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Medicines, Volume 11, Issue 8 (December 2024) – 4 articles

Cover Story (view full-size image): Medicines (ISSN 2305-6320) is an international, peer-reviewed, and open-access journal aimed at disseminating cutting-edge research in the field of drug discovery and clinical application. This journal welcomes manuscripts covering a wide range of aspects, including the search for target molecules (e.g., receptors), specificity, side effects, hormesis (bimodal actions), emergence of resistance during long-term administration, potentiation by combinational treatment with more than two drugs, and factors that modify its pharmacological actions (such as sex differences, aging, environmental factors, and physiological fluids). Our aim is to encourage scientists to publish their experimental and theoretical results in as much detail as possible. Full details must be provided when publishing an experiment so that the results can be reproduced.
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1 pages, 154 KiB  
Retraction
RETRACTED: Zulfiqar et al. Obesity and Frailty Syndrome in the Elderly: Prospective Study in Primary Care. Medicines 2022, 9, 38
by Abrar-Ahmad Zulfiqar, Perla Habchi and Ibrahima Amadou Dembele
Medicines 2024, 11(8), 22; https://doi.org/10.3390/medicines11080022 - 18 Dec 2024
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Abstract
The journal retracts the article titled “Obesity and Frailty Syndrome in the Elderly: Prospective Study in Primary Care” [...] Full article
9 pages, 195 KiB  
Article
Utility of Aprepitant in the Management of Pediatric Patients with Cyclical Vomiting Syndrome
by Aravind Thavamani, Sindhoosha Malay, Jasmine Khatana, Sujithra Velayuthan and Senthilkumar Sankararaman
Medicines 2024, 11(8), 21; https://doi.org/10.3390/medicines11080021 - 11 Dec 2024
Viewed by 653
Abstract
Introduction: Cyclical vomiting syndrome (CVS) is a recurrent debilitating illness characterized by intense episodes of nausea and emesis with widely varied pharmacological management across the country. Aprepitant is now increasingly used in patients with CVS. The impact of aprepitant as an abortive [...] Read more.
Introduction: Cyclical vomiting syndrome (CVS) is a recurrent debilitating illness characterized by intense episodes of nausea and emesis with widely varied pharmacological management across the country. Aprepitant is now increasingly used in patients with CVS. The impact of aprepitant as an abortive therapy in the readmission of pediatric patients with CVS is currently unknown. Methodology: We analyzed all pediatric patients with a primary diagnosis of CVS using the ICD-10 code in the Pediatric Health Information System database of the Children’s Hospital Association. We evaluated the demographic data, comorbid conditions, and management details during the inpatient stay. CVS patients who received aprepitant during their inpatient hospitalization were compared with patients without aprepitant use. Seven-day readmission rate for CVS was used as the outcome variable to assess the effectiveness of the aprepitant in aborting an episode. Propensity score matching was used to match the two cohorts. Results: We analyzed 1775 patients of which 96 received aprepitant during the inpatient hospitalization. The aprepitant group had a more severe hospitalization course as evidenced by an increased duration of hospital stay (5 vs. 3 days) and total hospitalization costs ($11,790 vs. $6380). There were no significant differences in the 7-day (17% vs. 16%, p = 0.91) readmission rate and results were not altered by propensity score matching. Conclusions: Aprepitant use as an abortive therapy did not affect the 7-day CVS-related readmission rate. Further prospective studies are needed to explore the role of aprepitant as an abortive agent in the management of CVS in the pediatric population. Full article
14 pages, 370 KiB  
Review
Safety Implications of Off-Label Medication Use in Athletes: A Narrative Review
by Vítor Silva, Ricardo Madeira, João Joaquim and Cristiano Matos
Medicines 2024, 11(8), 20; https://doi.org/10.3390/medicines11080020 - 15 Nov 2024
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Abstract
In recent years, the off-label use of medications in sports has increased significantly, primarily driven by psychological and social factors. Athletes frequently misuse drugs without adequate medical supervision, relying on unreliable sources of information, which leads to improper usage and serious health risks. [...] Read more.
In recent years, the off-label use of medications in sports has increased significantly, primarily driven by psychological and social factors. Athletes frequently misuse drugs without adequate medical supervision, relying on unreliable sources of information, which leads to improper usage and serious health risks. This narrative review analyzes literature from PubMed® (Medline), Scopus®, and Web of Science® databases, focusing on studies up to December 2023, to examine the safety concerns related to off-label drug use in sports. The review presents an overview of the off-label use of pharmacological substances by athletes, focusing on both hormonal and non-hormonal drugs. Hormonal substances such as anabolic steroids and growth hormones, and non-hormonal agents like diuretics and β2-agonists, are frequently abused. These practices are associated with severe side effects, including infections, cardiovascular complications, hormonal imbalances, psychological disorders, dependence, and even cases of death. The study emphasizes the need for stronger regulation, public awareness initiatives, and preventive strategies to mitigate the health risks associated with this growing trend. Full article
12 pages, 2693 KiB  
Article
Does Ortho-Substitution Enhance Cytotoxic Potencies in a Series of 3,5-Bis(benzylidene)-4-piperidones?
by Subhas S. Karki, Umashankar Das, Jan Balzarini, Erik De Clercq, Hiroshi Sakagami, Yoshihiro Uesawa, Praveen K. Roayapalley and Jonathan R. Dimmock
Medicines 2024, 11(8), 19; https://doi.org/10.3390/medicines11080019 - 30 Oct 2024
Viewed by 1137
Abstract
Background: A series of 3,5-benzylidene-4-piperidones, 1an, were prepared to evaluate the hypothesis that the placement of different groups in the ortho-location of the aryl rings led to compounds with greater cytotoxic potencies than structural analogs. Methods: The bioevaluation of 1a [...] Read more.
Background: A series of 3,5-benzylidene-4-piperidones, 1an, were prepared to evaluate the hypothesis that the placement of different groups in the ortho-location of the aryl rings led to compounds with greater cytotoxic potencies than structural analogs. Methods: The bioevaluation of 1an was undertaken using human Molt/4C8 and CEM cells as well as murine L1210 cells. Correlations were sought between the interplanar angles θA and θB and the cytotoxic potencies. A QSAR analysis was also undertaken. In order to evaluate whether these compounds demonstrated greater toxicity to neoplasms than non-malignant cells, 1an were evaluated against HSC-2, HSC-3, HSC-4 and HL60 neoplasms as well as non-malignant HGF, HPC and HPLF cells. Results: A positive correlation was noted between the interplanar angle θA of one of the aryl rings and the adjacent olefinic linkage with IC50 values in the Molt4/C8 screens. The QSAR analysis revealed a positive correlation between the Hansch pi (π) value of the aryl substituents and the IC50 values of the compounds towards the Molt4/C8 and CEM cells. The dienones in series 1 demonstrated higher tumor-selective toxicity towards HSC-2, HSC-3, HSC-4 and HL-60 neoplasms than HGF, HPC and HPLF cells. Conclusions: The bioevaluations revealed some support for greater cytotoxic potencies to be displayed by compounds having ortho-substituents. Full article
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