Gene/Protein Disease Symptom Drug Enzyme Compound
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Query: UMLS:C0033774 (pruritus)
 14,546 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

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.
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PMID:[Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride' (olopatadine), an antiallergic drug]. 1149 28

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).
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PMID:Pharmacological, pharmacokinetic and clinical properties of olopatadine hydrochloride, a new antiallergic drug. 1204 81

Ocular allergy affects > 20% of the general population and many therapeutic preparations are available to individuals experiencing the most common forms--seasonal and perennial allergic conjunctivitis. 0.1% Olopatadine topical ophthalmic solution is currently approved for the treatment of allergic signs and symptoms in patients > or = 3 years of age. Olopatadine is available in Europe as Opatanol) and in > 30 other countries as Patanol. It inhibits mast cell degranulation and antagonises histamine receptors to manage the itching, redness, chemosis, tearing and lid swelling of the ocular allergic reaction, and its mast cell stabilising ability has been demonstrated both in vitro (using human conjunctival mast cells) and in vivo (human clinical experience). This article reviews both the laboratory and clinical information available on olopatadine, prefaced by a discussion of the current understanding of the ocular allergic reaction and followed by the future implications for this compound. Both laboratory and clinical studies have established the efficacy, safety and comfort of olopatadine in several study design models and comparisons to other antiallergy medications. The application of olopatadine, specifically in the management of lid swelling, an allergic sign recalcitrant to therapy and nasal allergic symptoms has also been established. In the future, a new formulation containing 0.2% olopatadine exhibits a duration of action up to 24 h, supporting once-daily dosing.
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PMID:A review of olopatadine for the treatment of ocular allergy. 1533 Jul 35

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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PMID:Properties of olopatadine hydrochloride, a new antiallergic/antihistaminic drug. 1564 65

Intense pruritus and cutaneous reactivity represent cardinal features of eczema. The resulting scratching behaviors alter neuronal conditions of the spinal dorsal horn where the primary sensory afferent fibers transmit cutaneous stimulation and deteriorate eczematous skin lesions. We investigated the effects of olopatadine hydrochloride (olopatadine) on alteration of neuronal conditions of the spinal dorsal horn and eczematous skin lesions induced by contact dermatitis. Eczematous lesions were induced by repeated application of diphenylcyclopropenone (DCP) in BALB/c mice. Olopatadine suppressed scratching behavior caused by repeated application of DCP in mice. Increased expressions of c-Fos and substance P in the spinal dorsal horn following DCP application were improved by olopatadine. Furthermore, olopatadine diminished the number of infiltrating cells and levels of cytokines in eczematous skin lesions resulting from DCP application. Olopatadine improves neurological conditions in the spinal cord and eczematous skin lesions in a murine contact dermatitis model.
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PMID:Neuronal conditions of spinal cord in dermatitis are improved by olopatadine. 1693 47

Olopatadine hydrochloride ophthalmic solution 0.2% (Pataday, Alcon) is a new formulation of olopatadine hydrochloride ophthalmic solution, the first topical ocular antiallergic agent indicated for once-daily dosing. The aim of this study was to evaluate the safety, efficacy, onset, and duration of action of olopatadine 0.2% in the treatment of allergic conjunctivitis. Using the conjunctival allergen challenge, this double-masked, randomized by eye, parallel-group study included four visits over a 5-week period. Subjects were screened for eligibility (visit 1) and their ocular allergic responses were confirmed at visit 2. The efficacy of olopatadine in reducing the signs and symptoms of allergic conjunctivitis was evaluated at onset of action (visit 4) and 16 hours (visit 3) after masked medication instillation. The primary efficacy parameter was ocular itching. Safety parameters were also evaluated. Ninety subjects were evaluated. Olopatadine 0.2% was significantly (p < 0.001) more effective than placebo in the treatment of ocular itching at all time points at both the onset of action and the 16-hour allergen challenges. Olopatadine 0.2% was significantly (p < 0.03) more effective than placebo in the reduction of conjunctival redness, chemosis, and eyelid swelling at all time points (with the exception of conjunctival redness, which was significantly reduced at five of six time points). There were no serious adverse events and no treatment-related adverse events. Once-daily dosing with olopatadine 0.2% reduced the signs and symptoms of allergic conjunctivitis with a rapid and prolonged duration of action. Safety analyses indicated that olopatadine 0.2% was safe and well tolerated in subjects with a history of allergic conjunctivitis.
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PMID:Efficacy of olopatadine ophthalmic solution 0.2% in reducing signs and symptoms of allergic conjunctivitis. 1788 10

Olopatadine 0.1% (Patanol) and olopatadine 0.2% (Pataday) ophthalmic solutions are topical ocular anti-allergic agents with antihistaminic and mast cell stabilizing properties. The efficacy of two doses of olopatadine 0.1% was compared to one dose of olopatadine 0.2% in the prevention of ocular itching associated with allergic conjunctivitis over 24 hours. This double-masked conjunctival allergen challenge (CAC) study found no significant difference in the mean itching scores between two drops of olopatadine 0.1% and one drop of olopatadine 0.2%. Both showed significant activity at the 24-hour time point and were statistically superior to placebo. No adverse events occurred while on drug therapy.
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PMID:Efficacy of once-daily olopatadine 0.2% ophthalmic solution compared to twice-daily olopatadine 0.1% ophthalmic solution for the treatment of ocular itching induced by conjunctival allergen challenge. 1808 65

Allergic conjunctivitis is an inflammatory condition of the ocular surface characterized by ocular itching, redness, tearing, chemosis, and eyelid swelling. The purpose of this study was to assess the comparative efficacy of an ophthalmic antihistamine/mast cell stabilizer solution and an intranasal steroid at reducing the signs and symptoms of allergic conjunctivitis induced by the conjunctival allergen challenge (CAC) model. Sixty subjects were enrolled in a single center, randomized, placebo-controlled, parallel-treatment, four-visit CAC study. After titration and confirmation of the allergic reaction at visits 1 and 2, subjects were randomized at visit 3 into one of 4 treatment groups (olopatadine 0.2% ophthalmic solution, fluticasone furoate nasal spray, a tear substitute, or saline nasal spray), dosed with study medication, and challenged 15 minutes later, after which ocular allergic signs and symptoms were assessed. Subjects continued treatment of the assigned medication for 6 days. At visit 4, subjects underwent similar procedures to those performed at visit 3. Fifty-nine subjects completed the study. Olopatadine 0.2% ophthalmic solution showed statistical and clinical superiority over fluticasone furoate nasal spray at all post-CAC time points after a single dose (p < 0.001) and after a 1-week loading period (p < 0.01) for ocular itching, the primary end point. Similarly, olopatadine 0.2% showed statistical and clinical superiority over fluticasone furoate for the majority of time points for ocular redness, tearing, chemosis, and eyelid swelling. Olopatadine 0.2% ophthalmic solution was statistically and clinically superior to fluticasone furoate nasal spray for the relief of signs and symptoms of allergic conjunctivitis.
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PMID:A comparison of olopatadine 0.2% ophthalmic solution versus fluticasone furoate nasal spray for the treatment of allergic conjunctivitis. 1946 11

Olopatadine is a tricyclic compound with antihistaminic, mast cell-stabilizing, and anti-inflammatory properties. In the United States olopatadine is approved as a b.i.d. ophthalmic solution, Patanol (Alcon Laboratories, Inc., Fort Worth, TX) to treat all signs and symptoms of allergic conjunctivitis and as a q.d. formulation, Pataday (Alcon Laboratories, Inc.), to treat itching associated with allergic conjunctivitis. A nasal spray, Patanase (Alcon Laboratories, Inc.), was approved in 2008 for treatment of the symptoms of seasonal allergic rhinitis. The available data on olopatadine was assessed with regard to future uses through a comprehensive literature review and a Roundtable Discussion held at the 2009 meeting of the American Academy of Allergy Asthma and Immunology. The unique mechanisms of action of olopatadine still under study include mast cell stabilization, potent H(1)-anthistaminic activity, and anti-inflammatory effects. Data support consideration of nasal olopatadine for as-needed use for episodic symptoms of allergic rhinitis, for treatment of nonallergic rhinitis, and for use in combination with topical steroids for patients with moderate-to-severe allergy symptoms.
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PMID:Comprehensive review of olopatadine: the molecule and its clinical entities. 2040 93

Adequate treatment is critical for maintaining a good level of quality of life (QOL) during the pollen season in patients suffering from seasonal allergic rhinitis (SAR). Olopatadine, a histamine H(1)-receptor antagonist, has been approved in the United States and Europe for the treatment of AR and allergic conjunctivitis as a nasal spray and an ophthalmic solution, respectively. We conducted a randomized, double-blind, placebo-controlled study to determine whether orally administered olopatadine for prophylactic purposes might also be effective for the control of nasal allergy symptoms, especially nasal congestion, in patients with SAR due to Japanese cedar pollen (SAR-JP). A total of 110 patients with SAR caused by JP were randomized to the treatment. The subjects recorded their nasal and ocular allergic symptom scores in a diary, and their QOL was assessed by the Japanese version of the Rhinoconjunctivity Quality of Life Questionnaire. Treatment with oral olopatadine significantly suppressed sneezing (p < 0.001), rhinorrhea (p < 0.001), and nasal congestion (p < 0.05). The total QOL score during the peak JP season was superior in the olopatadine group than in the placebo group (p < 0.05). However, orally administered olopatadine did not exert any significant effect against eye itching and watering of the eyes, unlike olopatadine nasal spray. Treatment with olopatadine tablets yielded superior QOL scores in the domains of usual daily activities and outdoor activities when compared with placebo. No serious adverse effects of the treatment were reported during the study period. These results suggest that oral olopatadine treatment may be a useful alternative treatment strategy for AR.
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PMID:Efficacy of oral olopatadine hydrochloride for the treatment of seasonal allergic rhinitis: A randomized, double-blind, placebo-controlled study. 2081 19


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