Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride (olopatadine), an antiallergic drug.

Abstract

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.

Exploring New Frontiers in Asthma Management for Optimal and Economic Outcomes

“…The decision to initiate allergen immunotherapy depends on the extent to which symptoms can be reduced by allergen avoidance and medications and the amount, type, and adverse effects from pharmacotherapy. 18 In a meta-analysis of 20 randomized, placebo-controlled, double-blind trials of allergen immunotherapy for asthma, the combined odds of symptomatic improvement from immunotherapy for any allergen was 3.2. 19 The odds of reduction in bronchial hyperreactivity were 6.8.…”

“…Oral administration of the drug prevented antigen-induced bronchial hyperresponsiveness, airway inflammation, and the immediate and late asthmatic responses to allergen challenge in animals. 17,18 However, inhibitors of thromboxane synthetase (an enzyme responsible for synthesis of thromboxane A 2 ) did not reduce methacholine-induced airway hyperresponsiveness in humans with asthma. 19,20 Additional experience with thromboxane A 2 synthesis inhibitors, thromboxane release inhibitors, and thromboxane receptor antagonists is needed before it can be determined if they will have a role in asthma therapy.…”

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“…Olopatadine belongs to the class of topical antiallergic drugs used for the treatment of allergic conjunctivitis, allergic rhinitis, chronic uriticaria, eczema dermatitis, psoriasis vulgaris and pruritius cutaneous 1 . Its IUPAC name is {(11Z)-11-[3-(dimethylamino)propylidene]-6, 11-dihydrodibenzo [b, e]oxepin-2-yl}acetic acid and its structure is shown in Figure 1.…”

Safety and efficacy of olopatadine hydrochloride nasal spray for the treatment of seasonal allergic rhinitis

“…3,4 An oral form, 2.5-and 5-mg tablets, has been approved as Allelock (Kyowa Hakko Co Ltd, Tokyo, Japan) in Japan for the treatment of allergic rhinitis, chronic urticaria, atopic dermatitis, prurigo, cutaneous pruritus, psoriasis vulgaris, and erythema exudativum multiforme. 5 The pharmacokinetics, pharmacology, and clinical trials of the oral dosage have also been reviewed. 5 Olopatadine (10 mg/kg by mouth) has also been shown to inhibit the nasal symptoms of allergic rhinitis in sensitized guinea pigs by inhibiting the release of histamine and possibly peptide leukotrienes into the nasal cavity.…”

“…5 The pharmacokinetics, pharmacology, and clinical trials of the oral dosage have also been reviewed. 5 Olopatadine (10 mg/kg by mouth) has also been shown to inhibit the nasal symptoms of allergic rhinitis in sensitized guinea pigs by inhibiting the release of histamine and possibly peptide leukotrienes into the nasal cavity. 6 This article describes the first multicenter clinical trial designed to evaluate the safety and efficacy of 0.4% and 0.6% olopatadine in the form of a nasal spray (443 and 665 g, respectively, of olopatadine hydrochloride per spray) vs placebo spray in the treatment of patients with SAR.…”