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Ocular Immunology and Inflammation Nov 2021: This study evaluated the efficacy and safety of once-daily Alcaftadine 0.25% (AGN-229666) for prevention of signs and symptoms of Japanese cedar-pollen allergic... (Comparative Study)
Comparative Study Randomized Controlled Trial
: This study evaluated the efficacy and safety of once-daily Alcaftadine 0.25% (AGN-229666) for prevention of signs and symptoms of Japanese cedar-pollen allergic conjunctivitis.: This was a single-center, placebo-, and comparator-controlled study using the Ora-CAC® model of allergic conjunctivitis. The primary endpoint was ocular itching 16 hours after Alcaftadine 0.25% instillation; efficacy at 16 hours was compared with 0.1% Olopatadine, 4 hours after instillation. Secondary endpoints included conjunctival hyperemia.: 263 Japanese subjects were enrolled; 224 completed the trial. Alcaftadine 0.25% was statistically superior to vehicle for relief of ocular itching at 16 hours ( < .0001). Alcaftadine 0.25% at 16 hours was non-inferior to Olopatadine at 4 hours. Alcaftadine 0.25% was significantly better than vehicle for relief of conjunctival hyperemia. All treatments showed a low frequency of ocular adverse events.: Once-daily Alcaftadine 0.25% is safe and effective in preventing signs and symptoms of Japanese cedar-pollen allergic conjunctivitis.
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
PubMed: 32501774
DOI: 10.1080/09273948.2020.1760309 -
Turkish Journal of Pharmaceutical... Dec 2019Forced degradation determines the intrinsic stability of a molecule by establishing degradation pathways in order to identify the likely degradation products (DPs). The...
OBJECTIVES
Forced degradation determines the intrinsic stability of a molecule by establishing degradation pathways in order to identify the likely degradation products (DPs). The objective of the present research was to establish intrinsic stability and forced degradation profiling of olopatadine hydrochloride.
MATERIALS AND METHODS
The intrinsic stability of olopatadine hydrochloride was evaluated by RP-HPLC, where a mixture of 0.1% formic acid and organic phase (methanol:acetonitrile; 50:50 % v/v) was used as mobile phase at 1.0 mL/min in gradient mode. Different stress conditions were employed to explore the intrinsic stability of olopatadine hydrochloride.
RESULTS
In acidic condition, five DPs, i.e. OLO1, OLO2, OLO3, OLO4, and OLO5, were observed. OLO5 was the major DP that increased with time and the peak area of OLO was decreased. In addition to OLO3 and OLO5, two more DPs were observed in alkaline condition, i.e. OLO6 and OLO7. OLO5 and OLO6 were two major DPs; OLO5 increased with time while OLO6 had a zigzag pattern of peak area with time. All DPs of neutral condition were also found in acidic condition while OLO3 and OLO5 were common in all three types of hydrolytic degradation.
CONCLUSION
Thus, OLO has similar pattern of degradation profiling in all hydrolytic conditions (acidic, alkaline, and neutral). No degradation was found in thermal, ultraviolet light, or oxidative conditions over 10 days. OLO-Imp was recognized as an analogue structure of OLO and proposed as 11-[(3-dimethylamino)-propylidene]-6,11-dihydro-dibenz[b,e]oxepin-2-propanoic acid in standard drug. OLO1 was identified as (2-(4-(dimethylamino) butyl) phenyl)methanol, which may be formed by cleavage of the tricyclic ring in neutral condition.
PubMed: 32454741
DOI: 10.4274/tjps.galenos.2018.83007 -
The American Journal of Nursing Jun 2020
Topics: Diclofenac; Humans; Nonprescription Drugs; Olopatadine Hydrochloride; Prescription Drugs
PubMed: 32443119
DOI: 10.1097/01.NAJ.0000668720.40197.20 -
Journal of Ocular Pharmacology and... Sep 2020Olopatadine hydrochloride 0.1% is one of the known primary topical treatments in ocular allergy. Although olopatadine is a worldwide used medication, the changes in... (Randomized Controlled Trial)
Randomized Controlled Trial
Pupil Diameter, Corneal Thickness, and Anterior Chamber Alterations Following Topical Olopatadine Hydrochloride 0.1%: A Single-Masked Randomized Controlled Clinical Study.
Olopatadine hydrochloride 0.1% is one of the known primary topical treatments in ocular allergy. Although olopatadine is a worldwide used medication, the changes in pupil diameter, cornea, and anterior chamber associated with its use have not been studied in detail. In this prospective study, we aimed to determine the amount of mydriasis and explore the possible corneal and anterior chamber alterations after 0.1% topical olopatadine. A total of 77 eyes from 77 ocular-allergy diagnosed patients between 18 and 40 years were investigated in this prospective study. Thirty-nine eyes of 39 patients received topical olopatadine, and 38 eyes of 38 patients received sterile distilled water, randomly. Pentacam (Oculus Optikgeräte GmbH, Wetzlar, Germany) topography was used to assess the pupil and anterior chamber measurements at baseline and after 45 min of olopatadine or sterile distilled water instillation. The differences between the baseline and 45th-min measurements for corneal thickness, anterior chamber depth, angle, and volume did not reach a statistical significance in the olopatadine or control groups. The pupil diameter significantly increased from 3.19 ± 0.62 to 3.36 ± 0.62 mm in the olopatadine group ( < 0.001), and remained relatively unchanged in the control group ( = 0.06). Olopatadine 0.1% does not lead to a significant change in corneal topography or anterior chamber parameters. However, it causes a slight but statistically significant increase in pupil diameter.
Topics: Administration, Ophthalmic; Adolescent; Adult; Anterior Chamber; Anti-Allergic Agents; Cornea; Corneal Topography; Female; Humans; Male; Olopatadine Hydrochloride; Prospective Studies; Pupil; Young Adult
PubMed: 32250190
DOI: 10.1089/jop.2020.0007 -
Journal of Investigational Allergology... Feb 2020
Topics: Child, Preschool; Drug Hypersensitivity; Drug-Related Side Effects and Adverse Reactions; Humans; Hypersensitivity, Immediate; Infant; Male; Olopatadine Hydrochloride; Polyethylene Glycols; Recurrence; Skin; Skin Tests
PubMed: 32077856
DOI: 10.18176/jiaci.0447 -
Medicine Feb 2020Allergic 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...
BACKGROUND
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.
METHODS
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.
RESULTS
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.
CONCLUSION
Our review will provide useful information to judge whether olopatadine hydrochloride eye drops is an effective intervention for patients with AC.
ETHICS AND DISSEMINATION
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 REGISTRATION NUMBER
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
PubMed: 32049778
DOI: 10.1097/MD.0000000000018618 -
Journal of Pharmaceutical Sciences May 2020Olopatadine HCl is an antiallergic drug used for the management of allergic conjunctivitis. Currently, it is delivered via eye drop solution, which is highly inefficient...
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
PubMed: 32007507
DOI: 10.1016/j.xphs.2020.01.022 -
Annals of Allergy, Asthma & Immunology... Feb 2020GSP301 is an investigational fixed-dose combination nasal spray of olopatadine hydrochloride (antihistamine) and mometasone furoate (corticosteroid). (Randomized Controlled Trial)
Randomized Controlled Trial
BACKGROUND
GSP301 is an investigational fixed-dose combination nasal spray of olopatadine hydrochloride (antihistamine) and mometasone furoate (corticosteroid).
OBJECTIVE
To evaluate efficacy and safety of GSP301 in patients with seasonal AR (SAR).
METHODS
In this phase 2, double-blind, parallel-group study, patients (≥12 years of age) with SAR were equally randomized to twice-daily GSP301 (olopatadine 665 μg and mometasone 25 μg), once-daily GSP301 (olopatadine 665 μg and mometasone 50 μg), twice-daily or once-daily olopatadine monotherapy (665 μg), mometasone monotherapy (twice-daily 25 μg or once-daily 50 μg), or placebo for 14 days. The primary endpoint-mean change from baseline in morning and evening reflective Total Nasal Symptom Score (rTNSS)-was analyzed using analysis of covariance (ANCOVA; P < .05 = statistically significant). Average morning and evening 12-hour instantaneous TNSS (iTNSS), ocular symptoms, individual symptoms, onset of action, quality of life, and adverse events (AEs) were also assessed.
RESULTS
A total of 1111 patients were randomized. Twice-daily GSP301 provided statistically significant and clinically meaningful rTNSS improvements vs placebo (P < .001), twice-daily olopatadine (P = .049), and mometasone (P = .004). Similar significant improvements in iTNSS were observed with twice-daily GSP301 vs placebo (P < .001) and twice-daily mometasone (P = .007); improvements were not significant vs olopatadine (P = .058). Once-daily GSP301 provided significant rTNSS and iTNSS improvements vs placebo and once-daily olopatadine (P < .01, all) but improvements were not significant vs mometasone. Treatment-emergent AEs rates were 10.8%, 9.5%, and 8.2%, with twice-daily GSP301, once-daily GSP301, and placebo, respectively.
CONCLUSION
Twice-daily GSP301 treatment was efficacious and well tolerated, providing statistically significant and clinically meaningful improvements in rTNSS (primary endpoint) vs placebo and both monotherapies.
TRIAL REGISTRATION
Clinicaltrials.gov Identifier NCT02318303.
Topics: Drug Administration Schedule; Drug Combinations; Drug Therapy, Combination; Female; Humans; Male; Middle Aged; Mometasone Furoate; Nasal Sprays; Olopatadine Hydrochloride; Rhinitis, Allergic, Seasonal; Treatment Outcome
PubMed: 31734334
DOI: 10.1016/j.anai.2019.11.007 -
BMC Ophthalmology Nov 2019To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on...
BACKGROUND
To investigate the cytotoxicities of the topical ocular dual-action anti-allergic agents (alcaftadine 0.25%, bepotastine besilate 1.5%, and olopatadine HCL 0.1%) on human corneal epithelial cells (HCECs) and their anti-allergic effects on cultured conjunctival epithelial cells.
METHODS
A Methylthiazolyltetrazolium(MTT)-based calorimetric assay was used to assess cytotoxicities using HCECs at concentrations of 10, 20 or 30% for exposure durations of 30 min, 1 h, 2 h, 12 h or 24 h. Cellular morphologies were evaluated by inverted phase-contrast and electron microscopy. Wound widths were measured 2 h, 18 h, or 24 h after confluent HCECs monolayers were scratched. Realtime PCR was used to quantify anti-allergic effects on cultured human conjunctival cells, in which allergic reactions were induced by treating them with Aspergillus antigen.
RESULTS
Cell viabilities decreased in time- and concentration-dependent manners. Cells were detached from dishes and showed microvilli loss, cytoplasmic vacuoles, and nuclear condensation when exposed to antiallergic agents; alcaftadine was found to be least cytotoxic. Alcaftadine treated HCECs monolayers showed the best wound healing followed by bepotastine and olopatadine (p < 0.0001). All agents significantly reduced the gene expressions of allergic cytokines (IL-5, IL-25, eotaxin, thymus and activation-regulated chemokine, and thymic stromal lymphopoietin) and alcaftadine had the greatest effect (p < 0.0001 in all cases).
CONCLUSIONS
Alcaftadine seems to have less side effects and better therapeutic effects than the other two anti-allergic agents tested. It may be more beneficial to use less toxic agents for patients with ocular surface risk factors or presumed symptoms of toxicity.
Topics: Anti-Allergic Agents; Benzazepines; Cell Survival; Cells, Cultured; Conjunctiva; Cornea; Epithelial Cells; Humans; Imidazoles; Olopatadine Hydrochloride; Piperidines; Pyridines
PubMed: 31703568
DOI: 10.1186/s12886-019-1228-5 -
Indian Journal of Ophthalmology Sep 2019With increasing environmental pollution, the incidence of allergic conjunctivitis is increasing. Newer anti-allergic medications with combined anti-histaminic and mast... (Randomized Controlled Trial)
Randomized Controlled Trial
PURPOSE
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.
METHODS
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.
RESULTS
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.
CONCLUSION
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
PubMed: 31436181
DOI: 10.4103/ijo.IJO_2112_18