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Issue Information
(Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - June 22, 2023 Category: Drugs & Pharmacology Tags: ISSUE INFORMATION Source Type: research

Antimicrobial stewardship: Prescribing across the primary care health professions
We examined the patterns of antibiotic prescribing by medical and non-medical prescribers (dentists, nurse practitioners, and midwives) in Australia. We explored trends in the dispensed use of antibiotics (scripts and defined daily dose [DDD] per 1000 population/day) by Australian prescribers over the 12-year period, 2005 –2016. We obtained data on dispensed prescriptions of antibiotics from registered health professionals subsidized on the Pharmaceutical Benefits Scheme (PBS). There were 216.2 million medical and 7.1 million non-medical dispensed prescriptions for antibiotics over 12 years. The top four antibiot ics f...
Source: Pharmacology Research and Perspectives - June 8, 2023 Category: Drugs & Pharmacology Authors: Samantha A. Hollingworth, Treasure McGuire, Mieke Van  Driel, Nelufa Begum, Pauline J. Ford, Glenda Hawley, Laurence J. Walsh Tags: ORIGINAL ARTICLE Source Type: research

CNS4 causes subtype ‐specific changes in agonist efficacy and reversal potential of permeant cations in NMDA receptors
Working hypothesis of CNS4 mechanism of action: Changes in glutamate concentration alter agonist binding domain (ABD) intersubunit interaction, that plays a crucial role in desensitization leading to channel constriction. CNS4 (blue) preferentially reverses the low glutamate (broken heart) induced changes in ABD conformation back to normal glutamate-like ABD conformation facilitating cation influx through the NMDA receptor channel. This will be experimentally evaluated in the future. AbstractThe NMDA subtype of glutamate receptor serves as an attractive drug target for the treatment of disorders evolving from hyper- or hyp...
Source: Pharmacology Research and Perspectives - June 7, 2023 Category: Drugs & Pharmacology Authors: Seth C. Boehringer, Tulia V. Johnston, Lina Cortez Kwapisz, Pamela J. VandeVord, Blaise M. Costa Tags: ORIGINAL ARTICLE Source Type: research

Syringin inhibits endogenous volume regulated anion channel currents of HEK293 cells in hypotonic circumstances
In this study, we found that syringin moderately inhibited VRAC currents in a dose-dependent manner. The potential binding of syringin to LRRC8 protein was predicted through in silico molecular docking, which suggests an affinity of −6.6 kcal/mol and potential binding sites of arginine 103 and leucine 101. Our results herein characterize syringin as an inhibitor of the VRAC channels, which provides valuable insights for the future development of VRAC channel inhibitors. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - June 7, 2023 Category: Drugs & Pharmacology Authors: Ziwei Xu, Wei Yao, Minyan Liang, Song Wang, Longhui Lu, Jingjing Wang, Na Zhu, Liping Huang Tags: ORIGINAL ARTICLE Source Type: research

A phase I, first ‐in‐human study investigating the safety, tolerability, and pharmacokinetics of the maturation inhibitor GSK3739937
We report the safety and pharmacokinetic properties of the HIV-1 maturation inhibitor GSK3739937 (GSK'937) in healthy participants. This was a phase I, first-in-human, double-blind, randomized, placebo-controlled, single- (part 1) and multiple- (part 2) dose escalation study with an additional open-label relative bioavailability and food effect study (part 3). Participants received oral ascending single doses (10 –800 mg) in part 1, up to 18 once-daily 25- to 100-mg or 3 once-weekly 500-mg doses in part 2, and single 100-mg doses as powder-in-bottle or tablet (in fed and fasted states) formulations in part 3. Primary a...
Source: Pharmacology Research and Perspectives - June 3, 2023 Category: Drugs & Pharmacology Authors: Paul D. Benn, Ying Zhang, Lesley Kahl, Thomas J. Greene, Veronica Bainbridge, Cindy Fishman, Bo Wen, Martin Gartland Tags: ORIGINAL ARTICLE Source Type: research

Management of pharmacovigilance during the COVID ‐19 pandemic crisis by the safety department of an academic sponsor: Lessons learnt and challenges from the EU DisCoVeRy clinical trial
Safety and communication data circuit. AbstractThe current COVID-19 pandemic was an exceptional health situation, including for drug use. As there was no known effective drug for COVID-19 at the beginning of the pandemic, different drug candidates were proposed. In this article, we present the challenges for an academic Safety Department to manage the global safety of a European trial during the pandemic. The National Institute for Health and Medical Research (Inserm) conducted a European multicenter, open-label, randomized, controlled trial involving three repurposed and one-in development drugs (lopinavir/ritonavir,IFN- ...
Source: Pharmacology Research and Perspectives - June 3, 2023 Category: Drugs & Pharmacology Authors: No émie Mercier, Drifa Belhadi, Aline DeChanet, Christelle Delmas, Juliette Saillard, Marina Dumousseaux, Soizic Le Mestre, Claire Fougerou‐Leurent, Assia Ferrane, Charles Burdet, Hélène Espérou, Florence Ader, Maya Hites, Nathan Peiff Tags: REVIEW Source Type: research

Oral antibiotics lower mycophenolate mofetil drug exposure, possibly by interfering with the enterohepatic recirculation: A case series
We present three cases in which MPA exposure severely decreased after oral antibiotic coadministration. By diminishing gut bacteria β-glucuronidase activity, oral antibiotics can prevent deglucuronidation of the inactive MPA-7-O-glucuronide metabolite to MPA and thereby possibly prevent its enterohepatic recirculation. This pharmacokinetic interaction could result in rejection, which makes it clinically relevant in solid organ transplant recipients, especially when therapeutic drug monitoring frequency is low. Routine screening for this interaction, preferably supported by clinical decision support systems, and pragmatic ...
Source: Pharmacology Research and Perspectives - May 29, 2023 Category: Drugs & Pharmacology Authors: Mirjam Simoons, Kishan A. T. Naipal, Huib Jong, Caroline M. Hoed, Brenda C. M. Winter, Midas B. Mulder Tags: SHORT REPORT Source Type: research

Impact of a computerized physician order entry system on medication safety in pediatrics —The AVOID study
ConclusionThe implementation of a CPOE system resulted in a reduction of issues regarding medication, particularly MEs with the potential to harm patients decreased significantly. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - May 24, 2023 Category: Drugs & Pharmacology Authors: Stefan Wimmer, Irmgard Toni, Sebastian Botzenhardt, Regina Trollmann, Wolfgang Rascher, Antje Neubert Tags: ORIGINAL ARTICLE Source Type: research

Exploring Australian pharmacists' views toward reducing the risk of medicines ‐related harm in aged care residents
This study aimed to explore Australian pharmacists' views toward reducing the risk of medicines-related harm in older residents. Qualitative, semi-structured interviews were conducted with 15 Pharmacists across Australia providing services (e.g., through the provision of medication reviews, supplying medications, or being an embedded pharmacist) to RACFs identified via convenience sampling. Data were analyzed by thematic analysis using an inductive approach. Medicines-related harm was thought to occur due to polypharmacy, inappropriate medicines, anticholinergic activity, sedative load, and lack of reconciliation of medici...
Source: Pharmacology Research and Perspectives - May 24, 2023 Category: Drugs & Pharmacology Authors: Sheraz Ali, Colin M. Curtain, Gregory M. Peterson, Mohammed S. Salahudeen Tags: ORIGINAL ARTICLE Source Type: research

Effect of a high ‐fat and high‐calorie food on the pharmacokinetics of a novel, potent GABA analog HSK16149 in healthy subjects
This study demonstrated that HSK16149 can be administered with or without food. (Source: Pharmacology Research and Perspectives)
Source: Pharmacology Research and Perspectives - May 20, 2023 Category: Drugs & Pharmacology Authors: Qingqing Wu, Huijuan Zhu, Rong Song, Mengqi Zhang, Fangqiong Li, Weifang Zeng, Wei Wang, Jingying Jia, Chen Yu, Yanmei Liu Tags: ORIGINAL ARTICLE Source Type: research