Division of Pharmacodynamics, Keio University Faculty of Pharmacy, Tokyo, Japan.
Discipline of Pharmacy , Curtin Medical School, Faculty of Health Sciences, Curtin University, Perth, Australia.
Pharmazie. 2024 Jun 1;79(6):98-100. doi: 10.1691/ph.2024.4518.
Urticaria is induced by the histamine released from mast cells which develops wheals (edema) as a visual feature. In clinical practice, second-generation histamine H -receptor blockers are routinely used as the first-line symptomatic treatment for urticaria. Nevertheless, not much research has directly examined the second-generation histamine H-receptor blockers' ability to reduce edema. In this study, we directly evaluated the anti-edematous activities of three second-generation histamine H-receptor blockers available in the market (epinastine hydrochloride, cetirizine hydrochloride, and levocetirizine hydrochloride) using a λ-carrageenan-induced footpad edema model. One hour before the induction of edema with 1% λ -carrageenan injection, all second-generation histamine H -receptor blockers (5, 10, 50 and 100 mg/kg) were subcutaneously administered to rats. At 0.5 and 3 hours after λ -carrageenan administration, the edema volume was evaluated using a Plethysmometer. Epinastine hydrochloride significantly suppressed the edema growth in a dose-dependent manner. Cetirizine hydrochloride showed a slight anti-edematous effect, while levocetirizine significantly inhibited the development of edema in a dose-dependent manner. On the other hand, dextrocetirizine did not prevent edema from growing. In summary, second-generation histamine H -receptor blockers, at least those examined in this study, may be able to reduce the clinical symptoms of urticaria associated with edema. Levocetirizine hydrochloride is also anticipated to have stronger anti-edematous effects than cetirizine hydrochloride because levocetirizine is responsible for cetirizine's anti-edematous activity.
荨麻疹是由肥大细胞释放的组胺引起的，其特征性表现为风团（水肿）。在临床实践中，第二代组胺 H 受体阻滞剂通常被用作荨麻疹的一线对症治疗药物。然而，很少有研究直接检查第二代组胺 H 受体阻滞剂减轻水肿的能力。在这项研究中，我们使用 λ-角叉菜胶诱导的足底肿胀模型直接评估了市场上三种可用的第二代组胺 H 受体阻滞剂（盐酸依匹斯汀、盐酸西替利嗪和盐酸左西替利嗪）的抗水肿活性。在 1% λ-角叉菜胶注射诱导水肿前 1 小时，将所有第二代组胺 H 受体阻滞剂（5、10、50 和 100mg/kg）皮下给予大鼠。在 λ-角叉菜胶给药后 0.5 和 3 小时，使用体积描记器评估水肿体积。盐酸依匹斯汀以剂量依赖性方式显著抑制水肿生长。盐酸西替利嗪显示出轻微的抗水肿作用，而左西替利嗪则以剂量依赖性方式显著抑制水肿的发展。另一方面，右旋西替利嗪不能防止水肿生长。总之，第二代组胺 H 受体阻滞剂，至少在本研究中检查的那些，可能能够减轻与水肿相关的荨麻疹的临床症状。盐酸左西替利嗪也有望比盐酸西替利嗪具有更强的抗水肿作用，因为左西替利嗪负责西替利嗪的抗水肿活性。
