Ebastine: the effect of a new antihistamine on psychomotor performance and autonomic responses in healthy subjects.

Vincent, John; Sumner, D. J.; Reid, JL

doi:10.1111/j.1365-2125.1988.tb05289.x

Cited by 45 publications

(26 citation statements)

References 26 publications

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“…Thus, RU may show a separation between the therapeutic dose and a dose likely to cause objective CNS impairment. Similar observations have earlier been made with terfenadine [14,18], astemizole [19], cetirizine [42] or ebastine [20]. The reason for the selective action of the therapeutic doses is not clear but may include factors such as lipid solubility or reflect a different mechanism of drug action at the periphery and in the CNS [23].…”

Section: Discussionsupporting

confidence: 63%

“…These side-effects can interfere with the performance of daytime activities and not only place the patient at an increased risk of accidents in situations such as driving and operation of machinery, where high levels of alertness are required [17], but also reduce compliance with treatment regimens due to excessive fatigue and malaise. Clinical trials have consistently demonstrated that the second-generation antihistamines have a much more favourable therapeutic index and a significantly lower incidence of sedative effects than their predecessors and so represent a major advance in antihistamine therapy [18][19][20][21][22].…”

Section: Introductionmentioning

confidence: 99%

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Central and Peripheral Evaluation of Rupatadine, a New Antihistamine/Platelet-Activating Factor Antagonist, at Different Doses in Healthy Volunteers

et al. 2004

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Aims: To assess peripheral anti-H₁ and central nervous system (CNS) activity of single increasing doses of rupatidine fumarate (RU), a new antihistamine/platelet-activating factor antagonist compound, in comparison with hydroxyzine and placebo. Methods: Eighteen healthy young subjects of both sexes took part in a crossover, randomised, double-blind, placebo-controlled study. Treatments tested were: RU 10, 20, 40 and 80 mg and hydroxyzine 25 mg, as a positive standard. Before and several times after drug intake, peripheral anti-H₁ activity was appraised by the skin reactivity to intradermal injection of histamine. CNS effects were also obtained by objective tests of psychomotor performance and subjective mood scales. Results: All active treatments showed a significant reduction of the wheal and flare reaction in relation to placebo, RU displaying a potent dose-dependent inhibition pattern. The global nonparametric Friedman test to changes from placebo in 15 objective variables from psychomotor performance showed a significant impairment of similar magnitude after hydroxyzine 25 mg (p = 0.01) and RU 80 mg (p = 0.02), but this was slower in development and recovery after the latter. After RU 40 mg, a smaller impairment was also obtained (p = 0.04). Activity (p = 0.01) and drowsiness (p = 0.02) scales showed significant changes, the subjects feeling less active and more drowsy after all active treatments. Conclusion: RU presents a potent dose-dependent peripheral anti-H₁ activity, displaying psychomotor impairment activity only at the highest dose (80 mg), while therapeutically relevant lower doses (10 and 20 mg) were similar to placebo.

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Section: Discussionsupporting

confidence: 63%

Section: Introductionmentioning

confidence: 99%

Central and Peripheral Evaluation of Rupatadine, a New Antihistamine/Platelet-Activating Factor Antagonist, at Different Doses in Healthy Volunteers

et al. 2004

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“…The borderline differences were occasionally found between placebo and ebastine, at separate test times or with the times combined, but the real differences were small and the significances partly result from different baseline values or from a statistical aoinflation. They could, however, refer to small concentrations of carebastine in the central nervous system, and since Vincent et al (1988b) reported impaired performance from larger doses of ebastine, it might be preferable to take daily doses in the evening. The effects of diazepam, though not very strong in the present trial, clearly differed from those recorded after placebo and ebastine.…”

Section: Discussionmentioning

confidence: 99%

“…Ebastine is well absorbed and extensively converted to its active carboxylic acid metabolite carebastine during the first pass through the liver. The elimination half-life of carebastine in man is 10 to 16 h (Vincent et al, 1988b); it is moderately accumulated during the treatment with therapeutic doses of ebastine once daily for 1 week, and the local responses to intradermal histamine are suppressed by over 50% for 24 h (Vincent et al, 1988b) with plasma concentrations of carebastine (100 ,ug 1-1) resulting from a daily dose of 20 mg ebastine.…”

Section: Introductionmentioning

confidence: 99%

Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine.

Mattila

Aranko

Kuitunen

1993

Brit J Clinical Pharma

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1 We have given 12 healthy subjects the H1-antihistamine ebastine (20 mg) or placebo in a randomized double-blind and crossover study for 1 week each. The subjects were tested for drug effects on day 6 of each period, and for interactions of ebastine with oral 15 mg diazepam (DZ) on day 7. On both days, the testing runs were at baseline and 1.5, 3, 4.5 and 6 h after intake. 2 The performance was evaluated both objectively (digit symbol substitution, flicker fusion, Maddox wing, simulated driving, body balance) and subjectively (visual analogue scales, questionnaires in the morning were 82 ,ug l-1 on day 6 and 85 ,ug 1-1 on day 7. The rise (+ 150%) in plasma carebastine after an extra 20 mg ebastine was not modified by DZ. Ebastine did not affect performance objectively or subjectively, yet borderline drowsiness was recorded during the first 3 h. On day 7, plasma DZ concentrations peaked (mean 480 ,g 1-1) at 1.5 h after the intake. DZ produced impaired performance in various objective tests, and drowsiness, weakness, clumsiness, mental slowness and poor performance were reported on visual analogue scales. Ebastine neither modified plasma DZ concentrations nor increased DZ effects. 4 We conclude that treatment with 20 mg ebastine once daily for 1 week provides steady concentrations of carebastine in plasma, without impairment of skilled performance or important interactions with diazepam.

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“…The effects of ebastine were generally similar to those of placebo in tests of vigilance, cognitive performance, visual motor coordination, subjective estimates of drowsiness and driving performance (37,(81)(82)(83)(84). In one study, ebastine 10 mg caused a marginally significant increase in choice reaction time compared with placebo at 8 h after a single dose (95% CI for the difference 0.01-0.23), and a dose of 50 mg (2.5 times the maximum recommended dose) caused an increase in this parameter at 4 and 8 h (95% CI for the difference at both timepoints 0.01-0.25) as well as modest increases in indices of sedation (P < 0.05 vs placebo) (81). Neither dose affected critical flicker fusion.…”

Section: Cns Tolerabilitymentioning

confidence: 99%

Ebastine in allergic rhinitis and chronic idiopathic urticaria

Sastre

2008

Allergy

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Histamine is a key mediator in the development of allergy symptoms, and oral H1‐antihistamines are among the most widely used treatments for symptomatic relief in conditions such as allergic rhinitis and chronic urticaria. Ebastine is a second‐generation antihistamine which has been shown to be an effective treatment for both seasonal and perennial allergic rhinitis. In controlled clinical trials in adult and adolescent patients with allergic rhinitis, ebastine 10 mg once‐daily improved symptoms to a significantly greater extent than placebo and to a similar extent as loratadine 10 mg and cetirizine 10 mg (both once‐daily), while ebastine 20 mg proved to be more effective than these two comparator antihistamines. In addition, ebastine was significantly more effective than placebo at relieving the symptoms of chronic idiopathic urticaria. Ebastine provides efficacy throughout the 24‐h dosing interval with once‐daily administration and clinical benefit is seen from the first day of treatment. Small studies have found beneficial effects for ebastine in patients with other disorders, including cold urticaria, dermographic urticaria, atopic asthma, mosquito bites and (in combination with pseudoephedrine) the common cold. In addition to the regular ebastine tablet, a fast‐dissolving tablet (FDT) formulation, which disintegrates in the mouth without the aid of a drink, is also available. It has been shown to be bioequivalent to the regular tablet, and to be significantly more effective than desloratadine at reducing histamine‐induced cutaneous wheals. A number of patient surveys demonstrated that the majority of individuals who tried the fast‐dissolving formulation reported it to be convenient for use, fast‐acting and preferred it to their previous antihistamine medication. Perhaps most importantly, a large proportion of patients indicated that they would prefer to use this new formulation in the future. Ebastine has a rapid onset of action and it can be administered once‐daily, with or without food. Dose modifications are not needed in elderly patients, or in those with renal or mild to moderate hepatic impairment. Ebastine is generally well‐tolerated, and clinical studies showed that at usual therapeutic doses of 10 and 20 mg once‐daily, it had no clinically relevant adverse effects on cognitive function and psychomotor performance or on cardiovascular function. In conclusion, ebastine is an effective and generally well‐tolerated treatment for allergic rhinitis and chronic idiopathic urticaria. In addition to the regular tablet formulation, ebastine is available as a FDT, providing a treatment option that is particularly convenient for patients.

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Ebastine: the effect of a new antihistamine on psychomotor performance and autonomic responses in healthy subjects.

Cited by 45 publications

References 26 publications

Central and Peripheral Evaluation of Rupatadine, a New Antihistamine/Platelet-Activating Factor Antagonist, at Different Doses in Healthy Volunteers

Central and Peripheral Evaluation of Rupatadine, a New Antihistamine/Platelet-Activating Factor Antagonist, at Different Doses in Healthy Volunteers

Diazepam effects on the performance of healthy subjects are not enhanced by treatment with the antihistamine ebastine.

Ebastine in allergic rhinitis and chronic idiopathic urticaria

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