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BMC Ophthalmology Nov 2019To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on...
BACKGROUND
To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells.
METHODS
A Methylthiazolyltetrazolium(MTT)-based calorimetric assay was used to assess cytotoxicities using HCECs at concentrations of 10, 20 or 30% for exposure durations of 30 min, 1 h, 2 h, 12 h or 24 h. Cellular morphologies were evaluated by inverted phase-contrast and electron microscopy. Wound widths were measured 2 h, 18 h, or 24 h after confluent HCECs monolayers were scratched. Realtime PCR was used to quantify anti-allergic effects on cultured human conjunctival cells, in which allergic reactions were induced by treating them with Aspergillus antigen.
RESULTS
Cell viabilities decreased in time- and concentration-dependent manners. Cells were detached from dishes and showed microvilli loss, cytoplasmic vacuoles, and nuclear condensation when exposed to antiallergic agents; alcaftadine was found to be least cytotoxic. Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001). All agents significantly reduced the gene expressions of allergic cytokines (IL-5, IL-25, eotaxin, thymus and activation-regulated chemokine, and thymic stromal lymphopoietin) and alcaftadine had the greatest effect (p < 0.0001 in all cases).
CONCLUSIONS
Alcaftadine seems to have less side effects and better therapeutic effects than the other two anti-allergic agents tested. It may be more beneficial to use less toxic agents for patients with ocular surface risk factors or presumed symptoms of toxicity.
Topics: Anti-Allergic Agents; Benzazepines; Cell Survival; Cells, Cultured; Conjunctiva; Cornea; Epithelial Cells; Humans; Imidazoles; Olopatadine Hydrochloride; Piperidines; Pyridines
PubMed: 31703568
DOI: 10.1186/s12886-019-1228-5 -
Clinical, Cosmetic and Investigational... 2012The long-term follow-up of chronic urticaria (CU) is important to ensure the adequate treatment of patients. Olopatadine hydrochloride is one of the second-generation...
BACKGROUND
The long-term follow-up of chronic urticaria (CU) is important to ensure the adequate treatment of patients. Olopatadine hydrochloride is one of the second-generation nonsedating antihistamines.
METHODS
This study was designed to assess the optimal dose of olopatadine to suppress symptoms of chronic urticarial itch in well-controlled patients. After CU patients were treated with 10 mg olopatadine, patients having a visual analog scale (VAS) itch score of less than 20 were randomly allocated into one of three groups: 10 mg/day (n = 35), 5 mg/day (n = 30), or no medication (n = 32).
RESULTS
The suppressive effects of both the 5 mg and 10 mg olopatadine treatments on the VAS itch score were more significant and longer lasting over a period of 4 weeks than the no-medication treatment. Both the 5-mg group and the 10-mg group showed improved urticarial symptoms and maintained their VAS itch score within normal limits compared to the no-medication group. The differences between the 5-mg and 10-mg groups were not significant.
CONCLUSION
These results demonstrate that treatment with olopatadine at a dose of 5 mg once daily is effective and safe for the management and prevention of CU symptoms for itch in well-controlled patients.
PubMed: 23055763
DOI: 10.2147/CCID.S36812 -
Annals of Allergy, Asthma & Immunology... Oct 2021Birch pollen is a prevalent aeroallergen during the springtime allergy season. In field studies, variable allergen exposure and environmental factors can affect data... (Observational Study)
Observational Study
BACKGROUND
Birch pollen is a prevalent aeroallergen during the springtime allergy season. In field studies, variable allergen exposure and environmental factors can affect data quality while environmental exposure units (EEUs) deliver controlled, standardized, and reproducible allergen exposures.
OBJECTIVE
To inform study design for EEU trials evaluating antiallergic therapies.
METHODS
In this prospective study, 76 participants with birch allergy experienced 3 exposures to birch pollen: (1) an out-of-season EEU challenge (two 3-hour sessions on consecutive days); (2) a natural seasonal exposure; and (3) an in-season EEU challenge (3-hour exposure for 2 weeks after birch pollen season initiation).
RESULTS
The total nasal symptom score, total ocular symptom score, and total symptom score (TSS = total nasal symptom score plus total ocular symptom score) were assessed every 30 minutes and daily during EEU and natural exposures. A high association between TSSs and day 2 of the out-of-season and in-season EEU challenges was noted, with a good association between the maximum TSS during the natural and in-season EEU challenges, and natural season and day 2 of the out-of-season EEU challenge (P < .001 for all). Participants had higher maximum change from the baseline TSS during day 2 of the out-of-season EEU challenge (12.4) vs the following: (1) first day (9.8); (2) in-season EEU challenge (8.4); and (3) natural seasonal exposure (7.6) (P < .001 for all).
CONCLUSION
A strong association was seen between the presence of allergy symptoms and exposure to birch pollen in the EEU (maximum change in symptom scores during day 2) and in the field. A hybrid trial design may be useful to demonstrate the clinical efficacy of novel antiallergic therapies requiring fewer participants and shorter timelines and expediting treatment availability.
Topics: Adult; Allergens; Anti-Allergic Agents; Betula; Cetirizine; Environmental Exposure; Female; Humans; Male; Mometasone Furoate; Olopatadine Hydrochloride; Pollen; Prospective Studies; Rhinitis, Allergic, Seasonal; Seasons; Severity of Illness Index
PubMed: 34186172
DOI: 10.1016/j.anai.2021.06.015 -
Romanian Journal of Ophthalmology 2016To report the case of a 14-year-old male patient, with bilateral atopic keratoconjunctivitis with corneal ulcer. The patient complained of bilateral red, itchy eyes,...
To report the case of a 14-year-old male patient, with bilateral atopic keratoconjunctivitis with corneal ulcer. The patient complained of bilateral red, itchy eyes, decreased vision, photophobia, difficulty opening the eyelids upon awakening, palpebral edema, excessive tearing, along with yellowish mucous discharge. He had a two-year history of chronic blepharitis and recurrent episodes of conjunctivitis that were treated with Tobramycin and corticosteroid eye drops over the years. The patient's past medical history was significant for atopic dermatitis (AD) and he had a family history for atopy. At the eye exam: his best-corrected visual acuity at the initial presentation was 0.2 in the right eye and 1.0 in the left eye. The following elements were found upon the slit lamp biomicroscopy: Eyelids - +4 palpebral edema (pseudoptosis), Dennie-Morgan fold and Herthoge's sign were both present, tylosis; Conjunctiva - hyperaemia, cobblestone appearance of the tarsal papillae in both eyes, +2 chemosis; Cornea - corneal edema with a 8 mm × 4 mm epithelial defect in the inferior part of the cornea, covered partially by the lied, that stained positive with fluorescein dyes. Using the Evaluation Signs Severity for Allergic Ocular Diseases, a diagnosis of bilateral atopic keratoconjunctivitis with a grade 3 status for the right eye and a grade 2 status, was made. It was decided that he should be administered Olopatadine hydrochloride and Sodium cromoglicate eye drops, along with Moxifloxacin and steroid eye drops. The microbiological exam tested positive for staphylococcus aureus, and, based on the sensitivity pattern, Chloramphenicol eye drops had to be added to the treatment. After 2 weeks, his symptoms diminished, pain was significantly relieved and inflammation was markedly reduced, but the corneal ulcer persisted. In order to prevent corneal perforations, amniotic membrane transplantation (AMT) was used to promote epithelialization. A month later, the epithelial defect healed smoothly in an underlying vascular stromal scar and the visual acuity improved to 0.4 RE. This case demonstrated the role of patient history and close clinical obser-vation in the diagnosis of AKC. As this case showed, the use of topic medication along with amniotic membrane transplantation (AMT) was successful in the treatment of atopic keratoconjunctivitis and secondary staphylococcal aureus keratitis.
Topics: Administration, Ophthalmic; Adolescent; Anti-Allergic Agents; Anti-Asthmatic Agents; Anti-Bacterial Agents; Blepharitis; Conjunctivitis, Allergic; Corneal Ulcer; Cromolyn Sodium; Dermatitis, Atopic; Drug Therapy, Combination; Eye Infections, Bacterial; Fluoroquinolones; Glucocorticoids; Humans; Male; Moxifloxacin; Olopatadine Hydrochloride; Ophthalmic Solutions; Staphylococcal Infections; Staphylococcus aureus
PubMed: 29450349
DOI: No ID Found -
Cellular Physiology and Biochemistry :... 2015Besides its anti-allergic properties as a histamine receptor antagonist, olopatadine stabilizes mast cells by inhibiting the release of chemokines. Since olopatadine...
BACKGROUND/AIMS
Besides its anti-allergic properties as a histamine receptor antagonist, olopatadine stabilizes mast cells by inhibiting the release of chemokines. Since olopatadine bears amphiphilic features and is preferentially partitioned into the lipid bilayers of the plasma membrane, it would induce some morphological changes in mast cells and thus affect the process of exocytosis.
METHODS
Employing the standard patch-clamp whole-cell recording technique, we examined the effects of olopatadine and other anti-allergic drugs on the membrane capacitance (Cm) in rat peritoneal mast cells during exocytosis. Using confocal imaging of a water-soluble fluorescent dye, lucifer yellow, we also examined their effects on the deformation of the plasma membrane.
RESULTS
Low concentrations of olopatadine (1 or 10 µM) did not significantly affect the GTP-γ-S-induced increase in the Cm. However, 100 µM and 1 mM olopatadine almost totally suppressed the increase in the Cm. Additionally, these doses completely washed out the trapping of the dye on the cell surface, indicating that olopatadine counteracted the membrane surface deformation induced by exocytosis. As shown by electron microscopy, olopatadine generated inward membrane bending in mast cells.
CONCLUSION
This study provides electrophysiological evidence for the first time that olopatadine dose-dependently inhibits the process of exocytosis in rat peritoneal mast cells. Such mast cell stabilizing properties of olopatadine may be attributed to its counteracting effects on the plasma membrane deformation in degranulating mast cells.
Topics: Animals; Anti-Allergic Agents; Cell Degranulation; Cell Membrane; Cells, Cultured; Dibenzoxepins; Exocytosis; Fluorescent Dyes; Male; Mast Cells; Membrane Potentials; Microscopy, Confocal; Microscopy, Electron; Olopatadine Hydrochloride; Patch-Clamp Techniques; Peritoneum; Rats; Rats, Wistar
PubMed: 25591779
DOI: 10.1159/000369704 -
Dermatology Research and Practice 2010Effects of olopatadine hydrochloride, a histamine H(1) receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with...
Effects of olopatadine hydrochloride, a histamine H(1) receptor antagonist, on histamine-induced skin responses were evaluated in 10 healthy subjects in comparison with placebo, fexofenadine hydrochloride, and bepotastine besilate. Olopatadine significantly suppressed histamine-induced wheal, flare, and itch, starting 30 minutes after oral administration. Olopatadine was more effective than fexofenadine and bepotastine. None of the drugs studied impaired performance of word processing tasks. These results suggest that olopatadine can suppress skin symptoms caused by histamine soon after administration.
PubMed: 20886023
DOI: 10.1155/2010/638051 -
The World Allergy Organization Journal Feb 2013To identify the incidence of allergic conjunctivitis in patients with allergic rhinitis.
AIMS
To identify the incidence of allergic conjunctivitis in patients with allergic rhinitis.
METHODS
One hundred and eighty seven consecutive patients with allergic rhinitis (AR) were directly questioned if they have allergic conjunctivitis (AC) and this was clarified using standard screening questions relating to red, itchy and watery eyes recorded through a total ocular symptom score (TOSS). Patients were also asked about further symptoms that may be attributable to AC: eyelid dermatitis, frequent blinking; eye sensitivity and frontal headache from squinting or. blinking. All patients were given a drop of olopatadine hydrochloride 0.1% in each eye to help identify "silent" disease. 20 healthy non-atopic controls were also treated with olopatadine drops and questioned on ocular symptoms.
RESULTS
Fifty five percent of patients with AR were identified as having AC by direct questioning and the use of the TOSS questionaire. A further 41% were identifiable by asking additional questions and performing therapeutic challenge with olopadatine.
CONCLUSIONS
AC is a frequent comorbid condition occurring in 95% of our patients with AR. Only 55% of patients were able to identify that they had AC based on standard screening questions. Additional specific questioning and a therapeutic challenge in suspected patients can help identify patients who may benefit from treatment of AC.
PubMed: 23663473
DOI: 10.1186/1939-4551-6-4 -
BMC Ophthalmology Jul 2009Benzalkonium chloride (BAC) is a common preservative used in ophthalmic solutions. The aim of this study was to compare the cytotoxic effects of BAC-containing...
BACKGROUND
Benzalkonium chloride (BAC) is a common preservative used in ophthalmic solutions. The aim of this study was to compare the cytotoxic effects of BAC-containing ophthalmic solutions with a BAC-free ophthalmic solution using an organotypic 3-dimensional (3-D) corneal epithelial model and to determine the effects of latanoprost ophthalmic solution and its BAC-containing vehicle on corneal thickness in a monkey model.
METHODS
The cytotoxicity of commercially available BAC-containing ophthalmic formulations of latanoprost (0.02% BAC) and olopatadine (0.01% BAC) was compared to that of BAC-free travoprost and saline in a corneal organotypic 3-D model using incubation times of 10 and 25 minutes. To compare the extent of differentiation of 3-D corneal cultures to monolayer transformed human corneal epithelial (HCE-T) cell cultures, expression levels (mRNA and protein) of the corneal markers epidermal growth factor receptor, transglutaminase 1 and involucrin were quantified. Finally, latanoprost ophthalmic solution or its vehicle was administered at suprapharmacologic doses (two 30 microL drops twice daily in 1 eye for 1 year) in monkey eyes, and corneal pachymetry was performed at baseline and at weeks 4, 13, 26 and 52.
RESULTS
In the 3-D corneal epithelial culture assays, there were no significant differences in cytotoxicity between the BAC-containing latanoprost and olopatadine ophthalmic solutions and BAC-free travoprost ophthalmic solution at either the 10- or 25-minute time points. The 3-D cultures expressed higher levels of corneal epithelial markers than the HCE-T monolayers, indicating a greater degree of differentiation. There were no significant differences between the corneal thickness of monkey eyes treated with latanoprost ophthalmic solution or its vehicle (both containing 0.02% BAC) and untreated eyes.
CONCLUSION
The lack of cytotoxicity demonstrated in 3-D corneal cultures and in monkey studies suggests that the levels of BAC contained in ophthalmic solutions are not likely to cause significant direct toxicity to epithelium of otherwise normal corneas.
Topics: Animals; Anti-Allergic Agents; Antihypertensive Agents; Benzalkonium Compounds; Cell Line; Cloprostenol; Dibenzoxepins; Drug Evaluation; Epithelium, Corneal; Humans; Latanoprost; Macaca fascicularis; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Preservatives, Pharmaceutical; Prostaglandins F, Synthetic; Time Factors; Travoprost
PubMed: 19638217
DOI: 10.1186/1471-2415-9-5 -
Allergy, Asthma, and Clinical... 2020MP-AzeFlu is relatively new a pharmaceutical drug used in the treatment of allergic rhinitis. It is comprised of azelastine hydrochloride (AZE), a potent...
MP-AzeFlu is relatively new a pharmaceutical drug used in the treatment of allergic rhinitis. It is comprised of azelastine hydrochloride (AZE), a potent histamine-H1-receptor antagonist and fluticasone propionate (FP), corticosteroid. It's somewhat bitter taste (often considered a disadvantage) can be attributed to AZE. We here hypothesize that MP-AzeFlu may induce some of its beneficial effects through activation of bitter taste receptors (Tas2R), which have recently been described in human airways. In the nose Tas2Rs induce secretion of antimicrobial peptides and increase ciliary activity, while in the lung they cause airway smooth muscle relaxation. The mechanisms behind Tas2R-mediated effects are not yet fully known. In order to evaluate the role of Tas2R in the effects induced by MP-AzeFlu the dilatory response of pre-contracted isolated airways from Balb/c mice was investigated in tissue bath myographs in the presence or absence of various well-characterized pharmacological antagonists or their corresponding vehicles. MP-AzeFlu caused a potent dose-dependent relaxation of pre-contracted airways, an effect probably mediated by its AZE component. The dilatory effect of MP-AzeFlu and AZE both mimicked the response induced by the Tas2R agonist, chloroquine, but was independent of histamine receptor (H1-, H2- and H3-), prostaglandins, cAMP and cGMP involvement, all known to be common pathways for airway dilation. Other bitter-tasting antihistamines (i.e. olopatadine and desloratadine) also relaxed airway segments. These data support the notion that MP-AzeFlu has the ability to activate Tas2R in the same way as chloroquine. The effect appears to be mediated by AZE, but not via the histamine receptor. Activation of Tas2R by MP-AzeFlu may contribute to its superior efficacy over FP observed in controlled clinical trials in patients with moderate/severe allergic rhinitis.
PubMed: 32514276
DOI: 10.1186/s13223-020-00438-w -
Indian Journal of Ophthalmology May 2023The main objective of this study is to explore the efficacy of olopatadine 0.1% treatment in the resolution of symptoms of vernal keratoconjunctivitis (VKC) among the...
Assessment of the efficacy of olopatadine 0.1% in the treatment of vernal keratoconjunctivitis in terms of clinical improvement based on total ocular symptom score and ocular surface disease index.
PURPOSE
The main objective of this study is to explore the efficacy of olopatadine 0.1% treatment in the resolution of symptoms of vernal keratoconjunctivitis (VKC) among the Indian population.
METHODS
This single-center, prospective cohort study involved 234 patients with VKC. Patients were treated with olopatadine 0.1%, twice daily for a period of 12 weeks and then followed up in 1 week, 4 week, 3 month, and 6 month. The extent of relief in the symptoms of VKC was measured using total ocular symptom score (TOSS) and ocular surface disease index (OSDI).
RESULTS
In the present study, the dropout rate was 5.6%. Total of 136 males and 85 females with a mean age of 37.68 ± 11.35 years completed the study. TOSS score reduced from 58.85 to 5.06 and the OSDI score reduced from 75.41 to 11.2 with statistical significance (P < 0.01) from 1 week to 6 week after olopatadine 0.1% treatment. The data showed relief in subjective symptoms of itching, tearing, and redness, and relief in discomfort in functions related to ocular grittiness, visuals like reading, and environmental like tolerability in dry conditions. Further, olopatadine 0.1% was effective in both males and females, and patients across ages 18-70 years.
CONCLUSION
Based on TOSS and OSDI scores, the findings of this study validate safety and tolerability as revealed by low adverse effects and moderate efficacy of olopatadine 0.1% in reducing VKC symptoms in a broader age group (18-70 years) of both genders.
Topics: Humans; Female; Male; Adult; Middle Aged; Adolescent; Young Adult; Aged; Olopatadine Hydrochloride; Conjunctivitis, Allergic; Prospective Studies; Dibenzoxepins; Eye; Ophthalmic Solutions
PubMed: 37203036
DOI: 10.4103/ijo.IJO_2048_22