Antispasmodic Drugs Research Articles

An Efficient Synthesis of Anti-spasmodic Drug Mebeverine Hydrochloride

An efficient synthetic process for an antispasmodic drug and active pharmaceutical ingredient of Mebeverine hydrochloride 1 is reported in this communication. It is used for stomach cramps and irritable bowel syndrome (IBS). The treatment for irritable bowel syndrome involves lot of drugs like (Dicyclomine hydrochloride, Linaclotide.etc) available in market, but Mebeverine hydrochloride (1) is most effective than any other drug. Earlier manufacturing 1 process reported yield < 46% and used high volumes of reagents and expensive catalyst. We developed new commercial process for 1 with economically, environmentally favored conditions. Proposed synthetic route contains three stages with overall yield of 77% and Purity by HPLC NLT 99.7%.

Dicyclomine-Induced Esophagitis Dissecans Superficialis

Abstract Introduction/Objective Esophagitis dissecans superficialis (EDS) is a rare benign condition of the esophagus, characterized by desquamation of superficial epithelium of the esophageal lining. Etiology is uncertain, considered idiopathic in most cases. EDS can be associated with medications, hot beverages, chemical irritants, celiac disease and skin bullous disorders. It has a predilection for the distal and/or middle esophagus. Methods/Case Report We report a case of a 25-year-old otherwise healthy female with mild gastrointestinal symptoms over 3 years. Her symptoms had worsened over a period of 2-3 weeks, and she complained of lower abdominal cramping associated with constipation. No rectal bleeding or melena was reported. Labs including complete blood count and comprehensive metabolic panel were within normal range values. A presumptive diagnosis of irritable bowel syndrome was made by gastroenterologist. Antispasmodic drug, Dicyclomine 10 mg capsule (a blue capsule), was prescribed. After 4 weeks, a scheduled esophagogastroduodenoscopy revealed patchy plaque-like mucosal changes, characterized by blue discoloration, in the upper third of esophagus. Microscopically, biopsy showed strips of squamous mucosa with a thick layer of parakeratosis, basal cell hyperplasia and foci of minimal inflammation. There were multiple transverse splits at different levels in the parakeratotic layer. A pathologic diagnosis of EDS was established. A further clinical investigation demonstrated that the patient was swallowing medication without water. Results (if a Case Study enter NA) NA Conclusion In conclusion, we present the first case of Dicyclomine-Induced EDS secondary to an irritant effect of waterless medication ingestion. Recognition of this rare entity and clinical correlation are important as it can pose a diagnostic challenge to pathologists and clinicians.

Hyoscine butylbromide in pain reduction associated with ultrasound-guided manual vacuum aspiration: a randomized placebo-controlled trial

Research questionWhat is the effect of adding an anti-spasmodic drug to an existing ultrasound-guided manual vacuum aspiration (USG-MVA) protocol to alleviate immediate post-procedure abdominal cramping pain in women treated for early pregnancy loss? DesignDouble-blind, placebo-controlled, randomized controlled trial conducted between February 2018 and January 2020. Participants were assigned to receive a 1-ml intravenous injection containing 20-mg hyoscine butylbromide (HBB) (n=55) or saline (n =56) as a control immediately before USG-MVA. Primary outcome was reduced abdominal pain after adding a 20-mg dose of HBB to the current pain control regimen. Secondary outcomes were vaginal pain, complications and side-effects, women's pre- and post-procedure psychological state, physiological stress (saliva alpha-amylase) and procedure pain control satisfaction. Two-way mixed ANOVA was used to evaluate the main effects and interactions. ResultsVAS abdominal pain scores in the HBB group were 16% lower immediately after and 21% lower 2 h after surgery (not statistically significant). Two-way ANOVA indicated that time (F[1108] = 83.41, P < 0.001) was the only significant main effect for reduced abdominal pain after the procedure and vaginal pain score (F[1108] = 180.1, P < 0.0001) but not drug received. No adverse events were reported. No significant difference was found for psychological state, physiological stress and procedure pain control satisfaction between the two groups. ConclusionsAnti-spasmodic drugs can help to reduce abdominal cramping pain associated with USG-MVA; HBB produced an insignificant decrease in abdominal pain score. Further studies with longer acting or larger doses of anti-spasmodic drugs are warranted.

The biliary continuum: an up-to-date look at biliary tract diseases

In the structure of gastrointestinal diseases, the pathology of the hepatobiliary system currently ranks second in frequency of occurrence. The stages of diseases of the biliary system can be combined into the so-called “biliary continuum”, when one patient has a consistent development of pathogenetically related diseases of the biliary tract. The progressive course of functional motility disorders of the biliary tract gradually leads to the development of organic pathology, including chronic cholecystitis, the subsequent development of gallstone disease and possible postcholecystectomy complications. Among the diseases of the biliary system, one of the most frequently used diagnoses is chronic cholecystitis. The development of chronic cholecystitis is associated with repeated attacks of acute inflammation or prolonged irritation of large gallstones. The clinical aspects of chronic cholecystitis and other pathologies included in the the «biliary continuum» largely depends on concomitant dyskinesia. There are several directions for the treatment of pathologies of the biliary system: diet therapy, medication, endoscopic and surgical treatment. According to the latest guidelines, the most important direction in modern therapy of diseases of the biliary system is the restoration of the motility of the biliary tract and the normalization of the physicochemical properties of bile. The central place in the treatment of diseases of the “biliary continuum” is given to antispasmodic drugs. The administration of antispasmodics is recommended in order to relieve biliary pain and dyspeptic symptoms caused by spasm of smooth muscles, as well as to control the inflammatory process due to a decrease in the release of pro-inflammatory substances. This article describes in detail the importance of the recovery of the biliary tract motor activity and the improvement of the physico-chemical properties of bile acids.

The effect of Hyoscine Butylbromide on the rate of vaginal delivery in cases of secondary arrest of cervical dilatation: A rondomized controlled clinical trial

Abstract Background For decades, health providers have worked to manage labor actively and safely, with the goal of shortening the duration of painful labor. Reduction of cesarean sections and maternal complication is also an important aspect of labor management. Antispasmodic are commonly administrating during labor in both developing and developed countries, although there is a paucity of scientific reports validating this. Hyoscine butylbromide is an effective antispasmodic drug. Therefore, We aim to assess efficacy of Hyoscine butylbromide on rate of vaginal delivery in cases of 2ry arrest of cervical dilatation. Objective To assess whether the intravenous injection of hyoscine butylbromide is effective in progress of labor in which cases with 2ry arrest of cervical dilatation. Patients and Methods The study included 100 pregnant women (PG, P1, P2, P3) conducted at Ain Shams University Maternity Hospital, the inclusion Criteria were: term uncomplicated singleton pregnancy in a spontaneous active labor, with cephalic presentation. The patient must be free from any medical disorder associated with pregnancy and free from any obstetric complication. Cases were subdivided into 2 groups: Study group: 50 patients received 40mg iv Hyoscine Butylbromide (as Buscopan 20mg\mrl) when the cervix &amp;gt;4cm dilated and was &amp;gt;50% effaced. Control group: 50 patients received 2ml saline as placebo. Results Significant increase in vaginal delivery rate (72%) in Hyoscine group; compared to Saline group (52%); with significant statistical difference (p = 0.04). Highly significant decrease in 1st and 2nd stage labor time in Hyoscine group; compared to Saline group; with highly significant statistical difference (p &amp;lt; 0.05 respectively). These results observed without significant difference as regards 3rd stage labor time and postpartum hemorrhage (p &amp;gt; 0.05), APGAR score and NICU admission (p &amp;gt; 0.05). Conclusion From the current study we can conclude that HBB 40 mg is safe and effective in increasing vaginal delivary rate in cases of 2ry arrest of 12 dilatation. It is effective in decreasing first and second stage of labor. It has no maternal or neonatal adverse effect. It is easy and available.

Visible-light photoredox-catalyzed selective carboxylation of C(sp3)−F bonds with CO2

Visible-light photoredox-catalyzed selective carboxylation of C(sp3)−F bonds with CO2

Drugs that reduce the motility of the gastrointestinal tract

Spastic reactions of smooth muscles of visceral organs play an important role in the pathogenesis of many diseases, the main drugs for relief of which are antispasmodic drugs. The article describes in detail the mechanisms of development of spastic abdominal pain and possible ways to correct it. The mechanisms of influence of the main myotropic antispasmodics on the gastrointestinal tract are given. Particular attention is paid to the peculiarities of pharmacodynamics, pharmacokinetics, listed indications, contraindications, features of drug interaction.

INTERVENTIONS FOR THE TREATMENT OF IRRITABLE BOWEL SYNDROME: A REVIEW OF COCHRANE SYSTEMATIC REVIEWS.

Irritable bowel syndrome (IBS) is a complex gastrointestinal disorder, whose understanding is relatively uncertain, and the treatment guidance decision still represents a challenge. To identify and critically appraise systematic reviews (SRs) published in the Cochrane Database of SRs (CDSR) on the effects of interventions (pharmacological and non-pharmacological) for the treatment of IBS. The search was conducted at the Cochrane Library in May 2020. The methodological quality of the SRs was evaluated by the AMSTAR-2 tool. Eight SRs with moderate to high quality were included, which addressed the treatments: (a) pharmacological: volume agents, antispasmodics, antidepressants and tegaserod; and (b) non-pharmacological: homeopathy, acupuncture, phytotherapy, biofeedback, psychological interventions and hypnotherapy. The results were favorable to antispasmodic drugs and antidepressants regarding the improvement of clinical symptoms. There was no difference between volume agents or tegaserod when compared to placebo. Acupuncture and homeopathy showed a little improvement in symptoms compared to placebo, but the certainty of this evidence was considered low to very low. Psychological interventions seem to improve the overall assessment of the patient and relief symptoms such as abdominal pain. However, there was no long-term follow-up of these patients. The results of the other treatments were considered uncertain due to the high risk of bias. Considering the low quality of the studies included in the SRs, pharmacological treatment with antispasmodics and antidepressants seems to be beneficial for patients with IBS. Among non-pharmacological interventions, psychological interventions seem to be beneficial. However, further clinical trials are recommended with greater methodological rigor to prove these findings.

Graphite Studded with Facile-Synthesized Cu2O Nanoparticle-Based Cubes as a Novel Electrochemical Sensor for Highly Sensitive Voltametric Determination of Mebeverine Hydrochloride

Herein, a feasible chemical reduction method followed by intensive mixing was applied for the preparation of an attractive material based on graphite studded with cuprous oxide nanoparticle-based cubes (Cu2ONPs–C@G). Transmission electron microscope (TEM), scanning electron microscope (SEM), X-ray diffraction (XRD) and cyclic voltammetry (CV) were utilized for characterization. Cuprous oxide nanoparticles (Cu2ONPs), with a diameter range mainly distributed from 4 to 20 nm, aggregate to form microcubes (Cu2ONPs–C) with an average diameter of about 367 nm. Paste electrode was prepared using Cu2ONPs–C@G (Cu2ONPs–C@G/PE) for voltametric quantification of the musculotropic antispasmodic drug: mebeverine hydrochloride (MEB). The electrochemical behavior of MEB was studied using CV, and the optimum analytical parameters were investigated using square wave adsorptive anodic stripping voltammetry (SWAdASV). Moreover, density functional theory (DFT) was used to emphasize the ability of MEB to form a complex with Cu2+, confirming the suggested electrochemical behavior of MEB at Cu2ONPs–C@G/PE. With good stability and high reproducibility, SWAdASV of Cu2ONPs–C@G/PE shows successful quantification of MEB over the concentration range of 5.00 × 10−11–1.10 × 10−9 M with lower limit of detection (LOD) and lower limit of quantification (LOQ) values of 2.41 × 10−11 M and 8.05 × 10−11 M, respectively. Finally, accurate quantification of MEB in dosage forms (tablets) and biological fluids (spiked human urine and plasma samples) was achieved using Cu2ONPs-C@G/PE.

Is inguinal hernia repair safe for testicular atrophy? Our 10 year results

Background: We aimed to determine the incidence and predictors of testicular atrophy (TA) in patients undergoing inguinal hernia repair at our hospital.Methods: The total patient number is 578.The patients were divided Group-1 (developed testicular atrophy) and Group-2 (did not develop testicular atrophy). The testicles were evaluated with Scrotal Color Doppler Ultrasonography (SCDU) in preoperative and postoperative third month.Results: Median age in the Group - 1 and Group - 2 respectively is 64,0±12,3 (47-81) and 48,9±17,4 (18-89) (p=0.037). TA developed in 5.01% (29/578) of the patients. We determined that TA developed more often in the patients who are over the age of 40 (p=0.007), in secondary cases (p&lt;0.001), in open repair (p&lt;0.001), those who do not use perioperative narcotic and Nonsteroidal Anti-Inflammatory Drugs (NSAIDs) (p&lt;0.001), those who use perioperative antispasmodic drugs (p=0.017), those having a rheumatic disease(RD) and diabetes mellitus(DM) (p&lt;0.001).Results of multivariate analysis, testicular atrophy development increases when perioperative NSAID is not used ( OR:13.24; 95% CI:4.19-41.87; p&lt;0.001) , perioperative narcotic is not applied (OR:13.91; 95% CI:4.35-44.55; p&lt;0.001) and RD exists (OR:0.10; 95%CI:0.03-0.35; p&lt;0.001).Conclusions: Advanced age, DM and rheumatic disease, not using perioperative NSAIDs, narcotic drugs and antispasmodic drugs increases the risk of testicular atrophy.

Repositioning antispasmodic drug Papaverine for the treatment of chronic myeloid leukemia.

Papaverine is a benzylisoquinoline alkaloid from the plant Papaver somniferum (Opium poppy). It is approved as an antispasmodic drug by the US FDA and is also reported to have anti-cancer properties. Here, Papaverine's activity in chronic myeloid leukemia (CML) is explored using Saccharomyces cerevisiae, mammalian cancer cell lines, and in silico studies. The sensitivity of wild-type and mutant (anti-oxidant defense, apoptosis) strains of S. cerevisiaeto the drug Papaverine was tested by colony formation, spot assays, and AO/EB staining. In vitro cytotoxic effect was investigated on HCT15 (colon), A549 (lung), HeLa (cervical), and K562 (Bcr-Abl positive CML), and RAW 264.7 cell lines; cell cycle, mitochondrial membrane potential, ROS detection analyzed in K562 cells using flow cytometry and apoptotic markers, Bcr-Abl signaling pathways examined by western blotting. Molecular docking and molecular dynamics simulation of Papaverine against the target Bcr-Abl were also carried out. Investigation in S. cerevisiae evidenced Papaverine induces ROS-mediated apoptosis. Subsequent in vitro examination showed that CML cell line K562 was more sensitive to the drug Papaverine. Papaverine induces ROS generation, promotes apoptosis, and inhibits Bcr-Abl downstream signaling. Papaverine acts synergistically with the drug Imatinib. Furthermore, the docking and molecular dynamic simulation studies supported that Papaverine binds to the allosteric site of Bcr-Abl. The data presented here have added support to the concept of polypharmacology of existing drugs and natural compounds to interact with more than one target. This study provides a proof-of-concept for repositioning Papaverine as an anti-CML drug.

Фармакология спазмолитических средств, применяемых в терапии синдрома раздраженного кишечника

Objective of the Review: To describe and compare some pharmacodynamic and pharmacokinetic parameters of antispasmodic drugs used in complex management of irritable bowel syndrome (IBS) in the Russian Federation. Key Points. IBS is a chronic recurrent disease associated with abdominal pain and bowel disorders. The key factors of IBS pathogenesis include intestinal motility disorders and visceral hypersensitivity. Both processes are controlled by endocrine and neural systems. In a target cell, voltage-operated calcium channels mediate neuronal signals for unstriped muscles to contract and for glands to start secreting. Antispasmodic drugs are a group of products that have been used for IBS management for decades. The review describes contemporary idea of molecular mechanisms to control contraction of GIT muscle cells and a comparison of antispasmodic drugs used in complex therapy of IBS in the Russian Federation. Their key pharmacodynamic and pharmacokinetic characteristics are discussed. Conclusion. The fundamental difference of mebeverine (Duspatalin) is its ability to normalise bowel motility in patients with IBS without the need in complete motility suppression. Also, its inability to block muscarinic receptors and stimulate opioid receptors is another advantage in improving the quality of life of patients. Keywords: pharmacodynamics, pharmacokinetics, antispasmodic drugs, therapy of irritable bowel syndrome, mebeverine.

Possibilities of carboxytherapy for diseases of the cardiovascular system

The aim of the study was to analyze the mechanisms of action and pharmacodynamics of carboxytherapy in diseases of the cardiovascular system (CVS). Materials and methods. An analysis of domestic and foreign experience in the use of carboxytherapy for diseases of CVS. Results and discussions. The mechanism of action of carboxytherapy is based on the principle of the introduction of carbon dioxide (CO2) in the patient's body, due to which many pathological disorders can be eliminated. Inhalation and non-inhalation introduction of CO2 into the body has been used for medicinal purposes for many decades. The empirical (off label) use of this therapy in course of time has gained a wide clinical evidence base. There is a large amount of clinical evidence in the world of the effective use of carboxytherapy in many fields of medicine, including those with CVS diseases. It is proved that CO2 introduced into the body penetrates freely through cell membranes and has antihypoxic, vasodilating, antioxidant, anti-ischemic, antispasmodic and other positive effects. Therefore, carboxytherapy contributes to a complex of pharmacological effects inherent of traditional antianginal, hypotensive, antispasmodic and other drugs that are widely used in the treatment of CVS diseases. Conclusions. An analysis of domestic and foreign experience in carboxytherapy shows that the effects of CO2 in diseases of the CVS are achieved by improving oxygenation and microcirculation, anti-anginal, anti-inflammatory, antihypertensive, antispasmodic, anti-oxidant, and analgesic effects of this gas. Carboxytherapy is an alternative, promising and safe method of treating diseases of the cardiovascular system.

Outcomes of a Swallowable Intragastric Balloon (Elipse™) on 96 Overweight and Obese Patients.

The traditional gastric balloons have been used for several years to reduce weight in overweight and obese patients, but the need for sedation and upper endoscopy leading to several limitations. The current series is the first study that evaluates the safety and effectiveness of the swallowable gastric (Elipse™) balloon in our population on the national level. Ninety-six patients (mean BMI was 33.6 ± 4.3kg/m2) participated in this study. All patients swallowed one Elipse™ balloon intended to remain in the stomach for 4months, self-empty, and then pass. Each balloon was filled with 550mL of filling fluid. Anti-emetics and anti-spasmodic drugs were prescribed for 2-3days after insertion; proton pump inhibitor was prescribed twice daily 1week before the procedure and continued until the end of residence time (16-20weeks). In the current series, at end of the procedure (after 4months), the overall mean weight loss (WL) was 11.2 ± 5.1kg, mean waist circumference reduction was 10.9 ± 2.1cm, and a mean BMI reduction was 4.9 ± 2.0kg/m2. The percentage of total body weight loss (TBWL%) was 12.1 ± 5.2%. The Elipse™ therapy reported improvements in the metabolic parameters investigated. This swallowable gastric balloon (Elipse™) can be safely and successfully swallowed, filled, imaged, and passed with accepted weight loss and clinical improvement in factors related to the metabolic syndrome.

Evaluation of the efficacy of Latakaranja as Antispasmodic Drug in Kastaartava - A Randomised Clinical Control Trial

Kastaartava (Dysmenorrohea) is a greek word, describes about painful menstruation which the Pratyatmaka Lakhshans of various Yonivyapad that are Vatala Yonivyapad, Udavartini Yonivyapad, Paripluta Yonivyapad, Mahayoni and Vataja Artava Dusti that affects 75% of adolscents, 25-50% of adult women and 5-20% having dysmenorrhea. It is a common reason for losing time at school or work or visiting family doctor. Morbid Vatadosha especially Apanavata is a causative factor of Kastaartava. Vatahara properties are beneficial considering the morbidity and complications that are caused by Kastaaratava, mentioned above herbal preparation has been tried here. This research work is randomized control clinical study with Pre-test and Post-test design. 40 patients suffering from Kastaaratava (Dysmenorrohoea) were selected randomly for study. The selected patients were divided into 2 groups, 20 patients each. The selected 20 patients in Group A (Trial group) were administered Latakaranja Beeja Churna orally. The selected 20 patients in Group B (Controlled group) were administered Rajapravartini Vati. The duration of treatment was for 03 days of menstruation for 2 menstrual cycles and followup for the next menstrual cycle. After the completion of the clinical trial, it was found that in Rajapravartini Vati, there was highly significant result in Cramping pain in abdomen, Irritability, Tenderness in Breast, Back pain and Headache, where as Latakaranja Beeja Choorna there is also significant result in Cramping pain in Abdomen, Irritability, Tenderness in Breast, Back Pain, Headache and Vomiting but statistically considering average mean Latakaranja Choorna shows comparatively lesser effective than Rajapravartini Vati. By the statistical results it can be concluded that Rajapravartini Vati has better result when compared to Latakaranja Choorna in the present study.

Apendagite epiploica: um diagnóstico diferencial: relato de caso

Objetivo: Descrever um caso de apendagite epiploica em paciente atendido na Clínica Gastromed, enfatizando os aspectos clínicos, propedêuticos e o tratamento adotado. Metodologia: Trata-se de um estudo retrospectivo que irá abordar o caso de paciente com apendagite epiploica, utilizando para isso o prontuário do paciente em questão. Será realizada durante todo período de estudo consultas a literatura disponível e pertinente ao assunto, tais como: artigos científicos, livros, revistas, etc. Resultados: Paciente masculino, 38 anos, procura atendimento em 20/05/2019 com queixa de diarreia, febre não aferida e mialgia. Ao exame do abdomem, desconforto a palpação superficial e profunda em fossa ilíaca esquerda, não apresentando dor à descompressão brusca, sem outras alterações. A tomografia computadorizada de abdomem inferior revelou estrutura ovoide com densidade de gordura, com a dimensão de 1,5 x 0,8 cm, com a região central hiperdensa, na porção antimesentérica do colón, sugerindo apendagite epiploica incipiente, no colón esquerdo. Foi submetido a acompanhamento domiciliar com antiinflamatório não esteroidal e antiespasmódico, com evolução favorável. Conclusão: Nas condições que foram realizados o presente estudo podemos concluir que apendagite epiplóica é uma condição clínica incomum que inclui em seu diagnóstico diferencial diversas patologias cujo tratamento é cirúrgico ilustrando a importância do raciocínio clínico adequado.

The efficacy of the submucosal injection of lidocaine during endoscopic submucosal dissection for colorectal neoplasms: a multicenter randomized controlled study

BackgroundEndoscopic submucosal dissection (ESD) is currently a common procedure although it requires a long procedural time. We conducted a prospective study to determine the efficacy and safety of lidocaine injection for shortening the procedural time and relieving bowel peristalsis during ESD.MethodsA multicenter randomized controlled study was conducted in three hospitals. Ninety-one patients who underwent colorectal ESD were enrolled. Patients were randomly divided into two groups using the envelope method: the lidocaine group and saline group. The primary endpoint was the procedural time, and the secondary endpoints were the procedural time in each part of the colon and the grade of bowel peristalsis and the incidence and amounts of antispasmodic drugs use and adverse events.ResultsThe patients’ demographics were not markedly different between the two groups. The mean procedural time in the lidocaine group was not markedly different from that in the saline group. In contrast, at the proximal site, the procedural time in the lidocaine group (57 min) was significantly shorter in the saline group (80 min). The grade of bowel peristalsis in the lidocaine group (0.67) was significantly lower than in the saline group (1.17). Antispasmodic drug use was significantly rarer in the lidocaine group than in the saline group. The incidence of adverse events was not markedly different between the two groups.ConclusionsLocal lidocaine injection is a feasible option for preventing bowel peristalsis, particularly in the proximal colon, leading to a reduced procedural time for ESD and decreased antispasmodic drug use.University Hospital Medical Information Network Center (UMIN number: 000022843).

Antispasmodic Drug Drofenine as an Inhibitor of Kv2.1 Channel Ameliorates Peripheral Neuropathy in Diabetic Mice.

SummaryDiabetic peripheral neuropathy (DPN) is a common diabetic complication and has yet no efficient medication. Here, we report that antispasmodic drug drofenine (Dfe) blocks Kv2.1 and ameliorates DPN-like pathology in diabetic mice. The underlying mechanisms are investigated against the DPN mice with in vivo Kv2.1 knockdown through adeno associated virus AAV9-Kv2.1-RNAi. Streptozotocin (STZ) induced type 1 or db/db type 2 diabetic mice with DPN exhibited a high level of Kv2.1 protein in dorsal root ganglion (DRG) tissue and a suppressed neurite outgrowth in DRG neuron. Dfe promoted neurite outgrowth by inhibiting Kv2.1 channel and/or Kv2.1 mRNA and protein expression level. Moreover, it suppressed inflammation by repressing IκBα/NF-κB signaling, inhibited apoptosis by regulating Kv2.1-mediated Bcl-2 family proteins and Caspase-3 and ameliorated mitochondrial dysfunction through Kv2.1/CaMKKβ/AMPK/PGC1α pathway. Our work supports that Kv2.1 inhibition is a promisingly therapeutic strategy for DPN and highlights the potential of Dfe in treating this disease.

Novel water-soluble lubricant for the preparation of tiemonium methylsulfate fast-dissolving tablets

The rapid delivery and self-administration of antispasmodics are very essential for the treatment of pain associated with smooth muscle spasms. Tiemonium methylsulfate (TMS) is a well-known antispasmodic drug used in the treatment of muscle spasms of different organs. New oral dissolving tablets (ODTs) of the drug were formulated using l-leucine as a new and highly water-soluble lubricant and evaluated. The obtained tablets were of sufficient mechanical strength and low friability and disintegrated and dissolved rapidly. About 98% of the drug was dissolved in the first 15 min without any solid residues in the buccal cavity. There was no difference observed between the dissolution profiles of pure drug and drug formulated in ODTs. The in vitro antispasmodic effect of TMS was not affected by incorporation of the drug in the tablet form. The obtained results strongly support the development of ODTs containing TMS for rapid and noninvasive treatment of painful smooth muscle spasms.

Pharmacological and Non-pharmacological Treatments of Irritable Bowel Syndrome and Their Impact on the Quality of Life: A Literature Review.

Irritable bowel syndrome (IBS) is a non-organic gastrointestinal disorder that adversely affects the quality of life (QoL). The etiology of the disease is not fully understood, and appropriate treatment is still a matter of debate. Therefore, we feel that a review that describes the different treatment methods of treatment is needed to provide the correct clues. A comprehensive literature search was performed on PubMed, including randomized clinical trials and review articles. We carefully reviewed the different treatment options mentioned in the published research papers and compared their results to address the treatment options for IBS. The current literature review reveals that pharmacological treatments such as antidepressants, vitamin D, probiotics, and antispasmodic drugs and non-pharmacological treatments including cognitive-behavioral therapy (CBT), acupuncture, anise, and diet modification can help control the symptoms of IBS and improve the QoL of patients.