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Romanian Journal of Ophthalmology 2019We evaluated the histamine's role in regulating the iris vasomotricity in rats, using as a research tool topical olopatadine, a selective H1 blocker, which is indicated...
We evaluated the histamine's role in regulating the iris vasomotricity in rats, using as a research tool topical olopatadine, a selective H1 blocker, which is indicated for the treatment of allergic conjunctivitis and ranitidine, a selective H2 blocker mainly used for the treatment of peptic ulcer disease. Two groups of six Wistar rats anesthetized with ketamine 200 mg/kg body weight were used. They received distilled water in conjunctival instillations, initially and after 5 minutes, olopatadine 2.5 mmol/ l for the first group, respectively ranitidine 2.5 mmol/ l for the second group. The changes of the iris arteriolar and venular diameters were recorded. Both olopatadine and ranitidine produced statistically significant iridal arteriolar vasoconstriction and ranitidine determined statistically significant venuloconstriction, while distilled water did not produce any statistically significant effect. There is a vasodilator histaminergic tone exerted through the histaminergic H1 and H2 receptors in the iris arterioles and, respectively, through the H2 receptors in the iridal venules. Olopatadine, a topical H1 antagonist used in the treatment of ocular allergies, may interfere with the humoral regulation of the iris arteriolar tone. Ranitidine, an H2 antagonist, decreased the diameter of the iris arterioles and venules, when administered topically in rats.
Topics: Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Conjunctiva; Conjunctivitis, Allergic; Disease Models, Animal; Drug Therapy, Combination; Histamine H2 Antagonists; Male; Olopatadine Hydrochloride; Ranitidine; Rats; Rats, Wistar; Triterpenes; Vasoconstriction
PubMed: 31198894
DOI: No ID Found -
Pain Nov 2016Itch is a major indicator of psoriasis, but the underlying mechanisms behind this symptom are largely unknown. To investigate the neuronal mechanisms of psoriatic itch,...
Itch is a major indicator of psoriasis, but the underlying mechanisms behind this symptom are largely unknown. To investigate the neuronal mechanisms of psoriatic itch, we tested whether mice subjected to the imiquimod-induced psoriasis model exhibit itch-associated behaviors. Mice received daily topical applications of imiquimod to the rostral back skin for 7 days. Imiquimod-treated mice exhibited a significant increase in spontaneous scratching behavior directed to the treated area as well as touch-evoked scratching (alloknesis). To characterize this model, we measured the mRNA expression levels of pruritogens and itch-relevant receptors/channels using real-time reverse transcription PCR. The mRNA expression of MrgprA3, MrgprC11, and MrgprD decreased gradually over time in the dorsal root ganglion (DRG) cells. There was no significant change in the mRNA expression of TRPV1 or TRPA1 in DRG cells. TRPV4 mRNA expression was transiently increased in the DRG cells, whereas TRPM8 mRNA was significantly decreased. The mRNA expression levels of histidine decarboxylase and tryptophan hydroxylase 1, as well as the intensity of histamine and serotonin immunoreactivity, were transiently increased in the skin on day 2, returning to baseline by day 7. Histamine H1-receptor antagonists, chlorpheniramine and olopatadine, significantly inhibited spontaneous scratching on day 2, but not day 7. Neither chlorpheniramine nor olopatadine affected alloknesis on day 2 or day 7. These results may reflect the limited antipruritic effects of histamine H1-receptor antagonists on human psoriasis. The imiquimod-induced psoriasis model seems to be useful for the investigation of itch and its sensitization in psoriasis.
Topics: Adjuvants, Immunologic; Aminoquinolines; Animals; Anti-Inflammatory Agents, Non-Steroidal; Antipruritics; Chlorpheniramine; Disease Models, Animal; Ganglia, Spinal; Gene Expression Regulation; Histidine Decarboxylase; Imiquimod; Male; Mice; Mice, Inbred C57BL; Olopatadine Hydrochloride; Pain Measurement; Pruritus; Random Allocation; Skin; TRPV Cation Channels; Tryptophan Hydroxylase
PubMed: 27437787
DOI: 10.1097/j.pain.0000000000000674 -
Annals of Allergy, Asthma & Immunology... Feb 2019GSP301 nasal spray is a fixed-dose combination of the antihistamine olopatadine hydrochloride and the corticosteroid mometasone furoate intended for seasonal allergic... (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
GSP301 nasal spray is a fixed-dose combination of the antihistamine olopatadine hydrochloride and the corticosteroid mometasone furoate intended for seasonal allergic rhinitis (SAR) treatment.
OBJECTIVE
To evaluate the efficacy and safety of once-daily or twice-daily GSP301 in a ragweed pollen environmental exposure chamber.
METHODS
In this randomized, double-blind, double-dummy study, adults (18-65 years old) with SAR were equally randomized to 665 μg of olopatadine and 25 μg of mometasone (twice-daily GSP301), 665 μg of olopatadine and 50 μg of mometasone (once-daily GSP301), a US Food and Drug Administration-approved formulation of 137 μg of azelastine and 50 μg of fluticasone twice-daily (AzeFlu), a US Food and Drug Administration-approved formulation of 665 μg of olopatadine twice-daily, or placebo (twice-daily). During 2 visits (baseline and end of 14-day treatment), participants assessed SAR symptoms at specified time points. The primary end point-mean change from baseline in instantaneous total nasal symptom score (iTNSS) for twice-daily or once-daily GSP301 vs placebo-was analyzed by analysis of covariance. Onset of action, ocular symptoms, and adverse events were assessed.
RESULTS
A total of 180 participants were randomized. Treatment with twice-daily or once-daily GSP301 provided statistically significant improvements in iTNSS vs placebo (twice-daily GSP301: least squares mean difference, -3.60; 95% confidence interval [CI], -4.89 to -2.30; once-daily GSP301: least squares mean difference, -3.05; 95% CI, -4.35 to -1.76; P < .0001 for both). Significant improvements in iTNSS with twice-daily GSP301 occurred by 10 minutes after dosing (-1.26; 95% CI, -2.30 to -0.21; P = .02) and were maintained at all later time points except one (2.5 hours). Treatment-emergent adverse events occurred in 22.2%, 30.6%, 25.0%, 22.2%, and 16.7% of participants in the twice-daily GSP301, once-daily GSP301, AzeFlu, olopatadine, and placebo groups, respectively.
CONCLUSION
In an environmental exposure chamber model, twice-daily and once-daily GSP301 treatments were well tolerated and provided statistically significant and clinically meaningful SAR symptom improvement vs placebo.
TRIAL REGISTRATION
ClinicalTrials.gov Identifier: NCT03444506.
Topics: Adult; Double-Blind Method; Drug Administration Schedule; Drug Combinations; Environmental Exposure; Female; Humans; Male; Middle Aged; Mometasone Furoate; Nasal Sprays; Olopatadine Hydrochloride; Rhinitis, Allergic, Seasonal
PubMed: 30321655
DOI: 10.1016/j.anai.2018.10.011 -
Asia Pacific Allergy Apr 2012Olopatadine hydrochloride ophthalmic solutions are treated for allergic conjunctival diseases that are a selective histamine H1 receptor antagonist and an inhibitor of...
BACKGROUND
Olopatadine hydrochloride ophthalmic solutions are treated for allergic conjunctival diseases that are a selective histamine H1 receptor antagonist and an inhibitor of the release of mediators including histamine from the human mast cells. Substance P (SP) levels are increased in tears of patients with allergic conjunctivitis. However, little is known about the regulation of SP release by anti-allergic ophthalmic solutions.
OBJECTIVE
We investigated that the effect of olopatadine hydrochloride ophthalmic solutions (olopatadine 0.1% and olopatadine 0.2%) on rat conjunctivitis models compared with other anti-allergic ophthalmic solutions.
METHODS
Conjunctivitis was induced by subconjunctival injection of histamine or intravenous injection of ovalbumin in rats passively sensitized with anti-ovalbumin anti-serum. The releases of SP were determined in the conjunctiva and tears using rat antigen-induced conjunctivitis models.
RESULTS
Olopatadine 0.1% and 0.2% significantly inhibited the increased conjunctival dye leaked in the histamine- or antigen-induced hyperpermeability. The inhibitory effects by olopatadine were more potent than by other tested anti-allergic ophthalmic solutions. Moreover, olopatadine significantly inhibited the release of SP from the conjunctiva.
CONCLUSION
These results indicate that olopatadine ophthalmic solutions appear to exert additional SP release inhibition besides dual-action such as selective histamine H1 receptor antagonistic action and mast cell stabilization action.
PubMed: 22701861
DOI: 10.5415/apallergy.2012.2.2.115 -
Experimental and Therapeutic Medicine Feb 2019Therapeutic effects and safety of houttuynia eye drops combined with olopatadine hydrochloride eye drops on vernal keratoconjunctivitis (VK) were evaluated. A total of...
Therapeutic effects and safety of houttuynia eye drops combined with olopatadine hydrochloride eye drops on vernal keratoconjunctivitis (VK) were evaluated. A total of 926 patients with VK were collected in the Eye Hospital of Wenzhou Medical University from July 2011 to January 2017. Patients were divided into group A, B and C according to the use of different eye drops. Group A included 276 patients who were treated with houttuynia eye drops; group B included 305 patients who were treated with olopatadine hydrochloride eye drops; group C included 345 patients who were treated with houttuynia eye drops and olopatadine hydrochloride eye drops. Treatment was performed for 14 days. Eye symptoms before and after treatment, and at 1 h, 7 days and 14 days after drug administration were compared among groups to evaluate the therapeutic effect. At 1 h after drug administration, highest excellent rate was observed in group C, followed by group A, and good outcome rate was significantly higher in group C than in the other two groups (P<0.05), and effective rate was also significantly higher in group C than in the other two groups (P<0.05). At 7 days after treatment, excellent rate was significantly higher in group C than in the other two groups (P<0.05), and effective rate was higher in group C than in group B (P<0.05). At 14 days after treatment, excellent rate was significantly higher in group C than in the other two groups (P<0.05), while lowest good outcome rate and ineffective rate were found in group C, and no significant differences were found between group A and B (P>0.05). Houttuynia ophthalmic solution and olopatadine hydrochloride eye drops can both achieve good effect in the treatment of VK, and combined use of them can increase the efficacy and shorten treatment period. So, the combined treatment should be popularized.
PubMed: 30679995
DOI: 10.3892/etm.2018.7079 -
Archives of Dermatological Research May 2012Since most first-generation antihistamines have undesirable sedative effects on the central nervous systems (CNS), newer (second-generation) antihistamines have been... (Randomized Controlled Trial)
Randomized Controlled Trial
Effects of single therapeutic doses of promethazine, fexofenadine and olopatadine on psychomotor function and histamine-induced wheal- and flare-responses: a randomized double-blind, placebo-controlled study in healthy volunteers.
Since most first-generation antihistamines have undesirable sedative effects on the central nervous systems (CNS), newer (second-generation) antihistamines have been developed to improve patients' quality of life. However, there are few reports that directly compare the antihistaminic efficacy and impairment of psychomotor functions. We designed a double-blind, placebo controlled, crossover study to concurrently compare the clinical effectiveness of promethazine, a first-generation antihistamine, and fexofenadine and olopatadine, second-generation antihistamines, by measuring their potency as peripheral inhibitors of histamine-induced wheal and flare. Further, we investigated their sedative effects on the CNS using a battery of psychomotor tests. When single therapeutic doses of fexofenadine (60 mg), olopatadine (5 mg) and promethazine (25 mg) were given in a double-blind manner to 24 healthy volunteers, all antihistamines produced a significant reduction in the wheal and flare responses induced by histamine. In the comparison among antihistamines, olopatadine showed a rapid inhibitory effect compared with fexofenadine and promethazine, and had a potent effect compared with promethazine. In a battery of psychomotor assessments using critical flicker fusion, choice reaction time, compensatory tracking, rapid visual information processing and a line analogue rating scale as a subjective assessment of sedation, promethazine significantly impaired psychomotor function. Fexofenadine and olopatadine had no significant effect in any of the psychomotor tests. Promethazine, fexofenadine and olopatadine did not affect behavioral activity, as measured by wrist actigraphy. These results suggest that olopatadine at a therapeutic dose has greater antihistaminergic activity than promethazine, and olopatadine and fexofenadine did not cause cognitive or psychomotor impairment.
Topics: Adolescent; Dibenzoxepins; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Olopatadine Hydrochloride; Promethazine; Pruritus; Psychomotor Performance; Rhinitis, Allergic, Seasonal; Terfenadine; Urticaria; Young Adult
PubMed: 22130869
DOI: 10.1007/s00403-011-1192-2 -
Contact Lens & Anterior Eye : the... Apr 2023To compare the ocular comfort at application of topical, over-the-counter, 0.7% olopatadine and 0.035% ketotifen fumarate anti-allergy eye drops.
PURPOSE
To compare the ocular comfort at application of topical, over-the-counter, 0.7% olopatadine and 0.035% ketotifen fumarate anti-allergy eye drops.
METHODS
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.
RESULTS
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.
CONCLUSION
This study found that topically applied 0.7% olopatadine drops were initially more comfortable than 0.035% ketotifen fumarate drops.
Topics: Humans; Female; Adolescent; Young Adult; Adult; Male; Olopatadine Hydrochloride; Ketotifen; Conjunctivitis, Allergic; Dibenzoxepins; Double-Blind Method; Ophthalmic Solutions
PubMed: 36195538
DOI: 10.1016/j.clae.2022.101769 -
Clinical Ophthalmology (Auckland, N.Z.) Sep 2008Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H(1) receptor antagonist action, chemical mediator suppressive action, and...
Olopatadine hydrochloride exerts a wide range of pharmacological actions such as histamine H(1) receptor antagonist action, chemical mediator suppressive action, and eosinophil infiltration suppressive action. Olopatadine hydrochloride 0.1% ophthalmic solution (Patanol((R))) was introduced to the market in Japan in October 2006. In a conjunctival allergen challenge (CAC) test, olopatadine hydrochloride 0.1% ophthalmic solution significantly suppressed ocular itching and hyperemia compared with levocabastine hydrochloride 0.05% ophthalmic solution, and the number of patients who complained of ocular discomfort was lower in the olopatadine group than in the levocabastine group. Conjunctival cell membrane disruption was observed in vitro in the ketotifen fumarate group, epinastine hydrochloride group, and azelastine hydrochloride group, but not in the olopatadine hydrochloride 0.1% ophthalmic solution group, which may potentially explain the lower discomfort felt by patients on instillation. Many other studies in humans have revealed the superiority of olopatadine 0.1% hydrochloride eye drops to several other anti-allergic eye drops. Overseas, olopatadine hydrochloride 0.2% ophthalmic solution for a once-daily regimen has been marketed under the brand name of Pataday((R)). It is expected that olopatadine hydrochloride ophthalmic solutions may be used in patients with a more severe spectrum of allergic conjunctival diseases, such as vernal keratoconjunctivitis or atopic keratoconjunctivitis, in the near future.
PubMed: 19668750
DOI: 10.2147/opth.s3294 -
Clinical Ophthalmology (Auckland, N.Z.) Jan 2011To evaluate the effectiveness of alcaftadine 0.05%, 0.1%, and 0.25% ophthalmic solutions in treating the signs and symptoms of allergic conjunctivitis when compared with...
PURPOSE
To evaluate the effectiveness of alcaftadine 0.05%, 0.1%, and 0.25% ophthalmic solutions in treating the signs and symptoms of allergic conjunctivitis when compared with olopatadine hydrochloride 0.1% and placebo using the conjunctival allergen challenge (CAC) model.
METHODS
One hundred and seventy subjects were randomized and 164 subjects completed all visits. CAC was performed to determine and confirm subjects' eligibility at visits 1 and 2, respectively. The CAC was repeated at visit 3 (day 0 ± 3), 16 hours after study medication instillation, and at visit 4 (day 14 ± 3), 15 minutes after instillation. Ocular itching and conjunctival redness were evaluated after an allergen challenge, along with several secondary endpoints.
RESULTS
Alcaftadine 0.25% and olopatadine 0.1% treatments exhibited significantly lower mean scores compared with placebo for ocular itching and conjunctival redness at visits 3 and 4. Most adverse events were self-limiting and mild in severity. No serious treatment-related adverse events occurred.
CONCLUSION
Treatment with alcaftadine 0.25% ophthalmic solution resulted in mean differences of >1 unit (ocular itching) and approximately >1 unit (conjunctival redness), which was significant (P < 0.001) compared with placebo treatment. All doses of alcaftadine were safe and well tolerated in the population studied.
PubMed: 21339800
DOI: 10.2147/OPTH.S15379 -
Clinical Therapeutics Dec 2000Mast 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... (Clinical Trial)
Clinical Trial Comparative Study Randomized Controlled Trial
Comparison of the clinical efficacy and comfort of olopatadine hydrochloride 0.1% ophthalmic solution and nedocromil sodium 2% ophthalmic solution in the human conjunctival allergen challenge model.
BACKGROUND
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.
OBJECTIVE
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.
METHODS
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.
RESULTS
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.
CONCLUSION
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
PubMed: 11192137
DOI: 10.1016/s0149-2918(00)83044-1