Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria

Juhlin, Lennart; Vos, Christine De; Rihoux, J P

doi:10.1016/0091-6749(87)90014-5

Cited by 77 publications

(36 citation statements)

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“…Both of these effects were almost completely eliminated by the H 1 R antagonist, cetirizine, which is consistent with previous reports (Juhlin et al, 1987;Coulie et al, 1989Coulie et al, , 1991aSimons et al, 1990;Levander et al, 1991;Lahti and Haapaniemi, 1993;Grant , 1999;Furue et al, 2001;Morita et al, 2005). The ability of histamine to induce a wheal response is due to the expression of H 1 R on endothelial cells that control vascular permeability; thus, all compounds that inhibit the H 1 R will inhibit wheal responses.…”

Section: Discussionsupporting

confidence: 80%

The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

Kollmeier

Francke

Chen

et al. 2014

J Pharmacol Exp Ther

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The histamine H 4 receptor (H 4 R) is a promising target for the treatment of pruritus. A clinical study was conducted to evaluate the safety and efficacy of the H 4 R antagonist, JNJ 39758979 [(R)-4-(3-amino-pyrrolidin-1-yl)-6-isopropyl-pyrimidin-2-ylamine], on histamine-induced pruritus in healthy subjects. A single oral dose of 600 mg JNJ 39758979, 10 mg cetirizine, or placebo was administered in a randomized, three-period, double-blind, crossover study. Treatment periods were separated by 22-day washout periods. A histamine challenge was administered on day 21 and at 2 and 6 hours postdose on day 1 of each treatment period. The primary efficacy endpoint was the area under the curve (AUC) of pruritus score 0-10 minutes after the histamine challenge. Secondary efficacy endpoints included wheal and flare areas assessed 10 minutes after the histamine challenge. Safety was assessed for all subjects. Of the 24 enrolled subjects, 23 individuals completed the study. One subject withdrew after completing two treatment periods. Due to a carryover effect of JNJ 39758979, only treatment period 1 was used for pruritus-related evaluations. Compared with placebo, the reduction of the AUC of pruritus score was significant for JNJ 39758979 at 2 hours (P 5 0.0248) and 6 hours (P 5 0.0060), and for cetirizine at 6 hours (P 5 0.0417). In all treatment periods, JNJ 39758979 did not demonstrate a significant decrease in wheal or flare at either time point, although a significant reduction was achieved with cetirizine at 2 and 6 hours (P , 0.0001). Adverse eventss reported in .1 patient with JNJ 39758979 were headache (9%) and nausea (13%). In conclusion, JNJ 39758979 was effective in inhibiting histamine-induced pruritus in healthy subjects.

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Section: Discussionsupporting

confidence: 80%

The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

Kollmeier

Francke

Chen

et al. 2014

J Pharmacol Exp Ther

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“…Cetirizine, a second-generation antihistamine, inhibits the cutaneous response to histamine in animals and in man (Juhlin et al, 1987;Kontou-Fili et al, 1989;Rihoux & Van Neste, 1988;Simons et al, 1990), the bronchial response to histamine in asthmatic patients (Brik et al, 1987) and the nasal response to histamine in animals (Fireman et al, 1987). Despite its use in the treatment of allergic rhinitis, direct evidence of the antihistamine property of cetirizine in the human nose has not been reported yet.…”

Section: Introductionmentioning

confidence: 99%

Inhibition of histamine‐induced nasal obstruction by cetirizine in allergic rhinitis.

Braunstein¹,

Malaquin²,

Fajac³

et al. 1992

Brit J Clinical Pharma

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This double-blind randomized crossover placebo-controlled study was designed to assess objectively the nasal antihistamine effect of cetirizine in patients with allergic rhinitis and control subjects. Nasal challenge was performed by nebulization of increasing doubling doses of histamine (0; 0.04 to 1.28 mg/nostril) in six patients with allergic rhinitis and six control subjects on cetirizine (2 x 10 mg daily for 3 days) or placebo. Sneezings were counted and nasal obstruction was assessed by subjective scoring and by objective measurement of nasal airway resistance by posterior rhinomanometry. Histamine induced sneezing and a dose-dependent increase in nasal airway resistance and in perceived sensation of obstruction. Responses were greater in patients with allergic rhinitis compared with controls, although of borderline significance for nasal obstruction. Cetirizine totally abolished sneezing and significantly reduced increase in nasal airway resistance and perceived sensation of nasal obstruction both in normal and rhinitic subjects. Our results demonstrate by an objective measurement the nasal antihistamine effect of cetirizine. We propose this simple provocation test to assess the time-course of the effect of antihistamines and to compare the relative potency of related compounds.

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“…The principle indications for the use of second generation H1 receptor antagonists are in the treatment of disease with inflammatory component like allergic rhinitis, conjunctivitis, idiopathic urticarial and diseases of allergic nature like hayfever 24 , pollinosis 25 , dermographism 26 and atopic eczema 27 . There are established facts that state that histamine play a role as a mediator of inflammation.…”

Section: Discussionmentioning

confidence: 99%

Anti-Inflammatory Activity of H1 Receptor Antagonist Cetirizine in Animal Models

S.H¹,

Santoshkumar²

2013

jemds

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AIM:The present study was designed to study anti-inflammatory activity of Cetirizine in albino rats and compare with standard drug Diclofenac. MATERIAL & METHODS: 1. Carrageenin induced rat paw edema method (Acute inflammation): 5 animals in each group (3groups) received orally 4% Gum acacia, Diclofenac sodium and Cetirizine respectively one hour before carrageenin injection into right paw. The rat paw edema was measured with plethysmograph after 3 hours and percentage inhibition of edema was calculated in each group. 2. Rexin pellet granuloma method (Chronic inflammation): Four rexin pellets were implanted into dorsum skin of each rat of 3 groups (n=5), which include control, Diclofenac and Cetirizine respectively. The animals were treated with fixed doses of drugs once a day for 7 days including the day of implantation of pellets and on 8th day rexin pellets were removed after sacrificing animals. Rexin pellets were kept in incubator at 60 0 C overnight. Pellets were then weighed and percent inhibition of granuloma tissue was calculated. 3. Study of Mast cell counts. RESULT: Cetirizine showed significant anti-inflammatory activity both in acute and chronic animal models. CONCLUSION: Cetirizine may be used as potential drug for both acute and chronic inflammation due to its anti-inflammatory property.

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Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria

Cited by 77 publications

References 4 publications

The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

Inhibition of histamine‐induced nasal obstruction by cetirizine in allergic rhinitis.

Anti-Inflammatory Activity of H1 Receptor Antagonist Cetirizine in Animal Models

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Inhibiting effect of cetirizine on histamine-induced and 48/80-induced wheals and flares, experimental dermographism, and cold-induced urticaria

Cited by 77 publications

References 4 publications

The Histamine H4Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

The Histamine H4Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

Inhibition of histamine‐induced nasal obstruction by cetirizine in allergic rhinitis.

Anti-Inflammatory Activity of H1 Receptor Antagonist Cetirizine in Animal Models

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The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects

The Histamine H₄Receptor Antagonist, JNJ 39758979, Is Effective in Reducing Histamine-Induced Pruritus in a Randomized Clinical Study in Healthy Subjects