Promotility Medications – Now and in the Future

Karamanolis, George; Tack, Jan

doi:10.1159/000092883

Cited by 58 publications

(64 citation statements)

References 231 publications

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“…The Rome III working group defined functional dyspepsia as the presence of symptoms thought to originate in the gastroduodenal region, in the absence of any organic, systemic, or metabolic disease that is likely to explain them [Tack et al 2006]. Symptoms should be present for a minimum of 3 months; however, symptoms for greater than 6 months are typical.…”

Section: Functional Dyspepsiamentioning

confidence: 99%

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Review: Evaluation and management of dyspepsia

Harmon

Peura

2010

Therap Adv Gastroenterol

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Dyspepsia is a common clinical problem seen by both primary care physicians and gastroenterologists. Initial evaluation should focus on the identification and treatment of potential causes of symptoms such as gastroesophageal reflux disease (GERD), peptic ulcer disease, and medication side effects but also on recognizing those at risk for more serious conditions such as gastric cancer. This manuscript discusses the evaluation and management of dyspepsia including the role of proton-pump inhibitors, treatment of Helicobacter pylori, and endoscopy. Finally, treatment of refractory functional dyspepsia is addressed.

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Section: Functional Dyspepsiamentioning

confidence: 99%

“…Dyspepsia is defined as having one or more symptoms of epigastric pain, burning, postprandial fullness, or early satiation [Tack et al 2006]. Bloating and nausea often coexist with dyspepsia but are nonspecific and are thus not included in its definition.…”

Section: Introductionmentioning

confidence: 99%

Review: Evaluation and management of dyspepsia

Harmon

Peura

2010

Therap Adv Gastroenterol

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“…Serotonin gilt auch als wichtiger Neurotransmitter im enterischen Nervensystem. In der Humanmedizin existieren mittlerweile verschiedene Therapieansätze zur Behandlung gastrointestinaler Motilitätsstörungen bei denen Serotonin-Agonisten eine Schlüsselrolle spielen (Karamanolis und Tack 2006). Im equinen Darm scheinen bei der Regulation der Motorik vor allem 5-HT3-und 5-HT4-Rezeptoren eine Rolle zu spielen (Weiss et al 2002, Sasaki et al 2005.…”

Section: Kontrolle Durch Das Enterische Nervensystem (Ens) Und Durch unclassified

“…So hat der dopaminerge Antagonist Metoclopramid eine agonistische Wirkung auf 5-HT4-Rezeptoren und kann so lokal die gastrointestinale Motilität steigern (Abb. 2) (Karamanolis und Tack 2006). Die intestinale Motorik kann zum einen durch direkte Beeinflussung der glatten Muskulatur gesteuert werden, zum anderen sind auch die Neurone im myenterischen Plexus ein Angriffspunkt zur Modulation der Muskelaktionen.…”

Section: Kontrolle Durch Das Enterische Nervensystem (Ens) Und Durch unclassified

Characteristics and control of equine intestinal motility

Pfannkuche¹,

Gäbel²

2007

PHK

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ZusammenfassungIm equinen Intestinaltrakt können regionenabhängig spezifische Motilitätsmuster beschrieben werden. Die Kontrolle dieser motorischen Ereignisse erfolgt auf verschiedenen, miteinander verzahnten Ebenen. Der basale Taktgeber für die rhythmischen, wiederkehrenden Kontraktionen der glatten Muskulatur sind die "interstitiellen Zellen nach Cajal" (ICC Characteristics and control of equine intestinal motilityThe equine intestinal tract expresses region-and specific motility patterns. These motoric events are controlled on different levels, with the levels interacting with each other. Basal myogenic rhythm is given by the "interstitial cells of cajal" (ICC). ICCs generate periodic depolarisations of the smooth muscles. If the basic electrical activity of the gut reaches a distinct level, the depolarisations are able to induce contractions. Control of the intestinal activity level is accomplished by hormones and neurones. In this regard, neurones of the enteric nervous system (ENS) located in the myenteric plexus are most relevant. Myenteric neurones influence the smooth muscle by the release of distinct combinations of excitatory and inhibitory neurotransmitters. The mode of action of those neurotransmitters, e.g., acetylcholine, can be imitated, increased or blocked pharmacologically. The release of inhibitory neurotransmitters (e.g., nitric oxide) from enteric neurones is highly relevant for the pathogenesis of motility disturbances. Endogenous opioids also represent neurotransmitters in the ENS. They are able to inhibit propulsive motility patterns. The existence of opioid receptors on enteric neurones has to be taken into account by the application of opioids. The activity of the ENS is centrally modulated by the parasympathetic and sympathetic nervous system. The parasympathetic system increases gastrointestinal motility, whereby the sympathetic system exerts an inhibitory mode. Sympathetic inhibition of motility is important particularly with regard to the pathogenesis of hypomotility.Keywords: Motility, enteric nervous system, gastrointestinal tract, horse, peristalsis Generelle MotilitätsmusterDie Motilitätsmuster des equinen Gastrointestinaltrakts lassen sich sowohl entsprechend ihrer Funktion als auch regionenspezifisch einteilen. In ihrer Funktion dienen die Muster generell drei Zwecken: 1. Durchmischung des Chymus, 2. Weitertransport und 3. Speicherung. Entsprechend der vorrangigen Aufgabe des jeweiligen Abschnittes im Gastrointestinaltrakt sind die Motilitätsmuster in unterschiedlichem Maße ausgeprägt. MagenDer Magen dient primär der Speicherung der aufgenommenen Nahrung. Um dieser Funktion gerecht zu werden, sind im Magen Mechanismen angelegt, die bei Nahrungsaufnahme zur Relaxation der Magenwand führen und somit die Reservoirfunktion ermöglichen (Tack 2006

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“…19 It also acts as a moderate agonist at the serotonergic 5-HT 4 receptor and to a lesser extent on 5-HT 3 receptors. 20,21 The serotonergic (5-HT 4 ) component of Levosulpiride may enhance its therapeutic efficacy in gastrointestinal disorders. 22 This property, together with antagonism at D2 receptors, may contribute to its gastrointestinal prokinetic effect.…”

Section: Introductionmentioning

confidence: 99%

Design, Formulation and In-Vitro Evaluation of Sustained Release Tablet Formulations of Levosulpiride

Samie¹,

Bashir²,

Abbas³

et al. 2018

tjps

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ÖZAmaç: Levosulpirid, çeşitli gastrik bozuklukların tedavisinde yaygın olarak kullanılan bir gastroprokinetik ajandır; bununla birlikte, kısa yarı ömrü ve artan dozlama sıklığı, uyumsuzluk ve olası yan etkilere yol açar. Bu çalışmanın asıl amacı, biyolojik olarak resorbe olabilen selüloz türevlerini içeren Levosulpiridin sürekli salımlı bir formülasyonunu geliştirmektir. Gereç ve Yöntemler: Levosulpiridinin sürekli salım formülasyonları, salım modifiye eden polimerler olarak CMC sodyum, HPC ve HPMC gibi çeşitli selüloz türevlerinin farklı polimer-etkin madde ağırlık oranlarında kullanımıyla direkt basım yoluyla hazırlandı. Daha sonra, toz karışımları ve basılmış tabletler basım öncesi ve basım sonrası değerlendirmeye ve aynı zamanda FTIR analizlerine tabi tutuldu. UV/görünür ışık spektrofotometresi ile 214 nm dalga boyunda pH 6.8 tampon çözeltisinde model etkin maddenin tüm formülasyonları için in vitro salım çalışmaları gerçekleştirildi. Bulgular: FTIR sonuçları, bileşenler arasındaki etkileşimin fiziksel olduğunu ve farklı kinetik model verilerinden, salım profilinin Higuchi modeline en iyi şekilde uyum gösterdiğini doğruladı, çünkü sonuçlar yüksek doğrusallık gösterdi. Sonuçlar ayrıca, geliştirilmiş sürekli salım formülasyonları arasında F9 formülasyonunun ideal olduğunu gösterdi. Sonuç: Salım geciktirici polimer/taşıyıcı olarak CMC sodyum, HPC ve HPMC kullanılarak levosulpirid sürekli salımlı matrisler, başarıyla hazırlandı. Anahtar kelimeler: Levosulpirid, sürekli salım tabletleri, çözünme, uyum, polimerler Objectives: Levosulpiride is a widely used gastroprokinetic agent in the treatment of various gastric disorders; however, its short half-life and increased dosage frequency leads to non-compliance and possible adverse effects. The prime objective of the current study was to develop a sustained-release formulation of Levosulpiride incorporating bioresorbable cellulose derivatives. Materials and Methods: Sustained-release formulations of Levosulpiride were prepared through direct compression using various cellulose derivatives such as CMC sodium, HPC, and HPMC in different polymer-to-drug weight ratios as release-modifying polymers. The powder blends and compressed tablets were then subjected to pre-compressional and post-compressional evaluation, as well as FTIR analysis. In vitro release studies were performed for all formulations of the model drug in buffer solution of pH 6.8 at a wave length of 214 nm by a UV-visible light spectrophotometer. Results:The FTIR results confirmed that the interaction between components was physical, and from the different kinetic models data, the release profile was best expressed by the Higuchi model because the results showed high linearity. The results also showed formulation F9 to be the ideal one among the developed formulations, exhibiting sustained-release behavior. Conclusion: Levosulpiride sustained-release matrices were prepared successfully using CMC sodium, HPC, and HPMC as the release-retarding polymer/carrier.

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Promotility Medications – Now and in the Future

Cited by 58 publications

References 231 publications

Review: Evaluation and management of dyspepsia

Review: Evaluation and management of dyspepsia

Characteristics and control of equine intestinal motility

Design, Formulation and In-Vitro Evaluation of Sustained Release Tablet Formulations of Levosulpiride

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