Urticária aquagênica: relato de caso e revisão de literatura / Aquagenic urticaria: a case report and literature review

A urticária aquagênica é uma forma rara de urticária crônica induzida (UCInd) desencadeada por um estímulo específico. A patogênese não é totalmente compreendida, mas os sintomas se iniciam minutos após a exposição cutânea à água, independentemente de sua temperatura, e as urticas têm o padrão foliculocêntricas. O diagnóstico é confirmado através do teste de provocação, e o tratamento de primeira linha são os anti-histamínicos de segunda geração. Neste artigo, relatamos um caso de urticária aquagênica e fazemos uma breve revisão da literatura sobre o tema.

Aquagenic urticaria is a rare form of chronic inducible urticaria (CIndU) triggered by a specific stimulus. Pathogenesis is not fully understood, but symptoms appear minutes after cutaneous exposure to water, regardless of temperature, and wheals have a folliculocentric pattern. The diagnosis of CIndU is confirmed by provocation testing using established protocols, and first-line treatment is second-generation antihistamines. In this article, we report a case of aquagenic urticaria and provide a brief review of the relevant literature.

Síndrome DRESS por paracetamol / DRESS syndrome due to acetaminophen

A síndrome DRESS é uma entidade rara e distinta, caracterizada por acometimento cutâneo e envolvimento de órgãos internos, com risco potencial de morte. O diagnóstico e o tratamento pre- coces são de vital importância. Relatos de DRESS por paraceta- mol são raros na literatura, razão pela qual apresentamos este caso. Paciente do sexo masculino, 56 anos, com surgimento de rash maculopapular, febre, linfadenopatia e hipereosinofilia 3 semanas após suspensão de paracetamol, associados ao ante- cedente familiar de reação a fármaco. Evoluiu bem após pulso- terapia com metilprednisolona.

DRESS syndrome is a rare and distinct entity characterized by cutaneous manifestations and internal organs involvement with a potential risk of death. Early diagnosis and treatment are vi- tally important. Reported cases of DRESS syndrome due to ace- taminophen are rare in the literature, and that is the reason for this case report. A 56-year-old male patient with maculopapular rash, fever, lymphadenopathy, and hypereosinophilia three we- eks after suspension of acetaminophen, associated with a family history of drug reaction. It progressed well after pulse therapy with methylprednisolone.

Consensus on the diagnostic and therapeutic management of chronic spontaneous urticaria in adults - Brazilian Society of Dermatology

Abstract: Background: Urticarias are frequent diseases, with 15% to 20% of the population presenting at least one acute episode in their lifetime. Urticaria are classified in acute ( ≤ 6 weeks) or chronic (> 6 weeks). They may be induced or spontaneous. Objectives: To verify the diagnostic and therapeutic recommendations in chronic spontaneous urticaria (CSU), according to the experience of Brazilian experts, regarding the available guidelines (international and US). Methods: A questionnaire was sent to Brazilian experts, with questions concerning diagnostic and therapeutic recommendations for CSU in adults. Results: Sixteen Brazilian experts answered the questionnaire related to diagnosis and therapy of CSU in adults and data were analyzed. Final text was written, considering the available guidelines (International and US), adapted to the medical practices in Brazil. Diagnostic work up in CSU is rarely necessary. Biopsy of skin lesion and histopathology may be indicated to rule out other diseases, such as, urticarial vasculitis. Other laboratory tests, such as complete blood count, CRP, ESR and thyroid screening. Treatment of CSU includes second-generation anti-histamines (sgAH) at licensed doses, sgAH two, three to fourfold doses (non-licensed) and omalizumab. Other drugs, such as, cyclosporine, immunomodulatory drugs and immunosuppressants may be indicated (non-licensed and with limited scientific evidence). Conclusions: Most of the Brazilian experts in this study partially agreed with the diagnostic and therapeutic recommendations of the International and US guidelines. They agreed with the use of sgAH at licensed doses. Increase in the dose to fourfold of sgAH may be suggested with restrictions, due to its non-licensed dose. Sedating anti-histamines, as suggested by the US guideline, are indicated by some of the Brazilian experts, due to its availability. Adaptations are mandatory in the treatment of CSU, due to scarce or lack of other therapeutic resources in the public health system in Brazil, such as omalizumab or cyclosporine.

Guía clínica chilena de urticaria crónica espontánea / Chilean guidelines for chronic urticaria

Chronic urticaria (CU) is characterized by itchy wheals, angioedema or both lasting six weeks or more. It is classified as spontaneous (CSU) and inducible urticaria (CIndU), depending whether there is an identifiable trigger or not. CSU is the predominant form, affecting more than 75% of patients, although overlaps often occur. The prevalence of CSU throughout life is around 1.8% and predominates in women at a ratio of 2:1. The higher incidence of CSU is between 20 and 40 years of age and lasts between one to five years. However, in up to 20% of patients the disease may last longer. CSU not only hampers quality of life, but also affect performance at work and school. The diagnosis of CSU is mainly clinical, and laboratory tests are required depending on the clinical history of the patient. Extensive laboratory tests are usually unnecessary. Second generation anti-histamines are used as first line treatment for CSU treatment. In refractory patients, systemic treatments, such as cyclosporine or omalizumab are suggested. We herein report the first Chilean CSU guidelines.

Association of CACNA1C gene genetic polymorphism with the susceptibility as well as prognosis for chronic spontaneous urticaria / 中南大学学报(医学版)

To investigate the relationship between single nucleotide polymorphisms (SNPs) of CACNA1C (SNPs rs58619945, rs7316246 and rs216008) and susceptibility of chronic spontaneous urticaria (CSU) as well as the curative effect of non-sedating antihistamine drugs.
 Methods: Peripheral blood were extracted from 191 CSU patients to collect DNA. Urticaria Activity Score 7 (UAS7) and Dermatology Life Quality Index (DLQI) changes were collected from these patients with different non-sedating antihistamine drugs. PubMed retrieval system was used to select the 3 SNPs (rs58619945, rs7316246 and rs216008) of CACNA1C. Susceptibility of CSU and curative effect of non-sedating antihistamine drugs (desloratadine, mizolastine, fisofenadine) in 189 CSU patients and 105 controls with different SNPs were compared with Chi-squared test. Data of 105 southern Chinese controls were extracted from the 1 000 genome database.
 Results: Frequency of rs58619945 G allele in the CSU patients was significantly higher than that in the controls [OR(95%CI)=0.660(0.470-0.925), P=0.016]. However, there was no significant differences in rs7316246 and rs216008 between the CSU patients and the controls. Meanwhile there was no significant difference in general curative effect of the 3 drugs in the 3 SNPs (rs58619945: OR=0.843, P=0.454; rs7316246: OR=2.103, P=0.102; rs216008: OR=0.237, P=0.363). There was significant difference in different alleles of rs216008 in the patients administered by desloratadine [OR(95%CI)=0.480(0.247-0.933), P=0.029]. No difference was shown in the 3 SNPs in patients administered by mizolastine.
 Conclusion: The rs58619945 A/G might be related to susceptibility of CSU, and the rs216008 mutation might affect drug response of desloratadine.

Association between desloratadine and prednisolone in the treatment of children with acute symptoms of allergic rhinitis: a double-blind, randomized and controlled clinical trial / Associação entre desloratadina e prednisolona no tratamento de crianças com sintomas agudos de rinite alérgica: ensaio clínico duplo-cego, randomizado e controlado

Abstract Introduction: A combination of antihistamines and oral corticosteroids is often used to treat acute symptoms of allergic rhinitis. Objective: To evaluate safety and efficacy of desloratadine plus prednisolone in the treatment of acute symptoms of children (2-12 years) with allergic rhinitis, and to compare it to dexchlorpheniramine plus betamethasone. Methods: Children with moderate/severe persistent allergic rhinitis and symptomatic (nasal symptoms score [0-12] ≥ 6) were allocated in a double-blind, randomized fashion to receive dexchlorpheniramine plus betamethasone (n = 105; three daily doses) or desloratadine plus prednisolone (n = 105; single dose followed by two of placebo) for 7 days. At the beginning and end of the evaluation, the following were obtained: nasal symptoms score, extra nasal symptoms score, peak nasal inspiratory flow, blood biochemistry, and electrocardiogram. Ninety-six children of the dexchlorpheniramine plus betamethasone group and 98 of the desloratadine plus prednisolone group completed the protocol. Results: The two groups were similar regarding initial and final nasal symptoms scores, extra nasal symptoms scores and peak nasal inspiratory flow. A drop of 76.4% and 79.1% for nasal symptoms score, 86.0% and 79.2% for extra nasal symptoms score, as well as an increase of 25.2% and 24.3% for peak nasal inspiratory flow occurred for those treated with desloratadine plus prednisolone and dexchlorpheniramine plus betamethasone, respectively. There were no significant changes in blood chemistry. Sinus tachycardia was the most frequent electrocardiogram change, but with no clinical significance. Drowsiness was reported significantly more often among those of dexchlorpheniramine plus betamethasone group (17.14% × 8.57%, respectively). Conclusion: The desloratadine plus prednisolone combination was able to effectively control acute symptoms of rhinitis in children, improving symptoms and nasal function. Compared to the dexchlorpheniramine plus betamethasone combination, it showed similar clinical action, but with a lower incidence of adverse events and higher dosing convenience.

Resumo Introdução: A associação entre anti-histamínicos e corticosteroides orais é frequentemente empregada no tratamento de sintomas agudos de rinite alérgica. Objetivo: Avaliar a segurança e eficácia da associação desloratadina + prednisolona no tratamento de sintomas agudos de crianças (2-12 anos) com rinite alérgica e compará-las com as da associação dexclorfeniramina + betametasona. Método: Crianças com rinite alérgica persistente moderada/grave e sintomáticas (escore de sintomas nasais [0-12] ≥ 6) foram alocadas de modo duplo-cego e randômico para receber dexclorfeniramina + betametasona (n = 105; três doses diárias) ou desloratadina + prednisolona (n = 105; dose única seguida por duas de placebo) por 7 dias. No início e no fim da avaliação foram obtidos: escore de sintomas nasais, escore de sintomas extranasais, pico de fluxo inspiratório nasal, bioquímica sanguínea e eletrocardiograma. Do total, 96 crianças do grupo dexclorfeniramina + betametasona e 98 do grupo desloratadina + prednisolona concluíram o protocolo. Resultados: Os dois grupos foram iguais com relação ao escore de sintomas nasais, escore de sintomas nasais extranasais e pico de fluxo inspiratório nasal iniciais e finais. Observou-se queda de 76,4% e 79,1% nos escores para escore de sintomas nasais, de 86,0% e 79,2% para escore de sintomas extranasais, assim como incremento de 25,2% e de 24,3% para o pico de fluxo inspiratório nasal para os grupos desloratadina + prednisolona e dexclorfeniramina + betametasona, respectivamente. Não houve alterações significativas da bioquímica sanguínea. Taquicardia sinusal foi a alteração do eletrocardiograma mais encontrada, mas sem significância clínica. Sonolência foi significantemente mais referida entre os tratados com dexclorfeniramina + betametasona do que entre os desloratadina + prednisolona (8,57% × 17,14%, respectivamente). Conclusão: A associação desloratadina + prednisolona foi capaz de controlar efetivamente os sintomas agudos de rinite em crianças, melhorou sintomas e a função nasal. Na comparação com a associação dexclorfeniramina + betametasona, demonstrou ação clínica semelhante, mas com menor incidência de eventos adversos e maior comodidade posológica.

A case of levocetirizine-induced liver injury

Levocetirizine is a second-generation nonsedative antihistaminic agent that has been demonstrated to be safe and effective for treating allergic disease. There was only one case report of levocetirizine-induced liver toxicity, but a liver biopsy was not performed. In this article, we present the first case of levocetirizine-induced liver injury with histologic findings. A 48-year-old man was hospitalized with jaundice and generalized pruritus that had developed after 2 months of therapy with levocetirizine for prurigo nodularis. Laboratory findings revealed acute hepatitis with cholestasis. A liver biopsy demonstrated portal inflammation and hepatitis with apoptotic hepatocytes. The patient fully recovered 3 weeks after withdrawing levocetirizine. Although levocetirizine is safe and effective, physicians should be aware of its potential hepatotoxicity.

An overview and considerations in prescribing H1-antihistamine

H1-antihistamines have been prescribed widely for the treatment of allergic diseases, such as rhinitis, atopic dermatitis, and urticaria besides common colds since the 1940s. H1-antihistamines are classified by chemical structures (akylamine, piperazine, piperidine, ethanolamine, ethylendiamine, and phenothiazine) or functionally by permeability through blood brain barrier (first or second generation). The first generation antihistamines have been prescribed up to now with several adverse effects such as central nervous system dysfunction, anticholinergic and antiserotonic action and cardiotoxicity with overdose. Hence second generation antihistamines are recommended for the treatment of allergic rhinitis and urticaria. Physicians should consider concomitant diseases or medications when prescribing first generation antihistamines.

Uremic pruritus in hemodialysis patients: treatment with desloratidine versus gabapentin / Prurido urêmico em pacientes em hemodiálise: tratamento com desloratidina versus gabapentina

INTRODUCTION: Uremic pruritus is common among dialysis patients. Effective treatments are not readily available. Early evidence with antihistamines and gabapentin indicate variable effects. OBJECTIVE: To compare the efficacy and side effects of gabapentin and desloratadine in patients with dialysis pruritus. METHODS: Prospective, open-label, cross-over clinical trial in 22 patients on chronic hemodialysis with sustained pruritus over a period of at least 60 days. After a one-week run-in period, we assigned patients to three weeks of either gabapentin 300 mg thrice weekly or desloratadine 5 mg thrice weekly. After a one-week washout period, each patient crossed-over to the alternate regimen for three more weeks. The primary endpoint of the study was the change in the visual analogue pruritus score (VAS). RESULTS: Nineteen subjects completed the two treatment blocks and were available for analysis. VAS scores decreased with both treatments (5.95 to 4.6 with gabapentin, p = 0.07; 5.89 to 3.4 with desloratadine, p = 0.004), but only desloratadine reached statistical significance. There were no differences when comparing the final pruritus score with gabapentin and desloratadine (4.6 versus 3.4, p = 0.16) Excessive sedation was common with gabapentin. Desloratadine was well tolerated. CONCLUSION: Desloratadine provides significant relief of uremic pruritus compared with no therapy. gabapentin has marginal efficacy. Desloratadine is better tolerated than gabapentin.

INTRODUÇÃO: Prurido urêmico é comum entre pacientes em diálise. Tratamentos eficazes não estão disponíveis até o momento. Provas recentes com anti-histamínicos e gabapentina indicam vários efeitos. OBJETIVO: Comparar a eficiência e os efeitos colaterais da gabapentina e da desloratadina em pacientes com prurido na diálise. MÉTODOS: Estudo prospectivo, aberto e comparativo com 22 pacientes em hemodiálise crônica com prurido constante durante um período de pelo menos 60 dias. Após uma semana, submetemos os pacientes a três semanas de gabapentina 300 mg, três vezes por semana, ou desloratadina 5 mg três vezes por semana. Após um período de eliminação de uma semana, os pacientes trocaram de regime por mais três semanas. O objetivo primário do estudo foi a mudança na escala visual analógica (EVA) de prurido. RESULTADOS: Dezenove indivíduos completaram os dois tratamentos e foram submetidos à análise. Os escores da EVA caíram com ambos os tratamentos (5,95 para 4,6 com gabapentina, p = 0,07; 5,89 para 3,4 com desloratadina, p = 0,004), mas somente a desloratadina teve significância estatística. Nenhuma diferença foi observada ao comparar o escore final do prurido com gabapentina e desloratadina (4,6 versus 3,4, p = 0,16). Excesso de sedação foi comum com gabapentina. A desloratadina teve alto nível de tolerância. CONCLUSÃO: A desloratadina dá alívio significante do prurido urêmico quando comparada a nenhum tratamento. A gabapentina tem eficiência marginal. A desloratadina tem maior nível de tolerância em relação à gabapentina.

Futura study: evaluation of efficacy and safety of rupatadine fumarate in the treatment of persistent allergic rhinitis / Estudo futura: avaliação da eficácia e segurança do fumarato de rupatadina no tratamento da rinite alérgica persistente

Allergic rhinitis affects 10-30 percent of the population, negatively impacting one's quality of life and productivity. It has been associated with sinusitis, otitis media, sleep disorders, and asthma. Rupatadine is a second generation antihistamine with increased affinity to histamine receptor H1; it is also a potent PAF (platelet-activating factor) antagonist. It starts acting quite quickly, offers long lasting effect, and reduces the chronic effects of rhinitis. AIM: this study aims to assess the efficacy and safety of rupatadine in the treatment of persistent allergic rhinitis. MATERIALS AND METHOD: this is a multi-centric open prospective study. This study included 241 patients from 13 centers in Brazil and was held between October of 2004 and August of 2005. Signs and symptoms of rhinitis and tolerance to medication were analyzed after one and two weeks of treatment. RESULTS: reduction on general scores from 8.65 to 3.21 on week 2 (p<0.001). All signs and symptoms improved significantly in the first day of treatment (p<0.001), except for nasal congestion and secretion, which improved from the second day of treatment (p<0.001). Adverse events occurred in 19.9 percent of the cases, 27.7 percent on week 1. CONCLUSION: rupatadine effectively controls persistent allergic rhinitis; it is safe and presents low incidence of side effects.

A rinite alérgica acomete 10 a 30 por cento da população, interferindo na qualidade de vida e na capacidade produtiva. Está associada à sinusite, otite, roncopatias e asma. A Rupatadina é um anti-histamínico de segunda geração, com elevada afinidade ao receptor histamínico H1 e potente inibição do fator ativador plaquetário (PAF). Tem rápido início de ação, longa duração e reduz os efeitos crônicos da rinite. OBJETIVO: Avaliar a eficácia e segurança da rupatadina no tratamento da rinite alérgica persistente. MATERIAL E MÉTODO: Estudo multicêntrico, aberto, prospectivo. Foram selecionados 241 pacientes em 13 centros no Brasil durante o período de outubro de 2004 a agosto de 2005. Foram analisados os sinais e sintomas da rinite e a tolerabilidade após 1 e 2 semanas. RESULTADOS: Redução do escore geral de 8,65 para 3,21 na semana 2 (p<0,001). Todos os sinais e sintomas melhoraram significativamente, e no primeiro dia de tratamento (p<0,001), com exceção da obstrução e secreção nasal, a partir do segundo dia (P<0,001). A frequência de eventos adversos foi 19,9 por cento, sendo 27,7 por cento na 1ª semana. CONCLUSÕES: A rupatadina é eficaz no controle da rinite alérgica persistente, é segura e apresenta baixos índices de efeitos colaterais.

Clinical research of Ibudilast on treating the steroid resistant allergic rhinitis / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To compare the efficacy and safety of histamine H1 receptor antagonist loratadine with Leukotriene receptor antagonist Ibudilast in steroid resistant allergic rhinitis in a randomized controlled clinical trial.@*METHOD@#Thirty-five cases were treated by Ibudilast, and 34 cases by loratadine. Score system was used to compare the therapeutic effect of these two drugs on clinical symptoms and signs.@*RESULT@#Ibudilast shows a better curative effect than loratadine in the improvement of the total scores on clinical symptom and signs(P<0.05). Scores of symptoms and signs in Ibudilast group after 3, 7, 14 days decreased significantly by means of square analysis of single factor (P<0.01). No complication was observed.@*CONCLUSION@#Ibudilast can effectively alleviate the clinical symptoms and signs of steroid resistant allergic rhinitis with confirmed efficacy and safety, thus is recommended in steroid resistant allergic rhinitis. Increased doses or prolonged treatment of steroid is inappropriate.

Efficacy of montelukast and loratadine as treatment for allergic rhinitis in children.

The objective of this study was to compare the effectiveness of montelukast combined with loratadine once daily to loratadine alone for a 2-week treatment course of allergic rhinitis in a randomized, double-blind placebo controlled trial which enrolled 115 children, 6- 15-years-old. The patients were randomly assigned to receive montelukast and loratadine (treatment group) or placebo and loratadine (control group). The primary outcome was the mean percent change of the total daytime nasal symptom scores (PDTS) and secondary outcomes were the mean percent changes of the nighttime nasal, daytime eye and composite symptom scores (PNTS, PES, PCS), as well as the nasal secretion, turbinate swelling and nasal congestion scores (PNSS, PTSS, PNCS). There were no significant differences in the PDTS of the 2 groups. The change in the night time nasal congestion score (PNTS-congestion) was higher in the treatment group, but not statistically significant (p = 0.077). Only the mean percent change in decreased turbinate swelling was significantly greater in the montelukast and loratadine group than the loratadine alone group (-22 +/- 7 vs. -1 +/- 5, p < 0.05).

Neurotrophins: are they meaningful in chronic spontaneous urticaria?

Plasma neurotrophin levels are elevated in patients with allergic and autoimmune diseases. The present study was designed to investigate the serum neurotrophin levels in 42 patients displaying chronic spontaneous urticaria, as well as 22 healthy control subjects. Blood samples were obtained from subjects during their first visit to the clinic, and then again after one month of desloratadine therapy. No significant difference was found between patient and control groups in terms of basal serum neurotrophin levels. However, basal nerve growth factor levels in patients whose symptoms persisted despite treatment were significantly lower than those of the drug-responsive patients and the control group. In treatment-responsive patients, nerve growth factor increased after suppression of the symptoms. Our study suggests that chronic spontaneous urticaria is linked with changes serum nerve growth factor levels, and that the deregulation of neurotrophins may contribute to urticaria pathophysiology.

Comparative efficacy of levocetirizine, desloratidine and fexofenadine by histamine wheal suppression test.

BACKGROUND: Histamine is the major mediator of allergic reactions. Newer H1 antihistaminics like levocetirizine, fexofenadine, and desloratadine are used in the treatment of seasonal and perennial allergic rhinitis and urticaria. The ability to block the cutaneous response to intradermal histamine is used to evaluate the potential of antihistamines. AIMS: To compare the potency, onset, and duration of action of the commonly used antihistamines-levocetirizine, fexofenadine, and desloratadine. METHODS: Thirty volunteers were given three single doses of levocetirizine, fexofenadine and desloratadine at weekly intervals. A pretest was performed by using the intradermal histamine prick test. After administration of the drugs, the intradermal test was repeated at (1/2), 1, 2, 3, 6 and 24 h, and the sizes of the wheal were measured. The mean values were taken and were compared by using Levene's t-test. RESULTS: At 30 min, fexofenadine showed a statistically significant suppression of wheal size compared to levocetirizine and desloratadine. Two and three hours after administration, levocetirizine and fexofenadine showed statistically significant inhibition of wheal size while only levocetirizine had this effect after six hours when compared to desloratadine. Desloratadine showed greater inhibition of wheal size at the end of 24 h when compared to levocetirizine and fexofenadine but this was not statistically significant. CONCLUSIONS: Fexofenadine had the earliest onset of action while levocetirizine showed maximum inhibition of wheal response after three and six hours.

The effect of desloratadine on quality of life of patients with seasonal allergic rhinitis / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To assess the effect of desloratadine on quality of life (QOL) in patients with seasonal allergic rhinitis.@*METHOD@#A randomized, double-blind, placebo-controlled study was designed on fifty patients with seasonal allergic rhinitis. The patients were randomly divided into three groups: A group: taking desloratadine by mouth and taking spraying of normal sodium; B group: placebo group, taking placebo by mouth and taking spraying of normal sodium; C group: taking desloratadine by mouth and taking spraying of Nasonex. Rhinitis quality of life (RQOL) questionnaire was used to evaluate QOL of patients with seasonal allergic rhinitis. The method of taking tabella was one tablet, one time a day; the method of taking spraying was one spray each nostril, once a day. The investigation lasted for two weeks. The RQOL questionnaire was administered at the start of the treatment and after one and two weeks of treatment by the telephone follow-up investigation.@*RESULT@#After 1 and 2 weeks of treatment, symptoms scores were significantly decreased in the A group and C group compared with the placebo group (P < 0.05). After 1 and 2 weeks of treatment by the methods of A and C, the QOL of patients with seasonal allergic rhinitis was significantly improved compared with placebo group (P < 0.05). There was no QOL improvement in the placebo group.@*CONCLUSION@#Desloratadine could decrease symptom scores and improve QOL in patients with seasonal allergic rhinitis. The RQOL questionnaire could help doctor to effectively evaluate QOL in patients with seasonal allergic rhinitis, because of its integrity and convenience.

Observation on cardiovascular safety of loratadine in treatment of persistent allergic rhinitis / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To evaluate cardiovascular safety of loratadine, a second generation H1-antagonist, in treatment of patients with allergic rhinitis.@*METHOD@#A total of 50 patients with persistent allergic rhinitis were enrolled, of which 19 cases (38.0%) had a history of cardiovascular diseases and/or presented abnormal electrocardiogram (ECG) findings without prolonged QT-interval. For all patents, 10 mg loratadine tablet was oral administrated once-daily for 30 days. ECG examinations were carried out both before and after treatment. Cardiovascular effects of loratadine were determined by the comparison of two ECGs.@*RESULT@#All patients had no alterations in sinus rhythm after administration of loratadine for 30 days. There were no significant differences of heart rates, P durations, PR or QRS intervals between the baseline and end-point ECGs (P > 0.05), as well as no significant prolongation of the QT or QTc corrected for heart rate using Bazett' formula (P > 0.05).@*CONCLUSION@#Cardiovascular safety of loratadine, a second generation H1-antagonist, is confirmed in long-term treatment of persistent allergic rhinitis at a recommended dose.

Effect of cetirizine hydrochloride on the expression of substance P receptor and cytokines production in human epidermal keratinocytes and dermal fibroblasts / 药学学报

To investigate the effect of cetirizine hydrochloride on the expression of neurokinin 1 receptor (NK-1R) and cytokines production induced by substance P (SP) in HaCaT cells (a human epidermal keratinocyte cell line) and dermal fibroblasts. The effect of cetirizine on the expression of NK-1R protein was detected by flow cytometry and Western blotting analysis. The modulation of cetirizine on the production of interferon (IFN)-gamma, interleukin (IL)-1beta, IL-6 and IL-8 in HaCaT cells and fibroblasts was measured by ELISA. The results showed that cetirizine significantly inhibited the expression of NK-1R in HaCaT cells and fibroblasts. SP induced the production of IFN-gamma, IL-1beta and IL-8 in both cell types. Cetirizine 1-100 micromol x L(-1) inhibited SP-induced IL-1beta and IL-8 production in HaCaT cells and fibroblasts, while had no effect on the production of IFN-gamma in both cells. Both SP and cetirizine had no effect on the secretion of IL-6 in HaCaT cells and fibroblasts. These findings suggest that cetirizine may be involved in the treatment of SP-induced skin inflammation by inhibiting the expression of substance P receptor and regulation the production of IL-1beta and IL-8 in epidermal keratinocyte and dermal fibroblasts.

Efficacy and safety of Mizolastine in the treatment of perennial allergic rhinitis / 临床耳鼻咽喉头颈外科杂志

OBJECTIVE@#To investigate the efficacy and safety of Mizolastine in the treatment of perennial allergic rhinitis.@*METHOD@#Multicentric random Double-blind parallel-controlled study was adopted, and compared with placebo and Cetirizine. Patients (n = 177) were grouped, seventy-two in Mizolastine group, sixty-nine in Cetirizine and thirty-six in placebo group.@*RESULT@#In the seventh curative day symptomatic and sign marks in Mizolastine group and Cetirizine group were lower, but the mark in Mizolastine group reduced more than in Cetirizine group and placebo group. Mizolastine group is better than Cetirizine group in improvement of nasal obstruction and itching with Visual analogue scale. In the twenty first curative day reduction of symptomatic and sign marks in Mizolastine group was lower than Cetirizine group, but no statistic difference. There were 27 adverse events, no serious adverse events in 177 patients during experimental period. Most adverse events were headache and dryness in mouth and eyes. There were 10 cases adverse events in Mizolastine group, one case was related with experiment and four cases might be related with experiment. There were 14 cases adverse events in Cetirizine group, one case was related with experiment and four cases might be related with experiment. There were three cases adverse events in placebo group.@*CONCLUSION@#Generally speaking the efficacy of Mizolastine in treatment of perennial allergic rhinitis is better than Cetirizine, Bad events are less. It is safe.

New antihistamines: a critical view

OBJETIVO: Avaliar criticamente os mais novos anti-histamínicos anti-H1 e os diferentes termos utilizados para denominá-los, com base na revisão de evidências sobre o papel dos anti-H1 no tratamento das doenças alérgicas. FONTES DOS DADOS: Artigos originais, revisões e consensos indexados nos bancos de dados MEDLINE e PUBMED de 1998 a 2006. Palavra chave: anti-histamínicos. SíNTESE DOS DADOS: Os anti-histamínicos de segunda geração diferenciam-se dos de primeira geração por sua elevada especificidade e afinidade pelos receptores H1 periféricos e pela menor penetração no sistema nervoso central (SNC), com conseqüente redução dos efeitos sedativos. Embora os anti-histamínicos de segunda geração sejam, geralmente, melhor tolerados do que seus predecessores, alguns efeitos adversos, principalmente cardiotoxicidade, surgiram com alguns deles. Nos últimos 20 anos, novos compostos, com diferentes farmacocinéticas, foram sintetizados. A maioria deles manifesta propriedades antiinflamatórias que independem de sua atividade no receptor H1. Aprimoramentos mais recentes, geralmente na forma de metabólitos ativos, levaram ao uso do termo anti-histamínico de terceira geração. Esse termo surgiu espontaneamente, sem uma descrição clara de seu significado e implicações clínicas, criando grande confusão entre os profissionais da saúde. CONCLUSÕES: Com base nas evidências sobre anti-histamínicos anti-H1, nenhum deles pode ser considerado como "anti-histamínico de terceira geração". Para tanto, seria preciso comprovar que a nova classe de anti-histamínicos possui vantagens clínicas distintas sobre os compostos existentes e preenche pelo menos três pré-requisitos: ausência de cardiotoxicidade, de interações medicamentosas e de efeitos sobre o SNC.

OBJECTIVE: To perform a critical evaluation of the more recent H1 antihistamines and the various terms used to describe them, based on a review of evidence on their role in the treatment of allergic disorders. SOURCES: Original articles, reviews and consensus documents published from 1998 to 2006 and indexed in the MEDLINE and PubMed databases. Keyword: antihistamines. SUMMARY OF THE FINDINGS: Second-generation antihistamines differ from first-generation ones because of their elevated specificity and affinity for peripheral H1 receptors and because of their lower penetration of the central nervous system (CNS), having fewer sedative effects as a result. Whilst second-generation antihistamines are in general better tolerated than their predecessors, some adverse effects, principally cardiotoxicity, have been observed with some of them. Over the last 20 years, new compounds with different pharmacokinetic properties have been synthesized. The majority of these exhibit anti-inflammatory properties that are independent of their action on the H1 receptor. More recent improvements, generally in the form of active metabolites, led to the use of the term third-generation antihistamines. This term emerged spontaneously, with no clear definition of its meaning or clinical implications, creating great confusion among healthcare professionals. CONCLUSIONS: On the basis of the evidence on H1 antihistamines, none of them deserve the title"third-generation antihistamine." As the Consensus Group on New Generation Antihistamines concluded, to merit this definition, a new class of antihistamines would have to demonstrate distinct clinical advantages over existing compounds and fulfill at least three prerequisites: they should be free from cardiotoxicity, drug interactions and effects on the CNS.