Osterlund A, Arlander E, Eriksson L I, Lindahl S G
Department of Anaesthesiology and Intensive Care, Karolinska Hospital and Institute, Stockholm, Sweden.
Anesth Analg. 1999 Jan;88(1):160-5. doi: 10.1097/00000539-199901000-00030.
Sameridine has both local anesthetic and partial mu-opioid receptor agonistic properties. The aim of this single-blinded, randomized, three-way cross-over study of 12 subjects was to investigate the effects on resting ventilation of two doses of sameridine: 0.15 mg/kg (S-Small) and 0.73 mg/kg (S-Large) compared with 0.10 mg/kg morphine. Each drug was infused IV over 20 min. Ventilation was measured by pneumotachography and in-line capnography, and sedation was rated by the subjects using a visual analog scale (VAS). Plasma was collected and analyzed for sameridine and morphine. At the end of drug infusion, minute ventilation (VE) and tidal volume (VT) were reduced in the S-Large group, and VE was reduced in the morphine group. End-tidal CO2 increased in both groups (P < 0.05), but respiratory rates remained unchanged. In the S-Small group, no ventilatory changes were recorded. In the S-Large group, the median sedation score was 6.8 cm with corresponding values in the morphine and S-Small groups of 3.3 and 2.5 cm, respectively. There was a relationship between the plasma concentration of sameridine and the depression of ventilation. We conclude that sameridine influences resting ventilation and that this effect is directly related to plasma concentrations of sameridine. From a ventilatory aspect, a clinical dose of sameridine with both local anesthetic and opioid properties seems safe.
Sameridine, a molecule with both local anesthetic and analgesic properties, impaired resting ventilation after a large IV dose (0.73 mg/kg), more so than 0.10 mg/kg IV morphine. A clinical dose of sameridine (0.15 mg/kg) did not have any effects on ventilation.
沙美替定具有局部麻醉和部分μ-阿片受体激动特性。这项针对12名受试者的单盲、随机、三向交叉研究的目的是，研究两剂量沙美替定（0.15mg/kg，小剂量沙美替定[S-小剂量组]；0.73mg/kg，大剂量沙美替定[S-大剂量组]）与0.10mg/kg吗啡相比，对静息通气的影响。每种药物均静脉输注20分钟。通过呼吸流速描记法和在线二氧化碳描记法测量通气，受试者使用视觉模拟量表（VAS）对镇静程度进行评分。采集血浆并分析其中的沙美替定和吗啡含量。在药物输注结束时，S-大剂量组的分钟通气量（VE）和潮气量（VT）降低，吗啡组的VE降低。两组的呼气末二氧化碳均升高（P<0.05），但呼吸频率保持不变。在S-小剂量组中，未记录到通气变化。在S-大剂量组中，镇静评分中位数为6.8cm，吗啡组和S-小剂量组的相应值分别为3.3cm和2.5cm。沙美替定的血浆浓度与通气抑制之间存在关联。我们得出结论，沙美替定影响静息通气，且这种作用与沙美替定的血浆浓度直接相关。从通气角度来看，具有局部麻醉和阿片样特性的临床剂量沙美替定似乎是安全的。
沙美替定是一种兼具局部麻醉和镇痛特性的分子，静脉大剂量（0.73mg/kg）给药后会损害静息通气，比静脉注射0.10mg/kg吗啡更明显。沙美替定的临床剂量（0.15mg/kg）对通气没有任何影响。
