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Functional Disorders of the Stomach and Duodenum
Published in Kevin W. Olden, Handbook of Functional Gastrointestinal Disorders, 2020
Arienti et al. (40) studied 30 patients treated with the antiemetic agent lev-osulpiride compared to placebo in a randomized double-blind study. Levo-sulpiride affects both the central and peripheral nervous systems. Its effect is exerted at the pre- and postsynaptic DA2 dopaminergic receptors, in both the submucosal and myenteric plexus. Arienti found that levosulpiride reduced dyspeptic symptoms significantly in the dyspeptic group over controls. No correlation was found between gastric emptying of either liquids or solids and dyspeptic symptoms assessed by symptom score. Arienti concluded that levosulpiride offered some benefit to patients with functional dyspepsia. However, the exact mechanism for this benefit remains unclear.
Psychopharmacology in gastrointestinal cohorts
Published in Simon R. Knowles, Laurie Keefer, Antonina A. Mikocka-Walus, Psychogastroenterology for Adults, 2019
Elspeth Carruthers, Julian Stern
Several reviews have concluded that olanzapine is safe and effective for the treatment and prophylaxis of nausea and vomiting, especially in chemotherapy [55]. A small RCT of flupenthixol and melitracen for FD found a significant improvement in global symptoms compared with placebo, and a systematic review of FD treatment found that antipsychotics such as levosulpiride conferred some benefit versus placebo [56, 57]. Quetiapine has also shown some benefit for GI symptoms in severe refractory FGIDs [32].
Development of levosulpiride-loaded solid lipid nanoparticles and their in vitro and in vivo comparison with commercial product
Published in Journal of Microencapsulation, 2020
Nadra Khaleeq, Fakhar-Ud Din, Anam Sajjad Khan, Samreen Rabia, Junaid Dar, Gul Majid Khan
Levosulpiride is a benzamide derived agent, belongs to atypical antipsychotics, mainly prescribed in depression and psychosis (Figure 1(A)). It shows activity by selective blockage of D2 receptors at presynaptic and postsynaptic neuron to inhibit synthesis and release of dopamine (Kim et al.2016, Din and Khan 2017). Levosulpiride effectively relives the symptoms of functional dyspepsia. Likewise, it has been found pharmacologically effective in premature ejaculation. Despite of its high clinical efficacy, levosulpiride is poorly aqueous soluble and less permeable (BCS Class IV drug) which makes it more challenging for the development of oral formulations and attaining optimum bioavailability (Lavania et al.2016). Besides, low pKa of the drug, pharmaceutical excipients used in the preparation of parenteral may cause severe pain and discomfort to the patient (Chitneni et al.2011).
Development and characterisation of levosulpiride-loaded suppositories with improved bioavailability in vivo
Published in Pharmaceutical Development and Technology, 2019
Levosulpiride is a derivative of benzamide group which is potentially used for the treatment of depression and psychiatric problems. It selectively blocks D2 receptors in submucosal and myoenteric plexus (Kim et al. 2016a; Fotaki et al. 2005). Levosulpiride enhances gastric evacuation and digestive signs in patients with functional dyspepsia and diabetic gastroparesis. Moreover, it has been successfully investigated for the treatment of premature ejaculation (Greco et al. 2002; Hussain et al. 2010). Beside all the related efficacy of levosulpiride, its poorly water solubility and low permeability (BCS Class IV drug) is a big challenge in developing various formulations, including oral and injectable formulations, for its therapeutic use (Ibrahim et al. 2013). Furthermore, because of its low pKa, various excipients are required for the development of injectable formulations, which sometimes results in severe pain to the patient leading to discomfort, after injection.