Bousquet J, Lebel B, Chanal I, Morel A, Michel F B
Clinique des Maladies Respiratoires, Montpellier, France.
J Allergy Clin Immunol. 1988 Nov;82(5 Pt 1):881-7. doi: 10.1016/0091-6749(88)90094-2.
Most oral drugs used for the treatment of allergic rhinitis are classified as H1-receptor antagonists, and although they represent major sales throughout the world, their mechanism of action is still poorly known. In an attempt to understand better the in vivo therapeutic effects of these drugs, a double-blind, crossover study was carried out. The study compared the effects of terfenadine and loratadine, nonsedative H1-receptor antagonists, on the immediate allergic response of the upper airways to challenge with orchard-grass pollens in 14 highly allergic subjects. Increasing numbers of pollen grains were insufflated into the nostrils, and the response of the subjects was assessed by examining symptoms and measuring the release of histamine and prostaglandin D2 in nasal secretions. Each drug was administered for a week before challenge. This study demonstrated the clinical efficacy of both drugs by comparison to that of a control day, since symptoms were observed for a significantly (p = 0.014) greater number of pollen grains. Only one patient had a significant release of histamine when they were treated with loratadine versus 10 during control day (p less than 0.0023) and six when they were treated with terfenadine (p less than 0.01). Prostaglandin D2 release occurred with a higher allergen dose when patients were treated with both drugs. This study indicates that some H1 antagonists also possess antiallergic activities.
大多数用于治疗过敏性鼻炎的口服药物被归类为H1受体拮抗剂，尽管它们在全球范围内销售额可观，但其作用机制仍鲜为人知。为了更好地了解这些药物的体内治疗效果，开展了一项双盲交叉研究。该研究比较了非镇静性H1受体拮抗剂特非那定和氯雷他定对14名高度过敏受试者上呼吸道对果园草花粉激发的即时过敏反应的影响。将越来越多的花粉颗粒吹入鼻孔，并通过检查症状以及测量鼻分泌物中组胺和前列腺素D2的释放来评估受试者的反应。每种药物在激发前服用一周。与对照日相比，该研究证明了两种药物的临床疗效，因为观察到症状出现时的花粉颗粒数量显著更多（p = 0.014）。使用氯雷他定治疗时，只有一名患者组胺显著释放，而对照日有10名（p < 0.0023），使用特非那定治疗时有6名（p < 0.01）。使用两种药物治疗时，前列腺素D2释放发生在更高的过敏原剂量下。这项研究表明一些H1拮抗剂也具有抗过敏活性。
