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Loratadine and cetirizine significantly improved symptoms (P < 0.002), significantly reduced eosinophil (P < 0.016) and metachromatic cell (P < 0.01) infiltration, levels of ECP (P < 0.002), EPO (P < 0.006) and histamine (P < 0.01) and ICAM-1 expression on nasal epithelial cells (P < 0.02). No difference was demonstrated between the two drugs.
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Levocetirizine 5 mg/day is an effective and well-tolerated treatment of PAR. In addition, levocetirizine is effective for the relief of nasal congestion.
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The most pronounced side effect of antiallergic histaminergic drugs (H1 antagonists) is sedation. These effects have been linked with the effects of histaminergic drugs on central H1 receptors. In the present study, we investigated the dose-response relationship of different antihistamines on the performance in a reaction-time task that has been developed for rats. The dose-response relationship of diphenhydramine, cetirizine and terfenadine were examined for the various behavioural measures in this task (i.e., reaction time, motor time, premature responses and number of trials completed). In addition, the effects of scopolamine were assessed to evaluate the cholinergic profile in this task. Diphenhydramine did not reliably affect the reaction time, but increased the motor time and the proportion of premature responses, and decreased the number of trials completed in a session. A low dose of cetirizine decreased the reaction time, whereas an increase in reaction time was found for the high dose. The motor time was increased after both doses of cetirizine. Terfenadine did not affect the responding of rats in the reaction-time task at the doses tested. The effects of scopolamine were very similar to those of diphenhydramine. The reaction-time task used in this study was able to dissociate different types of antihistamines on aspects of psychomotor function, which were likely to be related to central muscarinic or H1 antagonism. These findings suggest that the reaction-time task may be a sensitive tool for assessing effects of drugs on psychomotor function.
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This was a double-blind, randomized, placebo controlled, three-way cross-over study with a wash-out period of 7 +/- 2 days between each period. The study included 36 healthy volunteers (18--50 years, mean age = 32 years; 9 males). The objective measurement was the cutaneous reactivity to increasing concentrations of histamine (0, 5, 10, 20, 40, 80, 160 mg ml(-1)) administered by prick tests. The reactivity was evaluated by the wheal and flare areas (mm2). The AUC (area under curves) values of the wheal and flare areas as a function of the log2 transformed histamine concentration were calculated for each subject and treatment, and compared.
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Itching is a well known side-effect of opiate therapy. To gain insight into the possible contribution of opiate receptors to itching we compared the antipruritic effect of naltrexone (Nemexin), an opiate antagonist, to an H1-receptor antagonist and to placebo. In a double blind cross-over study on 15 healthy volunteers, 25 mg naltrexone or placebo was orally given 60 min prior to a histamine stimulus. In a second, otherwise identical experiment, 10 mg cetirizine, an H1 blocker, or placebo was orally given 12 h before the experiment to the same group of volunteers. Histamine was applied iontophoretically to the forearm skin and the following parameters were assessed thereafter: weal and flare size, itch intensity and the extension of the area of alloknesis ('itchy skin') around the application site. Naltrexone had no effect on the vascular histamine reactions 'weal' and 'flare', whereas cetirizine abolished the weal reactions and greatly diminished the flare reactions. Both naltrexone and cetirizine significantly diminished histamine induced itching. In contrast to placebo and cetirizine, naltrexone abolished alloknesis completely in four of 15 volunteers and in the others alloknesis was greatly reduced after naltrexone. Since vascular reactions to histamine are of peripheral origin, whereas alloknesis depends on central nervous mechanisms, our findings suggest a pronounced centrally mediated action of naltrexone on histamine induced pruritus.
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Cetirizine with or without albuterol significantly increased FEV1, peak expiratory flow rate, and forced expiratory flow rate between 25% and 75% of vital capacity relative to baseline and placebo but did not have a significant effect on forced vital capacity. The effect of 20 mg of cetirizine on FEV1 was generally greater than that of 10 or 5 mg, but the difference was statistically significant only at the 30-minute time point (p < 0.05). All three cetirizine doses produced significantly greater increases than placebo in FEV1 and forced expiratory flow rate between 25% and 75% of vital capacity for 8 hours and in peak expiratory flow rate for 7 hours (p < 0.02). Albuterol alone had a significant effect on the four pulmonary function variables from 1 to 5 hours after baseline (p < 0.05), which is consistent with albuterol's recommended dosing frequency of every 4 to 6 hours. Albuterol alone increased FEV1 significantly more than 5 mg of cetirizine alone but not 10 mg or 20 mg of cetirizine alone at 60, 90, and 120 minutes after baseline, but all three doses of cetirizine increased FEV1 significantly more than albuterol 7 and 8 hours after baseline (p < 0.05), indicating that the bronchodilatory action of cetirizine lasts longer than that of albuterol. Cetirizine neither potentiated nor inhibited the bronchodilatory action of albuterol, but the two drugs appeared to have an additive bronchodilatory effect. None of the cetirizine treatments caused a worsening of pulmonary function, and all were well tolerated.
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Cetirizine is well established in the treatment of symptoms of SAR, PAR or CIU. It demonstrated a corticosteroid-sparing effect and reduced the relative risk of developing asthma in sensitised infants with atopic dermatitis. Cetirizine was effective in the treatment of allergic cough and mosquito bites; however, its precise role in these indications has yet to be clearly established. On the basis of its favourable efficacy and tolerability profile and rapid onset of action, cetirizine provides an important option for the treatment of a wide range of allergic disorders.
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The aim of the study was to monitor the safety of levocetirizine prescribed in the primary care setting in England, in the immediate postmarketing period.
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Antihistamines are the cornerstone of treatment for many allergic diseases, such as allergic rhinitis and chronic urticaria. Since the discovery of their beneficial effects in the 1940s, scientists have found molecules with greater selectivity to block specific histamine receptors without some of the detrimental side effects that are seen if antihistamines cross the blood-brain barrier. Levocetirizine is the active enantiomer of cetirizine and a selective H(1)-histamine blocker. It exhibits many favourable characteristics of an ideal antihistamine, both pharmacodynamically and pharmacokinetically, including high bioavailability, rapid onset of action, limited distribution and low degree of metabolism. Furthermore, clinical trials indicate that it is safe and effective for the treatment of allergic rhinitis and chronic urticaria with a minimal amount of untoward effects.
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We have therefore designed a double-blind, crossover, placebo-controlled trial, with a 3-week treatment period using either 20 mg/day of cetirizine or placebo.