Cocaine and local anesthetics: Stimulant activity in rats with nigral lesions

Cocaine and several other local anesthetics were tested for their ability to induce rotational behavior in rats with unilateral 6-hydroxydopamine lesions of substantia nigra. Acute administration of bupivacaine, chloroprocaine, etidocaine, lidocaine, mepivacaine, procaine or tetracaine failed to induce active rotation in this sensitive assay of dopamine agonist activity. On the other hand, cocaine or dimethocaine treatment induced active rotation directed ipsilaterally to the lesioned side, indicating indirect dopamine agonist activity. Repeated administration of cocaine or dimethocaine at 1-week intervals resulted in increased rotational response (i.e., sensitization) while there was no suggestion of sensitization or induction of rotational behavior after weekly repeated administration of procaine or tetracaine. Daily administration of mepivacaine, procaine or tetracaine for 5 days also failed to induce rotation. Dimethocaine thus was found similar to cocaine and different from the other local anesthetics tested both in terms of frank stimulant activity and development of sensitization upon repeated administration.     

H-point计算分光光度法研究及其在复方盐酸丁卡因注射液中的应用

介绍几种Ｈ－ｐｏｉｎｔ法,并与常见的计算分光光度法进行了比较。将Ｈ－ｐｏｉｎｔ法用于复方盐酸丁卡因注射液测定的数据处理,表明Ｈ－ｐｏｉｎｔ法有效地消除干扰,有较高的精密度和准确度。盐酸丁卡因回收率为：Ｈ－ｐｏｉｎｔ法１０１．０％,ＲＳＤ为２．７％（ｎ＝７）,Ｋ系数Ｈ－ｐｏｉｎｔ法９９．１％,ＲＳＤ为１．８％（ｎ＝７）,三波长Ｈ－ｐｏｉｎｔ法９９．６％,ＲＳＤ为１．４％（ｎ＝７）。     

1%盐酸丁卡因凝胶在男性患者留置导尿术中的应用效果分析

目的 探讨1%盐酸丁卡因凝胶在男性患者留置导尿术中的应用效果.方法 选取209例需留置导尿的手术患者按完全随机分组的方法 分为观察组(n=107)和对照组(n=102).观察组采用1%盐酸丁卡因凝胶作为润滑剂行导尿术,对照组采用石蜡油作为润滑剂行导尿术,比较两组患者一次留置尿管成功率、全身麻醉前(T1)和麻醉苏醒期(T2)患者的血压、心率值以及躁动、疼痛评分.结果 两组患者的一次性置管成功率均较高96.26%(103/107)、93.14%(95/102),差异无统计学意义(P>0.05);T2期观察组患者的收缩压、舒张压[(122.96±11.50)、(76.23±6.28) mmHg]显著低于对照组[(146.92±8.92)、(89.48±4.33) mmHg],差异有统计学意义(P<0.001);T2期观察组患者的躁动评分、数字分级法(NRS)评分、Wong-Baker面部表情量表法(WBFPS)评分为[(0.80±0.64)、(2.65±0.88)、(1.47±0.49) 分]与对照组评分[(1.25±1.00)、(3.82±1.18)、(2.55±0.88) 分]相比较,差异有统计学意义(P<0.001).结论 在男性患者留置导尿术前应用盐酸丁卡因凝胶润滑尿道及导尿管,效果优于用石蜡油润滑尿道及导尿管.     

盐酸丁卡因胶浆的研制与质量控制

目的研制一种以泊洛沙姆为基质、含有盐酸丁卡因的胶浆,并制定质量控制标准。方法采用分光光度法对盐酸丁卡因进行含量测定。结果盐酸丁卡因的平均回收率为99．87％。RSD为0．45％。结论用分光光度法测定盐酸丁卡因胶浆中盐酸丁卡因的含量是可行的．本法简便、准确、重现性好。尤其适用于医院制剂快检。     

Methemoglobinemia and acute hemolysis after tetracaine lozenge use

Acquired methemoglobinemia is a rare but severe condition associated with oxidizing stressors, most notably medications. Although the symptoms can be life threatening, they usually respond promptly to exposure cessation and methylene blue injection. We describe the first case of methemoglobinemia associated with tetracaine lozenge use. A previously healthy 33-year-old man was admitted with fever, respiratory distress, cyanosis, and acute hemolysis. Physical findings and chest radiograph were normal. Low pulse oximetry readings contrasted with normal partial pressure of oxygen and calculated oxygen saturation. The methemoglobin level was 10.8%. The patient recovered with methylene blue injection and blood transfusions. He reported recent self-medication with tetracaine lozenges for a sore throat during a flu-like illness. No other cause of methemoglobinemia was found.     

荧光分光光度法测定利多卡因丁卡因注射液中盐酸丁卡因的含量

目的:建立荧光分光光度法测定利多卡因丁卡因注射液中盐酸丁卡因的含量.方法:以311nm为激发波长,370 nm为发射波长,测定相对荧强度.结果:盐酸丁卡因在0.4～1.2μg·ml-1浓度范围与相对荧光强度呈良好线性关系,r=0.999 8.平均回收率为100.1%,RSD0.8%.结论:本品专属性强,可用于该制剂中盐酸丁卡因的含量测定.     

高效液相色谱法测定复方庆大霉素膜中盐酸丁卡因的含量

目的 建立高效液相色谱法测定复方庆大霉素膜中盐酸丁卡因含量的方法.方法 色谱柱为Kromasil C18柱,流动相为甲醇-无水乙醇-水-三乙胺(70∶10∶20∶0.05),检测波长为310nm,流速1.0mL·min-1.结果 盐酸丁卡因在2.24～22.42μg·mL-1浓度范围内呈现良好的线性关系,回归方程:y=-23.1819X 109.46,r=0.9999;平均回收率为100.2%(n=9).结论 该方法简便、快速、准确、灵敏度高,适用于复方庆大霉素膜中盐酸丁卡因的含量测定.     

地卡因粘膜表面麻醉致严重全身毒性反应的救治与预防

本文报告１例需行纤维叫做镜检查而行地卡因咽部粘膜表面麻醉引起全身毒性反应致死的病例，以期引起临床工作者的高度重视。对地卡因致全身毒性反应的药理学基础，临床表现，抢救及预防措施进行了讨论。     

Comparison of hemodynamic and anesthetic effects of hyperbaric bupivacaine and tetracaine in spinal anesthesia

Purpose.To compare the anesthetic and hemodynamic effects and the predictive factor of anesthesia level of commonly used preparations of hyperbaric bupivacaine and tetracaine in spinal anesthesia. Methods.Two hundred patients aged 40 to 75 years with ASA physical status I or II were anesthetized spinally via the L4–5 interspace using 0.5% hyperbaric bupivacaine in 7.27% glucose (Bupivacaine group, n = 100) or 0.5% hyperbaric tetracaine dissolved in a 10% glucose solution (Tetracaine group, n = 100) in a lateral position. The volume of anesthetic used was decided by the resident according to the surgical procedure. Patients were returned to the supine position immediately after drug injection. Blood pressure, heart rate, and anesthesia level tested by cold sensation were measured for 30min. Results.Blood pressure and heart rate decreased significantly but without any differences between the groups. The volume of drug used was significantly larger in the Bupivacaine group (2.6 ± 0.5ml) than in the Tetracaine group (2.1 ± 0.4ml) to obtain the same maximum anesthesia level. The time to reach the maximum anesthesia level was significantly longer in the Bupivacaine group (18 ± 7min) than in the Tetracaine group (15 ± 6min). The volume of the drug was the only predictive factor of the maximum anesthesia level in both groups: Level (as expressed by the number of anesthetized segments from S5 to cephalad) = 1.55 × (volume in ml) + 13.06 in the Bupivacaine group, and 2.59 × (volume) + 11.46 in the Tetracaine group. Conclusion.In spinal anesthesia, hyperbaric tetracaine in 10% glucose induced a faster and higher spread of anesthesia than hyperbaric bupivacaine in 7.27% glucose without any differences in hemodynamics.