Diclofenac Sodium Eye Drops Research Articles

Supramolecular nanofiber of indomethacin derivative confers highly cyclooxygenase-2 (COX-2) selectivity and boosts anti-inflammatory efficacy

Herein, we report a facile method for converting carboxylate-containing indomethacin (Idm) into a cyclooxygenase-2 (COX-2) selective inhibitor via the amidation of an unnatural peptide sequence (Nal-Nal-Asp). The resulting indomethacin amides (i.e., Idm-Nal-Nal-Asp) have high selectivity for COX-2, and can self-assemble into a one-component supramolecular hydrogel that acts as a ‘self-delivery’ system for boosting anti-inflammatory efficacy. Self-assembled Idm-Nal-Nal-Asp hydrogel robustly inhibits COX-2 expression in lipopolysaccharide (LPS)-activated Raw 264.7 macrophages while also exhibits superior anti-inflammatory and antioxidant activities via reactive oxygen species (ROS)-related NF-κB and Nrf2/HO-1 pathways. Moreover, a rabbit model of endotoxin-induced uveitis (EIU) reveals that the Idm-Nal-Nal-Asp hydrogel outperforms clinically used 0.1 wt% diclofenac sodium eye drops in terms of in vivo anti-inflammatory efficacy via topical instillation route. As a rational approach to designing and applying COX-2 selective inhibitors, this work presents a simple method for converting non-selective nonsteriodal anti-inflammatory drugs (NSAIDs) into highly selective COX-2 inhibitors that can self-assemble into supramolecular hydrogel for anti-inflammation applications.

Antibacterial effect of povidone iodine disinfectant and antibiotic eye drops before cataract surgery

Objective: Investigate the distribution of bacteria in the conjunctival sac of two groups of cataract patients with different preoperative aseptic treatments, and compare the clinical effects of 0.5% povidone-iodine (PI) and antibiotic eye drops on killing conjunctival sac bacteria.Methods: 400 cases of patients (400 eyes) who underwent cataract surgery in the Department of Ophthalmology of Baogang Hospital in Inner Mongolia from October 2019 to October 2020 were selected in a randomized controlled study. They were randomly divided into the experimental group (group A) and the control group (group B), with 200 cases in each group. Group A: the patients were given Gatifloxacin Eye Gel (3 times/day, 1 drop/time) combined with Diclofenac Sodium Eye Drops (4 times/day, 1 drop/time) before the operation; 0.5% PI was administered to irrigate the conjunctival sac, with 0.9% SodiumChloride Injection washing after 3 min; 0.5% PI was administered to irrigate the conjunctival sac after operation. The corneal epithelium was observed after each irrigation. Group B: the patients were given Gatifloxacin Eye Gel (3 times/day, 1 drop/time) combined with Diclofenac Sodium Eye Drops (4 times/day, 1 drop/time) 2 days and 1 day before the operation; 0.9% Sodium Chloride Injection was administered to irrigate the conjunctival sac before and after surgical disinfection. Conjunctival sac specimens were collected for bacterial culture 2 hours before the operation, after irrigation, and after the procedure. The positive rate and the distribution of bacteria were compared between the two groups.Results: The difference in the positive rate of bacteria in the conjunctival sac between the two groups at different time points had a statistical significance (χ2 = 11.498, p < .022). Conjunctival sac specimens were collected on admission and 2 hours before the operation. There was no significant difference in the pathogens with positive results between the two groups (p = .955; p = .073); there was a substantial difference in the distribution of positive pathogens between the two groups before and after surgical disinfection (p < .001); there was a significant difference in the distribution of pathogens between the two groups after the operation (p = .005). For Staphylococcus epidermidis, Corynebacterium, Enterococcus faecalis, Streptococcus, and other Gram-positive bacteria, there was a significant difference in the disinfection methods between the two groups at different time points (p < .001); for Staphylococcus aureus, Gram-positive cocci, and Gram-negative bacteria, there was no significant difference in the disinfection methods between the two groups at different time points (p = .113; p = .224; p = .146). There was no significant difference between the two groups with 0-10 and 101-1000 bacterial colonies at different time points (p = .370 and .071, respectively). When there were 11-100 bacterial colonies, there was a significant difference between the two groups at different time points (p < .001). There was no significant difference in corneal epithelial injury between the two groups at other time points (χ2 = 4.133, p = .127).Conclusions: The combination of 0.5% PI disinfectant and antibiotic eye drops can effectively reduce the bacterial load of the conjunctival sac before operation. At the same time, it is safe and effective to irrigate the conjunctival sac with 0.5% PI disinfectant before the procedure.

Comparative Assessment of Short-Term Tendon-Scleral Postoperative Inflammation and α-Smooth Muscle Actin Expression following Oral and Topical Diclofenac Administration for Strabismus Surgery in Rabbits

PurposeWound healing and fibrosis modulation are considered pivotal for the long-term outcome of strabismus surgery. Nonsteroidal anti-inflammatory drugs, including diclofenac sodium, are inflammation suppressive drugs that may modulate wound healing, including postoperative inflammation. This study aimed to compare the effect of oral and 0.1% topical diclofenac sodium on short-term inflammation and α-smooth muscle actin (α-SMA) expression at the tendon-scleral attachment site following strabismus surgery in an experimental rabbit model.MethodsSuperior rectus recession was performed in 12 eyes of six New Zealand rabbits. Rabbits were divided into three groups: oral diclofenac 2 × 5 mg/kg for three days (group A), 0.1% diclofenac sodium eye drops 3 times/day for three days (group B), and controls (group C). On postoperative day 14, enucleation was performed. Macroscopic adhesion score, microscopic adhesion score, percentage of postoperative inflammation area (Masson’s trichrome staining), and α-SMA (immunohistochemistry staining) were assessed. Data analysis was performed using a semi-quantitative and quantitative assessment with ImageJ. All groups were compared with reciprocal staining intensity (RSI) values to measure α-SMA expression.ResultsAll groups showed no difference in macroscopic (p = 0.13) and microscopic adhesion scores (p = 0.28). The percentage of postoperative inflammation area in group B (12.44% (8.63–18.29)) was significantly lower than group A (26.76% (21.38–37.56) p = 0.03) and group C (27.80% (16.42–36.28), p = 0.04). Comparative RSI analysis found that group B had a significantly lower α-SMA expression than group C (174.08 ± 21.78 vs 212.58 ± 12.06, p = 0.04).ConclusionThe results suggest that compared to oral, the administration of topical diclofenac showed a more significant reduction of short-term postoperative inflammation and α-SMA expression at the tendon-scleral attachment site following strabismus surgery.

Cyclosporine (0.05%) Combined with Diclofenac Sodium Eye Drops for the Treatment of Dry Eye Disease.

Objective To assess the clinical efficacy of cyclosporine (0.05%) combined with diclofenac sodium eye drops (0.1%) in the treatment of dry eye disease. Methods A prospective analysis was performed on clinical information of 128 patients diagnosed with dry eye at the ophthalmic clinic of the General Hospital of Xinjiang Military Command of the Chinese People's Liberation Army from August 2020 to August 2021. Specifically, patients were randomly divided into a control group and a study group. In addition to conventional treatment, patients in the control group were treated with cyclosporine (0.05%) eye drops; while in the study group, patients received cyclosporine (0.05%) combined with diclofenac sodium eye drops (0.1%). Subsequently, comparisons and analysis were performed before and after treatment between the two groups in the clinical symptom questionnaire score of dry eye disease, the corneal fluorescein staining (CFS) score, determination of tear film break-up time (BUT), Schirmer I test (SIT) score, and curative effect. Results After treatment, the clinical symptom scores and CFS scores were decreased while the BUT and SIT scores were increased in both groups; besides, compared with the control group, the clinical symptom scores and CFS scores were much lower while the BUT and SIT scores were higher in the study group. Moreover, the overall response rate in the study group (96.9%) was much better than that in the control group (79.7%); and the differences between the two groups were statistically significant (p < 0.05). Conclusion The combination of cyclosporine (0.05%) and diclofenac sodium eye drops (0.1%) based on conventional treatment can be applied to the clinical treatment of dry eye disease due to its good clinical effects on relieving dry eye symptoms.

Clinical Analysis of Oral Loratadine Combined with Diclofenac Sodium Eye Drops in the Treatment of Allergic Conjunctivitis

Clinical Analysis of Oral Loratadine Combined with Diclofenac Sodium Eye Drops in the Treatment of Allergic Conjunctivitis

Enzyme-instructed self-assembly of peptide-drug conjugates in tear fluids for ocular drug delivery

In vivo self-assembly of small molecules offers an excellent opportunity for targeted and long-term accumulation of a therapeutic agent at the lesion site. Here we demonstrate the strategy of enzyme-instructed self-assembly (EISA) by designing a phosphorylated peptide-drug (IBF-HYD-GFFpY) precursor through the ester bond to release active drugs at the target site. Meanwhile, the in vivo assembly can be achieved by the catalysis of alkaline phosphatase (ALP) in the tear fluid for ocular drug delivery efficiently. The in vitro enzymatic experiments indicate that the dephosphorylation of IBF-HYD-GFFpY occurs firstly with the yield of IBF-HYD-GFFY which subsequently self-assembles into the supramolecular hydrogel to afford sustained drug release over 96 h. In the treatment of lipopolysaccharide (LPS)-activated Raw 264.7 macrophages, IBF-HYD-GFFpY exerts the more potent anti-inflammatory efficacy than that of free ibuprofen (IBF) at the concentration of 200 μM. Moreover, the aqueous solution of IBF-HYD-GFFpY via topical instillation hardly causes ocular irritation, and displays longer precorneal retention compared to the conventional eye drop formulation. In addition, in the in vivo study, a rabbit model of endotoxin-induced uveitis (EIU) evidences the comparable therapeutic efficacy of IBF-HYD-GFFpY eye drops with that of clinically used 0.1 wt% diclofenac (DIC) sodium eye drops by the reduction of macrophage and leukocyte influx. This work, in situ EISA in the tear microenvironment directing in vivo self-assembly of small molecules, may guide a powerful approach for developing enzymatic self-assembled molecules as an efficient delivery system of ocular drugs.

Macular Alteration of Topical Diclofenac Sodium after Phacoemulsification Surgery in Diabetic Patients

BACKGROUND: Cystoid macular edema (CME) is a serious complication of cataract surgery in a diabetic patient. CME was found 1–19% after phacoemulsification surgery. Nonsteroidal anti-inflammatory drugs inhibit cyclooxygenase-1, cyclooxygenase-2, and endoperoxides. Inhibition of these enzymes also reduces macular thickening. AIM: The aim of the study was to assess macular thickness alteration after application of 1.00 mg diclofenac sodium eye drops in diabetic patients who receive phacoemulsification surgery. METHODS: This study was a quasi-experimental study. A total of 40 eyes diabetic retinopathy patients having phacoemulsification surgery were randomized to 100 mg diclofenac sodium (n = 20) or placebo eye drops (n = 20), three drops daily on 1 day before surgery until 30 days post-operative. The main outcome measures macular thickness using Ocular Coherence Tomography before and after (14 and 30 days) phacoemulsification. RESULTS: Utilizing an independent t-test, this study had significantly inner macular (p = 0.0001) and central macular (p = 0.008) thickness differences in the diclofenac sodium group during surgery until 14 days postoperatively. However, significant changes in the outer macular thickness were absent. There were no notable alterations in the center, inner, and outer macular thickness in the diclofenac sodium group until 30 days postoperatively. In the placebo group, no significant changes were found in the macular thickness at every point of time. CONCLUSION: Two statistically significant central and inner macular thicknesses in the diclofenac sodium group until 14 days postoperatively were present. There were no significant changes in the center, inner, and outer macular thickness in the diclofenac sodium group until 30 days postoperatively.

Clinical value of Loratadine combined with Diclofenac sodium eye drops in the treatment of allergic conjunctivitis

Clinical value of Loratadine combined with Diclofenac sodium eye drops in the treatment of allergic conjunctivitis

双氯芬酸钠滴眼液与翼状胬肉中增殖细胞核抗原表达水平的关系

双氯芬酸钠滴眼液与翼状胬肉中增殖细胞核抗原表达水平的关系

Clinical observation on intracorneal injection of different anti-fungal drugs for the treatment of fungal keratitis caused by injury due to chestnut

Objective To observe the clinical efficacy of injection of different anti-fungal drugs in corneal stroma for the treatment of fungal keratitis caused by injury due to chestnut stab. Methods Eighty-three eyes of 83 cases of fungal keratitis caused by chestnut were randomly divided into three groups. The etiological results of all cases were obtained by fungal culture. After corneal debridement, patients in group A, group B and group C received the injection of fluconazole, amphotericin B and voriconazole in corneal stroma respectively on the basis of using 5% natamycin eye drops. The effect of the treatments for the three groups were observed. Results The first pathogenic bacteria was the Alternaria of the pathogen accounting for 34.9% (29 cases), followed by Fusarium 30.1% (25 cases) and Aspergillus 15.7% (13 cases). The cure rates of three groups were 70.3% (19/27), 76% (18/25) and 90.3% (28/31) respectively. The average cure rate of group C was higher than that of group A and B, and the differences were statistically significant (χ2=5.349, 4.895; P=0.021, 0.027). There was no statistically significant difference in the cure rate between group A and B (χ2=0.027, P=0.869). The cure time of group C was (22.48±8.36)d which was shorter than that of group A (27.40±3.97)d and group B (28.76±5.12)d and the differences were statistically significant (t=2.544, 3.006; P=0.014, 0.004). There was no statistically significant difference in the cure time between group A and B (t=1.069, P=0.290). Two cases in group B suffered eye irritation symptoms, and the symptom disappeared after the use of Diclofenac Sodium eye drops for two days. No adverse reactions during the treatment occurred in the remaining cases. All cases were followed up for 1-3 months and no puncture tract scar formed or no recurrent case happened. Conclusion The main pathogenic bacteria of fungal keratitis by chestnut stab are Alternaria and Fusarium. The injection of fluconazole, amphotericin B and voriconazole respectively in corneal stroma can bring better curative effect, especially the voriconazole and for severe cases the curative effect of voriconazole is better than that of fluconazole and amphotericin B. Key words: Keratitis, fungal; Chestnut stab; Etiological examination; Antifungal drugs; Injection, in corneal stroma

Clinical research of loratadine and diclofenac sodium eye drops for allergic conjunctivitis

Clinical research of loratadine and diclofenac sodium eye drops for allergic conjunctivitis

Cytotoxicity research of three non-steroidal anti-inflammatory eye drops in human corneal epithelial cells

Background Diclofenac sodium eye drops, pranoprofen eye drops and bromfenac sodium hydrate eye drops are three clinical commonly used nonsteroidal anti-inflammatory drugs(NSAIDs). The variation of cytoxicity among these drugs and whether the cytoxicity is related to the supplements are also unknown. Objective This study was to compare the cytotoxicity of three non-steroidal anti-inflammatory eye drops and their active components with cultured human corneal epithelial cells (HCECs) in vitro, and to discuss toxic origins of these drugs. Methods HCECs were cultured in different drugs with the final concentration of 0.10%, 0.05%, 0.02% and 0.01%. Cell proliferation was evaluated by MTT assay. Then, 0.002% eye drops (1∶50) was added, and the migration and damage of the cells were deceted by transwell migration assay and lactate dehydrogenase (LDH) assay. Results The cytotoxicity of three nonsteroidal anti-inflammatory eye drops on HCECs was concentration-dependent (all at P=0.00). Diclofenac sodium eye drops showed the most dominant effects on the proliferation, migration and damage of HCECs among the three eye drops, while bromfenac sodium eye drops showed the least effect on the cell damage (proliferation: Fdrug=20.25, P=0.00; migration: F=103.43, P=0.00; damage: Fdrug=164.16, P=0.00). Compared with the eye drops, their active components showed less cytoxicity. Pranoprofen appeared the least effects on the proliferation, migration and damage of HCECs (proliferation: Fdrug=332.27, P=0.00; migration: F=332.27, P=0.00; damage: Fdrug=154.83, P=0.00). Conclusions The cytotoxicity of diclofenac sodium eye drops is more obvious than that of pranoprofen eye drops or bromfenac sodium hydrate eye drops. The cytotoxicity of the three eye drops originates from their supplements or the interaction between the supplements and active components. Key words: Non-steroidal anti-inflammatory eye drops; Cytotoxicity; Active components; Supplements

Clinical observation of diclofenac sodium eye drops for postoperative recurrence of pterygium

Clinical observation of diclofenac sodium eye drops for postoperative recurrence of pterygium

Development and evaluation of fast forming nano-composite hydrogel for ocular delivery of diclofenac

In this paper, a fast forming nano-composite hydrogel was developed for potential application in ocular drug delivery. The optical transmission (OT) as well as rheological properties of nano-composite hydrogel was characterized. The developed nano-composite hydrogel given a high diclofenac micelles loading and provided a sustained release manner of diclofenac within 6h. The developed nano-composite hydrogel formulation was administrated into the eye as flowable solution, quickly forming a hydrogel that is able to resist of the blinking and flushing of tear, yet resulting in the prolonged residence time of pre-corneal. In vivo eye irritation test suggested that the developed nano-composite hydrogel was none-eye irritation might be suitable for various ocular applications. In vivo pharmacokinetic study indicated that the developed nano-composite hydrogel could significantly increase the bioavailability of diclofenac and maintain the concentration of diclofenac in aqueous humor above MEC at least 24h after administration as compared with that of the commercial diclofenac sodium eye drops, which might be able to reduce the frequency of administration for patients.

Contrast Sensitivity and Eye Drops

Purpose: To evaluate the influence of commonly used eye drops on contrast sensitivity (CS). Design: Prospective study. Participants: One hundred twenty volunteers (120) were enrolled. Methods: The CS of ophthalmologically healthy individuals was evaluated at baseline examination before the instillation, 20 and 40 minutes after the instillation of diclofenac sodium and commonly used antiglaucoma eye drops (latanoprost, brimonidine tartrate, combination of dorzolamide hydrochloride and timolol maleate). CS was assessed at 7 spatial frequencies varying from 1.5 c/d to 20 c/d by the use of Mentor B-VAT II-SG video acuity tester. Results: Diclofenac sodium induced a mild, however statistically significant decrease on the CS in 4 out of 30 subjects 20 minutes after instillation at the spatial frequency of 1.5 c/d and 3 c/d (p p > 0.05). Brimonidine tartrate decreased CS in 4 out of 30 subjects 20 minutes after the instillation at a high spatial frequency (20 c/d) yet this decrease was marginally statistically significant (p = 0.057). CS returned to baseline scores 40 minutes after the instillation for all drugs. Conclusions: Diclofenac sodium eye drops had a mild temporal effect on the low spatial frequencies of 1.5 c/d and 3 c/d in some individuals. Latanoprost and dorzolamide/timolol had a non-statistically significant effect on the same spatial frequencies. Brimonidine eye drops had a temporal effect on the high spatial frequency of 20 c/d with marginal statistical significance. The CS scores returned to normal, in all cases, within the next 40 minutes after the instillation. Ophthalmologists should be aware of the fact that some eye drops may have an influence on CS.

Drug-drug interaction between ciprofloxacin and diclofenac ophthalmic drops at ocular level

In present times, there has been interest in multi-drug combinations for treatment of ocular infections, which are more commonly antibiotics and analgesics. Ciprofloxacin and diclofenac sodium were used concomitantly and pharmacokinetic drug-drug interactions between them were studied. To investigate disposition kinetics of ciprofloxacin eye drops (0.3%) alone and with co-administration of diclofenac sodium eye drops (0.1%) for pharmacokinetic drug-drug interaction(s). A randomized clinical trial was conducted in 84 human volunteers and the aqueous humor samples were collected from the eyes at various time intervals and concentration of ciprofloxacin in aqueous humor was determined using a validated reversed-phase high performance liquid-chromatography/ultraviolet detection method. The results were subjected to statistical analysis to determine whether a statistically significant difference was observed between the two groups. The mean age of the patients in this study ranged from 40 to 83 years, and gender distribution was 46.0% female and 54.0% males. The maximum concentration of ciprofloxacin in aqueous humor observed was 0.47 ± 0.057 µg/ml at 0.83 h. While the maximum concentration with concurrent administration of ciprofloxacin with diclofenac sodium was 0.44 ± 0.00577 µg/ml at 0.25 h. Time to reach maximum concentration was decreased to 0.3 h. t1/2abs and tα1/2 were not significantly affected by co-administration of the ciprofloxacin eye drops with the diclofenac sodium eye drops (P = 0.73), however, t1/2βwas significantly affected (P = 0.036). Similarly, apparent volume of distribution, volume of central compartment, steady-state distribution volume, AUC0-t and MRT were also significantly reduced due to concurrent administration of the diclofenac sodium eye drops with the ciprofloxacin eye drops (P = 0.021, 0.0.017, 0.05, 0.01 and 0.04). On the other hand, the ocular Clt was significantly elevated (P = 0.04), while absorption rate constant (P = 0.58) was non significantly decreased due to concurrent administration of the diclofenac sodium eye drops, while Cmax was not significantly affected. Diclofenac sodium affects the pharmacokinetics of ciprofloxacin when co-administered with ciprofloxacin eye drops. Key words: Ciprofloxacin ophthalmic drops, pharmacokinetics drug-drug interaction, aqueous humor.

Allergic contact dermatitis due to diclofenac sodium in eye drops

Eyelid dermatitis and/or periocular dermatitis (ED/PD) is commonly seen in a variety of skin diseases such as seborrheic dermatitis, atopic dermatitis and psoriasis, but is most often associated with allergic contact dermatitis (ACD). Here, a case of ACD in an 82-year-old man is described; he used 0.1% diclofenac sodium eye drops and exhibited pruritic erythema on the eyelids. Patch test for diclofenac sodium eye drops was positive. Further patch tests revealed a positive reaction to diclofenac sodium (monosodium 2-[2, 6-dichlorophenylamino] phenylacetate), which was the main component in the eye drop medicine. Diclofenac sodium is a non-steroidal anti-inflammatory drug (NSAID), and is frequently used in everyday oral medications, topical ointments, gel agents and eye drops. Case reports on ACD caused by diclofenac sodium eye drops are extremely rare. Nevertheless, it is necessary to consider ACD due to diclofenac sodium when a patient with ED/PD has a history of use of diclofenac sodium eye drops.

Effect of bromfenac ophthalmic solution on ocular inflammation following cataract surgery

This study compared the post-cataract surgery anti-inflammatory effects of topical treatment with 0.1% bromfenac, 0.1% betamethasone or both on postoperative anterior chamber inflammation and corneal swelling. Seventy-two patients with no eye disease other than cataract were enrolled in a prospective, randomized study to undergo phacoemulsification combined with intraocular lens implantation. After cataract surgery, patients were randomized to treatment with bromfenac, betamethasone or both agents. Twenty-five eyes were assigned to bromfenac, 23 to betamethasone and 24 to the combined treatment group. Inflammatory reactions in the anterior chamber were measured with laser flare photometry preoperatively and at 1 and 3 days, 1 and 2 weeks, and 1 and 2 months postoperatively. Intraocular pressure (IOP) and corneal thickness were measured at the same time-points. Best corrected visual acuity (BCVA) was measured preoperatively and at 2 days, 1 and 2 weeks, and 1 and 2 months postoperatively. Specular microscope endothelial photography of the central region of the cornea was performed preoperatively and at 3 months after surgery. There were no significant differences among the bromfenac, betamethasone and combined treatment groups in BCVA, IOP, aqueous flare or corneal thickness. Cystoid macular oedema was present in one eye treated with betamethasone. There were no significant differences in anti-inflammatory effects among the three treatments. These findings suggest that bromfenac is as effective as betamethasone in minimizing inflammatory reactions after cataract surgery.

Clinical trial of diclofenac sodium (Naclof) eye drops on Nigerians

Twenty-eight eyes of 26 age-matched patients who had planned extracapsular cataract extraction with or without intraocular lens implantation were enrolled into a double blind randomised actively controlled study of 2 groups. Each group of 14 eyes was assigned to receive 0.1% diclofenac sodium (Naclof) eye drops or 1% prednisolone acetate eye suspension. The patients received either 0.1% Diclofenac sodium eye drops or 1.0% prednisolone acetate eye suspension four times a day as their post operative anti-inflammatory medication for a period of four weeks. No significant difference was noticed in the subjective assessment of pain and conjunctival injection in the 28 days follow-up period except day 1 in the diclofenac sodium group (0.05> p >0.01). Other measured objective variables of inflammation such as anterior chamber cells and flare showed no significant difference from the 3rd-28th postoperative days (0.05< p > 0.20). The result demonstrated that 0.1% diclofenac sodium eye drops was as effective as 1% prednisolone acetate eye suspension in the control of postoperative inflammation after cataract surgery, and could serve as a viable alternative to topical steroids in Nigerians who are steroid responders.

Topical diclofenac sodium decreases the substance P content of tears.

To explore the mechanism by which diclofenac sodium eyedrops exert an adverse effect on the cornea. In 10 healthy Japanese volunteers, 0.1% diclofenac sodium solution was instilled into one eye 3 times daily for 2 weeks. Only vehicle was applied to the other eye. Tear samples were taken before drug treatment, at 2 weeks (on the final day of treatment), and at 4 weeks. Prostaglandin E(2) and substance P concentrations in tears were measured using enzyme immunoassays. After treatment for 2 weeks, concentrations of both prostaglandin E(2) and substance P in tears from diclofenac sodium-treated eyes had decreased significantly, and both had returned to baseline levels by 4 weeks. No significant changes were seen in prostaglandin E(2) and substance P levels in vehicle-treated eyes at any time points. Diclofenac sodium eyedrops concurrently reduced concentrations of prostaglandin E(2) and substance P in tears. Depletion of substance P (a pain-associated neurotransmitter) by diclofenac sodium may promote development of corneal complications.