Gene/Protein Disease Symptom Drug Enzyme Compound
Pivot Concepts:   Target Concepts:
Query: UMLS:C0042109 (urticaria)
 6,569 document(s) hit in 31,850,051 MEDLINE articles (0.00 seconds)

Urticaria is a cutaneous syndrome characterized by dermal edema (wheal) and erythema (flare) that blanches with pressure. The lesions typically last less than 24 hours and are usually pruritic. In 1983, Christensen and Maibach summarized the theory behind the use of histamine H1 receptor antagonists (antihistamines) in clinical dermatology. These agents remain the mainstay of treatment for urticaria. This article reviews the medical literature on the effectiveness of antihistamines in urticarial syndromes, including acute, chronic idiopathic and the physical urticarias. Older antihistamines, such as chlorpheniramine and hydroxyzine, are effective in the treatment of urticarias, but they also have marked sedative and anticholinergic effects. Newer nonsedating antihistamines (second-generation antihistamines) have been developed that have reduced adverse effects because they do not cross the blood-brain barrier; these agents (acrivastine, cetirizine, loratadine, mizolastine, fexofenadine, ebastine, azelastine and epinastine) cause significantly less sedation and psychomotor impairment than their older counterparts. A review of the literature reveals that there are few studies which document the efficacy of second-generation antihistamines in the treatment of acute urticaria, a biologic entity that usually resolves within 3 weeks. We did not identify controlled studies that suggested superiority of any antihistamine in the treatment of acute urticaria. Loratadine or cetirizine, and possibly mizolastine, appear to be treatments of choice for chronic idiopathic urticaria. For symptomatic dermatographism, the combination of an antihistamine and an H2 antagonist, e.g. chlorpheniramine and cimetidine, appears to be effective. Very few studies have been conducted on the use of antihistamines in the treatment of cold, cholinergic, and pressure urticaria. Antihistamines are the mainstay of urticarial therapy. This evidence-based review suggests that there are efficacy differences between newer, nonsedating antihistamines and older agents in some forms of the disorder. Clearly, further well-controlled clinical trials in larger numbers of patients are needed to clarify the role of these agents in the treatment of urticaria.
 ...
PMID:Treatment of urticaria. An evidence-based evaluation of antihistamines. 1170 18

Allergic rhinitis (AR) is a global health concern and shares a high comorbidity with asthma. Recent research suggests that different allergic diseases, such as AR, asthma, allergic conjunctivitis and chronic idiopathic urticaria (CIU), are evoked by common pathological mechanisms characterised by the release of histamine and other inflammatory mediators. Although H(1) receptor antagonists are the mainstay of therapy for allergic disease, the unacceptably high incidence of anticholinergic and CNS-related side effects of first-generation H(1) antagonists led to the search for improved second-generation H(1) antagonists. While many of these agents were largely devoid of CNS side effects, their tendency for drug-drug interactions (e.g., terfenadine and astemizole) resulted in an increased incidence of cardiotoxicity. Furthermore, second-generation H(1) antagonists exhibited weak anti-inflammatory properties and had no effect on nasal congestion. These observations emphasised the need for newer anti-allergic agents with a broader spectrum of activity and an improved safety profile. Among the newer H(1) antagonists currently in clinical development, desloratadine and mizolastine are the most widely studied. Both have a rapid onset of action, and desloratadine has demonstrated clinical efficacy in AR, CIU and seasonal asthma. Desloratadine has several advantages over other H(1) antagonists in that it has proven decongestant activity, a sparing effect on the use of bronchodilators (beta(2)-agonists) and a low potential for drug interactions. The broad anti-inflammatory properties of desloratadine and mizolastine, which distinguish these agents from other H(1) antagonists in clinical development (e.g., norastemizole and levocetirizine), suggest they may have a more profound impact on the underlying disease in patients suffering from different forms of allergy. The lack of clinical efficacy and safety data on rupatadine and HSR-609, both novel H(1) antagonists, precludes an accurate assessment of their potential for treating allergic disease. Epinastine and efletirizine are being developed exclusively for topical application and are unlikely to play a significant role in the management of allergic diseases as a whole.
 ...
PMID:Antihistamines in late-phase clinical development for allergic disease. 1182 15

Desloratadine, a potent, once-daily, orally active, nonsedating, histamine H1-receptor antagonist, inhibits the release of histamine and other inflammatory mediators. Once-daily desloratadine therapy rapidly reduces the symptoms of perennial allergic rhinitis and seasonal allergic rhinitis (SAR), reduces the use of inhaled albuterol by patients with SAR and concomitant asthma, and improves symptoms and quality of life in patients with chronic idiopathic urticaria. An open-label, observational study in SAR patients revealed that desloratadine therapy significantly reduced nasal, ocular, dermal, asthma, and total symptoms, and enabled half of the patients with concomitant asthma to reduce their use of asthma medications. Globally, more than 91% of patients and physicians judged desloratadine to have excellent or good efficacy, and more than 98% judged it to have excellent or good tolerability. Furthermore, desloratadine therapy improved quality of life, decreasing by more than 10-fold the percentage of patients whose daily activities and/or sleep were moderately or severely affected by SAR. Allergic rhinitis, a major chronic airway disease that is a risk factor for asthma, warrants extended diagnostic procedures and well-tolerated therapy that encompasses the entire airway, addresses multiple steps in the allergic inflammatory cascade, and is effective on nasal, ocular, dermal, asthma, and total symptoms.
 ...
PMID:Therapeutic points of intervention and clinical implications: role of desloratadine. 1249 24

Urticaria is defined by weals (hives), with or without angioedema, that appear and peak in minutes to hours, usually disappear within 24 h, and are accompanied by pruritus that worsens during the night. Urticaria is caused by cutaneous mast cell degranulation, attributed to immunological, nonimmunological, and idiopathic causes. Chronic idiopathic urticaria (CIU) is the diagnosis when the pathophysiological mechanism of persistent urticaria remains unclear; up to half of patients with CIU have functional autoantibodies directed against the high-affinity receptor for IgE (FcepsilonRI) or against IgE itself, which appear to induce mast cell degranulation. Systemic histamine H1-receptor antagonists, such as desloratadine, are central to the management of CIU. The efficacy and safety of desloratadine, 5 mg once daily, was studied in a double-blind, randomized, placebo-controlled, multicentre trial that included 190 patients, ages 12 and above, with at least a 6-week history of CIU and experiencing a flare of at least moderate severity. Desloratadine was superior to placebo in controlling pruritus and total symptoms after the first dose, and its superiority was maintained throughout the full 6 weeks of the study. Measures of sleep, daily activity, therapeutic response, and global CIU status were also significantly improved with desloratadine after the first dose and maintained throughout the study.
 ...
PMID:Chronic urticaria: impact of allergic inflammation. 1249 25

Our understanding of the pathophysiology of allergy has moved to the molecular level, while study of epidemiology and genetics has revealed risks of developing allergies based on environmental and genetic profiles, and pharmacoeconomic data have enabled accurate measurement of the immense burden of allergic disease. These advances in allergy research have affected its management, particularly the search for new antiallergy therapies. New therapies should intervene in the systemic allergy inflammatory cascade and provide clinical efficacy that extends to multiple allergic disease states. In addition, these new therapies should present no additional safety issues, offer improvements over existing therapies, and have an impact on disease-impaired quality of life. In vitro studies show that desloratadine, a new, once-daily, nonsedating, selective histamine H1-receptor antagonist, blocks the systemic allergy cascade at multiple points. Desloratadine 5 mg once daily relieves the symptoms of chronic idiopathic urticaria and of both seasonal (SAR) and perennial allergic rhinitis. In patients with concomitant asthma and SAR, asthma symptoms are relieved and beta2-agonist medication use is decreased by desloratadine. Unlike many other second-generation histamine H1-receptor antagonists, desloratadine provides the added benefit of efficacy against nasal obstruction in SAR. Desloratadine improves quality of life by decreasing the impact of allergic symptoms on sleep and on daily activities.
 ...
PMID:Advances in allergy management. 1249 27

Desloratadine, the active metabolite of loratadine, is a new antihistamine. Because of its anti allergy properties, desloratidine has an affinity for histamine receptors 25 to 100 times greater to those of the usual antihistamines, coupled with a capacity to inhibit the production of pro-inflammatory mediators. When evaluated in healthy volunteers, the half life of desloratadine has been estimated at 27 hours, which is comparable with a night time length of action. Many clinical studies made with patients suffering with allergic rhinitis or chronic idiopathic urticaria have shown a rapid symptom reduction, lasting 24 hours after first taking. This action was correlated with an improvement in socio-professional activity, sleep and quality of life in general. In patients suffering from allergic rhinitis, rhinomanometry showed a significant improvement in nasal congestion by desloratadine. The clinical advantages of desloratadine on antihistamines taken previously were measured in a study made on almost 48,000 patients, of whom 91% found its efficacity satisfactory. By its powerful action, coupled with an excellent tolerance profile, desloratadine represents a real therapeutic advance for allergic patients.
 ...
PMID:[The place of new antihistamines in allergy management. Apropos of desloratadine]. 1257 24

A new competitive histamine H(1)-receptor antagonist with superior binding affinity at this receptor as compared with other common antihistamines, desloratadine is the active metabolite of loratadine, the most extensively used agent of this class. Under development for the treatment of allergic rhinitis and urticaria and currently awaiting regulatory approval in the United States, desloratadine was recently approved and became commercially available in Europe for the treatment of allergic disease. Desloratadine is at least 50-fold more potent in vitro and appears to be 10-fold more potent in vivo than loratadine. The new antihistamine is metabolized to 3-hydroxydesloratadine, which retains biological activity. Absorption of orally administered desloratadine is dose proportional, and desloratadine achieves steady-state concentrations after approximately 5 doses with once-daily administration. This is consistent with mean half-life values of 24-27 h and a 24-h dosing interval. The absorption of desloratadine is not affected by food and there are no clinically relevant drug-drug interactions. In randomized, double-blind, placebo-controlled clinical trials, a single 5 mg dose of desloratadine conferred significant relief of seasonal allergic rhinitis (SAR) symptoms - including the complaint of nasal congestion - within hours of the first dose, and these effects were sustained both for the entire 24-h dosing interval and up to 2-4 weeks with once-daily treatment (5 mg/day). In addition, patients with seasonal exacerbations of mild to moderate asthma derived similar clinical benefits from desloratadine, with significant, first-dose relief of both SAR-related complaints such as nasal congestion as well as asthma symptoms. In addition, beta(2) agonist requirements for symptom management were significantly reduced from baseline in these asthma patients when treated with the 5 mg/day desloratadine regimen as compared with placebo. Also experiencing marked relief of symptoms upon treatment with desloratadine were patients with chronic idiopathic urticaria, who exhibited significant first-dose relief of pruritus and sustained reductions in this symptom, numbers of lesions (and size of largest hive) and sleep disturbances, with a marked improvement in their ability to carry out activities of daily living. The clinical benefits of desloratadine in the above clinical settings were accompanied by general improvements in quality of life. Desloratadine does not cross the blood-brain barrier, as demonstrated by both human studies using cognitive indices as well as work in animal models. Desloratadine is well tolerated, and no significant drug-related (or food-related) adverse effects were noted when the agent was administered together with cytochrome P450 inhibitors (e.g., ketoconazole, erythromycin). Administration of desloratadine has not been shown to cause any significant changes in cardiac activity at therapeutic doses, even at 9-fold higher doses, or in the presence of P450 inhibitors. Nor does administration of desloratadine lead to sedation, even in the presence of alcohol. (c) 2001 Prous Science. All rights reserved.
 ...
PMID:Desloratadine: A preclinical and clinical overview. 1276 22

Chronic idiopathic urticaria (CIU) manifests as frequently occurring, short-lived wheals, surrounded by a bright-red flare, and often accompanied by angioedema. The cause of CIU is undefined and its diagnosis requires exclusion of other conditions with somewhat similar symptoms. Recent evidence has indicated that IgG autoantibodies directed against high-affinity IgE receptors (FcepsilonRI) may be involved in the pathophysiology of CIU. Following the release of mast cell or basophil-derived histamine, this mediator binds to H(1) and H(2) receptors, leading to vasodilatation and increased vascular permeability. Individuals with CIU may be unable to conduct normal daily activities; therefore, prompt initiation of effective treatment is essential. General management of patients should include avoidance of substances likely to trigger or intensify episodes. Treatment with antihistamines is the mainstay of pharmacotherapy for CIU. Selection of antihistamine therapy for patients with CIU should be based on the following key properties: (1) proven clinical efficacy in providing a high rate of symptom improvement, (2) rapid onset of action and a long-lasting response, and (3) an excellent safety profile and a high degree of tolerability. The benefit of some second-generation antihistamines is limited by sedation, drug-drug interactions, or a variable therapeutic response. The H(1)-receptor antagonist desloratadine is a new, once-daily treatment option that is potent and nonsedating, and has a low potential for drug-drug interactions. Desloratadine has a rapid onset of action and has been shown to effectively and safely reduce pruritus and the number and size of hives in patients with CIU, leading to improvements in quality of life.
 ...
PMID:Chronic idiopathic urticaria for the generalist. 1279 12

Desloratadine is a once-daily, non-sedating, non-impairing, selective histamine H1-receptor antagonist. It relieves the symptoms of seasonal allergic rhinitis (including nasal obstruction and congestion, and morning symptoms), perennial allergic rhinitis and chronic idiopathic urticaria by blocking multiple critical steps in the systemic allergic cascade and downregulating key allergy-induced inflammatory mediators. It also relieves asthma symptoms and decreases rescue medication use in patients with seasonal allergic rhinitis and comorbid asthma. Numerous clinical studies have demonstrated that desloratadine is safe, well tolerated and free of serious cardiac effects. Pharmacokinetic studies have demonstrated a low propensity for drug-drug or drug-food interactions. This review outlines the mechanism of action, efficacy and safety of desloratadine for the treatment of allergic inflammatory disorders.
 ...
PMID:Review of desloratadine for the treatment of allergic rhinitis, chronic idiopathic urticaria and allergic inflammatory disorders. 1625 82

Allergic disease is an increasing problem worldwide. Allergic rhinitis, an inflammatory response to an allergen, affects an estimated 20-40 million people in the US, while chronic idiopathic urticaria is a dermatoallergic condition that affects 0.1-3% of people in the US and Europe. The primary goals of treatment for allergic rhinitis are to reduce symptoms, which include sneezing, rhinorrhoea and nasal congestion, improve quality of life and prevent the sequelae associated with this disease, while the goal for chronic idiopathic urticaria is the rapid and prolonged control of symptoms. Quantitatively, histamine is the most abundant mediator present during an allergic episode - thus, antihistamines (historically called histamine H(1) receptor antagonists, now called H(1) receptor inverse agonists) are a first-line defense against allergic rhinitis and chronic idiopathic urticaria. Although first-generation antihistamines can cause sedation and cognitive impairment, second-generation antihistamines are relatively non-sedating and free of such adverse events owing to their comparative inability to penetrate the blood-brain barrier. Desloratadine is one such second-generation antihistamine and is indicated for the treatment of allergic diseases, including allergic rhinitis and chronic idiopathic urticaria. It has proven efficacy against the symptoms associated with seasonal and perennial allergic rhinitis, including nasal congestion, and chronic idiopathic urticaria. As a result, it has been shown to improve patients' quality of life. The safety and efficacy profiles of desloratadine are well established, and published postmarketing analyses have assessed >54 000 patients. Although earlier second-generation antihistamines have been associated with cardiovascular adverse effects, desloratadine has been shown to be safe and well tolerated at nine times the recommended dose. In addition, it has been shown to not interact with concomitantly administered drugs and food. Overall, current data indicate that desloratadine is a safe and effective treatment for allergic diseases.
 ...
PMID:The safety and efficacy of desloratadine for the management of allergic disease. 1632 13


<< Previous 1 2 3 Next >>