The effect of cetirizine and loratadine on codeine-induced histamine release in human skin in vivo assessed by cutaneous microdialysis

Perzanowska, M.; Malhotra, Diya; Skinner, Sandford L.; Rihoux, J P; Bewley, Anthony; Petersen, Lars Jelstrup; Church, Martin K.

doi:10.1007/bf02252321

Cited by 23 publications

(28 citation statements)

References 31 publications

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“…Since 1953, when Arunlakshana and Schild 9 showed that H1 antihistamines had the ability to inhibit the release of histamine from mast cells, several in vitro and in vivo studies have been conducted to determine whether these drugs have properties, other than the inhibition of histamine effects, that could contribute to the clinical efficacy of allergic diseases control. It has been postulated that some of the anti-inflammatory effects of H1 antihistamines follow their interaction with HRs, whereas others are independent of these receptors.…”

Section: Anti-inflammatory Properties Of H 1 Antihistaminesmentioning

confidence: 99%

“…4 In reality, these anti-inflammatory effects are questioned when studied in vivo. In 1996, Perzanowska et al 9 administered orally two H1 antihistamines -cetirizine and loratadine -both in the dose of 10 mg/day, four hours before the induction of histamine release through codeine intradermal injections of 3 mg/L and 10 mg/L. Results showed a clear reduction of the allergic response in the development of the erythema and dermal edema.…”

Section: Anti-inflammatory Properties Of H 1 Antihistaminesmentioning

confidence: 99%

See 1 more Smart Citation

Histamina, receptores de histamina e anti-histamínicos: novos conceitos

Criado

Maruta

et al. 2010

An. Bras. Dermatol.

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Drugs with antihistamine action are the most commonly prescribed medication in daily dermatologic practice, both to adults and children. This article addresses new concepts of the role of histamine receptors (H1 receptors) and discusses the anti-inflammatory effects of these drugs. Second generation antihistamines differs from first generation because of their high specificity and affinity for peripheral H1-receptors. Second generation antihistamines are also less likely to produce sedation because they have less effect on the central nervous system. Although the efficacy of the various H1-antihistamines in the treatment of allergic patients is similar, even when comparing first-and second-generation drugs, these drugs are still very different in terms of their chemical structure, pharmacology and toxic properties. Consequently, knowledge of their pharmacokinetic and pharmacodynamic characteristics is essential for a better medical care, especially that offered to pregnant women, children, the elderly, and patients with comorbidities. Keywords: Histamine; Histamine H1 receptors antagonists; Histamine receptors; Histamine release; Histamine H1 antagonists, non-sedating; Receptors, histamine H1Resumo: As drogas com ação anti-histamínica estão entre as medicações mais comumente prescritas na prática dermatológica diária, tanto em adultos como em crianças. Este artigo aborda os novos conceitos da função dos receptores de histamina (receptores H1) e discute os efeitos anti-inflamatórios dessas drogas. A segunda geração de anti-histamínicos difere da primeira geração devido a sua elevada especificidade e afinidade pelos receptores H1 periféricos e devido a seu menor efeito no sistema nervoso central, tendo como resultado menores efeitos sedativos. Embora a eficácia dos diferentes anti-histamínicos H1 (anti-H1) no tratamento de doentes alérgicos seja similar, mesmo quando se comparam anti-H1 de primeira e de segunda geração, eles são muito diferentes em termos de estrutura química, farmacologia e propriedades tóxicas. Consequentemente o conhecimento de suas características farmacocinéticas e farmacodinâmicas é importante para a melhor prática médica, especialmente em gestantes, crianças, idosos e doentes com comorbidades. Palavras-chave: Antagonistas da histamina H1 não sedativos; Antagonistas dos receptores H1 de histamina; Histamina; Liberação de histamina; Receptores de histamina; Receptores de histamina H1

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Section: Anti-inflammatory Properties Of H 1 Antihistaminesmentioning

confidence: 99%

Section: Anti-inflammatory Properties Of H 1 Antihistaminesmentioning

confidence: 99%

Histamina, receptores de histamina e anti-histamínicos: novos conceitos

Criado

Maruta

et al. 2010

An. Bras. Dermatol.

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“…It has been debated for years whether antihistamines impaired the release of inflammatory mediators or simply blocked the effect of the released mediators. While H-1 antihistamines reduced wheal and flare reactions, they did not reduce the level of allergen-or codeine-induced histamine release or that of PgD2 synthesis in the underlying skin during experimental studies (73,79,80). The ability of microdialysis to differentiate between the effects on the vasculature and those of the release of inflammatory mediators has also been applied in studies of glucocorticosteroids (81), beta-2 agonists (72,82), muscle relaxants (83,84), or heparin (85).…”

Section: Immediate Hypersensitivitymentioning

confidence: 96%

Microdialysis of Inflammatory Mediators in the Skin: A Review

Hersini¹,

Melgaard²,

Gazerani³

et al. 2014

Acta Derm Venerol

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Skin microdialysis is an established method for in vivo sample collection from the extracellular fluid space. This method has been extensively used in studies of inflammatory reactions in the skin of animals and humans. Skin microdialysis consists of the implantation of semi-permeable probes into the upper dermis, perfusion with a physiological buffer, and the recovery of the substances that diffused from the skin into the perfusion fluid. Microdialysis allows the simultaneous assessment of the temporal variations of inflammatory mediator release in the skin as well as the monitoring of vascular and sensory functions. By the aid of this technique, potential associations can be found between functional changes and a variety of substances and mediators released at the site of interest. This allows further insights into the possible mechanisms underlying physiological and pathophysiological events in the skin, including cutaneous inflammation. This review provides a comprehensive but not exhaustive review of the use of microdialysis in studies of experimental and clinical inflammatory reactions in the skin in animals and humans.

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“…To test the clinical significance of this effect, two H 1 antihistamines, cetirizine and loratadine, were administered at a dose of 10 mg orally, 4 h before the provocation of histamine release by intradermal injections of 3 and 10 mg/ml of codeine [59] . The results showed a clear inhibition of the ensuing weal and flare responses, demonstrating that the drugs had been absorbed and were bioactive.…”

Section: Receptor-independent Mechanismsmentioning

confidence: 99%

Antihistamines

Church¹,

Maurer²

2014

History of Allergy

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The discovery of histamine, its physiological role and reversal of its pharmacological effects by antihistamines takes us on a journey through the origins of modern physiology and the rising understanding of pharmacology at the end of the 19th and the early part of the 20th centuries. This journey, which has been traced in the excellent historical review by Michael Emanuel [Clin Exp Allergy 1999;29:1-11], is populated by some of the greatest scientists of the era, including six Nobel laureates - Bovet, Dale, Ehrlich, Richet, Windaus and Black. In addition, it laid the basis of medicinal chemistry not only for antihistamines, but also for the discovery of a plethora of drugs still in use today.

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The effect of cetirizine and loratadine on codeine-induced histamine release in human skin in vivo assessed by cutaneous microdialysis

Abstract: Neither cetirizine nor loratadine inhibited codeine-induced histamine release or modified the time course of its release in human skin in vivo when given in clinically used doses which are sufficient to significantly reduce weal and flare responses.

Cited by 23 publications

References 31 publications

Histamina, receptores de histamina e anti-histamínicos: novos conceitos

Histamina, receptores de histamina e anti-histamínicos: novos conceitos

Microdialysis of Inflammatory Mediators in the Skin: A Review

Antihistamines

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