Review of cetirizine hydrochloride for the treatment of allergic disorders

@article{Portnoy2004ReviewOC,
  title={Review of cetirizine hydrochloride for the treatment of allergic disorders},
  author={Jay M. Portnoy and Chitra Dinakar},
  journal={Expert Opinion on Pharmacotherapy},
  year={2004},
  volume={5},
  pages={125 - 135}
}
Cetirizine hydrochloride is an orally-active and selective histamine (H1)-receptor antagonist. It is a second-generation antihistamine and a human metabolite of hydroxyzine. Therefore, its principal effects are mediated via selective inhibition of peripheral H1 receptors. The antihistaminic activity of cetirizine has been documented in a variety of animal and human models. In vivo and ex vivo animal models have shown negligible anticholinergic and antiserotonergic activity. In clinical studies… Expand
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References

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Receptor effects of cetirizine.
TLDR
It is suggested that cetirizine's reduced incidence of sedative side effects may stem part from its selectivity for H1 receptors over sites involved in sedation, and partly from its relative exclusion from the CNS. Expand
Receptor effects of cetirizine.
TLDR
It is suggested that cetirizine's reduced incidence of sedative side effects may stem part from its selectivity for H1 receptors over sites involved in sedation, and partly from its relative exclusion from the CNS. Expand
Cetirizine: actions on neurotransmitter receptors.
First-generation H1-antagonist antihistamines, such as hydroxyzine, have the ability to cross the blood-brain barrier and cause sedation, which limits their usefulness in the treatment of allergicExpand
Effect of cetirizine, a new histamine H1 antagonist, on airway dynamics and responsiveness to inhaled histamine in mild asthma.
TLDR
In subjects with mild asthma, orally administered cetirizine provides significant dose-dependent protection against histamine-induced bronchoconstriction, which in the doses studied is superior to that produced by the parent compound, hydroxyzine. Expand
Effect of cetirizine on histamine- and leukotriene D4-induced bronchoconstriction in patients with atopic asthma.
TLDR
The small protective effect after a single dose against LTD4-induced bronchoconstriction indicates a nonspecific rather than a specific receptor antagonism, and suggests subsensitivity of H1 receptors developing in human airways. Expand
Cetirizine inhibition of histamine-induced bronchospasm.
TLDR
Cetirizine's efficacy was compared with that of a placebo and oral hydroxyzine (25 mg) in 10 patients with mild asthma and the new compound provided significant protection in a dose-dependent manner against histamine-induced bronchospasm. Expand
Cutaneous antihistaminic action of cetirizine and dose-related EEG concomitants of sedation in man.
TLDR
The existence of some histaminergic (H1) specificity of the mechanisms modulating vigilance and of a threshold dose of cetirizine for sedative action is suggested. Expand
Hypothetical Mechanisms of Action of an H1–Antihistamine in Asthma
TLDR
All the data collected up to now suggest the possible existence in the molecule of a central key mechanism of action on resident cells especially involved in cell trafficking and bronchial inflammation, i.e a down–regulating effect on the nuclear factorKB (NFKB). Expand
The clinical safety of H1‐receptor antagonists: An EAACI position paper *
TLDR
Since antihistamines are used to treat non-life-threatening disorders, their risk/benefit ratio must be carefully evaluated and the safety issue is of central importance because of the widespread use of antihistamine in current medical practice. Expand
A pharmacokinetic-pharmacodynamic modelling of the antihistaminic (H1) effects of cetirizine.
TLDR
The pharmacokinetic-pharmacodynamic modelling developed here characterizes the time course of cetirizine effect on histamine-induced skin reactions (wheal and flare) and shows that at this dosage the histamines-induced flare was at least 80% inhibited at the start of the second administration and the response control was nearly total. Expand
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