OBJECTIVETo observe the efficacy of intravenous scopolamine in the prevention of postoperative nausea and vomiting (PONV) after cesarean section (CS).

METHODSA total of 260 pregnant women with American Society of Anesthesiologists (ASA) Physical Status Classification class I-II who underwent elective CS under combined spinal-epidural anesthesia (CSEA) were randomly divided into four groups (n = 65): at the end of surgery, 0.3 mg/5 ml scopolamine (scopolamine group), 4 mg/5 ml ondansetron (ondansetron group), 0.3 mg scopolamine plus 4 mg ondansetron per 5 ml (combination group), or 0.9% normal saline 5 ml (control group) were intravenously infused, respectively. The episodes of PONV and adverse effects were observed within 24 hours after operation.

RESULTSThe incidences of PONV within 24 hours after surgery were 87.7%, 89.2%, and 92.3%, respectively, in scopolamine group, ondansetron group, and combination group, which were all significantly higher than that in control group (73.8%) (all P < 0.05). However, the incidences of PONV showed no significant difference among these three groups (P > 0.05). No significant difference in the incidence of adverse effects was observed among the four groups (P > 0.05).

CONCLUSIONIntravenous scopolamine (0.3 mg), with a comparable efficacy as ondansetron 4 mg, can effectively decrease the incidence of PONV after CS.

Administration, Intravenous ; Adult ; Cesarean Section ; Female ; Humans ; Middle Aged ; Ondansetron ; administration & dosage ; therapeutic use ; Postoperative Nausea and Vomiting ; prevention & control ; Scopolamine Hydrobromide ; administration & dosage ; therapeutic use ; Treatment Outcome

The study aims to elucidate the characteristics of pharmacokinetics of scopolamine hydrobromide oral disintegrative microencapsule tablets in healthy Beagle dogs. Chromatographic separation was performed on a C18 column (100 mm x 3.0 mm, 3.5 microm) with methanol - 2 mmol x L(-1) ammonium formate (25 : 75) as the mobile phase. A trip-quadrupole tandem mass spectrum with the electrospray ionization (ESI) source was applied and positive ion multiple reaction monitoring mode was operated. Six Beagle dogs were randomly devided into two groups. They received oral single dose of scopolamine hydrobromide oral disintegrative microencapsule tablets 0.6 mg (test tablet) or scopolamine hydrobromide normal tablets (reference tablet). Plasma samples were collected at designed time. Plasma concentration of scopolamine hydrobromide was determined by LC-MS/MS and pharmacokinetic parameters were calculated. The pharmacokinetic parameters of test tablet vs reference tablet were as follows: C(max): (8.16 +/- 0.67) ng x mL(-1) vs (3.54 +/- 0.64) ng x mL(-1); t1/2: (2.83 +/- 0.45) h vs (3.85 +/- 0.82) h; t(max): (1.25 +/- 0.27) h vs (0.42 +/- 0.09) h; AUC(0-12h): (25.06 +/- 3.75) h x ng x mL(-1) vs (9.59 +/- 1.02) h x ng x mL(-1); AUC(0-infinity): (26.30 +/- 3.92) h x ng x mL(-1) vs (10.80 +/- 1.45) h x ng x mL(-1); MRT(0-12h): (3.38 +/- 0.34) h vs (3.86 +/- 0.26) h; MRT(0-infinity): (3.98 +/- 0.63) h vs (5.37 +/- 1.00) h. The absorption rate and AUC of test tablet is different from that of reference tablet. The bioavailability of test tablet is better than those of reference tablet.
Administration, Oral ; Animals ; Area Under Curve ; Biological Availability ; Capsules ; Chromatography, Liquid ; Dogs ; Drug Stability ; Female ; Male ; Muscarinic Antagonists ; administration & dosage ; blood ; pharmacokinetics ; Random Allocation ; Scopolamine Hydrobromide ; administration & dosage ; blood ; pharmacokinetics ; Spectrometry, Mass, Electrospray Ionization ; Tablets ; Tandem Mass Spectrometry

The purpose of this study is to investigate the memory enhancing effect and underlying molecular mechanism of arabinoxylan (AX), a major component of dietary fiber in wheat against scopolamine (SCO)-induced amnesia in Sprague-Dawley (SD) rats. Diverse behavior tests including Y-maze, Morris water maze, and passive avoidance tests were performed to measure cognitive functions. SCO significantly decreased the spontaneous alterations in Y-maze test and step-through latency in passive avoidance test, whereas increased time spent to find the hidden platform in Morris water maze test compared with the sham control group. In contrast, oral administration of AX (25 mg/kg and 50 mg/kg) effectively reversed the SCO-induced cognitive impairments in SD rats. Furthermore, AX treatment up-regulated the expression of brain-derived neurotrophic factor (BDNF) in the cortex and hippo-campus via promoting activation of cAMP response element binding protein (CREB). Therefore, our findings suggest that AX can improve SCO-induced learning and memory impairment possibly through activation of CREB and up-regulation of BDNF levels, thereby exhibiting a cognition-enhancing potential.
Administration, Oral ; Amnesia ; Animals ; Brain-Derived Neurotrophic Factor ; Cyclic AMP Response Element-Binding Protein ; Dietary Fiber ; Learning* ; Maze Learning ; Memory* ; Rats ; Rats, Sprague-Dawley ; Scopolamine Hydrobromide ; Triticum ; Up-Regulation

Gastrodia elata (GE) is traditionally used for treatment of various disorders including neurodegenerative diseases such as Alzheimer's disease. To investigate the neuroprotective effect of GE, amyloid-beta peptide (Abeta)-treated PC12 cells were cultured with GE aqueous extract. In vitro assay demonstrated that 50 microM of pre-aggregated Abeta was lethal to about a half portion of PC12 cells and that Abeta aggregate-induced cell death was significantly decreased with GE treatment at < or =10 mg/mL in a dose-dependent manner. To further examine in vivo cognitive-improving effects, an artificial amnesic animal model, scopolamine-injected Sprague-Dawley rats, were orally administered the extract for 6 weeks followed by behavioral tests (the passive avoidance test and Morris water maze test). The results showed that an acute treatment with scopolamine (1 mg/kg of body weight) effectively induced memory impairment in normal rats and that the learning and memory capability of scopolamine-treated rats improved after prolonged administration of GE extract (50, 250 and 500 mg/kg of body weight for 6 weeks). These findings suggest that a GE regimen may potentially ameliorate learning and memory deficits and/or cognitive impairments caused by neuronal cell death.
Administration, Oral* ; Alzheimer Disease ; Animals ; Body Weight ; Cell Death ; Gastrodia* ; Learning* ; Memory Disorders ; Memory* ; Models, Animal ; Neurodegenerative Diseases ; Neurons ; Neuroprotective Agents ; PC12 Cells ; Rats* ; Rats, Sprague-Dawley ; Scopolamine Hydrobromide

OBJECTIVETo investigate whether transdermal scopolamine increased cardiac vagal activity in patients during the acute phase of myocardial infarction.

METHODS30 patients with a first acute myocardial infarction and preserved sinus rhythm who were on no drug that could influence the sinus node were randomly assigned to either treatment group or placebo group. Measures of heart rate variability (HRV) in patients given drug or placebo were obtained by digital 24 hour Holter recording before and after treatment. Baroreflex sensitivity was performed using the phenylephrine method.

RESULTSNo significant differences was found in the indices of the time domain and the frequency domain in both groups before treatment. Patients with transdermal scopolamine showed a significant increase in the standard deviation of normal RR intervals (SDNN), standard deviation of all five min mean normal RR intervals (SDANN), root mean square of differences of successive normal RR intervals (rMSSD), total power (TP, 0.000. - 0.40 Hz), low frequency peak (LF, 0.040 - 0.15 Hz), high frequency peak (HF, 0.15 - 0.40 Hz), and Baroreflex sensitivity after treatment (P < 0.05 - 0.01). These indices did not change in patients given placebo.

CONCLUSIONLow doses of transdermal scopolamine safely increase cardiac parasympathetic activity and improve autonomic indices in patients with acute myocardial infarction.

Administration, Cutaneous ; Adult ; Aged ; Baroreflex ; drug effects ; Dose-Response Relationship, Drug ; Female ; Heart ; innervation ; Heart Rate ; drug effects ; Humans ; Male ; Middle Aged ; Myocardial Infarction ; physiopathology ; Scopolamine Hydrobromide ; pharmacology ; Vagus Nerve ; drug effects ; physiopathology

This study is to prepare scopolamine hydrobromide nanoparticles-in-microsphere system (SH-NiMS) and evaluate its drug release characteristics in vitro. SH nanoparticles were prepared by ionic crosslinking method with tripolyphosphate (TPP) as crosslinker and chitosan as carrier. Orthogonal design was used to optimize the formulation of SH nanoparticles, which took the property of encapsulation efficiency and drug loading as evaluation parameters. With HPMC as carrier, adjusted the parameters of spray drying technique and sprayed the SH nanoparticles in microspheres encaposulated by HPMC was formed and which is called nanoparticles-in-microsphere system (NiMS). SH-NiMS appearances were observed by SEM, structure was obsearved by FT-IR and the release characteristics in vitro were evaluated. The optimized formulation of SH nanoparticles was TPP/CS 1:3 (w/w), HPMC 0.3%, SH 0.2%. The solution peristaltic speed of the spray drying technique was adjusted to 15%, and the temperature of inlet was 110 degrees C. The encapsulation product yeild, drug loading and particle sizes of SH-NiMS were 94.2%, 20.4%, and 1256.5 nm, respectively. The appearances and the structure of SH-NiMS were good. The preparation method of SH-NiMS is stable and reliable to use, which provide a new way to develop new dosage form.
Chitosan ; chemistry ; Cross-Linking Reagents ; Delayed-Action Preparations ; Drug Carriers ; chemistry ; Drug Compounding ; methods ; Microscopy, Electron, Scanning ; Microspheres ; Nanoparticles ; chemistry ; Particle Size ; Polyphosphates ; chemistry ; Scopolamine Hydrobromide ; administration & dosage ; chemistry ; Spectroscopy, Fourier Transform Infrared

PURPOSE: To investigate the prevalence of paralytic ileus after spinal operation in the supine or prone operative position and to determine the efficacy of prophylactic gastrointestinal motility medications in preventing symptomatic paralytic ileus after a spinal operation. MATERIALS AND METHODS: All patients received spinal surgery in the supine or prone operative position. The study period was divided into two phases: first, to analyze the prevalence of radiographic and symptomatic paralytic ileus after a spinal operation, and second, to determine the therapeutic effects of prophylactic gastrointestinal motility medications (postoperative intravenous injection of scopolamine butylbromide and metoclopramide hydrochloride) on symptomatic paralytic ileus after a spinal operation. RESULTS: Basic demographic data were not different. In the first phase of this study, 27 patients (32.9%) with radiographic paralytic ileus and 11 patients (13.4%) with symptomatic paralytic ileus were observed. Radiographic paralytic ileus was more often noted in patients who underwent an operation in the prone position (p=0.044); whereas the occurrence of symptomatic paralytic ileus was not different between the supine and prone positioned patients (p=0.385). In the second phase, prophylactic medications were shown to be ineffective in preventing symptomatic paralytic ileus after spinal surgery [symptomatic paralytic ileus was observed in 11.1% (4/36) with prophylactic medication and 16.7% (5/30) with a placebo, p=0.513]. CONCLUSION: Spinal surgery in the prone position was shown to increase the likelihood of radiographic paralytic ileus occurrence, but not symptomatic paralytic ileus. Unfortunately, the prophylactic medications to prevent symptomatic paralytic ileus after spine surgery were shown to be ineffective.
Adjuvants, Anesthesia/*administration & dosage/pharmacology ; Adult ; Aged ; Antiemetics/*administration & dosage/pharmacology ; Female ; Gastrointestinal Motility/*drug effects/physiology ; Humans ; Injections, Intravenous ; Intestinal Pseudo-Obstruction/drug therapy/epidemiology/*prevention & control ; Lumbar Vertebrae/radiography/*surgery ; Male ; Metoclopramide/*administration & dosage/pharmacology ; Middle Aged ; Postoperative Complications/epidemiology ; Prevalence ; Prone Position ; Prospective Studies ; Republic of Korea ; Scopolamine Hydrobromide/*administration & dosage/*pharmacology ; Spinal Fusion/*adverse effects ; Supine Position ; Treatment Outcome

Based on the report of previous clinical study which showed cholinergic receptor antagonist scopolamine had antidepressant activity, this study was to investigate the antidepressant activity of scopolamine and explore its effective dose in mice, and to evaluate the effect of scopolamine on the central nervous system and learning/memory ability at its antidepressant effective dose. Tail suspension test, forced swimming test, step-down passive avoidance test and open field test were used to evaluate its effects on mice. Compared with the vehicle control group, single-dose administration of scopolamine (0.1-0.4 mg x kg(-1), ip) significantly decreased the immobility time (P < 0.01 or P < 0.001) in tail suspension test, and significantly decreased the immobility time (P < 0.001) in forced swimming test, but had no effect on the step-down latency and errors in step-down passive avoidance test. Scopolamine (0.1 and 0.2 mg x kg(-1), ip) had no influence on the locomotor activity in open field test, while at dose of 0.4 mg x kg(-1) significantly increase the locomotor activity. These results showed that scopolamine produced reliable antidepressant effect at doses of 0.1 and 0.2 mg x kg(-1), without impairment on learning and memory, as well as excitory or inhibitory effect on central nervous system in mice.
Animals ; Antidepressive Agents ; administration & dosage ; pharmacology ; Avoidance Learning ; drug effects ; Behavior, Animal ; drug effects ; Cholinergic Antagonists ; administration & dosage ; pharmacology ; Depression ; physiopathology ; prevention & control ; Hindlimb Suspension ; Male ; Memory ; drug effects ; Mice ; Mice, Inbred ICR ; Motor Activity ; drug effects ; Random Allocation ; Scopolamine Hydrobromide ; administration & dosage ; pharmacology ; Swimming

OBJECTIVETo study on the effect of acteoside on learning and memory of dementia mice.

METHODMice were orally administered with acteoside for 10 days. Scopolamine was used to establish the acquired learning disability in mice. Their learning and memory were detected with a behavioral experiment (step-down test). After the behavior test, corticocerebral and hippocampus tissues of mice were detected with biochemical indexes, including GSH-Px, T-SOD, MDA, TChE and contents of protein in brain tissues.

RESULTMice were administered with acteoside for 10 d in advance to alleviate the acquired learning disability induced by scopolamine. Compared with the model group, acteoside increased the latency period in the step-down test and reduced error times. Besides, acteoside increased the activity of GSH-Px, T-SOD, TChE and protein content in their brain tissues, but decreased MDA content.

CONCLUSIONActeoside can significantly alleviate the acquired learning disability in mice induced by scopolamine. Its mechanism may be related with its effect of inhibiting the generation of free radicals in mice and improving the function of the central cholinergic system.

Animals ; Behavior, Animal ; drug effects ; Brain ; drug effects ; metabolism ; Drugs, Chinese Herbal ; administration & dosage ; pharmacology ; Glucosides ; administration & dosage ; pharmacology ; Glutathione Peroxidase ; metabolism ; Learning ; drug effects ; Male ; Memory Disorders ; chemically induced ; drug therapy ; Mice ; Phenols ; administration & dosage ; pharmacology ; Scopolamine Hydrobromide ; adverse effects ; Superoxide Dismutase ; metabolism