Vitreous penetration of topical moxifloxacin and gatifloxacin in humans

PURPOSE: To determine the vitreous penetration of the new fourth-generation topical fluoroquinolones moxifloxacin 0.5% and gatifloxacin 0.3%. METHODS: A prospective randomized clinical trial comprising 12 eyes of 12 patients scheduled for pars plana vitrectomy between August 2003 and September 2003 was performed in a clinical practice. The patients were randomly assigned to receive topical moxifloxacin 0.5% (n = 6) or gatifloxacin 0.3% (n = 6). One half the patients in each antibiotic group received 1 drop every 15 minutes for a total of 3 doses starting 1 hour before surgery, and the other one half self-administered the antibiotic drop 4 times daily for 3 days before surgery and at 7 am on the day of surgery. Undiluted vitreous samples were obtained and analyzed using high-performance liquid chromatography. RESULTS: Either moxifloxacin 0.5% or gatifloxacin 0.3% was detected in the vitreous in all 12 patients in the study. There was no significant difference between the mean vitreous concentration of moxifloxacin 0.5% given over 1 hour preoperatively (0.012 +/- 0.011 microg/mL) and that given in the 3-day regimen (0.011 +/- 0.008 microg/mL) (P = 0.93). There was also no significant difference between the mean vitreous concentration of gatifloxacin 0.3% given over 1 hour preoperatively (0.001 +/- 0.0003 microg/mL) and that given over 3 days (0.008 +/- 0.006 microg/mL) (P = 0.11). Vitreous concentrations of moxifloxacin 0.5% and gatifloxacin 0.3% in each eye were all lower than the 90% minimum inhibitory concentration for the commonest bacterial isolates causing endophthalmitis. With both dosing regimens, the mean vitreous concentration of moxifloxacin 0.5% was higher than that of gatifloxacin 0.3% administered at the same regimen, but this was not statistically significant. CONCLUSION: Both topical moxifloxacin 0.5% and gatifloxacin 0.3% penetrated the vitreous in the uninflamed eye, but the vitreous concentrations attained were all lower than the 90% minimum inhibitory concentration for the commonest bacterial pathogens causing acute postoperative endophthalmitis.     

Topical prophylaxis with moxifloxacin prevents endophthalmitis in a rabbit model

PURPOSE: The prophylaxis potential of the topical antibiotic, 0.5% moxifloxacin (Vigamox), was evaluated to prevent endophthalmitis after bacterial anterior chamber challenge in a rabbit model. DESIGN: An in vivo laboratory investigation. METHODS: Three regimens of topical 0.5% moxifloxacin were tested for prophylaxis to prevent endophthalmitis: (1) (full prophylaxis) moxifloxacin drops every 15 minutes for 1 hour (five drops), anterior chamber challenge with 5 x 10(4) colony-forming units of Staphylococcus aureus, one drop of moxifloxacin, and four more drops applied over the next 24 hours; (2) (preprophylaxis) prechallenge prophylaxis, S. aureus challenge, and no postchallenge prophylaxis; and (3) (postprophylaxis) no prechallenge prophylaxis, S. aureus challenge, and postchallenge prophylaxis. A saline control was tested concurrently in all three experiments. At 24 hours after injection, the eyes were evaluated by slit lamp in a masked fashion for clinical signs of endophthalmitis, and the anterior and posterior chambers were cultured for bacteria. RESULTS: The median clinical scores for the moxifloxacin group were significantly lower than the saline group for all three treatment regimens. The median clinical score for the full prophylaxis regimen was significantly lower than the preprophylaxis and postprophylaxis regimens alone. The anterior and posterior chambers were negative for S. aureus in all three moxifloxacin treatment regimens. CONCLUSIONS: In a rabbit model, a "proof of principle" was demonstrated that topical antibiotic therapy pre- and postintraocular bacterial challenge could prevent bacterial endophthalmitis. Surgical prophylaxis with topical 0.5% moxifloxacin (Vigamox) may prove to be a valuable adjunct for the prevention of endophthalmitis.     

Effects of intravitreal moxifloxacin and dexamethasone in experimental Staphylococcus aureus endophthalmitis

PURPOSE: To evaluate the effects of intravitreal moxifloxacin and moxifloxacin and dexamethasone combination in an experimental rabbit model of Staphylococcus aureus endophthalmitis. METHODS: The right eyes of 24 rabbits weighing 2 to 3 kg were used. Ten thousand colony-forming units (CFU) of S. aureus in 0.1 ml saline solution were inoculated into the vitreous cavity. The eyes were randomly assigned to one of the four groups equally. Twenty-four hours after the inoculation of S. aureus, group 1 received 50 microg moxifloxacin, group 2 received 50 microg moxifloxacin plus 400 microg dexamethasone, and group 3 received 1 mg vancomycin intravitreally. No treatment was given to group 4. Clinical examination scores were recorded. Vitreous aspirates were obtained for microbiological analysis just before sacrifice, and the eyes were enucleated for histopathologic examination. Statistical analysis was performed using Kruskal-Wallis and Mann-Whitney U tests. RESULTS: In all treatment groups, mean number of CFU and histopathologic score were significantly lower compared with control group (p<0.05), and the difference between treatment groups was not statistically significant (p>0.05). The clinical score was not significantly different between groups (p>0.05). CONCLUSIONS: Intravitreal injection of 50 microg moxifloxacin was effective in the treatment of S. aureus endophthalmitis. Bacteriological, histopathologic, and clinical outcomes after treatment using moxifloxacin, moxifloxacin and dexamethasone combination, and vancomycin were comparable. Intravitreal moxifloxacin may be an option in the treatment of S. aureus endophthalmitis.     

前房内给予莫西沙星预防眼内炎在白内障手术中的应用

目的：评价在白内障手术中采用前房内应用莫西沙星预防眼内炎的安全性和效果。

方法：选取2012年1-6mo在我院行白内障手术患者65例65眼。部分患者手术结束时前房给予莫西沙星,另外一部分作为对照组未使用莫西沙星。对患者术前和术后logMAR最佳矫正视力、眼内压、角膜水肿、前房形态进行检查。

结果：共33例患者(男19,女14)使用了莫西沙星,平均年龄64.81±11.61(41～82)岁; 32例患者(男15,女17)没有使用,平均年龄65.43±11.10(42-81)岁。患者的年龄(P=0.827)和性别(P=0.396)无统计学差异。术前两组的最佳矫正视力均接近20/130。术后,莫西沙星组和对照组的最佳矫正视力分别为20/25和20/23(P=0.160)。术前莫西沙星组眼内压为14.93±2.77(11-21)mmHg,对照组为15.06±2.42(12-21)mmHg(P=0.850)。术后,两组眼内压均无统计学差异\〖莫西沙星组：14.06±2.31(10-19)mmHg; 对照组：14.03±2.36(10-19)mmHg(P=0.726)\〗。两组角膜水肿(P=0.623)与前房细胞发生率(P=0.726)均无统计学差异。

结论：白内障手术后给予莫西沙星预防眼内炎是安全而有效的。     

Comparative penetration of moxifloxacin and gatifloxacin in rabbit aqueous humor after topical dosing

PURPOSE: To evaluate the aqueous penetration of the fourth-generation fluoroquinolones moxifloxacin and gatifloxacin. SETTING: University of Arizona, Tucson, Arizona, USA. METHODS: Forty eyes of 20 New Zealand white rabbits were divided into 2 experimental groups. In Experiment I rabbits (20 eyes), a commercial preparation of topical gatifloxacin 0.3% was administered to 9 eyes and moxifloxacin 0.5% to 9 eyes; 2 eyes served as a control. Eyes were dosed according to a keratitis protocol; ie, every 15 minutes for 4 hours. The aqueous humor was sampled 10 minutes after the last dose. Experiment II rabbits (20 eyes) were dosed according to a cataract prophylaxis protocol; ie, 4 times a day for 10 days. The aqueous humor was sampled 1 hour after the last dose of antibiotic in 12 eyes and 24 hours after the last dose in 8 eyes. High-performance liquid chromatography was used to determine the fluoroquinolone concentration. RESULTS: In the keratitis dosing protocol, the mean concentration of moxifloxacin in the aqueous (n=9) was 11.057 microg/mL (range 7.66 to 18.87 microg/mL), which was significantly higher than the mean concentration of gatifloxacin (n=8) (7.570 microg/mL [range 4.75 to 10.86 microg/mL]) (P=.030). In the cataract prophylaxis dosing protocol, the mean aqueous concentration of moxifloxacin (n=6) was 1.745 microg/mL (range 0.92 to 3.87 mg/mL). The mean concentration of gatifloxacin (n=6) was 1.207 microg/mL (range 0.44 to 2.44 microg/mL). The difference was not statistically significant (P=.359). CONCLUSIONS: Higher mean levels (x1.46) of aqueous penetration were achieved with moxifloxacin than with gatifloxacin in the keratitis-dosing model. There was no statistically significant difference between the 2 drugs in the cataract prophylaxis dosing model. Both antibiotics had aqueous levels in excess of the minimum inhibitory concentration for most pathogenic organisms in both models.     

Prevention of Staphylococcus aureus endophthalmitis with topical gatifloxacin in a rabbit prophylaxis model.

PURPOSE: The aim of this study was to investigate the prophylactic use of 0.3% gatifloxacin drops to prevent endophthalmitis in a rabbit model. METHODS: Forty (40) New Zealand white rabbits were randomly placed into group A (20 rabbits) where they received 1 drop of 0.3% gatifloxacin in their right eye every 15 min (0, 15, 30, and 45 min), or group B (20 rabbits) where they received 1 drop of balanced salt solution (BSS) in their right eye every 15 min (0, 15, 30, and 45 min). Following this treatment regimen, the anterior chamber of each rabbit was injected with 0.025 mL of saline containing 5 x 10(5) colonyforming units of a clinical isolate of Staphylococcus aureus (vancomycin-sensitive). After the inoculum injection, the treatment regimen continued: group A (1 drop of 0.3% gatifloxacin) or group B (1 drop of BSS) immediately postinjection, 6, 12, 18, and 24 h, at which time the animals were examined in a masked fashion, photographed, anesthetized, euthanized, and the aqueous and vitreous humors collected to determine the number of viable bacteria. RESULTS: The median clinical scores for the gatifloxacin group were significantly lower than the control group (P < 0.05). Bacterial recovery of S. aureus was significantly higher in the control group in both the aqueous and vitreous humor (P < 0.05). CONCLUSIONS: Gatifloxacin-treated eyes demonstrated significantly less inflammation, infection, and culture-positive endophthalmitis (P < 0.05), compared to the control animals. It is important to further investigate the clinical implications from this prophylatic study.     

Intravitreal moxifloxacin injections in acute post-cataract surgery endophthalmitis: Efficacy and safety

Purpose:The aim of this study was to evaluate the efficacy and safety of intravitreal moxifloxacin injections in the treatment of acute post-cataract surgery endophthalmitis with visual acuity equal to or greater than hand movements.Methods:Fifty two patients with post-cataract surgery endophthalmitis who presented within 6 weeks with visual acuity equal to or greater than hand movements received two intravitreal moxifloxacin injections 48 h apart. Patients with prior history of ocular disease or treatment were excluded. Patients were followed up to 3 months either for resolution of endophthalmitis or worsening of disease. Number of patients who achieved visual acuity equal to or better than 20/40 and 20/200 at the third-month follow-up visit were compared with the number of patients at presentation, using Chi-square test. In addition, pretreatment LogMAR visual acuity at the time of presentation was compared with posttreatment visual acuity at end of third month using paired t test.Results:Fifty (96.15%) patients showed complete resolution of endophthalmitis while three patients required vitrectomy. Forty-one (78.85%) and 49 (94.23%) patients achieved visual acuity equal to or better than 20/40 and 20/200, respectively, at the third-month follow-up visit as compared to eight (15.38%) and 13 (25%) patients, respectively, at presentation (P < 0.05). In addition, mean LogMAR visual acuity at the time of presentation was 0.755 which improved to 0.307 at the third-month follow-up visit (P < 0.05). None of the patients developed hypersensitivity reactions to intravitreal moxifloxacin.Conclusion:Intravitreal moxifloxacin injections showed promising results in acute post-cataract surgery endophthalmitis.     

Endogenous endophthalmitis treated with systemic ciprofloxacin and linezolid

Endogenous endophthalmitis is a serious sight-threatening condition. The role of intravitreal antibiotics is controversial. We present a case of endogenous endophthalmitis successfully treated with a combination of systemic ciprofloxacin and linezolid. The authors have stated that they do not have a significant financial interest or other relationship with any product manufacturer or provider of services discussed in this article. The authors also do not discuss the use of off-label products, which includes unlabeled, unapproved, or investigative products or devices.     

The effect of moxifloxacin and gatifloxacin on long-term visual outcomes following photorefractive keratectomy

PURPOSE: To compare the effect of gatifloxacin and moxifloxacin on visual outcomes after photorefractive keratectomy (PRK). METHODS: Thirty-five PRK patients were treated postoperatively with gatifloxacin (Zymar) in one eye and moxifloxacin (Vigamox) in the fellow eye. Postoperative regimens were otherwise identical. In a previous study (initial phase), we evaluated epithelial healing. In this study (second phase), we compared uncorrected visual acuity (UCVA), best spectacle-corrected visual acuity (BSCVA), manifest spherical equivalent (MSE), and corneal haze at 6 months postoperatively for 32 patients using the Wilcoxon signed ranks test. RESULTS: No statistically significant difference was noted between eyes treated with Zymar and Vigamox in terms of UCVA, BSCVA, MSE, or corneal haze at 6 months postoperatively. Two (6%) Vigamox-treated eyes versus 0 (0%) Zymar-treated eyes lost one line of BSCVA from preoperative examination. Median UCVA and MSE were equivalent for both groups. CONCLUSIONS: At 6 months after PRK, there was no significant difference in visual outcomes with either antibiotic.     

三种抗生素的抗菌活性及角膜上皮细胞毒性比较

目的比较左氧氟沙星、加替沙星和莫西沙星的抗菌活性及对角膜上皮细胞的毒性作用。方法细菌与细胞共孵育1h后,抗生素处理1h,行荧光染色和CFU计数;MTT法和划痕法检测细胞的增生和迁移能力,评价3种抗生素的细胞毒性作用。结果 3种抗生素的抗菌效果均非常显著,其中莫西沙星对金黄色葡萄球菌和左氧氟沙星对绿脓杆菌的抑菌活性最强,对凝固酶阴性葡萄球菌和黏质沙雷菌的抗菌效果差异无统计学意义;在质量浓度低于125mg/L时,左氧氟沙星的毒性明显低于莫西沙星和加替沙星。结论莫西沙星、左氧氟沙星和加替沙星3种抗生素在抗菌活性和上皮细胞毒性方面存在一定差异。     

The effect of fourth-generation fluoroquinolones gatifloxacin and moxifloxacin on epithelial healing following photorefractive keratectomy

PURPOSE: To compare the rate of epithelial healing following photorefractive keratectomy (PRK) with two commercially available fourth-generation fluoroquinolones, gatifloxacin (Zymar, Allergan, Irvine, California) and moxifloxacin (Vigamox, Alcon Laboratories, Fort Worth, Texas). DESIGN: Double-masked, randomized, prospective trial. METHODS: Thirty-five subjects received gatifloxacin in one eye and moxifloxacin in the fellow eye following PRK with a 9.0-mm epithelial defect. Patients were examined daily after surgery until the epithelium had healed completely in both eyes. Beginning on post-operative day 3, photos were taken and used to confirm epithelial healing or measure the area of residual epithelial defects. Healing times and defect sizes were compared using the Wilcoxon signed-ranks test. RESULTS: Both eyes healed on the same day in 18 of the 35 subjects (51.4%). In 13 of 35 (37.1%) subjects, the moxifloxacin-treated eye healed first, compared with only four of 35 (11.4%) subjects whose gatifloxacin-treated eye healed first. All six of the eyes that took 2 days longer than their fellow eye to heal were gatifloxacin-treated. Median healing time for both groups was 4 days (moxifloxacin range: 3 to 7 days; gatifloxacin range: 3 to 9 days; P = .01), but only 69% of gatifloxacin-treated eyes had healed by day 4 compared with 80% of the moxifloxacin-treated eyes. Overall, on each post-operative day, defect sizes were greater for the gatifloxacin-treated eyes. This difference was statistically significant on day 4 (P = .027). CONCLUSIONS: Eyes treated with moxifloxacin healed faster and had smaller defects compared with those treated with gatifloxacin. This provides another factor to consider in selecting antibiotic prophylaxis for corneal refractive surgery.     

Comparison of corneal surface effects of gatifloxacin and moxifloxacin using intensive and prolonged dosing protocols

PURPOSE: To compare the effects of the commercial formulations of moxifloxacin and gatifloxacin on rabbit corneal epithelium using two dosing protocols: high-frequency dosing for bacterial keratitis and cataract surgery prophylaxis. METHODS: Forty eyes of 20 New Zealand white rabbits were randomized to receive topical gatifloxacin, topical moxifloxacin, or no drops as controls. Eighteen eyes received 1 drop of antibiotic every 5 minutes for 15 minutes followed by 1 drop every 15 minutes for 4 hours. Twelve eyes received topical gatifloxacin or topical moxifloxacin 4 times a day for 10 days. Rabbits were euthanized, eyes enucleated, and the corneas separated, washed, and fixed; scanning electron microscopy was performed. Photomicrographs of three separate areas from the corneal apex were taken at x1200 and x3000 for each cornea. Two masked, experienced examiners then graded the corneal epithelial damage. RESULTS: In the high-frequency dosing group, mean corneal damage score for eyes treated with gatifloxacin was 1.593, that for moxifloxacin was 1.407, and control was 1.000. No statistically significant difference was found between gatifloxacin and moxifloxacin (P = 0.41), gatifloxacin and control (P = 0.14), or moxifloxacin and control (P = 0.23). In the cataract surgery prophylaxis group, mean corneal damage scores for eyes treated with gatifloxacin was 1.167, that for moxifloxacin was 1.368, and control was 1.000. No statistically significant difference was found between gatifloxacin and moxifloxacin (P = 0.23), gatifloxacin and control (P = 0.08), or moxifloxacin and control (P = 0.23). CONCLUSION: Despite differences in formulations, with short-term dosing neither gatifloxacin nor moxifloxacin appears to be toxic to the corneal epithelium in this rabbit model.     

Acute and bilateral uveitis secondary to moxifloxacin

CASE REPORT: We report a case of a 77-year-old woman with an anterior acute bilateral uveitis and pigmentary dispersion after treatment of a neumococic pneumonia with moxifloxacin. Her response to treatment was good but she presented as a result of treatment abundance of pigment over all the structures of the anterior segment. DISCUSSION: Many drugs can produce uveitis. After Med-line revision, we can not find any previously reported case of anterior Uveitis associated with fourth generation quinolones.     

Topical 0.5% moxifloxacin prevents endophthalmitis in an intravitreal injection rabbit model.

INTRODUCTION: Intravitreal injections for the treatment of retinal disease have increased the risk of endophthalmitis. We developed a rabbit model to investigate whether topical 0.5% moxifloxacin could prevent endophthalmitis after an intravitreal injection. METHODS: A rabbit model of intravitreal injection to produce endophthalmitis was developed by injecting triamcinolone into the vitreous through a depot of subconjunctival Staphylococcus aureus (10(7) cfu). Endophthalmitis was evaluated clinically and confirmed by culture. The model was tested with a commercially available brand of topical 0.5% moxifloxacin (N = 10) and saline (N = 10). In brief, after bacterial subconjunctival challenge, a topical treatment was administered every 15 min for 1 h. Immediately thereafter, triamcinolone was injected into the vitreous through the treated bacterial depot. Topical 0.5% moxifloxacin and saline were administered QID over the next 72 h. All rabbits were examined daily, euthanized, and tested for viable bacteria when clinical signs of endophthalmitis were observed. RESULTS: Anti-infective treatment with topical 0.5% moxifloxacin prevented the development of endophthalmitis (0/9 rabbits), compared to topical saline (6/10 rabbits; P = 0.01; power = 0.99). CONCLUSIONS: Topical 0.5% moxifloxacin provided effective prophylaxis to prevent endophthalmitis after an intravitreal injection of triamcinolone. This unique model may prove valuable to demonstrate prophylaxis for other anti-infectives at an intravitreal injection site.