Pilocarpine Disposition and Salivary Flow Responses Following Intravenous Administration to Dogs
Pilocarpine Disposition and Salivary Flow Responses Following Intravenous Administration to Dogs
复制标题
狗静脉注射后毛果芸香碱的分布和唾液流量反应
DOI：
10.1023/a:1015814730154
复制
发表时间：
1992
影响因子：
3.7
通讯作者：
P. Kramer
中科院分区：
文献类型：
--
作者：
M. Weaver;J. Tanzer;P. Kramer
口服匹罗卡品可增加口干(口干)患者的唾液流量。本研究检测了犬静脉注射硝酸匹罗卡品的药代动力学和药效学反应(唾液)。在225-600微克/公斤的剂量范围内呈线性处置；血药浓度为10-120微克/公斤。消除迅速，一般是两相的，最终消除半衰期约为1.3小时。毛果芸香碱的全身清除量高(2.22±0.49 L/kg/小时)，其稳态分布体积(2.3±0.64 L/kg)与许多其他基本药物相当。所有剂量的匹罗卡品均可引起可测量的颌下和腮腺唾液流量，并可随时间保持恒定。累积颌下唾液流量与毛果芸香碱总剂量呈线性相关。血浆匹罗卡品浓度与稳态和输注后颌下唾液流量均呈线性相关。
Oral doses of pilocarpine increase salivary flow rates in patients afflicted with xerostomia (dry mouth). This study examined the pharmacokinetics of and a pharmacodynamic response (salivation) to intravenous pilocarpine nitrate administration in dogs. Disposition was linear over a dose range of 225–600 µg/kg; plasma concentrations were 10–120 µg/L. Elimination was rapid and generally biphasic, with a terminal elimination half-life of approximately 1.3 hr. The systemic clearance of pilocarpine was high (2.22 ± 0.49 L/kg/hr) and its steady-state volume of distribution (2.30 ± 0.64 L/kg) was comparable to that of many other basic drugs. All doses of pilocarpine induced measurable submaxillary and parotid salivary flow rates which could be maintained constant over time. Cumulative submaxillary saliva flow was linearly related to total pilocarpine dose. Plasma pilocarpine concentration was linearly related to both steady-state and postinfusion submaxillary salivary flow rates.