A comparison between astemizole and other antihistamines on sleep-wakefulness cycles in dogs

Wauquier, A.; Broeck, W.A.E. Van Den; Awouters, F.; Janßen, Paul

doi:10.1016/0028-3908(81)90078-2

Cited by 46 publications

(13 citation statements)

References 12 publications

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“…Electroencephalographic experimental models used to evaluate the sedative potential of standard or classical antihistamines have been based on the study of the sleepwakefulness patterns in the rat [8], in the cat [19,34] and in the dog [12], In these three species, diphenhydramine increased the time spent in SWS, which is consistent with the clinical finding that somnolence is usually seen with first-generation antihistamine therapy. However, whether or not new antihistamines (e.g.…”

Section: Discussionsupporting

confidence: 64%

“…With regard to the incidence of waking behavior. H i-receptor agonists such as 2-thiazolylethylamine or histamine, when administered by the intracerebroventricular route in rats or when injected locally into the ventrolateral posterior hypothalamus in cats, increase wakefulness (W) and decrease slow wave sleep (SWS) [7,8], In contrast, the histamine synthesis inhibitor, a-fluoromethylhistidine, or the earlier H|-receptor antagonists pyrilamine, diphenhydramine, chlor pheniramine reduce W and increase SWS in rats, cats and dogs [7,[9][10][11][12], Antihistamines are the most widely prescribed drugs for the treatment of allergic diseases but a major limita tion of early H|-receptor antagonists is their liability for inducing a variety of undesirable side effects; for example, they often cause drowsiness and impair performance [13][14][15].…”

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

confidence: 99%

“…Recently, a new generation of H|-receptor antagonists (astemizole, cetirizine, loratadine, mequitazine, terfenadine) has been developed and classified as 'nonsedating' antihistamines owing to the fact that they do not interfere with CNS functions and, in addition, poorly cross the blood-brain barrier [10,12,[16][17][18][19][20][21][22], Nevertheless, con flicting results have been reported concerning the central effects of some of these new antihistamines; for instance, terfenadine was found to increase SWS in dogs [23] and astemizole reduced REM sleep in cats [10].…”

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

confidence: 99%

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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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Section: Discussionsupporting

confidence: 64%

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

confidence: 99%

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

confidence: 99%

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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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“…In addition, pyrilamine prevents the effect on sleep and W produced by HI-receptor agonists (Wauquier et al, 1981;Monti et al, 1985;Monti et al, 1986;Lin et al, 1986).…”

Section: Introductionmentioning

confidence: 92%

Effects of a-fluoromethylhistidine on sleep and wakefulness in the rat

Monti

D'Angelo

Jantos

et al. 1988

J. Neural Transmission

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The histamine synthesis inhibitor a-fluoromethylhistidine (a-FMH, 50 mg/kg, i.p.) significantly reduced wakefulness (W) and light sleep and increased slow wave sleep (SWS) and REM sleep during the light period in rats housed under 12 h light/12 h dark conditions (12L/12D). When animals were housed under 16 h light/8 h dark (16L/8D) they remained awake for a longer period of time during the dark as compared to the 12L/12D lighting cycle. Under this condition a-FMH 50 mg/kg significantly decreased W and increased SWS. Our results tend to indicate that histamine intervenes in sleep-wakefulness regulation. In addition, histamine could be partly involved in the abnormally increased incidence of W observed during the dark in rats housed under 16L/8D conditions.

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“…The antihistamines used also decreased REM sleep and this action might reflect the central anticholinergic action ( fig. 3) [ Wauquier et al, 1981b], In contrast, astemizole, the prototype of a new series of compounds with potent antihistaminic properties, at a dose largely exceeding the antihistamine dose was devoid of any significant effect on sleep-wakefulness patterns [Wauquier and Niemegeers, 1981;Wauquier et al, 1981b] (fig. 2).…”

Section: Prediction In Humansmentioning

confidence: 99%

Drug Effects on Sleep-Wakefulness Patterns in Dogs

Wauquier¹

1983

Neuropsychobiology

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Sleep-wakefulness patterns in dogs were studied using computerized on-line analysis and off-line sleep stage classification. A short description of the methods is given and the results of the analysis are discussed, touching on the problem of similarities and dissimilarities with sleep-wakefulness patterns in cats. Examples are given of species differences with respect to the effects of narcotic analgesics. The predictability of results obtained in the dog with respect to humans is discussed using as an example the sedative effects of antihistamines and the absence of such effects in response to a specific H₁-antagonist, astemizole. The role of neuro transmitters in sleep is studied, especially the role of dopamine by using dopamine antagonists (pimozide, domperidone) and dopamine agonists (apomorphine).

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A comparison between astemizole and other antihistamines on sleep-wakefulness cycles in dogs

Cited by 46 publications

References 12 publications

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

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

Effects of a-fluoromethylhistidine on sleep and wakefulness in the rat

Drug Effects on Sleep-Wakefulness Patterns in Dogs

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