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1.
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   
2.
Introduction: Topical corticosteroids are an important pharmacotherapy for the management of various inflammatory conditions affecting the anterior segment of the eye. However, medications in this class are associated with well-known risks including increased intraocular pressure (IOP) and development of cataracts. The topical corticosteroid loteprednol etabonate (LE) was developed with the specific intention of minimizing these side effects.

Areas covered: The focus of this review is to examine published efficacy and safety data for LE, a drug engineered to undergo rapid metabolism to inactive metabolites with the goal of improved safety. Two decades of clinical research focused on LE formulations are reviewed, including the use of LE in combination with tobramycin. The cumulative body of experience affirms the concept that the molecular design of LE confers certain safety benefits without compromising the desired anti-inflammatory efficacy of a topical corticosteroid.

Expert opinion: Loteprednol etabonate is a mainstay for topical therapy of a wide variety of commonplace and niche conditions of the ocular surface and the anterior segment, including in the healing post-operative patient. Its versatility and safety allow eye care providers to recommend both acute induction as well as chronic maintenance therapy with appropriate follow-up.  相似文献   

3.
Purpose. As a safe anti-inflammatory corticosteroid, the utility of loteprednol etabonate (LE) for the treatment of gastrointestinal inflammation, via oral and rectal administration, was investigated in rats. Methods. In vivo, LE solution and suspension were orally administered (20 mg/kg), and various LE preparations (solution, suspension & suppository) were applied in rectal loops (0.2 mg per loop). In vitro, various GI tissues were used to study the stability and partition of LE. Results. After oral administration of LE solution, LE reached the upper GI tract effectively, but not the colon, due to absorption and/or decomposition. In suspension, LE reached most of the GI tract (except rectum) in 8 hr and showed little absorption. After rectal applications, LE remained intact in the rectal loop for more than five hours with a slow rate of disappearance, however, LE distributed in the rectal membrane to some extent. The concentrations of LE and its inactive metabolites in plasma after both oral and rectal administrations were lower than the detection limit (0.1 µg/ml) at anytime during the experiments. In vitro, LE in solution was stable in stomach, but not in cecum, due to the hydrolysis by the cecal resident micro flora. In solution, LE distributed into the mucosal membranes efficiently (about 2.5 ~ 4.0 µg/g tissue). Conclusions. The results suggest that LE can be orally or rectally delivered in the GI tract for the topical treatment of the inflammatory bowel disease.  相似文献   
4.
BACKGROUND: Loteprednol etabonate (LE) is a novel soft steroid that was designed to improve the benefit/risk ratio of topical corticosteroid therapy. This study assesses the clinical efficacy and safety of three different doses of LE nasal spray in seasonal allergic rhinitis (SAR). METHODS: In this single-center, double-blind, placebo-controlled, parallel-group trial 165 subjects with SAR to grass pollen received daily single doses of either 100, 200, 400 microg LE nasal spray, or placebo for 14 days. The patients underwent three 4-h allergen challenges with grass pollen in an environmental exposure unit at a screening visit (baseline) and on days 7 and 14 of treatment. Standardized nasal symptom scores were obtained every 20 min. Nasal flow, nasal secretions, and FEV(1) were measured every hour during allergen challenges. RESULTS: After 14 days of treatment, patients who received 400 microg LE had significantly lower total nasal symptom scores compared with those receiving placebo (P = 0.007). LE400 reduced rhinorrhea, nasal congestion, nasal itching, the amount of nasal secretions, and improved nasal flow as compared with placebo (P < 0.05). LE100 and LE200 were not significantly different from placebo. All treatments were well tolerated. CONCLUSIONS: Loteprednol 400 microg once daily is superior to placebo and the only effective dose tested in improving nasal symptoms and objective parameters in patients with SAR.  相似文献   
5.
Purpose: To compare the efficacy and safety of postoperative topical loteprednol etabonate (LE) 0.5% with dexamethasone (DEX) 0.1% for the treatment of inflammation following pars plana vitrectomy (PPV).

Methods: A total of 150 eyes of 150 patients who underwent transconjunctival PPV for various diagnoses were included in this prospective, randomized study. The patients were assigned into two groups as Group LE (= 75) and Group DEX (= 75). Intraocular inflammation, intraocular pressure (IOP), and the intensity of postoperative pain were compared between the groups.

Results: The mean IOP was higher in the patients treated with DEX (p > 0.05). The need for anti-glaucoma medications was significantly lower in Group LE (5.3%) than in Group DEX (17.3%) (p = 0.020). Tyndall scores were less in Group DEX at postoperative Days 1 (p = 0.01) and 3 (p = 0.017). On Day 1, it was more likely for patients to have mild or moderate pain in Group LE (p < 0.001). On Day 3, the number of the patients with no pain was higher in Group DEX (p = 0.005).

Conclusions: Although DEX is more effective in the early postoperative days, LE appears to be as effective in controlling inflammatory response following PPV in the long-term. Topical LE is associated with less increase in the IOP and a lower need for anti-glaucoma medications.  相似文献   

6.
Purpose: To compare the efficacy of loteprednol etabonate 0.5%/tobramycin 0.3% (LE/T) and dexamethasone 0.1%/tobramycin 0.3% (DM/T) ophthalmic suspensions in reducing select signs of blepharitis.

Methods: Data were pooled from two studies (one from the USA; one from China) of adults (n = 627) with blepharokeratoconjunctivitis treated with LE/T or DM/T four times daily for 2 weeks (safety population). Efficacy analyses included 495 eyes (247 LE/T, 248 DM/T) with any baseline sign of blepharitis.

Results: At Day 15, the least squares mean change from baseline in composite blepharitis severity was similar between LE/T (–2.86) and DM/T (–2.99) (90% CI for mean treatment difference: –0.35, 0.11). Intraocular pressure (IOP) increases ≥10 mmHg over baseline were reported for 1 US patient (DM/T group) and 19 Chinese patients (6 LE/T; 13 DM/T).

Conclusions: LE/T was similarly effective in reducing the signs of blepharitis compared with DM/T, but demonstrated a better safety profile with respect to changes in IOP.  相似文献   

7.
目的:观察妥布霉素地塞米松联合氯替泼诺在治疗前葡萄膜炎中的抗炎作用及不良反应。方法:选择我院门诊于2008-02/2010-10就诊的前葡萄膜炎患者90例,随机分为A,B,C三组,A组采用妥布霉素地塞米松眼液,B组采用氯替泼诺眼液,C组采用妥布霉素地塞米松联合氯替泼诺眼液,连续随访6wk,观察炎症消退情况及出现的不良反应。结果:A组炎症反应消退快、病程短,但少数患者出现药物性高眼压;B组炎症反应消退较慢,无药物性高眼压现象;C组炎症反应消退快、病程短,无高眼压现象。结论:对前部葡萄膜炎患者治疗的不同阶段,联合两种糖皮质激素眼液治疗能快速控制炎症、缩短病程、安全有效地预防或降低并发症。  相似文献   
8.
目的 比较依碳酸氯替泼诺滴眼液和双氯芬酸钠滴眼液治疗季节性过敏性结膜炎的有效性和安全性。 方法 季节性过敏性结膜炎病人44例,随机分为依碳酸氯替泼诺滴眼液组(A组)和双氯芬酸钠滴眼液组(B组),A、B组分别采用依碳酸氯替泼诺与双氯芬酸钠滴眼液每天点眼4次。根据用药后临床症状和体征进行疗效评价;并对治疗过程中所有不良事件进行记录。结果 治疗14 d后,A组结膜改变和眼部瘙痒程度改变的有效率为95.2%,B组为69.6%,两组有效率比较差异有显著性(χ2=4.86,P〈0.05);A组畏光和分泌物消失占76.1%,B组占21.7%,两组比较差异有显著性(χ2=13.05,P〈0.01)。两组药物相关不良事件的发生情况比较差异无显著性(P〉0.05)。结论 依碳酸氯替泼诺滴眼液能明显缓解季节性过敏性结膜炎病人的临床症状, 治疗效果优于双氯芬酸钠滴眼液, 其安全性与双氯芬酸钠滴眼液类似。  相似文献   
9.
  1. Loteprednol etabonate (LE) is a soft corticosteroid with two labile ester bonds at 17α- and 17β-positions. Its corticosteroidal activity disappears upon hydrolysis of either ester bond. Hydrolysis of both ester bonds produces the inactive metabolite, Δ1-cortienic acid (Δ1-CA).

  2. The simple high-performance liquid chromatography method using acetic acid gradient was developed for the simultaneous determination of LE and its acidic metabolites.

  3. LE was hydrolyzed in rat plasma with a half-life of 9?min. However, LE hydrolysis was undetectable in rat liver and intestine. LE hydrolysis in rat plasma was completely inhibited by paraoxon and bis(p-nitrophenyl) phosphate, thus identifying carboxylesterase as the LE hydrolase. Rat plasma carboxylesterase had a Km of 6.7?μM for LE.

  4. In contrast to the disappearance rate of LE in rat plasma, the formation rate of 17α-monoester and Δ1-CA was markedly low, and a main hydrolysate of LE was not detected in rat plasma.

  5. The metabolism of LE proceeded via different pathways in human and rat plasma. LE was slowly hydrolyzed by paraoxonase in human plasma to 17α-monoester with a half-life of 12?h, but by carboxylesterase in rat plasma to yield undetectable products, presumed to include the unstable 17β-monoester.

  相似文献   
10.
目的 :对氯替泼诺控制眼部炎症的有效性和安全性进行系统评价。方法 :检索MEDLINE获得 8篇以往发表的论文 ,并根据临床和统计标准进行合并分析。通过计算优势比来评估氯替泼诺治疗的安全性和有效性 ,并按照固定效应模型对优势比进行合并。结果 :总计 1 660例病人纳入荟萃分析。与安慰剂和泼尼松龙相比 ,眼内压升高的合并危险差分别为 1 % (95 %可信区间 ,-1 % ,3 % ) ,-5 % (95 %可信区间 ,-9% ,0 % )。与安慰剂相比 ,炎症控制的合并危险差分别为 :术后炎症 3 1 %(95 %可信区间 ,2 2 % ,40 % ) ,春季结膜炎 2 8%(95 %可信区间 ,1 9% ,3 7% ) ,过敏性结膜炎 2 6%(95 %可信区间 ,1 8% ,3 5 % ) ;而与泼尼松龙相比 ,急性前葡萄膜炎控制的合并危险差为 -1 5 %(95 %可信区间 ,-2 5 % ,-4% )。结论 :氯替泼诺可以控制眼部炎症 ,如 :术后炎症、春季结膜炎、过敏性结膜炎、急性前葡萄膜炎 ,是既有效又安全的糖皮质激素  相似文献   
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