No full-text available
To read the full-text of this research,
you can request a copy directly from the authors.
Review of the therapeutic use of simethicone in gastroenterology
Abstract
Background: The history of simethicone covers more than 50 years. The main properties of simethicone are the defoaming reduction of surface tension and the reduction of surface viscosity and hydrophobicity which enable simethicone to spread easily over surfaces. It is not absorbed and is virtually non-toxic. While its use is well-established in diagnostic procedures, therapeutic studies have sometimes been contradictory. Objective: To assess the therapeutic efficacy and safety of simethicone taking into account clinically relevant end points and following the guidelines provided by the Cochrane Collaboration. Methods: The data sources consulted were bibliographic databases, references from review articles and books, as well as personal contacts up to September 07. All papers were screened and those dealing with prospective clinical trials were summarized in a table by indication, study design and methodological quality. Results: Out of a total of 83 publications, 14 concerning diagnostic procedures and 23 therapeutic trials were retained for closer analysis. Good evidence of efficacy was found for antifoaming in diagnostic work-ups and as a therapeutic agent in: 1 st) Functional dyspepsia, (4 trials; 266 patients simethicone vs. 310 controls) with simethicone superior to placebo and to cisapride, and 2 nd) traveller's diarrhoea, (2 large trials; 248 simethicone patients vs. 244 placebo) with simethicone superior to placebo (increased efficacy when combined with an μ-opioid-agonist). Data are not conclusive in: 1) 'IBS-like' symptoms (2 trials; 80 patients simethicone vs. 54 controls); 2) in post-operative management of intestinal activity (4 mostly old trials; 847 patients simethicone vs. 631 controls); 3) Infantile colics, (7 trials; 306 infants simethicone vs. 296 controls); and 4) as an add-on, against symptoms of gastroesophageal reflux, (3 studies) and in partial adhesive small-bowel obstruction (1 trial). Conclusions: Simethicone may be beneficial in the various indications in which its intraluminal defoaming and coating action are desired. RCTs have shown its efficacy in some indications, in addition to its well-established uses in diagnostic procedures. More RCTs for non-confirmed indications are needed, particularly in view of the very large safety margin of simethicone.
... We found three systematic reviews comparing the effects of simethicone versus placebo on duration of crying or presence of colic in infants. [1] [7] [19] The two earlier reviews [1] [7] have been superseded by the most recent review [19] and are therefore not discussed further here. ...
... We found three systematic reviews comparing the effects of simethicone versus placebo on duration of crying or presence of colic in infants. [1] [7] [19] The two earlier reviews [1] [7] have been superseded by the most recent review [19] and are therefore not discussed further here. ...
... The review included three open-label RCTs that did not meet Clinical Evidence inclusion criteria for this review, and are therefore not discussed further. [19] The first RCT identified by the review (double-blind, crossover, 83 infants aged 2-8 weeks) compared 0.3 mL of simethicone versus placebo (duration of treatment, average of 1 week) before feeds. [20] It found no significant difference in colic (using the standard colic definition), when rated by carers, between simethicone and placebo (28% improved with simethicone v 37% with placebo v 20% with simethicone plus placebo; effect size for simethicone v placebo -0.10, 95% CI -0.27 to +0.08). ...
Colic in infants causes one in six families (17%) with children to consult a health professional. One systematic review of 15 community-based studies found a wide variation in prevalence, which depended on study design and method of recording. METHODS AND OUTCOMES: We conducted a systematic review and aimed to answer the following clinical question: What are the effects of treatments for colic in infants? We searched: Medline, Embase, The Cochrane Library, and other important databases up to September 2009 (Clinical Evidence reviews are updated periodically, please check our website for the most up-to-date version of this review). We included harms alerts from relevant organisations such as the US Food and Drug Administration (FDA) and the UK Medicines and Healthcare products Regulatory Agency (MHRA).
We found 27 systematic reviews, RCTs, or observational studies that met our inclusion criteria. We performed a GRADE evaluation of the quality of evidence for interventions.
In this systematic review we present information relating to the effectiveness and safety of the following interventions: advice to increase carrying, advice to reduce stimulation, casein hydrolysate milk, cranial osteopathy, crib vibrator device, focused counselling, gripe water, infant massage, low-lactose milk, simethicone, soya-based infant feeds, spinal manipulation, and whey hydrolysate milk.
... It is not absorbed and is virtually non-toxic. While its use in diagnostic procedures is well-established, the therapeutic effects in a number of gastroenterological indications are contradictory (Meier and Steuerwald, 2007). In infantile colic, a number of smaller simethicone trials (Danielsson and Hwang, 1985;Metcalf et al., 1994;Sethi and Sethi, 1988) have been published, but evidence did not reach the threshold of significance (Biagioli et al., 2016). ...
... Nevertheless, for most colicky patients paediatricians in Germany and Poland are prescribing simethicone or a pro-/synbiotic (according to the unpublished results from surveys performed by our research team among German and Polish paediatricians). Despite its wide use, there is little evidence that simethicone has significant effects in infantile colic compared to a placebo treatment (Biagioli et al., 2016, Lucassen, 2010Meier and Steuerwald, 2007). ...
The aim of the study was to determine effects of administration of simethicone and a multi-strain synbiotic on the crying behaviour of colicky babies. The study design consisted of an open-label, two parallel treatment group study involving 87 infants aged 3-6 weeks with infantile colic (defined as crying episodes lasting 3 or more hours per day and occurring at least 3 days per week within 3 weeks prior to enrolment) randomly, unequally [1:1.5] assigned to receive simethicone (n=33) or a multi-strain synbiotic (n=54) orally for 4 weeks. The multi-strain synbiotic contained Lactobacillus acidophilus LA-14, Lacticaseibacillus casei R0215, Lacticaseibacillus paracasei Lp-115, Lacticaseibacillus rhamnosus GG, Ligilactobacillus salivarius Ls-33, Bifidobacterium lactis Bl-04, Bifidobacterium bifidum R0071, Bifidobacterium longum R0175 and fructooligosaccharides). Primary outcome measures were the responder rates (effect ≥50% reduction from baseline) of the measures ‘crying days last 3 weeks’, ‘average evening crying duration last 3 weeks’ and ‘reduction of average number of crying phases per day last three weeks’ at the end of treatment. The study is registered at ClinicalTrials.gov under NCT 04487834. Significantly higher responder rates (effect ≥50% reduction from baseline) of the multi-strain synbiotic compared to simethicone were found for the measures ‘crying days last 3 weeks’ (72% vs 18%, P<0.0001) and ‘average evening crying duration last 3 weeks’ (85% vs 39%, P=0.0001). No significant difference was found for the measure ‘reduction of average number of crying phases per day last three weeks’ (50% vs 42%, P=0.4852). No adverse effects were reported for the two treatment groups. Based on these results, the multi-strain synbiotic can be considered as an interesting therapeutic possibility for the treatment of infantile colic, worthwhile to be investigated further in non-clinical and clinical studies.
... It reduces the surface tension of gas in the intestines, allowing small gas bubbles to coalesce. Its efficacy in the treatment of functional dyspepsia is well established 9 . These properties enable simethicone to facilitate the passage of gas and alleviate bloating symptoms. ...
This study aimed to assess the impact of adding pancreatin (a pancreatic enzyme derivative) to standard treatment on patients diagnosed with Irritable Bowel Syndrome (IBS) and Type 2 Diabetes Mellitus (T2DM). IBS and T2DM frequently coexist, leading to significant gastrointestinal symptoms and a decrease in quality of life. Gastrointestinal symptoms arising in T2DM patients present challenges in management for both clinicians and patients. Standard treatments may not fully address these symptoms. Recent studies suggest that pancreatic enzyme replacement therapy may offer additional benefits. This study investigates whether adding pancreatin to standard treatment can improve gastrointestinal outcomes in this patient population. Conducted as a prospective observational study, the research involved patients diagnosed with IBS according to Rome IV criteria and having concomitant T2DM. The patients were divided into two groups: one receiving standard dual treatment (otilinium bromide + simethicone) and the other receiving a triple therapy including a pancreatin derivative in addition to the standard treatment. Various clinical scores and measurements, including Visual Analog Scale (VAS), Bristol Stool Chart (BSC), Irritable Bowel Syndrome-Severity Scoring System (IBS-SSS), and Irritable Bowel Syndrome Quality of Life Instrument (IBS-QOL), were assessed before and after treatment. The study comprised 121 patients, with a median age of 41 years (interquartile range [IQR] 38–48), of whom approximately 70.2% were female. Fifty-eight patients (47.9%) received dual therapy, while sixty-three patients (52.1%) received triple therapy. Before treatment, both groups exhibited similar pre-treatment Bristol stool scale results: normal (39.7% and 49.2%) and constipation (37.9% and 31.7%) in the dual and triple therapy subgroups, respectively (p > 0.05). Post-treatment, the triple therapy group showed a significantly higher proportion of normal cases on the Bristol stool scale (82.5%) compared to the dual therapy group (44.8%) (p < 0.001). After treatment, the triple therapy group demonstrated statistically significant improvements in VAS score (p < 0.001), IBS-SSS (p < 0.001), and IBS-QOL (p < 0.001) compared to the dual therapy group. There were no significant differences between groups in BMI, HbA1c levels, duration of diabetes, or diabetes treatment at baseline (p > 0.05 for all parameters). The findings suggest that adding pancreatin to standard therapies significantly enhanced the quality of life for patients with both IBS and T2DM, demonstrating improvements across various symptom measurements and indicating the potential benefits of this supplementary therapy in managing gastrointestinal symptoms in this population. Further studies are warranted to explore its broader clinical implications and mechanisms of action.
... Dimethicone and simethicone are anti-flatulent agents were found in two antacids. Antifoaming properties of these agents reduce the stomach gases and discomfort, which exacerbate hyperacidity (Meier & Steuerwald, 2007). Sodium alginate in combination with buffering salts is available in oral suspension formulation. ...
Background: Antacids are frequently used as over-the-counter (OTC) medications to reduce symptoms of dyspepsia and to neutralize stomach acidity. Evaluation of antacids efficacy depends on in vitro testing like acid neutralizing capacity (ANC) and acid neutralization potential (ANP). The purpose of this study was to examine ANC, ANP, and other characteristics of commercially available antacid formulations (both liquid and solid formulations) in the Gaza Strip. Methods: Both liquid (n=2) and solid (n=4) antacid formulations were acquired from the Gaza Strip’s central community pharmacies. Preliminary antacid test (PAT) was carried out to determine if the tested formulation is classified as antacid. The general monograph <301> in USP34/NF29 was used for the estimation of ANC, while ANP was investigated using Rossett Rice procedure. Both tests were conducted to evaluate the efficacy of antacid. In addition, cost effectiveness per formulation and statistical analysis test of data were calculated. Results: All formulations were classified as antacids because they all passed the PAT test (pH of antacid-HCl over 3.5). The ANC of antacids (n=6) varied from 8.74±0.37 to 29.14±0.84 mEq per minimum labeled dose (MLD). The ANC/MLD ratios for solid formulations were higher than those of liquid formulations. No statistically significant difference in ANC/MLD between the two groups was estimated (P˃.0.05). ANP test - the time duration during which an antacid formulation maintains pH above 3.5 - ranged from 43 to 90 minutes. According to this study liquids were inefficient in acid neutralization and expensive as a result. Conclusions: The ANC and ANP results indicated the better neutralizing efficacy and duration of solid antacids in comparison to liquids. A1 and A2 formulations– calcium and magnesium salt based solid antacids had the most appropriate properties in terms of efficacy, onset and duration of neutralizing activity. Antacids in the form of chewable tablets were the most cost-effective formulations. It is recommended to examine more batches of the same antacids and to add ANC data on the label of antacids.
... Simethicone (SIM), α-(trimethylsilyl)-ω-methylpoly[oxy(dimethylsilylene)], is present with silicon dioxide to enhance defoaming properties of silicon. It is used as an anti-foaming agent to minimize bloating, distress, or pain due to excessive gas [4][5][6][7][8]. ...
Background
A new, validated, and selective RP-HPLC technique was established for quantitative estimation of Dicyclomine HCl and Simethicone in the pharmaceutical oral liquid drop formulations. The chromatographic conditions were adjusted using Luna C18 (25 cm × 0.46 cm, 5 μm) column, water-methanol mixture (80:20, v/v) as solvent system and pH adjustment up to 7.4 using orthophosphoric acid. The absorbance was observed at 289 nm λmax injecting 20 μl sample solution and maintain the ambient temperature (30 °C) with 1 ml per min flow rate.
Results
The retention times of Dicyclomine HCl and Simethicone were determined 2.962 and 4.091 min, respectively. The developed analytical technique was validated for accuracy, precision, linearity, specificity, sensitivity, ruggedness, and robustness as per ICH guidelines. The LOD was found to be 0.72 and 0.57 μg per ml for Dicyclomine HCl and Simethicone, respectively. But, LOQ was 2.19 and 1.73 μg per ml, respectively.
Conclusions
This validated method showed good precision (RSD% < 1) with acceptable linearity (≥ 0.999). Intra- and inter-day relative RSD of retention times and AUC (area under curve) were found to be less than 2.0%. The method was also significantly useful as economic technique for simultaneous quantitative determination of Dicyclomine HCl and Simethicone in the bulk and pharmaceutical formulation.
... Это приводит к уменьшению вздутия живота, устранению дискомфорта и болей в животе, уменьшению рефлюкса, улучшению переваривания и всасывания пищи. Возможно ускорение моторики кишечника и обволакивающее действие [42][43][44]. Эффективность симетикона в снижении болевой реакции при младенческой колике показана в исследовании K.S. Sethi, J.K. Sethi в 1988 г. [45]. Кроме того, В. Danielsson, С.Р. ...
Infant colic is a common cause of parental anxiety and, as a result, help-seeking behaviour. However, the relationship between breastfeeding and colic is currently not fully understood. The article presents data from various studies of the relationship between breastfeeding and colic. On the one hand, the severity of infant colic may lead to the early cessation of exclusive breastfeeding due to the mother’s fear that the baby’s crying is the result of the ineffectiveness of breastfeeding and the unreasonable transition to supplemental feeding. On the other hand, many authors have identified the protective effect of breastfeeding in relation to infant colic a less pronounced degree of infant colic is reported in the group of children, who are breastfed as compared to the children, who are formula-fed. Therefore, the task of the paediatrician is to provide competent counselling for the anxious parents of an infant with colic using evidence-based medicine (EBM) databases, which will help preserve the mother’s breastfeeding. In most cases, due to competent counselling of the parents, the severity of infant colic may be reduced by improving the quality of breastfeeding (ensuring proper breast grabbing to reduce aerophagy, increasing the proportion of consumption of the so-called «back» milk), reducing anxiety of the parents and increasing the perception of breastfeeding self-efficacy levels by mothers. This may increase the duration of breastfeeding of the infants with infant colic.
... It was first approved for use by the US Food and Drug Administration in 1952 (9). Simethicone may act as a topical mucosal barrier providing protection against irritants such as gastric acid, biliary salts and acetylsalicylic acid (9,10). In the treatment of IBS, a meta-analysis showed that global symptoms and bloating were improved by the addition of simethicone to antispasmodic agents (11). ...
Background:
Bloating is a common symptom reported by around 16% to 31% of the general population. Functional bloating is diagnosed in patients with recurrent symptoms of bloating who do not meet the diagnostic criteria of irritable bowel syndrome or other functional gastrointestinal disorders.
Methods:
This double-blind, multicentre, randomised study compared the safety and efficacy of APT036 (xyloglucan plus tyndallized Lactobacillus reuteri and Bifidobacterium brevis; Aprotecol®) and simethicone in treating functional bloating in adults. APT036 or simethicone were administered orally (3 times/day) for 20 consecutive days, with evaluations at baseline, and on Days 2, 10, 20 (end of treatment) and 30 (follow-up visit). The main outcome measure was safety. Efficacy was assessed at each visit by patient-reported symptom severity (Likert scale) and abdominal girth measurement. A hydrogen breath test was performed at baseline and Day 20.
Results:
Both APT036 (n=54) and simethicone (n=54) were well tolerated by study subjects; no adverse effects were reported with either treatment. Compared with simethicone, APT036 significantly reduced abdominal distension (P=0.008) and flatulence (P=0.010) from baseline to Day 30. The baseline hydrogen breath test confirmed the presence of small intestinal bacterial overgrowth (SIBO) in all subjects. At Day 20, mean hydrogen gas elevation was below the threshold for a diagnosis of SIBO (<12 ppm above basal on glucose administration) in both study arms.
Conclusions:
Both APT036 and simethicone had good safety profiles but APT036 was superior to simethicone in relieving symptoms of functional bloating.
This study's objective was to Developed and validated a new Reverse Phase- High-Performance Liquid Chromatography (RP-HPLC) method for the determination of Impurities in Dicyclomine HCl capsules. The method was developed by adapting the USP API monograph and checked for feasibility study and applied to capsule formulation, In this API methods methods not suitable for estimation of impurities in capsule formulation, hence study was made in changing the column for Known impurity, diluent composition, pH of the mobile phase, Flow rate change and different mobile phases for unknown impurities. By trailed with above explained aspects developed new method for determination of impurities in capsule formulation. This method was developed with an emphasis on specific, linear, accurate andreproducible and compliant with International Council for Harmonization (ICH) guidelines for methodvalidation.Theobtainedresultsofvalidationpa rameterwithintheAcceptance criteria. This implies high reliability of % impurities present in determination of Dicyclomine Hcl capsules with accuracy in method precision samples. In conclusion, the newly developed RP-HPLC methods provides an efficient and precise tool for estimation of impurities in capsule formulations. This facilitates accurate impurity contentassessmentsinroutinequalitycontroltestsforp harmaceuticalcompanies.This study makes a significant contribution to the evolution of pharmaceutical analytical techniques, offering valuable insights into the use of validated RPHPLCmethod.
The aim of this study (ClinicalTrials.gov registration NCT04666324) was to determine the effects of a nine-strain synbiotic and simethicone on the duration of crying and the gut inflammation marker calprotectin in colicky babies aged 3–6 weeks, diagnosed using the Wessel criteria. The open-label study comprised a control group of non-colicky babies (n = 20) and two parallel treatment groups (each n = 50) to which colicky babies were randomly and equally assigned to receive the multi-strain synbiotic or simethicone orally for 28 days. Primary outcome measures were the change in daily crying duration and the level of fecal calprotectin on days 1 and 28 of the study. Administration of the synbiotic resulted in a rechange of crying duration of −7.18 min/day of treatment, while simethicone had a significantly smaller effect (−5.74 min/day). Fecal calprotectin levels in colicky babies were significantly elevated compared to those in non-colicky babies. Treatment with the nine-strain synbiotic resulted in a significant lowering of fecal calprotectin at the end of the study, while no such effect was found for simethicone. No adverse effects were reported. Study results confirm earlier findings of crying duration reductions in colicky babies by the synbiotic, an effect that might be linked to its anti-inflammatory properties.
The mechanism of the foam-inhibiting action of simethicone, mainly used against flatulence, has been studied. Its effect on foaming systems containing synthetic gastric juice and a surface-active substance (anionic surfactant, cationic surfactant, soap solution) was quantitated by measuring the surface tension, foam stability and initial foam density. The effect of simethicone on each of the examined systems was the result of the combination of two actions: the drainage of liquid from foam films and the rupture of relatively thick liquid films. The mechanism of these actions may be described as the liquid drainage followed by bridging of the liquid film by polydimethylsiloxane droplets, helped by hydrophobic silica particles also present in the antifoaming agent, leading to the rupture of the film surface and air escape.
Unlabelled:
Infantile colic concerns about 10-30% of all newborns and has been defined as a condition characterized by paroxysmal episodes of unexplained full force crying for at least three days a week and continuing for one week or more in a thriving well-nourished infant. The disorder more likely occurs in the evening, without identifiable causes and resolves spontaneously by the fourth month of life. The several factors involved in the etiopathogenesis (food intolerance or allergy to cow's milk protein, intolerance to lactose, intestinal hyperperistalsis, neuro-hormonal immaturity, maternal anxiety and familial stress), make the management of infants with colics difficult. We propose a scoring system for the evaluation of colics in infants based on: 1) crying intensity and duration; 2) accompanying characteristics of crises (e.g. meteorism, family history for allergic disease, type of feeding, type of stools); 3) evaluation of parents' opinion of their infants' crying. Type of management is based on the score: a) crying that is unrelated to colics: treatments referred to specific diagnosis. b) crying that is related to colics but not severe: first and second step of management; c) crying that is related to colics and is severe: third step of management.
Management:
first step: pacifier, rocking, dull continuous background noise, hot water bottle on the abdomen, herbal tea, simethicone. Second step: pharmacological treatment and periodic controls. Pharmacological treatment include antispastic drugs (e.g. cimetropium bromide). Third step: dietary modification and/or pharmacological treatment: mothers of breast-fed infants are given a diet with no milk or products containing its proteins, or fish, or eggs. Infants who are not breast-fed receive soy milk and if symptoms continue soy milk is substituted with hydrolyzed casein milk formula. Pharmacological treatment include antispastic drugs (e.g. cimetropium bromide and in non responders dicyclomine hydrochloride). Dietary modifications appear more suitable than pharmacological treatment in resolving symptoms, since side effects of drugs have been described and our recent results indicate appropriate dietary modifications offer better results than pharmacological treatment in resolving crises. However, before interrupting dietary modifications and reintroducing cow's milk proteins, infant's tolerance to such proteins is tested. In any case because of the good prognosis and rapid regression of symptoms, dietary regimens or pharmacological treatment should only be applied if really necessary and for brief periods under medical supervision.
A double blind trial was performed in patients with Cesarean section in order to study the effect of Simeticon (Stuart Pharmaceutical Company, Pasadena, California) on the occurrence of subjective and objective signs of gas distress during the immediate postoperative period. The results obtained with Simeticon show a highly significant reduction of the analysed subjective complaints (nausea, vomiting, meteorism, discomfort in the stomach, abdominal pains) in relation to placebo. Peristaltic movements in patients treated with Simeticon appeared in the first two days in 100% of cases and only in 30% in the placebo group. Flatulence also appeared in all the patients receiving Simeticon, in contrast to only 20% in the placebo group. There was no difference in spontanous defecation between the groups. On the basis of the results obtained, and considering the non-toxicity of the drug, its chemical inertnees, good tolerance, and simple use, the authors consider simeticon very useful for the prevention and therapy of postoperative discomfort due to gas accumulation and gastro-intestinal distention after Cesarean section.
It has been suggested that pre-procedural oral simethicone improves visibility in upper GI tract endoscopy. We examined three-hundred-thirty patients referred for upper endoscopy who were randomized and were required to swallow a placebo solution or one of three liquid simethicone solutions 15 min prior to the examination. These solutions contained 65 mg, 65 mg and 195 mg of drug dissolved in 90 ml, 30 ml and 90 ml of water, respectively. Patients treated with both dosages of simethicone revealed significantly less foam and bubbles in both the stomach and the duodenum compared to placebo. Only the 90 ml volume adequately cleared both locations. The reduction of examination time could be found both in patients with an intact stomach and in patients with or without gastric bile reflux, but was most striking in patients with previous gastric resection (examination time being reduced by almost 50% and the need of adjunctive lavage being reduced about 20 fold compared to placebo). In conclusion, pre-procedural oral simethicone should be routinely considered in patients with previous gastric resection. The utility of the drug is less evident in patients with normal gastric anatomy.
The results of studies of the effect of simethicone on abdominal gas-related symptoms have been contradictory. In a randomized, double-blind cross-over study, 10 healthy volunteers were given 30 g lactulose and 600 mg simethicone or placebo. End-expiratory breath samples were collected and analyzed for H2 and gastrointestinal symptoms registered. There were no differences in biochemical parameters or symptom score between simethicone and placebo. In contrast to previous studies, we used a sufficiently large dose of lactulose to produce gastrointestinal symptoms, a higher dose of simethicone and placebo tablets containing the same additives as the simethicone tablets. There was no demonstrable effect of simethicone on symptoms or intestinal gas production caused by carbohydrate malabsorption.
Fifty-three patients with symptomatic reflux oesophagitis were entered into a single centre randomized study comparing the effects of a dimethicone/antacid (Asilone Gel) and an alginate/antacid (Gaviscon liquid) on symptoms and endoscopic changes over an 8-week period. Both treatments significantly improved heartburn, acid regurgitation and flatulence. Dimethicone/antacid but not alginate/antacid, produced a significant improvement in oesophagitis, oesophageal ulceration and histological grade of inflammation over the 8-week treatment period so that 14 patients treated with dimethicone/antacid and 10 with alginate/antacid had normal endoscopic oesophageal appearances at the end of the study. The difference in improvement between the two patient groups did not reach significance however, except for dimethicone/antacid improving histological changes (P less than 0.05). These findings suggest that dimethicone/antacid and alginate/antacid are equally effective in treating symptomatic reflux oesophagitis although dimethicone/antacid may have an advantage in improving oesophageal histological appearances.
The gastric potential difference (PD) was measured in ten healthy volunteers after sodium taurocholate intake. This bile salt was given after treatment with dimethicone or placebo in a cross-over design study.
With dimethicone the fall in PD was lower (16.1 vs. 24.8 mV,) and shorter (32.5 vs. 51.0 min) than with the placebo.
Our result suggests that the silicone can prevent the formation of the gastric lesions induced by bile salts.
The effect of simethicone in improving visibility during colonoscopy was randomly studied in 97 patients receiving either simethicone (N = 49) or placebo (N = 48) in a colon lavage solution. Visibility was assessed by the amount of bubbles and the degree of haziness noted during colonoscopy. The degree of bubbles was scored on a scale of 0 to 3, and haziness was scored on a scale of 0 to 2. Patients receiving simethicone had significantly less bubbles (p less than 0.001) and less haziness (p less than 0.01) in the colon when compared to placebo-treated patients. These data indicate that the addition of simethicone to the colonic lavage solution results in improved colonic visibility and may result in technically easier and more accurate colonoscopy.
Dimethicone is a common additive to antacids, although its value in the treatment of reflux oesophagitis is unproven. Its efficacy was assessed by comparing the effect of a dimethicone-containing antacid gel (Asilone Gel) with a simple antacid gel in a double-blind trial in 45 patients with reflux oesophagitis. Thirty-eight patients completed the eight-week course of therapy.
Antacid therapy alone resulted in a significant improvement of both symptoms and oesophagitis in gastro-oesophageal reflux. The inclusion of dimethicone in the antacid gel preparation did not confer any benefit in terms of symptomatic assessment but did confer a small advantage with regard to objective markers of oesophageal inflammation, suggesting that a dimethicone-containing antacid is of value in the treatment of symptomatic gastro-oesophageal reflux.
To overcome the effects of intestinal gas which may be a problem for ultrasound examinations, a double-blind study was undertaken in 42 patients in whom the first ultrasound examination was unsatisfactory due to excessive intestinal gas. The patients received either a liquid dimeticon preparation over 24 hours (total dosage 480 mg) or a placebo. Criteria for the evaluation of the treatment were the ability to visualize the pancreas, the aorta and the para-aortic region at the second examination. The quality of the ultrasonic images was found to be improved in 52% of the controls by repetition and in 71% of the test substance group, the difference being not significant (p greater than 0.05). It is concluded that: It is worthwhile asking the patient to return for a second examination 24 hours later before resorting to invasive and/or expensive procedures when the first scan was of poor quality and liquid dimeticon has no significant defoaming effect in these patients.
The mucosal protective and antiflatulent properties of polydimethylsiloxane (PMS) alone, or containing free silica have been examined in rats. Both PMS and PMS + 6% silica significantly protected rat gastric mucosa from the irritant effects of aspirin but there was no significant difference between the protective effect of each agent. The antiflatulent property of PMS, as determined by X-ray measurements of foam production in the rat stomach, was significantly enhanced by the addition of free silica.
Twenty four subjects with a history of frequent discomfort associated with eating, participated in a double blind crossover study to compare the effectiveness of simethicone and an identical appearing placebo in the relief of the symptoms they experienced on challenge with a test meal. Simethicone was significantly more effective in relieving these patients' symptoms, especially those directly related to gaseous accumulations, gas, fullness, distension, bloating and pressure. Additionally, relief with simethicone came significantly faster than with placebo. A highly significant proportion of the subjects expressed an overall preference for the relief afforded by simethicone as compared to placebo. In conclusion, simethicone is highly effective in the relief of upper gastrointestinal symptoms, especially in those most closely related to gaseous distension.
Forty one patients participated in a double blind study comparing the efficacy of simethicone and placebo in relieving the symptoms of their troublesome functional upper gastrointestinal disorders. Patients were assigned randomly to parallel simethicone and placebo treatment groups and followed a fixed dosage regimen of study medication for a 10 day course of therapy. The main efficacy parameters measured were the changes in frequency and severity of 10 target symptoms of functional upper gastrointestinal disease and an overall (global) rating of clinical benefit. Highly significant decreases in frequency and severity of target symptoms were demonstrated in the simethicone versus the placebo group. Additionally, the global rating revealed highly significant clinical benefit to the simethicone treated patients as compared with those treated with placebo. It is concluded that simethicone is a safe and effective agent for the relief of the symptoms of functional upper gastrointestinal disease.
The addition of simethicone to the postoperative regimen of obstetric and gynecologic patients is shown to be a simple, safe and effective method for reducing gastrointestinal discomfort after major operations and for decreasing the incidence of ileus.
(C) 1971 The American College of Obstetricians and Gynecologists
The results of studies of the effect of simethicone on abdominal gas-related symptoms have been contradictory. In a randomized, double-blind, cross-over study, ten healthy volunteers were given 30 g lactulose and 600 mg simethicone or placebo. End-expiratory breath samples were collected and analyzed for H2, and gastrointestinal symptoms registered. There were no differences in biochemical parameters or symptom score between simethicone and placebo. In contrast to previous studies, we used a sufficiently large dose of lactulose to produce gastrointestinal symptoms, a higher dose of simethicone and placebo tablets containing the same additives as the simethicone tablets. There was no demonstrable effect of simethicone on symptoms or intestinal gas production caused by carbohydrate malabsorption.
The influence of dimeticone (Gel de Polysilane Midy) on the pharmacokinetics and pharmacodynamics of oral ethyl biscoumacetate was studied in 6 healthy volunteers in a randomised single dose, two-way cross-over study. Each volunteer received at one week interval a single dose (300 mg) of ethyl biscoumacetate, either alone or with dimeticone. Ethyl biscoumacetate levels were measured in plasma for 24 hours. Pharmacodynamic parameters were measured for 96 hours. Ethyl biscoumacetate peak concentration was significantly higher when administered with dimeticone (40.3 +/- 25.3 mg/l vs 31.0 +/- 25.7 mg/l; p = 0.031), without significant change in the area under curve. Other pharmacokinetic and pharmacodynamic parameters did not differ significantly. The slight increase of the ethyl biscoumacetate bioavailability with dimeticone in repeated dosing might have pharmacodynamic consequence; a clinical trial should address this question.
Oral sodium phosphate solution is better tolerated than polyethylene glycol when used for colonoscopy preparation, but visibility of the lumen can be impaired because of the presence of bubbles.
We studied 86 patients receiving either simethicone (n = 42) or placebo (n = 44) in addition to oral sodium phosphate to determine if simethicone improved visibility during colonoscopy. Colonoscopy was performed by a single blinded investigator. Five areas of the colon (rectosigmoid, descending, transverse, ascending, and cecum) were assessed for the presence of bubbles on withdrawal of the endoscope. Bubbles were scored as follows: 0, minimal or none; 1, covering half the lumen; 2, covering the entire circumference; 3 filling the entire lumen.
Thirteen patients in the placebo group and only one in the simethicone had significant bubbles ( > or = 1). Additionally, the mean bubble scores were greater in the placebo group in each region of the colon (p < or = 0.05 in rectosigmoid and ascending colon).
This study indicates that taking simethicone with an oral sodium phosphate preparation can improve colonic visibility by diminishing the presence of bubbles. Better visualization could improve detection of mucosal pathologic lesions.
To determine whether abdominal discomfort is a cause for distress symptoms in infants following administration of inhalational anesthesia, and to evaluate the effectiveness of simethicone in treating this discomfort.
Randomized, double-blinded study.
Large tertiary care, university-based medical center.
175 ASA physical status I and II infants under 28 months of age who underwent an inhalational anesthetic for a variety of procedures that were expected to cause relatively little pain.
Children were assessed for the presence of postoperative abdominal discomfort, and, if evident, were randomly given either simethicone or placebo in a double-blinded fashion.
Abdominal discomfort was measured using the Faces Legs Activity Cry and Consolability (FLACC) Behavioral Pain Scale. Scores were recorded pre-drug; at 10, 20, and 30 minutes following drug administration; and at discharge. If discomfort had not resolved within 15 minutes after the drug was given, routine analgesics or other medications were administered. Abdominal girth was measured preoperatively, on admission into the postanesthesia care unit (PACU), and at discharge. 21% of infants exhibited symptoms of abdominal discomfort postoperatively. Younger infants were at greater risk for this condition. 36 infants were given either placebo or simethicone, and of these, infants who received simethicone were comfortable earlier and required fewer rescue medications compared with placebo. There were no differences in ability to tolerate oral fluids prior to discharge or in the length of stay in the PACU.
Simethicone is a safe and inexpensive medication that may provide anesthesiologists with an effective treatment choice for suspected postoperative abdominal discomfort in infants.
Since dimethicone may be employed to improve gastrointestinal tolerability of non steroidal anti-inflammatory drugs (NSAIDs), we studied its influence on the pharmacokinetics of ketoprofen in subjects receiving a single oral dose of racemic ketoprofen.
In a cross-over experimental design, 12 healthy fasting volunteers were given a single oral dose (100 mg) of racemic ketoprofen, administered with or without dimethicone. The kinetic parameters measured were area under the concentration (AUC), maximum peak plasma concentration (Cmax), time to reach peak concentration (tmax), elimination half-life (t1/2), mean residence time (MRT) and urinary excretion for R and S enantiomers.
Dimethicone reduced the peak concentration of both R and S ketoprofen by about 10% (P<0.05) and also induced a slight but non-significant increase in the mean time to achieve peak concentration. However, this treatment had no significant effect on the bioavailability and the elimination of R and S enantiomers, as shown by AUC, t1/2 and MRT values. The absorption patterns were equivalent for both ketoprofen isomers, since plasma pharmacokinetic parameters were similar. Nevertheless, the urinary recovery was significantly lower for R ketoprofen than for its antipode. The administration of dimethicone did not alter this stereoselectivity.
The administration of dimethicone to alleviate the epigastralgic effects related to NSAIDs does not affect the efficacy of the treatment. Dimethicone did not significantly alter the bioavailability of ketoprofen, chosen as an example of an NSAID, especially that of the pharmacologically active S enantiomer.
To compare the efficacy of simethicone with cisapride in patients with functional (non-ulcer) dyspepsia.
After standardized diagnostic work-up and at least 6-days wash-out of medication, 177 patients with functional dyspepsia were enrolled; 173 of them (age 19-71 years) were randomized and treated using a double-dummy technique with simethicone (84 mg t.d.s.) or cisapride (10 mg t.d.s.). At baseline and after 2 and 4 weeks, the intensity of the symptoms was scored from 0 (absent) to 3 (severe) using a standardized symptom questionnaire. Efficacy of the treatment was judged by the patients as 'very good', 'good', 'moderate' or 'no effect'.
A total of 166 patients completed the trial. After 2 and 4 weeks, 34% and 46% (respectively), of the patients treated with simethicone judged the improvement in symptoms to be excellent compared to 13% and 22% (respectively) of patients treated with cisapride (P < 0.01). After 2 weeks the difference in the improvement in the global symptom score was significantly better (Delta30.7%, P < 0.001) for simethicone than for cisapride, while this difference failed statistical significance after 4 weeks (Delta10.2%, P=0.11).
In patients with functional dyspepsia, simethicone relieves symptoms during the first 2 weeks of treatment significantly better than cisapride.
This study was designed to show the benefits of filling echography probes with water mixed with dimethicone to preclude artifacts caused by bubbles.
One hundred consecutive healthy volunteers (42 males; mean age, 46 years; range, 17-72 years) were blindly randomized to undergo rectal ultrasonography using conventional degassed water or degassed aqueous solution made of 40 ml of water and 10 ml of dimethicone emulsion (1 ml/100 mg). All examinations performed by the same surgeon-unaware of nature of filler liquid-for ten minutes, and number of rectal ultrasonographies with artifacts attributable to air bubbles was recorded.
Endoluminal ultrasonography performed with conventional degassed water presented artifacts attributed to presence of air bubbles in 30 of 50 examinations (60 percent). When degassed aqueous solution was used, only 5 of 50 examinations showed artifacts caused by presence of air bubbles (10 percent). This difference was statistically significant (P < 0.0005). The use of conventional fluid was associated with artifacts secondary to the presence of air bubbles, adjusted odds ratio 13.5 (95 percent confidence interval, 4.56-39.88). During this experience, the solution did not damage ultrasound scanner.
We found that use of a dimethicone-degassed water mixture is simple, not expensive, safe, effective, and may reduce frequency of sonographic distortion in presence of air bubbles.
Nothing by mouth (NPO) is the standard treatment for small-bowel obstruction. Whether oral medications should be prohibited during treatment of adhesive, partial small-bowel obstruction is unclear. The goal of this study was to determine whether a combination of specific oral medications in adhesive, partial small-bowel obstruction will decrease the need for operative intervention.
Of 266 consecutive adult patients with partial small-bowel obstruction admitted at a tertiary medical center, 236 were randomized into 2 groups. Group I patients were treated with intravenous hydration, nasogastric tube decompression, and NPO. Group II patients were placed on intravenous hydration, nasogastric tube decompression, and oral fluids incorporating an oral laxative, a digestant, and a defoaming agent. We compared differences between the groups in (1) the number of patients having a successful nonoperative treatment, (2) complications, and (3) recurrence of symptoms.
A total of 116 and 120 patients comprised groups I and II, respectively. The number of patients treated successfully by a nonoperative approach was less in group I than in group II (77% vs 90%, P < .01). The complications and recurrence rate for groups I and II did not differ (4% vs 5% and 5% vs 4%, respectively).
The NPO status for patients with adhesive, partial small-bowel obstruction may not be necessary. This cocktail of oral medications can decrease the need for operative intervention in patients with presumed adhesive, partial small-bowel obstruction.
To compare efficacy and tolerability of a loperamide/simethicone (LOP/SIM) combination product with that of loperamide (LOP) alone, simethicone (SIM) alone, and placebo (PBO) for acute nonspecific diarrhea with gas-related abdominal discomfort.
In this multicenter, double-blind, 48-h study, patients were randomly assigned to receive two tablets, each containing either LOP/SIM 2 mg/125 mg (n = 121), LOP 2 mg (n = 120), SIM 125 mg (n = 123), or PBO (n = 121), followed by one tablet after each unformed stool, up to four tablets in any 24-h period. The primary outcome measures were time to last unformed stool and time to complete relief of gas-related abdominal discomfort. For time to last unformed stool, an unformed stool after a 24-h period of formed stools or no stools was considered a continuance of the original episode (stricter definition) or a new episode (alternate definition).
A total of 483 patients were included in the intent-to-treat analysis. The median time to last unformed stool for LOP/SIM (7.6 h) was significantly shorter than that of LOP (11.5 h), SIM (26.0 h), and PBO (29.4 h) (p < or = 0.0232 in comparison with survival curves) using the alternate definition; it was numerically but not significantly shorter than that of LOP (p = 0.0709) and significantly shorter than that of SIM and PBO (p = 0.0001) using the stricter definition. LOP/SIM-treated patients had a shorter time to complete relief of gas-related abdominal discomfort than patients who received either ingredient alone or placebo (all p = 0.0001). Few patients reported adverse events in the four treatment groups, none of which were serious in nature. Potential study limitations include the ability to generalize study results to the population at large, variability in total dose consumed, and subjectivity of patient diary data.
LOP/SIM was well-tolerated and more efficacious than LOP alone, SIM alone, or placebo for acute nonspecific diarrhea and gas-related abdominal discomfort.