Context: In the emergency department, patients with recent-onset atrial fibrillation are typically managed with intravenous antiarrhythmic agents. However, the currently used agents have a low efficacy and safety profile. Antazoline is an antihistaminic agent that has been shown to have a strong antiarrhythmic effect when administered intravenously, facilitating rapid conversion to normal sinus rhythm. Aims: To systematically review the literature on the safety and efficacy of antazoline in the treatment of recent-onset short-duration atrial fibrillation and to compare the clinical efficacy of antazoline to that of other antiarrhythmic agents listed in clinical guidelines. Methods: The study was written in accordance with the Preferred Reporting Items for Systematic Reviews and Meta-Analyses (PRISMA) protocol. A comprehensive search of databases (PubMed, Scopus, ScienceDirect, Web of Sciences, Google Scholar, Clinical trial.gov) for relevant studies in English from inception to 2021 using keywords involving “antazoline” AND other terms such as “antiarrhythmic”, “atrial fibrillation”, and “arrhythmia”. Results: Of the 478 studies identified, 446 were screened, and 7 were included, one of which was a randomized control trial, and the others were observational studies. The majority of studies indicated that antazoline resulted in rapid cardioversion to sinus rhythm. When compared to other pharmacological cardioversion options, antazoline achieved higher cardioversion rates than amiodarone or propafenone and was generally a safer option. Conclusions: Antazoline appears to be an effective pharmacological agent for the rapid cardioversion of short-term atrial fibrillation. More randomized clinical trials, however, should be conducted to strengthen the evidence.
Objectives Over the past few decades, the accumulation of expired and unused medications in households has become a concern. Most people are unaware of how to properly dispose of unused and/or expired medicines. Our objective was to inspect the extent of expired medications within Arab households in United Arab Emirates (UAE), to determine which therapeutic groups yield greater amounts of unused medications, and evaluate drugs’ disposal practices. Methods This descriptive study was written in accordance with the STROBE (Strengthening the Reporting of Observational Studies in Epidemiology) checklist for cross-sectional studies. It was conducted among Arab households in UAE (n = 503) using an online questionnaire between November 2020 and January 2021. Questions were related to participants’ socio-demographics, the prevalence of expired medications in households and their disposal. Key findings Around 58% of the respondents had expired medications in their houses and 74% had drugs that were never used. The most common medicines left unused were analgesics (34%) followed by cosmetics (27%) and antibiotics (26%). More than 42% of expired medications were in solid dosage forms, 28% were semisolid and 24% were liquid dosage forms. The predominant disposal method among the surveyed participants was throwing medications into the garbage (86%). Conclusions Large quantities of expired medications in Arab households exist with a high prevalence of analgesics, antibiotics and cosmetics. Arab households are unaware of the proper drug disposal procedures. Therefore, community pharmacists are recommended to offer training on proper medication disposal practices and to encourage the public to return medications to pharmacies.
The need for new antibiotics has become a major worldwide challenge as bacterial strains keep developing resistance to the existing drugs at an alarming rate. Enoyl-acyl carrier protein reductases (FabI) play a crucial role in lipids and fatty acid biosynthesis, which are essential for the integrity of the bacterial cell membrane. Our study aimed to discover small FabI inhibitors in continuation to our previously found hit MN02. The process was initially started by conducting a similarity search to the NCI ligand database using MN02 as a query. Accordingly, ten compounds were chosen for the computational assessment and antimicrobial testing. Most of the compounds showed an antibacterial activity against Gram-positive strains, while RK10 exhibited broad-spectrum activity against both Gram-positive and Gram-negative bacteria. All tested compounds were then docked into the saFabI active site followed by 100 ns MD simulations (Molecular Dynamics) and MM-GBSA (Molecular Mechanics with Generalised Born and Surface Area Solvation) calculations in order to understand their fitting and estimate their binding energies. Interestingly, and in line with the experimental data, RK10 was able to exhibit the best fitting with the target catalytic pocket. To sum up, RK10 is a small compound with leadlike characteristics that can indeed act as a promising candidate for the future development of broad-spectrum antibacterial agents.
Despite available treatments, breast cancer is the leading cause of cancer-related death. Knowing that the tyrosine phosphatase SHP2 is a regulator in tumorigenesis, developing inhibitors of SHP2 in breast cells is crucial. Our study investigated the effects of new compounds, purchased from NSC, on the phosphatase activity of SHP2 and the modulation of breast cancer cell lines’ proliferation and viability. A combined ligand-based and structure-based virtual screening protocol was validated, then performed, against SHP2 active site. Top ranked compounds were tested via SHP2 enzymatic assay, followed by measuring IC50 values. Subsequently, hits were tested for their anti-breast cancer viability and proliferative activity. Our experiments identified three compounds 13030, 24198, and 57774 as SHP2 inhibitors, with IC50 values in micromolar levels and considerable selectivity over the analogous enzyme SHP1. Long MD simulations of 500 ns showed a very promising binding mode in the SHP2 catalytic pocket. Furthermore, these compounds significantly reduced MCF-7 breast cancer cells’ proliferation and viability. Interestingly, two of our hits can have acridine or phenoxazine cyclic system known to intercalate in ds DNA. Therefore, our novel approach led to the discovery of SHP2 inhibitors, which could act as a starting point in the future for clinically useful anticancer agents.
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