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目的:评价血管升压素受体拮抗剂托伐普坦片对中国健康男性的药效作用和其对血电解质的影响。方法:入选健康男性39名,分四组分别单次口服托伐普坦片15 mg(n=9),30 mg(n=10),60 mg(n=10)和120 mg(n=10),观察48 h内的尿量、血电解质浓度、饮水量变化,以及服药24 h后的体重变化和不良事件。结果:①受试者体重无明显改变,统计学比较无差异。②服药6 h内,6~12 h,12~24 h和24~48 h的4组尿量分别为15 mg组:(1 921±496),(2 977±389),(3 680±724),(3 948±398);30 mg组:(1 361±500),(2 631±661),(3 492±1 094),(4 518±802);60 mg组:(1 268±868),(2 167±1 074),(2 267±1 088),(3 981±1 667);120mg组:(1 302±624),(2 643±1 100),(2 460±660),(4 394±1 132)mL。③血清氯、钠浓度24 h内有升高,48 h恢复服药前水平,氯浓度升高超过正常高限(大于110 mmol.L-1),但未需处理。血钠浓度略高,血钾浓度略低,均在正常范围内变化,无临床意义改变。④血压,心率无明显影响;共有13例次(13/39,33.3%)有口干和口渴的症状,程度轻中度可以耐受。未见严重不良事件。结论:单剂口服托伐普坦片15,30,60或120 mg均有较强的排水利尿作用,且可持续24 h,有剂量依赖性。
OBJECTIVE: To evaluate the pharmacodynamic effects of the vasopressin receptor antagonist tolvaptan tablet on healthy Chinese men and its effect on blood electrolytes. Methods: Thirty-nine healthy male subjects were enrolled in this study. Each group was treated with tolvaptan 15 mg (n = 9), 30 mg (n = 10), 60 mg ), Urine output within 48 h, blood electrolyte concentration, changes in drinking water, and 24 h after taking the weight changes and adverse events. Results: ① There was no significant difference in body weight between the two groups. There was no statistical difference between the two groups. (2) The urine output in 6 h, 6 h, 12 h, 12 h, 24 h and 24 h, 48 h were 15 mg (921 ± 496), (2977 ± 389) and (3680 ± 724 ), (3 948 ± 398); 30 mg group: (1 361 ± 500), (2 631 ± 661), (3 492 ± 1 094), (4 518 ± 802) 868), (2 167 ± 1 074), (2 267 ± 1 088), (3 981 ± 1 667); 120 mg group: (1 302 ± 624), (2 643 ± 1 100), (2 460 ± 660 ), (4 394 ± 1 132) mL. Serum levels of chloride and sodium increased within 24 h and returned to pre-dose levels 48 h after treatment, with elevated chloride concentrations exceeding the normal high limit (> 110 mmol.L -1) without treatment. Slightly higher blood sodium concentration, blood potassium concentration is slightly lower, all within the normal range changes, no clinically relevant changes. ④ There was no significant effect on blood pressure and heart rate; there were 13 cases (13/39, 33.3%) with dry mouth and thirsty symptoms, with moderate and moderate degree of tolerance. No serious adverse events. CONCLUSION: 15, 30, 60 or 120 mg single dose of tolvaptan tablet has a strong drainage and diuretic effect, and can be sustained for 24 h in a dose-dependent manner.