Therapeutic effects of xylazine and dexmedetomidine in establishing the model of spinal cord inj ury in beagle dogs / 西安交通大学学报(医学版)

ABSTRACT:Objective To observe the anesthetic effects of xylazine and dexmedetomidine in establishing the model of spinal cord injury in beagle dogs.Methods Thirty female beagle dogs were randomly divided into 3 groups with 1 0 in each:xylazine group (group S ), dexmedetomidine group (group D ), and xylazine +dexmedetomidine group (group S+D).Basal anesthesia with ketamine was performed in all the dogs.Then group S was intramuscularly injected with xylazine discontinuously, group D was intravenously injected with dexmedetomidine 2μg/(kg·h)continuously,but group S+D was injected with xylazine and dexmedetomidine in combination.The heart rate (HR),respiratory frequency (RR),Ramsay score and spasm index (SI)were observed at the time of skin incision (T1),after the beginning of the operation 30 min (T2),before the end of the operation 30 min (T3),and the end of the operation(T4);and the usage of anesthetics was recorded.Results Compared with that in groups S and D,the usage of xylazine and dexmedetomidine in group S+D was decreased by 1/2 and 1/4,respectively (P<0.01),but HR and RR did not change significantly;the sedative effect was superior to that in S.No obvious increase in muscular tensility in the foreleg was observed before operation.Conclusion Xylazine and dexmedetomidine used in combination to establish the model of spinal cord injury in beagle dogs have advantages of better sedative effect,less respiratory depression and lower dosage of anesthetic drugs.

Sedative Effect of Sophora flavescens and Matrine

The present study investigated the sedative effects of Sophora flavescens (SF) and its bioactive compound, matrine through performing locomotor activity test and the electroencephalography (EEG) analysis in the rat. The underlying neural mechanism of their beneficial effects was determined by assessing c-Fos immunoreactivity and serotonin (5-HT) in the brain utilizing immunohistochemical method and enzyme-linked immunosorbent assay. The results showed that SF and matrine administration had an effect on normalization of caffeine-induced hyperactivity and promoting a shift toward non-rapid eye movement (NREM) sleep. c-Fos-immunoreactivity and 5-HT level in the ventrolateral preoptic nucleus (VLPO), a sleep promoting region, were increased in the both SF and matrine-injected groups. In conclusion, SF and its bioactive compound, matrine alleviated caffeine-induced hyperactivity and promoted NREM sleep by activating VLPO neurons and modulating serotonergic transmission. It is suggested that SF might be a useful natural alternatives for hypnotic medicine.

Sedative Effect of Sophora flavescens and Matrine

The present study investigated the sedative effects of Sophora flavescens (SF) and its bioactive compound, matrine through performing locomotor activity test and the electroencephalography (EEG) analysis in the rat. The underlying neural mechanism of their beneficial effects was determined by assessing c-Fos immunoreactivity and serotonin (5-HT) in the brain utilizing immunohistochemical method and enzyme-linked immunosorbent assay. The results showed that SF and matrine administration had an effect on normalization of caffeine-induced hyperactivity and promoting a shift toward non-rapid eye movement (NREM) sleep. c-Fos-immunoreactivity and 5-HT level in the ventrolateral preoptic nucleus (VLPO), a sleep promoting region, were increased in the both SF and matrine-injected groups. In conclusion, SF and its bioactive compound, matrine alleviated caffeine-induced hyperactivity and promoted NREM sleep by activating VLPO neurons and modulating serotonergic transmission. It is suggested that SF might be a useful natural alternatives for hypnotic medicine.

Research on hypnotic and anticonvulsant activities of total alkaloids in leaves of eucommia ulmoides / 中草药·英文版

Objective: To study the hypnotic and anticonvulsant activities of the leaves of Eucommia ulmoides (LEU), the total alkaloids were extracted from LEU using water-acid method. Methods: Mice were divided into five groups, including groups contained total alkaloids in three different doses, negative and positive control groups. Direct hypnotic experiment in mice, pentobarbital sodium synergistic experiment, and anticonvulsant experiment were used. The numbers of spontaneous activities, sleep rate, sleep latency, sleep time, convulsion rate, and convulsion latency of the mice were recorded and analyzed. Results: The total alkaloids from LEU could increase the sleep rate, significantly lengthen the sleep time, and shorten the sleep latency of mice. Even the low dose of total alkaloids (0.33 g/kg) showed significantly different activities with negative control group (physiological saline) with the synergistic effect of the superthreshold dose of pentobarbital sodium. Furthermore, the total alkaloids efficiently inhibited the convulsion caused by nikethamide. Conclusion: The total alkaloids from LEU have the excellent sedative, hypnotic, and anticonvulsant activities in mice, with high safety and little drug side effects. Therefore, they have the protential development prospects in sedative-hypnotic drugs. © 2014 Tianjin Press of Chinese Herbal Medicines.

Comparison of Treatment Response of Antipsychotics According to Sedative Effect in the Treatment of Patients with Delirium / 대한정신약물학회지

OBJECTIVE: The purpose of the study is to compare treatment responses and side effects of antipsychotic medications in hospitalized delirium patients. METHODS: Among delirium patients hospitalized 23 less-sedating agent group and 26 sedating agent group were included in the study. Less sedating agents are haloperidol and risperidone, and sedating agents are olanzapine and quetiapine. All candidates underwent Clinical Global Impression Scale (CGI), Delirium Rating Scale-Revised 98 (DRS-R 98), and Extrapyramidal Symptom Rating Scale during the treatment period. At baseline, 1st day, 2nd day, 3rd day, 4th day, 5th day, 6th day, 7th day, 10th day, and 14th day, we compared treatment responses and side effect profiles between two groups. RESULTS: The remission defined as below 16 score of DRS-R 98, and the remission rate of both group were 78.3% at less-sedating agent group, and 80.8% at sedating agent group. They showed no difference each other. Time to remission of less-sedating group was significantly shorter than sedating group, they were 2.89+/-1.41 days at less-sedating agent group, and 5.76+/-4.45 days at sedating agent group (p=0.015). After 2 days of treatment, less-sedating agent group showed greater decrement of CGI-S score than sedating agent group, the score were 3.22+/-1.20 at less-sedating agent, and 4.00+/-1.22 at sedating agent group (p=0.030). And DRS-R 98 score after 2 days of treatment showed difference between both group, less-sedating agent group was 17.00+/-8.88, and sedating group was 22.72+/-8.49, they were different statistically (p=0.044). The mean dosage of each drugs were haloperidol 1.93 mg, risperidone 0.71 mg, olanzapine 3.75 mg, and quetiapine 46.09 mg. But there were no significant differences of rate of adverse effects. CONCLUSION: There were no differences of total remission rate and rate of adverse effects between two groups for 2 weeks. But less-sedating agent group showed shorter time to remission and shorter duration of medication than sedating agent group. This study suggests that less-sedating agents are more suitable for early days of delirium treatment.

Tamizaje fitoquímico del Malvaviscus penduliflorus que crece en Cuba / Phytochemical screening of Malvaviscus penduliflorus growing in Cuba

Las flores de la especie Malvaviscus penduliflorus Cav, conocida popularmente en Cuba como pasiflora, se emplean como sedante en forma de decocción. Hasta el momento, sin embargo, no ha sido publicado ningún estudio sobre su composición química. OBJETIVO: realizar un tamizaje fitoquímico de los extractos acuosos de las flores y hojas de la especie M penduliflorus. MÉTODOS: se recolectaron las hojas y las flores frescas, se lavaron, desinfectaron y extrajeron a reflujo con agua (1:10) durante 2 h, de forma independiente. Los extractos se filtraron y se les hicieron las pruebas fitoquímicas de identificación. RESULTADOS: entre los grupos de compuestos identificados en los 2 extractos se encontraron saponinas, azúcares, alcaloides y flavonoides. Teniendo en cuenta la presencia de compuestos como flavonoides y alcaloides en las partes aéreas del M penduliflorus, así como los efectos farmacológicos reportados para extractos de esta especie, sería interesante realizar nuevos estudios que aporten evidencias sobre su eficacia y seguridad, como forma de avalar sus usos tradicionales

The Malvaviscus penduliflorus Cav species flowers popularly known in Cuba as pasiflora are used as sedative in the brew form. Until now, however, there isn't any study on its chemical composition. OBJECTIVE: to perform a phytochemical screening of aqueous extracts from the flowers and leaves of M. penduliflorus species. METHODS: the dry fresh leaves and flowers were washed, disinfected to extract with water reflow (1:10) during 2 h in an independent way. Extracts were filtered and underwent the phytochemical identification tests. RESULTS: among the compounds identified in the two groups were included the saponines, sugars, alkaloids and flavonoids. Taking into account the presence of compounds like the flavonoids and the alkaloids in aerial parts of M penduliflorus, as well as the pharmacological effects reported for the extracts of this species, it will be interesting to perform new studies providing evidences on its effectiveness and safety, as a way to assess its traditional uses

Locomotor model based on accumulate peripheral active time percent in ICR mice / 中国药理学通报

Aim To establish a novel locomotor model based on accumulate peripheral active time percent(APATP)in ICR mice induced by pentobarbital sodium(PB)and diazepam.Methods Total distance, accumulate peripheral active time and accumulate peripheral time were aquired from video tracking system with computer, and APATP in all groups was fit and got correspondent parameters with Drugs Analysis System 2.0. Logarithm of area under the curve(lgAUC_(0-60)), minimum APATP(lgP_(min)), and half time of steady-state locomotor activity(T_(1/2α)) were ready for evaluation.Results APATP decreased with time increasing in all groups gradually, and PB 10 mg·kg~(-1) and PB 15 mg·kg~(-1) had similar tendency.PB 10 mg·kg~(-1) and PB 15 mg·kg~(-1) all decreased APATP significantly throughout the time course.APATP in all mice was fit to kinetics equation.Compared with norm group, PB 5 mg·kg~(-1) decreased three parameters slightly(all P >0.05), and PB 10 mg·kg~(-1) and PB 15 mg·kg~(-1) had similar tendency.PB 10 mg·kg~(-1) (all P <0.05) and PB 15 mg·kg~(-1) (P <0.01, P <0.01 and P >0.05)decreased parameters.Compared with PB 10 mg·kg~(-1) , PB 15 mg·kg~(-1) increased reversely(P >0.05, P <0.05 and P <0.05).lgAUC_(0-60) and lgPmin were both linar with total distance(r 2=1.0000 and r 2=0.9995, both P <0.01), T_(1/2α) also showed similar tendcency as well as total distance.Refering PB 10 mg·kg~(-1) as positive drugs and norm as negative control, diazepam 2 mg·kg~(-1) and 4 mg·kg~(-1) depressed all parameters significantly compared with norm group(all P <0.01) and were similar as PB 10 mg·kg~(-1) , which indicated that sedative effect of diazepam was the same as PB 10 mg·kg~(-1) .Conclusion Locomotor activity model based on APATP may be used to evaluate drug effects on lomocotor activity induced by sedative hypnotics.

Anxiolytic and sedative effects of a combined extract of Passiflora alata Dryander and Valeriana officinalis L. in rats / Efeito ansiolítico e sedativo do extrato combinado de Passiflora alata Dryander e Valeriana officinalis L. em ratos

Este trabalho investigou o efeito do extrato combinado de Passiflora alata Dryander e Valeriana officinalis L. (EPV) em ratos submetidos aos testes do labirinto em cruz elevado (LCE) e campo aberto (TCA). Nenhum efeito foi detectado após o tratamento agudo ou repetido por 3 ou 7 dias com EPV (5, 10 or 20 mg/kg, gavagem) no LCE e TCA. Entretanto, ratos tratados por 15 dias com EPV (20 mg/kg) mostraram aumento na porcentagem de entradas e tempo gasto nos braços abertos no LCE, sem alterar a atividade locomotora no TCA, comparado ao controle. Diazepan (droga de referência, i.p.), aumentou os mesmos parâmetros analisados no LCE e OFT após o tratamento agudo ou por 15 dias. O tratamento agudo com 300 ou 600 mg/kg do EPV diminuiu significativamente a atividade locomotora no TCA. Estes resultados mostram que EPV produz efeito ansiolítico e sedativo, com ampla margem de segurança para o efeito ansiolítico.

This work investigated the effects of a combined extract of Passiflora alata Dryander and Valeriana officinalis L. (EPV) in rats under going elevated plus maze (EPM) and open- test (OFT). No effects were detected after acute or repeated (3 or 7-days) treatment with EPV (5, 10 or 20 mg/kg, by gavage), on the EPM or the OFT. However, rats treated for 15 day (20 mg/kg) with EPV showed increased percentage of entries and time spent in the open arms on the EPM without alter locomotor activity in the OFT compared to control group. Acute or a 15 day administration of diazepam (2 mg/kg, i.p.), increased the same parameters on the EPM and OFT. Acute treatment with 300 or 600 mg/kg of EPV, decreased the locomotor activity in the OFT. Results suggest anxiolytic and sedative effects for the EPV and reveal a wide dose range for the anxiolytic effect.

Sedative Effect and Cardiovascular Stability of Lidocaine during Endotracheal Intubation under Bispectral Index (BIS) Monitoring / 대한마취과학회지

BACKGROUND: Lidocaine's sedative effect has not been known well. The purpose of this study was to evaluate its sedative and cardiovascular effects during induction of anesthesia. METHODS: Twenty patients were randomly allocated to group I or II, with or without lidocaine 1.5 mg/kg intravenously (IV) before induction, respectively. The BIS, blood pressure and heart rate were measured at before and 2 minutes after lidocaine IV injection, preintubation, and 1, 2, 3 and 5 minutes after tracheal intubation. The enflurane concentrations were continuously maintained at 2 volume%. RESULTS: The BIS of group I was more decreased at 1 and 2 minutes after intubation than those of group II. The systolic blood pressures of group I were less increased at 1 and 2 minutes after intubation than those of group II. The diastolic blood pressures and heart rates of group I were not different from those of group II at each stage of the procedure. CONCLUSIONS: Lidocaine reduced BIS and blunted the intubation-induced systolic hypertensive response. In addition it is thought that it has a sedative effect and is effective to maintain cardiovascular stability after tracheal intubation.

Effects of the Sanjoin on the Rat Brain: Focused on Serotonin, Sleeping Time, Sleep EEG and Autonomic Activity

OBJECTS: Sanjoin, the seeds of Zizyphus vulgaris var. spinosus has been used as the most important hypnotic agent in chinese medicine to treat insomnia. This research was performed in order to examine the effect of betulinic acid and sanjoinine-A which are components of Sanjoin. METHOD: Sleeping time, sleep recordings of EEG, serum serotonin level, and locomotor activity were measured in rats which received betulinic acid and sanjoinine-A as sleep induction material extracted from Sanjoin. RESULTS: 1) Groups received betulinic acid, sanjoinine-A, and lorazepam showed increased sleep time than control group with saline. 2) Groups with betulinic acid, sanjoinine-A, lorazepam and saline recorded beta-wave in sleep recording of EEG. In there was no significant difference among all groups. 3) No significant difference in serum serotonin level among all groups was found. 4) In autonomic activity testing, groups of betulinic acid, sanjoinine-A, and lorazepam showed significantly more decreased in activity than saline group. In comparison of groups of betulinic acid and sanjoinine-A with a group of lorazepam, there was no significant difference. CONCLUSION: These results suggests that betulinic acid and sanjoinine-A have the sedative effect like lorazepam rather than sleep effect.

The Sedative Effect of Propofol and Midazolam in Pediatric Caudal Anesthesia / 대한마취과학회지

Pediatric patients often could not be cooperated with physician during various procedures. So, many agents such as inbalation anesthetics and intravenous anesthetics have been used to decrease pain, anxiety and awareness during regional anesthesia in children. The purpose of this study was to compare propofol with midazolam and inhalation anesthetics for emergence time from sedation in caudal anesthesia of children. Forty five patients were randomly divided three groups. In propofol group(Group P, n=15), induction dose of 1.0 mg/kg propofol(Diprivan) was received followed by continuous infusion of 3~5 mg/kg/hr. In midazolam group(Group M, n=15), induction dose of 0.15 mg/kg midazolam(Dormicum) was received followed by continuous infusion of 0.06~0.08 mg/kg/hr. In inhalation anesthetic group(Group E, n=15), O2-NO2-Enflurane(3L/min, 3L/min, 0.6~1.0 vo1% respectively) inhalated through face mask by non-rebreathing system for sedation. The blood pressure, heart rate, arterial oxygen saturation during anesthesia and emergence time, complications were measured. The results were as follows: 1) The blood pressure was significantly decreased in group M and E. Heart rate was also significantly increased in group M and E. 2) The arterial oxygen saturation was not significantly changed in each three groups. 3) In the group P and E, emergence time was shorter than in the group M. From the above results, we conclude that propofol is more excellent intravenous anesthetics than midazolam in respect to emergence time and hemodynamic changes in pediatric caudal anesthesia.

Cardiovascular Response, Analgesic and Sedative Effect according to the Dose of Epidural Clonidine / 대한마취과학회지

The subarachnoidal or epidural opioid reveals excellent analgesic effect for postoperative pain and intractable cancer pain, but its side effects such as nausea, vomiting, voiding difficulty, pruritus and respiratory failure limit its use. There were many studies for decreasing frequency and severity of side effects and reinforcing the analgesic effect of opioid by administrating other drugs. Clonidine is one of such drugs which is able to be administered epidurally with opioids for that purpose. We studied the changes of cardiovascular response, analgesic and sedative effect according to the dose of epidural clonidine. The analgesic effect of epidural clonidine was investigated in 30 patients who underwent anal surgery with epidural anesthesia using 15 ml of 1.5~2 % lidocaine.The time of maximal intensity of pain after disapperance of injected lidocaine was checked. Thirty patients were divided into three groups randomly. In group 1 (n=10), the dose of epidural clonidine was 50 ug; Group 2 (n=10) was 150 ug; Group 3 (n=10) was 450 ug. Changes in the arterial pressure, pulse rate, sedation state and SpO2 were observed before and during 60 minutes after epidural clonidine administration. And the analgesic effect was assessed by measuring VAS pain score. Blood pressures and pulse rates decreased according to increase of dosage of clonidine. Group 1 showed the analgesic effect of 34%, group 2 showed 77% and group 3 showed 81% at 60 minutes after administration. Sedation effect was seen in group 2 and 3 but SpO2 was not decreased significantly. We thought that the respiratory depression of epidural clonidine was not so significant to limit the use for the postoperative pain control. We conclude that it is better to administer clonidine with opioids epidurally than clonidine slone to get better analgesic effect and less sedative effect, because the analgesic effect of epidural clonidine increases according to increase of dosage but the sedative effect increases also.

Sedative and hypnotic effects of oil of spine date seeds from different extraction technologies in mice / 西安交通大学学报(医学版)

Objective To study the sedative and hypnotic effects of oil of spine date seeds by different extraction technologies(compression and supercritical CO2 extraction,OSDSE and OSDSS) in mice.Equivalence test was used to test the effects.Methods Spontaneous activity and tolerance were observed by photoelectric counting method after long-term intragastric administration of OSDSE and OSDSS in mice.The sleeping time and delitescence induced by above threshold dose of pentobarbital sodium and sleeping number induced by below threshold dose of pentobarbital sodium were utilized to observe the hypnotic effect of OSDSE and OSDSS in mice.Diazepam was applied as a positive control drug.Results OSDSE and OSDSS could obviously reduce spontaneous activity,increase sleeping time and sleeping number in mice,while the sleeping delitescence was shortened.All the effects induced by OSDSE and OSDSS were equivalent.The inhibitory effect of spontaneous activity was enhanced following repeated administration,while the effect of diazepam was reduced.Conclusion Both oils of spine date seeds can induce sedative and hypnotic effects without tolerance.They have equivalent effects on sedation and hypnosis.