Pharmacognostic screening and antiemetic evaluation of the ethanol extract of the leaves of Morinda lucida benth. (rubiaceae)

Emesis is a common side and adverse effect associated with many illnesses, even drugs. It is the act or process of vomiting. Causes vary from pregnancy, morning sickness, motion sickness, chemotherapy and so on. Emetics are drugs or substances that induce vomiting. Antiemetics are agents given to stop vomiting and to stop the nauseous feeling. Morinda lucida, Benth. family, Rubiacae. It is commonly known as brimstone tree. It is about 24m long, the branches are fibrous in nature and does not break easily, the tree bark is brown to grey, the leaves are green with green fruits. This project is focused on the pharmacognostic evaluation and antiemetic activities of the ethanol extract of the leaves of Morinda lucida. The plants were properly collected and identified by a taxonomist, then, air dried at room temperature, blended using an electric miller. The ethanol leaf extract of the plant was obtained using cold maceration, filtered and concentrated using rotary evaporator. The extract was used for antiemetic evaluations, pharmacognostic and chromatographic (thin layer chromatography) evaluations. The LD50 was determined using Lorkes method. Pharmacognostic evaluation shows the presence of, lignin, cellulose, saponin, tannis, alkaloids flavonoids. The LD50 shows that there was no death recorded. The result of the research shows that the ethanol extract of Morinda lucida on 2 weeks old chickens exhibited antiemetic effect. It can therefore be concluded that the ethanol extract of Morinda lucida possess antiemetic activity as claimed and the result of these findings can be of great importance to the development of new antiemetic drug.

Study of Antiemetic Potential of Ruta graveolens Extracts by Copper Sulphate and Brassica campestris Induced Emesis in Chicks

The antiemetic effect of aqueous and methanolic extracts of R. graveolens in young chicks was investigated. In addition, the phytochemical screening of the test plant and its acute toxicity studies were also conducted. Different doses of the extracts were tested for their antiemetic properties and were compared with the positive control antiemetic drug Chlorpromazine (150 mg/kg), Metoclopramide (50 mg/kg) and an untreated control (normal saline) against copper sulphate and Brassica-induced emesis. The phytochemical screening of R. graveolens showed that it contains certain alkaloids and flavonoids. It was found to be safe up to the dose of 2000 mg/kg body weight. The aqueous extracts in 50 and 150 mg/kg doses produced 41.49% and 66.49% inhibition of emesis, respectively by copper sulphate-induced emesis, while 34.66% and 57.95% inhibition of emesis, respectively by B. campestris-induced emesis. The methanolic extracts of Ruta graveolens in 50 and 150 mg/kg doses produced 46.80% and 70.20% inhibition of emesis, respectively by copper sulphate-induced emesis while 31.95% and 61.94%, respectively in Brassica campestris-induced chick emesis model. These results have suggested R. graveolens possess significant antiemetic properties that implicate its use as traditional medicine to treat emesis. However, further studies are needed to isolate the active principle(s) i.e. flavonoids contained in the plant drug tested and its real safety and efficacy as antiemetic agent.

Tricyclic Pyrazole-Based Compounds as Useful Scaffolds for Cannabinoid CB1/CB2 Receptor Interaction

Cannabinoids comprise different classes of compounds, which aroused interest in recent years because of their several pharmacological properties. Such properties include analgesic activity, bodyweight reduction, the antiemetic effect, the reduction of intraocular pressure and many others, which appear correlated to the affinity of cannabinoids towards CB1 and/or CB2 receptors. Within the search aiming to identify novel chemical scaffolds for cannabinoid receptor interaction, the CB1 antagonist/inverse agonist pyrazole-based derivative rimonabant has been modified, giving rise to several tricyclic pyrazole-based compounds, most of which endowed of high affinity and selectivity for CB1 or CB2 receptors. The aim of this review is to present the synthesis and summarize the SAR study of such tricyclic pyrazole-based compounds, evidencing, for some derivatives, their potential in the treatment of neuropathic pain, obesity or in the management of glaucoma.

Marijuana: A systems-based primer of adverse effects associated with use and an overview of its therapeutic utility

Marijuana use is on the rise in the United States. By the end of 2019, 33 states have legalized marijuana use and marijuana byproduct use for medical purposes. However, marijuana use does not come without side effects. This manuscript reviews the increasing usage of marijuana and the different forms (natural and synthetic) that patients may use when presenting to clinicians. It also addresses the biochemical and behavioral changes observed with marijuana use, including the location and changes associated with cannabinoid receptors (abbreviated CB1 and CB2). These two topics lead into an extensive review of the side effects of marijuana use. This manuscript discusses gastrointestinal side-effects, such as Cannabinoid Hyperemesis Syndrome, pancreatitis, and hepatotoxicity. It also briefly reviews cardiovascular, neurologic, and pulmonary side effects. This article provides an overview of therapeutic effects of marijuana including the antiemetic effect, its medical utility as an appetite stimulant, and usefulness in cancer patients post-chemotherapy. A thorough social history pertaining to marijuana use is an important consideration for clinicians in patients presenting with a variety of symptoms, including those effecting the gastrointestinal, cardiovascular, pulmonary, or neurologic systems.

Antiemetic Effect of Fruit Extracts of Trapa bispinosa Roxb. in Chick Emesis Model

Background: Vomiting and nausea are common symptoms associated with many diseased conditions. They also occur as side effects due to intake of certain medications. Natural remedies are nowadays being considered as a better alternate compared to allopathic medicine. Aim: The current study was designed to evaluate the antiemetic effect of hexane and ethanolic extracts of Trapa bispinosa Roxb fruit. Methodology: The study was conducted on young chicks aged 6-7 days using Copper sulfate (50 mg/kg) for the induction of emesis using oral route. Antiemetic effect was determined by observing the reduction in the number of retches in different groups of chicks. Metoclopramide and Chlorpromazine (150 mg/kg) were used as standard antiemetic agents. Chicks were treated with both extracts (ethanolic and hexane) at the dose of 150 mg/kg. Results: Hexane extract was found to be most effective when compared with all the groups. The results showed that T.bispinos Roxb. hexane extract was able to effectively prevent the copper sulfate induced emesis in chicks. Phytochemical analysis was also performed and it was predicted that the antiemetic effect of hexane extract might be due to the presence of alkaloids and triterpenoids. Conclusion: The positive effects obtained from this study showed that natural remedy might also be used as an alternate to allopathic medicine for nausea and vomiting.

The Prophylactic Effect of Oral Olanzapine on Postoperative Nausea and Vomiting in Laparoscopic Gynecological Surgery: A Randomized Clinical Trial

BackgroundAlthough the antiemetic effect of olanzapine on chemotherapy-induced nausea and vomiting has been characterized, the prophylactic role of olanzapine on postoperative nausea and vomiting (PONV) has not been fully elucidated. This clinical trial aims to examine the effectiveness of olanzapine for preventing PONV.MethodsPatients undergoing laparoscopic gynecological surgery at 5 university hospitals in Japan will be randomly assigned to receive either 5 mg of oral olanzapine or placebo 2 hours before the induction of anesthesia. All patients will receive intravenous dexamethasone at the induction of anesthesia. The primary outcome will be the incidence of postoperative nausea and vomiting within 24 hours after surgery. Secondary endpoints will include longitudinal changes in the incidence of postoperative nausea and vomiting and overall patient satisfaction.DiscussionThis trial will provide a high quality evidence whether olanzapine prevents PONV in gynecological laparoscopy patients at a high risk for PONV.Ethics and disseminationThe trial was approved by the institutional review board of the each participating study site. Study findings will be disseminated through peer-reviewed publications and in conference presentations.Trial registrationUMIN Clinical Trials Registry (UMIN-CTR) ID: 000022634, Registered on October 1, 2016 https://upload.umin.ac.jp/cgi-open-bin/ctr/ctr_view.cgi?recptno=R000026031

The Antiemetic Effect of Xiao-Ban-Xia-Tang Formula is Associated With Regulating CaM/CaMKII/ERK1/2 Signaling Pathway in Cisplatin and 1-phenylbiguanide Hydrochloride Induced Rat Pica Models

Background: Xiao-Ban-Xia-Tang (XBXT) formula is a traditional Chinese herbal formula for treating emesis. Chemotherapy-induced nausea and vomiting (CINV) are serious side effects of chemotherapy, which was closely related to the activation of 5-hydroxytryptamine 3 receptor (5-HT3R). In this paper, the effect of XBXT on cisplatin- and 1-phenylbiguanide hydrochloride (1-PBG, a selective 5-HT3R agonist)- induced pica behavior in male Wistar rats and inhibition of calmodulin/calmodulin-dependent protein kinase II/extracellular signal-regulated kinase 1/2 (CaM/CaMKII/ERK1/2) signaling pathway were investigated. Methods: XBXT (1.6 g/kg, twice daily) was orally administered from day 1 after intraperitoneal injection of cisplatin (6 mg/kg) and 1-PBG (25 mg/kg) to day 3. Pica behavior (consumption of kaolin, a type of clay) was recorded every 24 h. The expression and co-localization of CaM and 5-HT3R in small intestine and brain were detected by immunofluorescence. The expression of CaMKII, pCaMKII, ERK1/2, and pERK1/2 proteins were detected by Western blot. Results: XBXT treatment significantly decreased kaolin ingestion (pica) of rats after treatment of cisplatin and 1-PBG during both 0 - 24 h (respectively, from 1.57 g to 0.87 g; from 1.04 g to 0.11 g) and 0 - 72 h (respectively, from 2.98 g to 1.85 g; from 2.29 g to 0.35 g) periods. The fluorescence expression of CaM and 5-HT3R and expression of CaMKII, pCaMKII, ERK1/2 and pERK1/2 in the small intestine and brain of cisplatin- and 1-PBG-treated rats were remarkably suppressed by XBXT.Conclusions: The present study implies that inhibiting CaM/CaMKII/ERK1/2 signaling is an underlying mechanism of XBXT for treating CINV. These insights provide an experimental basis of XBXT for the clinical treatment of CINV.

Acute peripheral vestibular dysfunction: diagnostics and treatment

The aim of this article is to demonstrate ENT specialists, neurologists and general practitioners how to examine and treat patients with acute vertiginous complaints. Traditional otoneurologic testing that carried out for accurate topic diagnostics of acute vestibular dysfunction is described as available «Vestibular passport». Clinical diagnosis can be achieved after thorough assessment of patient’s complaints as well as history of the present illness. Gaze tests and posture control trials are demonstrated in details. Diagnostic value of each probe is shown from the viewpoint of differential diagnostics of peripheral and central vestibular dysfunction. High diagnostic value of registration and analysis of oculogyric reactions is presented by history cases of acute labyrinthopathy and acute vestibular neuronitis. In these cases absence of saccadic and pursuit gaze disturbances rule out central vestibular system dysfunction. The salient feature of these two variants of peripheral vestibular dysfunction is spontaneous nystagmus that revealed by Frenzel glasses. This significant oculomotor symptom as well as disturbances of static and dynamic postural control confirm patient’s vestibular complaints in objective way. Revelation of decompensation signs of vestibular dysfunction needs urgent medicine vertigo therapy and spare vestibular rehabilitation. Actually, medications of choice are sedative drugs with antiemetic effect, non-loop diuretics and glucocorticoids.

The Antiemetic Effect of Xiao-Ban-Xia-Tang Formula against Cisplatin-Induced Emesis is Mediated through Inhibition of NLRP3 Inflammasome Activation in a Rat Pica Model

Xiao-Ban-Xia-Tang (XBXT), a traditional Chinese medicine formula, has been used for the treatment of emesis for nearly 2000 years, but its underlying mechanism is not yet fully clarified. The purpose of this study is to reveal the antiemetic mechanisms of XBXT by focusing on the NLRP3 inflammasome pathway in a chemotherapy-induced rat pica model. The pica model was generated by a single intraperitoneal injection of cisplatin in this study. Consumption of kaolin (a type of clay) and food and body weight were recorded every 24 hours. Cisplatin-induced increase in kaolin consumption (pica) was used to quantify chemotherapy-induced nausea and vomiting (CINV). Tissue from the ileum and antrum was stained with hematoxylin eosin (HE) to observe pathological changes. The levels of reactive oxygen species (ROS) and inflammatory cytokines, including IL-1β and IL-18 in serum, were detected by ELISA. In addition, changes in the NLRP3 inflammasome activation in the ileum and antrum were investigated using western blot and immunofluorescence microscopy. The results showed that oral administration of XBXT and ondansetron inhibited acute and delayed pica and significantly protected against the gastrointestinal pathological injury induced by cisplatin. The levels of ROS, IL-1β, and IL-18 in the serum of cisplatin-treated rats were also remarkably decreased by XBXT and ondansetron. Moreover, we found that XBXT can inhibit cisplatin-induced NLRP3 inflammasome activation. The present study indicates that the inhibition of the NLRP3 inflammasome activation might be one of the potential mechanisms for the therapeutic effects of XBXT against CINV.