Effects of olopatadine hydrochloride on the release of thromboxane B2 and histamine from nasal mucosa after antigen–antibody reaction in guinea pigs

Kaise, Toshihiko; Akamatsu, Yukino; Ohmori, Kenji; Ishii, Akio; Karasawa, Akira

doi:10.1046/j.1440-1592.2001.00236.x

Cited by 7 publications

(6 citation statements)

References 18 publications

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“…Many clinical trials have been conducted to assess efficacy of olopatadine hydrochloride (Kaliner et al, 2010), however, few in vivo studies have evaluated its mechanism of action. In a sensitized guinea pig model, Kaise et al (2001) reported reduced thromboxane A 2 (TXA 2 ) concentration in the nasal lavage fluid following oral administration of olopatadine. This result is consistent with the findings of rat cell-culture models exhibiting reduction in Leukotriene C 4 (Chand et al, 1989; Hamasaki et al, 1996), which is derived from the same arachidonic acid pathway as thromboxane.…”

Section: Intranasal Antihistaminesmentioning

confidence: 99%

Modulation of Allergic Inflammation in the Nasal Mucosa of Allergic Rhinitis Sufferers With Topical Pharmaceutical Agents

et al. 2019

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Allergic rhinitis (AR) is a chronic upper respiratory disease estimated to affect between 10 and 40% of the worldwide population. The mechanisms underlying AR are highly complex and involve multiple immune cells, mediators, and cytokines. As such, the development of a single drug to treat allergic inflammation and/or symptoms is confounded by the complexity of the disease pathophysiology. Complete avoidance of allergens that trigger AR symptoms is not possible and without a cure, the available therapeutic options are typically focused on achieving symptomatic relief. Topical therapies offer many advantages over oral therapies, such as delivering greater concentrations of drugs to the receptor sites at the source of the allergic inflammation and the reduced risk of systemic side effects. This review describes the complex pathophysiology of AR and identifies the mechanism(s) of action of topical treatments including antihistamines, steroids, anticholinergics, decongestants and chromones in relation to AR pathophysiology. Following the literature review a discussion on the future therapeutic strategies for AR treatment is provided.

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Section: Intranasal Antihistaminesmentioning

confidence: 99%

Modulation of Allergic Inflammation in the Nasal Mucosa of Allergic Rhinitis Sufferers With Topical Pharmaceutical Agents

et al. 2019

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“…In order to investigate the mechanism of the amelioration of allergic rhinitis by olopatadine, the effects of the drug on the increase of histamine, LTs and TXB 2 concentrations in nasal lavage fluid (NALF) following intranasal antigen challenge in sensitized guinea pigs were investigated [23,24]. In actively sensitized animals, the concentrations of LTs and histamine increased 10 min after antigen challenge [23] and in passively sensitized animals the concen-trations of TXB 2 and histamine increased 10 min after antigen challenge [24]. Oral administration of olopatadine (10 mg/kg) to actively sensitized animals significantly inhibited the increase in histamine and reduced the increase in LTs.…”

Section: Inhibitory Effects On the Production And Release Of Chemicalmentioning

confidence: 99%

Properties of Olopatadine Hydrochloride, a New Antiallergic/Antihistamine Drug

Ohmori

Hasegawa

Tamura

et al. 2011

Arzneimittelforschung

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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.

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“…In actively sensitized animals, the concentrations of peptide-LTs and histamine increased 10 min after the antigen challenge (32). The concentrations of TXB 2 and histamine increased 10 min after antigen challenge in passively sensitized animals (33). Oral administration of olopatadine at 10 mg/ kg significantly prevented the increase in histamine and tended to inhibit the increase in peptide LTs in actively sensitized animals.…”

Section: -2 Mode Of Action 2-2-1 Histamine H1-receptor Antagonistimentioning

confidence: 99%

“…In order to investigate the mechanism for the amelioration of allergic rhinitis by olopatadine, its effects on the increase in histamine, peptide-LTs and TXB2 concentrations in nasal lavage fluid (NALF) following the intranasal antigen challenge in sensitized guinea pigs were investigated (32,33). In actively sensitized animals, the concentrations of peptide-LTs and histamine increased 10 min after the antigen challenge (32).…”

Section: -2 Mode Of Action 2-2-1 Histamine H1-receptor Antagonistimentioning

confidence: 99%

Pharmacological, Pharmacokinetic and Clinical Properties of Olopatadine Hydrochloride, a New Antiallergic Drug

Ohmori

Hayashi

Kaise

et al. 2002

Japanese Journal of Pharmacology

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ABSTRACT-Olopatadine hydrochloride (olopatadine, 11-[(Z)-3-(dimethylamino)propylidene]-6,11-dihydrodibenz [b,e]oxepin-2-acetic acid monohydrochloride) is a novel antiallergic/ histamine H 1 -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 H 1 -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, pruritis 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).

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Effects of olopatadine hydrochloride on the release of thromboxane B2 and histamine from nasal mucosa after antigen–antibody reaction in guinea pigs

Cited by 7 publications

References 18 publications

Modulation of Allergic Inflammation in the Nasal Mucosa of Allergic Rhinitis Sufferers With Topical Pharmaceutical Agents

Modulation of Allergic Inflammation in the Nasal Mucosa of Allergic Rhinitis Sufferers With Topical Pharmaceutical Agents

Properties of Olopatadine Hydrochloride, a New Antiallergic/Antihistamine Drug

Pharmacological, Pharmacokinetic and Clinical Properties of Olopatadine Hydrochloride, a New Antiallergic Drug

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