The structure of a major active metabolite of the nonsedating antihistamine loratadine was confirmed by synthesis. The metabolite 3 was prepared from 3-methyl pyridine in twelve steps.

BACKGROUND Botanical products are frequently used for treatment of nasal allergy. Three of these substances, Cinnamomum zeylanicum, Malpighia glabra, and Bidens pilosa, have been shown to have a number of anti-allergic properties in-vitro. The current study was conducted to determine the effects of these combined ingredients upon the nasal response to allergen challenge in patients with seasona...

BACKGROUND Proinflammatory mediators such as the cysteinyl leukotrienes are important in the pathophysiology of allergic rhinitis. This study evaluated the efficacy and tolerability of montelukast, a cysteinyl leukotriene receptor antagonist, given once daily in the morning for treatment of seasonal (fall) allergic rhinitis for 4 weeks. METHODS This was a randomized, double-blind trial with a...

It has been reported that some of H1 receptor antagonists have important effects on cardiovascular system. Terfenadine as a non-sedative H1 receptor antagonist has an arrhythmogenic activity. In this study we have shown the effects of four antihistamine drugs: terfenadine, loratadine, clemastine and diphenhydramine, on the rate and contractions of isolated rat atria. Terfenadine (1-10 µM) cause...

Background: Azelastine hydrochloride is an H1-receptor antagonist with antiinflammatory properties that is available in the US as Astelin Nasal Spray for the treatment of seasonal allergic rhinitis. The symptoms of seasonal allergic rhinitis can initially be treated with monotherapy using either an antihistamine or an intranasal corticosteroid. Patients whose symptoms do not respond adequately ...

BACKGROUND The CC-chemokine receptor-3 (CCR3) has emerged as a target molecule for pharmacological intervention in allergic inflammation. OBJECTIVE To examine whether a dual CCR3 and H1-receptor antagonist (AZD3778) affects allergic inflammation and symptoms in allergic rhinitis. METHODS Patients with seasonal allergic rhinitis were subjected to three seven days' allergen challenge series. ...

Allergic rhinitis (AR) is a chronic inflammatory disease of rhino-ocular mucosa, affecting up to 40% of population worldwide. Chinese herbal medicines and Acupuncture, adopted thousands of years in China, has good effect on allergic rhinitis. This study evaluates the effects of Moxibustion with Chinese herbal in treating patients with allergic rhinitis over a 1-year follow-up. A randomized cont...

It is accepted that studies evaluating histamine-induced wheal and flare reactions in the skin represent a simple and reliable method for demonstrating pharmacodynamic activity and pharmacokinetics of the H1-receptor antagonists. In this study, the effects of single oral doses of acrivastine (8 mg), loratadine (10 mg) and cetirizine (10 mg) on the histamine-induced wheal and flare reactions wer...

In the present work Loratadine and Phenylephrine Bilayer tablets were prepared by compressing Loratadine layer as direct compressible layer which is an immediate release layer and Phenylephrine hydrochloride by wet granulation method as sustained release layer which are compressed using Bilayer tableting machine. The tablets were evaluated for thickness, hardness, friability, and weight variati...