The aim of the present study was to analyze the protective and hemodynamic effects of dexmedetomidine in hypertensive cerebral hemorrhage (HCH) patients during perioperative period. In total, 50 HCH patients were selected and randomly divided into two groups, one group was administered with dexmedetomidine and the other groups with midazolam. The mean arterial pressure (MAP), heart rate (HR) and blood oxygen saturation (SpO2) were monitored in the two groups of patients before and during the operation. The MAP, HR, SpO2 and PETCO2 recorded 5 min after admission into the operation room was considered T1, the same parameters recorded 10 min after drug administration were considered T2, just after starting the operation were considered T3 and 30 min after start of operation were considered T4. The preoperative sedation and analgesia were evaluated by the Ramsay scoring method and the neuron-specific enolase (NSE) and S100 protein (S100β) were estimated using ELISA. The patients of the midazolam group experienced mild respiratory depression during the period of sedation. Levels of, MAP, HR and PETCO2 were significantly increased whereas SPO2 was decreased (P<0.05). The MAP, HR, SPO2 and PETCO2 were stable during the period of sedation (P>0.05). The plasma concentrations of epinephrine and norepinephrine at T1 were similar in the two groups (P>0.05), but decreased after drug administration. This decrease was more prominent in the dexmedetomidine group patients (P<0.05) than midazolam group patients. The epinephrine and norepinephrine concentrations just after starting operation (T3) were higher than the basal level (T1) in the midazolam group, but close to the basal level in the dexmedetomidine group (P<0.05). The serum concentration of NSE and S100β in the two groups showed no difference (P>0.05) at the end of operation (T5), but after 24 h of operation (T7) NSE and S100β in the dexmedetomidine group were significantly lower compared to the midazolam group (P<0.05). In conclusion, the administration of dexmedetomidine for patients with HCH during perioperative period is safe and serves as an effective sedative, without causing respiratory depression and does not influence stable haemodynamics with certain brain protective effect.

Dexmedetomidine [Dex] is an α2-adrenoceptor agonist which provides sedation, analgesia and anxiolytic effects, thus making it a potentially useful anesthetic premedication. A number of clinical trials have been conducted to compare the sedative effect of Dex versus midazolam [Mdz], a conventional sedative agent in anesthesia. Nevertheless, consensus has not been achieved on which agent is superior to the other in terms of the overall benefit to patients. In this study, we have isolated four independent studies containing randomized, controlled, clinical trials on patients and compare the efficacy and safety of these two agents as a premedication in anesthesia. In the studies of the catheter ablation of atrial fibrillation and surgical correction of scoliosis deformities, Dex treatment resulted in a better sedative and analgesic effects, reflected by a reduced pain, a lower dose of analgesic agents required, and greater sedation scores than Mdz treatment. Similarly, intranasal Dex premedication in the children's dental rehabilitation and adenotonsillectomy, Dex also yielded a better efficacy. Taken together, Dex provides an improved premedication for sedation and analgesia, as well as the protective effects on the end organs. This study has provided evidence for optimized sedation protocol in anesthesia. J o u rn al of A n e s th es ia & C li n ic a l Resea rc h

Protein kinase C (PKC) plays a key role in neurotransmission in the central nervous system, and targeting PKC domain is considered as a strategy to modulate the anaesthetic effects. In this study, we described a synthetic pipeline to perform high-throughput virtual screening against a large library of 3D structural natural products released recently in order to discover those potential PKC modulators. A total of 100 natural products with top scores were raised, from which 12 promising candidates were tested to determine their inhibitory potencies against PKC. As might be expected, the promiscuous kinase inhibitor staurosporine showed a high PKC inhibitory activity (IC50 = 64 nM), and other two tested compounds, i.e. fisetin and tetrahydropapaverine, were also highly potent with their activities at nanomolar level (IC50 = 370 and 190, respectively).