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Resumen Introducción El síndrome de intestino irritable (SII) afecta del cinco al 20% de los individuos alrededor del mundo. En México (Veracruz) se ha documentado una prevalencia de 16.9%. Su diagnóstico se basa en los criterios de Roma III y su tratamiento tiene diferentes enfoques; dentro del farmacológico están los fármacos agonistas de los receptores de la serotonina (5-HT4). La eficacia del tegaserod ha sido establecida en pacientes con SII con estreñimiento (SII-E); la prucaloprida se considera un fármaco con potencial terapéutico para ese padecimiento, ya que muestra mayor afinidad para el receptor 5-HT4 con respecto al tegaserod y acelera el tránsito colónico. Sin embargo, se requieren mayores datos de estudios clínicos controlados aleatorizados que lo comprueben. Objetivo Comparar la eficacia de la prucaloprida con la del tegaserod en el tratamiento del intestino irritable con estreñimiento, por medio de la escala de Bristol, la escala global de síntomas y síntomas asociados. Material y métodos Se establecieron dos grupos de pacientes (A y B) de forma aleatorizada: hombres y mujeres de entre 18 y 50 años de edad, con criterios de Roma III para SII-E; fueron sometidos a una misma dieta. Al grupo A se le administró prucaloprida en dosis de 2 mg vía oral cada 24 horas por dos semanas. Al grupo B se le administraron 6 mg de tegaserod cada 12 horas por dos semanas. La evolución clínica de cada paciente se valoró cada semana durante las dos semanas del periodo de estudio, incluyendo las evaluaciones de la escala adaptada y validada de Bristol y de la escala global de síntomas y síntomas asociados. Resultados Se incluyeron 22 pacientes, 21 (95.5%) del sexo femenino, con una proporción 1:21; la edad promedio fue de 37.27 años; 11 (50%) recibieron prucaloprida y el resto, tegaserod. Para evaluar la asociación entre el tratamiento otorgado y los síntomas de «plenitud rectal, esfuerzo al evacuar y urgencia al evacuar¼, se utilizó la prueba exacta de Fisher, que no fue estadísticamente significativa (p > 0.05); para «distensión abdominal, movimientos abdominales y escala de Bristol¼, se utilizó U de Mann-Whitney; no fue estadísticamente significativa (p > 0.05). Sin embargo, para «dolor abdominal¼, con la misma prueba, sí se encontró diferencia estadísticamente significativa (p < 0.05). De los tratados con prucaloprida, uno (9%) presentó diarrea, tres (27%) cefalea y uno (9%) cefalea y náuseas; con tegaserod, dos (18%) tuvieron diarrea, dos (18%) cefalea y uno (9%) cefalea y náuseas. Conclusiones Ambos, la prucaloprida y el tegaserod, mejoran en cierto grado todos los síntomas evaluados para el SII-E, pero la prucaloprida mejora de manera significativa y en menor tiempo el síntoma de «dolor abdominal¼. Se evidenció que el evento de diarrea implicó un cambio de tratamiento en ambos grupos.
Abstract Introduction Irritable bowel syndrome (IBS) affects 5-20% of all individuals around the world. In Mexico (Veracruz), a prevalence of 16.9% has been documented. Its diagnosis is based on the Rome III criteria, and its treatment has different approaches; within the pharmacological options are the serotonin receptor agonist drugs (5-HT4). The effectiveness of tegaserod has been established in patients with IBS with constipation (IBS-C), considering prucalopride as a drug with therapeutic potential for this condition, since it shows greater affinity for the 5-HT4 receptor than tegaserod, and accelerates colonic transit. However, more data from randomized controlled trials that prove this are required. Objective To compare the efficacy of prucalopride versus tegaserod in the treatment of irritable bowel with constipation, by means of the Bristol scale, the global scale of symptoms and associated symptoms. Material and methods Two groups of patients were established (A and B) in a randomized manner: men and women between 18 and 50 years of age with Rome criteria III for IBS-C; all were given the same diet. In group A, Prucalopride was administered at a dose of 2 mg orally every 24 hours for two weeks. In group B, 6 mg of tegaserod were administered every 12 hours for two weeks. The clinical evolution of each patient was assessed each week during the two weeks of the study period, including the assessments of the adapted and validated Bristol scale, and the global scale of symptoms and associated symptoms. Results Twenty-two patients were included, 21 (95.5%) female, with a 1:21 ratio; the average age was 37.27 years; 11 (50%) received prucalopride, and the rest, tegaserod. To evaluate the association between the treatment given and the symptoms of «rectal fullness, evacuation effort and evacuation urgency¼, Fisher's exact test was used, being not statistically significant (p > 0.05); for «abdominal distension, abdominal movements and Bristol scale¼, Mann-Whitney U was used, being not statistically significant (p > 0.05); however, for «abdominal pain¼, with the same test, a statistically significant difference was found (p < 0.05). Of those treated with prucalopride, one (9%) had diarrhea, three (27%) headache, and one (9%) headache and nausea; with tegaserod, two (18%) had diarrhea, two (18%) headache, and one (9%) headache and nausea. Conclusions Both, prucalopride and tegaserod improve to some degree all the symptoms evaluated for IBS-C, but prucalopride significantly and more promptly improves the symptom of «abdominal pain¼. It was evidenced that the diarrhea event implied change of treatment in both groups.
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INTRODUCTION: Tegaserod has been used for treatment of irritable bowel syndrome (IBS) but there is no data regarding its effect on Korean patients. The aim of this study was to evaluate the effect of tegaserod on symptoms and quality of life (QOL) in Korean female IBS patients with constipation and to evaluate the usefulness of the IBS-QOL in clinical study. METHODS: A prospective, open labeled, multicenter study was performed. Female patients fulfilling Rome II criteria for IBS received 6 mg of tegaserod twice a day for 4 weeks. The efficacy on IBS symptoms and QOL was assessed using 7-point scaled symptom questionnaire and IBS-QOL questionnaire, respectively. RESULTS: A total of 81 female patients (range 18-73 years of age) were enrolled in this study. Tegaserod therapy significantly reduced the overall symptom scores after 4 weeks (p <0.01). The improved symptoms included abdominal discomfort or pain, hard or lumpy stool, straining during a bowel movement, feeling of incomplete bowel movement, and abdominal fullness or bloating. The IBS-QOL of responders to tegaserod treatment was also significantly improved after 4 weeks (p <0.01). Furthermore, improvement of symptom scores significantly correlated with improvement of the IBS-QOL scores (r = -0.60, p <0.001). CONCLUSIONS: Tegaserod 6 mg given twice daily improved the QOL as well as the bowel symptoms in Korean female IBS patients with constipation. The IBS-QOL can be used as a reliable end-point in clinical study.
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Female , Humans , Constipation , Indoles , Irritable Bowel Syndrome , Prospective Studies , Quality of Life , Surveys and Questionnaires , Rome , Sprains and StrainsABSTRACT
Objectives Tegaserod may enhance upper gut transit, but, its prokinetic effects on antral/small bowel motility and how this compares with erythromycin is unknown. We prospectively assessed and compared the effects of tegaserod and erythromycin on upper gut motility. Methods In an open label, non-crossover study, 22 patients (M/F=4/18; mean age=37 years) with symptoms of upper gut dysmotility underwent 24-hour ambulatory antroduodenojejunal manometry with a six-sensor solid state probe. The effects of 12 mg oral tegaserod were compared with 125 mg intravenous erythromycin by quantifying pressure wave activity and assessing motor patterns. Results Motor activity increased (p<0.05) in antrum, duodenum and jejunum with both drugs when compared to baseline period. The motor response with tegaserod was higher (p<0.05) in jejunum and occurred during the second or third hours, whereas with erythromycin, it was higher (p<0.05) in antrum and occurred within 30 minutes. After tegaserod, a ‘fed-response’ like pattern was seen whereas after erythromycin, large amplitude (>100 mmHg) antral contractions at 3 cycles per minute were seen. Following tegaserod and erythromycin, phase III MMCs occurred in 12 (55%) and 8 (36%) patients respectively (p>0.05). Conclusions Both drugs increase upper gut motility and induce MMC’s, but exert a differential response. Tegaserod produces a more sustained prokinetic effect in the duodenum/ jejunum, whereas erythromycin predominantly increases antral motor activity.
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Introducción: en un grupo de ratas se produjo diarrea o estreñimiento inducido por el uso de medicamentos favorecedores de la secreción o medicamentos constipadores. En estas ratas se utilizo el bromuro de pinaverio y el tegaserod como medicamentos favorecedores o de la disminución de la frecuencia defecatoria o como promotores de la defecación, respectivamente. Este trabajo tiene como objetivo averiguar hasta que punto estos medicamentos pueden ser utilizados como tratamiento efectivo en el síndrome de intestino irritable. Métodos: se utilizaron 12 ratas femeninas, adultas, de la raza Sprague Dowley, las cuales se distribuyeron de la siguiente manera: 2 ratas control para diarrea, 4 a las que se les indujo diarrea con una mezcla de fenolftaleina y sulfato de magnesio y 2 de ellas se trataron con tegaserod y 2 con bromuro de pinaverio. En el estreñimiento se utilizaron 2 ratas control, a 4 de ellas se les aplicó loperamida para inducir el estreñimiento y se trataron 2 con tegaserod y 2 con bromuro de pinaverio. Resultados: ratas con diarrea: con respecto a estas ratas las variaciones de peso conseguidas entre los controles y la medicadas fueron altamente significativas, indicando que ambos medicamentos mejoraron el estado patológico de las mismas. Ratas con estreñimiento: con respecto a estas ratas lo único importante es que la ganancia de peso fue significativa en las que recibieron bromuro de pinaverio. Conclusión: en nuestro estudio demostramos que tanto el tegaserod como el bromuro de pinaverio pueden ser efectivos en la diarrea, así como en el estreñimiento en un modelo experimental en ratas.
Introduction: Diarrhea or constipation was induced in a group of rats by the use of drugs that stimulate secretion or drugs inducing constipation. In these rats pinaverium bromide and tegaserod were used as a drug inducing less bowel movement or as a facilitator of defecacion, respectively. This work has as its main objective to find out until what point can these drugs be used as an efective treatment for irritable bowel syndrome. Methods: 12 adult female rats, Sprague Dowley breed, were used. They were distributed in the following way: 2 as control for diarrhea, 4 of them had induced diarrhea with a phenolphthalein mixture and magnesium sulphate; 2 with Tegaserod and 2 with Pinaverium Bromide. In constipation, 2 rats were used as control, 4 of them were administered loperamide to induce constipation, and 2 were treated with Tegaserod and 2 with Pinaverium Bromide. Results: Rats with Diarrhea: With respect to these rats, the variations in weight obtained among controls and the medicated group were highly significant, indicating that both drugs improved their pathological condition. Rats with Constipation: With respect to these rats the one important thing is that gain weight was significant only in the group that received Pinaverium Bromide. Conclusion: In our study we demonstrated that both, Tegaserod and Pinaverium Bromide can be effective treating diarrhea and constipation in an experimental model in rats.
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0.05).Conclusion Omeprazole and Tegaserod improved the reflux symptoms of the NERD patients.Omeprazole improves abnormal acid exposure but not abnormal bile exposure.Tegaserod improved neither abnormal acid exposure nor abnormal bile exposure.
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Objective To study the clinical effect on C-IBS treated with tegaserod and bifico combined. Methods 156 patients were randomly divided into one therapy group (group A) and two control group (group B, group C). Patients in the group A were given tegaserod and bifico therapy, while those in group B were given tegaserod therapy and group C were given bifico therapy. Results After 4 weeks' clinical treatment, the rates of remission were 94.6% in group A,7 9.1 % in group B and 54.2% in group C. There were significant statistical differences among three groups(P
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Objective To investigate the effects of tegaserod on visceral sensitivity and explore the regulating mechanism.Methods Forty-two male Spragre-Dawley rats,which were induced colonic inflammation by intraluminal administration of trinitrobenzenesulfonic acid(TNBS),were randomly divided into eight groups.In the three colorectal distention(CRD) treated groups(n=6),abdominal contractions were recorded after 3,7 and 14 days of intra-gastric administration of tegaserod 2mg/kg d.In the three CRD control groups(n=4),abdominal contractions were recorded after 3,7 and 14 days of intra-gastric injection of saline 2.0mL/d.In immunohistochemistry(IH) treated group(n=6) and IH control group(n=6),samples of colon were removed and processed for SP and CGRP immunohistochemistry after 7 days of intra-gastric administration of tegaserod and saline,respectively.Results Abdominal contractions induced by colonic distention decreased significantly at 1.2mL and 1.6mL distention volume after 3 days of tegaserod administration(P
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0.05).Conclusions Certain cases of GERD may have the symptoms of pharyngolaryngitis.After being treated with omeprazole or tegaserod,the patients with abnormal acid reflux may get significant symptomatic improvements.
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Objective To evaluate the efficacy of tegaserod in treating overlapping symptoms of chronic constipation and dyspepsia or reflux.Methods Eighty eight patients with overlapping symptom were enrolled and randomly divided into:tegaserod group(TEG group,received tegaserod 6 mg bid), PPI group(esomeprazole 40 mg qd)and combined group(tegaserod 6 mg bid and esomeprazole 40 mg qd).Esomeprazole was taken 30 min-prior to the meals in the morning.Each group was treated for 4 weeks.Endpoints to evaluate the clinical efficacy including complete relief rates(CRRs)of epigastric symptoms,the total scores of gastrointestinal symptoms,gastric emptying and colonic transit time and gastric sensation.Results The total scores of gastrointestinal symptoms were all significantly decreased in three groups after four-week therapy,which were more decreased markedly in TEG group(7.23?3.13)and the combined group(5.13?2.26)than that in PPI group(13.58?2.02,P
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Objective To assess the effects of tegaserod on rat with visceral hypersensitivity. Methods Neonatal SD rats were randomized to receive colonic acetic acid irritation between postnatal days 8 and 21 as visceral hypersensitive model (Group H) or by saline intrarectally as control group (Group C). While rats were grown-up, rectal distention (RD) was performed by a balloon rapidly inflated with increasing volumes of saline (0.4, 0.8 and 1.2 ml) for 20 seconds at five-minute intervals. The 5 subgroups of Group H were injected randomly with saline, vehicle (1-methyl-2-thpyrrolidone) or tegaserod at doses of 0.1, 0.3 and 1 mg/kg i.p., respectively. The 2 subgroups of Group C were injected with saline or tegaserod at dose of 1 mg/kg i.p.. RD was performed 10 min after injection and abdominal withdrawal reflex (AWR) was recorded, and then c-Fos expression in spinal cord (L6-S1) was analyzed quantitatively by immunohistochemistry. Results 1) Compared to saline, vehicle did not affect AWR and c-Fos expression. 2) Compared to saline, tegaserod significantly (P
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OBJECTIVE: To study the bioequivalence of tegaserod maleate dispersible tablets in healthy volunteers.METHODS: A single oral dose of 6mg test or reference preparations of tegaserod maleate was given to 22 healthy volunteers in a randomized crossover study.The plasma concentrations of tegaserod were determined by LC/MS/MS assay.RESULTS: The main pharmacokinetic parameters of test and reference products were as follows: tmax(0.86? 0.22) and(1. 01? 0.24) h;Cmax(2.21? 0.69) and(2.05? 0.64) ng? mL1;AUC0～ 17(6.35? 2.48) and(6.47? 1.99) ng? h? mL-1,AUC0～ ∞(6.69? 2.59) and(6.70? 2.03) ng? h? mL-1,respectively.The relative bioavailability of test to reference preparation was(98.2? 22.1) %.CONCLUSION: The reference preparation and the test preparation are bioequivalent.