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… 

The potential impact of 1st and 2nd generation antihistamines on male fertility

TLDR
It is reported that the second-generation antihistamine cetirizine hydrochloride has potent and significant effects on male fertility compared with the first-generation H1 antihistamines pheniramine maleate through its changes in prolactin, LH, and FSH levels.

Cetirizine per os: exposure and antihistamine effect in the dog

TLDR
A once-daily dosing regimen of 2–4 mg/kg cetirizine per os clearly provides a sufficient antihistamine effect and may be an option to treat histamine-mediated inflammation in the dog based on this experimental protocol but additional clinical studies are required.

Focus on the cetirizine use in clinical practice: a reappraisal 30 years later

TLDR
Cetirizine belongs to the second-generation family, so, it is very selective for peripheral H1 receptors, is potent and quickly relieves symptoms, exerts additional anti-allergic/anti-inflammatory effects, and is usually well-tolerated.

Cetirizine as a Causative Agent for Drug Induced Methemoglobinemia: A Case Report and Review.

TLDR
An unusually high systemic load of the drug speculatively saturated and overwhelmed the protective enzyme systems, which resulted in clinical manifestation of MHb, the first documentation of cetirizine as a causative agent for drug induced MHb.

Effects of cyproheptadine and cetirizine on eosinophilic airway inflammation in cats with experimentally induced asthma.

TLDR
In cats with experimentally induced asthma, cyproheptadine and cetirizine were not effective in decreasing airway eosinophilic inflammation or in altering several other measured immunologic variables.

Effects of antihistamines on the H295R steroidogenesis - Autocrine up-regulation following 3β-HSD inhibition.

Pharmacokinetics of cetirizine in healthy cats.

TLDR
The half-life of cetirizine in cats is compatible with once-daily dosing, and the extent of protein binding is high.

The protective role of l-carnitine against 1st- and 2nd-generation antihistamine-induced liver injury in mice

TLDR
Co-treatment of l-carnitine with chlorpheniramine maleate and cetirizine hydrochloride significantly improved the deteriorated hepatic function as indicated by reduction in the serum levels of ALT, AST, ALP and albumin levels compared with control and untreated groups.

3, 19-diacetyl-14-deoxy-11,12-didehydroandrographolide (srs27) antagonises inflammatory response and oxidative stress in in vitro and in vivo asthma models

TLDR
SRS27 was less toxic compared with AGP, which suggests that a simple chemical modification of DDAG produces a compound with CysLT and NO inhibitory activity similar to AGP but maintained the toxicity profile similar to DDAG, it is interesting to note.

References

SHOWING 1-10 OF 87 REFERENCES

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.

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.

Cetirizine: actions on neurotransmitter receptors.

Effect of cetirizine on histamine- and leukotriene D4-induced bronchoconstriction in patients with atopic asthma.

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.

Cutaneous antihistaminic action of cetirizine and dose-related EEG concomitants of sedation in man.

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).

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.

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.
...