Antihistamine effects on actual driving performance in a standard test: a summary of Dutch experience, 1989-94

The review summarizes the major results of eight double-blind, placebo-controlled, volunteer studies undertaken by three independent institutions for showing the effects on actual driving performance of "sedating" and "nonsedating" antihistamines (respectively, triprolidine, diphenhydramine, clemastine and terfenadine, loratadine, cetirizine, acrivastine, mizolastine, and ebastine). A common, standardized test was used that measures driving impairment from vehicular "weaving" (i.e., standard deviation of lateral position (SDLP)). Logical relationships were found between impairment and dose, time after dosing, and repeated doses over 4–5 days. The newer drugs were generally less impairing, but differences existed among their effects, and none was unimpairing at doses 1–2 × the currently recommended levels. One or possibly two of the newer drugs possessed both performance-enhancing and -impairing properties, depending on dose, suggesting two mechanisms of action.     

扑苯黄片中三组分的HPLC测定

用ＨＰＬＣ同时测定扑苯黄片中三组分的含量。采用Ｓｐｈｅｒｉｓｏｒｂ ＣＮ柱，操作简单，结果准确。对乙酰氨基酚、盐酸伪麻黄碱、盐酸苯海拉明的回收率分别为１００．３％、９９．８％、９９．５％，ＲＳＤ分别为０．２９％、０．５１％、０．４５％。     

组胺受体在枳实调节小鼠小肠运动中的作用

目的：探讨枳实调节胃肠功能的作用机制,方法：采用活性碳末指示法,以小鼠在灌服不同药物一定时间后小肠碳末推进率为指标分析小肠的运动功能。结果：灌服枳实煎液可明显提高小鼠小肠碳末推进率,此效应可被H1受体拮抗剂苯海拉明阻断而不能被H2受体拮抗剂西米替丁阻断。结论：枳实增强小肠运动功能的作用与H1受体有关。     

远志增强大鼠子宫平滑肌峰电活动实验研究

目的:探讨远志对未孕大鼠子宫平滑肌电活动的影响及其机制.方法:用Biolap410生物机能仪进行记录,分别进行5种阻断剂使用前后,远志水煎醇沉液(以下简称远志)对子宫平滑肌电活动的影响.结果:远志可使未孕大鼠子宫平滑肌的电活动频率加快,持续时间延长,峰面积加大.酚妥拉明、苯海拉明、异博定、消炎痛等能全部或部分阻断其兴奋作用,但阿托品无明显影响.结论:远志对大鼠子宫平滑肌电活动增强作用主要通过H1受体、L型钙通道、α受体发挥作用,也与前列腺素的合成与释放有关,而与M受体无关.     

HPLC法测定复方氨酚苯海拉明片中盐酸麻黄碱和盐酸苯海拉明的含量

目的建立HPLC法测定复方氨酚苯海拉明片中盐酸麻黄碱和盐酸苯海拉明的含量。方法用Kromasil C18(250 mm×4.6 mm,5μm)色谱柱;流动相甲醇-乙腈-1%十二烷基硫酸钠溶液(26∶32∶42)(冰醋酸调pH值3.1),检测波长257 nm。结果线性范围,盐酸麻黄碱:1.228 8~11.059 2μg,r=0.999 9,盐酸苯海拉明:1.216 8~10.951 2μg,r=1.000 0;平均回收率,盐酸麻黄碱98.79%,RSD%=0.59%,盐酸苯海拉明100.44%,RSD%=0.57%。结论本方法简便、准确、灵敏度高、重现性好,可更好地控制本品的质量。     

高效液相色谱法测定美息伪麻拉明分散片中组分含量的研究

目的:采用高效液相色谱法考察并建立了测定复方制剂美息伪麻拉明分散片中对乙酰氨基酚(Par)、氢溴酸右美沙芬(Dex)、盐酸苯海拉明(Dip)和盐酸伪麻黄碱(Pse)的含量。方法:色谱柱为Diamonsil-C_(18)(200mm×4.6mm,5μm),测定Par用乙腈-甲醇-0.05mol·L~(-1)磷酸二氢钾溶液(5:1:25)为流动相,检测波长为245nm,测定Dex、Dip和Pse用pH3.3甲酸钠缓冲液-乙腈-甲醇-十二烷基硫酸钠(32:28:5:0.06=V:V:V:W)为流动相,检测波长为256nm。结果:Par、Dex、Pse、Dip浓度在2.06～20.60μg·mL~(-1),0.11～1.06,0.20～2.02,0.10～1.01mg·mL~(-1)范围内与峰面积呈良好的线性关系,r分别为0.999 7,0.999 4,0.999 5,0.999 7。平均回收率依次为100.2％,99.28％,100.6％,100.7％。结论:本法精密度好,结果准确可靠。适用于该复方制剂的质量检验分析。     

组胺对分化的3T3L1细胞UCP2表达的影响

目的 探索组胺对脂肪细胞能量代谢的影响及其作用机制。方法 培养3T3L1细胞，诱导分化为白色脂肪细胞，运用RT-PCR以及Western-blot技术检测组胺和苯海拉明对白色脂肪细胞中UCP2 mRNA水平和蛋白质表达水平的影响。结果 白色脂肪细胞在不同剂量组组胺的刺激下，UCP2的表达值在不同剂量组之间存在显著差异（P〈0.05），UCP2的表达水平随着组胺剂量的增加而增加，在组胺剂量为30μmol·L^-1时达到最高值；在相同剂量组胺下，观察不同时间对细胞内UCP2表达的影响，结果发现，不同时间组之间也存在显著性差异（P〈0.05），当时间为6h时，UCP2表达量达到最高；苯海拉明剂量依赖性地抑制脂肪细胞UCP2 mRNA水平和蛋白质的表达。结论 组胺可以刺激分化成熟的3T3L1细胞中UCP2的表达，其机制与激活H1受体有关。     

侧脑室注射组织胺对大鼠胃酸分泌的影响

从侧脑室注射组织胺观察其对大鼠胃酸分泌影响的实验表明,组织胺有刺激胃酸分泌的作用,此作用可分别被H_1受体阻断剂苯海拉明和H_2 受体阻断剂甲氰咪胍部分阻断。提示了侧脑室注射组织胺增加胃酸分泌的效应是通过H_1和H_2受体实现的。     

Diphenhydramine produces local cutaneous analgesia in response to dorsal skin noxious stimuli in the rat

Although diphenhydramine has been shown to produce longer duration of spinal block than lidocaine, few studies disclose its skin infiltrative anesthesia when compared with a long‐lasting local anesthetic, bupivacaine. The purpose of this study was to investigate whether diphenhydramine elicited cutaneous analgesia in comparison with bupivacaine. After inhibition of cutaneous trunci muscle reflex via subcutaneous injection of drugs in rats, we examined the local anesthetic effect of diphenhydramine and bupivacaine as infiltrative cutaneous analgesia in a dose‐dependent fashion. We showed that diphenhydramine, as well as bupivacaine displayed a dose‐dependent cutaneous analgesia in response to dorsal cutaneous noxious stimuli. The relative potency (50% effective dose) was bupivacaine (0.023 [0.013–0.035]%) > diphenhydramine (0.078 [0.068–0.091]%; P < 0.001). On an equipotent basis, diphenhydramine had a similar duration of action to bupivacaine. Neither local injection of saline nor intraperitoneal administration of a large dose of diphenhydramine or bupivacaine produced cutaneous analgesia (data not shown). We conclude that diphenhydramine is less potent than bupivacaine at producing cutaneous analgesia. At equipotent doses for infiltrative cutaneous analgesia, the duration of action of diphenhydramine is equal to that of bupivacaine.