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

For three decades, traditional H1 antihistamines have been used in the treatment of allergic diseases. They are effective in reducing histamine-related symptoms, but the use of such agents has been limited by sedation and anticholinergic side effects. These adverse effects are fewer with the recently introduced H1 antihistamines. One of these, cetirizine, a human metabolite of hydroxyzine, is characterized by its high selectivity for the H1 receptor site and its reliable and consistent inhibition of histamine-induced allergic reactions. It also blocks eosinophil infiltration to the site of allergen-induced cutaneous reactions. Cetirizine has proved effective in the treatment of seasonal and perennial allergic rhinitis and urticaria. It is excreted primarily by renal mechanisms. It is well tolerated by elderly patients. Cetirizine has a low rate of penetration of the blood-brain barrier, and it has minimal central nervous system impairment. Furthermore, it can be given once a day. Cetirizine's low incidence of sedation and anticholinergic side effects contribute to its high profile of safety. In this article the characteristics, pharmacology, pharmacokinetics, and mode of action of cetirizine are reviewed.
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PMID:Cetirizine: antiallergic therapy beyond traditional H1 antihistamines. 197

Cetirizine, a piperazine derivative and carboxylated metabolite of hydroxyzine, is a potent histamine H1-receptor antagonist with antiallergic properties. It has marked affinity for peripheral histamine H1-receptors and, at the standard dose of 10mg daily, lacks the CNS depressant effects of standard antihistamines. In addition, it inhibits histamine release and eosinophil chemotaxis during the secondary phase of the allergic response. Results from controlled clinical trials indicate that cetirizine is an effective and well tolerated treatment of seasonal and perennial allergic rhinitis and chronic idiopathic urticaria. Cetirizine appears to be as effective as conventional dosages of terfenadine, chlorpheniramine and hydroxyzine in relieving symptoms associated with these disorders and produces a markedly lower incidence of sedation than chlorpheniramine, hydroxyzine and several other standard antihistamines. Thus, cetirizine appears to provide a useful alternative to other 'nonsedating' antihistamines; cetirizine may also have a future role in the treatment of allergic asthma and certain forms of physical urticaria.
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PMID:Cetirizine. A review of its pharmacological properties and clinical potential in allergic rhinitis, pollen-induced asthma, and chronic urticaria. 198 54

Cetirizine is a new anti-allergic compound with a potent, long-acting, and specific antihistaminic property. Strongly active in the therapy of urticaria and seasonal or perennial rhinitis, it has been shown to inhibit the in vivo eosinophil attraction at skin sites challenged with allergen in atopic patients. In the present work, we confirmed that, at a therapeutical concentration, this molecule had a potent inhibitory action in vitro on eosinophil chemotaxis induced either by N-formyl-Met-Leu-Phe or platelet-activating factor and also on the IgE-dependent stimulation of platelets. These observations appear in favour of a possible role for cetirizine in the modulation of inflammatory cell interactions in allergic processes.
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PMID:Inhibition of human eosinophil chemotaxis and of the IgE-dependent stimulation of human blood platelets by cetirizine. 252 57

Urticaria is a rather common, often vexing skin disease, characterized by evanescent, pruritic, erythematous wheals, and sometimes by giant hives (angioedema). The cause of chronic urticaria remains unknown in 75 to 80 percent of the cases. Its pathogenesis is related to the activation of tissue mast cells by many immunologic or non-immunologic mechanisms, resulting in a release of biologically active products. The therapeutic possibilities in practice are discussed. Non-sedative antihistaminic drugs of the H1 type (Terfenadine, Astemizole, Loratidine and Cetirizine) are the main stay in the treatment of urticaria. In case of failure the sedative non-selective antihistaminics from the old generation are used. Particular emphasis is given the possibilities to combining various antiallergic drugs. The combination of a H1 and H1 antihistamine can be effective in individual patients.
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PMID:[Therapy of acute and chronic urticaria and of Quincke's edema]. 256 13

The efficacy of cetirizine dihydrochloride, a new H1-antagonist with minimal sedative or anticholinergic side effects was evaluated in 30 patients with chronic idiopathic urticaria. In the first part of the study, cetirizine 10 mg and placebo were compared in a double-blind cross-over trial. In the second part, patients who did not respond adequately in the first part were randomized, still double-blind, to receive 10 mg cetirizine either once daily or twice daily. In the first part, treatment was discontinued by 17 patients on placebo and two patients on cetirizine because of lack of efficacy. Cetirizine dihydrochloride was found significantly to reduce occurrence of weals, erythema and pruritus compared with placebo (P less than 0.001). Twenty-six of the patients improved on cetirizine and two on placebo. Mild sedation was noted by two patients on cetirizine and by one on placebo.
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PMID:Treatment of chronic urticaria with cetirizine dihydrochloride a non-sedating antihistamine. 290 Jun 48

Cetirizine, the carboxylated metabolite of hydroxyzine, is a specific and long-acting histamine H1-receptor antagonist. It has marked antiallergic properties and inhibits eosinophil chemotaxis during the allergic response. Clinical trial results indicate that cetirizine is an effective and well tolerated treatment for seasonal/perennial allergic rhinitis and chronic idiopathic urticaria in adults, and for seasonal/perennial allergic rhinitis in children. Cetirizine 10 mg/day appears to be as effective as conventional dosages of other established antihistamines such as astemizole, hydroxyzine, ketotifen, loratadine or terfenadine in relieving symptoms of these disorders, and is associated with a significantly lower incidence of sedation than hydroxyzine. However, when sedation was subjectively assessed, cetirizine appeared to be more sedating than placebo, loratadine or terfenadine in some clinical trials. This difference was not observed in several other double-blind studies. In contrast, when assessed objectively in pharmacodynamic comparisons, cetirizine was rarely more sedating than placebo or other second generation histamine H1-receptor antagonists. Cetirizine may also have a role in the treatment of certain forms of physical urticaria, atopic dermatitis and reactions to mosquito bites. In addition, it is being studied for the treatment of allergic asthma in adults and children. The pharmacokinetic profile and predominantly renal excretion of cetirizine suggest that this agent may have a reduced potential for adverse drug interactions involving hepatic enzyme systems compared with other histamine H1-receptor antagonists which are extensively metabolised. Thus, cetirizine, with its rapid onset and long duration of action, appears to provide a useful alternative to the antihistamine agents in clinical use.
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PMID:Cetirizine. A reappraisal of its pharmacological properties and therapeutic use in selected allergic disorders. 751 Jun 11

The effect of cetirizine, 10 mg at night, on dermographic urticaria, was studied in 19 patients. The study design was a randomized, double-blind, crossover comparison with placebo, each treatment being given for 7 days. Patients kept a daily diary of itch and weal severity (100-mm linear analogue scale), and recorded sleep disturbance. The dermographic weal response was measured objectively with a spring-loaded stylus, and the weal threshold calculated from the force/response curve. There was a small, insignificant subjective response to placebo, but no objective response. On cetirizine, the subjective assessment of wealing was reduced from 34.3 +/- 6.7 (mean +/- SEM, 0-100 scale) to 16.8 +/- 4.1 (P = 0.02), itch was reduced from 43.2 +/- 6.6 to 19.4 +/- 4.1 (P = 0.001), and nights disturbed from 46.2 to 8.8% (P = 0.03). There was a shift to the right in the position of the force/response curve, and the wealing threshold increased from 24.6 +/- 3.2 to 54.7 +/- 4.4 g/mm2 (P = 0.00001), but there was no correlation between change in itch scores and wealing threshold. Cetirizine 10 mg daily is an effective treatment in dermographic urticaria, and its usefulness will depend on the prevalence of unwanted effects.
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PMID:The effect of cetirizine on symptoms and wealing in dermographic urticaria. 825 55

In a 20-d, double-blind, randomized, parallel study, the efficacy of cetirizine and terfenadine was compared in 30 patients with chronic idiopathic urticaria. Subjects were randomly divided into two 15-patient groups. The first group was given cetirizine (10 mg once daily); the second terfenadine (60 mg twice daily). Cetirizine proved to be more effective than terfenadine in controlling urticaria symptoms. In fact, the score of the investigators' overall assessment was significantly lower in the cetirizine-treated group than in the terfenadine-treated group. Moreover, patient evaluation by a visual analog scale and symptoms assessed on a 4-point scale showed a better improvement in the cetirizine group. The number and severity of side-effects were similar in both treatment groups.
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PMID:A comparison of the efficacy of cetirizine and terfenadine. A double-blind, controlled study of chronic idiopathic urticaria. 836 64

Cetirizine (once daily), a highly selective H1-antagonist, is efficacious for treating seasonal allergic rhinitis (SAR), perennial allergic rhinitis, and chronic idiopathic urticaria. A 4-week, randomized, double-blind, placebo-controlled trial investigated the safety and efficacy of cetirizine syrup (5 or 10 mg daily) in 209 children ages 6 to 11 years with SAR. Parents assisted patients in recording symptom severity (sneezing, nasal discharge, itchy eyes, itchy nose or mouth, conjunctivitis, nasal congestion) daily. A total symptom severity (TSS) score was derived from all symptoms, excluding nasal congestion. At baseline, TSS was comparable for all groups (range 6.8-7.0). Cetirizine 10 mg produced a significantly greater mean TSS reduction (3.2) than placebo (P < 0.05) over the treatment period. Cetirizine 5 mg once daily produced mean reductions in weekly symptom scores of 2.4; this did not differ statistically from placebo. Furthermore, cetirizine 10 mg significantly improved symptoms of itchy eyes, nose, or mouth. The most commonly reported adverse reactions to both cetirizine and placebo were headache, pharyngitis, and abdominal pain, which did not occur with an incidence statistically different from that of placebo. Once-daily cetirizine is safe for treating SAR in children ages 6-11 years. Once-daily cetirizine 10 mg provides effective improvement in symptoms and is well tolerated.
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PMID:Once-daily cetirizine effective in the treatment of seasonal allergic rhinitis in children aged 6 to 11 years: a randomized, double-blind, placebo-controlled study. 911 92

Itching reflects a distinct quality of cutaneous nociception elicited by chemical or other stimuli to neuronal receptors at the superficial layers of the skin and muco-cutaneous orifices. Although recent experimental studies of the conduction and perception of itch have yielded deeper insight into the physiology of this sensory quality, little is known about the neuromechanisms involved in pruritus accompanying many inflammatory skin diseases, in particular, in atopic eczema. Previous case-control studies of our research group with patients suffering from atopic eczema (AE) revealed significantly diminished itch perception after iontophoretic application of different doses of histamine as well as substance P (i.c. injected). Further experiments using acetylcholine (ACh, i.c.) clearly demonstrated that ACh elicits pruritus instead of pain in patients with AE. The first part of the present review deals with the results of our most recent case-control studies on histamine-induced itch perception in atopics devoid of eczema as well as in patients with urticaria or psoriasis compared to atopics with or without manifest eczema. We demonstrated that both focal itch and perifocal alloknesis (i.e., itch elicited by a slight mechanical, otherwise non-itching stimulus) were significantly reduced in eczema-free atopics yet were normal in non-atopics suffering from urticaria or psoriasis. In further studies using ACh i.c. injected into the uninvolved skin of patients with AE, lichen ruber, psoriasis, type IV contact eczema, or non-specific nummular eczema (n = 10/each group), all the atopics and 6/10 psoriatics felt itch instead of burning pain, but none of the others did. Different doses of vasoactive intestinal peptide (VIP) i.c. applied to the controls and the atopics with or without eczema did not markedly increase the intensity of nociceptive sensations. However, ACh induced pain in the controls, pure pruritus in the atopics with acute eczema, and a 'mixture' of pain and itch in the atopics just free from eczema. Obviously, the quality of sensations evoked by ACh and VIP depends on the inflammatory or non-inflammatory state of the atopic skin. In a placebo-controlled, double blind study on histamine-induced focal itch and alloknesis with healthy subjects (n = 15) using naltrexone (opioid receptor antagonist) and cetirizine (H1-blocking agent), naltrexone was found to significantly reduce both itching and alloknesis. Cetirizine reduced focal itch but failed to influence the alloknesis phenomenon. The wheal and flare reaction was suppressed only by cetirizine. These different effects point to a mainly CNS-based activity of naltrexone but a peripheral level effect of cetirizine. Due to long-lasting experience with group sport as a supporting adjuvant for inpatients with AE, we evaluated, by clinical, psychometric, and physiological studies, the therapeutic efficacy of controlled physical exercise in addition to otherwise equal anti-eczematous therapy for both voluntary participants and non-participants in sports by performing several case-control studies, one followed-up to 6 months after the patients' discharge from the hospital. Regular moderate exercises neither deteriorated nor impeded the recovery from AE, ameliorated the participants' scratch controlling ability and significantly their depressed emotional mood. The non-participants failed to achieve these aims. Sweating-induced itch was inhibited in almost all participants if simple skin care (clearing by warm shower, ointment) and short-term rest were used by informed patients. In conclusion, there are several indications that itching is elicited in individuals inclined to cutaneous atopy, regardless of their eczematous or just eczema-free state, by a different physiological pathway from that in non-atopic individuals. Therefore, antipruritic agents influencing the centrally altered nociception of atopics are needed and may be expected in near future. (ABSTRACT TRUNCATED)
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PMID:Recent studies of cutaneous nociception in atopic and non-atopic subjects. 1009 77


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