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苯二氮?类药物有着易变的剂量反应,以往的研究对其血浆浓度和效果之间的关系估价不同.苯二氮?类药物的PKa值和类脂化合物溶解度能使其迅速进入中枢神经系统(CNS)并达到血液和脑脊液(CSF)间的快速均衡,因而适于研究药物剂量—效应关系.患者口服3-羟安定后所测得的血浆非结合3-羟安定与CSF中该药水平密切相关(r=0.81).因此,与CNS中神经元所接触的CSF药物浓度值应能反映此药物的浓度—效应关系.26名泌尿外科术前的男性病人在腰麻前1～4小时口服3-羟安定,剂量10～40mg不等.在腰麻前抽取腰部CSF并同时采取静脉血样分别测定药物浓度.对麻醉前的镇静程度用6个级别加以评价.结果口服药物剂量为0.123～0.597mg/kg,平均0.339mg/kg(SD0.099).血浆3-羟安定水平为296～
Benzodiazepines have a variable dose response, and previous studies have evaluated the relationship between plasma concentration and effect.Phenylbenzazepines PKa values and lipid compound solubility make it rapidly enter the central nervous system System (CNS) and achieve rapid equilibration between the blood and cerebrospinal fluid (CSF), thus making it suitable for investigating dose-response relationships in patients.Patients with plasma unconjugated 3-hydroxybalance and CSF as measured after oral 3- (R = 0.81) .Therefore, the value of CSF drug concentration in contact with neurons in the CNS should reflect the concentration-response relationship of the drug.26 male patients undergoing preoperative urology performed 1 to 4 Hour oral administration of 3-hydroxyAb level, the dose of 10 ~ 40mg range in the waist before spinal anesthesia to take the waist and taking venous blood samples were measured drug concentration.The sedation level before anesthesia was evaluated using 6 levels.Results Oral drug dose was 0.123 ~ 0.597mg / kg, an average of 0.339mg / kg (SD0.099) plasma 3-hydroxyblock level of 296 ~