Inhibitory effect of terfenadine on mediator release from human blood basophils and eosinophils

Nabe, Makoto; Agrawal, Devendra K.; Sarmiento, Emmanuel U.; Townley, Robert G.

doi:10.1111/j.1365-2222.1989.tb02426.x

Cited by 52 publications

(28 citation statements)

References 20 publications

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“…Other investigators reported similar results using hyperventilation [14] or exercise [15]. Furthermore, we have shown that terfenadine inhibits his tamine release from human basophils and leukotriene C4 production from human eosinophils [16], Terfenadine has also been shown to be potentially beneficial in asthma, in single dose studies, by inducing significant bronchodilitation at clinically relevant doses, even without a loading dose [12,13,15,17]. Recently, we have reported the effect of terfenadine on bronchoconstriction, dermal response, and leukopenia in duced by PAF [17].…”

Section: Introductionsupporting

confidence: 82%

Effect of Terfenadine on Neutrophil and Eosinophil Chemotactic Activities after Inhalation of Platelet-Activating Factor in vivo and on Neutrophil Chemotaxis in vitro

Okada

Hopp

Miyagawa

et al. 1992

Int Arch Allergy Immunol

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In this double-blind crossover study we evaluated the effect of terfenadine on the rise in neutrophil chemotactic activity (NCA) and eosinophil chemotactic activity (ECA) in serum induced by platelet-activating factor (PAF) inhalation in 8 asthmatics. Additionally, we examined the direct effect of terfenadine on neutrophil chemotaxis in vitro in 7 allergic subjects. NCA and ECA in serum after PAF inhalation and neutrophil chemotaxis were measured using a modified Boyden chamber method. An initial elevation of NCA after PAF inhalation was inhibited by terfenadine, but the effect was diminished after subsequent PAF inhalations. Terfenadine showed no effect on ECA. In vitro PAF- and fMLP-induced neutrophil chemotaxis were significantly inhibited by terfenadine. These results suggest that terfenadine may have antiallergic properties in addition to its H₁ receptor blockade.

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Section: Introductionsupporting

confidence: 82%

Effect of Terfenadine on Neutrophil and Eosinophil Chemotactic Activities after Inhalation of Platelet-Activating Factor in vivo and on Neutrophil Chemotaxis in vitro

Okada

Hopp

Miyagawa

et al. 1992

Int Arch Allergy Immunol

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“…promethazine, chlorpheni ramine, cyclizine, diphenhydramine, pyrilamine [4], ketotifen [5], oxatomide [6], azatadine [7], terfenadine [8,9]. The inhibitory effect varies between different types of anti histamine [4], Most of these studies were made in vitro and higher concentrations were used than are expected to reach the mast cells following oral administration.…”

Section: Discussionmentioning

confidence: 99%

“…The 'mast cell stabilizing' effect of antihis tamines has so far mainly been studied in vitro [3][4][5][6][7][8] but recently also in vivo [9][10][11], The aim of the present investigation was to examine the release-inhibiting effect in vivo in human skin. We used a virtually noninvasive method based upon the premise that an antihistamine inhibiting the release process would be expected to cause a more pro nounced inhibition of the response to a releas ing agent than to that evoked by histamine per se.…”

Section: Introductionmentioning

confidence: 99%

Inhibitory Effect of Loratadine and Clemastine on Histamine Release in Human Skin

Hägermark

Wahlgren²,

Giös³

1992

Skin Pharmacol Physiol

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The inhibitory effect of the two H₁ antagonists clemastine and loratadine on histamine release in human skin was studied in 15 volunteers. The antihistamines and placebo were administered orally (clemastine 2 mg twice a day, loratadine 10 mg once a day) for 5 days according to a double-blind, crossover design. Clemastine caused a significant sedation in comparison with placebo, whereas there was no difference between loratadine and placebo in this respect. After 5 days’ medication, flare reaction was induced by intradermal injection of histamine and the histamine liberator compound 48/80. The antihistamine dosages were approximately equipotent and inhibited the flare response induced by histamine to about the same extent, whereas the flares induced by compound 48/80 were still more inhibited by both drugs. The results indicate that clemastine and loratadine not only inhibit histamine effects at H₁ receptor level, but have additional suppressive effects, probably due to inhibition of mast cell degranulation. The simple, virtually noninvasive, in vivo technique described in this paper does not require chemical analysis of the released mediators and could be used to screen ‘mast cell stabilizing’ effects of various antihistamines.

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“…In addition antihistamine drugs, now classifi ed as H 1 -inverse agonists, possess anti-infl ammatory actions which are independent of their actions on the H 1 receptor. In vitro and animal experiments have shown that besides anti-cholinergic properties, H 1 antihistamines also suppress IgE-mediated histamine release from basophils and mast cells [25] . They also inhibit eosinophil chemotaxis, adhesion molecule expression and cytokine transcription [26][27][28] .…”

Section: Mode Of Action Of H 1 Antihistamines In the Skinmentioning

confidence: 99%

Antihistamines in Dermatology

Greaves¹

2005

Skin Pharmacol Physiol

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Along with antibiotics, antihistamines are the most widely used systemic drugs in dermatology. This is attributable to the major role played by histamine in common diseases such as urticaria and atopic eczema. Of the currently recognised four subtypes of G protein-coupled histamine receptors, only the H₁ and H₂ subtypes have been positively identified in human skin. Traditionally believed to be competitive antagonists of histamine, H₁ and H₂ antihistamines are now considered to behave as inverse agonists. By consensus, H₁ antihistamines are classified as ‘first generation’ (associated with troublesome side-effects including somnolence, anti-adrenergic and atropine-like actions) and ‘second-generation’ compounds (in which these side-effects are reduced or absent). The main indications for H₁ antihistamines in skin are suppression of pruritus in urticaria and atopic eczema, both of which are associated with increased mast cell numbers and tissue histamine levels. However the evidence basis for use in atopic eczema is ambiguous and controversial, even though these drugs are widely used in practice. Currently, significant side-effects are mainly confined to the first-generation compounds and are especially troublesome in the elderly. Psychomotor impairment may persist throughout the day following administration. Anti-cholinergic and anti-α-adrenergic blockade and cardiotoxicity (torsade de pointes) may also occur with first-generation antihistamines. Two early low-sedation second-generation antihistamines caused arrhythmias in a small number of patients but these compounds have now been withdrawn. Generally, the second-generation H₁ antihistamines are well tolerated.

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Inhibitory effect of terfenadine on mediator release from human blood basophils and eosinophils

Cited by 52 publications

References 20 publications

Effect of Terfenadine on Neutrophil and Eosinophil Chemotactic Activities after Inhalation of Platelet-Activating Factor in vivo and on Neutrophil Chemotaxis in vitro

Effect of Terfenadine on Neutrophil and Eosinophil Chemotactic Activities after Inhalation of Platelet-Activating Factor in vivo and on Neutrophil Chemotaxis in vitro

Inhibitory Effect of Loratadine and Clemastine on Histamine Release in Human Skin

Antihistamines in Dermatology

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