acrivastine and Urticaria

The new H1 antihistamines are a major therapeutic advancement in the treatment of allergic disorders such as urticaria and allergic rhinitis. Their efficacy combined with greatly reduced sedating and anticholinergic side effects makes the new class of H1 antihistamines the first-line treatment in the management of urticaria and mild angioedema. The choice of a particular low-sedating H1 antihistamine depends on pharmacokinetic considerations, the severity of the problem (systemic steroids and epinephrine are the first-line treatment for severe angioedema), and the requirement for limiting the frequency of administration. The efficacy of the new H1 antihistamines in the treatment of itch due to atopic eczema and systemic disease remains uncertain, and further controlled clinical trials are needed to elucidate their possible role in these conditions.

Topics: Astemizole; Cetirizine; Dermatitis, Atopic; Histamine H1 Antagonists; Humans; Loratadine; Terfenadine; Triprolidine; Urticaria

Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine was more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine was superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine caused less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine. Thus, acrivastine is an effective addition to drugs currently available for the treatment of patients with allergic diseases in whom a histamine H1-receptor antagonist is indicated. Because of its rapid onset of action acrivastine will be particularly useful for 'on demand' therapy in patients with intermittent symptoms.

Topics: Dermatitis, Atopic; Histamine H1 Antagonists; Humans; Rhinitis, Allergic, Seasonal; Triprolidine; Urticaria

Topics: Cetirizine; Cyproheptadine; Histamine H1 Antagonists; Humans; Hydroxyzine; Loratadine; Rhinitis, Allergic, Seasonal; Triprolidine; Urticaria

The general human and skin pharmacology of acrivastine, its clinical utility and some important concepts of the use of H1-antihistamines in dermatology are discussed. The drug has potent H1-antihistamic activity yet a low sedative profile as compared with first generation agents. Acrivastine is rapidly absorbed with peak inhibition of flare areas occurring at 90 min and peak activity against weals at 120 min after drug administration. No accumulation of the drug following multiple dosing has been demonstrated. Due to these effects the drug has a high level of patient acceptability and a high level of useful activity in a range of histamine-mediated dermatoses.

Topics: Histamine H1 Antagonists; Histamine Release; Humans; Pyridines; Triprolidine; Urticaria

Leukotriene receptor antagonists have shown some efficacy in t he treatment of asthma. Injection of LTC4, LTD4 and LTE4 into the skin leads to a weal-and-flare reaction, suggesting an involvement of leukotrienes in the pathogenesis of urticaria. Indeed, various reports have indicated a beneficial effect for leukotriene receptor antagonists in patients with chronic urticaria.. To determine the therapeutic effect of the leukotriene receptor antagonist zafirlukast in patients with chronic urticaria.. The study was a double-blind, placebo-controlled, cross-over study lasting for 12 weeks. Fifty-two patients with chronic urticaria were investigated at a university hospital. The patients were randomized to receive 20 mg zafirlukast b.i.d. or placebo and cross-over was scheduled after 6 weeks. The efficacy of the treatment was evaluated by a daily symptom score, six physical examinations, the requirement of rescue antihistamines (acrivastine) and an overall assessment by the patient andthe investigating physician.. Forty-six patients completed the study: zafirlukast was well tolerated without alteration of the investigated laboratory parameters. In comparison with placebo, treatment with zafirlukast resulted in no significant positive effect for any of the efficacy measures. Moreover, we were unable to identify any subgroup of patients with chronic urticaria responding with a therapeutic benefit.. The leukotriene receptor antagonist zafirlukast does not provide a significant therapeutic benefit at a dose of 20 mg b.i.d. in patients with chronic urticaria.

Topics: Adolescent; Adult; Aged; Chronic Disease; Cross-Over Studies; Double-Blind Method; Drug Administration Schedule; Female; Histamine H1 Antagonists; Humans; Indoles; Leukotriene Antagonists; Male; Middle Aged; Phenylcarbamates; Sulfonamides; Tosyl Compounds; Treatment Outcome; Triprolidine; Urticaria

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 were compared in 60 healthy volunteers. The wheal and flare responses were produced by prick test using 1% histamine solution. Measurements were performed before the ingestion of antihistamines (baseline values) and afterwards at 15, 30, 90, 240, 360 min and 24 h. The values obtained for each antihistamine were compared with each other and with baseline values. Cetirizine was found to be superior to acrivastine and loratadine for the suppression of wheal and flare responses at 240, 360 min and 24 h (P < 0.05) and acrivastine was superior to the other two antihistamines for the suppression of flare response at 30 min (P < 0.05). Our results indicate that a single dose of cetirizine provides a more effective and long acting suppression on wheal and flare reactions in urticaria when compared to acrivastine and loratadine.

Topics: Adult; Cetirizine; Cross-Over Studies; Female; Histamine; Histamine H1 Antagonists; Humans; Loratadine; Male; Middle Aged; Single-Blind Method; Triprolidine; Urticaria

The purpose of this study was to assess the time of onset of action of acrivastine in suppressing the wheal response to histamine (10 mg/ml) and allergen (10,000 and 100,000 BU/ml) in the skin prick test. Ten subjects with a well-documented allergy to pollen received single doses of 8 mg of acrivastine and placebo according to a randomized, double-blind, placebo-controlled, crossover treatment design. Duplicate skin prick tests were performed 0, 15, 20, 25, 30, and 60 min after medication. The results demonstrated a statistically significant suppression of the wheal reactions 15-20 min after medication, depending on the reaction producers used. The sum of all three producers showed a statistically significant effect on the wheal reaction 15 min after medication. The upper 95% confidence limit for time lag from dosing of acrivastine until reduction from placebo level commences was 6.5 min. The study substantiates that orally administered acrivastine has a rapid onset of action in the skin of allergic subjects. The results indicate that allergen SPT is a more sensitive tool for studying antihistaminergic activity than histamine SPT.

Topics: Administration, Oral; Adult; Allergens; Confidence Intervals; Double-Blind Method; Female; Histamine; Histamine H1 Antagonists; Humans; Male; Middle Aged; Pollen; Skin Tests; Time Factors; Triprolidine; Urticaria

Acrivastine is a short acting histamine H1-receptor antagonist with a rapid onset of action. Double-blind clinical trials have shown acrivastine (usually 8mg three times daily) to be an effective and well tolerated antihistamine in the treatment of chronic urticaria and allergic rhinitis. Acrivastine was more effective than placebo and similar in efficacy to clemastine or terfenadine in the treatment of seasonal allergic rhinitis. In the treatment of dermatoses in which histamine has a pathogenetic role, the efficacy of acrivastine was superior to that of placebo and similar to that of usual dosages of clemastine, hydroxyzine, chlorpheniramine, cyproheptadine or terfenadine. Acrivastine caused less drowsiness than clemastine, the incidence of adverse effects being indistinguishable from that with placebo or terfenadine. Thus, acrivastine is an effective addition to drugs currently available for the treatment of patients with allergic diseases in whom a histamine H1-receptor antagonist is indicated. Because of its rapid onset of action acrivastine will be particularly useful for 'on demand' therapy in patients with intermittent symptoms.

Topics: Dermatitis, Atopic; Histamine H1 Antagonists; Humans; Rhinitis, Allergic, Seasonal; Triprolidine; Urticaria

A total of 21 patients with a diagnosis of chronic idiopathic urticaria were assessed in a fully randomized, double-blind, crossover study to investigate the efficacy of 8 mg acrivastine versus 20 mg hydroxyzine and placebo administered three times daily. Both acrivastine and hydroxyzine were found to be effective, and significantly better than placebo, in controlling signs and symptoms of urticaria. No significant differences were found between the active preparations. Hydroxyzine was associated with significantly more reports of drowsiness than was placebo.

Topics: Adult; Chronic Disease; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Hydroxyzine; Male; Placebos; Pyridines; Triprolidine; Urticaria

Patients (n = 56) with a diagnosis of chronic idiopathic urticaria were assessed in a fully randomized, double-blind, crossover study to investigate the efficacy of acrivastine at two doses (8 and 4 mg) versus 60 mg terfenadine and placebo administered three times daily. All three active preparations were found to be effective, and significantly better than placebo, in controlling the signs and symptoms of urticaria. No significant differences were found between the active preparations, although in some cases efficacy trends favoured 8 mg acrivastine and terfenadine over 4 mg acrivastine. No significant differences were noted between the active treatments and placebo with regard to reports of drowsiness.

Topics: Adult; Benzhydryl Compounds; Chronic Disease; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Placebos; Pyridines; Terfenadine; Triprolidine; Urticaria

Twenty patients of mean age 41.3 years, with a diagnosis of chronic idiopathic urticaria were assessed in a fully randomized, double-blind, crossover study to investigate the efficacy of acrivastine at two doses (8 mg and 4 mg) versus 1 mg clemastine and placebo, given three times per day. All active preparations were found to be effective, and significantly better than placebo, in controlling the signs and symptoms of urticaria. There was a higher incidence of sedation with clemastine than with either acrivastine or placebo, although this difference did not achieve statistical significance in this small study.

Topics: Adult; Chronic Disease; Clemastine; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Placebos; Pyridines; Pyrrolidines; Random Allocation; Triprolidine; Urticaria

A total of 20 patients with a diagnosis of chronic idiopathic urticaria were entered into a fully randomized, double-blind, crossover study to investigate the efficacy of 8 mg acrivastine versus 4 mg chlorpheniramine three times daily. Data from 16 patients were available for analysis. Both acrivastine and chlorpheniramine were found to be effective in relieving the signs and symptoms of urticaria. There were no significant differences between the two treatments, although efficacy trends were generally in favour of acrivastine over chlorpheniramine throughout the study.

Topics: Adult; Chlorpheniramine; Chronic Disease; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Pyridines; Random Allocation; Triprolidine; Urticaria

Twenty-four healthy volunteers were entered into a double-blind, crossover study conducted to establish the time of onset of action and the time to peak activity of acrivastine in suppressing the weal and flare responses to intradermally injected histamine. Volunteers received single doses of 8 mg acrivastine and placebo according to a fully randomized, balanced treatment plan. Acrivastine significantly (P less than 0.001) reduced both the weal and flare responses induced by histamine challenge 30 min after oral dosing, as compared with placebo. Peak inhibition of the flare response was seen at 90 min, and maximal suppression of the weal response occurred at 120 min after administration of acrivastine.

Topics: Clinical Trials as Topic; Double-Blind Method; Histamine; Histamine H1 Antagonists; Humans; Pyridines; Random Allocation; Triprolidine; Urticaria

Twelve patients with symptomatic dermographism were entered into a double-blind, crossover study. Patients received 8 mg acrivastine three times daily, 60 mg terfenadine three times daily or placebo, according to a fully randomized balanced treatment plan. Subjective clinical assessments were performed and the response to experimentally induced dermographism was assessed. Both active treatments were well tolerated and were shown to be significantly more effective than placebo in the treatment of symptomatic dermographism and in reducing the signs and symptoms of wealing induced by a dermographometer.

Topics: Adult; Benzhydryl Compounds; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Pyridines; Random Allocation; Terfenadine; Triprolidine; Urticaria

Ten patients with cholinergic urticaria (CU) were entered into a double-blind, placebo-controlled, cross-over study. They were scheduled to receive acrivastine 8 mg t.d.s., hydroxyzine hydrochloride 20 mg t.d.s. and placebo according to a fully randomized, balanced treatment plan. Subjective clinical assessments and objective measurements following exercise challenge were performed during the study period. Both acrivastine and hydroxyzine were shown to be effective and well tolerated in the treatment of cholinergic urticaria. In addition, a trend was demonstrated for both active agents to improve peak expiratory flow rate (PEFR) following exercise, when compared with placebo, and this trend reached statistical significance in the case of acrivastine (p less than 0.05).

Topics: Adult; Aged; Clinical Trials as Topic; Double-Blind Method; Drug Evaluation; Exercise; Female; Histamine H1 Antagonists; Humans; Hydroxyzine; Male; Middle Aged; Peak Expiratory Flow Rate; Placebos; Pyridines; Triprolidine; Urticaria

A double-blind, crossover trial with a new triprolidine derivative, acrivastine (BW 825C; 8 mg 3 times daily), cyproheptadine (4 mg 3 times daily) and placebo was carried out in 18 patients suffering from idiopathic cold urticaria. Acrivastine and cyproheptadine significantly (p less than 0.01) reduced weal areas following ice cube challenge when compared to placebo. Acrivastine was found to be significantly more effective (p less than 0.01) than cyproheptadine in reducing weal areas. Furthermore, cyproheptadine caused significantly more drowsiness than acrivastine (p = 0.021) or placebo (p = 0.013), which did not differ from each other. This study shows that acrivastine is an effective agent in the treatment of cold urticaria and suggests that acrivastine in the dose used lacks adverse effects, such as drowsiness, traditionally associated with antihistamine therapy.

Topics: Adult; Clinical Trials as Topic; Cold Temperature; Cyproheptadine; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Placebos; Pyridines; Random Allocation; Sleep Stages; Triprolidine; Urticaria

Topics: Adolescent; Adult; Aged; Chronic Disease; Clemastine; Clinical Trials as Topic; Double-Blind Method; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Pyridines; Pyrrolidines; Random Allocation; Triprolidine; Urticaria

20 patients with a diagnosis of chronic idiopathic urticaria were entered into a double-blind placebo-controlled cross-over study. All patients completed the trial and during the assessment period they were treated with placebo, BW 825C (4 mg) and BW 825C (8 mg) according to a fully randomised and balanced treatment plan. Both doses of BW 825C were found to be highly effective and significantly better than placebo in controlling signs and symptoms of urticaria. Few adverse reactions were reported and in this small group of patients there was no significant difference from placebo in reports of drowsiness or any other side-effects.

Topics: Adult; Aged; Chronic Disease; Clinical Trials as Topic; Female; Histamine H1 Antagonists; Humans; Male; Middle Aged; Pyridines; Random Allocation; Sleep Stages; Triprolidine; Urticaria