olopatadine-hydrochloride and Conjunctivitis--Allergic

Allergic conjunctivitis (AC) is a multifactorial and common type of ocular surface disease that affects many people. The quality of life for AC patients can be significantly decreased caused by symptoms of ocular itching, swelling, redness, and tearing. Topical antihistaminics, mast cell stabilizers, non-steroidal anti-inflammatory drugs (NSAIDs), and steroids have been widely used to treat AC. Many clinical trials have indicated that olopatadine hydrochloride eye drops can provide quick relief of symptoms and signs. The purpose of this review is to evaluate systematically the effectiveness of olopatadine hydrochloride eye drops for treating AC.. A systematic review of all of the randomized controlled trials on the effectiveness and safety of olopatadine hydrochloride eye drops for AC will be conducted. We will search PubMed, Web of Science (WOS), EMBASE (OVID), the Cochrane Library, Google Scholar, China National Knowledge Infrastructure (CNKI), China Science and Technology Journal database (VIP), Wanfang Database, and CBM, from the database inception date to October 31, 2019. There are no language or publication status restrictions. Registers of clinical trials, potential gray literature, reference lists of studies, and conference abstracts will also be searched. Two reviewers will independently read the articles, extract the data information, and assess the quality of the studies. Data will be synthesized by a heterogeneity test. The primary outcomes include the main symptom and sign scores before and after treatment, the eye redness index, the presence of eosinophils in the conjunctival scraping. Quality of life, the total treatment efficacy, and safety will be evaluated as the secondary outcomes. RevMan V.5.3 software will be used for the meta-analysis.. The study will provide an objective and normative systematic review to evaluate the effectiveness and safety of olopatadine hydrochloride eye drops for the treatment of AC.. Our review will provide useful information to judge whether olopatadine hydrochloride eye drops is an effective intervention for patients with AC.. It is not necessary to obtain ethical approval as participants are not involved patients. The protocol and results will be published in a peer-reviewed journal. The systematic review will also be disseminated electronically and in print to help guide health care practice and policy.. PROSPERO CRD42019132232.

Topics: Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Quality of Life; Randomized Controlled Trials as Topic; Treatment Outcome

To address the current trends of therapeutic mechanisms for treatment of allergic conjunctivitis (AC), based on topical antihistamines and mast cell stabilizers (MCS).. The antihistamine drug alcaftadine has H4 receptor inverse agonism, anti-inflammatory and MCS activities. The antihistamines levocabastine and azelastine are more effective than placebo in treatment of AC symptoms in randomized controlled trials (RCTs). The topical dual-action antihistamines/MCS olopatadine, azelastine, ketotifen, and epinastine are commonly used in Europe and in the United States for mild subtypes of AC. For the main symptoms of AC, ocular itch and conjunctival hyperemia, epinastine 0.05% was superior to placebo, but equal or more effective than olopatadine 0.1%, while the later was more effective than ketotifen. High concentration olopatadine 0.77% had longer duration of action, better efficacy on ocular itch, and a similar safety profile to low-concentration olopatadine 0.2%. The new formulas of topical dual-action agents present longer duration of action, leading to a decreased frequency of use.. The topical dual-action agents are the most effective agents treating signs and symptoms of mild forms of AC. There is superiority to the high-concentration olopatadine drug over other agents on ocular itch, with prolonged effect when used once-daily.

Topics: Administration, Ophthalmic; Anti-Allergic Agents; Benzazepines; Conjunctivitis, Allergic; Cromolyn Sodium; Dibenzazepines; Histamine Antagonists; Humans; Hyperemia; Imidazoles; Ketotifen; Nedocromil; Olopatadine Hydrochloride; Phthalazines; Piperidines; Pruritus; Pyridines; Pyrimidinones

Olopatadine hydrochloride is an antihistamine and mast cell stabilizer available as oral, intranasal and ocular preparations. Most of the practical applications of olopatadine therapy focus on the treatment of allergic rhinoconjunctivitis via intranasal and ocular routes. Areas covered: This article was created from a comprehensive literature search with information taken from meta-analyses, systematic reviews, and clinical trials of children and adults. The articles that have been selected, evaluate the use of intranasal and ocular antihistamines and their role in allergic rhinoconjunctivitis. Expert opinion: Olopatadine is significantly more effective than placebos in relieving the symptoms of allergic rhinoconjunctivitis. It can function both as a viable alternative or addition to first line therapies such as intranasal steroids and oral antihistamines.

Topics: Administration, Intranasal; Administration, Ophthalmic; Administration, Oral; Adult; Anti-Allergic Agents; Clinical Trials as Topic; Conjunctivitis, Allergic; Histamine H1 Antagonists; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Treatment Outcome

To assess the safety and efficacy of topical olopatadine versus placebo and other topical anti-allergic medications in treating allergic conjunctivitis.. We systematically searched the literature for randomized-controlled trials that included patients with allergic conjunctivitis, compared olopatadine versus placebo or alternative anti-allergic medications, and examined itch, conjunctival hyperemia, composite symptom or sign scores, and/or occurrence of adverse events. We assessed the safety and efficacy of topical olopatadine when compared with placebo or alternative anti-allergic medications using meta-analysis.. When compared with placebo, topical olopatadine is associated with a pooled-mean difference (MD) in ocular itch of -1.33 (p < 0.00001) and ocular hyperemia of -0.92 (p < 0.00001). When compared with other agents, olopatadine was inferior to alcaftadine on ocular itch (pooled-MD = 0.39; p < 0.00001) but comparable with epinastine and ketotifen.. Topical olopatadine is a safe and effective treatment modality for allergic conjunctivitis, whereas alcaftadine appears to be superior to olopatadine in reducing ocular itch.

Topics: Administration, Ophthalmic; Anti-Allergic Agents; Benzazepines; Conjunctivitis, Allergic; Dibenzazepines; Histamine H1 Antagonists; Humans; Imidazoles; Ketotifen; Olopatadine Hydrochloride; Ophthalmic Solutions; Treatment Outcome

This meta-analysis was designed to assess the efficacy, as well as the safety of loteprednol etabonate (LE) ophthalmic suspension compared with placebo and other commonly used eye drops for treatment of allergic conjunctivitis.. Comprehensive searches of randomized controlled trials were carried out in a database of Medline, Embase, and the Cochrane Library. Eight qualified studies were included. This study assessed the reduction from baseline in scores of cardinal signs and symptoms, proportion of patients with improvement of allergic signs and symptoms, and incidence of clinically significant intraocular pressure (IOP) elevation (IOP elevation ≥10 mmHg).. The results showed that topical LE was significantly superior to placebo in reduction from baseline in signs scores (standardized mean difference [SMD] = -0.48; 95% confidence interval [CI] = -0.65 to -0.32) and symptoms scores (weighted mean difference [WMD] = -0.51; 95% CI = -0.64 to -0.38) of allergic conjunctivitis, and as effective as olopatadine and fluorometholone acetate. Topical LE was associated with a higher improvement rate of signs (risk ratio [RR] = 1.53; 95% CI = 1.26-1.86; I (2 )= 57%) and symptoms (RR = 1.29; 95% CI = 1.15-1.46; I (2 )= 54%) than placebo and the positive control treatment. Clinically significant IOP elevation was more frequent in the group of LE than the group of control treatment (pooled odds ratio = 3.03; 95% CI = 1.04-8.80), which was affected by the response to corticosteroid of the individual patient and the wearing of contact lenses.. Topical LE is effective in treating allergic conjunctivitis. However, it should be used with caution due to the higher incidence of IOP elevation compared with placebo and olopatadine. A large-scale trial would be required to confirm the effect of different concentrations of LE on IOP.

Topics: Anti-Allergic Agents; Conjunctivitis, Allergic; Humans; Intraocular Pressure; Loteprednol Etabonate; Olopatadine Hydrochloride; Publication Bias

Vernal keratoconjunctivitis (VKC) is an unusually severe sight-threatening allergic eye disease, occurring mainly in children. Conventional therapy for allergic conjunctivitis is generally not adequate for VKC. Pediatricians and allergists are often not familiar with the severe clinical symptoms and signs of VKC. As untreated VKC can lead to permanent visual loss, pediatric allergists should be aware of the management and therapeutic options for this disease to allow patients to enter clinical remission with the least side effects and sequelae. Children with VKC present with severe ocular symptoms, that is, severe eye itching and irritation, constant tearing, red eye, eye discharge, and photophobia. On examination, giant papillae are frequently observed on the upper tarsal conjunctiva (cobblestoning appearance), with some developing gelatinous infiltrations around the limbus surrounding the cornea (Horner-Trantas dot). Conjunctival injections are mostly severe with thick mucus ropy discharge. Eosinophils are the predominant cells found in the tears and eye discharge. Common therapies include topical antihistamines and dual-acting agents, such as lodoxamide and olopatadine. These are infrequently sufficient and topical corticosteroids are often required for the treatment of flare ups. Ocular surface remodeling leads to severe suffering and complications, such as corneal ulcers/scars. Other complications include side effects from chronic topical steroids use, such as increased intraocular pressure, glaucoma, cataract and infections. Alternative therapies for VKC include immunomodulators, such as cyclosporine A and tacrolimus. Surgery is reserved for those with complications and should be handled by ophthalmologists with special expertise. Newer research on the pathogenesis of VKC is reviewed in this article. Vernal keratoconjunctivitis is a very important allergic eye disease in children. Complications and remodeling changes are unique and can lead to blindness. Understanding of pathogenesis of VKC may lead to better therapy for these unfortunate patients.

Topics: Adrenal Cortex Hormones; Anti-Inflammatory Agents, Non-Steroidal; Blindness; Child; Conjunctivitis, Allergic; Corneal Ulcer; Cyclosporine; Dibenzoxepins; Eosinophils; Histamine H1 Antagonists, Non-Sedating; Humans; Immunosuppression Therapy; Olopatadine Hydrochloride; Oxamic Acid

Ophthalmic disorders are highly prevalent in the United States, with approximately 3.5 million individuals aged at least 40 either blind or having impaired vision. This article reviews the current leading agents and pipeline therapies for the treatment of anterior ocular inflammatory disease (AOID).. There has been great progress in the understanding of ocular pathophysiology in recent years. Although current treatments for AOID are effective and well tolerated in many patients, a continued demand persists for more efficacious alternatives to the limited modalities available to clinicians.. Several promising modalities for AOID, particularly for allergic conjunctivitis, immune treatments for uveitis and dry eye syndrome are in late-stage development that could offer optimal treatment paradigm once available in the clinic.

Topics: Anti-Infective Agents; Antibodies, Monoclonal; Chemokine CCL11; Clinical Trials as Topic; Conjunctivitis, Allergic; Cyclosporine; Dibenzoxepins; Dry Eye Syndromes; Fluoroquinolones; Histamine H1 Antagonists; Humans; Immunotherapy; Levofloxacin; Moxifloxacin; Olopatadine Hydrochloride; Uveitis, Anterior

Ocular allergic diseases are characterized by specific activation of conjunctival mast cells with subsequent release of preformed and newly formed mediators. Mast cells are thus the first therapeutic target of ocular anti-allergic treatments.. In this review, a Medline literature search was conducted on conjunctival mast cells, their role in ocular allergy and mast cell stabilization by ocular anti-allergic compounds.. Olopatadine hydrochloride, a mast cell stabilizer and histamine receptor antagonist, has been shown to inhibit mast cell activation in an in vitro model of human mast cell culture, reducing histamine and TNF-alpha release and upregulating proinflammatory mediators in conjunctival epithelial cells. In the in vivo conjunctival allergen challenge (CAC) model in allergic subjects, combined with objective evaluations of tear mediators and cytology, olopatadine reduced histamine tear levels and all aspects of allergic inflammation, confirming the positive clinical effects observed in active allergic patients.. Mast cells play a central role in the pathogenesis of ocular allergy. The CAC model is ideal for assessing the mast cell stabilizing effects of anti-allergic compounds. This review of clinical studies demonstrates the superiority of olopatadine compared with other topical allergic drugs.

Topics: Administration, Topical; Animals; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists, Non-Sedating; Histamine Release; Humans; Mast Cells; Olopatadine Hydrochloride; Ophthalmic Solutions; Treatment Outcome

Multiple action drugs, such as azelastine, epinastine, ketotifen and olopatadine, have recently been suggested to combine antihistaminic effect, mast cell stabilization and anti-inflammatory action. This pharmaceutical class is, therefore, rapidly becoming the first choice for prevention and treatment for allergic conjunctivitis.. Increasing in-vitro studies have been performed to investigate the mast-cell-stabilizing effect of multiple action drugs. Most of the study results agree that these drugs are able to inhibit histamine and several neoformed mediators, including cytokines and arachidonic acid-derived products, from mast cells. However, the mechanisms of action have not yet fully been elucidated. Most of the results from clinical trials as well as the in-vivo experimental studies, including the conjunctival provocation model, support the evidence of a stabilizing effect of these drugs.. Evidence of a different inhibitory effect of multiple action compounds on the pro-inflammatory mediators released from the mast cells suggests the possibility to target different phases of the allergic reaction, leading to a potential improvement in the management of allergic patients.

Topics: Animals; Anti-Inflammatory Agents; Arachidonic Acid; Conjunctivitis, Allergic; Cytokines; Dibenzazepines; Dibenzoxepins; Histamine; Histamine Antagonists; Humans; Imidazoles; Immunity, Innate; Ketotifen; Mast Cells; Olopatadine Hydrochloride; Phthalazines

Olopatadine 0.2% is the first topical ophthalmic antihistamine/mast cell stabilizer indicated for once-daily dosing.. This review provides a comprehensive description of the pharmacology of the olopatadine molecule, as well as of the clinical efficacy, tolerability, and safety of olopatadine 0.2% ophthalmic solution.. References cited in this review were obtained from the PubMed biomedical literature database. Also included were several posters presented at nationally renowned ophthalmology-related conferences.. Olopatadine 0.2% was found to be a safe and effective medication for the reduction of itching with a duration of action of up to 24 h. The added convenience of a once-a-day dosing regimen is a major advancement in this drug class.

Topics: Anti-Allergic Agents; Clinical Trials as Topic; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists, Non-Sedating; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Treatment Outcome

Topics: Animals; Capillary Permeability; Clinical Trials as Topic; Conjunctivitis, Allergic; Cytokines; Dibenzoxepins; Histamine Antagonists; Humans; Hypersensitivity, Immediate; Inflammation Mediators; Olopatadine Hydrochloride; Ophthalmic Solutions; Passive Cutaneous Anaphylaxis; Tumor Necrosis Factor-alpha

Topics: Anti-Allergic Agents; Anti-Bacterial Agents; Anti-Inflammatory Agents; Child; Conjunctivitis, Allergic; Dexamethasone; Diagnosis, Differential; Dibenzoxepins; Diphenhydramine; Drug Combinations; Drug Therapy, Combination; Humans; Male; Nurse Practitioners; Nursing Assessment; Olopatadine Hydrochloride; Referral and Consultation; Tobramycin

Allergic eye disease is a term that refers to a number of disease processes that affect about one-fifth of the world's population. Although the more advanced forms of the disease can be sight threatening, the most disabling effects are due to the clinical manifestations, and hence quality of life, with some patients having seasonal exacerbations of their symptoms, whereas others have symptoms that are present throughout the year. Recent increased understanding of the cellular and mediator mechanisms that are involved in the various disease manifestations has greatly facilitated the development of more effective treatment options. Newer topical medications are being used that have multiple actions, such as an antihistaminic effect coupled with mast-cell stabilisation, and which require reduced daily dosing due to their longer duration of action. With greater research into newer therapies and more effective modes of delivery, improved healthcare outcomes with a lower economic burden will be achieved for patients with allergic eye disease.

Topics: Administration, Oral; Administration, Topical; Adrenal Cortex Hormones; Anti-Allergic Agents; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Cost of Illness; Dibenzoxepins; Drug Administration Schedule; Health Care Costs; Histamine H1 Antagonists; Humans; Immunosuppressive Agents; Mast Cells; Olopatadine Hydrochloride; Phthalazines; Quality of Life; Randomized Controlled Trials as Topic; Tacrolimus; Vision Disorders

Azelastine hydrochloride 0.05% and olopatadine hydrochloride 0.1% are topical ocular allergy treatments that have demonstrated multiple pharmacologic actions, including antihistamine, mast cell stabilization, and inhibition of proinflammatory mediators. In this article, the mechanisms of action, efficacy, and tolerability of these two agents on ocular signs and symptoms are examined. By studying the various target sites of drug action, an enhanced clinical response algorithm of these topical ocular agents can be implemented to maximize the response for patients suffering from ocular allergy.

Topics: Administration, Topical; Anti-Allergic Agents; Anti-Inflammatory Agents, Non-Steroidal; Clinical Trials as Topic; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists; Histamine H2 Antagonists; Humans; Mast Cells; Olopatadine Hydrochloride; Phthalazines

Ocular allergy affects > 20% of the general population and many therapeutic preparations are available to individuals experiencing the most common forms--seasonal and perennial allergic conjunctivitis. 0.1% Olopatadine topical ophthalmic solution is currently approved for the treatment of allergic signs and symptoms in patients > or = 3 years of age. Olopatadine is available in Europe as Opatanol) and in > 30 other countries as Patanol. It inhibits mast cell degranulation and antagonises histamine receptors to manage the itching, redness, chemosis, tearing and lid swelling of the ocular allergic reaction, and its mast cell stabilising ability has been demonstrated both in vitro (using human conjunctival mast cells) and in vivo (human clinical experience). This article reviews both the laboratory and clinical information available on olopatadine, prefaced by a discussion of the current understanding of the ocular allergic reaction and followed by the future implications for this compound. Both laboratory and clinical studies have established the efficacy, safety and comfort of olopatadine in several study design models and comparisons to other antiallergy medications. The application of olopatadine, specifically in the management of lid swelling, an allergic sign recalcitrant to therapy and nasal allergic symptoms has also been established. In the future, a new formulation containing 0.2% olopatadine exhibits a duration of action up to 24 h, supporting once-daily dosing.

Topics: Animals; Anti-Allergic Agents; Blepharitis; Conjunctivitis, Allergic; Contact Lenses; Dibenzoxepins; Histamine H1 Antagonists; Humans; Mast Cells; Olopatadine Hydrochloride; Ophthalmic Solutions; Randomized Controlled Trials as Topic; Rhinitis

Olopatadine hydrochloride (CAS 140462-76-6, KW-4679, AL-4943A; hereinafter referred to as olopatadine) is a novel antiallergic drug that is a selective histamine H1 receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and thromboxane from human polymorphonuclear leukocytes and eosinophils. Olopatadine also inhibits the tachykininergic contractions in guinea pig bronchi by prejunctional inhibition of peripheral sensory nerves. Oral administration of olopatadine at doses of 0.03 mg/kg or higher reduces the symptoms of experimental allergic cutaneous responses and rhinoconjunctivitis in sensitized animals. Preclinical and clinical evaluations have demonstrated that olopatadine is a safe drug. After oral administration to healthy volunteers, olopatadine was rapidly and extensively absorbed. Unlike most other antiallergic drugs which are eliminated via hepatic metabolism, olopatadine is mainly excreted into urine. Olopatadine did not affect cytochrome P450 activities in human liver microsomes and consequently drug-drug metabolic interactions are unlikely. In double-masked clinical trials, olopatadine was shown to be effective at alleviating symptoms of allergic diseases. The drug (Allelock) was approved in Japan for the treatment of allergic rhinitis, chronic urticaria, eczema dermatitis, prurigo, cutaneous pruritus, psoriasis vulgaris and erythema exsudativum multiforme in December, 2000. An ophthalmic solution of olopatadine is also useful for the treatment of allergic conjunctivitis: this formulation (Patanol) was approved in the USA and the European Union for the treatment of seasonal and perennial allergic conjunctivitis in 1996 and 2002, respectively.

Topics: Animals; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Histamine Antagonists; Humans; Hypersensitivity; Olopatadine Hydrochloride; Rhinitis, Allergic, Perennial; Rhinitis, Allergic, Seasonal; Urticaria

Ocular allergies are very common and range in intensity from mild, self-resolving, acute conditions to serious, chronic disease that can severely affect vision. The vast majority of sufferers experience relatively mild symptoms, which are often seasonal in nature. Treatments should be simple, comfortable and very safe. They should be able to respond to an ongoing attack but also provide long-term relief from symptoms. Mast cell degranulation is central to all forms of ocular allergic disease and so treatment has concentrated on preventing this process or antagonizing the effects of the primary mediator, histamine. Olopatadine is a relatively new selective H1 antagonist that has mast cell stabilizing properties and has been shown to affect release of TNFalpha and various cytokines from conjunctival epithelial cells. This paper reviews the local ocular use of olopatadine and discusses the place of the drug in the treatment of allergic eye disease.

Topics: Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists; Humans; Mast Cells; Olopatadine Hydrochloride

Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride) is a novel antiallergic/histamine H1-receptor antagonistic drug that was synthesized and evaluated in our laboratories. Oral administration of olopatadine at doses of 0.03 mg/kg or higher inhibited the symptoms of experimental allergic skin responses, rhinoconjunctivitis and bronchial asthma in sensitized guinea pigs and rats. Olopatadine is a selective histamine H1-receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and thromboxane from human polymorphonuclear leukocytes and eosinophils. Olopatadine also inhibited the tachykininergic contraction in the guinea pig bronchi by prejunctional inhibition of peripheral sensory nerves. Olopatadine exerted no significant effects on action potential duration in isolated guinea pig ventricular myocytes, myocardium and human ether-a-go-go-related gene channel. Olopatadine was highly and rapidly absorbed in healthy human volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was considerably low in the clearance of olopatadine in humans. Olopatadine is one of the few renal clearance drugs in antiallergic drugs. Olopatadine was shown to be useful for the treatment of allergic rhinitis and chronic urticaria in double-blind clinical trials. Olopatadine was approved in Japan for the treatment of allergic rhinitis, chronic urticaria, eczema dermatitis, prurigo, pruritus cutaneous, psoriasis vulgaris and erythema exsudativum multiforme in December, 2000. Ophthalmic solution of olopatadine was also approved in the United States for the treatment of seasonal allergic conjunctivitis in December, 1996 (Appendix: also in the European Union, it was approved in February 2002).

Topics: Animals; Anti-Allergic Agents; Asthma; Clinical Trials as Topic; Conjunctivitis, Allergic; Dibenzoxepins; Drug Administration Routes; Histamine H1 Antagonists; Humans; Hypersensitivity; Inflammation Mediators; Olopatadine Hydrochloride; Ophthalmic Solutions; Pruritus; Rhinitis, Allergic, Perennial; Urticaria

Topics: Administration, Ophthalmic; Adult; Allergens; Benzazepines; Conjunctivitis, Allergic; Cryptomeria; Double-Blind Method; Female; Histamine H1 Antagonists; Histamine H1 Antagonists, Non-Sedating; Humans; Imidazoles; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Pollen; Prospective Studies; Treatment Outcome

To compare the efficacy and safety of Alcaftadine 0.25%, Olopatadine hydrochloride 0.2%, and Bepotastine besilate 1.5% ophthalmic solutions in the treatment of allergic conjunctivitis.. This is a prospective, observer-masked, comparative study of 180 patients with mild to moderate allergic conjunctivitis, randomized into three groups of 60 patients each. Each group was assigned to be treated with one of the three treatment options namely Alcaftadine 0.25%, Olopatadine hydrochloride 0.2% and Bepotastine besilate 1.5% ophthalmic solutions. Patients were followed-up at regular intervals with relief and resolution of symptoms and signs noted using Total Ocular Scoring System (TOSS) and hyperaemia scale.. All three topical medications were effective in resolving symptoms of the patients with mild to moderate allergic conjunctivitis. Baseline mean TOSS scores for Alcaftadine group, Olopatadine group and Bepotastine besilate group were (7.68±2.32), (7.65±2.32) and (7.45±2.27) respectively as compared to the corresponding TOSS scores on 14. All three topical ophthalmic medications used in the study are safe and effective in the treatment of allergic conjunctivitis. However, Bepotastine and Alcaftadine appear to outweigh Olopatadine in resolving the symptoms of allergic conjunctivitis.

Topics: Anti-Allergic Agents; Benzazepines; Conjunctivitis, Allergic; Double-Blind Method; Humans; Imidazoles; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Prospective Studies; Pyridines; Treatment Outcome

With increasing environmental pollution, the incidence of allergic conjunctivitis is increasing. Newer anti-allergic medications with combined anti-histaminic and mast cell stabilization action can help reducing the use of topical steroids for milder form of disease. There is no study directly comparing olopatadine (0.1%), bepotastine (1.5%), and alcaftadine (0.25%) for mild to moderate allergic conjunctivitis cases. Hence, we decided to methodically study the efficacy of three topical medications.. Prospective, observer-masked clinical trial enrolled 45 patients with 15 patients in each of the three groups. Patients with mild to moderate allergic conjunctivitis were sequentially assigned to respective groups, and relief of symptoms and signs were noted upto 1-month follow-up.. All three topical medications faired almost equally in resolving symptoms of the patients with mild to moderate allergic conjunctivitis, and most of them reported complete relief after 1 week of use of medication. Few cases with limbal or palpebral papillae reported symptomatic relief after use of medication, but the resolution of these signs was not noted in all three groups.. We concluded similar efficacy of three medications in relieving symptoms and inefficacy in regressing palpebral and limbal papillae in cases of allergic conjunctivitis.

Topics: Adolescent; Adult; Anti-Allergic Agents; Benzazepines; Child; Conjunctiva; Conjunctivitis, Allergic; Dose-Response Relationship, Drug; Female; Follow-Up Studies; Histamine H1 Antagonists; Humans; Imidazoles; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Prospective Studies; Pyridines; Single-Blind Method; Treatment Outcome; Young Adult

Topics: Adult; Benzazepines; Cedrus; Conjunctivitis, Allergic; Dose-Response Relationship, Drug; Double-Blind Method; Female; Follow-Up Studies; Histamine H1 Antagonists; Humans; Imidazoles; Incidence; Japan; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Pollen; Retrospective Studies; Seasons; Treatment Outcome

Olopatadine is an antihistamine and mast cell stabilizer used for treating allergic conjunctivitis. Olopatadine 0.7% has been recently approved for daily dosing in the US, which supersedes the previously approved 0.2% strength. The objective of this analysis was to characterize patients who have better itching relief at 24 h when taking olopatadine 0.7% treatment instead of olopatadine 0.2% (in terms of proportions of responses) and relate this to the severity of baseline itching as an indirect metric of a patient's sensitivity to antihistamines. A differential odds model was developed using data from two conjunctival allergen challenge (CAC) studies to characterize individual-level and population-level response to ocular itching following olopatadine treatment and the data was analyzed retrospectively. This modeling analysis was designed to predict 24 h ocular itching scores and to quantify the differences in 24 h itching relief following treatment with olopatadine 0.2% versus 0.7% in patients with moderate-to-high baseline itching. A one-compartment kinetic-pharmacodynamic E

Topics: Adolescent; Adult; Aged; Allergens; Conjunctivitis, Allergic; Double-Blind Method; Female; Histamine Antagonists; Histamine H1 Antagonists; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Pruritus; Retrospective Studies; Treatment Outcome; Young Adult

Allergic conjunctivitis (AC) is a disease of various agents that affects the physical and mental health of children. Although the most effective therapy has not been found so far, it is essential to explore the considerable therapeutic method. We compared the clinical efficacy of olopatadine, emedastine, loteprednol etabonate (LE), and vehicle for treating seasonal allergic conjunctivitis (SAC) in Chinese children.. Eighty cases of 160 eyes aged from 5 to 10 years with SAC were available and those subjects were randomly distributed into 4 groups. Both their eyes received olopatadine hydrochloride 0.1% twice a day, emedastine difumarate 0.05% twice a day, or LE 0.5% 4 times a day, respectively, whereas those of the control group received artificial tears (AT) 0.5% 3 times a day. This study was conducted successfully and the observations were collected before treatment and on day 8 (±1 day) and day 15 (±2 days) afterward. The principal measurement of efficacy was focused on the signs and symptoms of the subjects, evaluated before and after treatment, in addition to visual acuity (VA) and fundus oculi.. On day 8 (±1 day) and day 15 (±2 days), all the antiallergic agents were found to be more effective than vehicle (p < 0.05) in terms of all the symptoms and signs. However, there was no statistical significance (p ≥ 0.05) shown among the treatment groups. There were no evident changes in VA and no clinically significant changes were observed in fundus oculi.. After the treatment, the efficacy presented a similar distribution among the trial groups.

Topics: Anti-Allergic Agents; Asian People; Benzimidazoles; Child; Child, Preschool; Conjunctivitis, Allergic; Female; Humans; Loteprednol Etabonate; Male; Olopatadine Hydrochloride; Single-Blind Method; Treatment Outcome

To assess the efficacy and safety of a novel once-daily 0.77% olopatadine hydrochloride ophthalmic solution in subjects with allergic conjunctivitis (AC) using the conjunctival allergen challenge (CAC) model.. In this 5-week, multicenter, double-masked, phase 3, randomized trial, subjects aged ≥18 years with a history of AC and a confirmed positive bilateral CAC response were randomized 2:2:2:1 to receive olopatadine 0.77%, olopatadine 0.2%, olopatadine 0.1%, or vehicle, respectively, following a single topical dose in each eye. The primary objective was superiority of olopatadine 0.77% over all comparators on ocular itching according to a 0 to 4 scale (0 = none and 4 = incapacitating itch) at 24-hour duration of action and over vehicle only at the onset of action (3, 5, and 7 minutes after CAC for both).. In total, 345 subjects were randomized. Olopatadine 0.77% was superior to the vehicle at alleviating ocular itching at all post-CAC time points at the onset of action and at 24 hours (difference in means: -0.9 to -1.5; P < 0.0001). Superiority in relieving ocular itching was also demonstrated for olopatadine 0.77% versus olopatadine 0.2% and 0.1% at 24 hours (difference in means: -0.3 to -0.5; P < 0.05). Additionally, olopatadine 0.77% significantly improved conjunctival redness and total redness compared with all comparators at the onset of action (differences in means: -0.3 to -0.6 and -0.8 to -2.0, respectively; both P < 0.05). No safety concerns for olopatadine 0.77% were identified.. Olopatadine 0.77% demonstrated a rapid onset and prolonged duration of action. It was superior to all comparators in alleviating AC-associated ocular itching with a favorable safety profile.Clinical Trial Registration-URL: http://www.clinicaltrials.gov. Unique identifier: NCT01743027.

Topics: Administration, Topical; Adolescent; Adult; Aged; Allergens; Conjunctivitis, Allergic; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Middle Aged; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Pharmaceutical Vehicles; Treatment Outcome; Visual Acuity; Young Adult

To evaluate the therapeutic effects of low-effective steroid fluorometholone 0.1% and non-steroidal anti-inflammatory ketorolac 0.4% when concomitantly used with olopatadine 0.01% in relieving clinical signs and symptoms of acute seasonal allergic conjunctivitis (SAC).. In this randomized, placebo-controlled, multi-center study, 104 eyes of 52 patients with the diagnosis of SAC were conducted. The patients were assigned into two groups to receive either olopatadine and fluorometholone one eye and placebo in the contralateral eye or olopatadine and ketorolac one eye and placebo in the contralateral. The clinical signs (chemosis, mucus secretion, eyelid edema) and symptoms (itching, redness, tearing, burning) of the patients were evaluated by summing up the scores using a 3-point scale. Results were analyzed by Mann-Whitney U test, p values less than 0.05 were defined as significant.. All parameters were improved less amount on the first day of the treatment in both groups, however, significant reduction in clinical signs and symptoms were seen on the 10th day compared with those receiving placebo. Fluorometholone was found superior to ketorolac in reducing redness, mucus secretion, chemosis and eyelid edema (p = 0.032 for redness, p = 0.028 for mucus secretion, p = 0.030 for chemosis, p = 0.042 for eyelid edema) and both drugs were similar in alleviating the symptoms itching, burning and tearing (p = 0.074 for itching, p = 0.064 for burning, p = 0.072 for tearing).. Fluorometholone was better than ketorolac in relieving redness, chemosis, mucus secretion and eyelid edema when concomitantly used with olopatadine, however, these two drugs were found equal in attenuating the symptoms itching, burning and tearing.

Topics: Acute Disease; Adolescent; Adult; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Dibenzoxepins; Drug Combinations; Female; Fluorometholone; Histamine H1 Antagonists, Non-Sedating; Humans; Ketorolac; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Placebos; Seasons; Treatment Outcome; Young Adult

To compare preservative-free ketotifen 0.025% ophthalmic solution to olopatadine 0.1% ophthalmic solution in with the treatment of seasonal allergic conjunctivitis (SAC) in clinical practice.. This was a comparative, randomised, investigator-masked, pilot clinical study in adult patients with documented history of SAC and presenting with moderate to severe itching and conjunctival hyperemia. Eligible patients initiated either ketotifen or olopatadine treatment at a dose of one drop twice daily for 28days. The resolution of ocular signs and symptoms was assessed on day 7 and day 28. Itching was also assessed within 15minutes following the first instillation (day 0). Conjunctival impression cytology was performed at each visit to assess the evolution of ICAM-1 expression (day 0, 7 and 28).. Seventy-five patients were randomised (ketotifen: 38 patients; olopatadine: 37 patients). At day 28, the composite score for primary criteria (itching, tearing, and conjunctival hyperemia) improved from 6.8±1.2 to 0.9±1.0 in the Ketotifen group, without statistically significant difference between treatment groups (P=0.67). There was no relevant difference between treatment groups in other efficacy parameters, except a trend for a more rapid resolution of conjunctival hyperemia in the Ketotifen group. Both drugs were well tolerated, with a trend for a better tolerability reported by patients on ketotifen compared to those on olopatadine at day 7 (P=0.054).. A rapid and comparable improvement in SAC was achieved after 28days of treatment with both preservative-free ketotifen and preserved olopatadine ophthalmic solutions, with a slightly better ocular tolerance with unpreserved ketotifen 0.025% eye drops.

Topics: Adult; Aged; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Female; Humans; Ketotifen; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Pilot Projects; Preservatives, Pharmaceutical; Seasons; Severity of Illness Index; Treatment Outcome; Young Adult

Epinastine hydrochloride is a selective histamine H1 receptor antagonist that also inhibits IgE receptor-mediated histamine release from mast cells.. To show the superiority of epinastine 0.05% ophthalmic solution (epinastine) to placebo ophthalmic solution (placebo) and noninferiority to olopatadine 0.1% ophthalmic solution (olopatadine) for cedar pollen antigen-induced ocular itching and conjunctival hyperemia.. The study was conducted in ophthalmologically asymptomatic adult volunteers with seasonal allergic conjunctivitis using a conjunctival allergen challenge test. Subjects were randomized into 3 groups (n = 87) to evaluate superiority to placebo (visits 4 to 6) and 2 groups (n = 86) to evaluate noninferiority to olopatadine (visit 7). At each visit, a single administration of the study medication was instilled at 15 minutes (visit 4), 4 hours (visit 5), 8 hours (visit 6), and 4 hours (visit 7) before the conjunctival allergen challenge test. Ocular itching and conjunctival hyperemia of allergic conjunctivitis were assessed after the conjunctival allergen challenge test.. For the primary end point, epinastine showed superiority to placebo for the inhibition of ocular itching and conjunctival hyperemia induced at 4 hours after the dose (equivalent to 4-times-daily dosing). For the secondary end points, epinastine significantly inhibited itching and conjunctival hyperemia induced at 15 minutes and 8 hours after the dose (equivalent to 2-times-daily dosing) compared with placebo. In addition, epinastine demonstrated noninferiority to olopatadine for ocular itching and conjunctival hyperemia. No adverse drug reactions or serious adverse events were reported throughout the study, indicating that epinastine has a good safety profile.. Epinastine is effective and safe for the treatment of allergic conjunctivitis.. Clinicaltrials.gov identifier NCT01363700.

Topics: Adult; Allergens; Anti-Allergic Agents; Cedrus; Conjunctiva; Conjunctivitis, Allergic; Dibenzazepines; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Hyperemia; Imidazoles; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Platelet Aggregation Inhibitors; Pollen; Rhinitis, Allergic, Seasonal; Young Adult

The efficacy and safety of the once-daily topical ophthalmic solutions, alcaftadine 0.25% and olopatadine 0.2%, in preventing ocular itching associated with allergic conjunctivitis were evaluated.. Pooled analysis was conducted of two double-masked, multicenter, active- and placebo-controlled studies using the conjunctival allergen challenge (CAC) model of allergic conjunctivitis. Subjects were randomized 1:1:1 to receive alcaftadine 0.25%, olopatadine 0.2%, or placebo. The primary efficacy measure was subject-evaluated mean ocular itching at 3 min post-CAC and 16 h after treatment instillation. Secondary measures included ocular itching at 5 and 7 min post-CAC. Ocular itch was determined over all time points measured (3, 5, and 7 min) post-CAC and the proportion of subjects with minimal itch (itch score<1) and zero itch (itch score=0) was also assessed.. A total of 284 subjects were enrolled in the two studies. At 3 min post-CAC and 16 h after treatment instillation, alcaftadine 0.25% achieved a significantly lower mean itch score compared with olopatadine 0.2% (0.50 vs. 0.87, respectively; P=0.0006). Alcaftadine demonstrated a significantly lower mean itch score over all time points compared with olopatadine (0.68 vs. 0.92, respectively; P=0.0390); both alcaftadine- and olopatadine-treated subjects achieved significantly lower overall mean ocular itching scores compared with placebo (2.10; P<0.0001 for both actives). Minimal itch over all time points was reported by 76.1% of alcaftadine-treated subjects compared with 58.1% of olopatadine-treated subjects (P=0.0121). Treatment with alcaftadine 0.25% and olopatadine 0.2% was safe and well tolerated; no serious adverse events were reported.. Once-daily alcaftadine 0.25% ophthalmic solution demonstrated greater efficacy in prevention of ocular itching compared with olopatadine 0.2% at 3 min post-CAC (primary endpoint), and over all time points, 16 h post-treatment instillation. Alcaftadine and olopatadine both provided effective relief compared with placebo and were generally well tolerated.

Topics: Adult; Allergens; Anti-Allergic Agents; Benzazepines; Conjunctivitis, Allergic; Double-Blind Method; Drug Monitoring; Female; Humans; Imidazoles; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Outcome Assessment; Pruritus

The objective of this study was to compare the efficacy and safety of olopatadine versus epinastine in healthy Japanese adults with a history of allergic conjunctivitis to Japanese cedar pollen.. This Phase IV double-blind randomized controlled clinical trial comprised three clinical visits over 30 days. Screening tests were performed to identify subjects with a history of allergic conjunctivitis to Japanese cedar pollen in terms of skin sensitivity and positive bilateral reactions to a conjunctival allergen challenge (CAC) with Japanese cedar pollen at Visit 1, and confirmation by a positive bilateral CAC reaction at Visit 2. At Visit 3, the subjects were randomized to receive one drop of olopatadine HCl ophthalmic solution 0.1% (olopatadine) in the left or right eye (1:1 ratio). All subjects received one drop of epinastine HCl ophthalmic solution 0.05% (epinastine) in the contralateral eye as an active control. Five min later, the subjects underwent bilateral CAC tests with one drop of the allergen solution at the concentration that elicited positive reactions at Visits 1 and 2. Efficacy outcomes included the severity of ocular itching at 5, 7, and 15 min and the severity of conjunctival hyperemia at 7, 15, and 20 min after the CAC test, as graded by the investigator by biomicroscopy.. Fifty people participated in this study (25 per group). Olopatadine significantly reduced ocular itching at 7 and 15 min (both p<0.05) and conjunctival hyperemia at 7 and 20 min (p=0.0010 and p<0.05, respectively) after allergen exposure compared with epinastine. There were no adverse events for either treatment.. The results of this single-dose study suggest that olopatadine is superior to epinastine in terms of suppressing ocular itching and hyperemia induced by Japanese cedar pollen during CAC tests. Further studies are needed to confirm these findings in real-life settings.

Topics: Adult; Allergens; Anti-Allergic Agents; Conjunctivitis, Allergic; Cryptomeria; Dibenzazepines; Double-Blind Method; Female; Humans; Imidazoles; Japan; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Pollen; Severity of Illness Index; Skin Tests; Treatment Outcome

Seasonal allergic conjunctivitis (SAC) is caused by seasonal allergens and usually manifests as ocular itching and bulbar conjunctival injection (redness). Treatment options for SAC include corticosteroids and dual-acting antihistamine and mast-cell stabilizers.. Our objective was to compare the efficacy and tolerability of loteprednol etabonate (LE), a C-20 ester-based corticosteroid, with those of olopatadine, a dual-acting antihistamine mast-cell stabilizer, in Chinese patients.. This was a multicenter, randomized, investigator-masked, parallel group study. Patients with acute SAC experiencing grade 4 ocular itching and grade 2 or higher bulbar conjunctival injection received either LE suspension 0.2% QID at 4-hour intervals or olopatadine solution 0.1% BID at 6- to 8-hour intervals bilaterally for 15 days. Primary efficacy end points included the change from baseline (CFB) in ocular itching and bulbar conjunctival injection at day 15. The primary analysis tested the noninferiority of LE suspension 0.2% to olopatadine solution 0.1%. Tolerability outcomes included the incidence of adverse events (AEs), biomicroscopy findings, visual acuity, and intraocular pressure.. A total of 300 patients were randomly assigned, and 293 were included in the per-protocol population (LE, n = 147; olopatadine, n = 146). Mean (SD) CFB at day 15 in the LE and olopatadine treatment groups, respectively, was -3.74 (0.47) and -3.28 (0.91) for ocular itching and -1.91 (0.52) and -1.71 (0.59) for bulbar conjunctival injection. The 95% CI for the differences in CFB in ocular itching (-0.59 to -0.27) and bulbar conjunctival injection (-0.27 to -0.08) was less than the prespecified noninferiority limit of 0.3. Treatment differences in CFB were significantly better with LE compared with olopatadine for both end points (P ≤ 0.0006). Ocular AEs were few and similar between treatment groups. There were no clinically significant biomicroscopy or visual acuity findings, and no patient experienced a clinically significant increase in intraocular pressure (≥10 mm Hg).. Results of this investigator-masked study with Chinese patients suggest LE suspension 0.2% was noninferior to olopatadine solution 0.1% for the treatment of SAC. Both LE suspension 0.2% and olopatadine solution 0.1% were well tolerated. ClinicalTrials.gov identifier: NCT01435460.

Topics: Administration, Ophthalmic; Adult; Androstadienes; Anti-Allergic Agents; China; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Administration Schedule; Humans; Loteprednol Etabonate; Olopatadine Hydrochloride

Olopatadine hydrochloride ophthalmic solution, 0.2% (olopatadine 0.2%) is approved for allergic conjunctivitis when instilled twice-daily. The objective of this study was to evaluate the efficacy and safety of olopatadine 0.2% (instilled twice-daily) versus vehicle and olopatadine 0.1% (instilled 4-times daily) in Japanese patients with allergic conjunctivitis.. A multicenter, parallel-group, double-masked, randomized, conjunctival allergen challenge (CAC) study. Patients > or = 18 years of age with histories of allergic conjunctivitis were treated with either olopatadine 0.2% or olopatadine 0.1% in a single eye and the vehicle in the contralateral eye at 1 visit.. Overall, 267 patients were enrolled. Olopatadine 0.2% was superior to its vehicle for ocular itching (p < 0.0001 at the time of observation) and marginally superior for total redness (p = 0.0543 at the time of observation). Olopatadine 0.2% was similar to olopatadine 0.1% for ocular itching at the time of observation. No trends were identified through a review of safety parameters.. Olopatadine 0.2% (instilled twice-daily) is safe, well tolerated, superior to the vehicle, and similar to olopatadine 0.1% in preventing ocular itching. Olopatadine 0.2%, which can be instilled less often than olopatadine 0.1%, is a useful new option for allergic conjunctivitis in Japanese patients that could potentially result in better treatment compliance.

Topics: Adolescent; Adult; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Female; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Pruritus; Treatment Outcome; Young Adult

The purpose of this study was to compare the efficacy of olopatadine with fluorometholone in contact lens-induced mild to moderate papillary conjunctivitis.. A randomized, double-masked study was conducted. Eighty-five (n = 170 eyes) soft contact lens users with mild to moderate papillary conjunctivitis were enrolled. Patients were randomly assigned to three groups to receive olopatadine 0.1%, fluorometholone 0.1%, or both. All drugs were instilled twice daily for 8 weeks. Contact lens use was discontinued during initial 4 weeks of therapy and subsequently patients were prescribed monthly disposable lenses. Patients were followed up every 2 weeks, and variables assessed were symptoms and signs, tear film status, and intraocular pressures.. Decrease in ocular redness, itching, and tearing along with improvement in contact lens tolerance was comparable in all the three groups. Olopatadine was more effective in reducing redness than fluorometholone at 8 weeks (P=0.01). Improvement in congestion and papillary reaction was comparable in all groups. There was a significant increase in tear break up time of more than 2 sec for fluorometholone and no significant increase for olopatadine. The olopatadine and fluorometholone groups had significant increase of more than 2 mm in Schirmer test and more than 3 sec in tear break up time. In patients with subnormal and borderline tear functions, significant improvement was observed with both drugs. After 8 weeks of use of fluorometholone, there was a significant increase in intraocular pressure (P=0.003).. Olopatadine and fluorometholone were the most effective for papillary conjunctivitis followed by olopatadine monotherapy and then fluorometholone monotherapy. Olopatadine is effective in alleviating signs and symptoms of contact lens-induced mild to moderate papillary conjunctivitis and is comparable with fluorometholone in efficacy.

Topics: Anti-Allergic Agents; Conjunctiva; Conjunctivitis, Allergic; Contact Lenses; Diagnosis, Differential; Dibenzoxepins; Double-Blind Method; Drug Therapy, Combination; Female; Fluorometholone; Follow-Up Studies; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Severity of Illness Index; Treatment Outcome; Young Adult

We aimed to compare the clinical efficacy and ocular surface variables of olopatadine, ketotifen fumarate, epinastine, emedastine and fluorometholone acetate ophthalmic solutions in preventing the signs and symptoms of seasonal allergic conjunctivitis (SAC).. This was a prospective, randomized, double-blinded and placebo-controlled study. A total of 100 patients with SAC were randomly assigned to one of five groups, in which they were administered olopatadine, ketotifen fumarate, epinastine, emedastine or fluorometholone acetate, instilled twice daily for 2 weeks. One eye of each patient was treated with the study drug and the other was treated with a placebo. Signs and symptoms of allergic conjunctivitis (itching, redness, tearing, chemosis and eyelid swelling) were scored on a 4-point scale. Each symptom was assessed at baseline and then again after 1 and 2 weeks of treatment. Ocular surface variables were assessed by conjunctival impression cytology.. At weeks 1 and 2, all antiallergic agents were significantly more effective than placebo in alleviating itching, redness, tearing, chemosis and eyelid swelling. Fluorometholone acetate was significantly less effective than the other agents in reducing itching and redness at all control visits. Ocular surface findings by impression cytology improved significantly after all treatments compared with placebo.. In patients with SAC, olopatadine, ketotifen, epinastine and emedastine are more efficacious than fluorometholone acetate in preventing itching and redness. All the antiallergic agents gave similar results in terms of reducing tearing, chemosis and eyelid swelling. Our data showed that impression cytology parameters improved after treatment with antiallergic agents in patients with SAC.

Topics: Adolescent; Adult; Anti-Allergic Agents; Benzimidazoles; Child; Conjunctival Diseases; Conjunctivitis, Allergic; Dibenzazepines; Dibenzoxepins; Double-Blind Method; Edema; Eyelid Diseases; Female; Fluorometholone; Histamine H1 Antagonists; Humans; Imidazoles; Ketotifen; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Prospective Studies; Pruritus; Seasons; Tears; Treatment Outcome; Young Adult

Olopatadine, an antihistamine used in allergic conjunctivitis, is under development as a nasal preparation for the treatment of allergic rhinitis.. To evaluate the efficacy of olopatadine in suppressing symptoms and biomarkers of the immediate reaction induced by nasal allergen provocation and to compare olopatadine with azelastine in the same model.. The study was approved by the Johns Hopkins University institutional review board, and all subjects gave written consent. We studied 20 asymptomatic subjects with seasonal allergic rhinitis. The study had 2 randomized, double-blind, placebo-controlled, crossover phases that evaluated 2 concentrations of olopatadine, 0.1% and 0.2%. In a third exploratory phase, olopatadine, 0.1%, was compared with topical azelastine, 0.1%, in a patient-masked design. Efficacy variables were the allergen-induced sneezes, other clinical symptoms, and the levels of histamine, tryptase, albumin, lysozyme, and cysteinyl-leukotrienes (third study only) in nasal lavage fluids.. Both concentrations of olopatadine produced significant inhibition of all nasal symptoms, compared with placebo. Olopatadine, 0.1%, inhibited lysozyme levels, but olopatadine, 0.2%, inhibited histamine, albumin, and lysozyme. The effects of olopatadine, 0.1%, were comparable to those of azelastine, 0.1%.. Olopatadine, at 0.1% and 0.2% concentrations, was effective in suppressing allergen-induced nasal symptoms. At 0.2%, olopatadine provided evidence suggestive of inhibition of mast cell degranulation.

Topics: Adult; Allergens; Anti-Allergic Agents; Conjunctivitis, Allergic; Cross-Over Studies; Dibenzoxepins; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Nasal Provocation Tests; Olopatadine Hydrochloride; Phthalazines; Rhinitis, Allergic, Seasonal

Olopatadine hydrochloride 0.2% (Pataday, Alcon, Fort Worth, USA) is a topical ocular anti-allergic agent that has shown high rates of efficacy in treating ocular itching, the primary symptom of allergic conjunctivitis, and allows for once-daily dosing. Since some patients suffer from signs or symptoms of dry eye in addition to ocular allergy, this study was designed to evaluate the safety of olopatadine 0.2% in a population of patients with both allergic conjunctivitis and dry eye.. This was a single-center, 3-visit, double-masked, randomized study. Fifty-two patients diagnosed with ocular allergy and mild-to-moderate dry eye were evaluated. After a run-in period, patients were randomized to receive either olopatadine hydrochloride 0.2% or a tear saline, and self-dosed once-daily for 1 week. Outcome measures included tear film break-up time, corneal and conjunctival staining, tear volume and flow as measured by fluorophotometry, Schirmer's test, injection, and symptom evaluations.. No significant differences between the treatment groups were observed (p > 0.05). No serious adverse events occurred during the trial. Variability in the presentation of dry eye can hinder the observation of treatment effects. Although the study design facilitated the comparison of olopatadine 0.2% against an agent that was certain to not exacerbate dry eye, future comparison of olopatadine 0.2% against other agents in its drug class would provide useful information about relative drug tolerabilities.. As there were no significant changes in the signs and symptoms of dry eye, olopatadine hydrochloride 0.2% is safe to use in ocular allergy patients with mild-to-moderate dry eye.

Topics: Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Dry Eye Syndromes; Female; Health Status Indicators; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Sodium Chloride; Treatment Outcome

Olopatadine 0.2% (Pataday, Alcon Laboratories Inc., Fort Worth, Texas, USA) and epinastine 0.05% (Elestat, Inspire Pharmaceuticals, Inc., Durham, NC, USA) are topical ocular anti-allergic agents. Both are H(1) antihistamine/mast cell stabilizers indicated for the treatment of ocular itching associated with allergic conjunctivitis.. To compare the efficacy and comfort of olopatadine 0.2% with epinastine 0.05%, in the prevention of ocular itching associated with allergic conjunctivitis following conjunctival allergen challenge (CAC).. This was a 7 week, four visit, double-masked, randomized, placebo-controlled CAC study. Visit 1 screened subjects for positive ocular allergic responses and Visit 2 confirmed those responses. At Visit 3, 92 subjects were randomized into one of four treatment groups to receive one drop of study medication in each eye: (1) olopatadine 0.2%/placebo, (2) epinastine 0.05%/placebo, (3) olopatadine 0.2%/epinastine 0.05%, (4) placebo/placebo. Subjects were challenged 12 h after drop instillation to evaluate duration of action. At Visit 4, subjects were challenged 5 min after drop instillation to evaluate onset of action. Drop comfort was assessed at Visit 4. MAIN OUTCOME MEASURES;. This article focuses on the results of the onset-of-action challenge (Visit 4). At Visit 4, ocular itching was assessed at 3, 5, and 7 min and redness was assessed at 7, 15, and 20 min post-challenge. Drop comfort was assessed upon instillation, at 30s, and at 1, 2, and 5 min post-instillation. Olopatadine 0.2%-treated eyes exhibited significantly lower mean ocular itching scores versus epinastine 0.05%-treated eyes at 5 (p = 0.024) and 7 min (p = 0.003) post-challenge. Olopatadine 0.2%-treated eyes exhibited significantly lower mean redness scores versus epinastine 0.05%-treated eyes at all time points post-challenge (ciliary: p < or = 0.013, conjunctival: p < or = 0.015, episcleral: p < or = 0.006). Olopatadine 0.2% was rated as significantly more comfortable than epinastine 0.05% at 1 min post-drop instillation (p = 0.003). All adverse events were non-serious and unrelated to study medication. Although the CAC model reproduces allergic responses that are not environmentally-induced, patients experience varying severities of responses as are seen in real-world situations.. Olopatadine 0.2% was superior to epinastine 0.05% in preventing ocular itching and redness at onset when induced by the CAC model.

Topics: Adolescent; Adult; Aged; Allergens; Color; Conjunctivitis, Allergic; Dibenzazepines; Dibenzoxepins; Dose-Response Relationship, Drug; Double-Blind Method; Female; Humans; Imidazoles; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Satisfaction; Placebos; Pruritus; Treatment Outcome

Olopatadine 0.1% (Patanol) and olopatadine 0.2% (Pataday) ophthalmic solutions are topical ocular anti-allergic agents with antihistaminic and mast cell stabilizing properties. The efficacy of two doses of olopatadine 0.1% was compared to one dose of olopatadine 0.2% in the prevention of ocular itching associated with allergic conjunctivitis over 24 hours. This double-masked conjunctival allergen challenge (CAC) study found no significant difference in the mean itching scores between two drops of olopatadine 0.1% and one drop of olopatadine 0.2%. Both showed significant activity at the 24-hour time point and were statistically superior to placebo. No adverse events occurred while on drug therapy.

Topics: Adult; Allergens; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Pruritus; Skin Tests; Treatment Outcome

Topics: Administration, Topical; Adolescent; Adult; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Prospective Studies; Treatment Outcome

A new formulation of olopatadine hydrochloride ophthalmic solution (olopatadine 0.2%) was evaluated in two separate, randomized, placebo-controlled, double-masked, hybrid environmental studies intended to determine efficacy and safety in subjects with histories of seasonal allergic conjunctivitis or rhinoconjunctivitis.. In these 10- and 12-week trials (conducted April-August 2003 and July-December 2001, respectively), subjects assessed their ocular signs and symptoms. Additionally, subjects in the 10-week trial evaluated the frequency of their nasal symptoms while subjects in the 12-week trial evaluated both the frequency and severity of their nasal symptoms. The two trials had a combined enrollment of 500 subjects (217 males, 283 females) including 44 children aged 10-17 years; the combined population was 81.4% Caucasian, 9.2% Black, 2% Hispanic, and 7.4% other. Daily throughout these studies, either ragweed (fall study) or grass (spring study) pollen counts were obtained from each investigative center. Slope analyses were conducted on the nasal symptom assessments by pollen count.. The nasal results from the two clinical trials are presented herein. In the fall study, relative to placebo, olopatadine 0.2% significantly reduced the frequency of pollen effects on sneezing (p = 0.0355) and itchy nose (p = 0.0032), and reduced the severity of pollen effects on sneezing (p = 0.0451), itchy nose (p = 0.0178), and runny nose (p = 0.0327). In the spring study, olopatadine 0.2% significantly reduced the frequency of pollen effects on sneezing (p = 0.0017) and runny nose (p = 0.0031) relative to placebo. In the fall trial, 2 subjects discontinued due to treatment-related adverse events (tachycardia and dry eye), while in the spring study, no subject discontinued due to a treatment-related adverse event. No subject in either study suffered a treatment-related serious adverse event.. For the subjects enrolled in these studies, olopatadine 0.2% appeared to be safe, well-tolerated, and effective in significantly reducing the frequency and/or severity of some effects of pollen on nasal symptoms.

Topics: Adolescent; Adult; Child; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Placebos; Rhinitis, Allergic, Perennial

The signs and symptoms of allergic conjunctivitis include ocular redness and itching. Two treatment options currently indicated for acute ocular allergic reaction are pheniramine maleate 0.3%/naphazoline hydrochloride 0.025% ophthalmic solution, an over-the-counter antihistamine/vasoconstrictor combination; and olopatadine hydrochloride 0.1% ophthalmic solution, a prescription antihistamine/mast cell stabilizer.. This study was designed to compare, at onset of action, the relative effectiveness of pheniramine/naphazoline and olopatadine, when administered before conjunctival allergen challenge (CAC), using the ocular allergy index (OAI) as the primary end point.. This was a prospective, randomized, double-masked, contralateral, active- and placebo-controlled, single-center study of the CAC model. The first 2 study visits established and confirmed the subjects' ocular allergic reaction (no medication administered). At visit 3, the subjects were randomly assigned to 1 of 3 contralateral (right eye vs left eye) treatment combinations: pheniramine/naphazoline + olopatadine, pheniramine/naphazoline + placebo, or olopatadine + placebo. Medication was given 10 minutes before CAC. The subjects' erythema in the ciliary, conjunctival, and episcleral vessel beds; eyelid swelling; chemosis; and itching were evaluated at 7, 12, and 20 minutes after CAC. The OAI was calculated as a composite score of 6 signs and symptoms of allergic conjunctivitis to assess global severity. Between-treatment differences in OAI scores were used to evaluate efficacy. Subjects were asked their eye drop preference at the conclusion of visit 3.. Subjects (n = 83) ranged in age from 20 to 70 years (mean, 42.5 years), 61.4% (n = 51) were female, and 94.0% (n = 78) were white. Both pheniramine/naphazoline and olopatadine were associated with significantly lower OAI scores than placebo at all 3 time points (all, P < 0.001). OAI scores were significantly lower with pheniramine/naphazoline than with olopatadine at 12 and 20 minutes (P = 0.005 and P = 0.001, respectively).. In this patient sample, studied in a CAC model of onset of action, prophylactic pheniramine/naphazoline was more effective than olopatadine and placebo in alleviating the signs and symptoms of the acute ocular allergic reaction, as measured by the OAI.

Topics: Administration, Topical; Adult; Aged; Allergens; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Combinations; Female; Humans; Male; Middle Aged; Naphazoline; Olopatadine Hydrochloride; Ophthalmic Solutions; Pheniramine

Topical antiallergic agents, such as antihistamines and mast-cell stabilizers, are the main therapeutic options for seasonal allergic conjunctivitis (SAC). Ketotifen fumarate and olopatadine HCl have dual action that offers a combination of these 2 mechanisms. Although clinical studies comparing the efficacy of these 2 drugs have shown that both were effective in the treatment of SAC, the results were contradictory and did not include the effects of these drugs on inflammatory markers.. The aims of this study were to compare the clinical efficacy of topical ketotifen and olopatadine eye drops and to determine the effects of these 2 drugs on the expression of cell adhesion molecules (CAMs) and inflammatory markers in conjunctival surface cells in patients with SAC.. This 30-day, randomized, double-masked, artificial tear substitute (ATS)-controlled clinical trial was conducted at the Department of Ophthalmology, Karadeniz Technical University, School of Medicine, Trabzon, Turkey. Patients with SAC were included in the study and randomly assigned to 1 of 3 groups: topical ketotifen fumarate 0.025% ophthalmic solution, topical olopatadine HCl 0.1% ophthalmic solution, or ATS (control group). All drugs were administered 2 drops per eye BID for 30 days. At the beginning of the study (day 0; baseline), on day 15, and on day 30, clinical scores (itching, tearing, redness, eyelid, swelling, and chemosis) and conjunctival impression cytology specimens were obtained. The percentages of cells expressing intercellular adhesion molecule 1, vascular CAM-1, human leukocyte antigen-DR, and beta1-integrin (CD29) from conjunctival impression cytology specimens were determined using flow cytometry. Patients were questioned about adverse events (AEs) at each visit. Ocular discomfort on installation of the drugs was recorded as an AE.. Thirty-nine patients (20 men, 19 women; age range, 18-61 years) with SAC were included. Twelve patients received ketotifen; 13, olopatadine; and 14, ATS. In both active-treatment groups, the improvements of clinical scores (tearing and itching) were more pronounced compared with those in the ATS group, although the day-30 difference in tearing score between the olopatadine and ATS groups was not statistically significant. No significant within-group or between-group differences in mean scores for redness, chemosis, or eyelid swelling were found. The expression rates of CAMs and inflammatory markers in conjunctival surface cells were significantly more reduced with ketotifen and olopatadine compared with ATS. However, clinical and flow cytometric parameters were improved with ATS at 15 and 30 days compared with baseline. No AEs were observed during the study period.. In this short-term study in a selected, small study population with SAC, ketotifen and olopatadine diminished the expression of CAMs and inflammatory markers on the conjunctival surface cells effectively. Both active treatments were more efficacious compared with ATS and were well tolerated.

Topics: Adolescent; Adult; Anti-Allergic Agents; Cell Adhesion Molecules; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Female; HLA-DR Antigens; Humans; Integrin beta1; Ketotifen; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Pruritus; Seasons; Tears; Time Factors

Ocular allergies cause itching, redness, chemosis, tearing, and swelling of the eyelids in sensitized individuals. The options available for treatment of ocular allergy include olopatadine 0.1% (Opatanol; Patanol [US]) and ketotifen 0.025% (Zaditen; Zaditor [US]). Patient preference for an eye drop can often be a primary factor in determining the level of compliance and satisfaction with any given therapy.. This study sought patient perspective on eye drop efficacy in controlling signs and symptoms of allergic conjunctivitis and eye drop comfort. Also evaluated were the factors considered by patients when making decisions of preference.. One hundred patients with previous history and current symptoms of seasonal or perennial allergic conjunctivitis were enrolled at two centers (Athens, Greece, N = 50; Padova, Italy, N = 50) for this two visit, double-masked study. Qualified patients received two masked bottles of medication (one olopatadine, one ketotifen) and were asked to use both medications as needed over the course of four weeks, but not to exceed usage of two drops of medication per eye per day. At the second visit, patients answered five questions comparing the two masked medications in terms of preference, drop comfort, and efficacy in treatment of signs and symptoms. Patients also defined the factors upon which they based these decisions.. A significantly greater percentage of patients (81%) selected olopatadine when asked which medication they preferred; which they found more comfortable; which they found more efficacious in reducing symptoms of allergy; and which they would select if visiting the doctor's office (P < 0.0001). Seventy-six percent (76%) of patients considered both efficacy and comfort when making their preference decisions (P < 0.0001). No adverse events were volunteered or elicited.. In this study, patients preferred to use the anti-allergy eye drop olopatadine over ketotifen after using both drops and evaluating relative efficacy and comfort during the course of four weeks. A significantly greater percentage of the patients preferred to use olopatadine during the study period, found it more efficacious and comfortable, and would select olopatadine if visiting their doctor's office during allergy season.

Topics: Administration, Topical; Adolescent; Adult; Aged; Anti-Allergic Agents; Child; Choice Behavior; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Ketotifen; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Satisfaction; Treatment Outcome

Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol) and epinastine hydrochloride 0.05% ophthalmic solution (Elestat) are two topical antiallergic agents. Olopatadine is indicated for the treatment of the signs and symptoms of allergic conjunctivitis that include itching, redness, tearing, lid swelling, and chemosis. Epinastine is indicated for the prevention of itching associated with allergic conjunctivitis.. This study compared the clinical efficacy of olopatadine and epinastine in the prevention of itching and conjunctival redness in the conjunctival allergen challenge (CAC) model.. This was a prospective, randomized, double-masked, contralaterally-controlled, single center allergen challenge study. Ninety-six subjects with a history of allergic conjunctivitis were screened, and the 66 who responded to conjunctival allergen challenge at visits 1 and 2 were randomized into 1 of 3 treatment groups at visit 3 to receive one drop of study medication in each eye: (1) olopatadine in one eye and epinastine in the fellow eye, (2) olopatadine in one eye and placebo in the fellow eye, and (3) epinastine in one eye and placebo in the fellow eye. Five minutes after study drop instillation, subjects were bilaterally challenged with the allergen concentration that had elicited a positive conjunctival allergic response at Visits 1 and 2. Subjective itching assessments were given at 3 min, 5 min, and 7 min post challenge. Objective redness and chemosis assessments were made at 10 min, 15 min, and 20 min post challenge. Paired sample two-tailed t-tests were performed on the mean scores at each time point to assess statistical significance in the differences between treatments. MAIN OUTCOME MEASURES;. Fifty-three subjects were randomized into the olopatadine/epinastine treatment group, the primary analysis group. Olopatadine treated eyes exhibited significantly lower mean itching and conjunctival redness scores than the contralateral epinastine treated eyes, -0.19 (p = 0.003) and -0.52 (p < 0.001), respectively. Olopatadine treated eyes also exhibited significantly less chemosis -0.24 (p < 0.001), ciliary redness -0.55 (p < 0.001), and episcleral redness -0.58 (p < 0.001) than epinastine treated eyes.. Olopatadine is significantly more effective than epinastine in controlling itching, redness and chemosis associated with allergic conjunctivitis in the CAC model.

Topics: Administration, Topical; Adult; Allergens; Anti-Allergic Agents; Conjunctivitis, Allergic; Diagnostic Techniques, Ophthalmological; Dibenzazepines; Dibenzoxepins; Double-Blind Method; Female; Humans; Imidazoles; Male; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Prospective Studies; Treatment Outcome

To compare the efficacy of olopatadine and levocabastine in reducing ocular allergic itching and vascular hyperemia (redness) induced by conjunctival allergen challenge.. The study was a randomized, double-masked, contralateral study using the conjunctival allergen challenge (CAC) model. At Visit 1, subjects with a positive allergen skin test and a history of allergic conjunctivitis were administered increasing concentrations of allergen until at least a moderate grade 2 ocular itching and conjunctival redness response was obtained in both eyes. Allergic signs were graded on standardized 0-4 scales. Subjects who reacted positively were re-challenged at Visit 2 with the pre-determined concentration of allergen. Subjects who again responded with at least a grade 2 bilateral ocular itching and conjunctival redness score at Visit 2 were eligible for drug evaluation. At Visit 3, subjects received olopatadine in one eye and levocabastine in the contralateral eye according to a computer-generated randomization scheme generated prior to commencement of the study. Ocular discomfort was then graded in both eyes. Subjects were bilaterally challenged with the predetermined concentration of allergen 27 min after topical drug administration, such that the first post-challenge assessment was made 30 min post-drug instillation. Allergic signs and symptoms were evaluated at 3 min, 10 min, and 20 min postchallenge and safety and efficacy analyses were performed.. Sixty-eight subjects received study drug and were included in the safety and efficacy analyses. Ocular itching scores for olopatadine were significantly lower than levocabastine at 3 min and 10 min post-challenge (p < 0.001). Ocular redness scores for olopatadine were significantly lower than levocabastine at all time points post-challenge (p < 0.0001). Of all subjects, 4.41% reported ocular discomfort in the olopatadine eye and 26.5% in the levocabastine treated eye.. Olopatadine treated eyes had significantly less itching and redness than levocabastine treated eyes after conjunctival allergen challenge. Olopatadine was also associated with less discomfort upon instillation than levocabastine.

Topics: Adolescent; Adult; Aged; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Piperidines; Severity of Illness Index; Treatment Outcome

Olopatadine hydrochloride 0.1% ophthalmic solution is a topical antiallergy agent indicated for treatment of the signs and symptoms of allergic conjunctivitis. The purpose of this study was to evaluate the comfort of olopatadine used for contact lens wearers in the conjunctival allergen-challenge (CAC) model.. This was a single-center, randomized, double-masked, parallel-controlled CAC study. Contact lens-wearing subjects with a history of allergic conjunctivitis were randomized to receive olopatadine or placebo bilaterally. Fifteen minutes after study medication instillation, subjects inserted contact lenses. Allergen challenge was performed 10 minutes after contact lens insertion. Subjective evaluations of ocular comfort were obtained immediately and every minute after CAC, up to and including 10 minutes. Thereafter, comfort evaluations were made every 5 minutes up to and including 60 minutes. Subjects evaluated itching at 3, 7, and 10 minutes and redness was graded at 5, 10, and 20 minutes. All evaluations were graded on standardized scales. Subjects were given diaries in which to rate comfort at 2, 4, 6, 9, 12, and 13 hours and the time of contact lens removal.. At post-study medication instillation, post-lens insertion, and at time points from 1 to 10 minutes post-allergen challenge, ocular comfort evaluations were statistically superior in subjects receiving olopatadine as compared with those receiving placebo (P < 0.05). The difference in time until contact lens removal was clinically significant, with subjects who were treated with olopatadine wearing lenses for an average of 2.1 hours longer than placebo group.. As evidenced by significantly greater comfort and longer duration of lens wear, olopatadine provides superior comfort to contact lens wearers suffering from the signs and symptoms of seasonal allergic conjunctivitis, as induced by the CAC model.

Topics: Adult; Allergens; Anti-Allergic Agents; Conjunctiva; Conjunctivitis, Allergic; Contact Lenses; Dibenzoxepins; Double-Blind Method; Drug Evaluation; Female; Histamine H1 Antagonists; Humans; Male; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Satisfaction

The most common form of allergic ocular disease is seasonal allergic conjunctivitis, coinciding with the pollen season and generally associated with rhinitis. Symptoms of allergic conjunctivitis include ocular itching, hyperemia, tearing, mucus production, foreign body sensation, chemosis, and lid edema. Similarly, the primary symptoms of allergic rhinoconjunctivitis are nasal itching, irritation, sneezing, watery rhinorrhea, and congestion combined with ocular itching, tearing, and swelling.. This study compared olopatadine 0.1% ophthalmic solution with placebo eyedrops (over-the-counter artificial tear product), instilled in the eye, with regard to the prevention and relief of the ocular and nasal symptoms of seasonal allergic conjunctivitis and rhinoconjunctivitis.. This was a randomized, double-blind, parallel-group study, conducted at 7 US centers, to instill either olopatadine 0.1% ophthalmic solution or placebo eyedrops (artificial tears) in both eyes twice daily for 10 weeks. Patients were evaluated for efficacy (intent-to-treat) and safety. Only patients with proven grass pollen allergy (dermal and conjunctival allergen challenge tests) were selected; all patients were studied during the same period, historically shown to be grass season; and grass pollen counts were obtained.. A total of 131 patients (64 olopatadine; 67 placebo) were assessed for efficacy (intent-to-treat); 132 patients were assessed for safety. The mean (SD) age of participants was 38.53 (11.61) years (range, 18 to 87 years), and 58.0% were women (76/131), with no significant differences between groups for age or sex. In the olopatadine group, 1.6% of patients were black (1/64), compared with 14.9% of the placebo group (10/67) (P = 0.005). Mean scores of ocular itching and hyperemia were lower at all assessment times with olopatadine than placebo. The difference was statistically significant (P < 0.05) for itching on days 7, 14, 35, 63, and 70, and for hyperemia on days 14, 28, 42, and 63, after correction for multiplicity. Linear regression slopes predicting ocular itching and hyperemia from the pollen count were significantly lower (P < 0.003 and P < 0.035, respectively) with olopatadine than with placebo. Similar results were obtained for rhinorrhea, sneezing, and nasal itching (P < 0.006, P < 0.012, and P < 0.034, respectively). With placebo, the proportion of patients with frequent ocular itching and hyperemia increased as a function of pollen level; however, with olopatadine, the proportions remained low and virtually constant.. In the population studied, olopatadine 0.1% ophthalmic solution controlled ocular and nasal symptoms of allergic conjunctivitis and rhinocojunctivitis and was well tolerated when administered twice daily for 10 weeks.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Rhinitis, Allergic, Seasonal; Seasons

To compare the therapeutic effects of two ophthalmic solutions (0.1% olopatadine hydrochloride and 0.5% ketorolac tromethamine) with different pharmacological mechanisms on the clinical signs and Symptoms of seasonal allergic conjunctivitis (SAC).. Forty patients with the signs and symptoms of SAC (i.e. hyperaemia, itching, mucus discharge, tearing) were included in this placebo-controlled, randomized, parallel group, single centre study. In group 1 (20 patients) one eye of each patient was treated with olopatadine and the other with placebo. In group 2 (20 patients) one eye of each patient was treated with ketorolac solution and the other with placebo. The principal signs and symptoms of SAC (hyperaemia and itching) were evaluated at 30 mins and at 2, 7 and 15 days.. In group 1, both parameters improved significantly in eyes treated with olopatadine compared with those receiving placebo at all control examinations (all p < 0.05). Similarly, eyes treated with ketorolac showed significant reductions in signs and symptoms compared with those receiving placebo (all p < 0.05). When the clinical parameters of eyes treated with olopatadine were compared with those treated with ketorolac, the mean score of hyperaemia was found to be lower in the olopatadine group, but the difference was not statistically significant (all p > 0.05). However, the itching score was significantly lower in the olopatadine group from the second day through to the end of the study (p < 0.05).. Both olopatadine and ketorolac ophthalmic solutions were found to be effective in alleviating the clinical signs and symptoms of SAC compared to placebo. However, olopatadine reduces ocular itching significantly more than ketorolac.

Topics: Adolescent; Adult; Anti-Inflammatory Agents, Non-Steroidal; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Hyperemia; Ketorolac Tromethamine; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Therapeutic Equivalency

The eyelids are more susceptible than other tissues to swelling, acute inflammation, and resultant long-term damage. However, no precise, objective means of measuring eyelid swelling in the clinical setting has been developed.. The aims of this study were to assess the novel use of scanning and imaging technology for quantifying eyelid swelling and to use positive and negative controls to assess this new method for potential use in future clinical studies of eyelid swelling and pharmaceutical agents' effects on it.. This was a 1-visit, single-center, prospective, randomized, double-masked, placebo-controlled study using the conjunctival allergen challenge (CAC). After baseline examinations and eyelid scanning, medication was instilled as follows: olopatadine hydrochloride 0.1% ophthalmic solution in 1 eye and placebo in the other. An allergen solution to which patients had a history of reaction was instilled in each eye 15 minutes after instillation of medication. Evaluations were performed for itching (3, 5, and 7 minutes after CAC), redness and chemosis (10, 15, 20, and 30 minutes), subjective eyelid evaluation (15 and 30 minutes), and 3-dimensional (3D) objective eyelid scan (15 and 30 minutes).. One hundred seven patients were randomized. Fifty-six patients (35 women, 21 men; mean age, 44.7 years) were evaluable for efficacy. Results of the objective and subjective evaluations of eyelid swelling were consistent, indicating significantly less eyelid swelling in olopatadine-treated eyes than in those that received placebo (objective evaluation, P < 0.001 at 15 minutes, P < 0.017 at 30 minutes; subjective evaluation, P < 0.001 at 15 and 30 minutes). Patients rated eyelid swelling in the placebo eye as 2.31 times and 2.40 times greater than that in the olopatadine-treated eye at 15 and 30 minutes, respectively. However, the digitally scanned eyelid swelling was calculated to be 5.65 times and 1.76 times greater in the placebo eye at the same respective time points. Reduction of ocular chemosis was observed in olopatadine-treated eyes at all time points (P < 0.001).. In this study, eyelid swelling was quantifiably measured with 3D imaging technology. In this model, the standard antiallergy medication olopatadine, used as a positive control, significantly modulated eyelid swelling when used prophylactically. A negative control, artificial tears, did not significantly affect the allergic eyelid-swelling reaction. These results concurred with subjective grading but offered a more precise assessment of eyelid swelling.

Topics: Adult; Aged; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Eyelids; Female; Humans; Imaging, Three-Dimensional; Lasers; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Prospective Studies

It is presumed that exposure to allergens in the environment occurs through both the eyes and the nose. Allergic rhinoconjunctivitis is typically treated with a nasal spray or systemic antihistamine, neither of which may provide adequate relief of the ocular component of the disease.. This study was designed to gain a better understanding of the physiologic interaction between the conjunctival and nasal mucosa and thus help establish a profile for the most effective ocular treatment in patients whose allergies have both an ocular and a nasal component.. This was a single-center, randomized, double-masked clinical study using the conjunctival allergen challenge (CAC) and nasal allergen challenge (NAC) models. It compared the clinical signs and symptoms induced by CAC and NAC, the effects of drugs administered by 3 different routes, and the movement of fluorescein after instillation into the eye and nose (Jones test), and assessed levels of of inflammatory mediators in tears and nasal secretions. At visit l, subjects previously identified as CAC responders underwent NAC to determine the dose of allergen necessary to elicit a sufficient positive reaction. At visit 2, which took place 1 week later, subjects with a positive reaction at visit 1 were randomized to group A (CAC) or group B (NAC), and underwent challenge to confirm the allergen dose necessary to produce a positive reaction. Subjects who qualified were randomized to receive 1 of 3 treatments: olopatadine 0.1% ophthalmic solution, placebo nasal spray, and placebo tablets; mometasone furoate monohydrate 50-microg nasal spray, placebo topical solution, and placebo tablets; or fexofenadine hydrochloride 180-mg tablets, placebo topical solution, and placebo nasal spray. All study medications were administered according to their approved labeling: drops were administered twice daily in the eyes, and the nasal sprays and tablets were administered once daily. At visit 3, which took place 1 week after visit 2, subjects received study medication and 15 minutes later underwent CAC or NAC as before. The primary efficacy variables were ocular itching, ocular redness, and overall nasal symptoms (sneezing, rhino rrhea/postnasal drip, nasal pruritus, palatal pruritus, and nasal congestion) rated on standard scales. Peak nasal inspiratory flow (PNIF) was measured at each visit, and the Jones test was performed at visits 1 and 3. At baseline and after challenge at visits 2 and 3, tear and nasal lavage samples were collected from a subset of randomly selected subjects for analysis of eosinophil cationic protein and tryptase.. Seventy-three subjects (42 women, 31 men; mean age, 45.26 years [range, 21-73 years]) were screened, and all were randomized to treatment. Two subjects did not complete the study. CAC induced clinically significant (>1 unit difference) ocular and nasal signs and symptoms, whereas NAC induced clinically significant nasal signs and symptoms only. In group A, there was a greater reduction in ocular itching with olopatadine compared with mometasone and fexofenadine at 3 minutes (P = 0.003 and P = 0.008, respectively) and 5 minutes (P = 0.007 and P = 0.013) after challenge. Although the difference was not statistically significant, overall relief of conjunctival redness (average of 3 vessel beds) was greatest in the olopatadine group, followed by fexofenadine. In group B, prevention of total nasal symptoms was significantly greater with mometasone compared with fexofenadine at 20 minutes (P = 0.006) and 30 minutes (P = 0.014) after challenge. There were no statistically significant differences between treatment groups in nasal symptom scores at any time point after CAC. There were also no significant differences in PNIF between treatment groups. Fluorescein was present in nasal secretions within 5 minutes of being instilled into the eye; no fluorescein was detected in the eye after instillation into the nose.. In this study, exposure of the nasal mucosa to allergen resulted in allergic rhinitis, and exposure of the ocular the ocular surface to allergen resulted in conjunctivitis with a secondary effect in the nose. These results suggest movement of allergens, their mediators, and antiallergy drugs from the ocular surfaces into the nasal cavity, with no meaningful movement from the nasal cavity to the ocular surface. In this controlled model, both the systemic agent and the nasal spray failed to control ocular symptoms. The topical ophthalmic solution provided the most effective management of allergic ocular signs and symptoms, and the nasal spray was most effective for nasal symptoms. Combined use of a nasal spray and topical ophthalmic solution may provide maximal relief in patients whose allergies have both ocular and nasal components.

Topics: Administration, Intranasal; Administration, Oral; Administration, Topical; Adult; Aged; Allergens; Anti-Allergic Agents; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Male; Middle Aged; Mometasone Furoate; Nasal Mucosa; Olopatadine Hydrochloride; Ophthalmic Solutions; Pregnadienediols; Rhinitis, Allergic, Perennial; Tablets; Terfenadine; Time Factors

The purpose of this study was to assess the effects of olopatadine on the release of mast cell-derived mediators after conjunctival allergen challenge(CAC) in humans.. This was a double-masked, randomized, placebo-controlled clinical trial. Subjects with a clinical history of seasonal allergic conjunctivitis (but no current symptoms or treatment at baseline) were studied. At visit 1, subjects underwent bilateral CAC with increasing doses of allergen every 15 minutes until a significant clinical reaction was obtained, then were evaluated at 15 minutes and 5 hours after CAC. At visit 2 (2 weeks later), subjects were rechallenged to confirm the allergic response. Subjects exhibiting positive reactions at both visits (at both 15 minutes and 5 hours) were randomized and instructed to treat 1 eye with olopatadine and the contralateral eye with placebo (commercially available artificial ears) in a double-masked fashion twice daily for the 5 days immediately preceding visit 3. At visit 3, bilateral CAC was performed with the same dose as at visit 2. Itching and redness were recorded. Tear cytology for inflammatory cell counts(ie, neutrophils, eosinophils, and lymphocytes) was carried out using precolored slides, and cell numbers were counted at 400x magnification. Tear histamine was assessed using radioimmunoassay histamine measurement. Intercellular adhesion molecule (ICAM)-1/CD54 monoclonal antibody was used for immunohistochemical staining of conjunctival epithelial cells obtained by impression cytology. Slides were examined by 3 masked investigators and redness was classified on a scale of 0 (absent) to 3 (very intense).. Ten subjects completed the trial. Olopatadine significantly reduced postchallenge itching and redness compared with placebo (P < 0.01 and P < 0.03,respectively). Olopatadine also reduced the number of neutrophils and the total number of cells at 30 minutes (both P = 0.015), and the number of eosinophils(P < 0.001), neutrophils (P < 0.004), lymphocytes (P = 0.011), and total number of cells (P = 0.001) at 5 hours postchallenge compared with placebo. Tear histamine levels were significantly lower after challenge in the eyes pretreated with olopatadine compared with placebo (mean [SD], 7 [8] vs 22 [12] nmol/L; P = 0.04). Olopatadine significantly reduced tear histamine levels compared with those measured in the same eyes after CAC at visit 2 (P = 0.001), whereas placebo did not affect histamine levels. Olopatadine also significantly reduced ICAM-1 expression compared with placebo at 30 minutes and 5 hours postchallenge(P < 0.03 and P < 0.01, respectively).. In the present study, olopatadine significantly reduced the levels of histamine, cellular infiltrate, and ICAM expression compared with placebo after CAC, suggesting that it reduced the release of mast cell-derived mediators in humans. This inhibition of mediator release correlated with reduction of itching and redness.

Topics: Administration, Topical; Adult; Allergens; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Histamine; Histamine H1 Antagonists; Humans; Immunohistochemistry; Intercellular Adhesion Molecule-1; Male; Mast Cells; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Tears; Time Factors

Olopatadine hydrochloride 0.1% ophthalmic solution and loteprednol etabonate 0.2% ophthalmic suspension are topical antiallergic agents indicated for treatment of the signs and symptoms of allergic conjunctivitis and seasonal allergic conjunctivitis (SAC), respectively.. The purpose of this study was to compare the efficacy and tolerability of olopatadine, loteprednol, and placebo in inhibiting the early-phase allergic reaction (within 30 minutes) after conjunctival allergen challenge (CAC).. This was a single-center, randomized, double-masked, parallel-controlled CAC study. It consisted of 3 visits, with CAC performed at visit 1, confirmation and randomization at visit 2, and evaluation of the treatments at visit 3. Subjects with a history of allergic conjunctivitis were randomized to receive olopatadine, loteprednol, or placebo in a 2:2:1 ratio. Because loteprednol requires a loading period to achieve maximum efficacy, subjects assigned to this treatment received loteprednol QID bilaterally for a 14-day period; the olopatadine and placebo groups received placebo QID bilaterally during this period. At the evaluation visit, subjects received 1 drop of the assigned treatment in each eye. Fifteen minutes later, they were challenged with allergen. Subjects evaluated itching at 3, 5, and 10 minutes after challenge using a standardized 5-point scale; the investigator evaluated redness at 10, 15, and 20 minutes after challenge. Intraocular pressure (IOP) was measured at baseline and after the 14-day loading period. Nonparametric analyses were performed on the change from visit 2 to visit 3 in mean itching and redness scores for each time point, and on the change in mean IOP from visit 1 to visit 3.. Fifty subjects (86% white; 42% male, 58% female; age range, 21-71 years) were enrolled and completed the study (20 olopatadine, 20 loteprednol, 10 placebo). The allergens to which subjects reacted were ragweed pollen (40%), cat hair or dander (30%), grass pollen (24%), and tree pollen (6%). The difference in inhibition of itching and redness was clinically significant (> or =1 unit difference) and statistically significant (P < 0.05) in favor of olopatadine compared with loteprednol at all 3 time points. The loteprednol group had a statistically significant increase in IOP after 2 weeks of treatment (P < 0.001).. In the population studied, olopatadine was more efficacious than loteprednol in reducing the acute signs and symptoms of SAC during the early phase of the ocular allergic reaction and appeared to be better tolerated.

Topics: Adult; Aged; Androstadienes; Anti-Inflammatory Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Intraocular Pressure; Loteprednol Etabonate; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Treatment Outcome; Visual Acuity

One approach to treating allergic rhinoconjunctivitis is the concomitant use of an intranasal spray such as fluticasone propionate to alleviate nasal symptoms and a topical or systemic agent to relieve ocular symptoms. It has not yet been determined whether a topical or systemic agent is more effective for the latter purpose.. This study compared the efficacy of combined use of fluticasone and olopatadine with combined use of fluticasone and fexofenadine in the treatment of the signs and symptoms of allergic rhinoconjunctivitis.. This 2-site, randomized, double-masked, placebo-controlled, parallel-group study employed the conjunctival allergen challenge (CAC) model, a standardized method of inducing ocular and nasal signs and symptoms of allergic rhinoconjunctivitis. At visit 1, subjects underwent CAC to determine the dose of allergen required to elicit a positive reaction. The allergen dose was confirmed at visit 2, and, according to a randomization schedule, subjects were dispensed fluticasone, olopatadine, and placebo pill; fluticasone, fexofenadine, and tear substitute; or placebo nasal spray, placebo pill, and tear substitute. CAC took place at visit 3, after patients had used the assigned medications for 2 weeks. Study medication was instilled 2 hours before CAC, after which allergic signs and symptoms were graded on standardized scales. The primary efficacy variables were ocular itching, ocular redness, and overall nasal symptoms.. Eighty subjects completed the study: 30 received fluticasone and olopatadine, 30 fluticasone and fexofenadine, and 20 placebo. Women constituted 63.8% of the study population and men 36.3%; 91.3% were white, 3.8% black, 2.5% Hispanic, 1.3% Asian, and 1.3% other. Concomitant use of fluticasone and olopatadine produced significantly greater improvements in ocular itching at 3 and 7 minutes after CAC compared with fluticasone and fexofenadine (P < 0.05). There were no significant differences in redness scores between groups; however, concomitant use of fluticasone and olopatadine produced significantly greater improvements in redness at 2 time points in each of the 3 vessel beds (ciliary, conjunctival, and episcleral) compared with placebo, and fluticasone and fexofenadine produced significantly greater improvement in redness at 1 time point in I vessel bed compared with placebo (both comparisons, P < 0.05). The 2 treatments had similar effects on total nasal symptom efficacy scores.. In this study, concomitant use of the topical agents fluticasone and olopatadine was more effective than concomitant use of fluticasone plus fexofenadine for overall treatment of the signs and symptoms of induced allergic rhinoconjunctivitis.

Topics: Administration, Intranasal; Administration, Topical; Adult; Allergens; Androstadienes; Anti-Allergic Agents; Anti-Inflammatory Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Therapy, Combination; Female; Fluticasone; Histamine H1 Antagonists; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Rhinitis, Allergic, Perennial; Terfenadine; Treatment Outcome

Treatments for allergic conjunctivitis have various mechanisms of action. Cromolyn sodium stabilizes conjunctival mast cells by preventing calcium influx across the cell membrane, whereas olopatadine hydrochloride is both an antihistamine and a mast cell stabilizer.. This study compared the efficacy and tolerability of olopatadine and cromolyn in controlling the ocular signs and symptoms of seasonal allergic conjunctivitis.. This was a multicenter, randomized, double-masked, parallel-group trial. One group instilled olopatadine 0.1% ophthalmic solution and placebo BID, and the other instilled cromolyn 2% ophthalmic solution QID, both for 6 weeks. The formulation of cromolyn used in this study is currently available only in Europe and Australia.. The intent-to-treat efficacy and safety analyses included 185 patients, 91 in the olopatadine group and 94 in the cromolyn group. At 30 minutes after the first instillation, respective decreases of approximately 30% and approximately 20% were reported in self-rated ocular itching and redness with both treatments; by 4 hours, itching had decreased by approximately 38% in both groups. Differences between treatments were not statistically significant. At 4 hours, redness had decreased by approximately 38% and approximately 26% in the respective treatment groups. By day 42, both treatments had produced significant reductions from baseline in ocular signs and symptoms; however, the reductions in itching and redness were significantly greater with olopatadine compared with cromolyn (both variables, P < 0.05). The difference in physicians' impression of overall improvement on days 30 and 42 significantly favored olopatadine over cromolyn (both days, P < 0.05). Most patients (62.2%) had reacted positively to grass pollen at baseline. The regression slopes correlating itching and redness with pollen count were 5 times lower for olopatadine compared with cromolyn (P = 0.002 and P = 0.016, respectively), indicating that olopatadine's efficacy increased as the pollen count increased.. Six weeks' instillation of olopatadine 0.19% ophthalmic solution BID had a significantly greater effect on the ocular signs and symptoms of allergic conjunctivitis compared with 6 weeks' instillation of cromolyn 2% ophthalmic solution QID. Both treatments were well tolerated by patients in all age groups; however, olopatadine appeared to have better local tolerability in children aged <11 years.

Topics: Adolescent; Adult; Aged; Anti-Allergic Agents; Child; Child, Preschool; Conjunctivitis, Allergic; Cromolyn Sodium; Dibenzoxepins; Double-Blind Method; Humans; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Seasons

Olopatadine ophthalmic solution 0.1% (Patanol, Alcon Laboratories, Fort Woth, TX) is approved for the treatment of the signs and symptoms of allergic conjunctivitis. Loratadine 10 mg (Claritin, Schering-Plough, Madison, NJ) is a nonsedating oral antihistamine approved for the treatment of the signs and symptoms of allergic rhinitis.. To compare the efficacy of olopatadine used adjunctively with loratadine versus loratadine alone in patients with seasonal allergic conjunctivitis.. This three-center, observer-masked, treatment-controlled, randomized, parallel-group study involved patients aged 7 to 74 years with seasonal allergic conjunctivitis. Patients were treated for 7 days with either olopatadine twice daily adjunctive to loratadine once daily or only loratadine once daily. Efficacy variables (ocular itching and redness, physician's impression, patient's impression, patient diary ratings of ocular redness and itching), and safety parameters were evaluated during the screening visit and on days 0, 3, and 7. Patients completed the rhinoconjunctivitis quality of life questionnaire on days 0 and 7.. Ninety-four patients received study drug. Patients receiving olopatadine twice daily in addition to loratadine once daily exhibited less ocular itching (P = 0.0436) and rated their ocular condition as more improved compared with those receiving loratadine alone (P < 0.0022). Twenty minutes after initial dosing, olopatadine plus loratadine relieved ocular itching and redness significantly better than loratadine alone (P = 0.001). Both treatment groups showed clinically meaningful improvements in overall quality of life in all but one of the rhinoconjunctivitis quality of life questionnaire domains. Overall, and in most domains, olopatadine plus loratadine also provided significantly better (P < 0.05) quality of life than loratadine alone at day 7.. Compared with loratadine alone, olopatadine adjunctive to loratadine provides greater relief of ocular itching and redness, a better quality of life, and is well tolerated in patients with seasonal allergic conjunctivitis.

Topics: Adolescent; Adult; Aged; Asthenia; Child; Conjunctivitis, Allergic; Dibenzoxepins; Drug Therapy, Combination; Dyspepsia; Female; Humans; Loratadine; Male; Middle Aged; Olopatadine Hydrochloride; Xerostomia

Olopatadine hydrochloride 0.1% ophthalmic solution and azelastine hydrochlofide 0.05% ophthalmic solution are 2 topical antiallergic agents indicated for the treatment of itching of the eye associated with allergic conjunctivitis. Olopatadine has recently received US Food and Drug Administration (FDA) approval for an expanded indication for the treatment of signs and symptoms of allergic conjunctivitis, including itching, tearing, eyelid swelling, redness, and chemosis.. The purpose of this study was to compare the efficacy of olopatadine hydrochloride versus azelastine hydrochloride and placebo (artificial tears) in the conjunctival allergen challenge (CAC) model.. This was a prospective, randomized, double-masked, contralaterally controlled, multicenter, allergen-challenge study. Itching was chosen as the primary efficacy variable since it is the only FDA-approved indication these 2 agents have in common. Subjects with a history of allergic conjunctivitis who responded to the CAC at screening visits 1 and 2 were randomized to 1 of 3 treatment groups: olopatadine in 1 eye and azelastine in the other eye; olopatadine in 1 eye and placebo in the other eye; or azelastine in 1 eye and placebo in the other eye. At the assessment visit (visit 3), subjects received masked study medication according to the randomization scheme. After 5 minutes, subjects were bilaterally challenged with the allergen concentration that had elicited a positive conjunctival allergic response at visits 1 and 2. Immediately after challenge, subjects gave itching assessments (scale, 0 = no itching to 4 = severe itching) every 30 seconds for a total period of 20 minutes. Mean itching scores for all eyes were compared by treatment. Mean itching scores at each time point were compared between treatments using 2 sample t tests.. Of the 180 subjects screened, 111 responded to the CAC at visits 1 and 2 and completed the study; 65% (72/111) of patients were female, 87% (97/111) were white, and 49% (54/111) had brown irides. The mean age was approximately 40 years. Seventy-three eyes were treated with olopatadine, 75 with azelastine, and 74 with placebo. A single dose of 1 of the 3 study medications per eye was well tolerated by all subjects. Both treatments were significantly more effective than placebo at reducing itching postchallenge. Olopatadine was significantly more effective than azelastine in reducing itching at 3.5 minutes through 20 minutes postchallenge (average mean unit difference of -0.31; P < 0.05) in the CAC model.. In this population, olopatadine was significantly more effective than azelastine in the management of itching associated with allergic conjunctivitis in the CAC model.

Topics: Adult; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Phthalazines; Prospective Studies

The efficacy of Patanol, a topically applied anti-allergic agent, was evaluated in a group of patients with allergic conjunctivitis due to contact lens wear (GROUP I) and a group comprised of seasonal allergic conjunctivitis patients, vernal conjunctivitis patients and atopic keratoconjunctivitis patients (GROUP II).. One drop of Patanol was administered to each eye twice daily. Signs and symptoms were assessed 7, 14, and 28 days after initiation of drug therapy.. Itching/burning, tearing, hyperemia and papillary reaction were reduced to scores of 0/1 (absent/mild) in 85%, 90%, 81% and 62%, respectively, of GROUP I patients at Day 28. The allergic conditions in GROUP II patients also improved with Patanol treatment. Itching/burning, tearing, hyperemia and papillary reactions were absent/mild in 60%, 76%, 96% and 90%, respectively, of these patients at Day 28.. Patanol treatment effectively and rapidly alleviated the signs and symptoms of allergic conjunctivitis due to contact lens wear as well as vernal conjunctivitis, atopic keratoconjunctivitis and the common seasonal allergic conjunctivitis. Patanol allowed allergic patients to be more comfortable while permitting them to continue using contact lenses.

Topics: Acute Disease; Chronic Disease; Conjunctivitis, Allergic; Contact Lenses, Hydrophilic; Dibenzoxepins; Drug Evaluation; Histamine H1 Antagonists; Humans; Olopatadine Hydrochloride; Treatment Outcome

To compare the clinical efficacy of Patanol (olopatadine hydrochloride ophthalmic solution 0.1%) to Claritin (loratadine 10 mg) tablets, in the conjunctival allergen challenge model.. This was a randomized, double-masked, single center, contralateral controlled, antigen challenge model study. The concentration of allergen that elicited a positive response was determined at Visits 1 and 2 (itching > or = 2 and redness > or = 2 OU). At Visit 3, 29 subjects were randomized into two groups. Fifteen subjects received Claritin tablet and Patanol ophthalmic solution 0.1% in one eye and placebo in the contralateral eye. Fourteen subjects received placebo tablet and Patanol in one eye and placebo in the contralateral eye. One hour after drug administration, subjects were challenged with the antigen that elicited a positive response. At 3, 7, and 10 minutes, itching was subjectively evaluated. At Visit 4, the same procedure was followed as in Visit 3, but antigen challenge occurred 8 hours after drug instillation.. Results were analyzed by eye. Eyes treated with Patanol (concomitant with placebo tablet) had significantly lower ocular itching scores when compared to eyes treated with placebo (concomitant with Claritin) at 3, 7 and 10 minutes in the onset of action evaluation (p < 0.05). Eyes treated with Patanol (concomitant with placebo tablet) had significantly lower ocular itching scores at 7 minutes and there was a statistical trend (0.05 < p < 0.1) at 10 minutes in duration of action evaluation.. Patanol therapy was significantly more efficacious than Claritin in reducing ocular itching related to allergic conjunctivitis.

Topics: Acute Disease; Allergens; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Evaluation; Female; Histamine H1 Antagonists; Humans; Loratadine; Male; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Tablets; Time Factors

To compare the ocular comfort of two ophthalmic anti-allergic agents: olopatadine hydrochloride 0.1% and ketotifen fumarate 0.05%.. In a double-masked, multi-centered, randomized trial, 80 subjects were asked to make a 'forced choice' based on ocular comfort between one drop of olopatadine hydrochloride 0.1% instilled in one eye and one drop of ketotifen fumarate 0.05% instilled in the contralateral eye. At one site, the incidence of adverse reactions was also reported.. All subjects (100%) selected olopatadine as the more comfortable formulation. One site (n = 35) reported a 49% incidence of moderate burning and a 49% incidence of mild burning after ketotifen instillation. One subject (2% of population) at this site experienced no ocular discomfort with ketotifen. There were no reports of discomfort associated with olopatadine instillation.. Olopatadine is a more comfortable ophthalmic preparation than ketotifen.

Topics: Choice Behavior; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Histamine H1 Antagonists; Humans; Ketotifen; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Satisfaction

Mast cell stabilizers, such as the ocular antiallergic agent nedocromil sodium 2% ophthalmic solution, are not rapid acting and often require a loading period of > or =2 weeks for maximal efficacy. Olopatadine hydrochloride 0.1% ophthalmic solution is a member of a new class of topical antiallergic agents that have combined antihistaminic and mast cell-stabilizing properties.. The purpose of this study was to compare the clinical efficacy and comfort of olopatadine with those of nedocromil in the conjunctival allergen challenge model.. This was a single-center, 3-visit, randomized, double-masked, contralaterally controlled study. Seventy-five subjects with a history of allergic conjunctivitis were screened, and the 52 who responded to conjunctival allergen challenge at visits I and 2 were randomized by eye to receive olopatadine, nedocromil, or placebo (a "natural tears" lubricant eye drop). Because nedocromil may require a 2-week loading period for maximal efficacy, the eyes assigned to that agent received nedocromil for 14 days (between visits 2 and 3), whereas the eyes assigned to olopatadine or placebo received placebo during this period. Throughout the loading phase, subjects instilled 1 drop of the assigned masked medication in each eye twice daily. At the assessment visit (visit 3), subjects received I drop of masked olopatadine, nedocromil, or placebo in each eye and were asked to rate the comfort of each drop on a scale from 0 to 8. Fifteen minutes after instillation of medication, subjects were challenged with the allergen concentration that had elicited a positive conjunctival allergic response at the previous visits. Subjects then scored their itching on a scale from 0 to 4 at 3, 5, and 10 minutes after challenge. Mean itching scores for all eyes were compared by treatment. Paired t tests were performed on the mean itching and ocular comfort scores at each time point. At the end of the study, subjects were asked which treatment they preferred in terms of comfort and efficacy.. Forty-nine subjects completed the study. Forty eyes received olopatadine, 36 received nedocromil, and 22 received placebo. Olopatadine was clinically and statistically superior to nedocromil at reducing itching in the conjunctival allergen challenge model (mean unit difference: -1.60 at 3 minutes, -1.68 at 5 minutes, -1.19 at 10 minutes; P < 0.001). One drop of olopatadine was more efficacious than 29 drops of nedocromil. Olopatadine-treated eyes were rated as being significantly more comfortable than nedocromil-treated eyes (0.73 vs 1.55; P = 0.034). Of the 14 subjects treated with olopatadine and nedocromil who stated a preference, 10 (71%) were more satisfied with olopatadine than with nedocromil.. In the conjunctival allergen challenge model, olopatadine was more efficacious and comfortable than nedocromil in reducing the itching associated with allergic conjunctivitis.

Topics: Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Humans; Nedocromil; Olopatadine Hydrochloride; Ophthalmic Solutions; Patient Satisfaction; Placebos

This study was conducted to compare the efficacy and safety of olopatadine ophthalmic solution (0.1%) with ketorolac ophthalmic solution (0.5%) in a clinical model of acute allergic conjunctivitis. Olopatadine is a dual acting H1 histamine receptor antagonist and a mast cell stabilizer, shown to be effective in treating allergic conjunctivitis. Ketorolac is a non-steroidal anti-inflammatory drug approved in the United States for the relief of ocular itching associated with seasonal allergic conjunctivitis.. The provocative antigen challenge model was used in this randomized, double-blind, single-center, crossover study. The allergen and concentration that consistently elicited a positive allergic reaction was used for challenge. After at least 14 days, subjects were randomized to receive either olopatadine in one eye and placebo in the contralateral eye, or ketorolac in one eye and placebo in the contralateral eye. Twenty-seven minutes after drug instillation subjects were challenged with allergen. At 3, 10, and 20 minutes following allergen challenge, subjects graded ocular itching and were assessed for hyperemia in conjunctival, ciliary, and episcleral vessel beds. Approximately 14 days later, subjects received the alternate treatment in one eye and placebo in the contralateral eye. They were again challenged with allergen and their responses were rated in the same manner.. Olopatadine significantly (p < 0.0001) reduced both ocular itching and hyperemia in all three vessel beds compared to placebo at all time points tested following allergen challenge. Ketorolac did not significantly reduce itching and showed a trend of increased hyperemia compared to placebo. Olopatadine was significantly (p < 0.001) more effective than ketorolac in reducing hyperemia and ocular itching at all time points and was also significantly (p < 0.05) more comfortable than ketorolac as reported by subjects immediately following drug instillation.. The study demonstrated that olopatadine is effective and safe in preventing and treating ocular itching and hyperemia associated with acute allergic conjunctivitis and is more effective and more comfortable than ketorolac.

Topics: Acute Disease; Adult; Aged; Allergens; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Cross-Over Studies; Dibenzoxepins; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Ketorolac; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Safety; Seasons; Treatment Outcome

Allergic conjunctivitis very often occurs simultaneously with rhinitis in seasonal allergy sufferers. While systemic anti-allergic and antihistaminic agents are effective against many signs and symptoms of allergy, they may not adequately control ocular signs and symptoms in patients with multiple target organ hypersensitivity. Patanol (olopatadine hydrochloride 0.1% ophthalmic solution, Alcon Laboratories, Inc., Fort Worth, TX), a new effective anti-allergic mast cell stabilizer with antihistaminic properties, is approved for the prevention of ocular itching due to allergic conjunctivitis.. To determine whether Patanol in combination with the systemic antihistamine Claritin (loratadine, Schering, Kenilworth, NJ) reduces the ocular itching associated with allergic conjunctivitis more effectively than Claritin alone. A topical ocular antigen challenge induced the allergic conjunctivitis in 15 subjects.. This was a randomized, double-masked study in which the contralateral eye served as the control. On Visit 1, an allergen dose which elicited response scores > 2 for ocular itching was identified. Itching was graded by the subject using a 0 to 4 point scale. At Visit 2, the threshold allergen concentration was confirmed. At Visit 3, the onset of action challenge, in addition to Claritin (10 mg tablet), each subject received Patanol in one eye and placebo in the fellow eye in a randomized, double-masked fashion. Allergen was instilled one hour after dosing, and ocular itching was graded at 3, 7, 10 and 20 minutes after challenge. At Visit 4, the duration of action challenge, the same drug regimen was followed as in Visit 3. However, allergen challenge was performed eight hours after dosing, and itching graded after 3, 7, 10 and 20 minutes.. Patient eyes treated with Patanol were significantly less itchy than those treated with systemic Claritin alone at critical time points 3, 7, and 10 minutes after the onset of action challenge (p < 0.05), and at 3 and 7 minutes after the duration of action challenge (p < 0.05).. The addition of topical Patanol to systemic Claritin therapy significantly reduced ocular itching associated with allergic conjunctivitis compared to treatment with Claritin alone. These findings prove the added benefit of local Patanol therapy in the treatment of ocular allergic symptoms in patients receiving systemic antihistamines for concomitant systemic allergies.

Topics: Administration, Oral; Adult; Allergens; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Therapy, Combination; Female; Histamine H1 Antagonists; Humans; Loratadine; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Safety; Treatment Outcome

To evaluate the effectiveness and safety of olopatadine hydrochloride and to determine its optimal concentration and the onset and duration of action for treating allergic conjunctivitis. Olopatadine is a new topical ophthalmic antiallergic agent that demonstrates activity as both an antihistamine and a mast cell stabilizer. Two double-masked, randomized, placebo-controlled, contralateral eye comparison studies were conducted using the conjunctival allergen challenge model.. A total of 169 subjects received 0.05% or 0.1% olopatadine. Study subjects were healthy adult men and women with a history of active allergic conjunctivitis within the previous two seasons but not receiving current treatment. With an allergen dose that produced signs and symptoms of allergic conjunctivitis at visits 1 and 2, the conjunctival allergen challenge was performed 27 minutes after study drug administration at the third visit (onset-of-action challenge) and at 8 hours after study drug administration at the fourth visit (duration-of-action challenge). Olopatadine was administered in one eye and placebo in the opposite eye. Itching and redness were scored for both eyes at 3, 10, and 20 minutes after the conjunctival allergen challenge.. Both 0.05% and 0.1% concentrations of olopatadine were significantly (P < .05) more effective than placebo in inhibiting itching and redness at all evaluations when administered 27 minutes or 8 hours before the conjunctival allergen challenge. There were no serious or drug-related ocular or nonocular adverse events in either study.. These findings demonstrate the rapid and prolonged (at least 8 hours) ocular antiallergic action of olopatadine.

Topics: Adolescent; Adult; Aged; Aged, 80 and over; Allergens; Anti-Allergic Agents; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Drug Evaluation; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Models, Biological; Olopatadine Hydrochloride; Ophthalmic Solutions; Pollen; Safety

An ophthalmic antiallergic agent with selective H1 antihistaminic and mast cell stabilizing properties has been developed.. To evaluate efficacy and safety, determine optimal concentration, and demonstrate onset and duration of action of this new drug, olopatadine.. This was a placebo-controlled, randomized, double-masked, parallel-group, single-center study with five outpatient visits at least 7 days apart. Ninety-eight healthy, allergy-positive, subjects with a recent history of active allergic conjunctivitis not receiving current treatment participated. Conjunctival allergen challenge (CAC) tests were performed on visits 1 and 2 to identify an allergen and concentration that consistently elicited signs and symptoms of allergic conjunctivitis. On visits 3, 4, and 5, CAC was performed 27 minutes, 8 hours, and 6 hours, respectively, after instillation of one drop of olopatadine (0.01%, 0.05%, 0.1%, or 0.15%) in one eye and placebo in the other. Both eyes were scored for the intensity of itching and redness at 3, 10, and 20 minutes after the CAC.. All four concentrations of olopatadine were clinically and statistically superior to placebo in preventing ocular itching at all evaluations and preventing redness at most evaluations from immediately and 8 hours after drug administration. No drug-related adverse events were reported. The 0.1% concentration was found to be most effective.. The results indicate that olopatadine ophthalmic solution is safe and effective in the treatment of allergic conjunctivitis, with the 0.1% concentration of olopatadine being optimal. The rapid onset and at least 8 hour duration of action of olopatadine indicates that the drug can be used twice daily.

Topics: Adult; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Male; Middle Aged; Models, Immunological; Olopatadine Hydrochloride; Ophthalmic Solutions; Time Factors

This study found 0.7% olopatadine (Pataday Once Daily Relief Extra Strength) eye drops to provide better initial comfort than 0.3% pheniramine maleate/0.025% naphazoline hydrochloride (VISINE® Allergy Eye Relief Multi-Action Antihistamine and Redness Reliever) eye drops suggesting that patients may comply better with the Pataday than VISINE.. To compare the ocular comfort at instillation of Pataday and VISINE allergy eye drops.. Minimally symptomatic participants were recruited based upon Standard Patient Evaluation of Eye Dryness (SPEED) questionnaire scores (≤3 units); they also had minimal between-eye inter-ocular comfort differences as judged by visual analogue scale scores (VAS; ≤7 units). Baseline comfort was evaluated by eye with a VAS. One drop of Pataday or VISINE was then applied to the right eye with the alternative drop being applied to the left eye. The same VAS evaluated comfort by eye at drop instillation, and then at 30 seconds, 1 minute, and 2 minutes post-instillation. Drop experience was also evaluated with Likert questions. LogMAR visual acuities and bulbar conjunctival redness were evaluated pre- and post-drop instillation.. A total of 159 participants were recruited (mean ± SD age = 26.2 ± 7.5). The VAS found that eyes treated with Pataday were significantly more comfortable at instillation than eyes treated with VISINE. Likert questions indicated that participants significantly preferred Pataday drops compared to the VISINE drops at instillation with regards to overall eye comfort, eye stinging, eye burning, and foreign body sensation. There were no between drop differences in visual acuity, though eyes treated with VISINE were less red than eyes treated with Pataday.. Topically applied Pataday drops were more comfortable than VISINE drops.

Topics: Adolescent; Adult; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Humans; Naphazoline; Olopatadine Hydrochloride; Ophthalmic Solutions; Pheniramine; Young Adult

To compare the ocular comfort at application of topical, over-the-counter, 0.7% olopatadine and 0.035% ketotifen fumarate anti-allergy eye drops.. This study recruited participants who were minimally symptomatic based upon Standard Patient Evaluation of Eye Dryness (SPEED) questionnaire scores (≤3 units) and who had minimal between-eye inter-ocular comfort differences as judged by visual analog scale scores (VAS; ≤7 units). Baseline comfort was evaluated by eye with a VAS. One drop of 0.7% olopatadine or 0.035% ketotifen fumarate was then applied to the right eye with the alternative drop being immediately applied to the left eye. Participants were next evaluated with the same comfort VAS by eye at drop application, and then at 30 s, 1 min, and 2 min post-application. LogMAR visual acuities and bulbar conjunctival redness were evaluated pre- and post-drop application to judge initial changes.. This study enrolled 159 participants who had a mean ± SD age of 26.3 ± 7.7 years, and 78.6% of the participants were female. The VAS found that the 0.7% olopatadine drop was more comfortable than the 0.035% ketotifen fumarate drop at all time-points. There were no between-eye differences in LogMAR visual acuities, yet bulbar redness was significantly less in 0.7% olopatadine treated eyes compared 0.035% ketotifen fumarate treated eyes.. This study found that topically applied 0.7% olopatadine drops were initially more comfortable than 0.035% ketotifen fumarate drops.

Topics: Adolescent; Adult; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Female; Humans; Ketotifen; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Young Adult

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.. 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. 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. 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: Adolescent; Adult; Aged; Conjunctivitis, Allergic; Dibenzoxepins; Eye; Female; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Prospective Studies; Young Adult

Ophthalmic preparations that contain ketorolac tromethamine (KET) and olopatadine HCl (OLO) are used to relieve seasonal allergies and allergic conjunctivitis. Simultaneous quantification of KET and OLO was held by validated and simple spectrophotometric methods. KET was determined directly from the fundamental UV absorption spectra (at 323 nm), while OLO was determined after performing either dual wavelength or ratio derivative methods. The first method was based on measuring the absorbance difference (ΔA) between 243 and 291 nm, while the second depended on generating first derivative ratio spectra using 3.0 µg/mL KET as a divisor and measuring OLO responses at 234 nm (minima). Multiple standard addition method was applied to enable the determination of OLO which is considered as the weakly absorbing species as well as the minor component in a challenging dosage form ratio (4:1). The linearity ranges of the developed methods were 3-12 μg/mL and 4-40 μg/mL for KET and OLO, respectively. Simultaneous determination of both drugs was successfully implemented to lab prepared eye drops that contain KET, OLO and benzalkonium chloride as an inactive ingredient. Greenness assessment indicates minimal impact on environment. The developed methods determined the cited drugs with % recovery ± SD of 99.63 ± 0.01 for KET, 100.90 ± 0.02 and 100.31 ± 0.01 for OLO using dual wavelength and first derivative ratio methods, respectively. Using F-test and t-test at confidence level %95 to compare between the results of the presented methods and a reported method show no significant difference which allows precise, accurate, rapid, and simple quantification of quality control samples that contain KET and OLO.

Topics: Conjunctivitis, Allergic; Humans; Ketorolac Tromethamine; Olopatadine Hydrochloride; Ophthalmic Solutions; Spectrophotometry

Glaucoma is a neuropathy disorder and is generally treated by drugs. Allergic conjunctivitis is a common ophthalmologic disease. Paraoxonase 1 (PON1) is an organophosphate hydrolyzer and antiatherogenic enzyme. PON1 is known for preventing atherosclerosis through lipid-modifying features, as well as which has decisive actions of antiapoptosis, anti-inflammatory, antithrombosis, and antiadhesion antioxidant activity properties. Thus, reducing the enzyme levels in hyperthyroidism, chronic renal failure, glaucoma, diabetes mellitus, and cardiovascular diseases is a significant risk. This study was tested some ophthalmic drugs used to treat the diseases, such as glaucoma and allergic conjunctivitis, mentioned above, travoprost, latanoprost, ketotifen, emedastine, and olopatadine, for their inhibition activities against PON1. These drugs displayed the potent inhibition effect with IC

Topics: Aryldialkylphosphatase; Conjunctivitis, Allergic; Humans; Molecular Docking Simulation; Olopatadine Hydrochloride; Travoprost

Olopatadine HCl is an antiallergic drug used for the management of allergic conjunctivitis. Currently, it is delivered via eye drop solution, which is highly inefficient due to low bioavailability. Silicone contact lenses can be used to sustain the release of ophthalmic drugs. However, the presence of drug alters the optical transmittance and physical properties of the contact lens. The objective was to design a novel polyvinyl pyrrolidone (PVP)-coated olopatadine-ethyl cellulose microparticles-laden doughnut contact lens to sustained ocular delivery with limited alteration to the optical and swelling properties of the contact lens. The doughnut was implanted within the periphery of the lens using modified casting technique. Olopatadine HCl was loaded by soaking (SM-OL), direct loading (DL-OL), and doughnut casting method (DNT-OL). PVP (comfort agent) was loaded on the surface of contact lens for all the batches via novel curing technique. The in vitro olopatadine HCl release data of SM-OL (up to 48-72 h) and DL-OL batches (up to 72 h) showed high burst release, whereas DNT-OL batch showed sustained release up to 120 h without significant (p > 0.05) alteration in the optical and swelling properties of contact lens. All the batches showed sustained release of PVP up to 120 h. The in vivo studies in the rabbit tear fluid showed improvement in the olopatadine HCl and PVP retention time in comparison to eye drop solution. The PVP-loaded DNT-OL-500 lens showed tear stabilization (comfort wear) in Schirmer strip test (rabbits) with no protein adherence in comparison to DNT-OL-500 lens without PVP. The study demonstrated the successful delivery of olopatadine HCl and PVP-K30 from the doughnut contact lens for the extended period with limited alteration to the optical and swelling properties of contact lens.

Topics: Animals; Conjunctivitis, Allergic; Contact Lenses; Drug Liberation; Olopatadine Hydrochloride; Ophthalmic Solutions; Polyvinyls; Povidone; Rabbits

Topics: Anti-Allergic Agents; Conjunctivitis, Allergic; Cyproheptadine; Humans; Immunoglobulin E; Keratoconjunctivitis; Male; Middle Aged; Olopatadine Hydrochloride; Omalizumab

The aim of the current study was to investigate whether olopatadine and naphazoline hydrochloride reduce allergic conjunctivitis in mice through alterations in inflammation, NGF and VEGF. An allergic conjunctivitis mouse model was established using histamine or an antigen (ovalbumin), following which mice were treated with 1% olopatadine solution and/or 0.2 mg/ml of naphazoline hydrochloride. Histamine or antigen‑induced conjunctival vascular hyperpermeability was examined and the levels of inflammatory factors, cytokines, IgE, GMCSF and NGF were analyzed using ELISA in antigen‑induced conjunctival vascular hyperpermeability mice. In addition, VEGF protein expression was measured using western blotting in antigen‑induced mice. The results indicated that olopatadine and naphazoline hydrochloride significantly suppressed conjunctival dye leakage in mice with histamine or antigen‑induced conjunctival vascular hyperpermeability. In addition, treatment with olopatadine and naphazoline hydrochloride was able to reduce the levels of inflammatory factors (TNF‑α, IL‑1β and IL‑6), cytokines (IFN‑γ and IL‑4), IgE, GMCSF, and NGF in antigen‑induced conjunctival vascular hyperpermeability mice. The protein expression levels of VEGF in antigen‑induced conjunctival vascular hyperpermeability mice were reduced following treatment with olopatadine and naphazoline hydrochloride. These results suggest that treatment with olopatadine and naphazoline hydrochloride reduces conjunctivitis in mice via effects on inflammation, NGF and VEGF.

Topics: Animals; Blotting, Western; Conjunctivitis, Allergic; Cytokines; Disease Models, Animal; Drug Therapy, Combination; Enzyme-Linked Immunosorbent Assay; Female; Granulocyte-Macrophage Colony-Stimulating Factor; Histamine; Immunoglobulin E; Mice; Mice, Inbred BALB C; Naphazoline; Nerve Growth Factor; Olopatadine Hydrochloride; Ovalbumin; Vascular Endothelial Growth Factor A

Combination of the ability of contact lenses (CLs) to act as a physical barrier against airborne antigen and to serve as a sustained depot of antihistaminic drugs may improve the efficiency of treatments of some ocular allergic diseases. The aim of this work was to develop CLs that exhibit affinity to olopatadine by mimicking the composition of the natural H1-receptor for which olopatadine behaves as a selective antagonist. Functional monomers that match the chemical groups of the receptor and application of the molecular imprinting technology led to hydrogels able to load high amounts of olopatadine and to sustain the release once in contact with lachrymal fluid. Optimized hydrogels prepared with acrylic acid, 2-acrylamido-2-methyl-1-propanesulfonic acid and benzylmethacrylate as functional monomers provided in few hours olopatadine concentrations similar to those of commercially available eye drops but the levels could be sustained for a whole day, demonstrating their efficacy. Olopatadine-loaded CLs successfully passed the HET-CAM test of ocular irritancy and showed good compatibility with mast cells. They were able to inhibit the release of histamine and TNF-α from sensitized mast cells, proving their potential application in preventing and treating allergic conjunctivitis.. Contact lenses (CLs) with affinity for antiallergic drugs may constitute an advantageous alternative to eye drops in management of ocular allergies for both contact lens wearers and patients who eventually use neutral CLs as therapeutic platforms. The present work represents a step forward in the state of the art of drug-CL combo products by (i) mimicking the composition of the human receptor of the drug, (ii) exploring combinations of functional monomers that include a monomer (2-acrylamido-2-methyl-1-propanesulfonic acid; AMPSA) with a strong acid group (pKa<4) able to enhance the interaction of the network with olopatadine in the saline environment of the lachrymal fluid, and (iii) analysing in detail the antihistamic effects provided by olopatadine released from the CLs on sensitized mast cells.

Topics: Amino Acids; Animals; Biomimetic Materials; Cell Line; Cell Survival; Chickens; Conjunctivitis, Allergic; Contact Lenses; Drug Liberation; Histamine; Hydrogels; Mast Cells; Materials Testing; Mice; Molecular Imprinting; Olopatadine Hydrochloride; Tumor Necrosis Factor-alpha

Topics: Betamethasone; Child; Conjunctivitis, Allergic; Dibenzoxepins; Drug Therapy, Combination; Humans; Male; Olopatadine Hydrochloride; Recurrence

This study was undertaken to evaluate possible antiallergic effects of an extract of pigments from green sea urchin (Strongylocentrotus droebachiensis) shells. Effects were studied on animal models - guinea pig ileum contraction, rabbit eyes allergic conjunctivitis, and rabbit local skin irritation. The extract significantly reduced, in a dose-dependent manner, the histamine-induced contractions of the isolated guinea pig ileum with ID50 =1.2 µg/mL (in equivalents of spinochrome B), had an inhibitory effect on the model of ocular allergic inflammation surpassing the reference drug olopatadine, and did not show any irritating effect in rabbits. The extract predominantly contained polyhydroxy-1,4-naphthoquinone which would be responsible for the pharmacological activity. The active compounds of the extract were evaluated in silico with molecular docking. Molecular docking into H1R receptor structures obtained from molecular dynamic simulations showed that all spinochrome derivatives bind to the receptor active site, but spinochrome monomers fit better to it. The results of the present study suggest possibilities for the development of new agents for treating allergic diseases on the base of pigments from sea urchins shells.

Topics: Animal Shells; Animals; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Disease Models, Animal; Dose-Response Relationship, Drug; Guinea Pigs; Histamine; Ileum; Male; Molecular Docking Simulation; Naphthoquinones; Olopatadine Hydrochloride; Pigments, Biological; Rabbits; Skin; Strongylocentrotus

Fixed drug eruption (FDE) usually develops after oral administration and is described as a cutaneous reaction recurring at the same location each time the drug is taken. Olopatadine is both a H1 histamine receptor antagonist and a mast cell stabilizer, indicated for the treatment of allergic conjunctivitis. Here, we report a 14-year-old male patient who developed FDE localised on the lateral side of periorbital rim bilaterally, whilst applying olopatadine 0.1% ophthalmic solution for the treatment of allergic conjunctivitis. As far as we know, FDE due to olopatadine has not been previously reported in the literature. We deem it appropriate to report this case because FDE that results from the application of topical drugs is a rare event in the literature.

Topics: Administration, Topical; Adolescent; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Dibenzoxepins; Drug Eruptions; Humans; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Orbit; Orbital Diseases

Olopatadine hydrochloride ophthalmic solution, 0.2% (olopatadine 0.2%) is a multi-action agent approved in Japan for allergic conjunctivitis when used as a dose of 1 to 2 drops twice-daily. The objective of this study was to evaluate the long-term (10 weeks) safety and efficacy of olopatadine 0.2% in Japanese patients with allergic conjunctivitis when used as a dose of 2 drops twice-daily.. This was a single-insititution, open-label, single-group study of symptomatic patients > or = 12 years of age with allergic conjunctivitis.. A total of 110 Japanese patients were enrolled. From baseline to week 10, the mean (95% confidence interval) absolute changes were -2.4 (-2.7, -2.2) in ocular itching and the total hyperemia scores were -3.2 (-3.4, -2.9). Mean scores for all other efficacy variables were low at baseline (< or = 2.4) and decreased to < or = 0.6 by week 10. There were no serious adverse events. Mild eye irritation (1 patient) was the only treatment-related event. No safety concerns were identified in a review of the safety results.. Based on this study, olopatadine 0.2% is generally safe, well tolerated and effective when instilled as 2 drops in both eyes twice-daily in Japanese patients with allergic conjunctivitis and is a useful new option for ocular allergy management.

Topics: Adolescent; Adult; Anti-Allergic Agents; Child; Conjunctivitis, Allergic; Dibenzoxepins; Drug Administration Schedule; Female; Humans; Instillation, Drug; Japan; Male; Middle Aged; Olopatadine Hydrochloride

We present the case of an 11-year-old boy who had bilateral implantation of intrastromal corneal ring segments for progressive keratoconus and poor vision. No intraoperative or postoperative complications were seen, and 1 year postoperatively, the patient maintained good spectacle-corrected vision.. Neither author has a financial or proprietary interest in any material or method mentioned.

Topics: Child; Conjunctivitis, Allergic; Corneal Stroma; Corneal Topography; Dibenzoxepins; Drug Therapy, Combination; Functional Laterality; Humans; Intraoperative Complications; Keratoconus; Male; Olopatadine Hydrochloride; Polymethyl Methacrylate; Postoperative Complications; Prednisolone; Prostheses and Implants; Prosthesis Implantation; Visual Acuity

To evaluate the effectiveness of pre-seasonal treatment with topical olopatadine on the reduction of clinical symptoms of seasonal allergic conjunctivitis (SAC).. Prospective interventional case series.. Eleven patients with SAC received topical olopatadine in one eye at least two weeks before the onset of allergy symptoms, and the other eye served as the control. After the onset of allergic conjunctivitis, both eyes were treated with topical olopatadine. Visual analogue scale (VAS), which evaluated the subjective symptoms of ocular allergy, and the tear levels of histamine and substance P were measured up to six weeks.. At the onset of allergy symptoms, the VAS score in the pretreatment eyes was statistically significantly lower than that in the control eyes. The VAS score in the control eyes decreased with time but did not decrease to the level seen in the pretreatment eyes until four weeks later. The tear level of substance P at the onset of allergy symptoms was significantly suppressed in the pretreatment eyes, while the level of histamine was not suppressed. Alteration of the VAS scores in the pretreatment eyes significantly correlated with the level of substance P, but not of histamine.. To suppress clinical symptoms in patients with SAC, pre-seasonal treatment with topical olopatadine is effective. The effectiveness of treatment correlates with the tear level of substance P.

Topics: Administration, Topical; Adult; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine; Histamine H1 Antagonists, Non-Sedating; Humans; Immunoglobulin E; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Pain Measurement; Pollen; Premedication; Prospective Studies; Seasons; Substance P; Tears; Treatment Outcome

Antihistamines constitute the first line of therapy for allergic conjunctivitis, and are safe and effective in relieving the signs and symptoms of ocular allergy. Despite this, they are less effective than some other drugs in relieving delayed symptoms of allergic conjunctivitis. Recent evidence suggests that changes in the conjunctival epithelium may underlie aspects of delayed reactions. In this study we compared two antihistamines, olopatadine and alcaftadine, for their ability to modify epithelial cell changes associated with allergic conjunctivitis at time points selected to reflect late-phase reactions.. Studies employed a modified conjunctival allergen challenge model. Sensitized mice were challenged with topical allergen with or without drug treatments. Treatment groups were assayed for acute-phase (15 minutes) and delayed-phase (24 hours) responses. Groups were scored for allergy symptoms (redness, itch, tearing, and edema) and for conjunctival mast cell numbers. Delayed-phase groups were also examined for eosinophil numbers and for tight junctional protein expression.. Olopatadine-treated and alcaftadine-treated animals had similar efficacy profiles and mast cell numbers, suggesting both were effective at ameliorating symptoms of the acute phase. In contrast, alcaftadine-treated animals had significantly lower conjunctival eosinophil infiltration than either controls or olopatadine-treated animals. Allergen challenge caused a significant decrease in expression of the junctional protein, ZO-1, and this decrease was prevented by alcaftadine but not by olopatadine.. Alcaftadine displays therapeutic properties beyond its antihistamine action. These include an ability to reduce conjunctival eosinophil recruitment, and a protective effect on epithelial tight junction protein expression.

Topics: Animals; Anti-Allergic Agents; Benzazepines; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Disease Models, Animal; Eosinophils; Epithelium; Gene Expression Regulation; Imidazoles; Membrane Proteins; Mice; Mice, Inbred BALB C; Olopatadine Hydrochloride; Phosphoproteins; Tight Junctions; Time Factors; Zonula Occludens-1 Protein

The study shows the antihistaminic and anti-inflammatory efficient treatment with olopatadina 0.1%.. The study group consisting of 30 patients evaluated in the ophthalmological ambulatory between the period of april-august 2007 were diagnosed with acute seasonal allergic conjunctivites. Ig E and seric eosinofiles were quantified for all patients and the severity of conjunctivitis was evaluated by summing up the scores of the cardinal signs of allergic conjunctivitis: itching, conjunctival hyperemia and tearing. For a month every patients was treated with olopatadina 0.1% 2x1 drop/day. They were evaluated in day 1, day 8 and day 30. The tolerance of the treatment was judged by the reduced symptoms after olopatadine instilation.. The score in day 1 was higher in children under 16 years of age who presented itching and tearing. After day 8 of treatment the scores droped significantly and after a month the scores decreased highly to a percentage from 60-85%.. Choosing the best therapy in allergic conjunctivitis involves studying the mechanism implicated in triggering the allergy Olopatadina 0.1% with its double mechanism has proven to be efficient in moderate seasonal allergic conjunctivitis.

Topics: Adolescent; Adult; Aged; Anti-Allergic Agents; Child; Child, Preschool; Conjunctivitis, Allergic; Dibenzoxepins; Female; Humans; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Retrospective Studies; Seasons; Severity of Illness Index; Treatment Outcome

In order to compare the relative efficacy of topical antihistamines with balanced saline solution (BSS) and benzalkonium chloride (BC) in the early phase of allergic conjunctivitis in an animal model of ocular anaphylaxis, 96 male guinea pigs were sensitized with intraperitoneal egg albumin (EA) and aluminum hydroxide. Seventy-six animals were used for determination of Evans blue (EB) extravasation and 20 for clinical evaluation of the allergic response (redness, edema, discharge and itch-scratch response). Eighteen days after sensitization the animals were topically challenged by conjunctival instillation of EA and treated 15 min before and 15 min after challenge with commercially available drugs (ketotifen, ketotifen single dose units [SDU], olopatadine, azelastine, spaglumic acid and emedastine) and controls (BSS and BC). The animals used for EB quantification were anesthetized and received an intravenous injection of EB simultaneously to the topical challenge. The ocular extravasation of the colorant was determined by 620 nm absorbance spectrophotometry. The animals used for clinical evaluation were observed for clinical signs of the allergic reaction. EB ocular extravasation was significantly lower in the eyes treated by spaglumic acid and emedastine. The clinical scoring was consistent with EB extravasation, though the difference was not statistically significant. Spaglumic acid and emedastine seem to be the most useful drugs to reduce EB extravasation and allergic signs in an animal model of early phase allergic conjunctivitis.

Topics: Animals; Anti-Allergic Agents; Benzimidazoles; Coloring Agents; Conjunctivitis, Allergic; Dibenzoxepins; Dipeptides; Disease Models, Animal; Drug Evaluation, Preclinical; Evans Blue; Guinea Pigs; Histamine H1 Antagonists; Ketotifen; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Phthalazines; Severity of Illness Index; Treatment Outcome

Conjunctival mast cells (MCs) are important effector cells in seasonal allergic conjunctivitis, via histamine and cytokine secretion. Several new anti-allergic eye drops stabilize MCs and block histamine receptors, but their anti-inflammatory effects are unclear.. Anti-allergic drugs were compared for their anti-inflammatory effects in an in vitro model of human MC activation and in an experimental murine model of allergic conjunctivitis.. Human cord blood stem cell-derived (CBMC) and conjunctival biopsy-derived MCs were stimulated via FcepsilonRI, degranulation and histamine release were assayed at 1 h and cytokine secretion at 24 h using multiplex arrays. Mice sensitized to short ragweed pollen were given anti-allergics topically before allergen challenge, and conjunctival immuno-staining was performed at 24 h.. After a 1 h stimulation, 80% of the CBMC had degranulated and secreted histamine (27.9+/-4.7 ng/10(6) cells; P<0.05). Pre-treatment by all drugs significantly reduced histamine and TNF-alpha, whereas IL-5, IL-8, IL-10 and TNF-beta profiles were differentially decreased. For conjunctival biopsy-derived cultures (n=11), FcepsilonR1 stimulation increased histamine, TNF-alpha, TNF-beta, IL-5 and IL-8 levels and the production of IL-5, IL-6 (P<0.05), histamine and IL-8 (P<0.01) was inhibited by epinastine. In vivo, epinastine and olopatadine pre-treatment significantly reduced the clinical scores and eosinophil numbers (n=6; P<0.05) while epinastine also reduced neutrophils (P<0.02).. Differential effects on MC cytokine inhibition were observed, with epinastine inhibiting MC secretion of IL-5, IL-8, IL-10 and conjunctival neutrophil infiltration. The anti-allergic drugs have anti-histamine and mast-cell stabilizing properties but might differ in clinical improvement depending on the individual and the cytokines involved.

Topics: Animals; Anti-Allergic Agents; Cell Differentiation; Cell Movement; Cells, Cultured; Conjunctiva; Conjunctivitis, Allergic; Cytokines; Dibenzazepines; Dibenzoxepins; Eosinophilia; Female; Fetal Blood; Histamine Release; Humans; Imidazoles; Mast Cells; Mice; Mice, Inbred BALB C; Nedocromil; Neutrophils; Olopatadine Hydrochloride; Pollen; Proto-Oncogene Proteins c-kit; Receptors, IgE; Stem Cells

In an advertisement in this journal, Alcon Nederland BV has recommended Opatanol (olopatadin) as the 'first choice medication/NHG practice guideline for Red eye/Allergic conjunctivitis'. However, the practice guideline of the Dutch College of General Practitioners (NHG) mentions the following 3 antihistaminica as first choice for the treatment of red eye/allergic conjunctivitis: azelastin, levocabastin or olopatadin. Therefore, it is concluded that the Alcon advertisement is misleading.

Topics: Advertising; Anti-Allergic Agents; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists; Humans; Netherlands; Olopatadine Hydrochloride; Practice Guidelines as Topic

The mechanism by which eosinophils adhere to the ocular surface during allergic inflammation is unknown. This study examined whether the incubation of human conjunctival epithelial cells (HCEs) with tears from allergic subjects promotes eosinophil adhesion, and it examined the effect of treatment with olopatadine on this process.. Allergic subjects (n = 6) and nonallergic subjects (n = 4) were treated in season for 1 week with olopatadine in one eye while the other eye remained untreated. Tears were collected from both eyes with the use of a microcapillary tube. HCEs were acquired by enzymatic digestion of cadaveric conjunctival tissues. Confluent cultures of HCEs were treated with diluted tears for 24 hours before incubation with peripheral blood eosinophils (purified with negative magnetic bead selection). Eosinophil adhesion was measured with an eosinophil peroxidase assay.. Incubation of HCEs with tears from allergic subjects significantly upregulated eosinophil adhesion compared with eosinophil adhesion to untreated HCEs or with HCEs treated with nonallergic tears and untreated HCEs (P < 0.05). Eosinophil adhesion to HCEs treated with tears from olopatadine-treated allergic subjects was inhibited (P < 0.01) compared with tear-stimulated adhesion observed from untreated eyes. Percentage of inhibition was 43.3% +/- 13.9% (mean +/- SD). Blocking antibodies demonstrated that eosinophil adhesion to HCEs in vitro involved beta2 integrins on eosinophils but not intercellular adhesion molecule-1 on human HCEs.. Tears collected from allergic subjects contain bioactivity capable of upregulating eosinophil adhesion to HCEs in vitro. Inhibition of this process by treatment of subjects with olopatadine suggests that some of the cellular targets of this drug may play a role in promoting eosinophil adhesion.

Topics: Adult; Anti-Allergic Agents; Antibodies, Blocking; CD18 Antigens; Cell Adhesion; Cell Separation; Cells, Cultured; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Eosinophils; Epithelial Cells; Female; Humans; Intercellular Adhesion Molecule-1; Male; Middle Aged; Models, Biological; Olopatadine Hydrochloride; Skin Tests; Tears; Up-Regulation

This study estimated the health economic impact of olopatadine (Opatanol) compared to branded cromoglycate (Opticrom) and generic sodium cromoglycate in the treatment of seasonal allergic conjunctivitis (SAC) in the UK.. This was a modelling study performed from the perspective of the UK's National Health Service (NHS).. A decision model was constructed depicting the management of SAC sufferers who are 4 years of age or above over a typical allergy season of 4 months and considers the decision by a GP to initially treat a patient with olopatadine, branded or generic cromoglycate. The analysis assumed both drugs to be equally effective. Consequently, a cost-minimisation analysis was performed to identify the least costly alternative.. Starting treatment with olopatadine is expected to lead to a healthcare cost of 92 pounds sterling (95% CI: 46 pounds sterling; 150 pounds sterling) over 4 months compared to 109 pounds sterling (95% CI: 65 pounds sterling; 166 pounds sterling) with branded cromoglycate and 95 pounds sterling (95% CI: 51 pounds sterling; 152 pounds sterling) with generic cromoglycate, resulting in a 16% and 3% reduction in healthcare costs respectively over 4 months of treatment. This cost-difference is primarily due to fewer GP visits among olopatadine-treated patients.. Use of olopatadine instead of branded or generic cromoglycate affords an economic benefit to the NHS. Hence, within the limitations of the model, olopatadine is the preferred first-line treatment for use in SAC sufferers, since it is expected to lead to fewer GP visits, thereby releasing healthcare resources for alternative use.

Topics: Anti-Asthmatic Agents; Conjunctivitis, Allergic; Cromolyn Sodium; Decision Support Techniques; Dibenzoxepins; Drug Costs; Drugs, Generic; Humans; Olopatadine Hydrochloride; Seasons; United Kingdom

The eye drop Opatanol (its main component is olopatadine, which has an antihistaminic and membrane-stabilizing effect) in Hungary is not well known yet.. In 2004 and 2005 in the ragweed season we had treat with olopatadine eyedrop for 2 weeks (two times daily) 37 children, who had ragweed allergy. The average age of the 23 boys was 8.8 years, and for the 14 girls 10.5 years. In July and August of 2004 10 adult allergic female (average of their age: 29,2 years) also had receive olopatadine for 2 weeks. The severity of the symptoms was recorded by using a scale from 0 to 3 (where 3 indicates the most severe symptoms) before and 2 weeks after the beginning of the treatment, and the average was calculated.. The discomfort feeling decreased from 2.4 +/- 0.5 to 0.8 +/- 0.2 in children, and from 1.5 +/- 0.9 to 0 in adults, the itching from 2.5 +/- 0.4 to 0.2 +/- 0.1 in children, and from 1.6 +/- 1.2 to 0 in adults, the foreign body sensation from 1.6 +/- 0.9 to 0.7 +/- 0.4 in children, and from 1.3 +/- 1.1 to 0 in adults, the tearing from 1.9 +/- 0.9 to 1.0 +/- 0.3 in children, and from 1.0 +/- 1.0 to 0.1 in adults, and the redness from 2.2 +/- 0.4 to 1.1 +/- 0.2 in children and from 1.9 +/- 0.8 to 0.5 +/- 0.5 in adults. We observed side effect in one child (the redness of the conjunctiva increased after the application of the eye drop) and in two adults (burning sensation for short time, in the other case foreign body sensation for 30 seconds).. The anti-allergic eye drop olopatadine is a safe and effective treatment for seasonal allergic conjunctivitis even in childhood. It is comfortable, to use twice daily is sufficient.

Topics: Adolescent; Adult; Anti-Allergic Agents; Anti-Inflammatory Agents, Non-Steroidal; Child; Child, Preschool; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists, Non-Sedating; Humans; Hungary; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Retrospective Studies; Seasons; Severity of Illness Index; Treatment Outcome

To investigate the effects of topical epinastine and olopatadine on tear volume by using a mouse model.. Eighty-five C57BL6 mice (170 eyes) were treated twice daily with topical ophthalmic epinastine 0.05%, olopatadine 0.1%, or atropine 1% or served as untreated controls. A thread-wetting assay was used to measure tear volume at baseline and 15, 45, 90, 120, and 240 minutes after the last instillation of the drug on days 2 and 4 of treatment.. After 2 days of treatment, epinastine-treated mice showed greater mean tear volumes than olopatadine-treated mice did at 15, 45, 90, and 240 minutes, with statistical significance at 15 and 45 minutes (P<0.001). Olopatadine significantly reduced tear volume versus untreated controls at 15 and 45 minutes (P<0.001). After 4 days, tear volumes with epinastine treatment exceeded those with olopatadine treatment at all time points, with statistical significance at 45 minutes (P<0.05). Atropine rendered tears undetectable at 15, 45, and 90 minutes; tear volume returned to baseline levels at 240 minutes.. Topical epinastine did not inhibit tear secretion, whereas olopatadine caused a significant decrease in tear volume. Because of its neutral impact on the lacrimal functional unit, epinastine may be an especially good choice for the treatment of allergic conjunctivitis in patients with dry eye disease or in those who are at risk for developing dry eye.

Topics: Administration, Topical; Animals; Conjunctivitis, Allergic; Dibenzazepines; Dibenzoxepins; Female; Histamine H1 Antagonists; Histamine H1 Antagonists, Non-Sedating; Imidazoles; Lacrimal Apparatus; Male; Mice; Mice, Inbred C57BL; Olopatadine Hydrochloride; Ophthalmic Solutions; Tears

To study the effects of ketotifen fumarate, olopatadine, and levocabastine on ocular active anaphylaxis in guinea pigs and on ocular immediate hypersensitivity in albino rats.. Clinical grading scores and Evans blue dye leakage to eyelids and to eyeballs were assessed in five treatment groups (n = 10): ketotifen fumarate 0.025%, olopatadine 0.1%, levocabastine 0.05%, negative control, and positive control.. At 20 minutes after challenge, edema scores for ketotifen-treated guinea pigs were statistically significantly lower than those for levocabastine or olopatadine. Active treatment significantly reduced vascular leakage in both models. Ketotifen significantly reduced vascular leakage in eyelids compared with the other drugs. In guinea pigs, vascular leakage in eyeballs was significantly reduced with ketotifen fumarate compared with olopatadine and levocabastine.. In the guinea pig model, ketotifen was more effective than olopatadine and levocabastine at reducing conjunctival edema and vascular permeability in eyelids and eyeballs. In the rat model, ketotifen was more effective at reducing vascular permeability in eyelids than olopatadine and levocabastine.

Topics: Anaphylaxis; Animals; Capillary Permeability; Conjunctivitis, Allergic; Dibenzoxepins; Disease Models, Animal; Edema; Eyelids; Guinea Pigs; Histamine H1 Antagonists; Ketotifen; Male; Olopatadine Hydrochloride; Ophthalmic Solutions; Ovalbumin; Piperidines; Rats

The aim of this study was to investigate the effect of topical 0.1% olopatadine hydrochloride on goblet cell density, clinical signs, and symptoms of patients with vernal keratoconjunctivitis.. Between December 2002 and April 2003, 40 eyes of 20 patients with vernal keratoconjunctivitis and 10 healthy eyes of 5 control patients were evaluated prospectively and treated with 0.1% olopatadine hydrochloride. Both groups were observed clinically, subjective complaints were recorded, and changes in goblet cell density were obtained with brush cytology.. After the 2-month therapy, subjective complaints and clinical signs improved with therapy. Also, the clinical signs were improved with the therapy. As the severity of the signs and symptoms were reduced, goblet cell numbers in the brush cytologic specimens were reduced.. Olopatadine hydrochloride 0.1% is an effective agent for relieving the signs and symptoms of vernal keratoconjunctivitis. Also, it reduces the number of goblet cells, which, in turn, decreases the amount of mucus discharge in vernal keratoconjunctivitis during treatment.

Topics: Adult; Cell Count; Cell Degranulation; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Male; Mast Cells; Middle Aged; Olopatadine Hydrochloride; Prospective Studies

Topics: Anti-Allergic Agents; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Dibenzoxepins; Drug Monitoring; Histamine H1 Antagonists; Humans; Olopatadine Hydrochloride; Patient Education as Topic; Patient Selection

Topics: Anti-Allergic Agents; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Tablets

Olopatadine hydrochloride 0.1% eye drops represent a new class of anti-allergic agent with combined antihistaminic and mast cell-stabilizing properties.. The purpose of this study was to describe alterations in tear function and the ocular surface in patients with allergic conjunctivitis and to analyze the effect of topical olopatadine treatment on corneal sensitivity, tear function, and impression cytology variables.. This was a single-center, 3-visit, prospective, open-label study conducted in patients with allergic conjunctivitis. Patients received 1 drop of topical olopatadine hydrochloride 0.1% BID for 3 weeks. At each visit, patients and healthy control subjects underwent routine ophthalmic examinations and measurements of corneal sensitivity and tear function (Schirmer test of tear quantity, tear film break-up time [BUT], fluorescein staining of the cornea). All control subjects and a subgroup of patients also underwent conjunctival impression cytology for assessment of squamous metaplasia and goblet cell density. The outcomes of interest were changes in corneal sensitivity, tear function, and impression cytology variables after 3 weeks of treatment with olopatadine eye drops, both in patients with allergic conjunctivitis and between patients and controls.. At enrollment, the study included 46 eyes of 23 patients (9 men, 14 women; age range, 20-42 years) with allergic conjunctivitis; results were calculated based on the 21 patients who completed the study. The control group consisted of 70 eyes of 35 healthy subjects (13 men, 22 women; age range, 22-39 years). Before treatment, 64.3% of the eyes of patients with allergic conjunctivitis had a fluorescein staining score of >1 point, whereas after treatment, 14.3% had a score of >1 point (P < 0.001). Patients' mean (+/- SD) corneal sensitivity improved to 55.0 +/- 2.5 mm from the pretreatment value of 42.5 +/- 2.5 mm (P < 0.001). Mean BUT values before and after treatment were 8.1 +/- 3.5 and 14.0 +/- 7.0 seconds, respectively (P < 0.001). Before treatment, patients' mean squamous metaplasia grade was 2.5 +/- 0.5; at the end of treatment, it had decreased to 1.0 +/- 0.5 (P < 0.001). The mean pretreatment goblet cell density of 545 +/- 85 cells/mm2 improved to 1,090 +/- 100 cells/mm2 after treatment (P < 0.001).. In the patient population studied, the disorder of tear function, squamous metaplasia, and loss of ocular surface goblet cells associated with allergic conjunctivitis improved with topical olopatadine treatment.

Topics: Adult; Anti-Allergic Agents; Case-Control Studies; Conjunctivitis, Allergic; Cornea; Dibenzoxepins; Female; Humans; Male; Olopatadine Hydrochloride; Tears; Treatment Outcome

Topics: Androstadienes; Anti-Inflammatory Agents; Anti-Inflammatory Agents, Non-Steroidal; Conjunctivitis, Allergic; Dibenzoxepins; Humans; Loteprednol Etabonate; Olopatadine Hydrochloride; Ophthalmic Solutions

Olopatadine is a clinically effective dual-action (antihistamine/mast cell stabilizer) ophthalmic antiallergic agent. We have previously demonstrated that olopatadine inhibits tumor necrosis factor alpha (TNF-alpha) release from purified human conjunctival mast cells and that supernates from stimulated mast cells upregulate intercellular adhesion molecule 1 (ICAM-1) expression on epithelial cells via TNF-alpha.. To investigate the effect of olopatadine on the TNF-alpha-mediated mast cell upregulation of ICAM-1 expression on conjunctival epithelial cells.. Human conjunctival mast cells and epithelial cells were purified (>95%) from cadaveric tissue. Conjunctival mast cells were preincubated with three doses (30, 300, or 3,000 microM) of olopatadine or buffer alone for 30 minutes followed by 90-minute challenge with anti-immunoglobulin E (10 microg/mL). The resulting supernates were incubated with conjunctival epithelial cell monolayers for 24 hours along with the following treatments: rTNF-alpha, mast cell supernate + anti-TNF-alpha, recombinant (r)TNF-alpha + anti-TNF-alpha, the three doses of olopatadine, olopatadine supernates, olopatadine supernates + rTNF-alpha. ICAM-1 expression was measured using flow cytometry.. Anti-IgE-stimulated human conjunctival mast cell supernates upregulated human conjunctival epithelial cell ICAM-1 expression to the same extent as rTNF-alpha. ICAM-1 upregulation could be completely blocked with anti-TNF-alpha. Preincubation of conjunctival mast cells with olopatadine significantly blocked the ability of supernates to upregulate ICAM-1 on conjunctival epithelial cells. ICAM-1 expression could be restored by adding rTNF-alpha to the olopatadine-preincubated mast cell supernates.. Olopatadine is able to significantly decrease the anti-immunoglobulin E mast cell supernate-mediated upregulation of ICAM-1 on human conjunctival epithelial cells in vitro. This seems to be mediated through an effect on a TNF-alpha-specific mechanism.

Topics: Anti-Allergic Agents; Antibodies, Anti-Idiotypic; Cells, Cultured; Conjunctiva; Conjunctivitis, Allergic; Culture Media, Conditioned; Dibenzoxepins; Dose-Response Relationship, Drug; Drug Antagonism; Epithelial Cells; Histamine H1 Antagonists; Humans; Intercellular Adhesion Molecule-1; Mast Cells; Olopatadine Hydrochloride; Tumor Necrosis Factor-alpha; Up-Regulation

To compare the clinical efficacy and tolerance of 0.1% olopatadine hydrochloride (OHC) versus 0.05% ketotifen fumarate (KF) in the management of allergic conjunctivitis.. Eighty adult patients with a history of allergy (allergic conjunctivitis, hay fever, asthmatic bronchitis and dermatitis) that were showing allergic conjunctivitis signs and symptoms (itching, hyperemia, mucous discharge and tearing) at the time of inclusion in this study were evaluated. Patients were divided in two groups, A and B. Group A patients were treated with OHC and group B patients were treated with KF. Both groups received one drop in the affected eye every 12 hrs. The start time of this study was the first patient visit, in which the medication was instilled for the first time. Both groups of patients were evaluated 30 min, 48 hr., 7 days and 14 days later. Local tolerance of each medication was evaluated.. Clinical improvement of the signs and symptoms of allergic conjunctivitis occurred in 42.5% to 62.5% of the patients in Group A when assessed 30 min following the first topical ocular dose of olopatadine. However, mucous discharge was not affected. Forty-eight (48) hrs. after the first instillation, improvements in 57.5% to 75% of the patients were shown in every evaluated parameter. After 7 days of treatment, positive clinical results were observed in 80% to 87.5% of the treated patients. Except for the patients that were dismissed from the study before the seventh day of treatment due to the absence of therapeutic response (4/40), all patients satisfactorily completed the therapeutic plan by the seventh day. No intolerance reactions were observed in patients of this group. In Group B patients (KF), clinical improvement of the signs and symptoms measured in the study was shown in 20.0% to 47.5% 30 min after instillation. As observed with olopatadine, no improvement in the number of patients showing mucous discharge was noted at the 30-min time point. At 48 hr. after the first instillation, 27.5% to 48% of patients showed improvement in every evaluated parameter. After 7 days of treatment, improvement was observed in 60% to 75% of patients. On Day 14, positive responses were observed in 67.5% to 75% of patients. Seventeen and one-half percent of the patients were dismissed from the study before the seventh day of treatment due to the absence of a therapeutic response. Approximately 23% of the patients had mild reactions of intolerance (stinging) which was not a cause to discontinue the treatment.. Olopatadine hydrochloride controlled allergic conjunctivitis symptoms and signs more rapidly and to a greater extent than ketotifen fumarate. Fewer cases of treatment failure were noted with OHC, and no local intolerance reactions were observed, while KF triggered mild reactions (stinging) in 23% of patients.

Topics: Adult; Aged; Conjunctivitis, Allergic; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Ketotifen; Male; Middle Aged; Olopatadine Hydrochloride; Ophthalmic Solutions; Safety; Seasons; Treatment Outcome

To evaluate skin tests with clinical ocular allergy and to compare cutaneous hypersensitivity and seasonal allergic conjunctivitis in children.. A 10-year-old girl presented a typical seasonal allergic conjunctivitis, never treated and the onset occurred one year before. She was skin tested for the allergy. Complete blood tests were also performed. An ocular treatment was given: olopatadine over 45 days.. She showed a complete cutaneous anergy including histamine and codeine controls. Radioallergosorbent tests (RAST) found numerous great positivity to different allergens. Within 30 days under ocular treatment, she recovered completely from symptoms and clinical signs.. Clinical typical seasonal ocular allergy in children with cutaneous anergy should be explored further or at least treated. Cutaneous hypersensitivity should be evaluated more precisely with a larger study comparing results in general allergy and in ocular allergy where the anergy seems to be more frequent.

Topics: Child; Conjunctivitis, Allergic; Dermatitis, Allergic Contact; Dibenzoxepins; Female; Histamine H1 Antagonists; Humans; Immune Tolerance; Olopatadine Hydrochloride; Ophthalmic Solutions; Radioallergosorbent Test; Skin Tests

Topics: Adult; Child; Child, Preschool; Conjunctivitis, Allergic; Dibenzoxepins; Histamine H1 Antagonists; Humans; Olopatadine Hydrochloride; Ophthalmic Solutions; Pruritus

Olopatadine (AL-4943A; KW-4679) [(z)-11-[3-(dimethylamino)propylidene]-6, 11-dihydrodibenz[b,e]oxepine-2 acetic acid hydrochloride] is an anti-allergic agent which inhibits mast cell mediator release and possesses histamine H1 receptor antagonist activity. Studies were conducted to characterize the in vitro and in vivo pharmacological profile of this drug relevant to its topical ocular use. AL-4943A inhibits histamine release in a concentration-dependent fashion (IC50 = 559 microM) from human conjunctival mast cell preparations in vitro. Histamine release was not stimulated by AL-4943A at concentrations as high as 10 mM. In contrast, ketotifen stimulated histamine release at concentrations slightly higher than effective inhibitory concentrations. AL-4943A did not display any in vitro cyclooxygenase or 5-lipoxygenase inhibition. Topical ocular application of AL-4943A effectively inhibits antigen- and histamine-stimulated conjunctivitis in guinea pigs. Passive anaphylaxis in guinea pig conjunctiva was attenuated by AL-4943A applied 30 min prior to intravenous or topical ocular antigen challenge (ED50 values 0.0067% and 0.0170%, w/v, respectively). Antihistaminic activity in vivo was demonstrated using a model of histamine-induced vascular permeability in guinea pig conjunctiva. AL-4943A applied topically from 5 min to 24 hrs prior to histamine challenge effectively and concentration-dependently inhibited the vascular permeability response, indicating the compound has an acceptable onset and a long duration of action. Drug concentrations 5-fold greater than those effective against histamine-stimulated conjunctival responses failed to inhibit vascular permeability responses induced with either serotonin or Platelet-Activating-Factor. These data indicate that the anti-histaminic effect observed with AL-4943A is specific. These anti-allergic/antihistaminic activities of AL-4943A observed in preclinical model systems have been confirmed in clinical trials in allergic patients.

Topics: Administration, Topical; Anaphylaxis; Animals; Anti-Allergic Agents; Capillary Permeability; Conjunctiva; Conjunctivitis, Allergic; Dibenzoxepins; Dose-Response Relationship, Drug; Guinea Pigs; Histamine; Histamine H1 Antagonists; Histamine Release; Humans; Ketotifen; Male; Mast Cells; Olopatadine Hydrochloride; Ophthalmic Solutions; Rats; Rats, Sprague-Dawley

AL-4943A (Olopatadine) is a new antihistaminic and anti-allergic drug. It was tested for its ability to compete for [3H]pyrilamine, [3H]tiotidine and [3H]N-methyl histamine binding to H1, H2 and H3 histamine receptors, respectively. AL-4943A exhibited the highest affinity (Ki = 41.1 +/- 6.0 nM) for H1-receptors and a significantly lower affinity for H2- (Ki = 43,437 +/- 6,257 nM) and H3-receptors (Ki = 171,666 +/- 6,774 nM), respectively. These data showed AL-4943A to be an H1-selective compound, being 1,059- and 4,177-times more selective for H1- than H2- and H3-receptors. AL-4943A was more H1-selective than levocabastine, ketotifen, antazoline and pheniramine and, also, exhibited a low affinity for 38 nonhistamine receptor binding sites. AL-4943A antagonized histamine-induced phosphoinositide (PI) turnover in cultured human conjunctival epithelial cells (IC50 = 9.5 +/- 1.5 nM, n = 3), human corneal fibroblasts (IC50 = 19 nM) and transformed human trabecular meshwork cells (IC50 = 39.9 nM). These data have shown AL-4943A to be a high affinity, high potency H1-selective histamine antagonist. This information, coupled with a long duration of action in an in vivo model of allergic conjunctivitis, suggests that AL-4943A may be a useful drug to treat various ocular allergic diseases, including allergic conjunctivitis.

Topics: Anti-Allergic Agents; Binding, Competitive; Cell Line; Cells, Cultured; Conjunctiva; Conjunctivitis, Allergic; Cornea; Dibenzoxepins; Epithelium; Fibroblasts; Histamine; Histamine H1 Antagonists; Humans; Hydrolysis; Ligands; Olopatadine Hydrochloride; Phosphatidylinositols; Receptors, Histamine; Trabecular Meshwork

The effect of KW-4679 (Z)-11-[3-(dimethylamino) propylidene]-6,11-dihydrodibenz [b,e] oxepin-2-acetic acid hydrochloride, CAS 140462-76-6; proposed INN: olopatadine) on experimental conjunctivitis and rhinitis was studied in comparison with that of ketotifen (CAS 34580-14-8) using guinea pigs and rats, respectively. KW-4679 was effective in inhibiting the antigen- and histamine-induced conjunctivitis by both oral and topical administrations. These effects of KW-4679 were somewhat more potent than those of ketotifen. KW-4679 as well as ketotifen was more effective in inhibiting the histamine-induced conjunctivitis than that seen in antigen-induced conjunctivitis when they were given topically. KW-4679 inhibited the increased dye leakage into the nasal cavity induced not only by antigen in actively sensitized rats but also by histamine perfusion in non-sensitized rats by oral and topical administrations. Similar to ketotifen, the effect of KW-4679 on histamine-induced increase in dye leakage was almost same as that induced by antigen. The potency of KW-4679 was higher than that of ketotifen in the increased dye leakage induced by both antigen and histamine perfusion.

Topics: Administration, Oral; Administration, Topical; Allergens; Animals; Anti-Allergic Agents; Ascaris; Conjunctivitis, Allergic; Dibenzoxepins; Guinea Pigs; Histamine; Male; Olopatadine Hydrochloride; Rats; Rats, Wistar; Rhinitis, Allergic, Seasonal