Curran Monique P, Scott Lesley J, Perry Caroline M
Adis International Limited, Auckland, New Zealand.
Drugs. 2004;64(5):523-61. doi: 10.2165/00003495-200464050-00008.
Cetirizine is a selective, second-generation histamine H1 receptor antagonist, with a rapid onset, a long duration of activity and low potential for interaction with drugs metabolised by the hepatic cytochrome P450 system. Cetirizine was generally more effective than other H1 receptor antagonists at inhibiting histamine-induced wheal and flare responses. Cetirizine is an effective and well tolerated agent for the treatment of symptoms of seasonal allergic rhinitis (SAR), perennial allergic rhinitis (PAR) and chronic idiopathic urticaria (CIU) in adult, adolescent and paediatric patients. In adults with these allergic disorders, cetirizine was as effective as conventional dosages of ebastine (SAR, PAR, CIU), fexofenadine (SAR), loratadine (SAR, CIU) or mizolastine (SAR). This agent was significantly more effective, and with a more rapid onset of action, than loratadine in 2-day studies in environmental exposure units (SAR). In paediatric patients, cetirizine was as at least as effective as chlorphenamine (chlorpheniramine) [SAR], loratadine (SAR, PAR) and oxatomide (CIU) in the short term, and more effective than oxatomide and ketotifen (PAR) in the long term. Cetirizine was effective in reducing symptoms of allergic asthma in adults and reduced the relative risk of developing asthma in infants with atopic dermatitis sensitised to grass pollen or house dust mite allergens. It had a corticosteroid-sparing effect in infants with severe atopic dermatitis and was effective in ameliorating reactions to mosquito bites in adults. Cetirizine was well tolerated in adults, adolescents and paediatric patients with allergic disorders. In adult, adolescent and paediatric patients aged 2-11 years, the incidence of somnolence with cetirizine was dose related and was generally similar to that with other second-generation H1 receptor antagonists. Although, its sedative effect was greater than that of fexofenadine in some clinical trials and that of loratadine or fexofenadine in a postmarketing surveillance study. In infants aged 6-24 months, the tolerability profile of cetirizine was similar to that of placebo. Cetirizine did not have any adverse effects on cognitive function in adults, or cognitive function, behaviour or achievement of psychomotor milestones in paediatric patients. Cetirizine was not associated with cardiotoxicity.
Cetirizine is well established in the treatment of symptoms of SAR, PAR or CIU. It demonstrated a corticosteroid-sparing effect and reduced the relative risk of developing asthma in sensitised infants with atopic dermatitis. Cetirizine was effective in the treatment of allergic cough and mosquito bites; however, its precise role in these indications has yet to be clearly established. On the basis of its favourable efficacy and tolerability profile and rapid onset of action, cetirizine provides an important option for the treatment of a wide range of allergic disorders.
西替利嗪是一种选择性第二代组胺H1受体拮抗剂,起效迅速,作用持续时间长,与经肝细胞色素P450系统代谢的药物相互作用的可能性低。在抑制组胺诱发的风团和潮红反应方面,西替利嗪通常比其他H1受体拮抗剂更有效。西替利嗪是一种有效且耐受性良好的药物,可用于治疗成人、青少年和儿童患者的季节性变应性鼻炎(SAR)、常年性变应性鼻炎(PAR)和慢性特发性荨麻疹(CIU)症状。在患有这些过敏性疾病的成人中,西替利嗪与依巴斯汀(用于SAR、PAR、CIU)、非索非那定(用于SAR)、氯雷他定(用于SAR、CIU)或咪唑斯汀(用于SAR)的常规剂量效果相当。在环境暴露单元进行的为期2天的研究中(用于SAR),该药物比氯雷他定显著更有效,且起效更快。在儿科患者中,短期内西替利嗪至少与氯苯那敏(氯苯那敏)[用于SAR]、氯雷他定(用于SAR、PAR)和奥洛他定(用于CIU)效果相当,长期来看比奥洛他定和酮替芬(用于PAR)更有效。西替利嗪可有效减轻成人过敏性哮喘症状,并降低对草花粉或屋尘螨过敏原致敏的特应性皮炎婴儿患哮喘的相对风险。它对重症特应性皮炎婴儿有糖皮质激素节省作用,且对成人蚊虫叮咬反应有效。西替利嗪在患有过敏性疾病的成人、青少年和儿科患者中耐受性良好。在2 - 11岁的成人、青少年和儿科患者中,服用西替利嗪后嗜睡的发生率与剂量相关,且通常与其他第二代H1受体拮抗剂相似。尽管在一些临床试验中其镇静作用大于非索非那定,在一项上市后监测研究中大于氯雷他定或非索非那定。在6 - 24个月的婴儿中,西替利嗪的耐受性与安慰剂相似。西替利嗪对成人认知功能或儿科患者的认知功能、行为或精神运动发育里程碑的达成没有任何不良影响。西替利嗪与心脏毒性无关。
西替利嗪在治疗SAR、PAR或CIU症状方面已得到充分确立。它显示出糖皮质激素节省作用,并降低了对特应性皮炎致敏的婴儿患哮喘的相对风险。西替利嗪对过敏性咳嗽和蚊虫叮咬有效;然而,其在这些适应症中的确切作用尚未明确确立。基于其良好的疗效、耐受性和快速起效,西替利嗪为治疗多种过敏性疾病提供了一个重要选择。