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New H1‐receptor antagonists: clinical pharmacology

机译:新型H1受体拮抗剂:临床药理学

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SummaryThe non‐sedating, second‐generation H1‐receptor antagonists such as terfenadine, astemizole, loratadine and cetirizine differ considerably from each other in their pharmacokinetics and pharmacodynamics. They are generally well absorbed when administered orally. They have extremely variable serum elimination half‐life values. The maximum antihistaminic effect of these medications occurs several hours later than peak serum concentrations do. The duration of the antihistaminic effect is much longer than would be predicted from the serum elimination half‐life values. The relative incidence of anticholinergic and central nervous system adverse effects caused by these medications is similar to that produced by placebo. The introduction of the second‐generation H1‐receptor antagonists represents a major advance in symptomatic therapy of allergic disorders such as allergic rhinitis
机译:摘要非镇静性第二代H1受体拮抗剂,如特非那定、阿司咪唑、氯雷他定和西替利嗪,在药代动力学和药效学上存在很大差异。口服给药时,它们通常被很好地吸收。它们的血清消除半衰期值变化极大。这些药物的最大抗组胺作用比血清峰值浓度晚几个小时。抗组胺作用的持续时间比从血清消除半衰期值预测的要长得多。这些药物引起的抗胆碱能和中枢神经系统不良反应的相对发生率与安慰剂相似。第二代H1受体拮抗剂的引入代表了过敏性鼻炎等过敏性疾病对症治疗的重大进展

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