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地氯雷他定

Desloratadine.

作者信息

McClellan K, Jarvis B

机构信息

Adis International Limited, Mairangi Bay, Auckland, New Zealand.

出版信息

Drugs. 2001;61(6):789-96; discussion 797. doi: 10.2165/00003495-200161060-00007.

Abstract

Desloratadine is the orally active major metabolite of the nonsedating H1-antihistamine loratadine. The drug had no adverse cardiovascular effects in various animal models or when administered at 9 times the recommended adult dosage for 10 days in volunteers. Therapeutic dosages had no effects on wakefulness or psychomotor performance in healthy volunteers. No clinically significant interactions have been reported between desloratadine and drugs that inhibit the cytochrome P450 system, nor does the drug potentiate the adverse psychomotor effects of alcohol. Oral desloratadine 5 mg once daily for up to 4 weeks in patients with seasonal allergic rhinitis (SAR) significantly reduced nasal (including congestion) and non-nasal symptoms and improved health-related quality of life compared with placebo. Similar beneficial effects were observed in patients with SAR and coexisting asthma (in whom asthma symptoms and use of beta2-agonists were reduced). Desloratadine 5 mg once daily for 6 weeks significantly improved pruritus and reduced the number of hives compared with placebo in patients with chronic idiopathic urticaria (CIU). Sleep and daytime performance also improved. Desloratadine was well tolerated in clinical trials and had an adverse event profile similar to that of placebo in patients with SAR (with or without asthma) or CIU.

摘要

地氯雷他定是无镇静作用的H1抗组胺药氯雷他定的口服活性主要代谢产物。在各种动物模型中,或者在志愿者中按照推荐成人剂量的9倍给药10天时,该药物均未产生不良心血管影响。治疗剂量对健康志愿者的清醒状态或精神运动表现没有影响。尚未有地氯雷他定与抑制细胞色素P450系统的药物之间存在临床显著相互作用的报道,该药物也不会增强酒精对精神运动的不良影响。与安慰剂相比,季节性变应性鼻炎(SAR)患者口服地氯雷他定5mg每日一次,持续长达4周,可显著减轻鼻部(包括鼻塞)和非鼻部症状,并改善与健康相关的生活质量。在患有SAR且并存哮喘的患者中也观察到了类似的有益效果(哮喘症状减轻,β2激动剂的使用减少)。与安慰剂相比,慢性特发性荨麻疹(CIU)患者口服地氯雷他定5mg每日一次,持续6周,可显著改善瘙痒症状并减少荨麻疹数量。睡眠和日间表现也有所改善。在临床试验中,地氯雷他定耐受性良好,在患有SAR(伴或不伴哮喘)或CIU的患者中,其不良事件谱与安慰剂相似。

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