REVIEW ON CLINICALLY DEVELOPING ANTIBIOTICS

The world is running out of antibiotics. Between 1940 and 1962, more than 20 new classes of antibiotics were marketed. Since then, only two new classes of antibiotics were marketed. Now, not enough analogues are reaching the market to stem the tide of antibiotic resistance, particularly among gram-negative bacteria which indicates the need of novel antibiotics for their effective action. This review describes those antibiotics in late-stage clinical development. Most of them belong to existing antibiotic classes and a few with a narrow spectrum of activity are novel compounds directed against novel targets. The reasons for some of the past failures to find new molecules and a path forward to help attract investments to fund the discovery of new antibiotics are described

Electronic structure investigations of 1-amino-2,6-dimethylpiperidine by NMR spectral studies by ab initio and DFT calculations

In this work, a combined experimental and theoretical study on molecular structure, vibrational spectra of 1-amino-2,6-dimethylpiperidine (ADP) has been reported. The FTIR and FT-Raman spectrum have been recorded in the region 4000-400 cm-1 and 3500-50 cm-1, respectively. The molecular geometry, harmonic vibrational frequencies and bonding features of ADP have been calculated by using ab initio/HF and density functional theory/B3LYP methods with 6-31+G(d,p) basis set. A detailed interpretation of the FTIR, FT-Raman, NMR spectra of ADP has also been reported. Natural bond orbital analysis has been carried out to explain the charge transfer or delocalization of charge due to the intra-molecular interactions. Energy of the highest occupied molecular (HOMO) orbital and lowest unoccupied (LUMO) molecular orbital have been predicted

A PROSPECTIVE STUDY OF DRUG–DRUG INTERACTIONS AND ADVERSE DRUG REACTIONS AMONG STROKE PATIENTS IN A TERTIARY CARE HOSPITAL

ABSTRACTObjective: Our study attempts to get an insight into the drug–drug interactions (DDIs) and adverse drug reactions (ADRs) among stroke patients fromthe Neurology Department in a private hospital.Methods: In a prospective study spanning 6 months (May to October 2015), we have analyzed the prescription data of 221 patients with bothischemic and hemorrhagic stroke. Gender, age, social habits, length of stay, drug utilization pattern, DDIs reported from the database and clinicallyobserved, and ADRs of individual drugs were observed among the patients. Of 221 cases, 208 (94.11%) were ischemic, 12 (5.43%) were hemorrhagic,and 1 (0.45%) was transient ischemic attack.Results: A number of 140 patients were males and 80 were females. The mean age of the patients was between 41 and 70 years. In ischemic patients,357 major, 282 moderate, and 38 mild DDIs were reported using a specific database, while in hemorrhagic patients, 10 major, 7 moderate, and 1 mildinteraction were reported using a specific database. 18 DDIs were observed clinically and confirmed with evidence. 8 DDI-induced ADRs and 10 ADRscaused by individual drugs were observed in our study population. 18 DDIs were observed clinically and confirmed with evidence. 8 DDI-inducedADRs and 10 ADRs caused by individual drugs were observed in our study population.Conclusion: Drugs if wrongly prescribed may cause negative outcomes and pose significant challenge to health-care providers and may contribute tomorbidity and mortality. Clinical pharmacist can play an important role in identifying and resolving drug-related problems through pharmaceuticalcare practices.Keywords: Stroke, Drug–drug interactions, Adverse drug reactions, Clinical pharmacist

A PROSPECTIVE STUDY OF CLINICAL PROFILE OF STROKE IN A TERTIARY CARE HOSPITAL

ABSTRACTObjective: The objective of the work was to study the clinical profile of stroke in a tertiary care hospital.Methods: A prospective observational study on stroke was carried out for a period of 6-month (May 2015 to October 2015). A total of 241 inpatientsfrom Shri Preethi Hospital were incorporated in the study. The data were collected and evaluated by reviewing case files and patient interview.Result and Conclusion: Out of 241 patients, an incidence of ischemic stroke was found to be higher. The occurrence of stroke steeply rises with agewith male predominance. The burden of stroke tends to be more in rural, illiterate, and low socioeconomic status population. The study reveals riskfactors such as sedentary lifestyle, previous and family history of stroke, underlying disease like hypertension, diabetes. The circadian pattern in onsetshowed a significant peak in morning (6 am-12 pm) for Ischemic and afternoon (12 pm-6 pm) for hemorrhagic stroke. Topographic distribution ofcerebral infract and hemorrhage was found to be in parietal lobe and periventricular white matter, respectively. Mostly prescribed medication forischemic and hemorrhagic patients was antihypertensive and mannitol, respectively. The contraindication for thrombolytic therapy was found to below economic status and average delay in time of presentation to hospital. The study highlights the need for aggressive management of traditionalrisk factors, need for extensive work up in patient to find etiologies and need for more active interventions in community for the prevention of stroke.Keywords: Ischemic, Hemorrhagic, Circadian pattern, Antihypertensive

FORMULATION AND OPTIMIZATION OF PIOGLITAZONE SOLID DISPERSIONS PREPARED BY HOT MELT EXTRUSION TECHNIQUE

The main objective of the present study was to develop a novel and stable pioglitazone loaded solid dispersions with enhanced solubility and dissolution rate. Different drug-to-carrier ratios were prepared by employing hot melt extrusion technique. These formulations were characterized for solid state properties by differential scanning calorimetry, X-ray powder diffraction and FT-IR spectral studies. Formulations were further evaluated for dissolution and stability studies. The aqueous solubility of pioglitazone, in present formulation was improved by the presence of both the polymers. Solid-state characterization indicated pioglitazone was present as amorphous material in formulation with Soluplus and polyethylene glycol, due to efficient entrapment in polymer matrix. The diffraction patterns of solid dispersion indicated the amorphous nature of pioglitazone in solid dispersions. The dissolution rate of all the solid dispersions was found to be rapid when compared to pure pioglitazone. Pioglitazone in pure form has very slow dissolution rate, when compared with the solid dispersions. Thus the solid dispersion prepared with Soluplus and polyethylene glycol would be useful for delivering poorly soluble pioglitazone with enhanced solubility and dissolution rate.Key words: pioglitazone, soluplus, solid dispersions, melt extrusion technique

Leprosy post-exposure prophylaxis with single-dose rifampicin

_Objective:_ Leprosy post-exposure prophylaxis with single-dose rifampicin (SDRPEP) has proven effective and feasible, and is recommended by WHO since 2018. This SDR-PEP toolkit was developed through the experience of the leprosy postexposure prophylaxis (LPEP) programme. It has been designed to facilitate and standardise the implementation of contact tracing and SDR-PEP administration in regions and countries that start the intervention. _Results:_ Four tools were developed, incorporating the current evidence for SDRPEP and the methods and learnings from the LPEP project in eight countries. (1) th

A CRITICAL REVIEW ON HYPOTHESIS, PATHOPHYSIOLOGY OF SCHIZOPHRENIA, AND ROLE OF VITAMINS IN ITS MANAGEMENT

This review describes about the literatures addressing the role of vitamin supplementation in schizophrenia. Evidence is suggesting that vitamin supplementation includes Vitamin A, Vitamin D, Vitamin E, Vitamin B complex, and Vitamin C may be important in treatment. In schizophrenia, patients may have increased level of homocysteine (Hcy), due to the polymorphism in methylenetetrahydrofolate reductase and hypofunction of N-methyl-D-aspartate receptors. The vitamins main effects are reduced the Hcy level and maintain dopamine and serotonin levels. Add-on treatment with high-dose B vitamins including B6, B9, and B12 and also Vitamin D can significantly reduce symptoms of schizophrenia more than standard treatments alone

Menopause Induced Depression, Anxiety, Quality of Life, Lack of Sleep in Women: An Overview

Background: Menopause occurs between the ages of 40 and 50, and marks the end of a woman's menstrual cycle. A period of time during which a woman does not have a monthly cycle for more than 12 months is known as post-menopause. Women may suffer challenges in their daily lives during this period, such as depression, anxiety, and sleep loss, all of which can have a negative impact on their quality of life. A decrease in hormone production, such as estrogen and progesterone, can cause menopause. To treat psychological difficulties in menopausal women, drugs such as vortioxetine and paroxetine, as well as selective serotonin reuptake inhibitors (SSRI) and anti-depressants, were advised. Objective: To evaluate the effects in women how menopause inducing depression, anxiety, quality of life and lack of sleep. Methodology: The recent studies related to the aim of the review were undertaken through a literature search to evaluate the effects in women how menopause inducing depression, anxiety, quality of life and lack of sleep. Conclusion: Menopause, post-menopause, and peri-menopause are age-related causes in women who are going through the menstrual cycle. There is no need for medication during this time, but in severe cases, medications such as selective serotonin reuptake inhibitors (SSRI) and antidepressants should be administered and also for vaginal dryness and irritation Ospemifene is suggested. Many more clinical researches on the benefits of menopausal compilations will be needed in the future. Keywords: Menopause, post- menopause, depression, estrogen, progesteron

How does Heparan Sulfate and COVID-19 Work?: An Overview

Globally, the severe acute respiratory syndrome coronavirus-2 (SARS-CoV-2) had infected over 3 million individuals and claimed many lives producing a global epidemic that necessitates the rapid development of therapeutic solutions. The ideal technique for quickly deploying well-characterized medicines against novel infections is known as drug repurposing. Several repurposable medicines are currently being tested to see if they may be used to treat COVID-19. Heparin, which is commonly utilized to reduce thrombotic events associated with COVID-19-induced disease, is one such promising drug. Heparansulphate is prevalently expressed in mammalian tissues. CoV-2 requires the helping cofactor heparansulphate (HS) on the cell surface: knocking down genes related in HS formation or treating cells with an HS mimic both prevent spike-mediated viral entrance. Heparin/HS binds directly to spike and promotes viral entrance by facilitating the attachment of spike-bearing viral particles to the cell surface. As documented with cell surface-bound heparansulphate, heparin binding to the open conformation of the spike structurally supports the state and may enhance ACE2 binding. Thus, heparansulphate could potentially be utilised to prevent SARS-CoV-2 transmission, based on available datas also consumption of heparansulphate during SARS-CoV-2 cellular entrance may play a role in the thrombotic events associated with COVID-19 infection. Furthermore, this study provides the findings on the mechanism(s) by which heparansulphate could slow the progression of SARS-CoV-2 infection. Keywords: COVID-19, HeparanSulphate, Spike Protien

The New Outlook of Monoclonal Antibodies in Neutralizing Target Cells in COVID-19

Background: The deadly arrival of novel coronavirus (COVID-19) in late December 2019, caused by the Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2) has emerged worldwide causing a pandemic. The World Health Organization (WHO) has proved ineffectiveness against existing medications this influenced the prompt identification of Monoclonal antibodies (mAbs) which plays a vital role as the prophylactic application that helps in developing new interventions. Objectives: To study the effect of mAbs in high-risk individuals in treating COVID-19. Methodology: The recent studies related to the aim of the review were undertaken through a literature search to analyze the importance of mAbs in combating SARS-CoV-2. Results:  In several countries even though vaccines have reached the Emergency Use Authorization (EUA) people still rely on traditional medications. Besides repurposed drugs, recently many mAbs targeting S-protein of SARS-CoV-2 have been signed up for clinical trials. Currently, no specific neutralizing mAbs have been reported for SARS-CoV-2 and it may take several years for such antibodies to be readily available. The development of mAbs for preventing the SARS-CoV 2 infection is challenged by the threat of antibody-dependent enhancement, antibody-resistant against SARS-CoV-2 variants, acute respiratory infections, clinical trials and risk assessment, and inexplicable. The clinical trial data proved that there is no life-threatening Adverse Drug Reactions (ADR) occurred during mAbs therapy for COVID-19 patients. Conclusion: Establishing monoclonal antibodies will continue to be the best prophylactic application as it minimizes the risk of hospitalization in the high-risk individuals affected by SARS-CoV-2 infection. Keywords: COVID-19, Monoclonal antibodies (mAbs), Emergency Use Authorization (EUA), Severe Acute Respiratory Syndrome coronavirus 2 (SARS-CoV-2