Síndrome de intestino irritable: la importancia de los antiespasmódicos / Irritable bowel syndrome. Relevance of antispasmodics

Resumen El síndrome de intestino irritable se caracteriza por la existencia de dolor abdominal relacionado con cambios en el ritmo evacuatorio. A pesar de los avances en el conocimiento de su fisiopatología y de la aparición de nuevas formas terapéuticas, los antiespasmódicos se han mantenido en el tiempo como una forma efectiva para el manejo de los síntomas de este síndrome, en especial para el dolor. Así pues, el propósito de esta revisión es la búsqueda de evidencia científica que soporte el uso de antiespasmódicos en el manejo de los síntomas del síndrome de intestino irritable.

Abstract Irritable bowel syndrome is a disorder characterized by abdominal pain related to changes in bowel movements. Despite the progress made in the knowledge of its pathophysiology and the emergence of new therapeutic forms, antispasmodics have remained over time as an effective way to treat symptoms, especially pain. The purpose of this review is to search for scientific evidence on the use of antispasmodics in the treatment of irritable bowel symptoms.

Rol de los antiespasmódicos en el manejo del síndrome de intestino irritable (SII) / The role of antispasmodics in managing irritable bowel syndrome

Resumen El uso de los antiespasmódicos forma parte de la piedra angular del tratamiento en el síndrome de intestino irritable (SII), independientemente del subtipo. Consideramos relevante hacer una revisión de los medicamentos antiespasmódicos disponibles actualmente en Colombia, los cuales son usados crónicamente, de manera frecuente, en esta enfermedad.

Abstract Although antispasmodics are the cornerstone of treating irritable bowel syndrome, there are a number of antispasmodic medications currently available in Colombia. Since they are frequently used to treat this disease, we consider an evaluation of them to be important.

Camylofin dihydrochloride injection: a drug monograph review

Camylofin dihydrochloride is an anti-spasmodic drug available in India and other Latin American and African countries, for the treatment of abdominal colic and for acceleration of labor. Although, the drug has been in use for over six decades, with multiple citations in academic text books of repute, treatment protocols, and multiple research publications, there is no consolidated published information on the pharmacology and clinical details of camylofin. This drug statement/monograph is an attempt to collate and present scientific information that will come in handy to practicing obstetricians and gynaecologists, as well as other primary care physicians, when treating cases of abdominal colic or managing prolonged labor. Approved clinical indications, clinical pharmacology, dosage, contraindications, precautions, drug interactions, adverse effects, overdose and clinical evidence in different indications are covered herein.

Role of camylofin and its combinations in obstetrics and gynaecological practice: a review of Indian evidence

Anti-spasmodic drugs like camylofin are used in obstetrics and gynaecological practice for broadly two conditions - spasmodic abdominal pain and management of prolonged labor. Camylofin has been in use in India for almost six decades. As a spasmolytic, camylofin has demonstrated good efficacy and tolerability, both in the management of abdominal spasmodic pain and in augmentation of labor. Literature evidences has suggested that camylofin has demonstrated a statistically significant superiority, such as higher spasmolytic potency compared to other anti-spasmodics like drotaverine, hyoscine and valethamate. In some studies, camylofin maintained the superior efficacy, despite being given as a single dose compared to repeat doses of comparator drugs. Also, in augmentation of labor, camylofin single dose demonstrated superior efficacy when the comparator arm was given a combination of two anti-spasmodic drugs i.e. hyoscine and valethamate in three doses at hourly intervals. Clinical studies in abdominal colic pain revealed significant superiority of the camylofin-paracetamol combination over dicylomine paracetamol combination, this despite the camylofin combination containing 300mg paracetamol as compared to the dicyclomine combination containing 500mg paracetamol. Similar results, highlighting better outcomes in abdominal colic of different types, was shown in studies comparing camylofin-diclofenac combination compared with hyoscine (in renal colic) and also camylofin-mefenamic acid combination compared with dicyclomine-mefenamic acid combination (in menstrual colic). All the above clinical study results resonate in the findings of a recent survey with gynaecologists across the country, which showed that camylofin is considered as the anti-spasmodic most suitable for female patients compared to drotaverine, dicyclomine and hyoscine. Given the availability of strong clinical trial data in Indian women patients, camylofin along with its combinations holds a strong place in the armamentarium of practicing obstetricians and gynaecologists and can be a preferred choice of therapy in treatment protocols of abdominal spasmodic pain and augmentation of labor.

Antispasmodic and Myorelaxant Activity of Organic Fractions from Origanum majorana L. on Intestinal Smooth Muscle of Rodents

Aims: Origanum majorana (Lamiaceae) is a herbaceous and perennial plant that is used in the Moroccan traditional medicine for treating gastrointestinal disorders. The objectives of this study were to confirm the antispasmodic and the myorelaxant activity of organic fractions of Origanum majorana (OM) in rat and rabbit jejunum. Place and Duration of Study: Laboratory of Physiology, Genetic and Ethnopharmacology, Faculty of Sciences, Mohamed the First University, between September 2013 and July 2014. Methodology: The antispasmodic and the myorelaxant test evaluated in vitro on rat and rabbit intestines mounted inside an isolated organ system with a temperature of 37ºC, pH 7.4 and continuous oxygenation Results: The screening study showed those organic fractions of OM decreased the tone of contraction induced by the Carbachol 10-6 M and the KCl 25 mM in the jejunum. The maximum decrease was obtained by dichloromethane fraction of Origanum majorana (DFOM). DFOM induced dose-dependent and reversible inhibition in intestine contraction of rabbit jejunum with IC50 = 0.162 ± 0.002 mg/ml without any alteration of this effect in the presence of adrenergic inhibitors. Pretreatment of the tissue with this fraction (0.01-0.3 mg/ml) induced a dose-dependent shift of the dose-response curve of Carbachol and CaCl2 to the right. The pharmacological inhibitors such as Atropine, L-NAME, Hexamethonium, Nifedipine and Methylene blue did not alter the relaxing effect of DFOM. Conclusion: The results study confirms the antispasmodic and the myorelaxant effect of OM extract. Also, the results showed that adrenergic receptors, NO, guanylate cyclase or muscarinic receptors pathways did not involve in relaxation induced by DFOM suggesting that it exerts an antispasmodic effect on intestinal smooth muscle like a non-competitive antagonist towards the voltage-dependent calcium channels.

Antispasmodic activity from Serjania caracasana fractions and their safety

Abstract In a previous study, we reported the antispasmodic and gastroprotective effects of the Serjania caracasana (Jacq.) Willd., Sapindaceae, extract. In the present study, we evaluated the LD50, hemolytic and antispasmodic activities of its fractions and characterized its major constituents by isolation and GC-MS. The animals showed non-toxic symptoms with oral doses up to 2000 mg/kg, suggesting a safe oral administration. Furthermore, a low hemolytic activity was detected for the saponin fraction. Antispasmodic activity of the fractions was evaluated through carbachol-induced contractions in rat ileum. The hexane fraction was the most potent (IC50 68.4 ± 5.9 µg/ml) followed by the dichloromethane fraction (IC50 161.3.4 ± 40.7 µg/ml). Butanol fraction was the less effective (IC50 219.8 ± 60.3 µg/ml). The phytochemical study of the S. caracasana fractions afforded the isolation of friedelin, β-amyrin, allantoin and quercitrin. This is the first time that the presence of allantoin and quercitrin in the Serjania genus has been reported. Among the isolated compounds and those characterized by GC-MS, β-amyrin and β-sitosterol were present in the most active fractions, hexane and dichloromethane, and they may be related to its antispasmodic activity. In addition, spathulenol was only found in the hexane fraction and its presence might justify the highest antispasmodic activity observed for this fraction.

Possible Mechanism of Antispasmodic Action of Garcinia kola Seed Extract on Isolated Guinea Pig Ileum.

Aims: Garcinia kola is used in West African countries for the treatment of various ailments such as cough, tooth decay, asthma and menstrual cramps. The inhibitory effect of Garcinia kola seed extract (GKE) on drug-induced contractions was studied on iliac smooth muscle preparations of guinea pig to ascertain the validity of the use of Garcinia kola in traditional medicine and to elucidate its possible mechanism of action. Place and Duration of Study: The study was done in Post Graduate Laboratory, Department of Pharmacology, College of Medical Sciences, University of Calabar, Calabar-Nigeria, between November 2013 and April 2014. Methodology: The antispasmodic influence of GKE (0.02 – 1 mg/ml) on acetylcholine, histamine and potassium chloride -induced contractions were carried out. The effect of GKE in a Ca2+-free Tyrode medium and in the presence of adrenergic antagonists was also investigated. Results: The results revealed that GKE inhibited or attenuated the spasmogenic effects of histamine and potassium chloride in a dose-dependent manner and shifted their log. doseresponse curves to the right, with pA2 values of 2.09±0.06 and 3.25±0.07 respectively. Preadministration of propranolol, prazosin or labetalol had no attenuating influence on the antispasmodic effect of GKE. Iliac smooth muscle responses to cumulative increased [Ca2+] in a depolarizing bathing medium and in a Ca2+- free Tyrode solution were also blocked. Comparative antispasmodic potencies indicated that papaverine and aminophylline were more potent than the extract. Conclusion: These findings suggest that Garcinia kola seed extract acts neither via cholinergic nor adrenergic receptor mediation, but may involve interference with Ca2+ mobilization, thus sharing with papaverine and/or aminophylline similar mechanism(s) of action.

Antiasthma biological potency applied for Ephadra Herba quality evaluation / 中草药

Objective: To study the anti-asthma action and biological potency differences of Ephedra Herba from 37 different habitats. Methods: Taking the isolated tracheal smooth muscle from guinea pig to establish antiasthma pharmacological model, the ephedra decoction at different concentration was added to the sink by cumulative metrology method, antispasmodic percentage and biological potency value of Ephedra Herba from different habitats were calculated and the cluster analysis for the biological potency value of Ephedra Herba from different habitats was conducted. Results: Ephedra Herba had the antispasmodic acction to the isolated tracheal smooth muscle of guinea pig caused by histamine phosphate, and compared with the control medicine, Ephedra Herba from 20 habitats showed significant differences (P 0.05); Compared with the control medicine, the antiasthma biological potency of Ephedra Herba from 37 different habitats existed significant or very significant differences (P < 0.05, 0.01), and the antiasthma biological potency value was 22.35-489.04 U/g, while FL% was 13.15%-38.97%, which revealed that the high potency level had a difference of 21.88 times from the low one. And the antiasthma biological potency of Ephedra Herba had lowly significant correlation differences with the total determination of ephedrine and D-pseudephedrine; The Ephedra Herba with different antiasthma biological potency could be identified by cluster analysis method, in which the biological potency from 24 ones in total of 37 Ephedra Herba was higher than that in the control medicine and accounted for 64.86% of the total samples. Conclusion: The anti-asthma biological potency value of Ephedra Herba could quantitatively evaluate the quality of Ephedra Herba from different habitats.

O uso de brometo de pinavério no tratamento da síndrome do intestino irritável / The use of pinaverium bromide in the treatment of irritable bowel syndrome

A síndrome do intestino irritável (SII) é um distúrbio funcional do trato digestivo altamente prevalente, que causa significativo prejuízo da qualidade de vida e impacto econômico e no sistema de saúde. A fisiopatologia da SII é complexa e envolve alterações da motilidade intestinal, bem como aumento da sensibilidade visceral. Pela inexistência de um tratamento etiológico da SII, a abordagem terapêutica usual visa promover o alívio dos sintomas e a melhora da qualidade de vida. Juntamente com a dieta rica em fibras os antiespasmódicos são as medicações mais utilizadas no tratamento da SII. Assim, discutimos a eficácia e a segurança das medicações antiespasmódicas no tratamento da SII.

Efficacy and Safety of Tiropramide in the Treatment of Patients With Irritable Bowel Syndrome: A Multicenter, Randomized, Double-blind, Non-inferiority Trial, Compared With Octylonium

BACKGROUND/AIMS: Antispasmodics such as octylonium are widely used to manage irritable bowel syndrome (IBS) symptoms. However, the efficacy and safety of another antispasmodic, tiropramide, remain uncertain. We aimed to evaluate the efficacy and safety of tiropramide compared with octylonium in patients with IBS. METHODS: In this multicenter, randomized, non-inferiority trial, 287 patients with IBS (143 receiving tiropramide and 144 octylonium) were randomly allocated to either tiropramide 100 mg or octylonium 20 mg t.i.d (means 3 times a day) for 4 weeks. Primary endpoint was the mean change of abdominal pain from baseline assessed by visual analogue scales (VAS) score after 4 weeks of treatment. Secondary endpoints were the changes in abdominal pain from baseline at week 2 and in abdominal discomfort at weeks 2 and 4, using VAS scores, patient-reported symptom improvement including stool frequency and consistency, using symptom diaries, IBS-quality of life (IBS-QoL), and depression and anxiety, at week 4. RESULTS: The VAS scores of abdominal pain at week 4, were significantly decreased in both tiropramide and octylonium groups, but the change from baseline did not differ between the 2 groups (difference,-0.26 mm; 95% CI,-4.33-3.82; P = 0.901). Abdominal pain and discomfort assessed using VAS scores, diaries, and IBS-QoL were also improved by both treatments, and the changes from baseline did not differ. The incidence of adverse events was similar in the 2 groups, and no severe adverse events involving either drug were observed. CONCLUSIONS: Tiropramide is as effective as octylonium in managing abdominal pain in IBS, with a similar safety profile.

Antispasmodic Effects of Aqueous extract of Anthemis mauritiana Maire & Sennen Flowers.

The effects of aqueous extract of Anthemis mauritiana Maire & Sennen flowers (AM) on rabbit and rat jejunum were studied. The AM (0.1-3 mg/mL) showed reversibly relaxation of spontaneous contractions on isolated rabbit jejunal smooth muscle The spasmolytic effect was dose-dependent with IC50 value of 1,48 ± 0,02 mg/ml. Similarly this extract inhibited the contractions of rat jejunum induced by KCl (75mM) and Carbachol (CCh, 10-6M) with IC50 values of 0,48 ± 0,09 mg/ml and 1,53 ± 0,03 mg/ml respectively. Furthermore, AM exhibited an inhibitory effect on the dose-response curves induced by CCh and CaCl2 on rat jejunum. These results clearly demonstrated the antispasmodic effect of AM which was strongly suggested to be mainly due to the inhibitory effect on Ca++ influx through membrane of jejunal smooth muscle.

Tamizaje fitoquímico de Cassia uniflora Mill / Phytochemical screening of Cassia uniflora Mill

Introducción: Cassia uniflora Mill se emplea en el control aleloquímico de Parthenium hysterophorus; se ha reportado que presenta actividad larvicida frente a Aedes aegypti. Tradicionalmente se ha usado como antiespasmódico y para el tratamiento de erupciones cutáneas. Objetivo: realizar un tamizaje fitoquímico a los extractos etéreo, alcohólico y acuoso de la especie Cassia uniflora Mill para conocer los metabolitos secundarios que sean de interés biológico en la terapéutica. Métodos: se recolectaron partes aéreas y subterráneas de la planta, se lavaron, desinfectaron, secaron, pulverizaron y se sometieron a extracciones sucesivas con solventes de polaridad creciente. Los extractos se filtraron y se realizaron ensayos fitoquímicos de identificación. Resultados: el tamizaje fitoquímico, efectuado a los extractos etéreo, alcohólico y acuoso de las hojas, tallos, cáscaras de los frutos, semillas y raíces, demostró la existencia de varias familias de metabolitos secundarios de interés biológico y farmacológico, entre los que se destacan, por su significativa presencia, las quinonas y las coumarinas. Conclusiones: de acuerdo con la diversidad de metabolitos secundarios presentes en las partes evaluadas de C. uniflora, así como los efectos biológicos reportados para la especie, sería interesante realizar nuevos estudios que aporten evidencias sobre su eficacia y seguridad, como forma de avalar su empleo tradicional.

Introduction: Cassia uniflora Mill is used for the allelochemical control of Parthenium hysterophorus; and its larvicidal activity on Aedes aegypti has been reported. It has also been applied as antispasmodic agent and as treatment of cutaneous rash. Objective: to perform a phytochemical screening on alcoholic, ethereal and aqueous extracts from the Cassia uniflora Mill species to identify the secondary metabolites of biological interest in therapeutics. Methods: aerial and underground parts of the plant were harvested, washed, disinfected, dried, powdered and subjected to successive extractions with solvents of increasing polarity. The extracts were filtered to carry out phytochemical tests for identification. Results: the phytochemical screening of ethereal, alcoholic and aqueous extracts from leaves, stems, fruit peels, seeds and roots, confirmed the existence of several families of secondary metabolites of biological and pharmacological interest such as quinones and coumarins that stand out because of their significance presence. Conclusions: according to the diversity of secondary metabolites in the tested parts of Cassia uniflora Mill, as well as the biological effects reported for this species, it would be interesting to conduct new studies to find pieces of evidence on its effectiveness and safety, as a way of supporting traditional use of this plant.

Antispasmodic effects of Aloysia polystachya and A. gratissima tinctures and extracts are due to non-competitive inhibition of intestinal contractility induced by acethylcholine and calcium

The antispasmodic effects of acqueous extracts (AE) and tinctures (T) of Aloysia polystachya (Griseb.) Moldenke and Aloysia gratissima (Gillies & Hook.) Tronc., Verbenaceae, were studied on rat isolated ileum and duodenum. These plants are used for gastrointestinal disorders and as eupeptic in South America. Both AE non-competitively inhibited the dose-response curves (DRC) of ACh and the DRC of Ca2+ in high-[K+]o, as well as the T. The T of A. polystachya and A. gratissima respectively inhibited the ACh-DRC at the IC50 of 3.15±0.57 and 6.46±2.28 mg leaves/mL. The Ca2+- antagonist activity of both T occurred with IC50 respectively similar to those of the ACh-DRC, and was potentiated by the depolarization produced by 10 mM TEA, a blocker of K+- channels. The spasmolytic effect of T does not involve DA release and binding to D2, since it was not reduced by 10 µ M metoclopramide. Also, T induced dose-dependent relaxation on the tonic contracture produced by high -[K+]o and ACh. By TLC there were detected in the leaves the presence of carvone, and flavonoids such as quercetin and hesperidin. By HPLC there were not found vitexin nor isovitexin, identified in A. citriodora. The monoterpene (-)- carvone non-competitively inhibited the ACh-DRC (pD'2 of 4.0±0.1) and the DRC of Ca2+ (pD'2 of 3.86±0.19), suggesting that the Ca2+- influx blockade is the mechanism of its antispasmodic effect. Results suggest that the antispasmodic effect of A. polystachya and A. gratissima are mostly explained by the non-competitive blockade of Ca+2 influx. It could be associated to the presence of flavonoids, and in the tinctures to some spasmolytic components of the essential oil such as carvone.

Antispasmodic effect of Jatropha gossypiifolia is mediated through dual blockade of muscarinic receptors and Ca2+ channels

The antispasmodic activity of Jatropha gossypiifolia L., Euphorbiaceae, aerial parts was investigated in rodents using the mouse intestinal transit model and acetylcholine (ACh, 10-9 to 10-4 M) and calcium (CaCl2, 10-4 to 10-1 M)-induced contractions of isolated rat jejunum. Similar to atropine (1 mg/kg), oral doses of ethanolic extract (EE) of J. gossypiifolia (500, 1000 and 2000 mg/kg) produced a decrease in intestinal transit (37.6 to 57.1 percent) when compared with control. The ACh-induced contraction in the jejunum was inhibited by EE (0.5, 1.0 and 2.0 mg/mL), chloroformic (CF) and aqueous fractions (0.1 and 0.5 mg/mL) and methanolic subfraction (0.05 and 0.25 mg/mL), suggesting an antimuscarinic mechanism. CaCl2 - induced responses in jejunum were also attenuated in the presence of CF (0.05 and 0.1 mg/mL) implying a direct interference of CF with the influx of calcium ions in the cells. Only the organic fraction of the extract had a calcium-antagonist effect, whereas both chloroformic and aqueous fractions had anticholinergic effect. These results suggest that the antispasmodic effect of J. gossypiifolia may be due a combination of anticholinergic and calcium antagonist mechanisms.

Efecto relajante de las hojas de Ocimum basilicum y Foeniculum vulgare colombianas en íleon aislado de rata / Relaxing effect of the leaves of Colombian Ocimum basilicum and Foeniculum vulgare in a rat's cut off ileum

El hinojo y la albahaca han sido usadas por largo tiempo en la medicina popular como antiespasmódicos para mejorar las dolencias gastrointestinales y el cólico intestinal. Se evaluó el efecto in vitro de la infusión al 10 por ciento de hojas secas de Ocimum basilicum (albahaca) y Foeniculum vulgare (hinojo) cundiboyacenses y la mezcla 1:1 de ambas infusiones, en el tono de íleon precontraído de rata. Se observó una disminución del tono al comparar con el agua destilada en cantidades iguales, la cual fue dependiente de la dosis, con una diferencia estadísticamente significativa, para cada una de las plantas y la mezcla. No se encontró un efecto aditivo con la mezcla de ambas plantas. El estudio demostró el efecto relajante de las infusiones de albahaca e hinojo al 10 por ciento, en el tono del íleon precontraído de rata.

Fennel and basil have been used for a long time in popular medicine as antispasmodic to alleviate gastrointestinal colics and complaints. The effect of 10% of dry leaves of basilinfusion (Ocimum basilicum) as well as fennel infusion (Foeniculum vulgare) was evaluated. The mixture of both infusions 1:1 in the tone of a rat contracted ileum were also evaluated in vitro. A decrease in the tone compared with the distilled water in equal quantities was seen. This one was a dependent dose with a statistical meaningful difference for each oneof the plants and the mixture. We did not find out an additive effect with the two plants mixture. The study showed the relaxing effect of the fennel and basil 10% infusion, in the tone of the pre-contracted rat’s ileum.

Choleretic and antispasmodic effects of Lippia integrifolia aqueous extract / Efeitos colerético e antiespasmódico do extrato aquoso de Lippia integrifolia

The aqueous extract of the aerial parts of Lippia integrifolia has been assayed for its choleretic and antispasmodic effects. Doses of 250, 500 and 750 mg/kg administered orally in rats significantly increased the bile flow and the bile acid output. The extract also showed a significant reduction of the contractions induced by acetylcholine, CaCl2 and KCl on isolated rat jejunum. The total caffeoyl quinic acids derivatives content, expressed as chlorogenic acid was 0.10 percent w/v by spectrophotometric determination.

O extrato aquoso das partes aéreas de Lippia integrifolia foi ensaiado quanto aos seus efeitos colerético e antiespasmódico. Doses de 250, 500 e 750 mg/kg administradas oralmente em ratos aumentaram significativamente o fluxo biliar e a saída de ácidos biliares. O extrato também exibiu uma significativa redução das contrações induzidas por acetilcolina, CaCl2 e KCl em jejuno isolado de rato. O conteúdo total de derivados dos ácidos cafeoilquínicos, expressado como ácido clorogênico foi de 0.10 por cento w/v através de determinação espectrofotométrica.

Avaliação dos efeitos miorelaxante, antiespasmódico e antinociceptivo do extrato aquoso da Phoradendron piperoides (Kunt.) Trel. (Viscaceae) / Investigation on miorelaxant, antispasmodic and analgesic effects of the aqueous extract of Phoradendron piperoides

Foram investigados os efeitos miorelaxante, antiespasmódico e antinociceptivo do extrato aquoso liofilizado das folhas da Phoradendron piperoides. A toxicidade aguda também foi avaliada. No íleo isolado de cobaio, o extrato aquoso da P. piperoides (0,05 - 2,0 mg/mL) produziu relaxamento de forma concentração-dependente (IC50 = 0,114 mg/mL) e, na concentração de 1,5 mg/mL, reduziu a amplitude das contrações induzidas por carbacol (2 μM), histamina (2 μM) e BaCl2 (0,03 M) em 46,6; 38,6 e 55,3 por cento (p < 0,001), respectivamente. Em camundongos, o extrato aquoso liofilizado (100-400 mg/kg) não reduziu de forma significativa as contorções abdominais induzidas por ácido acético, não modificou o tempo de reação dos animais no teste da formalina e não aumentou o tempo de latência ao calor no teste da placa quente. No ensaio de toxicidade aguda utilizado, não foi detectada a morte de nenhum animal após tratamento com doses de até 5 g/kg (p.o.) do extrato. Em conclusão, os resultados obtidos indicam que o extrato aquoso da P. piperoides apresenta efeito antiespasmódico e baixa toxicidade aguda. O extrato, no entanto, não possui efeito antinociceptivo.

The present work evaluated the antinociceptive, miorelaxant and antispasmodic effects as well as the acute toxicity of the aqueous extract from leaves of Phoradendron piperoides. In guinea pig ileum, the plant extract (0.05 - 2.0 mg/kg) decreased the preparations basal tone in a dose-dependent manner (IC50 = 0.114 mg/mL) and it (1.5 mg/mL) reduced (p < 0.001) the contractions induced by carbachol (2 μM), histamine (2 μM) and BaCl2 (0.03M). The extract, at oral doses of 100, 200, and 400 mg/kg, did not manifest a significant antinociceptive effect in the writhing, formalin and hot-plate tests. Moreover, no animal deaths were observed in doses up to 5 g/kg. In conclusion, the aqueous extract of Phoradendron piperoides showed no antinociceptive effect and no acute toxicity in mice. Indeed, it revealed miorelaxant and antispasmodic activities that are probably miogenic and not specific for neurotransmitters.

A Clinical Usefulness of Premedication with Hyoscine-N-butyl bromide (Buscopan(R)) in Colonoscopy: A Randomized, Double Blinded, Prospective Study / 대한소화기내시경학회지

BACKGROUND: Use of antispasmodic medication prior to colonoscopy is controversial but someone believes antispasmodic may improve visualization of colonic mucosa and ease colonoscope insertion. So, we designed a study to assess the effect of premedication with the antispasmodic, hyoscine-N-butyl bromide(Buscopan(R)) on the performance of colonoscopy. METHODS: This study was prospective, double blinded, randomized, controlled study, One hundred three consecutive patients were randomized to receive intravenous buscopan lml(n=52) or placebo(n=51) combined with our standard initial medication(me-peridine 50 mg and midazolam 2 mg). Insertion of colonoscopy was timed, and 100 mm visual analogue scales (VAS) were used for asscssing difficulty of procedure, colonic motility, frequency of positional change, frequency of external compression, difficulty of assistance and degree of discomfort experienced by the patients. RESULTS: There were no significant differences of intubation time between buscopan group(mean time, 7.23 min., range 2~15) and placebo group(7.07 min., range 3~25), (p=0.83) and withdrawal time between buscopan group (6.46 min., range 2-22) and placebo group(6.76 min., range 2 25), (p=0.69). Also, there was no significant differences in intubation time between males and females(buscopan; males 7.00 min., females 7.60 min., p=0.34, placebo; males 7.0~5 min., females 7.08 min., p 0.44). The VAS scores checked by endoscopist(p=0.29), assistant(p=0.32) and patient (p=0.15) were not significantly different in both groups. There were no significant differences in intubation time, VAS scores nf endoscopist, assistant, and patients. CONCLUSION: Premedication with intravenous bu.opan has no advantage on colonoscopy procedure. Use of antispasmodic medication prior to colonoscopy was not considered as recommendable agent.