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Expert Opinion on Pharmacotherapy Aug 2017Olopatadine hydrochloride is an antihistamine and mast cell stabilizer available as oral, intranasal and ocular preparations. Most of the practical applications of... (Review)
Review
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
PubMed: 28656804
DOI: 10.1080/14656566.2017.1346085 -
Arzneimittel-Forschung 2004Olopatadine 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... (Review)
Review
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
PubMed: 15646365
DOI: 10.1055/s-0031-1297036 -
Japanese Journal of Pharmacology Apr 2002Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz[b,e]oxepin-2-acetic acid monohydrochloride) is a novel... (Review)
Review
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
PubMed: 12046981
DOI: 10.1254/jjp.88.379 -
JAMA Mar 2024Allergic rhinitis affects an estimated 15% of the US population (approximately 50 million individuals) and is associated with the presence of asthma, eczema, chronic or... (Review)
Review
IMPORTANCE
Allergic rhinitis affects an estimated 15% of the US population (approximately 50 million individuals) and is associated with the presence of asthma, eczema, chronic or recurrent sinusitis, cough, and both tension and migraine headaches.
OBSERVATIONS
Allergic rhinitis occurs when disruption of the epithelial barrier allows allergens to penetrate the mucosal epithelium of nasal passages, inducing a T-helper type 2 inflammatory response and production of allergen-specific IgE. Allergic rhinitis typically presents with symptoms of nasal congestion, rhinorrhea, postnasal drainage, sneezing, and itching of the eyes, nose, and throat. In an international study, the most common symptoms of allergic rhinitis were rhinorrhea (90.38%) and nasal congestion (94.23%). Patients with nonallergic rhinitis present primarily with nasal congestion and postnasal drainage frequently associated with sinus pressure, ear plugging, muffled sounds and pain, and eustachian tube dysfunction that is less responsive to nasal corticosteroids. Patients with seasonal allergic rhinitis typically have physical examination findings of edematous and pale turbinates. Patients with perennial allergic rhinitis typically have erythematous and inflamed turbinates with serous secretions that appear similar to other forms of chronic rhinitis at physical examination. Patients with nonallergic rhinitis have negative test results for specific IgE aeroallergens. Intermittent allergic rhinitis is defined as symptoms occurring less than 4 consecutive days/week or less than 4 consecutive weeks/year. Persistent allergic rhinitis is defined as symptoms occurring more often than 4 consecutive days/week and for more than 4 consecutive weeks/year. Patients with allergic rhinitis should avoid inciting allergens. In addition, first-line treatment for mild intermittent or mild persistent allergic rhinitis may include a second-generation H1 antihistamine (eg, cetirizine, fexofenadine, desloratadine, loratadine) or an intranasal antihistamine (eg, azelastine, olopatadine), whereas patients with persistent moderate to severe allergic rhinitis should be treated initially with an intranasal corticosteroid (eg, fluticasone, triamcinolone, budesonide, mometasone) either alone or in combination with an intranasal antihistamine. In contrast, first-line therapy for patients with nonallergic rhinitis consists of an intranasal antihistamine as monotherapy or in combination with an intranasal corticosteroid.
CONCLUSIONS AND RELEVANCE
Allergic rhinitis is associated with symptoms of nasal congestion, sneezing, and itching of the eyes, nose, and throat. Patients with allergic rhinitis should be instructed to avoid inciting allergens. Therapies include second-generation H1 antihistamines (eg, cetirizine, fexofenadine, desloratadine, loratadine), intranasal antihistamines (eg, azelastine, olopatadine), and intranasal corticosteroids (eg, fluticasone, triamcinolone, budesonide, mometasone) and should be selected based on the severity and frequency of symptoms and patient preference.
Topics: Humans; Budesonide; Cetirizine; Fluticasone; Histamine H1 Antagonists; Immunoglobulin E; Mometasone Furoate; Olopatadine Hydrochloride; Pruritus; Rhinitis, Allergic; Rhinorrhea; Sneezing; Triamcinolone; Glucocorticoids; Rhinitis; Histamine Antagonists; Administration, Intranasal
PubMed: 38470381
DOI: 10.1001/jama.2024.0530 -
Journal of Dermatological Science Jun 2014
Topics: Animals; Dibenzoxepins; Drug Evaluation, Preclinical; Female; Histamine H1 Antagonists, Non-Sedating; Hypohidrosis; Mice, Inbred C57BL; Olopatadine Hydrochloride
PubMed: 24667096
DOI: 10.1016/j.jdermsci.2014.02.004 -
Journal of Ophthalmic & Vision Research 2018Allergic conjunctivitis (AC) is associated with itching, redness, tearing, pain, and burning sensation in the eyes. The inflammatory process is caused by the mechanism...
PURPOSE
Allergic conjunctivitis (AC) is associated with itching, redness, tearing, pain, and burning sensation in the eyes. The inflammatory process is caused by the mechanism of immediate hypersensitivity due to direct contact with the allergen. This process triggers mast cells in the conjunctiva to activate and release mediators. The purpose of this study was to compare topical olopatadine and ketotifen in terms of effectiveness and safety for the management of AC.
METHODS
Patients clinically diagnosed with AC were randomized into two groups of 60 patients each and received either topical olopatadine HCl 0.1% or ketotifen fumarate 0.025%. They were followed up on the 4, 15, and 30 days to evaluate symptoms, signs, and quality of life (QOL) scoring.
RESULTS
There were a total of 120 patients (67 men and 53 women) with a mean age of 36.35 ± 11 years. Compared to baseline, scores of itching, tearing, redness, eyelid swelling, chemosis and papillae addition of all the individual scores mentioned above and QOL scores reduced significantly ( = 0.001) by the 4 and 15 days of olopatadine and ketotifen application. Compared with ketotifen, olopatadine significantly reduced itching, tearing, hyperemia, and total AC scores by the 4 day ( = 0.001) and conjunctival papillae by the 15 day ( = 0.001). Adverse reactions were reported in 10% and 18% of patients treated with olopatadine and ketotifen, respectively.
CONCLUSION
Compared to ketotifen, olopatadine provided quicker relief of symptoms, and improved symptoms of AC and QOL, with fewer side effects.
PubMed: 29719638
DOI: 10.4103/jovr.jovr_85_17 -
Nihon Yakurigaku Zasshi. Folia... Jul 2001Olopatadine is a selective histamine H1-receptor antagonist possessing inhibitory effects on the release of inflammatory lipid mediators such as leukotriene and... (Review)
Review
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. Oral administration of olopatadine inhibited passive cutaneous anaphylaxis in rats, experimental allergic rhinitis and bronchial asthmatic responses in actively sensitized guinea pigs. Olopatadine exerted no significant effects on action potential duration in isolated guinea pig myocardium and ventricular myocytes. Olopatadine was highly and rapidly absorbed in healthy volunteers. The urinary excretion of olopatadine accounted for not less than 58% and the contribution of metabolism was low in the elimination of olopatadine. 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.
Topics: Animals; Anti-Allergic Agents; Clinical Trials as Topic; Depression, Chemical; Dibenzoxepins; Histamine H1 Antagonists; Humans; Inflammation Mediators; Olopatadine Hydrochloride; Passive Cutaneous Anaphylaxis; Pruritus; Rhinitis, Allergic, Perennial; Urticaria
PubMed: 11496828
DOI: 10.1254/fpj.118.51 -
European Journal of Pharmacology Oct 2015Tacrolimus ointment is prescribed for patients with atopic dermatitis, although it is known to cause transient burning sensations and hot flashes in the applied skin....
Tacrolimus ointment is prescribed for patients with atopic dermatitis, although it is known to cause transient burning sensations and hot flashes in the applied skin. The aim of this study was to evaluate the effects of olopatadine hydrochloride (olopatadine), an antiallergic agent with a histamine H1 receptor (H1R) antagonistic activity, on the incidence of hot flashes induced by topical treatment with tacrolimus ointment in rats. Consequently, the skin temperature was increased by the topical application of tacrolimus ointment in rats, and the rise in skin temperature was inhibited by pretreatment with olopatadine in a dose-dependent manner. Inhibitory effect of olopatadine on tacrolimus-induced skin temperature elevation was significantly more potent than that of cetirizine hydrochloride, other antiallergic agent with H1R antagonistic activity, at doses in which both agents exhibit comparable H1R antagonistic activity in rats. These results suggest that H1R antagonistic activity-independent mechanism contribute to the inhibitory effect of olopatadine on tacrolimus-induced skin temperature elevation. Olopatadine also significantly inhibited increases in vascular permeability and nerve growth factor production in the skin induced by topical tacrolimus treatment. Thus, the onset of hot flashes in rats is quantitatively determined by measuring the skin temperature and olopatadine attenuates hot flashes induced by topical tacrolimus ointment in rats, suggesting that the combination application with olopatadine and tacrolimus ointment is useful for improving medication adherence with tacrolimus ointment treatment in patients with atopic dermatitis.
Topics: Administration, Topical; Animals; Anti-Inflammatory Agents, Non-Steroidal; Dose-Response Relationship, Drug; Hot Flashes; Male; Nerve Growth Factor; Ointments; Olopatadine Hydrochloride; Rats; Rats, Hairless; Tacrolimus; Treatment Outcome
PubMed: 26362749
DOI: 10.1016/j.ejphar.2015.09.008 -
The Annals of Pharmacotherapy May 2023To review the pharmacology, efficacy, and safety of intranasal olopatadine hydrochloride-mometasone furoate (OM) combination in the treatment of seasonal allergic... (Review)
Review
OBJECTIVE
To review the pharmacology, efficacy, and safety of intranasal olopatadine hydrochloride-mometasone furoate (OM) combination in the treatment of seasonal allergic rhinitis (SAR).
DATA SOURCES
The PubMed database and ClinicalTrials.gov were searched using the following terms: mometasone + olopatadine, GSP301, mometasone furoate, and olopatadine hydrochloride.
STUDY SELECTION AND DATA EXTRACTION
Articles published in English between January 1987 and August 2022 related to pharmacology, safety, and clinical trials were assessed.
DATA SYNTHESIS
In 2 phase II clinical trials, twice-daily (BID) and once-daily (QDay) intranasal OM demonstrated significant improvements in reflective total nasal symptom score (rTNSS) (BID < 0.001 and QDay < 0.001) and instantaneous total nasal symptom score (iTNSS) (BID < 0.001 and < 0.0001; QDay < 0.001 and < 0.0001). In 2 phase III clinical trials, BID OM showed significant improvements in rTNSS vs. placebo ( < 0.001), olopatadine monotherapy ( = 0.03 and = 0.003), and mometasone monotherapy ( = 0.02 and = 0.059).
RELEVANCE TO PATIENT CARE AND CLINICAL PRACTICE
OM is indicated for treatment of SAR symptoms. Caution with use must be considered for certain high-risk patients, existing tuberculosis; fungal, bacterial, viral, or parasitic infections; or ocular herpes simplex. Due to its quick and sustained onset of action, OM may be an ideal agent for initial treatment of moderate-severe SAR for patients 12 years and older.
CONCLUSION
OM significantly improves SAR symptoms and is a viable treatment option in short-term SAR.
Topics: Humans; Olopatadine Hydrochloride; Mometasone Furoate; Rhinitis, Allergic, Seasonal; Nasal Sprays; Administration, Intranasal; Double-Blind Method; Treatment Outcome
PubMed: 36123818
DOI: 10.1177/10600280221124230 -
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