A study to evaluate the antidiabetic effect of Syzygium cumini Linn. seed extract in high fructose diet induced diabetes in Albino Rats

Background: The objective of the study was to evaluate the antidiabetic effect of syzygium cumini linn. Seed extract in high fructose diet induced diabetes in albino rats.Methods: This study was conducted in two phases. In Phase I acute and chronic effects of three doses of Syzygium cumini Linn 200mg/kg, 400mg/kg and 800mg/kg was seen in euglycaemic rats. In Phase II, the above doses of Syzygium cumini Linn were seen in diabetes induced by high fructose diet was evaluated. 5 groups of 06 animals each. Group I was given normal saline orally. Group II, III and IV were given oral Syzygium extract in the dose of 200mg/kg, 400mg/kg and 800mg/Kg respectively. Group V was given glibenclamide suspension 10 mg/Kg orally. Blood glucose was measured before starting this phase (Day 0), at the end of fructose feeding (day 28) and weekly thereafter up to the end of the treatment period (i.e. on days 35,42,49,56).Results: In phase I of the study, Syzygium extract had no effect on the mean blood glucose levels when given in the doses of 200, 400 and 800 mg/kg, from 1-24 hours. After chronic administration to euglycemic rats for 4 weeks, Syzygium extract also did not produce any significant change in blood glucose levels when given at various doses from 200-800 mg/kg. Treatment with all the three doses of Syzygium cumini extract (200,400 and 800mg/kg) produced a significant reduction in the blood glucose level. (P value <0.001 as compared to group I). The glucose lowering effect started at the end of 1 weeks and it increased till the end of the study in all the groups.Conclusions: Syzygium cumini Linn extract has no effect on the blood glucose levels of euglycemic animals. Syzygium cumini Linn extract can reduce blood glucose levels in high fructose diet induced diabetic rats, in a dose dependent and time dependent manner

Prescription pattern among patients having mild to moderate bronchial asthma using metered dose inhaler and dry powder inhaler in tertiary hospital in western india

Background: Bronchial asthma is a syndrome characterized by airflow obstruction that manifests as shortness of breath, wheezing and cough. The treatment is tailored according to the severity of the disease. The drugs used for treatment of bronchial asthma include inhaled corticosteroids, beta-2 agonists, methylxanthines, leukotriene antagonists and mast cell stabilizers. Despite the availability of all these drugs, which are recommended for the treatment, not every patient achieves complete control of the disease. The reason behind this could be irrational prescribing of drugs for the treatment and errors in the technique of using inhaler devices. Though rational prescribing of drugs and correct technique for the use of inhaler can be improved by proper training of target population, but there is paucity of such data in our country.Methods: This study was planned to monitor prescription pattern and errors in use of inhalation devices, in patients diagnosed as cases of mild to moderate bronchial asthma, attending Out Patient Department (OPD) of respiratory medicine of a tertiary hospital. A total of 207 patients were recruited and their prescription pattern and inhalation technique were assessed.Results: The study showed that inhaled short acting β2-agonists and inhaled corticosteroids were the most commonly used drug groups, which were prescribed to all the patients in the study, followed by long acting β2-agonists, leukotriene antagonists and methylxanthines in decreasing order.Conclusions: As a conclusion, the treating physicians were prescribing according to the laid down guidelines. It is concluded that such studies should be periodically done to ensure the adherence to the treatment guidelines

Tenapanor: new approach to counter irritable bowel syndrome with constipation

Irritable bowel syndrome (IBS) is a functional gastrointestinal disorder chronic in nature and characterized predominantly by abdominal pain or discomfort associated with altered bowel habits, diagnosis requires characteristic symptoms during the last 3 months and onset ≥6 months ago. Symptom-based approaches for functional bloating, constipation and diarrhea are best utilised to identify IBS. IBS with constipation exerts significant impairment on work productivity by hampering quality of life. Inadequate relief by existing modalities, persistent hard stools and visceral abdominal pain demanded further clinical research. Tenanapor a novel molecule acts locally on gastrointestinal sodium/hydrogen exchanger isoform 3 (NHE3), an antiporter a counter transporter and exert antinociceptive effects on visceral sensation thereby decreases the frequency of abdominal pain. Action on NHE3 receptors located on small intestine and colon’s apical surface reduces the absorption of sodium and phosphate, with minimal systemic exposure. NHE3 Inhibition induced sodium absorption results in increase in water secretion into intestinal lumen resultant an accelerated intestinal transit time and softer stool consistency. Most common adverse reactions (≥2%) are diarrhea, abdominal distension, flatulence and dizziness. The drug is metabolised mainly by CYP3A4/5 and excreted in feaces (70%) and urine (7%). Tenapanor’s minimal systemic absorption is likely to be associated with a relatively inert safety and tolerability profile. Based on positive results from the phase III T3MPO trial program, tenapanor demonstrated promising results for IBS-C management and received US Food and Drug Administration approval as IBSRELA @ Ardelyx Pharma in September 2019 and augment existing modalities for management of IBS-C

Amisulpride: tackling postoperative nausea and vomiting not a nightmare any more

Vomiting and nausea remains concern in postoperative patients for anaesthesiologists and surgeons. Patients remain at risk for adverse medical consequences as wound dehiscence, dehydration, electrolyte derangement’s and gastric aspiration. This entity delays discharge and is one of the causes of unanticipated admission after ambulatory surgery. Presently dopamine (D2), serotonin (5-HT3), and histamine (H1) antagonists are widely used prophylactic agents, as is the corticosteroid dexamethasone, but the incidence of postoperative nausea and vomiting (PONV) is still appreciable. Safety concerns as QT interval prolongation has led to nearly phasing out of use of D2-antagonist Droperidol, a potent and most favoured formulation. With minimal studies and randomized studies to back up the efficacy of existing modalities viz 5HT-antagonist, promethazine, metoclopramide and dimenhydrinate for management of postoperative nausea and vomiting, need for evaluation, study and incorporation into formulary for management was always persisting. Amisulpride is an anti-psychotic agent, used routinely in >50 countries worldwide is a potent but atypical D2-antagonist with minimal adverse profile mainly QT interval prolongation, extrapyramidal signs and symptoms, which had plagued out other members of same class. In addition to D2 antagonism this drug exhibits potent antagonist action against D3 receptors, implicated in the emetic response. In pre clinical studies and multiple randomized controlled multicenter studies the effectiveness and safety of low dose intra venous Amisulpride was established and approved as Barhemsys @Acacia Pharma by US Food and drug administration in February 2020. This drug will soon add to protocol-based management of PONV

CHIRAL SWITCH- AN EMERGING STRATEGY IN THERAPEUTICS

During the last decade, drug chirality, more specifically the use of single enantiomers versus racemic mixtures has been in the forefront of discussions in scientific forums.This is because the left and right handed twins of a molecule behave quite differently from each other in a biological environment. This can frequently lead to an improvement in pharmacological and therapeutic profile of the molecule/drug. This understanding of the significance of stereo-chemistry coupled with advances in chemical technologies and further nudged by regulatory requirements has helped the increase in the development of individual isomers at the expense of racemic mixtures.Apart from the development of novel stereo-selective compounds, a number of racemates have been re-evaluated as potential single enantiomer agents with  the possibility of an improved pharmacological/therapeutic profile. These have been termed as Chiral Switches and have resulted in the re-birth of a number of agents as single enantiomers and have provided significant improvements over the racemic drug. Economic considerations are also playing a part with pharmaceutical companies increasingly using chiral switching as a marketing strategy to increase the patent longevity and profitability period of a drug. However, not all these switches have resulted in therapeutic superiority and in many instances, unpredicted adverse reactions have resulted. Before a switch to clinical use of single enantiomers is made, physicians should satisfy themselves from evidence based on well-conducted clinical trials that the chiral switch is cost-effective and improves the outcomes for patients.  KEY WORDS: Chirality, Chiral Switch, Enantiomer

FLIBANSERIN: A Happy Ending Solution to Hypoactive Sexual Desire Disorder

Hypoactive sexual desire disorder (HSDD) is a persistent or recurrent deficiency or absence of sexual desire. It can cause prominent distress and interpersonal difficulty of women. There have been drugs available to treat sexual disorders in men when there is no such drug for women. Nowadays, FDA approved Flibanserin to treat HSDD of premenopausal women. This drug Flibanserin has no novel mechanism of action but the possible mechanism of action is modulating serotonin and dopamine activity in brain parts as balance of these systems is significance for a normal sexual response. Keywords: Hypoactive Sexual Desire Disorder, Premenopausal women, FlibanserinÂ

A method to study the effect of bronchodilators on smoke retention in COPD patients: study protocol for a randomized controlled trial

<p>Abstract</p> <p>Background</p> <p>Chronic obstructive pulmonary disease (COPD) is a common disease, associated with cardiovascular disease. Many patients use (long-acting) bronchodilators, whilst they continue smoking alongside. We hypothesised an interaction between bronchodilators and smoking that enhances smoke exposure, and hence cardiovascular disease. In this paper, we report our study protocol that explores the fundamental interaction, i.e. smoke retention.</p> <p>Method</p> <p>The design consists of a double-blinded, placebo-controlled, randomised crossover trial, in which 40 COPD patients smoke cigarettes during both undilated and maximal bronchodilated conditions. Our primary outcome is the retention of cigarette smoke, expressed as tar and nicotine weight. The inhaled tar weights are calculated from the correlated extracted nicotine weights in cigarette filters, whereas the exhaled weights are collected on Cambridge filters. We established the inhaled weight calculations by a pilot study, that included paired measurements from several smoking regimes. Our study protocol is approved by the local accredited medical review ethics committee.</p> <p>Discussion</p> <p>Our study is currently in progress. The pilot study revealed valid equations for inhaled tar and nicotine, with an R²of 0.82 and 0.74 (p < 0.01), respectively. We developed a method to study pulmonary smoke retentions in COPD patients under the influence of bronchodilation which may affect smoking-related disease. This trial will provide fundamental knowledge about the (cardiovascular) safety of bronchodilators in patients with COPD who persist in their habit of cigarette smoking.</p> <p>Trial registration</p> <p>ClinicalTrials.gov: <a href="http://www.clinicaltrials.gov/ct2/show/NCT00981851">NCT00981851</a></p

Management of chronic obstructive pulmonary disease in India: a systematic review.

OBJECTIVES: Chronic diseases are fast becoming the largest health burden in India. Despite this, their management in India has not been well studied. We aimed to systematically review the nature and efficacy of current management strategies for chronic obstructive pulmonary disease (COPD) in India. METHODS: We used database searches (MEDLINE, EMBASE, IndMED, CENTRAL and CINAHL), journal hand-searches, scanning of reference lists and contact with experts to identify studies for systematic review. We did not review management strategies aimed at chronic diseases more generally, nor management of acute exacerbations. Due to the heterogeneity of reviewed studies, meta-analysis was not appropriate. Thus, narrative methods were used. SETTING: India. PARTICIPANTS: All adult populations resident in India. MAIN OUTCOME MEASURES: 1. Trialled interventions and outcomes 2. Extent and efficacy of current management strategies 3. Above outcomes by subgroup. RESULTS: We found information regarding current management - particularly regarding the implementation of national guidelines and primary prevention - to be minimal. This led to difficulty in interpreting studies of management strategies, which were varied and generally of positive effect. Data regarding current management outcomes were very few. CONCLUSIONS: The current understanding of management strategies for COPD in India is limited due to a lack of published data. Determination of the extent of current use of management guidelines, availability and use of treatment, and current primary prevention strategies would be useful. This would also provide evidence on which to interpret existing and future studies of management outcomes and novel interventions