A large number of G-protein-coupled receptors (GPCRs) show varying degrees of basal or constitutive activity. This constitutive activity is usually minimal in natural receptors but is markedly observed in wild type and mutated (naturally or induced) receptors. According to conventional two-state drug receptor interaction model, binding of a ligand may initiate activity (agonist with varying degrees of positive intrinsic activity) or prevent the effect of an agonist (antagonist with zero intrinsic activity). Inverse agonists bind with the constitutively active receptors, stabilize them, and thus reduce the activity (negative intrinsic activity). Receptors of many classes (α-and β-adrenergic, histaminergic, GABAergic, serotoninergic, opiate, and angiotensin receptors) have shown basal activity in suitable in vitro models. Several drugs that have been conventionally classified as antagonists (β-blockers, antihistaminics) have shown inverse agonist effects on corresponding constitutively active receptors. Nearly all H1 and H2 antihistaminics (antagonists) have been shown to be inverse agonists. Among the β-blockers, carvedilol and bucindolol demonstrate low level of inverse agonism as compared to propranolol and nadolol. Several antipsychotic drugs (D2 receptors antagonist), antihypertensive (AT1 receptor antagonists), antiserotoninergic drugs and opioid antagonists have significant inverse agonistic activity that contributes partly or wholly to their therapeutic value. Inverse agonism may also help explain the underlying mechanism of beneficial effects of carvedilol in congestive failure, naloxone-induced withdrawal syndrome in opioid dependence, clozapine in psychosis, and candesartan in cardiac hypertrophy. Understanding inverse agonisms has paved a way for newer drug development. It is now possible to develop agents, which have only desired therapeutic value and are devoid of unwanted adverse effect. Pimavanserin (ACP-103), a highly selective 5-HT2A inverse agonist, attenuates psychosis in patients with Parkinson's disease with psychosis and is devoid of extrapyramidal side effects. This dissociation is also evident from the development of anxioselective benzodiazepines devoid of habit-forming potential. Hemopressin is a peptide ligand that acts as an antagonist as well as inverse agonist. This agent acts as an antinociceptive agent in different in vivo models of pain. Treatment of obesity by drugs having inverse agonist activity at CB1/2 receptors is also underway. An exciting development is evaluation of β-blockers in chronic bronchial asthma—a condition akin to congestive heart failure where β-blockade has become the standard mode of therapy. Synthesis and evaluation of selective agents is underway. Therefore, inverse agonism is an important aspect of drug–receptor interaction and has immense untapped therapeutic potential.
Background: Excessive use of mobile phones, including smart phones, is found to result in various health related, social and psychological problems. Nomophobia expands to ‘No Mobile Phobia’, i.e., fear of being out of mobile phone contact. Previous studies on nomophobia have focused on the student populations, since the younger generation is more technology savvy. This questionnaire-based study aimed to know the prevalence and factors leading to nomophobia in general population.Methods: This study was conducted in western Gujarat from September 2018 to October 2018. A prevalidated questionnaire, containing three parts, the demographic details, details about the characteristics of mobile phone use and the Nomophobia Questionnaire (NMP-Q), was sent through emails and WhatsApp to 1000 individuals. The responses were tabulated and analyzed.Results: Out of 331 respondents 192 (58%) were males and 139 (42%) females. There was no significant difference in average NMP scores with respect to gender (p = 0.401), age brackets (p = 0.135), marital status (p = 0.123) and profession (p = 0.055). However, NMP scores were significantly more in individuals who spent more time on mobile phones per day (p = 0.000), checked their mobile phones more frequently (p<0.000) and in whom phantom ringing syndrome was also present (p<0.000). 241 respondents (72.80%) felt that their mobile phone use was consuming time and affecting their other daily activities.Conclusions: Nomophobia is an emerging health related adverse effect of prolonged mobile phone use. Interventions are required to promote judicious use of mobile phones.
Objectives:The study aims to understand the process and factors influencing the implementation of structured oral examination (SOE) for undergraduate medical students; in comparison with conventional oral examination (COE) in pharmacology.Methods:In a randomized, parallel group study, 123 students of pharmacology were divided into two groups, SOE (n = 63) and COE (n = 60). Students of each group were subdivided into two, and four examiners took viva voce individually. Three sets of questionnaires from autonomic nervous system were prepared, each having 15 items with increasing difficulty levels and were validated by subject experts and pretested. Ten minutes were allotted for each student for each viva. Feedback of students and faculty about the novel method was obtained.Results:SOE yielded significantly lower marks as compared to COE. There were significant inter-examiner variations in marks awarded in SOE and COE. Other factors influencing implementation were difficulty in structuring viva, rigid time limits, lack of flexibility in knowledge content, monotony, and fatigue. The students perceived this format not different from COE but felt that it required in-depth preparation of topic. Faculty opined that SOE led to less drift from main topic and provided uniform coverage of topics in given time.Conclusion:Conducting SOE is a resource-intensive exercise. Despite structuring, inter-examiner variability was not completely eliminated. The students’ performance was depended on factors related to examiners such as teaching experience, vernacular language used, and lack of training. Orientation and training of examiners in assessment strategies is necessary. Standardization of questionnaire is necessary before the implementation of SOE for summative assessment.
Background:Most of the academic teachers use four or five options per item of multiple choice question (MCQ) test as formative and summative assessment. Optimal number of options in MCQ item is a matter of considerable debate among academic teachers of various educational fields. There is a scarcity of the published literature regarding the optimum number of option in each item of MCQ in the field of medical education.Objectives:To compare three options, four options, and five options MCQs test for the quality parameters – reliability, validity, item analysis, distracter analysis, and time analysis.Materials and Methods:Participants were 3rd semester M.B.B.S. students. Students were divided randomly into three groups. Each group was given one set of MCQ test out of three options, four options, and five option randomly. Following the marking of the multiple choice tests, the participants’ option selections were analyzed and comparisons were conducted of the mean marks, mean time, validity, reliability and facility value, discrimination index, point biserial value, distracter analysis of three different option formats.Results:Students score more (P = 0.000) and took less time (P = 0.009) for the completion of three options as compared to four options and five options groups. Facility value was more (P = 0.004) in three options group as compared to four and five options groups. There was no significant difference between three groups for the validity, reliability, and item discrimination. Nonfunctioning distracters were more in the four and five options group as compared to three option group.Conclusion:Assessment based on three option MCQs is can be preferred over four option and five option MCQs.
INTRODUCTIONConventional radiography of the temporal bone (X-Ray mastoid bone) has not kept pace with the progress of modern otology and for this reason many otologists have felt that radiography of the temporal bone is of little value in CSOM. The diagnosis may be made entirely on clinical grounds and many surgeons feel that with experience and careful techniques the extent and nature of the pathology can be determined during the course of surgical exploration without prior information being required.The advent of HRCT has made a significant impact on the surgical management of individuals with middle ear disease. It confirms and expands upon the otoscopic findings, resolves clinical doubts, and in many circumstances plays a significant role in determining surgical technique when surgery is necessary. The surgical approach can be planned on the basis of HRCT findings.1 However, routine HRCT scanning prior to ABSTRACT Background: High Resolution Computed Tomography (HRCT) has widely replaced conventional techniques (X-Ray Mastoid bone) for temporal bone imaging. The most significant use of computed tomography lies in evaluation of cases of Chronic Suppurative Otitis Media (CSOM). The objective of the study was to evaluate the usefulness of HRCT scanning of temporal bone in defining the extent and severity of disease in patients with CSOM, thereby altering the surgical plan and outcome. Methods: This prospective study was conducted at a tertiary care hospital in Ahmedabad. After obtaining approval from IEC (Institutional Ethical Committee), study was carried out on 50 patients diagnosed with CSOM of atticoantral type. Written informed consent of all patients was taken before enrollment in the study. HRCT scan findings were reviewed and correlated with per-operative findings. Results: Out of total 50 patients of CSOM, 26 (52%) were males. Majority of the patients (70%) were in the age group of 11 to 30 years. Left ear was involved in 40% of the patients. Majority of the patients (80%) presented with chief complaint of otorrhoea. In the present study, External Auditory Canal (EAC) was seen normal in majority of patients (82%) both radio logically and per operatively. HRCT scan was found to be very sensitive (96%) in diagnosing cholesteatoma. The sensitivity of HRCT for diagnosing disease in epitympanum, antrum and aditus was found to be 100%, 97% and 88% respectively. CT scans diagnosed erosion of malleus with 100% sensitivity and specificity and erosion of incus with 91% sensitivity and 100% specificity. Conclusions: HRCT was helpful in determining the anatomy of the middle ear and mastoid, and accurately predicted the extent of the disease process of CSOM.
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