Bromfenac sodium hydrate ophthalmic solution in myopia and astigmatism eyes after sub-Bowman keratomileusis (SBK) METHODS: A case control study. Number of patients with low to moderate myopia (-6.00 D ≤ spherical equivalent < -2.00 D) in the test and control groups was 17 cases (32 eyes) and 20 cases (40 eyes), respectively. Number of patients with high myopia (-11.00 D ≤ spherical equivalent < -6.00 D) in the test and control groups was 22 cases (42 eyes) and 15 cases (26 eyes) respectively. The first day after SBK, 0.1% Bromfenac sodium hydrate eye drops was administrated 2 times/day in patients in the test group and continued for 10 and 14 days in low and high myopia, respectively. In the control group, 0.1% fluorometholone eye drops was used 4 times/day, then reduced gradually and continuously for 16 days. Visual acuity, computer refraction, intraocular pressure (IOP) and corneal topography examination were conducted at different postoperative period. Symptoms and related complications were recorded. Ranked data were statistically analyzed using the Wilcoxon rank sum test and quantitative data were analyzed using independent samples t-test. Results: For low to moderate myopic patients, average postoperative IOP and corneal curvature K2 after one and three months in the test group were (7.84 ± 1.35) and (8.13 ± 1.75) mm Hg(1 mm Hg = 0.133 kPa), and (38.66 ± 1.68) and (38.75 ± 1.45) D, respectively; in the control group, these parameters were (9.37 ± 1.28) and (9.47 ± 1.58) mm Hg and (39.56 ± 1.58), and (39.51 ± 1.50) D, respectively. All of these data in the test group were lower than those in the control group, the differences were statistically significant (t = -2.299, -2.112, P < 0.05). There were no significant differences (P < 0.05) in postoperative uncorrected visual acuity, spherical equivalent, corneal curvature K1, astigmatism CY, IOP (after 6 months) and corneal curvature K2 (after 6 months) between the test and control group. For the high myopic patients, mean postoperative uncorrected visual acuity in the test group and control group after 3 months were 5.14 ± 0.06 and 5.09 ± 0.07, respectively. The difference was statistically significant (t = 2.517, P = 0.015). There were no significant differences in symptoms between these two groups (two-sided test P > 0.1). High IOP and obvious myopia regression were not found in all patients. Conclusions: Bromfenac sodium hydrate eye drops (0.1%) can achieve the same therapeutic effect as fluorometholone eye drops after SBK and the former is better than the later in postoperative IOP control.
Effect of 0.1% Bromfenac for Preventing Macular Edema after Cataract Surgery in Patients with Diabetes
Korean J Ophthalmol 2020 Feb;34(1):46-55.PMID:32037749DOI:10.3341/kjo.2019.0044.
Purpose: To investigate the effect of 0.1% Bromfenac sodium hydrate ophthalmic solution for prevention of macular edema after cataract surgery in patients with diabetes. Methods: A retrospective analysis of 75 patients with diabetes who underwent cataract surgery was performed. Thirty-eight patients (52 eyes) were instilled with 0.1% bromfenac solution (bromfenac group) and 37 patients (46 eyes) were not (control group). Results: There were no significant preoperative between-group differences. Compared to the control group, at 1 month after surgery, the bromfenac group showed slightly better best-corrected visual acuity (0.12 ± 0.12 vs. 0.32 ± 0.42, p = 0.142), lower central macular thickness (265.58 ± 31.28 vs. 314.15 ± 76.11 μm, p < 0.001), and lower macular volume (8.46 ± 0.60 vs. 9.14 ± 1.53 mm³, p = 0.022). There were no significant differences between the two groups at 4 and 6 months postoperatively (p > 0.05). Mean changes in central macular thickness showed significant differences at 1 and 4 months postoperatively (-1.44 ± 11.72 and 10.44 ± 22.48 μm in bromfenac group vs. 47.19 ± 70.24 and 31.69 ± 48.04 μm in control group, p < 0.001 and p = 0.016) and mean changes in macular volume showed a significant difference at 1 month postoperatively (-0.08 ± 0.47 mm³ in bromfenac group vs. 0.58 ± 1.28 mm³ in control group, p < 0.001). There were no significant differences thereafter (p > 0.05). Conclusions: Treatment with 0.1% Bromfenac sodium hydrate ophthalmic solution showed good efficacy for preventing cystoid macular edema early after cataract surgery in patients with diabetes.
Effect of non-steroidal anti-inflammatory ophthalmic solution on intraocular pressure reduction by latanoprost
Br J Ophthalmol 2003 Mar;87(3):297-301.PMID:12598441DOI:10.1136/bjo.87.3.297.
Aim: To investigate the effects of a non-steroidal anti-inflammatory drug (NSAID) ophthalmic solution on latanoprost induced intraocular pressure (IOP) reduction using normal volunteers. Methods: This study was conducted as a prospective and observer masked clinical trial. 13 normal volunteers were enrolled. After measurement of basal IOP and ophthalmic examination, latanoprost ophthalmic solution was initially administered to both eyes once daily. Four weeks later, an NSAID ophthalmic solution, sodium 2-amino-3-(4-bromobenzoyl) phenylacetate sesquihydrate (refer to Bromfenac sodium hydrate), was co-administered to one randomly selected eye (NSAID group) twice daily for 2 weeks. The other eye was employed as a control (non-NSAID group). After withdrawal of the NSAID ophthalmic solution, latanoprost ophthalmic solution was continuously administered for another 2 weeks and was then withdrawn. After a 4 week washout, only Bromfenac sodium hydrate ophthalmic solution was administered to the eyes of the NSAID group for 2 weeks. During the study period, ophthalmic examination, including IOP measurement was performed in an observer masked fashion. Results: Before initiation of Bromfenac sodium hydrate, baseline IOPs of the non-NSAID group and the NSAID group were 15.73 (SD 1.97) mm Hg and 15.86 (2.06) mm Hg, respectively (p=0.88). Although latanoprost ophthalmic solution significantly reduced IOP in both groups, co-administration of Bromfenac sodium hydrate significantly inhibited latanoprost induced IOP reduction compared with the non-NSAID group. The IOPs of the non-NSAID and NSAID groups were 10.18 (1.17) mm Hg and 11.63 (1.35) mm Hg with a 2 week co-administration, respectively (p <0.01). Withdrawal of Bromfenac sodium hydrate ophthalmic solution diminished the difference between the two groups. Re-administration of bromfenac sodium ophthalmic solution only did not affect IOP. Conclusion: These results indicate that NSAID ophthalmic solution may interfere with IOP reduction by latanoprost ophthalmic solution in normal volunteers and that we should take this into account when treating patients with glaucoma using latanoprost ophthalmic solution.
Bromfenac eyedrops in the treatment of diabetic macular edema: a pilot study
Eur J Ophthalmol 2017 May 11;27(3):326-330.PMID:28009414DOI:10.5301/ejo.5000888.
Purpose: To evaluate the efficacy and safety of topical bromfenac in patients with newly diagnosed diabetic macular edema (DME). Methods: In this pilot study including 17 patients with monocular, newly diagnosed DME, diagnosis of DME was established by the detection of retinal thickening at or within 500 μm of the center of the macula on ophthalmoscopic examination, according to the Early Treatment Diabetic Retinopathy Study classification. Central macular thickness (CMT) was determined by optical coherence tomography. Bromfenac sodium hydrate 0.9 mg/mL eyedrops were administered in the affected eye twice daily for 30 days. Primary endpoints were changes in best-corrected visual acuity (BCVA) and CMT at the end of therapy. Results: Topical bromfenac significantly reduced mean CMT, from 465.41 ± 118.47 μm at baseline to 388.88 ± 152.63 μm posttreatment (p = 0.02). There was no significant change in BCVA and differences in mean macular volume fell just short of statistical significance (p = 0.06). Treatment was well-tolerated, and there were no topical or systemic side effects. Conclusions: Topical bromfenac twice daily may play a role in the reduction of DME. These preliminary results warrant further larger multicenter studies to confirm our findings and establish whether topical bromfenac may be of long-term benefit in the treatment of DME.
Comparison of a preservative-free nonsteroidal anti-inflammatory drug and preservative-free corticosteroid after uneventful cataract surgery: multicenter, randomized, evaluator-blinded clinical trial
J Cataract Refract Surg 2022 Jun 1;48(6):710-716.PMID:34629379DOI:10.1097/j.jcrs.0000000000000841.
Purpose: To compare the efficacy of nonsteroidal anti-inflammatory drugs (NSAIDs) and steroidal eyedrops for inflammation management after cataract surgery using slitlamp indicators. Setting: 11 eye centers in South Korea. Design: Randomized prospective multicenter study with a blinded evaluator. Method: In 125 (250 eyes) patients who underwent cataract surgery, Bromfenac sodium hydrate 0.1% (NSAID group) was applied twice a day in 1 eye, whereas the other eye was treated with fluorometholone 0.1% (steroid group), 4 times a day for 4 weeks postoperatively. The primary efficacy outcome was the presence of anterior chamber cells and flare at 1 week postoperatively. Anterior chamber cells and flare at 4 to 8 weeks, corrected distance visual acuity, central corneal thickness, conjunctival hyperemia, dry eye parameters, foveal thickness, and ocular and visual discomfort were evaluated as secondary outcomes. Results: At week 1, residual anterior chamber inflammation was not statistically significantly different between the groups (-1.03 ± 1.27 vs -0.95 ± 1.24, P = .4850). However, the NSAID group recovered from conjunctival hyperemia more rapidly than the steroid group (0.30 ± 0.52 vs 0.44 ± 0.81, P = .0144 at week 1). The increase in central corneal thickness in the NSAID group was less than that in the steroid group 1 week postoperatively (7.87 ± 22.46 vs 29.47 ± 46.60 μm, P < .0001). The change in foveal thickness in the NSAID group was significantly less than that in the steroid group (18.11 ± 68.19 vs 22.25 ± 42.37 μm, P = .0002). Lower levels of postoperative ocular and visual discomfort were reported in the NSAID group than in the steroid group under treatment. Conclusions: Preservative-free bromfenac was as effective as preservative-free fluorometholone eyedrops in anterior chamber inflammation control and showed better signs and symptoms after cataract surgery.