Cetirizine Exerts Anti-Inflammatory Effects on Human Neutrophils

Köller, Manfred; Hilger, Ralf A.; Rihoux, J P; König, Wolfgang

doi:10.1159/000237310

Cited by 23 publications

(15 citation statements)

References 10 publications

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“…In particular, cetirizine can facilitate proton transfer, a property of biological relevance [29] [30]. ± This study confirms the importance of conformational effects on the partition properties of cetirizine and hydroxyzine, with obvious pharmacokinetic implications.…”

Section: Resultssupporting

confidence: 70%

Ionic Partition Diagram of the Zwitterionic Antihistamine Cetirizine

Bouchard

Pagliara

Balen

et al. 2001

HCA

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A recent analysis of the lipophilicity profile of cetirizine in the octanol/water and dodecane/water systems revealed a partial intramolecular charge neutralization that can partly explain why cetirizine has pharmacokinetic properties differing from those of first-generation antihistamines such as hydroxyzine. As conformational changes are the principal driving force for this intramolecular effect, the present study deals with the partitioning of cetirizine and hydroxyzine in an apolar medium well-suited to reveal intramolecular interactions, namely the 1,2-dichloroethane/water system. The lipophilicity of the different electrical forms of cetirizine and hydroxyzine was studied by two-phase titrimetry and cyclic voltammetry. The differences in lipophilicity between the dicationic, monocationic, zwitterionic, and anionic species of cetirizine indicated intramolecular interactions via folded conformations, which render the molecule markedly more lipophilic than expected at physiological pH. Folded conformations were also found to predominate in monocationic and neutral hydroxyzine. The ionic partition diagram of cetirizine indicates that it acts as a proton transporter across interfaces under certain conditions of pH and Galvani potential difference. This study underlines the importance of conformational effects on the partition properties of cetirizine and hydroxyzine, as well as the complexity of its interfacial mechanisms of transfer. In particular, cetirizine can facilitate proton transfer, a property of potential biological relevance.

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Section: Resultssupporting

confidence: 70%

Ionic Partition Diagram of the Zwitterionic Antihistamine Cetirizine

Bouchard

Pagliara

Balen

et al. 2001

HCA

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“…Nevertheless, other antirelease activities of this drug were described more recently, using other cells and other mediators, and more importantly, physiological concentrations in vitro (±0.5 µ M ). Such concentrations of the drug inhibited the release of toxic products from atopic platelets [17]and eosinophils [18]and the release of LTB 4 from human neutrophils [19]. These in vitro data were confirmed in several in vivo conditions in atopic subjects.…”

Section: The Inhibition Of Mediator Releasementioning

confidence: 81%

Hypothetical Mechanisms of Action of an H1–Antihistamine in Asthma

Rihoux

Michel²,

Arnold³

et al. 1999

Int Arch Allergy Immunol

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Some recent clinical studies carried out with the potent H₁–antihistamine cetirizine (CTZ) suggest that this drug could be useful for the treatment of mild to moderate asthma and even for the prevention of the disease. Besides a potent antagonism of H₁–receptors at bronchial level, this drug was also shown to exert a large series of anti–inflammatory effects in in vitro, ex vivo and in vivo pharmacological models and also in clinical situations in atopic subjects. 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 factor_KB (NF_KB). This hypothesis was tested on human endothelial cells and a human epithelial pulmonary cell line using different experimental methods. The results showed that CTZ down–regulates the TNF–α–induced hyperactivation of NF_KB in these two different resident cells at physiological concentrations.

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“…Clinical studies of children demonstrated that cetirizine also possesses anti-inflammatory activity; it reduces production of leukotrienes in vitro [7,11]. Effect of the leukotriene level decrease is caused by the decreased migration of leukotriene-producing cells (eosinophils, basophils, and macrophages) towards the allergic response site [12].…”

Section: Pharmokokineticsmentioning

confidence: 99%

Clinical and Pharmacological Peculiarities of Cetirizine Use for the Therapy of Allergic Diseases in Children

Левина¹,

Намазова-баранова²,

Алексеева³

et al. 2014

Pediatr. farmakol.

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The review is dedicated to treatment of allergic diseases in childrenThe prevalence of allergic diseases such as seasonal and persistent allergic rhinitis, urticaria, atopic dermatitis and bronchial asthma has been steadily increasing in recent years. Allergic diseases have a tremendous impact on the quality of patients' life. Common pathogenetic link of development of any form of allergy (true and pseudoallergic) is the release of biologically active substances which leads to the development of one or another symptom complex (depending on the "shock" organ). The most important role in the pathophysiology of allergic diseases belongs to histamine mediator (5[2-aminoethyl]-imidazole) which is primarily contained in mast cells and basophils. The influence of histamine released from the IgE-activated mast cells during the early phase of an allergic reaction on organs and tissues mainly determines acute symptoms of allergic diseases. As a result of development of type I allergic reaction and the IgE-dependent degranulation of mast cells, the elevation of histamine concentration in blood plasma and tissue fluid takes place. The histamine level increase may also be caused by other mechanisms of cell activation: e.g., in the event of pseudoallergic reactions, the mast cell membrane is destroyed not by an antigen-antibody complex, but by some chemical or other agent. Pharmacological action of histamine is mediated through the stimulation of histamine receptors. Currently, four types of histamine receptors are known. Development of allergic reactions is mainly associated with the H1-histamine receptors, the activation of which leads to the contracture of smooth muscles of bronchi and gastrointestinal tract, increased vascular permeability, increased mucus secretion by nasal mucous glands and irritation of nerve endings. Histamine impact on histamine receptors results in the involvement of respiratory tract mucosae in the pathological process and occurrence of symptoms of allergic rhinitis and bronchial asthma, namely, itching, sneezing, swelling of mucosae, mucus hypersecretion and bronchospasm; when the ocular mucosa is affected, symptoms of allergic conjunctivitis take place, namely, itching, redness, swelling, lacrimation. The typical clinical effects of histamine on the skin are itching,

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Cetirizine Exerts Anti-Inflammatory Effects on Human Neutrophils

Cited by 23 publications

References 10 publications

Ionic Partition Diagram of the Zwitterionic Antihistamine Cetirizine

Ionic Partition Diagram of the Zwitterionic Antihistamine Cetirizine

Hypothetical Mechanisms of Action of an H1–Antihistamine in Asthma

Clinical and Pharmacological Peculiarities of Cetirizine Use for the Therapy of Allergic Diseases in Children

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