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1.
2.
We investigated the dose-escalation profile of dorzolamide used in combination with other antiglaucoma agents in patients with primary glaucoma and ocular hypertension. In a prospective, open-label study, 78 patients received dorzolamide 0.5% in addition to other topical antiglaucoma agents for > or =4 weeks. The concentration of dorzolamide was then escalated to 1.0% and intraocular pressure (IOP) measured every 4 weeks for 12 weeks. Dose escalation of dorzolamide from 0.5% to 1.0% resulted in a significant reduction in IOP throughout the 12 weeks of treatment at the higher dose. Mean baseline IOP was 19.7 mmHg. At 4, 8, and 12 weeks after dose escalation, mean IOP had decreased to 17.8 (-9.4%), 17.6 (-10.8%), and 17.5 (-10.7%) mmHg. No serious drug-related adverse effects were reported. These results indicate that dose escalation of dorzolamide from 0.5% to 1.0% is effective and well tolerated as adjunctive therapy for patients in whom IOP is insufficiently controlled by combination therapy.  相似文献   

3.
Dorzolamide is the first commercial topical carbonic anhydrase inhibitor approved by the Food and Drug Administration (FDA) for the treatment of glaucoma. In a prospective, open label, uncontrolled study on 245 glaucoma patients, dorzolamide significantly lowered the intraocular pressure at least 14% when used alone or in combination with one, two, or three other antiglaucoma medications over ten weeks. There were very few adverse reactions to dorzolamide. Dorzolamide is effective and safe when used alone or in combination with other topical antiglaucoma medications for the treatment of glaucoma.  相似文献   

4.
PURPOSE: To compare the efficacy and safety of unoprostone versus brimonidine both given twice daily in ocular hypertensive or primary open-angle glaucoma subjects. METHODS: After a 1-month washout period a baseline diurnal curve was measured every 2 hours from 08:00 hours (trough) to 20:00 hours in subjects with a trough intraocular pressure (IOP) and the pressure 24 mmHg. Qualified subjects were randomized to either brimonidine or unoprostone. After 6 weeks of treatment the period 1 diurnal curve was performed. Subjects were then switched to the opposite treatment for 6 weeks and the period 2 diurnal curve was performed. RESULTS: A total of 33 subjects were included in this study. In the brimonidine-treated group the trough IOP 20.1 +/- 2.8 mmHg was reduced from baseline up to 8 hours after dosing. In the unoprostone-treated group the trough IOP was 19.5 +/- 3.0 mmHg, which was statistically equal to that of brimonidine (p = 0.21), was reduced from baseline for 12 hours after dosing. Brimonidine decreased the IOP statistically more than unoprostone at 10:00 and 12:00 hours (p < 0.0001 and p = 0.02, respectively), while unoprostone reduced the IOP more than brimonidine at 18:00 and 20:00 hours (p = 0.002 and p = 0.05, respectively). Safety levels were similar between groups, but unoprostone caused more ocular stinging than brimonidine (p = 0.008). CONCLUSION: This study suggests that twice daily brimonidine demonstrates a statistically greater peak reduction in IOP than unoprostone. However, unoprostone, but not brimonidine, decreased IOP over the complete 12-hour daytime dosing cycle.  相似文献   

5.
PURPOSE: A long-term comparison of the ocular hypotensive efficacy and safety of unoprostone isopropyl 0.15% twice daily with that of timolol maleate 0.5% twice daily and betaxolol HCl 0.5% twice daily.DESIGN: This was a randomized, multicenter, double-masked, active-controlled 24-month clinical trial involving 27 centers in Europe and Israel. METHODS:The study population was composed of patients with primary open-angle glaucoma (including pseudoexfoliation) or ocular hypertension. After washout of antiglaucoma medications, intraocular pressure (IOP) was measured at 0, + 2, + 8, and + 12 hours. Patients were randomized in a 2:1:1 ratio to unoprostone, timolol, or betaxolol. Patients returned for examinations at 2 and 6 weeks and 3 and 6 months. RESULTS: 556 patients were randomized. Each drug produced a clinically and statistically (P <.001) significant reduction from baseline in 12-hour diurnal IOP at month 6 (- 4.3 mm Hg, unoprostone; - 5.8 mm Hg, timolol; - 4.9 mm Hg, betaxolol). Differences in adjusted treatment means between unoprostone and timolol and unoprostone and betaxolol were 1.57 mm Hg (95% CI: 1.00, 2.13) and 0.53 mm Hg (95% CI: - 0.03, 1.09), respectively. Unoprostone was clinically equivalent to betaxolol but did not have as great an IOP-lowering effect as timolol. Discontinued for inadequate control of IOP were 7%, 1%, and 4% of the patients for unoprostone, timolol, and betaxolol, respectively. There were no changes of note in visual acuity, pupil size, cup-to-disk ratio, visual fields, or iris color. Changes in heart rate and blood pressure were small, with no clinically significant differences between groups. CONCLUSIONS: Unoprostone provided a clinically significant IOP-lowering effect equivalent to betaxolol but not to timolol. The side effect profile of unoprostone appears to be comparable to other established IOP-lowering agents.  相似文献   

6.
Corneal epithelial disorders due to isopropyl unoprostone (unoprostone) eye drops, a prostaglandin F2alpha-related substance and antiglaucoma agent, have been reported since the agent became commercially available. The in vitro study was performed to clarify the mechanism of cell injury due to unoprostone. After Chang's human conjunctival cells were cultured and exposed for 2, 4 and 8 min to 0.03, 0.06, and 0.12% unoprostone and its vehicle containing 1% polysorbate 80, a cell growth assay and DNA histogram analysis using a flow cytometer and scanning electron microscopy were performed. The number of living cells was reduced, and the floating cell number increased immediately after exposure to 0.12% unoprostone for 8 min. When the cells were cultured for another 48 hr after exposure to unoprostone, the cell number was reduced dose and time dependently. Exposure for 2 min to 0.12% unoprostone showed no effect on the cell cycle. However, exposure for 2 min to 0.12% unoprostone caused alteration of the cell surface, such as reduction of microvilli and filopodia. The vehicle did not affect the cell surface or cell growth. These results suggest that clinically instilled eye drops ofunoprostone can affect cell structure, inhibit cell growth, and gradually cause corneal epithelial disorders.  相似文献   

7.
In a double-masked, randomized, controlled clinical trial, the authors evaluated the ocular hypotensive efficacy of twice-daily treatment with levobunolol (0.25 and 0.5%) and betaxolol (0.5%) in 85 patients with open-angle glaucoma or ocular hypertension. During the 3-month study, intraocular pressure (IOP) reductions in the two levobunolol groups were significantly greater than in the betaxolol group. From a mean baseline IOP of approximately 25 mmHg, overall mean reductions were 6.2 and 6.0 mmHg for the 0.25 and 0.5% levobunolol groups, respectively, and 3.7 mmHg for the betaxolol group. No clinically or statistically significant among-group differences were noted in the systemic safety variables evaluated. These data suggest that although all three treatments are effective, levobunolol provides a greater reduction in IOP than betaxolol.  相似文献   

8.
Adjunctive therapy for the management of glaucoma is commonly used. Unfixed combinations of the prostaglandin analog latanoprost and other glaucoma medications have been demonstrated to effectively lower intraocular pressure (IOP). The range of reported additional reductions in IOP compared to a monotherapy baseline are as follows: latanoprost-timolol (13-37%), latanoprost-pilocarpine 2% (7-14%), latanoprost and carbonic anhydrase inhibitors (15-24.1%), and latanoprost and dipivefrin (15-28%). There is a fixed combination of latanoprost (0.005%) and timolol (0.5%) that has been investigated in Phase III trials in Europe and the United States. In these trials, it was noted that the efficacy of the fixed combination was superior to either of the monotherapy components. After 12 months of follow-up of patients on fixed combination, there was no evidence of long-term drift. The new formulation appears to be safe and does not demonstrate any more side effects than either of the components. The convenience of a fixed combination may enhance patient compliance. Unfixed combination therapy with latanoprost and other antiglaucoma medications and the fixed combination formulation of latanoprost and timolol provide an effective and safe option for lowering IOP in glaucoma patients.  相似文献   

9.
The purpose of the present study was to study the effect of topical unoprostone on the circulation of human optic nerve head (ONH) and retina in normal subjects. Using laser-speckle tissue blood flow analysis, normalized blur (NB), a quantitative index of tissue blood velocity, was measured every 0.125 sec at a temporal ONH site, free of visible surface vessels. Measurements were averaged for 3 cardiac cycles (NB(ONH)). Color Doppler imaging (CDI) was also used to evaluate peak systolic blood velocity (PSV), end-diastolic velocity (EDV), and resistive index (RI) in the central retinal artery (CRA) and mean blood velocity (MV) in the central retinal vein (CRV). For baseline comparison (Day 0), recordings of bilateral NB(ONH) and intraocular pressure (IOP), blood pressure (BP), and pulse rate (PR) were recorded in healthy volunteers before, and 45, 90, 180, and 270 min after instillation of one drop of unoprostone vehicle. On Day 1 (the day after baseline measurements), and twice daily for 7 days, one drop of 0.12% unoprostone was instilled into one eye and its vehicle into the other in a double-blinded manner. Measurements as on Day 0 were recorded on Days 1 and 7. CDI measurements were performed before and at 45 and 180 min after morning instillation on Days 1 and 7. During baseline recordings, there were no significant changes in any parameters. After administration of topical unoprostone, IOP was significantly lower bilaterally with more reduction in the unoprostone-treated eyes on Day 7. On Day 7, the NB(ONH) of the unoprostone-treated eyes was significantly higher 45 min after instillation than baseline (P = 0.035 with Bonferroni's correction). Analysis of variance for repeated measurements also revealed significant difference between Day 0 and Day 7 (P = 0.0017). BP, PR, NB(ONH) in the eye that received only the vehicle, PSV, EDV, and RI in the CRA in both eyes, and MV in the CRV in both eyes changed little. Tissue blood velocity in the ONH increased, at least temporarily, following instillation of unoprostone twice daily for 7 days. Although the clinical implication of the increase is unclear, the effects of topical unoprostone on human ONH circulation deserve further consideration.  相似文献   

10.
A study of 30 subjects (10 normal and 20 having glaucoma) was done to find out the scleral rigidity in glaucoma cases as compared to normal. The effect of miotics, timolol (0.25%) and pilocarpine (2%) eye drops on the scleral rigidity in cases of glaucoma was observed.  相似文献   

11.
目的 探讨长期使用青光眼药物对患者眼表的影响.方法 收集局部使用青光眼药物3个月以上的患者65例108只眼,分为单种药物使用组(A组)和多种药物使用组(B组);另收集正常对照组(c组)25例25只眼.对所有观察对象进行泪膜破裂时间测定(BUT)、基础泪液分泌试验(ST)、角膜上皮荧光素染色、结膜上皮虎红染色以及结膜印迹细胞(IC)检查.结果 正常对照组BUT(12.25±5.40)s,ST(11.65±4.66)mm,A组BUT(6.97±4.87)8 9ST(7.19±5.36)mm,明显低于正常对照组(BUT P=0.000;STP=0.001). B组BUT(4.81±2.45)s,显著短于正常对照组(P=0.000)和A组(P=0.008);ST(5.20±2.97)mm,显著少于正常对照组(P=0.000)和A组(P=0.026).A组和B组的角膜荧光素染色评分和结膜虎红染色评分显著高于正常对照组.与正常对照组相比,A组和B组IC评分2-3级所占比例明显增高,结膜上皮表现出鳞状上皮化趋势.结论 长期使用青光眼药物会导致患者泪膜稳定性下降、泪液分泌减少,角膜上皮荧光素染色增多,结膜上皮杯状细胞减少、上皮细胞呈鳞状上皮化等泪膜、角膜和结膜的损伤.  相似文献   

12.
The purpose of the study is to measure corneal and conjunctival sensitivity in patients under glaucoma topical treatment as compared to a control group. It is a case–control study. Corneal and conjunctival esthesiometry were carried out through a Cochet–Bonnet esthesiometer. We took healthy individuals as controls, who did not use any type of ophthalmic topical medications and without history of ocular surface pathology or irritation. The study group was subdivided per number of applications (1, 2, and 3 or more applications). From a total 182 eyes from 91 patients, of which 26 (28.57 %) were controls and 65 (71.43 %) were in the study group, a mean corneal sensitivity of 58.98 ± 2.25 mm was found in the control group and 52.97 ± 6.41 mm in patients using topical medication. Mean conjunctival sensitivity was 18.80 ± 5.40 mm in the control group and 11.76 ± 5.45 mm in the study group. There was no statistically significant difference among groups when separated by 1, 2, and 3 or more applications. Eyes under use of timolol-containing medications showed lower sensitivity values as compared to other topical antiglaucoma medications. Corneal and conjunctival sensitivities are diminished in patients with chronic use of topical hypotensive medications and these results can explain the lack of correlation between signs and symptoms that is typically found in patients treated for glaucoma or ocular hypertension.  相似文献   

13.
谢巍 《国际眼科杂志》2015,15(3):424-427
目的:探讨局部应用抗青光眼药物对患者眼表结构的影响。
  方法:收集局部应用抗青光眼药物3mo以上的患者35例49眼和健康志愿者作为正常对照组45例45眼,药物治疗组分为A亚组(单独应用一种药物)和B亚组(联合应用两种及以上药物)。对所有患者及健康志愿者行泪膜破裂时间(BUT)、泪液分泌试验(SⅠt)、角膜上皮荧光素染色(FL)、结膜上皮虎红染色(RB)及结膜印迹细胞学检查(CIC)、黏蛋白MUC5AC检测。
  结果:正常对照SⅠt(11.54±5.47)mm/5min,BUT(11.86±3.13)s,FL和RB评分为(0.42±0.61)分、(0.37±0.98)分,药物治疗组SⅠt(8.11±4.30)mm/5min,BUT(7.49±2.62)s,FL和RB评分为(1.15±0.87)分、(1.28±1.08)分,两组相比差异具有统计学意义( t=3.395,P=0.001;t=7.363,P=0.001, t=-4.266,P=0.001;t=7.363,P=0.000);A亚组SⅠt(9.51±4.76)mm/5min,BUT(8.46±1.24)s,FL和RB评分为(0.91±1.03)分、(0.85±1.07)分;B亚组SⅠt (6.34±4.05)mm/5min,BUT(6.38±1.25)s,FL和RB评分为(1.84±1.14)分、(1.56±1.31)分,A亚组与B亚组相比差异具有统计学意义( t=2.514,P=0.012;t=5.844,P=0.000,t=-2.992,P=0.003;t=-2.072,P=0.043)。与正常对照组相比,药物治疗组的结膜上皮细胞体积变大,浆核比变小,细胞受损明显,药物治疗组的结膜印记细胞学检查评分明显增高,两组之间差异有统计学意义(u=6.354,P=0.000),A亚组与B亚组的结膜印记细胞学检查评分无统计学差异(u=0.69,P=0.48)。正常对照组及药物治疗组的杯状细胞密度分别为(68.37±12.82)个/mm2及(32.83±10.68)个/mm2,差异显著( t =14.610, P =0.000)。抗青光眼药物治疗后,A亚组和B亚组的杯状细胞密度分别为(39.12±9.35)个/mm2及(27.58±8.47)个/mm2,两者的差异具有统计学意义( t=4.530,P=0.001)。正常对照组的泪液MUC5AC含量为(32.61±8.65) ng/mL,药物治疗组的泪液MUC5AC明显减少(13.84±6.72)ng/mL,差异具有统计学意义(t=11.804,P=0.000)。抗青光眼药物治疗后,B亚组的泪液MUC5AC含量(10.67±4.58)ng/mL较A亚组(20.17±5.84) ng/mL明显减少,两者差异显著( t=6.349,P=0.000)。
  结论:局部应用抗青光眼药物会导致患者泪液分泌减少、泪膜稳定性下降,眼表结构受损,增加用药种类会加重这种损害。  相似文献   

14.

Purpose

We investigated the effects of unoprostone on neurite extension of cultured retinal pieces and axonal regeneration of retinal ganglion cells in the crushed optic nerve of adult cats.

Methods

The retinal pieces were cultured with unoprostone or its primary metabolite, M1, dissolved in DMSO or polysorbate for 14 days, and the number and length of Tau-1-positive neurites and glial processes labeled with anti-glial fibrillary acidic protein antibodies were examined. After the optic nerve was crushed, unoprostone was injected into the vitreous body and the crushed site. On day 12, wheat germ agglutinin-conjugated horseradish peroxidase was injected into the vitreous body to anterogradely label the regenerated axons. On day 14, the optic nerve was excised and longitudinally sectioned. After peroxidase reaction, the number of axons regenerating beyond the crush site was examined.

Results

The greatest number of neurites protruded from the cultured retinal pieces in 3 μM unoprostone and 3 μM M1. The neurite length was also the longest at 3 μM unoprostone and 3 μM M1, in which no glial processes were detected. After injections of 3 μM unoprostone, the final concentration in the vitreous humor, into the vitreous body and the crush site, the optic nerve fibers regenerated and extended beyond the crush site. In contrast, almost no fibers extended beyond the crush site after injection of phosphate-buffered saline.

Conclusions

The results indicate that intravitreal injection of unoprostone promotes regeneration of crushed optic nerve fibers in adult cats.  相似文献   

15.
PURPOSE: To evaluate the changes in conjunctival impression cytology specimens from patients receiving various topical antiglaucoma medications. DESIGN: Cross-sectional comparative study. METHODS: Impression cytology specimens were obtained from the eyes taking no topical medication (n = 20) and from the eyes taking various antiglaucoma medications (timolol n = 34; latanoprost n = 40; dorzolamide n = 32; timolol + latanoprost n = 30; timolol + dorzolamide n = 34). Specimens were graded on a scale of zero to three according to Nelson's method. RESULTS: Cytology scores were significantly higher in the medication group than the control group. Mean cytology scores of the control, timolol, latanoprost, dorzolamide, timolol + latanoprost, and timolol + dorzolamide group were 0.20, 1.62, 2.00, 1.75, 2.13, and 2.44, respectively. Among the medication groups, cytology scores were significantly lower in the monotherapy group than the fixed-combination therapy group. CONCLUSIONS: Various topical antiglaucoma medications induce a significant degree of squamous metaplasia. Conjunctival surface could be altered after the long-term use of antiglaucoma medication.  相似文献   

16.
Adverse effects of topical antiglaucoma drugs on the ocular surface   总被引:1,自引:0,他引:1  
Purpose : This study was designed to determine the effect of long‐term antiglaucoma topical medication on the ocular surface; measuring basal Schirmer’s and tear break‐up time tests using conjunctival impression cytology. Methods : The ocular surfaces of 30 control subjects (group 1), 24 primary open‐angle glaucoma patients treated with 0.5% betaxolol hydrochloride (group 2), 27 primary open‐angle glaucoma patients treated with 0.5% timolol maleate (group 3) and 26 primary open‐angle glaucoma patients treated with 0.5% betaxolol and 1% dipivefrin hydrochloride (group 4) were evaluated. Basal Schirmer’s and tear break‐up time tests were measured and ocular surface changes were determined by impression cytology. Impression cytology specimens of each group were graded and scored in the range 0–3 according to Nelson’s method. Results : Patients in groups 2, 3 and 4 showed statistically significant fewer normal basal Schirmer’s tests (wettability) and tear break‐up time tests (P < 0.01). Also, the conjunctival impression cytology scores were significantly higher in groups 2, 3 and 4 than in group 1 (P < 0.01). Conclusions : The conclusion was that it is possible that conjunctival surface and tear film function change after the long‐term use of antiglaucoma medication.  相似文献   

17.
18.
There have been no reports to date on long-term betaxolol instillation effects on the human optic nerve head (ONH) tissue circulation. The purpose of this study was to study the effect of topical 0.5% betaxolol on tissue blood velocity in the human ONH. Using a laser-speckle tissue blood flow analyzer, normalized blur (NB; a quantitative index of tissue blood velocity) was measured every 0.125 seconds at a temporal ONH site free of visible surface vessels. Measurements were averaged for 3 cardiac cycles (NB(ONH)). For baseline comparison (day 0), recordings of bilateral NB(ONH) and intraocular pressure (IOP), blood pressure (BP) and pulse rate (PR) were recorded in healthy volunteers before, and 2, 4.5, and 7 hr after, instillation of 30 microL of betaxolol vehicle, and again on day 21; IOP was also recorded on days 7 and 14. On day 1 (the day after baseline measurements), and twice daily for 3 weeks, 30 microL of 0.5% betaxolol into one eye and 30 microL vehicle was instilled into the other in a double-blind study. Measurements as on day 0 were again recorded on day 21; IOP was also recorded on days 7 and 14. During baseline recordings, no significant changes were noted in any parameters. After administration of topical betaxolol, IOP was significantly reduced, bilaterally, with greater reduction in the betaxolol-treated eyes on day 21. Also on day 21, the NB(ONH) of the betaxolol-treated eyes was significantly higher 4.5 hr after instillation than that of the comparable baseline recording (p = 0.035 with Bonferroni's correction); BP, PR, and NB(ONH) in the eye which received only the vehicle showed little change. Tissue blood velocity in the human ONH was increased at least temporarily by instillation of topical betaxolol twice daily for 3 weeks. Although the obtained increase is small and may be clinically insignificant, the potential of betaxolol that can affect the ONH tissue circulation in humans after 21 days of instillation is thought to deserve further investigation.  相似文献   

19.
BACKGROUND: In Canada, public drug plans may restrict the use of newer topical antiglaucoma agents. The goals of this retrospective study were to estimate the proportion of patients who, at the initiation of topical glaucoma therapy, had contraindications to the use of topical beta-blockers and to identify whether changes in formulary listing status (from restricted-drug list to generally available drug list) influenced the use of topical glaucoma agents in patients with contraindications to beta-blockers. METHODS: Claims databases administered by the Régie de l'assurance maladie du Quebec were used to identify incident users of beta-blockers (betaxolol and timolol) and newer antiglaucoma agents (brimonidine, dorzolamide and latanoprost) among patients aged 35 years or older. Drug claims and physician diagnoses were used to determine the prevalence of the following contraindications to the use of beta-blockers (including warnings and precautions): asthma or chronic bronchitis, diabetes, dysrhythmia and heart failure, all in the year preceding the initiation of therapy; or use of systemic beta-blockers at the time glaucoma therapy was started. The observation period was divided into 2 phases: the time during which newer agents were on the restricted-drug list (first-line use being limited to patients with contraindications to the use of beta-blockers; January 1997 to March 1999) and the time during which these agents were on the generally available drug list (that is, after reimbursement restrictions were relaxed; April 1999 to June 2000). RESULTS: Of the 20 309 eligible patients, 59.8% were female, and the mean age was 72 years. Contraindications to topical beta-blocker therapy were significantly more frequent among the patients using newer antiglaucoma agents than among those using beta-blockers (71.5% vs. 55.5%, p < 0.0001). Asthma and chronic bronchitis were also more frequent among the patients using the newer agents than among those using beta-blockers (43.1% vs. 22.5%, p < 0.0001). Among the patients without contraindications to topical beta-blocker therapy, the overall proportions started on therapy with a newer agent were 22.7% when there were reimbursement restrictions and 30.0% when the restrictions were relaxed (p < 0.0001). CONCLUSIONS: Among patients with contraindications to the use of beta-blockers, newer topical antiglaucoma agents were used more often than beta-blockers. Among patients without such contraindications, the use of the newer agents increased modestly when reimbursement restrictions were relaxed.  相似文献   

20.
AIM: To do a randomized prospective interventional study for comparing the effects of a single subconjunctival triamcinolone acetonide (SCTA) injection to tapering topical loteprednol in patients undergoing phacoemulsification surgery under topical anesthesia. METHODS: A total of 400 patients were randomized into 2 groups; Group A (200 patients) received 5 mg SCTA at the end of surgery and topical ketorolac tromethamine (0.5%) with ofloxacin (0.3%) combination for 3wk. Group B (200 patients) received tapering topical loteprednol etabonate (0.5%) along with ofloxacin (0.3%) and ketorolac tromethamine (0.5%) for 3wk. Outcomes evaluated were intraocular pressure (IOP), anterior chamber cells/flare and macular oedema postoperatively at 1, 6 and 12wk. RESULTS: Baseline parameters were almost similar in both the groups. No statistical difference was seen between the preoperative and postoperative IOP values for Group A (P=0.82) and Group B (P=0.61) and postoperative IOP values in between both groups (P=0.14) at 1wk. Incidence of cells/flare postoperative was statistically not significant (P=0.82) in both groups at all follow up visits. Postoperative macular oedema was not observed at any follow up visit. CONCLUSION: SCTA appears to be an effective alternative to prolong postoperative topical steroid use.  相似文献   

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