Sample records for cisapride

  1. Use of cisapride with contraindicated drugs in The Netherlands

    DEFF Research Database (Denmark)

    De Bruin, Marie L; Panneman, Martien J M; Leufkens, Hubert G M


    OBJECTIVE: To investigate the prevalence of concomitant use and coprescribing of cisapride with potentially interacting drugs to evaluate the impact of these warnings from 1994 to 1998. DESIGN: Retrospective follow-up study of patients using cisapride. SETTING: Data for this study were obtained f...

  2. Cisapride decreases gastric content aspiration in mechanically ventilated patients (United States)

    Pneumatikos, John; Koulouras, Basil; Frangides, Christ; Goe, Dian; Nakos, George


    Objective: To determine the effect of the prokinetic agent cisapride in the prevention of aspiration of gastric contents. Design: A prospective randomized two-period crossover study. Setting: Fourteen-bed polyvalent intensive care unit in a University Hospital. Patients: Eighteen intubated, mechanically ventilated patients who were seated in a semirecumbent position were studied. Method: Tc-99 m sulfur colloid (80 megabecquerels) was administered via nasogastric tube on 2 consecutive days. Patients randomly received cisapride (10 mg, via nasogastric tube) one day and a placebo the other. Bronchial secretions were obtained before and for 5 consecutive h after Tc-99 m administration. The radioactivity was measured in a standard amount (1ml) of bronchial fluid using a gamma counter and expressed as counts per min (cpm) after correction for decay. Results: Sixteen out of 18 (88%) patients had increased radioactivity in bronchial secretions. The radioactivity increased over time both with and without cisapride, although it was lower in patients receiving cisapride than in those receiving a placebo. The cumulative bronchial secretion radioactivity obtained when patients received cisapride was significantly lower than when patients received a placebo: 7540 ± 5330 and 21965 ± 16080 cpm, respectively (P <0.05). Conclusion: Our results suggest that aspiration of gastric contents exists even in patients who are kept in a semirecumbent position. Moreover, cisapride decreases the amount of gastric contents aspiration in intubated and mechanically ventilated patients and may play a role in the prevention of ventilator associated pneumonia. Cisapride, even with the patient in the semirecumbent position, did not completely prevent gastric content aspiration. PMID:11056722

  3. Cisapride decreasing orocecal transit time in patients with nonalcoholic steatohepatitis

    Institute of Scientific and Technical Information of China (English)

    Xiang-Sheng Fu; Feng Jiang


    BACKGROUND:Altered small-intestine motility, lengthening of orocecal transit time (OCTT), and small-intestinal bacterial overgrowth (SIBO) have been detected in patients with nonalcoholic steatohepatitis (NASH). These changes might be related to the progressive course and poor prognosis of the disease. This study was undertaken to investigate the effect of 4-week treatment with cisapride on OCTT. METHODS: Ten NASH patients without diabetes were included. Ten healthy individuals served as controls. OCTT was measured by lactulose breath test (LBT). Anti-endotoxin core antibodies (EndoCAb) IgG were also examined. The effect of cisapride (10 mg TID during 4 weeks) on LBT and serum EndoCAb IgG levels in NASH patients was investigated. RESULTS: The NASH patients had more signiifcantly prolonged OCTT (95±17 min) than the controls (59±18 min, P=0.00032). Cisapride administration decreased OCTT (from 95±17 min to 83±19 min, P=0.037), basal breathed H2 (from 9.87±1.60 ppm to 8.61±1.63 ppm, P=0.046) and EndoCAb IgG titers (from 5.24±0.68 GMU/ml to 4.20±0.72 GMU/ml, P=0.013) in NASH patients. CONCLUSIONS:The present data suggest the existence of deranged intestinal motility and endotoxemia in NASH patients. Cisapride administration during 4 weeks possibly restore intestinal motility and ameliorate endotoxemia in NASH patients.

  4. The effect of a single rectal dose of cisapride on delayed gastric emptying.The effect of a single rectal dose of cisapride on delayed gastric emptying.

    NARCIS (Netherlands)

    Brummer, R.J.M.; Schoenmakers, E.A.J.M.; Kemerink, G.J.; Heidendal, G.A.K.; Sanders, D.G.M.; Stockbrügger, R.W.


    Department of Gastroenterology, University Hospital Maastricht, The Netherlands. BACKGROUND: Cisapride has an established prokinetic effect in patients with delayed gastric emptying. However, rectal administration of the drug might be preferred in patients with either dysphagia or nausea due to gast

  5. Effects of cisapride on ulcer formation and gastric secretion in rats: comparison with ranitidine and omeprazol. (United States)

    Alarcón de la Lastra, C; Martin, M J; La Casa, M; López, A; Motilva, V


    1. The antiulcerogenic effects of cisapride, a potent benzamide-stimulating gastrointestinal motility agent, were studied on cold-resistant and pylorus-ligated gastric ulcers. Acidity, composition of gastric secretion, and quantitative and qualitative changes on mucus glycoprotein content were also determined. These effects were compared with those of ranitidine (50 mg/kg) and omeprazol (10 mg/kg). 2. Oral cisapride (10-100 mg/kg) dose-relatedly and significantly (P < 0.01, P < 0.05) decreased the severity of the lesions induced by cold-resistant stress. In stressed rats, cisapride increased the amount of mucus secretion and markedly enhanced the glycoprotein content. Morphometric evaluation of mucus secretion revealed a significant increase in both the PAS area (neutral glycoproteins) and Alcian blue area (sulfated glycoproteins). 3. In 4 h pyloric-ligated animals, cisapride (10-100 mg/kg) showed a significant reduction in the number and severity of ulcers (P < 0.01) and histamine concentration (P < 0.01, P < 0.001). In addition, at the highest doses (50-100 mg/kg), cisapride produced a significant decreases in acidity; however, it did not alter the gastric volume secretion or pepsin concentrations. 4. These results suggest that cisapride shows antiulcerogenic effects which could possibly be explained through antisecretory and cytoprotective mechanisms involving an enhancement of cuality and production of gastric mucus.

  6. Cisapride does not alter gastric volume or pH in patients undergoing ambulatory surgery.

    LENUS (Irish Health Repository)

    Lydon, A


    PURPOSE: To evaluate the efficacy of 20 mg cisapride p.o. in reducing residual gastric volume and pH in adult ambulatory surgical patients. METHODS: Using a prospective randomised double-blind controlled design, we administered either 20 mg cisapride p.o. or placebo preoperatively to 64 ASA 1-2 ambulatory surgical patients. Following induction of anesthesia we measured volume and pH of residual gastric contents, using blind aspiration through an orogastric tube. Parametric data were analysed using unpaired, one tail Students\\' t test. Non-parametric data were analysed using Fishers Exact test and Chi square analysis. Statistical significance was accepted at the probability level of < 0.05. RESULTS: Residual gastric volumes were similar in the two groups (19.5 +\\/- 23.8, 23.9 +\\/- 24.4 ml), in the cisapride and placebo groups respectively, P=0.24). Data shown are mean (+\\/- SD). The proportions of patients with a residual gastric volume exceeding 0.4 ml x kg(-1) were similar in the two groups (4 of 28, and 8 of 23 patients in the cisapride and placebo groups respectively, P=0.09). The pH of the residual gastric contents were similar in the cisapride and placebo groups (1.6 +\\/- 0.5, 1.4 +\\/- 0.5, respectively, P=0.26). The proportions of patients with pH < 2.5 was also similar in the cisapride and placebo groups (21 of 25, and 20 of 21 patients respectively, P=0.2). CONCLUSIONS: Preoperative administration of 20 mg cisapride p.o. to patients scheduled for outpatient surgery does not alter either the volume or the pH of gastric contents. Its use in this setting is of no apparent clinical benefit.

  7. Molecular structure of two gastrokinetic compounds, cisapride and R53757: comparison with dopaminergic D 2 antagonists (United States)

    Collin, S.; Vercauteren, D. P.; Evrard, G.; Durant, F.; Tollenaere, J. P.; Moereels, H.


    The crystal structures of the title compounds have been solved by direct methods from single crystal X-ray diffraction. Cisapride: monoclinic, space group P2 1/ n with a=34.210(4), b=7.642(2), c=9.435(1) Å, β=90.93(1)°, Z=4, final R factor=0.044 for 1178 observed reflections. R53757: monoclinic, space group P2 1/ n with a=28.896(3), b=8.054(2), c=10.957(2) Å, β=91.79(1)°, Z=4, final R factor=0.032 for 933 observed reflections. Cisapride, a non-dopamine blocking gastrokinetic, and its closely related analog, R53757, are compared to two very potent D 2 antagonists, tropapride and R48788. The analysis of the X-ray determined structures completed by theoretical conformational studies suggests that the structural requirements for all compounds studied seem to be very similar. As shown by PCILO calculations, the presence of a methoxy group on the cisapride piperidine ring does not prevent an optimal orientation of the three putative pharmacophoric elements described for the D 2 receptor. Only the nature of the nitrogen lateral chain differs between the D 2 antagonists and cisapride.

  8. Therapeutic effect of cisapride on gastric injury following hemorrhagic shock resuscitation in rats

    Institute of Scientific and Technical Information of China (English)

    ZHANG Lian-yang; WANG Zheng-guo; ZHU Pei-fang; XU Yan


    Objective: To investigate the therapeutic effect of cisapride on gastric injury following hemorrhagic shock resuscitation.Methods: 108 Wistar rats weighing (200 g±30 g) were randomly divided into a sham shock (SS) group (n=36), a hemorrhagic shock resuscitation (HS) group (n=36) and a hemorrhagic shock cisapride treated (HSC) group (n=36). Sampling at 1, 2 and 4 hours after resuscitation was done and 6 samples for each observation item were taken. The gastric blood flow volume was measured by isotope label biological microglobulin. Gastric pHi, gastric emptying, MDA and Na+-K+-ATPase of gastric mucosa were measured.Results: In the HSC group, the relative residual rate of gastric pigment decreased significantly, the gastric blood flow volume elevated; gastric pHi increased significantly at 2 hours; the level of mucosal MDA decreased at 4 hours, the activity of Na+-K+-ATPase increased and the lactic acid level in the portal vein decreased significantly compared to the HS group.Conclusions: After hemorrhagic shock resuscitation, cisapride contained the following functions,1) promoting gastric emptying, 2) increasing the blood flow of gastric blood flow volume and gastric pHi, 3) depressing the lactic acid concentration of the portal vein and improving MDA volume and Na+-K+ -ATPase activity of gastric mucosa. It suggests that after comple menting effective circulating blood volume for hemorrhagic shock resuscitation, early use of cisapride for gastric motility is helpful for an improvement of lasting ischemia and hypoxia in stomach.

  9. Effects of omeprazole and cisapride treatment in Japanese asthmatics with reflux esophagitis

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    Katsuya Fujimori


    Full Text Available In the United States and Europe, gastroesophageal reflux (GER is receiving attention as a potential cause of bronchial asthma. Few Japanese case reports have described this relationship. Therefore, we investigated the effect of omeprazole and cisapride on pulmonary function tests, blood gases and home peak expiratory flow rates (PEFR in six Japanese outpatients with asthma and proven GER. After 8 weeks of treatment, reflux esophagitis had improved in all patients. However, the parameters of pulmonary function showed no change other than a significant post- treatment increase in home PEFR (4.4-27.7% in three patients. These results suggest that anti-reflux (omeprazole and cisapride treatment will produce small improvements in the PEFR in some Japanese asthmatics with GER.

  10. Clinical Comparative Study on Massage Therapy and Cisapride in Treating Functional Dyspepsia

    Institute of Scientific and Technical Information of China (English)

    ZHANG Jia-fu; LIN Qiang; LIU Hong-bo; ZHOU Ping; XIAO Yuan-chun


    To observe the clinical efficacy of massage therapy and Cisapride in the treatment of functional dyspepsia (FD).Methods:Eighty subjects were randomized into two groups:treatment group in which 40 cases were treated by massage therapy and control group in which 40 cases were treated by Cisapride,with a course of 4 weeks;meanwhile,another 40 healthy people were taken as normal group.Abdominal fullness,acid regurgitation,diminished appetite and anorexia,nausea and vomiting and health survey were observed;symptom scores were recorded.Results:These two treatment methods were effective for FD.Conclusion:Mental disorder is one cause of FD;massage therapy is quite effective for it.

  11. Effect of cisapride on intestinal bacterial and endotoxin translocation in cirrhosis

    Institute of Scientific and Technical Information of China (English)

    Shun-Cai Zhang; Wei Wang; Wei-Ying Ren; Bo-Ming He; Kang Zhou; Wu-Nan Zhu


    AIM: To investigate the effects of cisapride on intestinal bacterial overgrowth (IBO), bacterial and endotoxin translocation, intestinal transit and permeability in cirrhotic rats.METHODS: All animals were assessed with variables including bacterial and endotoxin translocation, intestinal bacterial overgrowth, intestinal transit and permeability.Bacterial translocation (BT) was assessed by bacterial culture of MLN, liver and spleen, IBO by a jejunal bacterial count of the specific organism, intestinal permeability by determination of the 24-hour urinary 99mTc-DTPA excretion and intestinal transit by measurement of the distribution of 51Cr in the intestine.RESULTS: Bacterial translocation (BT) and IBO was found in 48 % and 80 % cirrhotic rats respectively and none in control rats. Urinary excretion of 99mTc-DTPA in cirrhotic rats with BT (22.2±7.8) was greater than these without BT (10.5±2.9). Intestinal transit (geometric center ratio) was significantly delayed in cirrhotic rats (0.31±0.06) and further more delayed in cirrhotic rats with BT (0.24±0.06) than these without BT (0.38±0.11). Cirrhotic rats with IBO had significantly higher rates of intestinal bacterial and endotoxin translocation, slower intestinal transit time and higher intestinal permeability than those without IBO. It was also found that BT was closely associated with IBO and the injury of intestinal barrier. Compared with the placebo group,cisapride-treated rats had lower rates of bacterial/endotoxin translocation and IBO, which was closely associated with increased intestinal transit and improved intestinal permeability by cisapride.CONCLUSION: These results indicate that endotoxin and bacterial translocation in cirrhotic rats may be attributed to IBO and increased intestinal permeability. Cisapride that accelerates intestinal transit and improve intestinal permeability might be helpful in preventing intestinal bacterial and endotoxin translocation.

  12. Gastric Emptying in Patients with Diabetes: Gastric Emptying Time, Retention Rate and Effect of Cisapride

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    Chung, Byung Chun; Choi, Chung Il; Gwak, Dong Suck; Lee, Jae Tae; Lee, Kyu Bo; Kim, Bo Wan; Chung, Jun Mo [Kyungpook National University School of Medicine, Daegu (Korea, Republic of)


    Gastic emptying scan in diabetic patients is widely used to assess the degree of motility disturbance and the symptoms such as nausea, vomiting, bloating, abdominal pain and early gastric fullness which we can't find anatomic lesion by fiberoscopic or barium study. In order to determine the relationship among diabetic gastropathy, neropathy, retinopathy and disease duration, gastric emptying scan using {sup 99m}Tc-tin colloid labeled scramble egg in hamburger was performed in 10 healthy male controls and 50 diabetic patients which were subdivided to no neuropathy, peripheral neuropathy and autonomic neuropathy groups according to the degree of diabetic neuropathy and no retinopathy, background retinopathy and proliferative retinopathy groups according to the degree of diabetic retinopathy. After medication of cisapride for 2 weeks, we observed the presence of improvement of gastric motility in diabetics. The results were as following: 1) In controls, gastric emptying time (GET1/2) was 75 +- 13.6 min and 2 hour gastric retension rate(GRR2) was 32 +- 11.1%. 2) In diabetics, GET/2 was prolonged more than 2 hours and GRR2 was 58 +- 23.1%. According to degree of neuropathy, GET1/2 was prolonged more than 2 hours in all three groups and GRR2 was 54+- 24.1% in no neuropathy group, 57 +- 24.3% in peripheral neuropathy group and 69 +- 24.6% in autonomic neuropathy group. According to degree of retinopathy, GET1/2 was 110 +- 23.4 min in no retinopathy group and prolonged more than 2 hours in other two groups and GRR2 was 45 +- 21.6% in no retinopathy group, 71 +- 19.7% in background retinopathy group and 73 +- 21.5% in proliferative retinopathy group. 3) After cisapride for 2 weeks, GET1/2 and GRR2 were improved as 90 +- 14.6 min and 40 +- 13.8% (initial GET1/2 and GRR2 were above 2 hours and 61 +- 15.4%). We can conclude from above findings that gastropathy in diabetic neuropathy suggesting main underlying factor in motility disorder. The degree of retinopathy and

  13. Does Cisapride, as a 5HT4 Receptor Agonist, Aggravate the Severity of TNBS-Induced Colitis in Rat?

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    Azadeh Motavallian


    Full Text Available There is a pressing need for research that will lead to the reveal of targets designed to analyse the possible pathways for the treatment of IBD. Because of the probable involvement of serotonin in inflammatory conditions of intestine and the important role of 5HT4 receptors in GI function, the investigation of the role of 5HT4 receptors in the pathogenesis of IBD will be interesting. The aim of this study was to investigate the effects of cisapride, a 5HT4 receptor agonist, in trinitrobenzenesulfonic-acid-(TNBS induced rat colitis. Two hours subsequent to induction of colitis using TNBS in rats, cisapride (2 mg/kg, intraperitoneally (i.p; 4 mg/kg, orally (p.o and dexamethasone (1 mg/kg, i.p; 2 mg/kg, p.o were administrated for 6 days. Animals were thereafter euthanized; macroscopic, histological, and biochemical assessments and ELISA test were carried out on distal colon samples. Our data showed that dexamethasone treatment (i.p, p.o significantly decreased macroscopic and microscopic damage and also biochemical markers, but there were no significant differences in aforementioned parameters between cisapride (i.p or p.o and TNBS-treated rats. It can be deduced that because the severity of colitis produced by TNBS is massive (through various pathways, cisapride could not bring about more colitis damages through 5HT4 receptors. Based on the present study further researches are required for investigating the exact roles of 5HT4 receptors in the pathogenesis of ulcerative colitis.

  14. Effect of hydroxypropyl-β-cyclodextrin on the stability of cisapride in oral suspensions

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    Jutima Boonleang


    Full Text Available Cisapride (CIS is a gastrointestinal prokinetic agent. It has been associated with rare, but serious cardiac side effects.However, it does not affect psychomotor functions or induce central depressant adverse effects. As liquid formulations arerequired in a number of cases, an oral suspension of CIS was developed from CIS tablets. The objective of this study was toinvestigate the effect of hydroxypropyl--cyclodextrin (HP--CD on the stability of CIS in oral suspension with an ultimateaim to formulate a more stable CIS oral suspension. Six batches of CIS oral suspensions, namely, 0 (control, 0.3, 1.6, and 3%HP--CD containing formulations were prepared. They were stored at 5°C and 30°C. The amounts of CIS in the suspensionswere determined by a validated stability-indicating HPLC-DAD method. The stability was assessed based on the 90%remaining. The changes in the amounts of CIS over time were statistically analyzed by ANOVA and ANCOVA. At 5°C, HP--CD had no significant effect on the stability of CIS. CIS in all four formulations was stable for at least 12.5 months. At 30°C,HP--CD affected the stability of CIS. CIS was most stable in 0.3% HP--CD containing formulation with the observed t90 ofapproximately 11 months as compared to 7 months in control formulation.

  15. Simultaneous stability-indicating HPLC method for the determination of cisapride, methylparaben and propylparaben in oral suspension

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    Jutima Boonleang


    Full Text Available A simultaneous stability-indicating HPLC method for the determination of cisapride, methylparaben and propylparabenin oral suspensions has been developed and validated. Baseline separation was achieved on a C18 column at room temperature(25°C by gradient elution with mobile phase consisting of solvent A: 10% v/v acetonitrile in 0.13% w/v sodium-1-pentanesulfonate pH 8 and solvent B: acetonitrile. The gradient program was as follows: 0-5 min: 20 to 56% solvent B; 5-7min: 56 to 85% solvent B; 7-10 min: 85% solvent B. The flow rate of mobile phase was 1.2 mL/min. The injection volume was20 L. Detection and peak purity assessments were performed by photo-diode array detector set at 275 nm with scan modein the range of 190-400 nm. The method was selective, accurate and precise. It provided chromatograms with good peak shapeand acceptable resolutions of greater than 4.4 for all analytes including the degradation products formed in oral suspensionsin about 8.5 min. All analyte peaks were pure. The accuracy of all analytes was in the range of 99.20-100.6%. The within-runand between-run relative standard deviations were less than 1.50%. The calibration curves for cisapride, methylparaben, andpropylparaben were linear over the concentration range of 10.0-75.0 g/mL, 8.0-100.0 g/mL, and 0.8-10.0 g/mL, respectivelywith r2 greater than 0.999. This developed method was successfully applied to the stability study of cisapride, methylparabenand propylparaben in oral suspension formulations.


    NARCIS (Netherlands)



    In a double-blind crossover study lower esophageal sphincter pressure and distal esophageal motility were studied in 10 patients with progressive systemic sclerosis or mixed connective tissue disease, following a single intravenous dose of cisapride or placebo. The measurements were carried out unde

  17. High-resolution manometric evaluation of the effects of cisapride on the esophagus during administration of solid and liquid boluses in awake healthy dogs. (United States)

    Ullal, Tarini V; Kass, Philip H; Conklin, Jeffrey L; Belafsky, Peter C; Marks, Stanley L


    OBJECTIVE To validate the use of high-resolution manometry (HRM) in awake, healthy dogs and compare the effects of bolus type (liquid vs solid) and drug treatment (saline [0.9% NaCl] solution [SS] vs cisapride) on esophageal pressure profiles. ANIMALS 8 healthy dogs. PROCEDURES In a crossover study, each dog received SS (10 mL) IV, and HRM was performed during oral administration of 10 boluses (5 mL each) of water or 10 boluses (5 g each) of canned food. Cisapride (1 mg/kg in 60 mL of SS) was subsequently administered IV to 7 dogs; HRM and bolus administration procedures were repeated. Two to 4 weeks later, HRM was repeated following administration of SS and water and food boluses in 4 dogs. Pressure profile data were obtained for all swallows, and 11 outcome variables were statistically analyzed. RESULTS After SS administration, predicted means for the esophageal contractile integral were 850.4 cm/mm Hg/s for food boluses and 660.3 cm/mm Hg/s for water boluses. Predicted means for esophageal contraction front velocity were 6.2 cm/s for water boluses and 5.6 cm/s for food boluses after SS administration. Predicted means for residual LES pressure were significantly higher following cisapride administration. CONCLUSIONS AND CLINICAL RELEVANCE Results indicated that HRM was feasible and repeatable in awake healthy dogs of various breeds and sizes. Stronger esophageal contractions and faster esophageal contraction velocity occurred during solid bolus and liquid bolus swallows, respectively. Lower esophageal sphincter pressure increased significantly following cisapride administration. Esophageal contractions and bolus transit latency should be further evaluated by HRM in clinically dysphagic dogs.

  18. Cisapride a green analytical reagent for rapid and sensitive determination of bromate in drinking water, bread and flour additives by oxidative coupling spectrophotometric methods (United States)

    Al Okab, Riyad Ahmed


    Green analytical methods using Cisapride (CPE) as green analytical reagent was investigated in this work. Rapid, simple, and sensitive spectrophotometric methods for the determination of bromate in water sample, bread and flour additives were developed. The proposed methods based on the oxidative coupling between phenoxazine and Cisapride in the presence of bromate to form red colored product with max at 520 nm. Phenoxazine and Cisapride and its reaction products were found to be environmentally friendly under the optimum experimental condition. The method obeys beers law in concentration range 0.11-4.00 g ml-1 and molar absorptivity 1.41 × 104 L mol-1 cm-1. All variables have been optimized and the presented reaction sequences were applied to the analysis of bromate in water, bread and flour additive samples. The performance of these method was evaluated in terms of Student's t-test and variance ratio F-test to find out the significance of proposed methods over the reference method. The combination of pharmaceutical drugs reagents with low concentration create some unique green chemical analyses.

  19. 阿片样物质介导多潘立酮和西沙必利对小鼠的镇痛作用%Opioid mediated anti-nociceptive effect of domperidone and cisapride in mice

    Institute of Scientific and Technical Information of China (English)

    Isabella TOPNO; Mohammed ASAD; Deepak Gopal SHEWADE; Chanolean SHASHINDRAN; Subramanyan RAMASWAMY


    AIM: To study the anti-nociceptive effect of domperidone and cisapride in mice. METHODS: Initially, the effect of these drugs on motor activity was tested using rotarod. The anti-nociception was tested using chemical and mechanical assay. In the chemical assay, the number of abdominal constrictions either in the saline treated animals or in the domperidone/cisapride (1, 5, or 10 mg/kg either po or ip) treated mice, were recorded for a period of 30 main after acetic acid challenge (10mL/kg, of 0.6 % acetic acid ip). In the tail clip assay, the time taken by the mouse to make attempts to dislodge the bulldog clamp placed at the tail (reaction time) was recorded with a cut off time of 30 s. The role of opioid pathways was examined by pretreating the animals with naloxone (1 mg/kg, ip) 30 min prior to domperidone and cisapride. RESULTS: Domperidone and cisapride, both reduced the number of abdominal constrictions when given orally or intraperitoneally.Domperidone (5 mg/kg) inhibited it to the extent of 57.0 % after po and 54.6 % after ip. The inhibition after cisapride ( 5 mg/kg ) was 65.1% ( po ) and 71.6 % (ip). Naloxone pretreatnent reduced this inhibition (57.0 % vs 10.3 % for domperidone and induced hyperalgesia by antagonizing the inhibition and enhanced analgesia to the extent of 28.4 % for cisapride ). The reaction time was increased by domperiidone (10 mg/kg, ip) from 1.6 s±l.0 s to 14.8s ±0.5 s and cisapride (10 mg/kg, ip) from 3.3 s ± 1.0s to 14.8 s ± 0.5 s. CONCLUSION: Domperidone and cisapride exhibited a significant anti-nocicepfve activity after oral as well as intraperitoneal administration.A role for opioid pathways is indicated. Since domperidone is likely to exert less extrapyramidal effects,it can be substituted for metoclopramide, which is now widely used as an analgesic either alone or as an adjuvant.

  20. Novel oxidative coupling reactions of cisapride or metaclopramide with phenoxazines and their applications in the determination of nitrite at trace level in environmental samples (United States)

    AL-Okab, Riyad Ahmed; Syed, Akheel Ahmed


    Phenoxazine (PNZ), 2-chlorophenoxazine (CPN) and 2-trifluoromethylphenoxazine (TPN) were used as new class of spectrophotometric reagents for the determination of nanoamounts of nitrite in presence of cisapride (CSP) and metaclopramide (MCP) as new electrophilic coupling reagents. The methods were based on the oxidation of CSP or MCP by nitrite in hydrochloric acid medium and coupling with PNZ, CPN or TPN to yield red color derivatives which were stable for about 3 h and having an absorbance maximum in the range 520-530 nm. Beer's law is obeyed for nitrite in the concentration range 0.08-0.80 and 0.13-1.60 μg ml -1 for phenoxazine-cisapride and phenoxazine-metaclopramide, respectively. The optimum reaction conditions and other important analytical parameters were established to enhance the sensitivity of these methods. Interference due to various non-target ions was also investigated. The methods were applied to the analysis of nitrite in environmental samples. The performance of proposed methods were evaluated by Student's t-test and variance ratio F-test indicated the significance of proposed methods over the reference spectrophotometric method (Association of Official Analytical Communities (AOAC) method for the determination of nitrite in water samples).

  1. Noninvasive Assessment of Gastric Emptying by Near-Infrared Fluorescence Reflectance Imaging in Mice: Pharmacological Validation with Tegaserod, Cisapride, and Clonidine

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    Hans-Ulrich Gremlich


    Full Text Available Noninvasive near-infrared fluorescence reflectance imaging (FRI is an in vivo technique to assess physiological and molecular processes in the intact organism. Here we describe a method to assess gastric emptying in mice. TentaGel™ beads with covalently bound cyanine dye (Cy5.5 conjugates as fluorescent probe were administered by oral gavage. The amount of intragastric beads/label was derived from the fluorescence signal intensity measured in a region of interest corresponding to the mouse stomach. The FRI signal intensity decreased as a function of time reflecting gastric emptying. In control mice, the gastric half-emptying time was in agreement with literature data. Pharmacological modulation of gastric motility allowed the evaluation of the sensitivity of the FRI-based method. Gastric emptying was either stimulated or inhibited by treatment with the 5-HT4 receptor agonists tegaserod (Zelnorm® and cisapride or the α2-receptor agonist clonidine, respectively. Tegaserod and cisapride dose-dependently accelerated gastric emptying. In contrast, clonidine dose-dependently delayed gastric emptying. In conclusion, FRI using fluorescently labeled beads allows the reliable determination of gastric emptying as well as the assessment of pharmacological interventions. The technique thus offers the potential to characterize molecular targets and pathways involved in physiological regulation and pharmacological modulation of gastric emptying.

  2. Dissolution Improvement of Cisapride by Solid Dispersion with HPMC%西沙必利-HPMC固体分散体对其体外药物释放的促进作用

    Institute of Scientific and Technical Information of China (English)

    魏振平; 毛世瑞; 毕殿洲; 李勇


    目的以羟丙基甲基纤维素(HPMC-E5 LV)为载体材料制备HPMC-西沙必利固体分散体,通过提高模型药物的溶解度来改善药物的体外释放.方法分别用乙醇和人工胃液将药物和载体材料溶解,使药物均匀分散在载体中, 减压干燥除去溶剂得到HPMC-西沙必利固体分散物; 用X射线粉末衍射法分别测定了纯载体材料、纯西沙必利、载体材料和西沙必利物理混合物以及载体材料和西沙必利固体分散体4:1的晶体衍射峰, 以确定是否有晶体存在; 分别考察纯西沙必利和HPMC-西沙必利固体分散体在水、人工胃液和人工肠液中的溶解度; 分别以纯西沙必利和载体材料和西沙必利固体分散体制备了西沙必利缓释片并考察了其在水和人工胃液中的药物释放.结果当载体与药物的比例达到4:1时,X 射线衍射实验表明药物的晶体峰已经消失, 形成无定型固体分散体; 与西沙必利原料药相比, 固体分散体中药物在人工胃液、水和人工肠液中的溶解度分别提高了239.4%、132.6% 和117.9%; 体外药物释放结果表明, 当以水和人工胃液为介质时,药物从固体分散体制备的缓释片中的释放速度要快于用纯原料药制备的缓释片中的释放速度, 体外释药规律可以用 Higuchi's 动力学方程描述.结论以HPMC为载体材料与西沙必利制成固体分散体, 可以通过改善药物的溶解度来加快缓释制剂中药物的溶出速度.%Aim To prepare a solid dispersion of cisapride with hydroxypropylmethyl cellulose (HPMC E5 LV) as carrier for the purpose of accelerating the in vitro drug release by means of improving the solubility of the model drug. Methods Alcohol and simulated gastric fluid (SGF) were used to dissolve cisapride and HPMC in order to make the model drug dispersed homogeneously in the carrier. The HPMC-cisapride solid dispersion was then obtained by conventional solvent evaporation method. Powder X

  3. Effect of cisapride combinning doxepin treating functional dispepsia in women' climacterium%西沙比利与多滤平联合治疗更年期功能性消化不良的疗效观察

    Institute of Scientific and Technical Information of China (English)

    刘伟; 孔令霞; 秦永春


    @@ 西沙比利(cisapride)是一种新型的全胃肠道动力药,目前广泛应用于临床,治疗各种胃肠道功能紊乱性疾病.功能性消化不良是更年期胃肠自主神经功能紊乱的常见症状.为了观察西沙比利对更年期功能性消化不良的疗效,我们应用西沙比利与多滤平联合治疗30例患者,并与单独使用多滤平治疗的30例患者进行比较,观察西药联合应用对更年期胃肠自主神经功能紊乱的治疗效果.

  4. Efeito da cisaprida e da fisioterapia respiratória sobre o refluxo gastroesofágico de lactentes chiadores segundo avaliação cintilográfica Effects of cisapride and chest physical therapy on the gastroesophageal reflux of wheezing babies based on scintigraphy

    Directory of Open Access Journals (Sweden)

    Maria Angela G.O. Ribeiro


    Full Text Available OBJETIVO: analisar o efeito da cisaprida e da fisioterapia respiratória em lactentes chiadores (LC, com doença do refluxo gastroesofágico (DRGE. MÉTODOS: avaliamos, prospectivamente, em 13 LC com DRGE e 12 sem DRGE, a densidade nuclear de tecnécio (99Tc em 3 topografias esofágicas. Os 2 grupos foram submetidos à investigação clínica, exames laboratoriais, radiológicos e cintilográficos para investigação etiológica da síndrome do LC e DRGE. A técnica fisioterápica denominada aceleração de fluxo expiratório (AFE foi realizada antes e após tratamento com cisaprida. O tempos totais de RGE(TTRGE, primeiramente durante a cintilografia basal, e em seguida, durante a AFE, foram analisados e somados, para cada topografia esofágica. RESULTADOS: a cisaprida diminuiu o TTRGE, com significância estatística somente no terço superior do esôfago (p OBJECTIVE: to evaluate the effect of cisapride and chest physical therapy on the gastroesophageal reflux of wheezing babies. METHODS: we prospectively assessed the presence of technetium (99Tc in the upper, middle, and lower esophagus of 25 wheezing babies (13 with GERD and 12 without GERD using scintigraphy. Both groups underwent clinical investigation, including laboratory, X-ray and scintigraphy tests, for the etiology of the wheezing baby syndrome (WBS and GERD. Expiratory Flow Acceleration (EFA was performed before and after treatment with cisapride. The total time of GER episodes was accounted for each portion of the esophagus during scintigraphy and during EFA. RESULTS: cisapride significantly reduced the total reflux time in the upper esophagus (P < 0.05, but showed no influence during EFA. After cisapride therapy, EFA increased the total reflux time in the upper and medium esophagus; however, no statistical significance was found. Infants with GERD presented a shorter total reflux time in the distal esophagus (P<0.05 during EFA. After cisapride treatment, no statistical

  5. 西沙必利联合双歧三联活菌治疗功能性消化不良的临床观察%Clinical Observation of Cisapride Combined with Bifid Triple Viable in the Treatment of Functional Dyspepsia

    Institute of Scientific and Technical Information of China (English)



    OBJECITVE: To observe the clinical efficacy of cisapride combined with bifid triple viable in the treatment of functional dyspepsia (FD). METHODS: From Jun. 2009 to Jun. 2010, 130 FD patients were randomly classified into 2 groups, which observation group with 65 cases was treated with cisapride combined with bifid triple viable and control group with 65 cases was only treated with cisapride. Clinical efficacy and main symptoms were observed and compared between 2 groups. RESULTS: The total effective rates(90.8% ) in observation group were significantly higher than in control group(67.7% ), there was significant difference (P<0.05). Compared with pre-treatment, the scores of postprandial fullness, epigastric pain, early satiety and nausea were significantly decreased after treatment in both 2 groups, there were significant differences(P<0.05). Moreover, the scores of postprandial fullness, epigastric pain, early satiety and nausea in observation group after treatment were significantly lower than those in control group, there were significant differences (P<0.05). CONCLUSION: Cisapride combined with bifid triple viable in the treatment of FD can improve clinical efficacy and clinical symptoms significantly, compared with cisapride alone.%目的:观察西沙必利联合双歧三联活茵治疗功能性消化不良(FD)的临床疗效.方法:将2009年6月-2010年6月在我院治疗的130例FD患者随机均分为2组,观察组65例采用西沙必利联合双歧三联活茵治疗,对照组65例仅采用西沙必利治疗,观察比较2组的临床疗效和主要症状变化.结果:观察组的总有效率(90.8%)明显高于对照组(67.7%),2组比较差异有统计学意义(P<0.05).2组治疗后餐后饱胀、上腹胀痛、早饱和恶心评分均较治疗前下降,且差异有统计学意义(P<0.05).观察组治疗后餐后饱胀、上腹胀痛、早饱和恶心评分均低于同期对照组,且差异有统计学意义(P<0.05).结论:西沙必利联

  6. Absorption kinetics of oral sotalol combined with cisapride and sublingual sotalol in healthy subjects

    NARCIS (Netherlands)

    Deneer, V.; A Lie, Huen; Proost, Hans; Kelder, J.C; Brouwers, J.R.B.J.; Kingma, J.H.


    Aims To study the absorption kinetics of sotalol following administration of different formulations. A formulation which results in fast absorption might be useful in the episodic treatment of paroxysmal supraventricular tachycardia (SVT), atrial fibrillation (Afib) or atrial flutter (Afl). Methods

  7. Drug: D02092 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D02092 Drug Cisapride (JAN); Cisapride monohydrate; Propulsid (TN) C23H29ClFN3O4. H...TINAL DISORDERS A03F PROPULSIVES A03FA Propulsives A03FA02 Cisapride D02092 Cisapride...rotonin 5-HT4-receptor [HSA:3360] [KO:K04160] Cisapride [ATC:A03FA02] D02092 Cisapride (JAN) CAS: 260779-88-

  8. Drug: D00274 [KEGG MEDICUS

    Lifescience Database Archive (English)

    Full Text Available D00274 Drug Cisapride (USAN/INN) C23H29ClFN3O4 465.1831 465.9455 D00274.gif Stimula...L GASTROINTESTINAL DISORDERS A03F PROPULSIVES A03FA Propulsives A03FA02 Cisapride D00274 Cisapride...hodopsin family Serotonin 5-HT4-receptor [HSA:3360] [KO:K04160] Cisapride [ATC:A03FA02] D00274 Cisapride (US

  9. 西沙比利对肝硬化大鼠小肠细菌及内毒素转位的影响%Effects of cisapride on intestinal bacterial and endotoxin translocation in cirrhotic rats

    Institute of Scientific and Technical Information of China (English)

    张顺财; 王唯; 任卫英; 周康; 贺伯明; 朱无难


    目的研究西沙比利对肝硬化大鼠小肠细菌过度生长(IBO),细菌及内毒素转位,小肠转运时间及小肠通透性的作用. 方法正常对照组大鼠25只,肝硬化对照组大鼠25只,肝硬化治疗组20只(用等渗盐水),另20只肝硬化大鼠用西沙比利治疗,动物均测定各种参数如细菌和内毒素转位,小肠细菌过度生长,小肠转运时间及通透性. 结果 48%肝硬化大鼠发生细菌转位,与无IBO肝硬化大鼠比较,IBO肝硬化大鼠的内毒素和细菌转位发生率高,肠转远时间延长,小肠通透性增高.BT的细菌与IBO主菌群一致.与对照组比较,西沙比利处理的肝硬化大鼠肠细菌和内毒素转位及IBO发生率降低,这与肠转运时间增快及通透性降低密切相关. 结论肝硬化大鼠内毒素和细菌转位可能是由于IBO和肠通透性增加的结果,而IBO的发生可能是由于肠转运时间延长所致.西沙比利可加速小肠转运时间,改善小肠通透性,这有助于防治小肠细菌和内毒素转位.

  10. 血浆中西沙必利胶囊的HPLC法分析及生物等效性研究%Determination and Bioequivalent Study of Cisapride in Human Plasma by HPLC

    Institute of Scientific and Technical Information of China (English)

    傅军; 熊玉卿


    目的:建立人血浆西沙必利的反相高效液相色谱荧光检测分析方法,并对其在人体内的生物等效性进行研究.方法:血浆样品在碱性条件下经三氯甲烷-异丙醇(9:1)提取,用KromasilC18柱,乙腈-0.05 mol@L-1磷酸盐缓冲液-三乙胺(39:60:1)为流动相,流速1.0 mL@min-1 ,荧光检测激发波长272 nm,发射波长350 mm等条件下,分析测定.结果:西沙必利在2.5~120μg@L-1浓度范围内呈良好线性关系(r=0.999 2).血浆最低检出浓度为1 ng@mL-1结论:本法准确灵敏,重现性好,可用于西沙必利的药代动力学研究.

  11. Drug treatment

    Institute of Scientific and Technical Information of China (English)


    950229 A controlled multi—center clinical trial oncisapride in treatment of functional dyspepsia.WANGBaoen(王宝恩),et al.Beijing Friendship Hosp,Bei-jing.100050.Chin J Intern Med 1995;34(3):180—184.A controlled muhi-centre clinical trial was con-ducted for evaluating the efficacy and safety of cis-apride in the treatment of 414 cases of functional dys-pepsia with 169 cases as control.Cisapride were given

  12. Effect of proton pump inhibitor combined with cisapride on difficultly treating bronchial asthma with gastroesophageal reflux disease%质子泵抑制剂联用西沙必利在治疗难治性支气管哮喘并胃食管反流病中的作用

    Institute of Scientific and Technical Information of China (English)

    李珂欣; 贺凤玲


    目的观察质子泵抑制剂联用西沙必利对难治性支气管哮喘并胃食管反流病的治疗作用.方法采用随机、双盲、安慰剂对照方法,将87例难治性支气管哮喘并胃食管反流病患者分为治疗组(45例)和对照组(42例),治疗组在常规抗哮喘药物治疗的同时加服奥美拉唑和西沙必利,对照组加服安慰剂.记录患者的哮喘评分、胃食管反流症状持续时间,按需吸入二丙酸倍氯米松的剂量,按需吸入β2受体激动剂的次数和测定患者的1 s用力呼气容积占预计值百分比(FEV1占预计值%),最大呼气容量百分比(PEF%)及PEF变异率的变化.结果治疗后2组每天哮喘症状计分、胃食管反流症状持续时间比较有显著性差异(P<0.01);治疗组按需吸入二丙酸倍氯米松的平均剂量显著减少(P<0.01);按需吸入β2受体激动剂的平均次数显著减少(P<0.01);治疗后FEV1占预计值%、PEF%及PEF变异率改善更明显(P<0.01).结论难治性支气管哮喘并胃食管反流病时,在抗哮喘药物进行治疗的基础上加用抗胃食管反流治疗,对难治性哮喘有明确的治疗作用.

  13. 雷尼替丁、甲氧氯普胺和西沙必利治疗功能性消化不良上腹痛40例%Treating functionality dyspepsia epigastralgia by Ranitidine. Cisapride Tablet and Metoclopramide in 40 cases

    Institute of Scientific and Technical Information of China (English)




  14. Relative efficacy of some prokinetic drugs in morphine-induced gastrointestinal transit delay in mice

    Institute of Scientific and Technical Information of China (English)

    AD Suchitra; SA Dkhar; DG Shewade; CH Shashindran


    AIM: To study the relative efficacy of cisapride,metoclopramide, domperidone, erythromycin and mosapride on gastric emptying (GE) and small intestinal transit (SIT)in morphine treated mice.METHODS: Phenol red marker meal was employed to estimate GE and SIT in Swiss albino mice of either sex. The groups included were control, morphine 1 mg/kg (s.c. 15min before test meal) alone or with (45 min before test meal p.o.) cisapride 10 mg/kg, metoclopramide 20 mg/kg,domperidone 20 mg/kg, erythromycin 6 mg/kg and mosapride 20 mg/kg.RESULTS: Cisapride, metoclopramide and mosapride were effective in enhancing gastric emptying significantly (P<0.001)whereas other prokinetic agents failed to do so in normal mice. Metoclopramide completely reversed morphine induced delay in gastric emptying followed by mosapride.Metoclopramide alone was effective when given to normal mice in increasing the SIT. Cisapride, though it did not show any significant effect on SIT in normal mice, was able to reverse morphine induced delay in SIT significantly (P<0.001)followed by metoclopramide and mosapride.CONCLUSION: Metoclopramide and cisapride are most effective in reversing morphine-induced delay in gastric emptying and small intestinal transit in mice respectively.

  15. Is this a reflux patient or is it a patient with functional dyspepsia with additional reflux symptoms?

    DEFF Research Database (Denmark)

    Funch-Jensen, P


    of functional dyspepsia is less documented and in most studies the symptomatic pattern could not predict the pharmacologic principle of clinical benefit. This may be because a separation between presence of symptoms and presence of symptoms as a major problem has not been taken into account. Cisapride...

  16. Prokinetic Therapy Reduces Aspiration Pneumonia in Tube-Fed Patients With Severe Developmental Disabilities (United States)

    Pareek, Namita; Williams, John; Hanna, Deborah; Johnson, William D.; Minocha, Anil; Abell, Thomas L.


    To evaluate the clinical benefit of prokinetic therapy in aspiration pneumonia in patients with developmental disabilities, we conducted a retrospective study; records of 22 tube-fed patients were reviewed from December 1990 to October 1998 for a mean of 22.7 months before and 38.9 months during Cisapride therapy. Numbers of hospital admissions…

  17. Paracetamol, widely used hardly understood

    NARCIS (Netherlands)

    C.D. van der Marel (Caroline)


    markdownabstract__Abstract__ Paracetamol (APAP), in the USA known as acetaminophen, is widely used both in hospital settings and at home for antipyresis and mild (postoperative) pain. Although APAP is available over the counter and is ranked on the third place, following nystatin and cisapride, whe

  18. Quality of life and cost-effectiveness of combined therapy for reflux esophagitis

    Institute of Scientific and Technical Information of China (English)

    姒健敏; 王良静; 陈淑洁; 赵岚; 戴宁


    Objective : To evaluate clinical, Quality of Life (QoL) and medical cost outcomes in patients with symptomatic reflux esophagitis (RE) receiving different "triple combination therapy". Methods: A muhicenter medical effectiveness trial conducted in 10 hospitals of 5 regions in Zhejiang Province. 248 patient-volunteers were assigned to 8 weeks of " triple combination therapy" with Lansoprazole plus Cisapride and Sucralfate or Ranitidine plus Cisapride and Sucralfate. Main outcomes assessment included symptoms scale scores, RE severity, QoL at baseline and 8 weeks. Medical cost data were collected with cost analysis questionnaire. Resuits: (1)More Lansoprazole group patients noted RE symptoms resolution than Ranitidine group(92.3 % vs 78.4%, P 0.05) . (2)RE significantly impaired QoL of patients( P 0.05 ) . Conclusion : RE significantly impaired QoL of patients. "Triple combination therapies" can significantly improve RE symptoms and QoL. Lansoprazole combination therapy was more cost-effective than Ranitidine combination group.

  19. Study on the preventive effects of different drugs on reflux esophagitis in rats

    Institute of Scientific and Technical Information of China (English)

    WANG Tao; GONG Jun; CHEN Jie; CHENG Peng; CHANG Yin; WANG Jin-hai


    Objective: To observe the damage of mixed reflux to the rat esophageal mucosa, and investigate the preventive effects of cisapride, nabumetone and hydrotalcite on the damaged esophageal mucosa. Methods: Three hundred sixty-eight Sprague-Dawley rats were treated as esophagoduodenostomy and divided into four groups in random. Group Y: operation + saline as positive controls; Group P: operation + cisapride; Group R: operation + nabumetone; Group D: operation + hydrotalcite. Different drugs were perfused in the 1 st week after operation. The lesions of esophageal mucosa were observed in the 5th, 9th, 13th, 17th, 22nd, 28th, 35th and 40th week respectively, and evaluated the preventive effects of these drugs. Results: The lesions of esophageal mucosa in group Y were more severe than other three groups in different time (P < 0.05), and the incidence of Barrett's esophagus(BE), severe atypical hyperplasia and esophageal adenocarcinoma (EAC) in group Y were higher than others. After 22 weeks, the lesions in group P were more severe than group R and D, and there were obvious differences in different time ( P < 0.05); but the incidence of BE, severe atypical hyperplasia and EAC in group P had no significant difference with group R and group D( P > 0.05). Conclusion: BE, severe atypical hyperplasia and EAC could occur because of severe reflux esophagitis for a long term. Cisapride, nabumetone and hydrotalcite could reduce mucosa injury in reflux esophagitis and resist the development of BE, severe atypical hyperplasia and EAC.In addition, the curative effects of nabumetone and hydrotalcite were better than cisapride.

  20. Update on the evaluation of a new drug for effects on cardiac repolarization in humans: issues in early drug development


    Salvi, Vaibhav; Karnad, Dilip R.; Panicker, Gopi Krishna; Kothari, Snehal


    Following reports of death from cardiac arrhythmias with drugs like terfenadine and cisapride, the International Conference for Harmonization formulated a guidance (E14) document. This specifies that all new drugs must undergo a ‘thorough QT/QTc’ (TQT) study to detect drug-induced QT prolongation, a surrogate marker of ventricular tachycardia, especially torsades de pointes (TdPs). With better understanding of data from several completed TQT studies, regulatory requirements have undergone som...

  1. Elenoside increases intestinal motility

    Institute of Scientific and Technical Information of China (English)

    E Navarro; SJ Alonso; R Navarro; J Trujillo; E Jorge


    AIM: To study the effects of elenoside, an arylnaphthalene lignan from Justicia hyssopifolia, on gastrointestinal motility in vivo and in vitro in rats.METHODS: Routine in vivo experimental assessments were catharsis index, water percentage of boluses,intestinal transit, and codeine antagonism. The groups included were vehicle control (propylene glycol-ethanolplant oil-tween 80), elenoside (i.p. 25 and 50 mg/kg),cisapride (i.p. 10 mg/kg), and codeine phosphate (intragastric route, 50 mg/kg). In vitro approaches used isolated rat intestinal tissues (duodenum, jejunum, and ileum). The effects of elenoside at concentrations of 3.2× 10-4, 6.4 × 10-4 and 1.2 × 10-3 mol/L, and cisapride at 10-6 mol/L were investigated.RESULTS: Elenoside in vivo produced an increase in the catharsis index and water percentage of boluses and in the percentage of distance traveled by a suspension of activated charcoal. Codeine phosphate antagonized the effect of 25 mg/kg of elenoside. In vitro, elenoside in duodenum, jejunum and ileum produced an initial decrease in the contraction force followed by an increase.Elenoside resulted in decreased intestinal frequency in duodenum, jejunum, and ileum. The in vitro and in vivo effects of elenoside were similar to those produced by cisapride.CONCLUSION: Elenoside is a lignan with an action similar to that of purgative and prokinetics drugs.Elenoside, could be an alternative to cisapride in treatment of gastrointestinal diseases as well as a preventive therapy for the undesirable gastrointestinal effects produced by opioids used for mild to moderate pain.

  2. Quality of life and cost-effectiveness of combined therapy for reflux esophagitis

    Institute of Scientific and Technical Information of China (English)

    姒健敏; 王良静; 陈淑洁; 赵岚; 戴宁


    Objective: To evaluate clinical, Quality of Life (QoL) and medical cost outcomes in patients with symptomatic reflux esophagitis (RE) receiving different ″triple combination therapy″. Methods: A multicenter medical effectiveness trial conducted in 10 hospitals of 5 regions in Zhejiang Province. 248 patient-volunteers were assigned to 8 weeks of ″ triple combination therapy″ with Lansoprazole plus Cisapride and Sucralfate or Ranitidine plus Cisapride and Sucralfate. Main outcomes assessment included symptoms scale scores, RE severity, QoL at baseline and 8 weeks. Medical cost data were collected with cost analysis questionnaire. Results: (1)More Lansoprazole group patients noted RE symptoms resolution than Ranitidine group(92.3% vs 78.4%, P0.05). (2)RE significantly impaired QoL of patients(P0.05). Conclusion: RE significantly impaired QoL of patients. ″Triple combination therapies″ can significantly improve RE symptoms and QoL. Lansoprazole combination therapy was more cost-effective than Ranitidine combination group.

  3. Effect of drug utilization reviews on the quality of in-hospital prescribing: a quasi-experimental study

    Directory of Open Access Journals (Sweden)

    Chabot Isabelle


    Full Text Available Abstract Background Drug utilization review (DUR programs are being conducted in Canadian hospitals with the aim of improving the appropriateness of prescriptions. However, there is little evidence of their effectiveness. The objective of this study was to assess the impact of both a retrospective and a concurrent DUR programs on the quality of in-hospital prescribing. Methods We conducted an interrupted time series quasi-experimental study. Using explicit criteria for quality of prescribing, the natural history of cisapride prescription was established retrospectively in three university-affiliated hospitals. A retrospective DUR was implemented in one of the hospitals, a concurrent DUR in another, whereas the third hospital served as a control. An archivist abstracted records of all patients who were prescribed cisapride during the observation period. The effect of DURs relative to the control hospital was determined by comparing estimated regression coefficients from the time series models and by testing the statistical significance using a 2-tailed Student's t test. Results The concurrent DUR program significantly improved the appropriateness of prescriptions for the indication for use whereas the retrospective DUR brought about no significant effect on the quality of prescribing. Conclusion Results suggest a retrospective DUR approach may not be sufficient to improve the quality of prescribing. However, a concurrent DUR strategy, with direct feedback to prescribers seems effective and should be tested in other settings with other drugs.

  4. Clinical Studies on Functional Dyspepsia Treated with Different Dosage-Form of Zhishi Xiaopi Pill Recipe (枳实消痞丸方)

    Institute of Scientific and Technical Information of China (English)

    窦丹波; 蔡淦; 王松坡; 倪克中; 唐静芬


    Objective: To explore the clinical effect of three different dosage-forms of Zhishi Xiaopi Pill (ZSXPP, 枳实消痞丸) recipe on functional dyspepsia (FD). Methods: The total of 158 patients were included in this study and were randomly divided into four groups. Three group patients of FD were respectively treated with three different dosage-forms of ZSXPP, while the control group were treated with cisapride. Results: The treatment outcome indicated that there was no difference in the total therapeutic efficacies of these four groups. The tension of vagus nerve and the plasma level of motilin in FD patients were significantly increased by the treatment with ZSXPP; the impaired contraction function of lower esophageal sphincter in some FD patients was improved, too. Conclusion: All of three different dosage-forms of ZSXPP were as effective as cisapride on FD. The efficacy was partly due to the improvement of esophageal and gastric dynamics which was probably related to the increasing of the tension of vagus nerve and the plasma level of motilin.

  5. Comparison between empirical prokinetics, Helicobacter testand-treat and empirical endoscopy in primary-care patients presenting with dyspepsia: A one-year study

    Institute of Scientific and Technical Information of China (English)

    Wayne HC Hu; CK Chan; Gabriel M Leung; WM Hui; SK Lam; Cindy LK Lam; WM Wong; KF Lam; KC Lai; YH Wong; Benjamin CY Wong; Annie OO Chan


    AIM: To investigate the optimal strategy to treat dyspeptic patients in primary care.METHODS: Dyspeptic patients presenting to primary care outpatient clinics were randomly assigned to:(1) empirical endoscopy, (2)Hpylori test-and-treat,and (3) empirical prokinetic treatment with cisapride.Early endoscopy was arranged if patients remained symptomatic after 2 wk. Symptom severity, quality-oflife (SF-36) as well as patient preference and satisfaction were assessed. All patients underwent endoscopy by wk 6. Patients were followed up for one year.RESULTS: Two hundred and thirty four patients were recruited (163 female, mean age 49). 46% were H pylori positive. 26% of H pylori tested and 25% of empirical prokinetic patients showed no improvement at wk 2follow-up and needed early endoscopy. 15% of patients receiving empirical cisapride responded well to treatment but peptic ulcer was the final diagnosis. Symptom resolution and quality-of-life were similar among the groups. Costs for the three strategies were HK$4343,$1771 and $1750 per patient. 66% of the patients preferred to have early endoscopy.CONCLUSION: The three strategies are equally effective. Empirical prokinetic treatment was the least expensive but peptic ulcers may be missed with this treatment. The H pylori test-and-treat was the most cost-effective option.

  6. Omeprazole for Refractory Gastroesophageal Reflux Disease during Pregnancy and Lactation

    Directory of Open Access Journals (Sweden)

    John K Marshall


    Full Text Available Symptomatic gastroesophageal reflux is a common complication of pregnancy and lactation. However, the safety of many effective medical therapies, including oral proton pump inhibitors, has not been well defined. The administration of oral omeprazole to a 41-year-old female during the third trimester of pregnancy, after ranitidine and cisapride failed to control her refractory gastroesophageal reflux, is reported. No adverse fetal effects were apparent, and the patient elected to continue omeprazole therapy (20 mg/day while breastfeeding. Peak omeprazole concentrations in breast milk (58 nM, 3 h after ingestion were less than 7% of the peak serum concentration (950 nM at 4 h, indicating minimal secretion. Although omeprazole is a potentially useful therapy for refractory gastroesophageal reflux during pregnancy and lactation, further data are needed to define better its safety and efficacy.

  7. 胃肠舒对胃肠平滑肌细胞内皮型一氧化氮合酶mRNA表达的影响%Effect of Weichangshu on release of nitrogen monoxidum and mRNA expression of endothelial nitricoxide synthase in gastrointestinal smooth muscle cells

    Institute of Scientific and Technical Information of China (English)

    郭金秀; 刘孟安


    Objective: To investigate the mechanism of Weichangshu promots gastrointestinal motility. Methods: Primary culture gastrointestinal smooth muscle cells, experiment was divided into Weichangshu high-dose group, Weichangshu middle-dose group, Weichangshu low-dose group, Cisapride group, and normal control group, tested drugs were used in each group interfere with cell 24h, detect the release of NO using Flow cytometry. Then extract the total RNA of cells, use reverse transcription-polymerase chain reaction, semi-quantitative analysis the changes of the expression of eNOS mRNA levels in gastrointestinal smooth muscle cells. Results: Compared with the normal control group, fluorescence intensity of NO release significantly reduced (P增多,Ca信号系统引发一系列生理功能而促进胃肠平滑肌收缩.

  8. Use of 24 h Esophageal pH Monitoring to Demonstrate Alkaline Reflux as a Complication of Gastric Bypass Surgery

    Directory of Open Access Journals (Sweden)

    J Patrick Shoenut


    Full Text Available A 35-year-old female who had previously undergone a gastric stapling procedure for morbid obesity presented with a persistent nocturnal cough that was treated over a three-year period as a gastric acid reflux complication of the bypass surgery. A barium swallow demonstrated gastroesophageal reflux, but the symptoms did not resolve after treatment with omeprazole and cisapride. Twenty-four hour esophageal pH monitoring subsequently found alkaline reflux in excess of 17% of the total time, with no acid reflux demonstrated. Surgical revision of the bypass Leaving the hiatus alone corrected the reflux complication and the symptoms resolved without further treatment. The diagnostic capability of pH monitoring is illustrated in a patient with an unusual surgical complication.

  9. [Therapeutic principles in gastroesophageal reflux]. (United States)

    Chassany, O; Elkharrat, D; Bergmann, J F; Segrestaa, J M


    Gastroesophageal reflux is a common disease. Its chronic course, even if mild, is sometimes complicated by erosive oesophagitis. Drug therapy acts against gastric acidity and motility disorders. Treatment of gastroesophageal reflux disease has three aims: improvement of symptoms and quality of life, healing erosive lesions and prevention of symptomatic and endoscopic relapses. Non-drug measures are always useful, even if their efficacy is not well established. Initial therapy of a symptomatic reflux or mild oesophagitis is most of the time effective (antacids, prokinetics, H2 receptor antagonists). Proton-pump inhibitors are also effective in healing and preventing severe oesophagitis. Questions about long-term treatment adverse events with powerful acid inhibitors, such as hypergastrinemia and the risk of gastric carcinoid tumours seem to be resolved. Studies are requested to define the optimal long-term maintenance treatment with cisapride, H2 receptor antagonists or proton-pump inhibitors at low doses in prevention of symptomatic and mild oesophagitis relapses.

  10. 止吐药物对大鼠实验性晕动病模型产生的胃排空抑制的影响%Effect of antiemetic drugs on decrease in gastric emptying in experimental model of motion sickness in rats

    Institute of Scientific and Technical Information of China (English)

    Gupta YK; Chaudhary G


    AIM: To study the effect of pretreatment with different antiemetic drugs on the motion sickness-induced inhibitionin gastric emptying. METHODS: The rats were rotated for a period of 45 min at the rate of 30 rotations per min.RESULTS: Rotating the rats caused a significant decrease in gastric emptying as compared to the non-rotatedgroup. Pretreatment with scopolamine (5 mg/kg, ip) did not reverse the delay in gastric emptying, while it per secaused inhibition of gastric emptying in the non-rotated group. Similarly other drugs mepyramine, cisapride, andgranisetron did not have any effect on delay in gastric emptying caused by rotation. However beta blocker propra-nolol could partially but significantly reverse the decrease in gastric emptying. CONCLUSION: The present studydemonstrated the potential use of propranolol as adjuvant with conventional antiemetics for motion sickness tocombat associated secondary symptoms.

  11. Effect of antiemetic drugs on decrease in gastric emptying in experimental model of motion sickness in rats

    Institute of Scientific and Technical Information of China (English)



    AIM:To study the effect of pretreatment with different antiemetic drugs on the motion sickness-induced inhibition in gastric emptying.METHODS:The rats were rotated for a period of 45 min at the rate of 30 rotations per min.RESULTS:Rotating the rats caused a significant decrease in gastric emptying as cvompared to the non-rotated group.Pretreatment with scopolamine(5 mg/kg,ip)did not reverse the delay in gastric emptying,while it per se caused inhibition of gastric emptying in the non-rotated group.Similarly other drugs mepyramine,cisapride,and granisetron did not have any effect on delay in gastric emptying caused by rotation.However beta blocker propranolol could partially but significantly reverse the decrease in gastric emptying.CONCLUSION:The present study demonstrated the potential use of propranolol as adjuvant with conventional antiemetics for motion sickness to combat associated secondary symptoms.

  12. Prevention of postoperative ileus

    DEFF Research Database (Denmark)

    Holte, Kathrine; Kehlet, H


    Postoperative ileus (PI) is a major contributor to postoperative morbidity and prolonged convalescence after major surgical procedures. The pathophysiology of PI is multifactorial, including activation of the stress response to surgery, with inhibitory sympathetic visceral reflexes and inflammatory...... mediators. We update evidence on the advances in the prevention and treatment on PI. As single interventions, continuous thoracic epidural analgesia with local anesthetics and minimally invasive surgery are the most efficient interventions in the reduction of PI. The effects of pharmacological agents have...... generally been disappointing with the exception of cisapride and the introduction of the new selective peripherally acting m-opioid antagonists. Presently, introduction of a multi-modal rehabilitation programme (including continuous epidural analgesia with local anesthetics, early oral feeding and enforced...

  13. Pharmacoelectrophysiology of viral-free induced pluripotent stem cell-derived human cardiomyocytes. (United States)

    Mehta, Ashish; Chung, YingYing; Sequiera, Glen Lester; Wong, Philip; Liew, Reginald; Shim, Winston


    Development of pharmaceutical agents for cardiac indication demands elaborate safety screening in which assessing repolarization of cardiac cells remains a critical path in risk evaluations. An efficient platform for evaluating cardiac repolarization in vitro significantly facilitates drug developmental programs. In a proof of principle study, we examined the effect of antiarrhythmogenic drugs (Vaughan Williams class I-IV) and noncardiac active drugs (terfenadine and cisapride) on the repolarization profile of viral-free human-induced pluripotent stem cell-derived cardiomyocytes (hiPSC-CMs). Extracellular field potential (FP) recording using microelectrode arrays demonstrated significant delayed repolarization as prolonged corrected FP durations (cFPDs) by class I (quinidine and flecainide), class III (sotalol and amiodarone), and class IV (verapamil), whereas class II drugs (propranolol and nadolol) had no effects. Consistent with their sodium channel-blocking ability, class I drugs also significantly reduced FPmin and conduction velocity. Although lidocaine (class IB) had no effects on cFPDs, verapamil shortened cFPD and FPmin by 25 and 50%, respectively. Furthermore, verapamil reduced beating frequencies drastically. Importantly, the examined drugs exhibited dose-response curve on prolongation of cFPDs at an effective range that correlated significantly with therapeutic plasma concentrations achieved clinically. Consistent with clinical outcomes, drug-induced arrhythmia of tachycardia and bigeminy-like waveforms by quinidine, flecainide, and sotalol was demonstrated at supraphysiological concentrations. Furthermore, off-target effects of terfenadine and cisapride on cFPD and Na( + ) channel blockage were similarly revealed. These results suggest that hiPSC-CMs may be useful for safety evaluation of cardioactive and noncardiac acting drugs for personalized medicine.

  14. High-content screening of drug-induced cardiotoxicity using quantitative single cell imaging cytometry on microfluidic device. (United States)

    Kim, Min Jung; Lee, Su Chul; Pal, Sukdeb; Han, Eunyoung; Song, Joon Myong


    Drug-induced cardiotoxicity or cytotoxicity followed by cell death in cardiac muscle is one of the major concerns in drug development. Herein, we report a high-content quantitative multicolor single cell imaging tool for automatic screening of drug-induced cardiotoxicity in an intact cell. A tunable multicolor imaging system coupled with a miniaturized sample platform was destined to elucidate drug-induced cardiotoxicity via simultaneous quantitative monitoring of intracellular sodium ion concentration, potassium ion channel permeability and apoptosis/necrosis in H9c2(2-1) cell line. Cells were treated with cisapride (a human ether-à-go-go-related gene (hERG) channel blocker), digoxin (Na(+)/K(+)-pump blocker), camptothecin (anticancer agent) and a newly synthesized anti-cancer drug candidate (SH-03). Decrease in potassium channel permeability in cisapride-treated cells indicated that it can also inhibit the trafficking of the hERG channel. Digoxin treatment resulted in an increase of intracellular [Na(+)]. However, it did not affect potassium channel permeability. Camptothecin and SH-03 did not show any cytotoxic effect at normal use (≤300 nM and 10 μM, respectively). This result clearly indicates the potential of SH-03 as a new anticancer drug candidate. The developed method was also used to correlate the cell death pathway with alterations in intracellular [Na(+)]. The developed protocol can directly depict and quantitate targeted cellular responses, subsequently enabling an automated, easy to operate tool that is applicable to drug-induced cytotoxicity monitoring with special reference to next generation drug discovery screening. This multicolor imaging based system has great potential as a complementary system to the conventional patch clamp technique and flow cytometric measurement for the screening of drug cardiotoxicity.

  15. Systematic review of the pharmacological agents for infants in the treatment of gastroesophageal reflux%婴幼儿胃食管反流病治疗药物的系统评价

    Institute of Scientific and Technical Information of China (English)

    李奇玉; 茅旭


    Objective This system review for the medicine of children gastroesophageal reflux disease(GERD) will provide the latest evidence based medicine evidence for pediatric clinical medication.Methods The documents of randomized controlled clinical trials of children GERD,which had been published in domestic and foreign journals from the year 2000 to 2010,had been retrieved and screened by the study inclusion criteria.According to the Jadad evaluation questionaire,the documents' quality had been evaluated.The efficiency rates of treatment were calculated respectively by the merger of same medicines,and the meta-analysis of different drugs had been done for evaluating the effect of different pharmacological therapeutic agents.In addition,the adverse events occurred during treatment were analyzed.Results There were 31 documents fitting inclusion criteria.2 015 cases of children ( 1039 cases in treatment groups and 976 cases in control groups) had been included in these randomized controlled clinical trials.In these documents the agents included:cisapride ( 18 articles ),erythromycin ( 8 articles ),motilium ( 5 articles ).The merger efficiency rates of these medicines were cisapride (93.43% ),erythromycin (92.86% ),motilium (93.06%) respectively.There were no significant difference in the efficiencies of the three drugs in the treatment of GERD ( P>0.05 ).In addition,the results of meta-analysis about treatment inefficiency,used with the postures therapy and support therapy as controls,were cisapride OR=0.15 ( OR 95% CI0.11~0.20),erythromycin OR =0.08 ( OR 95% CI 0.04~0.14 ),motilium OR=0.03 ( OR 95% CI 0.01~0.07).Furthermore,their adverse effect rates were cisapride 0.72% ( diarrhea 0.58%,somnolence 0.14% ),erythromycin 0.96% ( drug rashes 0.48%,slight increase of GOT 0.48% ),motilium 1.50% (diarrhea 1.50% ).Conclusion The efficiencies of smaller doses of erythromycin were better than cisapride,and not better than motilium;but the

  16. 凉润通络方及其拆方对糖尿病大鼠胃肠MOT、CCK、SS的影响%Effect of Liangruntongluo Recipe and its Modified Formula on Gastrointestinal MOT、 CCK、SS of Rats with Diabetes

    Institute of Scientific and Technical Information of China (English)

    李佃贵; 戎士玲; 王凤丽; 张永健


    目的 探讨凉润通络方及其拆方对糖尿病大鼠胃肠运动功能改善的机制.方法 雄性Wistar大鼠,注射链脲佐菌素(STZ)制作糖尿病大鼠模型.造模成功后,不予降糖药控制血糖,正常饲养18周后,大鼠分别予温水、凉润通络中药、单纯通络中药、单纯滋润中药、单纯清凉中药、西沙必利灌胃,6周后检测血浆中胃动素(MOT)、胆囊收缩素(CCK)、生长抑素(SS).结果 24周时糖尿病大鼠存在胃肠激素的紊乱,凉润通络方影响血液中胃肠激素的分泌和释放,作用靶点较宽,优于其拆方和西沙必利.结论 凉润通络方可改善糖尿病大鼠胃肠功能障碍.%Objective To study the mechanism of Liangruntongluo Recipe (Chinese medicines with functions of cooling, nourishing and dredging collaterals) and its modified formula in improving gastrointestinal function of diabete smellitus (DM) rats. Methods Male Wistar rats were used. Streptozotocin (STZ) was injected to rats to produce diabetic rat models. No Hypoglycemic drugs were administered to these rats to reduce blood glucose. After 18 weeks, warm water, Liangruntongino Recipe, Chinese medicines with function of nourishing, Chinese medicines with functions of cooling, and Cisapride were administered to the model rats. Detect the contents of plasma motilin (MOT), cholecystokinin (CCK), and somatostatin (SS) after 6 weeks. Results By affecting the secretion of gut hormone and having wide range of target, Liangrantongluo Recipe could regulate the disorder of gut hormone. The function of Liangruntongluo Recipe was better than its modified formula and cisapride.Conclusion Liangruntongluo Recipe can improve gastrointestinal dysfunction of DM rats.

  17. Effect of enterokinetic prucalopride on intestinal motility in fast rats

    Institute of Scientific and Technical Information of China (English)

    Hui-Bin Qi; Jin-Yan Luo; Xin Liu


    AIM: To evaluate the effects of prucalopride on intestinal prokinetic activity in fast rats and to provide experimental basis for clinical treatrnent of gastrointestinal motility diseases.METHODS: Gastrointestinal propulsion rate was measured by the migration rate of activated charcoal, which reflexes gastrointestinal motility function. 120 Spraque-Dawley rats were randomly divided into four groups and received an intravenous injection of physiological saline (served as control), prucalopdde 1 mg/kg, prucalopride 2 mg/kg and cisapride 1 mg/kg,respectively. The gastrointestinal propulsion rate was measured 1, 2 or 4 hours after intravenous injection of the drugs.RESULTS: Significant accelerations of gastrointestinal propulsion rate in prucalopride 1 mg/kg and 2 mg/kg groups were found compared with control group at 2 and 4 hours (83.2%±5.5%, 81.7%±8.5% vs70.5%±9.2%, P<0.01;91.2%±2.2%, 91.3%±3.9% vs86.8%±2.6%, P<0.01).The gastrointestinal propulsion rates at 1, 2 or 4 hours were faster in prucalopride 1 mg/kg and 2 mg/kg groups than in cisapride group (84.0%±11.7%, 77.1%±11.9% vs 66.3%±13.6%, P<0.01, P<0.05; 83.2%±5.5%, 81.7%±8.5% vs75.4%±5.9 %, P<0.01, P<0.05; 91.2%±2.2%,91.3%±3.9% vs 88.6%±3.5%,P<0.05, P<0.05). No difference of gastrointestinal propulsion rate was found between prucalopride 1 mg/kg group and prucalopride 2 mg/kg group (P>0.05).CONCLUSION: Prucalopride accelerates intestinal motility in fast rats, and has no dose dependent effect.

  18. [Irritable bowel syndrome]. (United States)

    Kocián, J


    Irritable bowel is a functional gastrointestinal disorder with chronic or relapsing symptoms of abdominal pain and impaired frequency and consistency of the faeces caused by obscure structural or biochemical deviations. The frequency of the condition in civilized countries is estimated to amount to 15-20% of the population and it accounts for 25-50% of all patients in gastroenterological ambulatory departments. From the clinical aspect the type with dominant diarrhoea, typically in the morning and very compelling, and the type with pain and constipation are known but even combinations of the two types are encountered. A psychosomatic disorder of the motility of the large bowel and its tonus is involved associated with enhanced pain perception. Despite great efforts to find aetiopathogenetic factors, knowledge still is at the level of obscure theories. The diagnosis is still established per exclusion after all organic causes are ruled out, i.e. we always have to differentiate between an irritable bowel from an irritated one. In therapy the patient's confidence in his doctor is most important and it is essential to gain the patient's active cooperation. In case of diarrhoea a low-residue diet is used, calcium carbonate, codeine, loperamide, conversely in constipation adequate dietary fibre, intake metoclopramide or cisapride. Pain is relieved by spasmolytics or Ca channel blockers in the smooth musculature of the large bowel. The associated dysbiosis is transformed into eubiosis by Lactobacillus or other bacterial products.


    Directory of Open Access Journals (Sweden)

    Singh Nidhi


    Full Text Available Drug interaction is an increasingly important cause of adverse reactions (ADR, and is the modification of the effect of one drug (object by the prior or concomitant administration of another drug (precipitant drug. Drug interaction may either enhance or diminish the intended effect of one or both drugs. For example severe haemorrhage may occur if warfarin and salicylates (asprin are combined. Precipitant drugs modify the object drug's absorption, distribution, metabolism, excretion or actual clinical effect. Nonsteroidal anti-inflammatory drugs, antibiotics and, in particular, rifampin are common precipitant drugs prescribed in primary care practice. Drugs with a narrow therapeutic range or low therapeutic index are more likely to be the objects for serious drug interactions. Object drugs in common use include warfarin, fluoroquinolones, antiepileptic drugs, oral contraceptives, cisapride and 3-hydroxy-3-methylglutaryl coenzyme A reductase inhibitors. Many other drugs, act as precipitants or objects, and a number of drugs act as both. The aim of present review is to throw light on the concept of drug interaction.

  20. Chinese medicine treatment of ful ness Syndrome%中医药治疗痞满证的临床分析

    Institute of Scientific and Technical Information of China (English)



      目的探讨中医药治疗痞满证的临床效果。方法随机抽取96例肝胃不和痞满证患者的临床资料,随机分组西沙必利治疗(对照组)与加服自拟中药方剂治疗(观察组)结果进行对比。结果中医药治疗痞满证的效果明显高于对照组,P﹤0.05,有显著性差异。结论中医药治疗痞满证的疗效良好,其治疗效果优于单纯的西药治疗,具有较高的临床应用价值。%Objective: To explore the ful ness of Traditional Chinese Medicine Syndrome results. Methods: 96 cases were randomly selected disharmony of liver and ful ness syndrome clinical data randomization cisapride treatment (control group) and intends to add services from traditional Chinese medicine prescription treatment (observation group) results were compared. Results: The ful ness of Chinese medicine treatment effect was significantly higher certificates, P ﹤0.05, significant difference. Conclusion: Chinese medicine treatment of ful ness permit good efficacy, the treatment is better than western medicine alone, with a high clinical value.

  1. Human engineered heart tissue as a versatile tool in basic research and preclinical toxicology.

    Directory of Open Access Journals (Sweden)

    Sebastian Schaaf

    Full Text Available Human embryonic stem cell (hESC progenies hold great promise as surrogates for human primary cells, particularly if the latter are not available as in the case of cardiomyocytes. However, high content experimental platforms are lacking that allow the function of hESC-derived cardiomyocytes to be studied under relatively physiological and standardized conditions. Here we describe a simple and robust protocol for the generation of fibrin-based human engineered heart tissue (hEHT in a 24-well format using an unselected population of differentiated human embryonic stem cells containing 30-40% α-actinin-positive cardiac myocytes. Human EHTs started to show coherent contractions 5-10 days after casting, reached regular (mean 0.5 Hz and strong (mean 100 µN contractions for up to 8 weeks. They displayed a dense network of longitudinally oriented, interconnected and cross-striated cardiomyocytes. Spontaneous hEHT contractions were analyzed by automated video-optical recording and showed chronotropic responses to calcium and the β-adrenergic agonist isoprenaline. The proarrhythmic compounds E-4031, quinidine, procainamide, cisapride, and sertindole exerted robust, concentration-dependent and reversible decreases in relaxation velocity and irregular beating at concentrations that recapitulate findings in hERG channel assays. In conclusion this study establishes hEHT as a simple in vitro model for heart research.

  2. The virtual heart as a platform for screening drug cardiotoxicity. (United States)

    Yuan, Yongfeng; Bai, Xiangyun; Luo, Cunjin; Wang, Kuanquan; Zhang, Henggui


    To predict the safety of a drug at an early stage in its development is a major challenge as there is a lack of in vitro heart models that correlate data from preclinical toxicity screening assays with clinical results. A biophysically detailed computer model of the heart, the virtual heart, provides a powerful tool for simulating drug-ion channel interactions and cardiac functions during normal and disease conditions and, therefore, provides a powerful platform for drug cardiotoxicity screening. In this article, we first review recent progress in the development of theory on drug-ion channel interactions and mathematical modelling. Then we propose a family of biomarkers that can quantitatively characterize the actions of a drug on the electrical activity of the heart at multi-physical scales including cellular and tissue levels. We also conducted some simulations to demonstrate the application of the virtual heart to assess the pro-arrhythmic effects of cisapride and amiodarone. Using the model we investigated the mechanisms responsible for the differences between the two drugs on pro-arrhythmogenesis, even though both prolong the QT interval of ECGs. Several challenges for further development of a virtual heart as a platform for screening drug cardiotoxicity are discussed.

  3. The virtual heart as a platform for screening drug cardiotoxicity (United States)

    Yuan, Yongfeng; Bai, Xiangyun; Luo, Cunjin; Wang, Kuanquan


    To predict the safety of a drug at an early stage in its development is a major challenge as there is a lack of in vitro heart models that correlate data from preclinical toxicity screening assays with clinical results. A biophysically detailed computer model of the heart, the virtual heart, provides a powerful tool for simulating drug–ion channel interactions and cardiac functions during normal and disease conditions and, therefore, provides a powerful platform for drug cardiotoxicity screening. In this article, we first review recent progress in the development of theory on drug–ion channel interactions and mathematical modelling. Then we propose a family of biomarkers that can quantitatively characterize the actions of a drug on the electrical activity of the heart at multi‐physical scales including cellular and tissue levels. We also conducted some simulations to demonstrate the application of the virtual heart to assess the pro‐arrhythmic effects of cisapride and amiodarone. Using the model we investigated the mechanisms responsible for the differences between the two drugs on pro‐arrhythmogenesis, even though both prolong the QT interval of ECGs. Several challenges for further development of a virtual heart as a platform for screening drug cardiotoxicity are discussed. Linked Articles This article is part of a themed section on Chinese Innovation in Cardiovascular Drug Discovery. To view the other articles in this section visit PMID:25363597

  4. Application of a rapid and selective method for the simultaneous determination of carebastine and pseudoephedrine in human plasma by liquid chromatography-electrospray mass spectrometry for bioequivalence study in Korean subjects. (United States)

    Lee, Myung-Jae; Lee, Heon-Woo; Kang, Jong-Min; Seo, Ji-Hyung; Tak, Seong-Kun; Shim, Wangseob; Yim, Sung-Vin; Hong, Seung Jae; Lee, Kyung-Tae


    We describe a simple, rapid and sensitive high-performance liquid chromatography-electrospray ionization tandem mass spectrometric method that was developed for the simultaneous determination of carebastine and pseudoephedrine in human plasma using cisapride as an internal standard. Acquisition was performed in multiple-reaction monitoring mode by monitoring the transitions: m/z 500.43 > 167.09 for carebastine and m/z 166.04 > 147.88 for pseudoephedrine. The devised method involves a simple single-step liquid-liquid extraction with ethyl acetate. Chromatographic separation was performed on a C(18) reversed-phase chromatographic column at 0.2  mL/min by isocratic elution with 10  mM ammonium formate buffer-acetonitrile (30:70, v/v; adjusted to pH 3.3 with formic acid). The devised method was validated over 0.5-100  ng/mL of carebastine and 5-1000  ng/mL of pseudoephedrine with acceptable accuracy and precision, and was successfully applied to a bioequivalence study involving a single oral dose (10  mg of ebastine plus 120  mg of pseudoephedrine complex) to healthy Korean volunteers.

  5. Pharmacological Therapy of Gastroesophageal Reflux in Preterm Infants

    Directory of Open Access Journals (Sweden)

    Luigi Corvaglia


    Full Text Available Although gastroesophageal reflux (GER is a very common phenomenon among preterm infants, its therapeutic management is still an issue of debate among neonatologists. A step-wise approach should be advisable, firstly promoting nonpharmacological interventions and limiting drugs to selected infants unresponsive to the conservative measures or who are suffering from severe GER with clinical complications. Despite of this, a concerning pharmacological overtreatment has been increasingly reported. Most of the antireflux drugs, however, have not been specifically assessed in preterm infants; moreover, serious adverse effects have been noticed in association to their administration. This review mainly aims to draw the state of the art regarding the pharmacological management of GER in preterm infants, analyzing the best piecies of evidence currently available on the most prescribed anti-reflux drugs. Although further trials are required, sodium alginate-based formulations might be considered promising; however, data regarding their safety are still limited. Few piecies of evidence on the efficacy of histamine-2 receptor blockers and proton pump inhibitors in preterm infants with GER are currently available. Nevertheless, a significantly increased risk of necrotizing enterocolitis and infections has been largely reported in association with their use, thereby leading to an unfavorable risk-benefit ratio. The efficacy of metoclopramide in GER’s improvement still needs to be clarified. Other prokinetic agents, such as domperidone and erythromycin, have been reported to be ineffective, whereas cisapride has been withdrawn due to its remarkable cardiac adverse effects.

  6. [Chronic idiopathic intestinal pseudo-obstruction: visceral myopathy. Report of 4 cases]. (United States)

    de Pini, A F; de Dávila, M T; Marín, A; Guastavino, E; Ruiz, J A; De Rosa, S


    Chronic intestinal pseudo-obstruction is the term applied to a heterogeneous group of functional motility disorders sharing a common clinical expression: signs and symptoms of bowel obstruction in absence of mechanical occlusion. It is caused by ineffective intestinal propulsion. The chronic form of intestinal pseudo-obstruction may be primary or secondary. Primary pseudo-obstruction or chronic idiopathic pseudo-obstruction (CIIP) defines a group of propulsive disorders having no recognized underlying diseases. This study presents four female patients, aged between 4 months to 7 years, and makes a review of the literature. The symptoms, very similar in three of them, were bilious vomiting, abdominal distention and constipation, alternating with diarrhea and malnutrition. The fourth patient, different from the others in the age of onset and evolution, only had severe constipation and abdominal bloating. The diagnostic was made by full thickness biopsies during laparotomy, getting specimens by mapping, at different heights of intestine and stomach. Samples were studied by optic and electronic microscopy and visceral myopathies were found. None of them had urinary disorders. Medical treatment consisted of total parental nutrition and/or enteral nutrition. Cisapride was not effective in the two patients who received it.

  7. Effect of Modified Sinisan(四逆散) on Anorectal Manometry of the Constipation Predominant Type of Irritable Bowel Syndrome

    Institute of Scientific and Technical Information of China (English)

    YU Su-ping; YE Hui; HA Nan-lin; DING Shu-qing; CHEN Gao


    Objective:To explore the mechanism in patients with irritable bowel syndrome (IBS) of the Forty-seven IBS patients with the constipation predominant type were randomly divided into the treated group (n=24) and the control group (n=23). Another group of 22 healthy subjects was set up for healthy control.The treated group was treated with modified SNS, and the control group was treated with Cisapride, the therapeutic course for both groups was 8 weeks. The changes of symptom scoring and anorectal manometry (the anorectal resting pressure, anal tract systolic pressure, anal tract diastolic pressure, rectal threshold feeling, maximal tolerance volume of rectum, and rectum compliance) of these two groups were recorded respectively and compared with each other. Results: Compared with the healthy control group, the rectal threshold feeling, maximal tolerance volume of rectum and rectal compliance of the treated groups got reduced significantly before treatment (P<0.05). After treatment, the symptom scoring, rectal threshold feeling and maximal tolerance volume of rectum were improved in both groups (P<0.05), and the improvement of the treated group was more significant than that of the control group(P<0.01). The total effective rate and recurrence rate of the treated group were superior to those of the control group significantly (P<0.05,P<0.01). Conclusion: SNS has good effect on IBS of the constipation predominant type.

  8. Tratamento cirúrgico da doença de refluxo gastroesofágico na esclerose sistêmica Surgical treatment of gastroesophageal reflux disease in systemic sclerosis

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    Percival D. Sampaio-Barros


    Full Text Available OBJETIVO: Os autores descrevem sua experiência com o tratamento cirúrgico da doença de refluxo gastroesofágico (DRGE em pacientes com esclerose sistêmica (ES. MÉTODOS: Foram selecionados 10 pacientes com DRGE que apresentavam esofagite grave e estenose esofágica, tratados previamente com doses recomendadas de drogas anti-secretórias (ranitidina e/ou omeprazol e pró-cinéticas (cisapride por mais de seis meses, sem melhora significativa. Todos os pacientes eram do sexo feminino e 8 eram caucasóides, sendo 7 com ES limitada e 3 com ES difusa. RESULTADOS: O tratamento cirúrgico foi realizado através de videolaparoscopia em 9 pacientes e por cirurgia aberta no outro paciente. Sete pacientes foram submetidos à técnica de Nissen modificada e 3 à técnica de Lind. Seis pacientes com estenose esofágica significativa necessitaram de dilatações endoscópicas no período pré-operatório. Avaliação pós-operatória três meses após a cirurgia revelou que 70% dos pacientes apresentaram resultado favorável, com melhora significativa da azia e da disfagia; 1 paciente necessitou de nova intervenção cirúrgica em conseqüência de uma hérnia paraesofágica no período pós-operatório, sendo realizada uma gastrectomia em Y de Roux. Uma boa evolução foi referida por 80% dos pacientes um ano após cirurgia e por 70% dois anos após cirurgia, observando-se dois óbitos. CONCLUSÕES: Os autores concluem que o tratamento cirúrgico da DRGE representa uma eficiente opção terapêutica em pacientes com ES e esofagite grave com estenose.OBJECTIVE: The authors describe the experience with the surgical treatment of gastroesophageal reflux disease (GERD in 10 patients with systemic sclerosis (SSc. METHODS: Criteria for surgery included GERD with severe chronic esophagitis and stricture, treated previously with recommended doses of antisecretory (ranitidine and/or omeprazole and prokinetic (cisapride drugs for more than six months, without

  9. Evidence-Based Recommendations for Short- and Long-Term Management of Uninvestigated Dyspepsia in Primary Care: An Update of the Canadian Dyspepsia Working Group (CanDys Clinical Management Tool

    Directory of Open Access Journals (Sweden)

    Sander JO Veldhuyzen van Zanten


    Full Text Available The present paper is an update to and extension of the previous systematic review on the primary care management of patients with uninvestigated dyspepsia (UD. The original publication of the clinical management tool focused on the initial four- to eight-week assessment of UD. This update is based on new data from systematic reviews and clinical trials relevant to UD. There is now direct clinical evidence supporting a test-and-treat approach in patients with nondominant heartburn dyspepsia symptoms, and head-to-head comparisons show that use of a proton pump inhibitor is superior to the use of H2-receptor antagonists (H2RAs in the initial treatment of Helicobacter pylori-negative dyspepsia patients. Cisapride is no longer available as a treatment option and evidence for other prokinetic agents is lacking. In patients with long-standing heartburn-dominant (ie, gastroesophageal reflux disease and nonheartburn-dominant dyspepsia, a once-in-a-lifetime endoscopy is recommended. Endoscopy should also be considered in patients with new-onset dyspepsia that develops after the age of 50 years. Conventional nonsteroidal anti-inflammatory drugs, acetylsalicylic acid and cyclooxygenase-2-selective inhibitors can all cause dyspepsia. If their use cannot be discontinued, cotherapy with either a proton pump inhibitor, misoprostol or high-dose H2RAs is recommended, although the evidence is based on ulcer data and not dyspepsia data. In patients with nonheartburn-dominant dyspepsia, noninvasive testing for H pylori should be performed and treatment given if positive. When starting nonsteroidal anti-inflammatory drugs for a prolonged course, testing and treatment with H2RAs are advised if patients have a history of previous ulcers or ulcer bleeding.

  10. Isolation of the serotoninergic 5-HT4(e) receptor from human heart and comparative analysis of its pharmacological profile in C6-glial and CHO cell lines (United States)

    Mialet, Jeanne; Berque-Bestel, Isabelle; Eftekhari, Pierre; Gastineau, Monique; Giner, Mireille; Dahmoune, Yamina; Donzeau-Gouge, Patrick; Hoebeke, Johan; Langlois, Michel; Sicsic, Sames; Fischmeister, Rodolphe; Lezoualc'h, Frank


    RT–PCR technique was used to clone the human 5-HT4(e) receptor (h5-HT4(e)) from heart atrium. We showed that this h5-HT4(e) receptor splice variant is restricted to brain and heart atrium. Recombinant h5-HT4(e) receptor was stably expressed in CHO and C6-glial cell lines at 347 and 88 fmol mg−1 protein, respectively. Expression of h5-HT4(e) receptors at the cell membrane was confirmed by immunoblotting. The receptor binding profile, determined by competition with [3H]-GR113808 of a number of 5-HT4 ligands, was consistent with that previously reported for other 5-HT4 receptor isoforms. Surprisingly, we found that the rank order of potencies (EC50) of 5-HT4 agonists obtained from adenylyl cyclase functional assays was inversely correlated to their rank order of affinities (Ki) obtained from binding assays. Furthermore, EC50 values for 5-HT, renzapride and cisapride were 2 fold lower in C6-glial cells than in CHO cells. ML10302 and renzapride behaved like partial agonists on the h5-HT4(e) receptor. These results are in agreement with the reported low efficacy of the these two compounds on L-type Ca2+ currents and myocyte contractility in human atrium. A constitutive activity of the h5-HT4(e) receptor was observed in CHO cells in the absence of any 5-HT4 ligand and two 5-HT4 antagonists, GR113808 and ML10375, behaved as inverse agonists. These data show that the h5-HT4(e) receptor has a pharmacological profile which is close to the native h5-HT4 receptor in human atrium with a functional potency which is dependent on the cellular context in which the receptor is expressed. PMID:10683202

  11. A distributed, collaborative intelligent agent system approach for proactive postmarketing drug safety surveillance. (United States)

    Ji, Yanqing; Ying, Hao; Farber, Margo S; Yen, John; Dews, Peter; Miller, Richard E; Massanari, R Michael


    Discovering unknown adverse drug reactions (ADRs) in postmarketing surveillance as early as possible is of great importance. The current approach to postmarketing surveillance primarily relies on spontaneous reporting. It is a passive surveillance system and limited by gross underreporting (computers located in different places, are capable of continuously and autonomously collaborating with each other and assisting the human users (e.g., the food and drug administration (FDA), drug safety professionals, and physicians). The agents should enhance current systems and accelerate early ADR identification. To evaluate the performance of the ADRMonitor with respect to the current spontaneous reporting approach, we conducted simulation experiments on identification of ADR signal pairs (i.e., potential links between drugs and apparent adverse reactions) under various conditions. The experiments involved over 275,000 simulated patients created on the basis of more than 1000 real patients treated by the drug cisapride that was on the market for seven years until its withdrawal by the FDA in 2000 due to serious ADRs. Healthcare professionals utilizing the spontaneous reporting approach and the ADRMonitor were separately simulated by decision-making models derived from a general cognitive decision model called fuzzy recognition-primed decision (RPD) model that we recently developed. The quantitative simulation results show that 1) the number of true ADR signal pairs detected by the ADRMonitor is 6.6 times higher than that by the spontaneous reporting strategy; 2) the ADR detection rate of the ADRMonitor agents with even moderate decision-making skills is five times higher than that of spontaneous reporting; and 3) as the number of patient cases increases, ADRs could be detected significantly earlier by the ADRMonitor.

  12. 中药内服外敷配合隔物灸治疗肝癌腹胀的临床观察%Observation on Traditional Chinese Medicine Orally Taken and Externally Applied Combined with Indirect Moxibustion in the Treatment of Hepato-cellular Carcinoma and Abdominal Distension

    Institute of Scientific and Technical Information of China (English)

    孙素芹; 常丽; 叶婷


    Objective To observe the clinical curative effect of traditional Chinese medicine orally taken and externally applied combined with indirect moxibustion in the treatment of hepatocellular carcinoma with abdominal distention. Methods 30 cases of patients were treated with traditional Chinese medicine orally taken and externally applied combined with indirect moxibustion, and the short-term efficacy was observed. Results The total effective rate of the 30 patients reaches 80%, compared with that (55.6%) of the cisapride group, the difference is statistically significant (P<0.05), and is suitable for various TCM syndrome types of hepatocellular carcinoma patients with abdominal distension. Conclusion Traditional Chinese medicine orally taken and externally applied combined with indirect moxibustion has the clinical effect of eliminating, reducing or alleviating hepatocellular carcinoma patients with abdominal distension.%目的:观察中药内服外敷配合隔物灸治疗肝癌腹胀的临床疗效。方法对30例患者均用中药内服外敷配合隔物灸治疗,观察近期疗效。结果30例患者总有效率达到80%,与西沙必利组(55.6%)相比,差异有统计学意义(P<0.05),且适用于多种中医辨证类型的肝癌腹胀患者。结论中药内服外敷配合隔物灸综合治疗能达到消除、减轻或缓解肝癌腹胀的临床效果。

  13. Drug binding to the inactivated state is necessary but not sufficient for high-affinity binding to human ether-à-go-go-related gene channels. (United States)

    Perrin, Mark J; Kuchel, Philip W; Campbell, Terence J; Vandenberg, Jamie I


    Drug block of the human ether-à-go-go-related gene K(+) channel (hERG) is the most common cause of acquired long QT syndrome, a disorder of cardiac repolarization that may result in ventricular tachycardia and sudden cardiac death. We investigated the open versus inactivated state dependence of drug block by using hERG mutants N588K and N588E, which shift the voltage dependence of inactivation compared with wild-type but in which the mutated residue is remote from the drug-binding pocket in the channel pore. Four high-affinity drugs (cisapride, dofetilide, terfenadine, and astemizole) demonstrated lower affinity for the inactivation-deficient N588K mutant hERG channel compared with N588E and wild-type hERG. Three of four low-affinity drugs (erythromycin, perhexiline, and quinidine) demonstrated no preference for N588E over N588K channels, whereas dl-sotalol was an example of a low-affinity state-dependent blocker. All five state-dependent blockers showed an even lower affinity for S620T mutant hERG (no inactivation) compared with N588K mutant hERG (greatly reduced inactivation). Computer modeling indicates that the reduced affinity for S620T compared with N588K and wild-type channels can be explained by the relative kinetics of drug block and unblock compared with the kinetics of inactivation and recovery from inactivation. We were also able to calculate, for the first time, the relative affinities for the inactivated versus the open state, which for the drugs tested here ranged from 4- to 70-fold. Our results show that preferential binding to the inactivated state is necessary but not sufficient for high-affinity binding to hERG channels.

  14. Cardiac arrest provoked by itraconazole and amiodarone interaction: a case report

    Directory of Open Access Journals (Sweden)

    Betrosian Alex


    Full Text Available Abstract Introduction Azoles, and specifically itraconazole, are often prescribed for the treatment of fungal diseases or empirically for persistent sepsis in patients who are neutropenic or in intensive care. Occasional cardiovascular adverse events have been associated with itraconazole use, and are usually attributed to the interaction of itraconazole with cisapride, terfenadine or digoxin. Its interaction with amiodarone has not been previously described. Case presentation A 65-year-old Caucasian man was admitted to the Intensive Care Unit at our facility for an extensive ischemic stroke associated with atrial fibrillation. Due to rapid ventricular response he was started on intravenous amiodarone and few days later itraconazole was also prescribed for presumed candidemia. After receiving the first dose our patient became profoundly hypotensive but responded rapidly to fluids and adrenaline. Then, two months later, itraconazole was again prescribed for confirmed fungemia. After receiving the first dose via a central venous catheter our patient became hypotensive and subsequently arrested. He was resuscitated successfully, and as no other cause was identified the arrest was attributed to septic shock and his antifungal treatment was changed to caspofungin. When sensitivity test results became available, antifungal treatment was down-staged to itraconazole and immediately after drug administration our patient suffered another arrest and was once again resuscitated successfully. This time the arrest was related to itraconazole, which was discontinued, and from then on our patient remained stable until his discharge to our neurology ward. Conclusions Itraconazole and amiodarone coadministration can lead to serious cardiovascular adverse events in patients who are critically ill. Intensivists, pharmacists and medical physicians should be aware of the interaction of these two commonly used drugs.

  15. Treating gastro-oesophageal reflux disease during pregnancy and lactation: what are the safest therapy options? (United States)

    Broussard, C N; Richter, J E


    Gastro-oesophageal reflux and heartburn are reported by 45 to 85% of women during pregnancy. Typically, the heartburn of pregnancy is new onset and is precipitated by the hormonal effects of estrogen and progesterone on lower oesophageal sphincter function. In mild cases, the patient should be reassured that reflux is commonly encountered during a normal pregnancy: lifestyle and dietary modifications may be all that are required. In a pregnant woman with moderate to severe reflux symptoms, the physician must discuss with the patient the benefits versus the risks of using drug therapy. Medications used for treating gastro-oesophageal reflux are not routinely or vigorously tested in randomised, controlled trials in women who are pregnant because of ethical and medico-legal concerns. Safety data are based on animal studies, human case reports and cohort studies as offered by physicians, pharmaceutical companies and regulatory authorities. If drug therapy is required, first-line therapy should consist of nonsystemically absorbed medications, including antacids or sucralfate, which offer little, if any, risk to the fetus. Systemic therapy with histamine H2 receptor antagonists (avoiding nizatidine) or prokinetic drugs (metoclopramide, cisapride) should be reserved for patients with more severe symptoms. Proton pump inhibitors are not recommended during pregnancy except for severe intractable cases of gastrooesophageal reflux or possibly prior to anaesthesia during labour and delivery. In these rare situations, animal teratogenicity studies suggests that lansoprazole may be the best choice. Use of the least possible amount of systemic drug needed to ameliorate the patient's symptoms is clearly the best for therapy. If reflux symptoms are intractable or atypical, endoscopy can safely be performed with conscious sedation and careful monitoring the mother and fetus.

  16. Drug-induced acute myocardial infarction: identifying 'prime suspects' from electronic healthcare records-based surveillance system.

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    Preciosa M Coloma

    Full Text Available BACKGROUND: Drug-related adverse events remain an important cause of morbidity and mortality and impose huge burden on healthcare costs. Routinely collected electronic healthcare data give a good snapshot of how drugs are being used in 'real-world' settings. OBJECTIVE: To describe a strategy that identifies potentially drug-induced acute myocardial infarction (AMI from a large international healthcare data network. METHODS: Post-marketing safety surveillance was conducted in seven population-based healthcare databases in three countries (Denmark, Italy, and the Netherlands using anonymised demographic, clinical, and prescription/dispensing data representing 21,171,291 individuals with 154,474,063 person-years of follow-up in the period 1996-2010. Primary care physicians' medical records and administrative claims containing reimbursements for filled prescriptions, laboratory tests, and hospitalisations were evaluated using a three-tier triage system of detection, filtering, and substantiation that generated a list of drugs potentially associated with AMI. Outcome of interest was statistically significant increased risk of AMI during drug exposure that has not been previously described in current literature and is biologically plausible. RESULTS: Overall, 163 drugs were identified to be associated with increased risk of AMI during preliminary screening. Of these, 124 drugs were eliminated after adjustment for possible bias and confounding. With subsequent application of criteria for novelty and biological plausibility, association with AMI remained for nine drugs ('prime suspects': azithromycin; erythromycin; roxithromycin; metoclopramide; cisapride; domperidone; betamethasone; fluconazole; and megestrol acetate. LIMITATIONS: Although global health status, co-morbidities, and time-invariant factors were adjusted for, residual confounding cannot be ruled out. CONCLUSION: A strategy to identify potentially drug-induced AMI from electronic healthcare

  17. Novas drogas no tratamento da dispepsia funcional New drugs for the treatment of functional dyspepsia

    Directory of Open Access Journals (Sweden)

    Luiz Ernesto de Almeida TRONCON


    any evidence of structural abnormalities or organic disease. Current pharmacological treatment of functional dyspepsia is largely empirical and involves anti-secretory or prokinetic drugs. Aims - To review recent advances in the understanding of the mechanisms involved in symptom production in functional dyspepsia, as well as the development of new drugs that may interfere with these mechanisms, which may lead to more rational and effective treatment of this clinical condition. Method - Systematic review of papers published in English for the last 10 years. Results - New drugs that increase propulsive gastroduodenal motor activity include new benzamides similar to cisapride, CCK-A blockers, agonists of opiate receptors and motilin agonists similar to erythromycin. A number of agents, including sumatriptan and buspirone, stimulates serotonin receptors in the myoenteric plexuses and have been shown to increase gastric accommodation to a meal. Finally, a number of new drugs that either increase thresholds for visceral perception or modify sensations is currently under investigation. This includes agents of several groups, such as octreotide, loxiglumide, ondansetron and other serotonin blockers, fedotozine and tricyclic antidepressant at low doses. Conclusions - Although these new drugs may improve the pharmacological approach to the treatment of functional dyspepsia, there is a need for randomized, controlled trials to assess their efficacy. Moreover, difficulties related to the identification of the mechanisms underlying symptoms may limit the utilization of these new drugs.

  18. 一例初诊胃食管反流性疾病患者的循证治疗%Evidence-Based Treatment for First-visit Gastro-esophageal Reflux Disease

    Institute of Scientific and Technical Information of China (English)

    季梦遥; 董卫国; 吕晓光; 吴娜; 彭秀兰


    Objective To make an individualized treatment plan for one first-visit gastro-esophageal reflux disease patient via evidence-based medicine methods.Methods The condition of the patient was evaluated comprehensively,then clinical problems were put forward according to PICO principle, and high-quality evidence was collected from The Cochrane Library (1990 to 2010), PubMed (1990 to 2010), and EMbase (1990 to 2010).The treatment plan was designed based on the evaluation of evidence, doctor's experience, and patient's preferences.Results A total of 17 RCTs and 10 meta-analyses/systematic reviews were included.The evidence showed that the therapeutic effect of PPI was better than that of H2RA, and meanwhile prokinetic drugs should be used.When PPI needed to be use for a long time, HP eradication operation was required for the combination of HP inflammation.Laparoscopic fundoplication surgery was a better choice if the operation was required.Based on the above evidence combined with the patient's preferences, the combination of general treatment, esomeprazole and cisaPride were adopted to treat.Meanwhile, anti-HP medicine was used to control the HP inflammation caused by the long-term maintenance therapy.The gastro-esophageal reflux symptoms were remarkably relieved six months after the treatment.Conclusion PPI plus prokinetic drugs, combined with HP eradication of gastroesophageal reflux surgery, can improve the clinical outcomes and patient's quality of life.However, longterm prognostic benefits need to be confirmed by further follow-up.%目的 借助循证医学方法为1例初诊胃食管反流性疾病患者确定治疗方案.方法 在充分评估患者情况后,按照PICO原则提出临床问题并转化,计算机检索Cochrane图书馆(1990~2010)、PubMed(1990~2010)、Embase(1990~2010),收集相关高质量证据进行评价,并结合医生经验及患者愿望制定治疗方案.结果 共纳入RCI 17篇,Meta分析/系统评价10篇.结果 显示,选用质

  19. 胃肠舒对胃肠平滑肌细胞一氧化氮释放的影响%Effect of Weichangshu on Release of Nitric Oxide in Gastrointestinal Smooth Muscle Cells

    Institute of Scientific and Technical Information of China (English)

    郭金秀; 刘孟安


    目的:探讨胃肠舒促胃肠动力的作用机制.方法:组织块法原代培养胃肠平滑肌细胞,实验分胃肠舒低、中、高剂量组、西沙必利组和正常对照组,各组分别用受试药物(正常对照组用DMEM干粉培养基)干扰细胞24 h,采用一氧化氮荧光探针(DAF-FMDA)反应30 min,流式细胞仪检测一氧化氮(NO)释放.结果:胃肠舒大、中剂量组与正常对照组比较,胃肠平滑肌细胞NO释放的荧光强度明显减弱(P<0.01,P<0.05),与西沙必利组相似.结论:胃肠舒促胃肠动力的作用机制可能是通过抑制胃肠平滑肌细胞内NO的生成,进而抑制相关酶的活化,拮抗环磷酸鸟苷(cGMP)的作用,从而使胞内Ca2+增多,Ca2+信号系统引发一系列生理功能而促进胃肠平滑肌收缩效应.%Objective:To investigate the mechanisms of Weichangshu in promoting gastrointestinal motility.Method:Gastrointestinal smooth muscle cells were primarily cultured with tissues.Animals were divided into a lowdose of Weichangshu group ( LW), a moderate-dose of Weichangshu group ( MW), a high-dose of Weichangshu group (HW),a cisapride group (CI) and a normal control group (NC).The gastrointestinal smooth muscle cells were interfered with tested reagents for 24 h in different groups ( normal group with DMEM for Group NC ) ), and with 3-Amino,4-aminomethy1-2', 7'-difluorescein, diacetate (DAF-FMDA) for 30min for reaction, and release of NO was detected by using a Flow cytometry.Result:Compared with Group NC, the fluorescence intensities of NO release were significantly reduced in Group HW and Group MW (P <0.01 ,P <0.05 ) ,which were similar to Group CI.Conclusion:Inhibition of generation of NO in gastrointestinal smooth muscle cells followed by inhibition of activation of correlated enzymes to antagonize formation of cGMP,leading to increase of intracellular Ca2+ to trigger series of physiological functions to accelerate gastrointestinal smooth muscle contraction may be involved in

  20. Current management of motor fluctuations in patients with advanced Parkinson's disease treated chronically with levodopa. (United States)

    Melamed, E; Zoldan, J; Galili-Mosberg, R; Ziv, I; Djaldetti, R


    Motor fluctuations after long-term administration of levodopa may be due to central pharmacodynamic mechanisms such as reduced striatal synthesis and storage of dopamine from exogenous levodopa and subsensitization of postsynaptic dopaminergic receptors. Peripheral pharmacokinetic mechanisms may be equally important, particularly in motor fluctuations of the "delayed on" (increased time latencies from dose intake to start-up of clinical benefit) and "no-on" (complete failure of a levodopa dose to exert an "on" response) types. Levodopa itself has a very poor solubility. In addition, there is delayed gastric emptying in many advanced patients. Therefore, an oral dose of levodopa may remain in the stomach for long periods of time before it passes into the duodenum where there is immediate absorption. Consequently, in order to overcome response fluctuations caused by impaired pharmacokinetic mechanisms and to improve its absorption, we recommend that levodopa be taken in multiple small doses, on an empty stomach, preferably crushed and mixed with a lot of liquid. Protein intake should be minimized. Prokinetic drugs such as prepulsid (Cisaprid) could be used to facilitate gastric motility and levodopa transit time. Administration of crushed levodopa through nasoduodenal or gastrojejunostomy tubes may be helpful in certain circumstances. Bypassing the stomach with subcutaneous injections of apomorphine may provide dramatic rescue from difficult "off" situations. Oral and s.c. administration of novel, extremely soluble prodrugs of levodopa, e.g., levodopa ethylester, may offer a new approach to overcome difficulties in levodopa absorption. Addition of dopamine agonists, MAO-B inhibitors, COMT inhibitors and controlled release levodopa preparations may be helpful in prolonging the duration of efficacy of each single levodopa dose. Levodopa, administered orally, usually combined with peripheral dopa decarboxylase inhibitors, continues to be the most widely-used and most

  1. Enteral nutrition in the critically ill-an overview%重症病人的肠内营养支持

    Institute of Scientific and Technical Information of China (English)



    blood flow and providing a source of energy locally for the enterocytes themselves.These effects maintain a healthy gastrointestinal mucosa thereby reducing the incidence of bacterial overgrowth and translocation.Nevertheless,hypo-caloric nutritional support is often the result of emphasising the enteral route.This is the case because even when using well designed feeding protocols,it may be difficult to achieve target rates of enteral feeding using nasogastric access;gastric stasis with large nasogastric aspirates(>2-3mL/kg) may delay feeding but this problem can sometimes be overcome by the prescription of prokinetics(cisapride or erythromycin).Needle jejunostomy is unpopular outside the setting of surgery for abdominal trauma or upper gastrointestinal malignancies.However,it is possible to pass a naso-jejunal tube blindly at the bedside in the majority of patients.Jejunal feeding is thought to be associated with a higher daily intake of protein and energy and a lower risk of aspiration but there are no randomised studies compating nasogastric with jejunal feeding in the critically ill.Others have suggested that a combination of parenteral and enteral nutrition should be used initially for the first few days of support so as to guarantee an adequate intake of energy and protein.As enteral feeding is established with an increasing hourly rate of administration,the parenteral nutrition is titrated downwards and withdrawn once full enteral nutritional support has been established.The disadvantages of this latter approach are firstly,it exposes the patient to the fisks of parenteral nutrition.Secondly,there is the additional cost of the parenteral nutrition and perhaps most importantly,there is no evidence to suggest that this combination feeding is any better than simple enteral nutrition on its own.Hypo-caloeic feeding may not necessarily be such a bad thing in the severely stressed,critically ill patient.Finally,there is the issue of the constituents of the feed