A multicenter, double-blind, randomized, noninferiority comparison of 14 days' treatment with oral olopatadine 10 mg or cetirizine 10 mg in Chinese adults with cutaneous pruritus.

OBJECTIVES: To assess whether olopatadine hydrochloride (OH) was noninferior to cetirizine in the treatment of cutaneous pruritus (CP). PATIENTS AND METHODS: Patients with CP presenting at seven centers in China were randomly allocated to double-blind treatment with 5 mg of OH orally twice a day or cetirizine 10 mg orally once a day for 2 weeks. Patients were followed up on days 7 and 14. Noninferiority was predefined as a 20% maximum difference in the reduction of symptom score reducing indices (SSRI). Both intention-to-treat (ITT) and per-protocol populations were analyzed. RESULTS: 174 patients (86 receiving OH and 88 cetirizine) were included in the ITT population. In the ITT population, the mean reduction in SSRI was 0.640 ± 0.274 in the OH group and 0.603 ± 0.289 in the cetirizine group. The one-sided 97.5% CI (-0.047) met the criteria for noninferiority. Noninferiority was also demonstrated for SSRI in the per-protocol population, with reductions of 0.640 ± 0.271 with OH and 0.596 ± 0.287 with cetirizine (97.5% CI -0.043).The total effectiveness rate (TER) was similar in the OH (90.0%) and cetirizine (80.0%) groups. The corresponding one-sided 97.5% CI (-1.0%) also demonstrated noninferiority. The incidence of adverse events was 47.1% in the OH group and 41.4% in the cetirizine group (p = 0.453). CONCLUSION: The efficacy of OH was noninferior to that of cetirizine in controlling itching indicating that it can be considered as a clinically relevant alternative therapy to cetirizine for the management of CP in adult Chinese patients.

The antagonism of histamine H1 and H4 receptors ameliorates chronic allergic dermatitis via anti-pruritic and anti-inflammatory effects in NC/Nga mice.

BACKGROUND: Although histamine H1 receptor (H1R) antagonists are commonly used to treat atopic dermatitis, the treatment is not always effective. The histamine H4 receptor (H4R) was recently described as important to the pruritus in dermatitis. Here, we investigated whether the combination of a H1R antagonist plus a H4R antagonist attenuates chronic dermatitis in NC/Nga mice. METHODS: Chronic dermatitis was developed by repeated challenges with picryl chloride on the dorsal back and ear lobes. The therapeutic effects of the H1R antagonist olopatadine and H4R antagonist JNJ7777120 on scratching and the severity of dermatitis were evaluated. In addition, the mechanisms responsible for the anti-allergic effects of H1R and/or H4R antagonism were examined using bone marrow-derived mast cells (BMMC) and keratinocytes. RESULTS: JNJ7777120 attenuated scratching behavior after a single administration and improved dermatitis, as assessed with clinical scores, pathology, and cytokine levels in skin lesions when administered repeatedly. These effects were augmented by combined treatment with olopatadine, having a similar therapeutic efficacy to prednisolone. JNJ7777120 inhibited dose-dependently the production of thymus and activation-regulated chemokine/CCL17 and macrophage-derived chemokine/CCL22 from antigen-stimulated BMMC. In addition, olopatadine reversed the histamine-induced reduction of semaphorin 3A mRNA in keratinocytes. CONCLUSION: Combined treatment with H1R and H4R antagonists may have a significant therapeutic effect on chronic dermatitis through the synergistic inhibition of pruritus and skin inflammation.

[A 10-week safety and efficacy evaluation of olopatadine, 0.2% instilled twice-daily in patients with allergic conjunctivitis in Japan].

PURPOSE: 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. SUBJECTS AND METHODS: This was a single-insititution, open-label, single-group study of symptomatic patients > or = 12 years of age with allergic conjunctivitis. RESULTS: 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. CONCLUSIONS: 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.

[A multicenter, double-masked, randomized evaluation of olopatadine 0.2% using the conjunctival allergen challenge model in Japanese patients with allergic conjunctivitis].

PURPOSE: 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. METHODS: 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. RESULTS: 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. CONCLUSIONS: 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.

Olopatadine hydrochloride inhibits capsaicin-induced flare response in humans.

Capsaicin, a vanilloid, has the potential for releasing substance P (SP) from sensory nerves. Topical application of capsaicin induces a flare response in the skin. However, it has not been clarified whether the release of SP is involved in the process of flare response or not. A potent antihistamine drug, olopatadine hydrochloride, is known to have inhibitory action against the release of SP. We examined the effects of olopatadine (at a dose of 5 mg) on skin reaction induced by topical application of capsaicin in 10 healthy subjects. The scores of capsaicin-induced flare responses after olopatadine administration were significantly lower at 30 min than at baseline. Our findings suggest that olopatadine hydrochloride could inhibit capsaicin-induced flare responses.

Comprehensive report of olopatadine 0.6% nasal spray as treatment for children with seasonal allergic rhinitis.

Allergic rhinitis (AR) is highly prevalent in children. Olopatadine, 0.6% nasal spray (olopatadine) is approved for the relief of seasonal allergic rhinitis (SAR) symptoms in children 6 years of age and older. The objective of this study is to provide a comprehensive report of all clinical studies conducted with olopatadine in children with SAR. A pooled analysis was conducted of 2 randomized, double-blind, 2-week, IRB-approved studies that compared olopatadine with placebo (1 spray/nostril twice-daily) in patients 6-11 years of age with SAR. Assessments included the reflective total nasal symptom score (rTNSS) and total ocular symptom score (rTOSS), the Pediatric Rhinoconjunctivitis Quality-of-Life Questionnaire (PRQLQ), and the Caregiver Treatment Satisfaction Questionnaire for Allergic Rhinitis (CGTSQ-AR). Safety results were reported for these studies in combination with a pediatric pharmacokinetic study. Olopatadine was superior to placebo for mean decrease in rTNSS (p = 0.0012) and rTOSS (p = 0.0094), mean decrease in overall PRQLQ score (p = 0.0003), and mean summary CGTSQ AR score (p = 0.0013); (n = 944). The most frequently reported treatment-related events in the olopatadine group were epistaxis and dysgeusia (bad taste) (n = 1,046). For SAR treatment in patients 6-11 years of age, olopatadine was superior to placebo in reducing the symptoms of SAR, improving quality of life, and satisfying caregivers. Olopatadine is a safe and effective treatment for SAR patients as young as 6 years of age and it has been demonstrated to reduce disease impact on the lives of these children and their families.

Synergetic effects of prednisolone and olopatadine on atopic dermatitis model of hairless mice.

We investigated the synergetic effects of glucocorticoid and histamine H1 receptor antagonists on an atopic dermatitis model. Hairless mice were used in this study and an atopic dermatitis model was made by repeated application of 2,4,6-trinitrochlorobenzene. The effects of glucocorticoid, histamine H1 receptor antagonists, and the simultaneous use of these drugs were investigated by measuring scratching behavior, skin symptoms and nerve growth factor (NGF) in the skin. Topical application of prednisolone significantly inhibited scratching behavior, skin symptoms and NGF contents in the skin by repeated application. Olopatadine also showed a significant effect on scratching behavior and NGF contents in the skin, whereas chlorpheniramine showed no significant inhibitory effect on these indices. Furthermore, the combined use of prednisolone and olopatadine potentiated the inhibition of scratching behavior, skin symptoms, and NGF in the skin. From these findings, olopatadine potentiated the inhibitory effect of prednisolone on the symptoms of atopic dermatitis by inhibiting NGF.

Evaluation of olopatadine hydrochloride nasal spray, 0.6%, used in combination with an intranasal corticosteroid in seasonal allergic rhinitis.

The combination of intranasal antihistamines and intranasal corticosteroids results in superior relief of seasonal allergic rhinitis (SAR) symptoms compared with monotherapy. This study was designed to evaluate the safety and efficacy of olopatadine hydrochloride nasal spray, 0.6% (OLO), administered in combination with fluticasone nasal spray, 50 micrograms (FNS), relative to azelastine nasal spray, 0.1% (AZE), administered in combination with FNS in the treatment of SAR. This was a multicenter, double-blind, randomized, parallel-group comparison of OLO + FNS versus AZE + FNS administered for 14 days to patients > or =12 years of age with histories of SAR. Efficacy assessments recorded by patients in a daily diary included nasal symptom scores. Safety was evaluated based on adverse events (AEs). Pretreatment values for reflective total nasal symptoms scores (rTNSS) were similar for both treatment groups. The mean (SD) 2-week average rTNSS was 4.28 (2.63) for OLO + FNS and 4.15 (2.63) for AZE + FNS; these scores were not statistically different between treatment groups. No significant differences (p > 0.05) between OLO + FNS and AZE + FNS were observed for the average 2-week percent changes from baseline in rTNSS or in the individual nasal symptoms (nasal congestion, rhinorrhea, itchy nose, and sneezing). Compared with baseline, both groups had statistically significant improvement in rTNSS (p < 0.05). No serious AEs were reported in either group during the study period. Overall, 19 AEs were reported in the OLO + FNS group and 29 AEs were reported in the AZE + FNS group. OLO, when administered adjunctively with FNS, is effective, safe, and well-tolerated in patients with SAR.

Efficacy of oral olopatadine hydrochloride for the treatment of seasonal allergic rhinitis: A randomized, double-blind, placebo-controlled study.

Adequate treatment is critical for maintaining a good level of quality of life (QOL) during the pollen season in patients suffering from seasonal allergic rhinitis (SAR). Olopatadine, a histamine H(1)-receptor antagonist, has been approved in the United States and Europe for the treatment of AR and allergic conjunctivitis as a nasal spray and an ophthalmic solution, respectively. We conducted a randomized, double-blind, placebo-controlled study to determine whether orally administered olopatadine for prophylactic purposes might also be effective for the control of nasal allergy symptoms, especially nasal congestion, in patients with SAR due to Japanese cedar pollen (SAR-JP). A total of 110 patients with SAR caused by JP were randomized to the treatment. The subjects recorded their nasal and ocular allergic symptom scores in a diary, and their QOL was assessed by the Japanese version of the Rhinoconjunctivity Quality of Life Questionnaire. Treatment with oral olopatadine significantly suppressed sneezing (p < 0.001), rhinorrhea (p < 0.001), and nasal congestion (p < 0.05). The total QOL score during the peak JP season was superior in the olopatadine group than in the placebo group (p < 0.05). However, orally administered olopatadine did not exert any significant effect against eye itching and watering of the eyes, unlike olopatadine nasal spray. Treatment with olopatadine tablets yielded superior QOL scores in the domains of usual daily activities and outdoor activities when compared with placebo. No serious adverse effects of the treatment were reported during the study period. These results suggest that oral olopatadine treatment may be a useful alternative treatment strategy for AR.

Comparison of olopatadine and fluorometholone in contact lens-induced papillary conjunctivitis.

PURPOSE: The purpose of this study was to compare the efficacy of olopatadine with fluorometholone in contact lens-induced mild to moderate papillary conjunctivitis. METHODS: 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. RESULTS: 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). CONCLUSIONS: 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.

Effects of olopatadine hydrochloride nasal spray 0.6% in the treatment of seasonal allergic rhinitis: a phase III, multicenter, randomized, double-blind, active- and placebo-controlled study in adolescents and adults.

BACKGROUND: Seasonal allergic rhinitis (SAR) is an allergen-induced inflammatory reaction that occurs during periods of high pollen count. Current treatments for SAR include allergen avoidance, systemic antihistamines, and steroidal and nonsteroidal intranasal sprays. Olopatadine is a selective antihistamine and an inhibitor of proinflammatory mediators from human mast cells. An intranasal formulation of olopatadine has been developed for the treatment of SAR. OBJECTIVE: The aim of this study was to compare the efficacy and tolerability of olopatadine hydrochloride nasal spray 0.6% (OLO) relative to azelastine hydrochloride nasal spray 0.1% (AZE) and an inactive vehicle in the treatment of SAR. METHODS: This Phase III, multicenter, randomized, double-blind, active- and placebo-controlled, parallel-group study was conducted at 21 centers across the United States. Eligible patients were aged > or =12 years and had a history of SAR and verified allergy to a prevalent local allergen. After a run-in period during which inactive vehicle was administered, patients were randomly assigned to OLO, AZE (active control), or inactive vehicle (identical to OLO; placebo control), 2 sprays in each nostril BID for 16 days. The timing of enrollment was correlated with the start of the allergy season at each site. Symptoms were recorded twice daily in an electronic diary. Efficacy assessments included changes in mean daily reflective total nasal symptom scores (TNSS). Tolerability was evaluated based on adverse events (AEs) and nasal, physical, and cardiovascular parameters. RESULTS: A total of 544 patients were randomized. The mean age was 36 years (range, 12-77 years); men and boys represented 32.2% of the population; and the patients were predominantly white (75.4%). The mean reductions from baseline in reflective TNSS were 26.8%, 29.9%, and 18.4% with OLO, AZE, and inactive vehicle, respectively (P = 0.003 OLO vs inactive vehicle; 95% CI, -2.5% to 8.7% OLO vs AZE [non-inferiority]). The most commonly reported treatment-related AE in the OLO and AZE groups was bitter taste (12.2% [22/180] and 19.7% [37/188], respectively). The prevalence and intensity of bitter taste were significantly lower with OLO than with AZE (P = 0.05 and P = 0.005, respectively). In the group that received inactive vehicle, the prevalence of bitter taste was 1.7% (3/176). The prevalences of other treatment-related AEs, including epistaxis and nasal discomfort, were < or =3.7% in each group and did not differ significantly between groups. CONCLUSIONS: In this small study in patients aged > or =12 years with SAR, the percentage reduction from baseline in TNSS was significantly greater with OLO (2 sprays in each nostril BID) compared with vehicle and not significantly different from that with AZE. OLO and AZE were similarly well tolerated, with the exception of prevalence and intensity of bitter taste, which were significantly lower with OLO.

Evaluation of the efficacy and safety of olopatadine and fexofenadine compared with placebo in Japanese cedar pollinosis using an environmental exposure unit.

BACKGROUND: Second-generation oral H1-antihistamines have become a mainstay of treatment for the symptoms of seasonal allergic rhinitis; however, the effect of olopatadine has not been widely reported to date. OBJECTIVES: To evaluate the efficacy of 2 oral H1-antihistamines, olopatadine and fexofenadine, in the treatment of the nasal symptoms of Japanese cedar pollinosis and their possible side effects. METHODS: This was a randomized, double-blind, placebo-controlled, crossover study conducted in an environmental exposure unit (EEU). Twenty volunteers suffering from Japanese cedar pollinosis were randomly divided into 3 groups and exposed to cedar pollen in the EEU with oral administration of olopatadine hydrochloride (5 mg), fexofenadine hydrochloride (60 mg), or placebo 1 hour prior to pollen exposure. Nasal symptoms, activity impairment, and subjective sleepiness were self-assessed during the study period. Attention was measured using the digit cancellation test. The trial was repeated after 4 and 7 weeks. RESULTS: Compared with placebo, olopatadine significantly improved nasal symptoms and activity impairment during pollen exposure (P < .05). There was no significant relief of nasal discharge or nasal congestion with fexofenadine throughout the 5-hour exposure to cedar pollen. Furthermore, olopatadine significantly reduced nasal congestion during the first 2 hours, as well as sneezing and nasal discharge 4 hours after admission to the EEU compared with fexofenadine (P < .05). There was no significant difference in the effect on subjective sleepiness among the 3 groups, and all 3 agents had little effect on attention. CONCLUSIONS: These findings suggest that olopatadine is more effective than placebo and fexofenadine in improving nasal symptoms of Japanese cedar pollinosis.

Safety and efficacy of olopatadine hydrochloride nasal spray 0.6% in pediatric subjects with allergic rhinitis.

Olopatadine (OLO) nasal spray 0.6% is indicated for treatment of seasonal allergic rhinitis (SAR) in subjects > or = 12 years of age. This study was designed to present the results of two studies that evaluated the efficacy, safety, and pharmacokinetics (PK) of OLO in children with allergic rhinitis (AR). These were multicenter, double-blind, randomized, parallel-group studies in subjects 6 to <12 years of age (study 1) and 2 to <6 years of age (study 2) with SAR (study 1) or AR (study 2). In study 1, nasal and ocular symptoms were scored for efficacy, and study 2 included PK analyses. In both studies, subjects were evaluated based on physical/nasal examinations and adverse events (AEs). Overall, 1188 subjects (study 1) and 132 subjects (study 2) were randomized, respectively. OLO (1 or 2 sprays/nostril, b.i.d.) was superior to vehicle in the percent decrease in reflective total nasal symptom scores (p < or = 0.0120). OLO 1 spray/nostril b.i.d. was also superior to vehicle in the percent decreases in reflective total ocular symptom scores (p < or = 0.0084), change from baseline in Pediatric Rhinoconjunctivitis Quality-of-Life Questionnaire scores (p < or = 0.0377), Caregiver Treatment Satisfaction Questionnaire scores (p < or = 0.0450), and proportions of subjects reporting improvements in Subject Global Assessments (p = 0.0035). The most frequently reported treatment-related events in the OLO group were bad/bitter taste and epistaxis. In subjects 6 to <12 years of age, OLO was superior to vehicle in the treatment of SAR. In subjects 2 to <12 years of age, OLO had an overall low rate of AEs and low systemic exposure.

[Effectiveness of olopatadine therapy in seasonal allergic conjunctivitis]. / Eficienta tratamentului cu olopatadina in conjunctivitele alergice sezoniere.

PURPOSE: The study shows the antihistaminic and anti-inflammatory efficient treatment with olopatadina 0.1%. METHOD: 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. RESULTS: 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%. CONCLUSIONS: 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.

Efficacy of once-daily olopatadine 0.2% ophthalmic solution compared to twice-daily olopatadine 0.1% ophthalmic solution for the treatment of ocular itching induced by conjunctival allergen challenge.

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.

An assessment of the onset and duration of action of olopatadine nasal spray.

OBJECTIVE: Seasonal allergic rhinitis (SAR) is a highly prevalent disease. This study was conducted to evaluate the onset and duration of action of three concentrations of olopatadine nasal spray. METHODS: This was a randomized, double-blind, single-dose, placebo-controlled study, conducted in an environmental exposure chamber in patients with SAR. A total of 320 patients were exposed to ragweed allergen in the chamber and randomized to olopatadine nasal spray 0.2%, 0.4%, 0.6%, or placebo nasal spray. Symptoms (sneezing, runny, itchy, and stuffy nose) were self-assessed during a 12-hour study period. RESULTS: All concentrations of olopatadine nasal spray provided clinically meaningful reductions in total nasal symptom scores at 30 minutes compared to the placebo. Olopatadine nasal spray 0.6% was significantly more effective (P < 0.05) than placebo nasal spray at all time-points starting at 90 minutes post-dose and continuing over 12 hours. CONCLUSIONS: Olopatadine nasal spray 0.6% demonstrated a fast onset of action and maintained an effect for at least 12 hours after dosing.

Duration of action of topical antiallergy drugs in a Guinea pig model of histamine-induced conjunctival vascular permeability.

The topical application of 0.1% olopatadine has been shown to provide significant attenuation of histamine-induced conjunctival vascular permeability (CVP) within 5 min and for as long as 24 h following a topical administration. The duration of the action of olopatadine was compared to that of epinastine, azelastine, and ketotifen. Male Hartley outbred guinea pigs (weighing 250-300 g) were administered a drug or vehicle as single O.D. topical drops, at times ranging from 4 to 24 h prior to histamine challenge. One (1) h prior to histamine challenge, the animals were administered 1 mL of Evans blue dye (1 mg/mL) through the marginal ear vein. Histamine (300 ng) was administered by a subconjunctival injection, and the guinea pigs were sacrificed 30 min later. CVP was assessed as the area and color intensity stained with Evans blue dye. The potencies of each drug were determined by calculating a 50% effective dose (ED(50)) for the inhibition of vascular leakage, compared to vehicle treatment, at each time point. Olopatadine was the only compound tested that was significantly effective 16 h following a single topical application. The ED(50) for olopatadine at 16 h was 0.031%. Epinastine, azelastine, and ketotifen were only significantly effective for up to 4 h. Olopatadine exhibited the longest duration of action for inhibition of histamine-induced vascular permeability in guinea pigs of any topical antiallergic drug tested. Concentrations of olopatadine, which provided a greater than 50% inhibition of the histamine-induced vascular response, were consistently less than 0.1% over a 16-h pretreatment interval.

[First Hungarian report of olopatadine eyedrop therapy in children and adults suffering from seasonal allergic conjunctivitis]. / Elso magyarországi beszámoló olopatadin hatóanyagú szemcseppel allergiás gyermek es felnott betegeken szerzett tapasztalatokról.

UNLABELLED: The eye drop Opatanol (its main component is olopatadine, which has an antihistaminic and membrane-stabilizing effect) in Hungary is not well known yet. PATIENTS AND METHODS: 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. RESULTS: 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). CONCLUSIONS: 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.