Anti-anaphylactic activity of the non sedative histamime H1 receptor antagonist SL 85.0324 in the rat and guinea pig

Lloyd, K.G.; Levrier, J.; Duval, Danièle; Prouteau, M.; Berry, Catherine; Scatton, B.

doi:10.1016/0014-2999(90)93056-v

Cited by 9 publications

(4 citation statements)

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“…Eighteen healthy, young male volunteers aged between 25 and 33 years [mean (SD) = 28 (2) years], weighing between 55 and 96 kg [79 (10) kg] and between 170 and 191 cm [183 (6) cm] in height were selected. All volunteers were screened during the l 5 days preceding drug administration and underwent a full medical examination, an ECG, routine laboratory tests (including haematology, blood chemistry and urinalysis) in order to confirm that they were normal.…”

Section: Actual Driving Testmentioning

confidence: 99%

“…Key words Mizolastine, Cetirizine, Ethanol interaction; psychomotor performance, antihistamine Mizolastine, a new benzimidazole derivative, is a selective, peripherally acting, histamine H~-receptor antagonist more potent in several animal models of allergy and asthma than astemizole, loratadine or terfenadine, and seems devoid of sedative effects in animals [1,2]. Mizolastine in single doses of 2 mg or more in healthy volunteers has antihistaminic activity (histamine challenge), being most effective at doses of 10 mg upwards [3,4].…”

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confidence: 99%

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Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects

Patat¹,

Stubbs²,

Dunmore³

et al. 1995

Eur J Clin Pharmacol

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The pharmacodynamic interaction between mizolastine, a new H1 antihistamine, and ethanol was assessed in a randomized, double-blind, three-way crossover, placebo-controlled study. Eighteen healthy young male volunteers received mizolastine 10 mg, or cetirizine 10 mg or placebo once daily for 7 days with a 1-week wash-out interval. An oral dose of ethanol or ethanol placebo, given 2 h after dosing on days 5 or 7 of each treatment period, was administered to achieve a peak blood alcohol concentration (BAC) of 0.7 g/l then maintained for 1 h by two further doses of ethanol. Driving ability and psychomotor performance were evaluated using actual and simulated driving tests, critical flicker fusion threshold (CFF), adaptive tracking and divided attention (DAT) tasks. Ethanol produced a significant decrement in all tasks up to 5.5 h after administration: an increase in steering movements of 4.6, in lateral deviation of 0.45 m, in braking reaction time of 80 ms, in driving test and DAT performance of + 3.2; and a decrease in CFF and in tracking speed of 2.6 m.s-1. Neither mizolastine nor cetirizine significantly impaired driving ability or arousal (CFF) compared with the placebo. However, both drugs significantly impaired DAT performance 6:00 h post-dose (increase of + 2.1 for mizolastine and + 2.4 for cetirizine). The tracking speed was significantly decreased 7:50 h after mizolastine administration (-1.3 m.s-1) and more consistently from 1:30 to 7:50 h after cetirizine administration (-1.4 m.s-1). No significant adverse interaction, i.e. potentiation, occurred between ethanol and either antihistamine.(ABSTRACT TRUNCATED AT 250 WORDS)

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Section: Actual Driving Testmentioning

confidence: 99%

mentioning

confidence: 99%

Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects

Patat¹,

Stubbs²,

Dunmore³

et al. 1995

Eur J Clin Pharmacol

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“…The antihistaminic effects occur within 2 h of allergy and asthma than astemizole, loratadine, or and lasts for at least 24 h. Mizolastine, at doses of up terfenadine and seems devoid of sedative effects in to 40 mg, is devoid of anticholinergic effects [6]. animals [1,2]. Mizolastine in single doses of 2 mg or At doses up to 20 mg, it causes no sedation or Correspondence: Dr Alain Patat, Synthelabo Recherche -Clinical Research Department, 31 Avenue Paul Vaillant Couturier, B.P.…”

Section: Introductionmentioning

confidence: 99%

Lack of interaction between a new antihistamine, mizolastine, and lorazepam on psychomotor performance and memory in healthy volunteers.

Patat¹,

Perault²,

Vandel³

et al. 1995

Brit J Clinical Pharma

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1 The possible interaction between ao new H1 antihistamine, mizolastine, and lorazepam was assessed in a randomised, double-blind, cross-over, placebo-controlled study involving 16 healthy young male volunteers who received mizolastine 10 mg or placebo once daily for 8 days with a 1 week wash-out interval. The interaction of mizolastine, at steady-state, with a single oral dose of lorazepam or placebo was assessed on days 6 or 8 of each treatment period. 2 Psychomotor performance and cognitive function were evaluated using objective tests (critical flicker fusion threshold, choice reaction time, tapping, arithmetic calculation, body sway) and self-ratings (visual analogue scale, ARCI) before and at 2, 4, 6 and 8 h after dosing. Short-term memory (Stemnberg memory scanning, immediate free recall of a word list) and long-term memory (delayed free recall and recognition of words and pictures) were assessed before and at 3 h after dosing. Pharmacodynamic interactions were evaluated by repeated measures ANOVA in a 2 x 2 factorial interaction model. 3 Mizolastine, 10 mg once daily, at steady-state, was devoid of sedation and detrimental effect on skilled performance and memory. 4 In contrast, a single 2 mg dose of lorazepam produced marked impairment of psychomotor performance, cognitive functions (significant reduction in flicker fusion threshold, tapping and arithmetic calculation and increase in reaction times and body sway) and subjective sedation from 2 to 8 h after dosing. In addition, lorazepam induced an anterograde amnesia, characterised by a decrease in delayed free recall and recognition, and a deficit in short term memory. 5 Mizolastine did not potentiate the detrimental effect of lorazepam. The time course and the intensity of the disruption induced by the combination of lorazepam and mizolastine closely paralleled the changes induced by lorazepam alone.Keywords mizolastine lorazepam antihistamine benzodiazepine interaction psychomotor performance memory cognitive function psychopharmacology

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“…cqand ob-adrenoceptors, and muscarinic receptors. Studies using mizolastine as a radioligand indicate absence of affinity for H?-receptors [2], As expected from its Hireceptor-blocking properties, mizolastine exhibits marked anti-anaphvlatic activity in animal models of allergy and asthma [3].…”

Section: Fluorophenyl)methyl]-l H-benzimidazo-2-yl]-4-piperidinyl]metmentioning

confidence: 99%

Mizolastine, a Novel Selective Histamine H<sub>1</sub> Receptor Antagonist: Lack of Sedative Potential on the EEG in the Rodent

Depoortere¹,

Decobert²,

Granger³

et al. 1995

Neuropsychobiology

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The sedative potential of mizolastine, a new, potent and selective antagonist of histamine H₁-receptors, has been evaluated in the rodent with EEG techniques. In chronically implanted rabbits, sedation was observed in ECoG recordings after intravenous injection of terfenadine (1–10 mg/kg) and loratadine (0.3–3 mg/kg) but not after intravenous injection of astemizole or mizolastine (1–10 mg/kg). In freely moving implanted rats, mizolastine and cetirizine (10 mg/kg i.p.) did not modify the sleep-wakefulness pattern recorded during the dark period nor did mizolastine alter the sleep architecture recorded in rats during the light period. In contrast, during the dark-period recording, astemizole, loratadine and terfenadine (10 mg/kg i.p.) increased the total duration of slow-wave sleep; this sleep-facilitating effect had a late onset of action, beginning 3 h after drug injection. In conclusion, the results obtained with astemizole, cetirizine, loratadine and terfenadine demonstrate their low sedative potential in the rat, and suggest that the absence or low incidence of sedation seen in humans with these drugs may be due to their limited ability to cross the blood brain-barrier, especially at recommended therapeutic doses. Mizolastine appears to be devoid of sedative effects in our experimental models irrespective of the route of administration used. These results predict a lack of sedative action in humans with mizolastine at therapeutic doses.

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Anti-anaphylactic activity of the non sedative histamime H1 receptor antagonist SL 85.0324 in the rat and guinea pig

Cited by 9 publications

References 0 publications

Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects

Lack of interaction between two antihistamines, mizolastine and cetirizine, and ethanol in psychomotor and driving performance in healthy subjects

Lack of interaction between a new antihistamine, mizolastine, and lorazepam on psychomotor performance and memory in healthy volunteers.

Mizolastine, a Novel Selective Histamine H<sub>1</sub> Receptor Antagonist: Lack of Sedative Potential on the EEG in the Rodent

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