Editorial (Thematic Issue: Topic on The Role of Drug Transport and Pharmacokinetics in Drug Efficacy and Safety Part 1)

2015 ◽  
Vol 16 (9) ◽  
pp. 730-731
Author(s):  
Changxiao Liu ◽  
Xin He
Keyword(s):  
Drug Transport ◽  
Drug Efficacy ◽  
Thematic Issue ◽  
Efficacy And Safety

scholarly journals Predicting drug-metagenome interactions: Variation in the microbial β-glucuronidase level in the human gut metagenomes

PLoS ONE ◽  
2021 ◽  
Vol 16 (1) ◽  
pp. e0244876
Author(s):  
Moamen M. Elmassry ◽  
Sunghwan Kim ◽  
Ben Busby
Keyword(s):  
Drug Response ◽  
Drug Efficacy ◽  
Metagenomic Data ◽  
Efficacy And Safety ◽  
Human Gut ◽  
Microbial Enzymes ◽  
Sequence Read Archive ◽  
Structural Analogues ◽  
Gut Metagenome

Characterizing the gut microbiota in terms of their capacity to interfere with drug metabolism is necessary to achieve drug efficacy and safety. Although examples of drug-microbiome interactions are well-documented, little has been reported about a computational pipeline for systematically identifying and characterizing bacterial enzymes that process particular classes of drugs. The goal of our study is to develop a computational approach that compiles drugs whose metabolism may be influenced by a particular class of microbial enzymes and that quantifies the variability in the collective level of those enzymes among individuals. The present paper describes this approach, with microbial β-glucuronidases as an example, which break down drug-glucuronide conjugates and reactivate the drugs or their metabolites. We identified 100 medications that may be metabolized by β-glucuronidases from the gut microbiome. These medications included morphine, estrogen, ibuprofen, midazolam, and their structural analogues. The analysis of metagenomic data available through the Sequence Read Archive (SRA) showed that the level of β-glucuronidase in the gut metagenomes was higher in males than in females, which provides a potential explanation for the sex-based differences in efficacy and toxicity for several drugs, reported in previous studies. Our analysis also showed that infant gut metagenomes at birth and 12 months of age have higher levels of β-glucuronidase than the metagenomes of their mothers and the implication of this observed variability was discussed in the context of breastfeeding as well as infant hyperbilirubinemia. Overall, despite important limitations discussed in this paper, our analysis provided useful insights on the role of the human gut metagenome in the variability in drug response among individuals. Importantly, this approach exploits drug and metagenome data available in public databases as well as open-source cheminformatics and bioinformatics tools to predict drug-metagenome interactions.

The Position of ADME Predictions in Multi-Objective QSAR

2021 ◽  
Vol 6 (1) ◽  
pp. 1-8
Author(s):  
Anna Tsantili-Kakoulidou
Keyword(s):  
Drug Efficacy ◽  
Clinical Development ◽  
Efficacy And Safety ◽  
Huge Amount ◽  
Multi Objective ◽  
Drug Candidates ◽  
Drug Molecules ◽  
Qsar Models ◽  
Adme Properties ◽  
Single Objective

ADME properties and toxicity predictions play an essential role in prioritization and optimization of drug molecules. According to recent statistics, drug efficacy and safety are principal reasons for drug failure. In this perspective, the position of ADME predictions in the evolution of traditional QSAR from the single objective of biological activity to a multi-task concept is discussed. The essential features of ADME and toxicity QSAR models are highlighted. Since such models are applied to prioritize existing or virtual project compounds with already established or predicted target affinity, a mechanistic interpretation, although desirable, is not a primary goal. However, a broad applicability domain is crucial. A future challenge with multi-objective QSAR is to adapt to the realm of big data by integrating techniques for the exploitation of the continuously increasing number of ADME data and the huge amount of clinical development endpoints for the sake of efficacy and safety of new drug candidates.

Editorial (Thematic Issue: Understanding the Role of Heteroreceptor Complexes in the Central Nervous System)

2014 ◽  
Vol 15 (7) ◽  
pp. 647-647 ◽  
Author(s):  
Kjell Fuxe ◽  
Dasiel Borroto-Escuela ◽  
Gilberto Fisone ◽  
Luigi Agnati ◽  
Sergio Tanganelli
Keyword(s):  
Central Nervous System ◽  
Nervous System ◽  
Thematic Issue ◽  
Heteroreceptor Complexes ◽  
The Central Nervous System

Social and Regulatory Consequences of Misleading Medical Information

1976 ◽  
Vol 6 (1) ◽  
pp. 50-55
Author(s):  
Arthur Ruskin
Keyword(s):  
Scientific Method ◽  
Medical Information ◽  
Drug Information ◽  
Medical Profession ◽  
Drug Efficacy ◽  
Efficacy And Safety

Arguing that the scientific method must be the ultimate test in determining drug efficacy and safety, Dr. Ruskin points out that the medical profession is often plagued by unscientific attitudes and “research.” Like their patients, physicians are influenced by nonscientific sources of drug information such as advertising and often trust their own “experience” rather than the results of controlled clinical and epidemiologic trials.

Cetirizine versus diphenhydramine in the prevention of chemotherapy-related hypersensitivity reactions

2018 ◽  
Vol 25 (6) ◽  
pp. 1396-1401 ◽  
Author(s):  
Charis G Durham ◽  
Deepthi Thotakura ◽  
Lauren Sager ◽  
Jennifer Foster ◽  
Jon D Herrington
Keyword(s):  
Blood Pressure ◽  
Heart Rate ◽  
Retrospective Study ◽  
Prospective Studies ◽  
Clinical Setting ◽  
Hypersensitivity Reactions ◽  
Efficacy And Safety ◽  
Infusion Reactions

Objective This study evaluated the role of cetirizine compared to diphenhydramine as premedications for patients receiving paclitaxel, cetuximab, and rituximab infusions. Historically, diphenhydramine has been linked with more sedation in comparison to cetirizine; however, it is unknown if cetirizine can replace diphenhydramine in the prevention of hypersensitivity reactions in patients receiving chemotherapy. Methods This is a retrospective study designed to assess infusion reactions occurring in patients receiving diphenhydramine or cetirizine premedication for rituximab, paclitaxel, or cetuximab therapies. Infusion reactions were defined as various symptoms such as flushing, itching, alterations in heart rate and blood pressure, and dyspnea plus the clinical setting of a concurrent or very recent infusion. Results A total of 207 patients were evaluated in this study with 83 patients receiving cetirizine and 124 diphenhydramine patients. Overall, the percentage of patients with at least one chemotherapy-related infusion event in the cetirizine group was 19.3% (95% CI 11.4–29.4) compared to diphenhydramine group 24.2% (95% CI 17.0–32.7), P = 0.40. Of the patients who received cetirizine and then experienced an event in the first cycle, 41.7% (95% CI 13.7–74.3) of the events were due to paclitaxel, 50.0% (95% CI 19.4–80.6) were due to rituximab, and 8.3% (95% CI 0.1–43.6) were due to cetuximab. Of the patients who received diphenhydramine and then experienced an event in the first cycle, 26.1% (95% CI 5.7–51.4) were due to paclitaxel, 73.9% (95% CI 48.6–94.3) were due to rituximab and none due to cetuximab. Conclusion Cetirizine appears to be a viable substitute for diphenhydramine for the prevention of infusions reactions with cetuximab, paclitaxel, and rituximab infusions in adults. Prospective studies are needed to determine the efficacy and safety of cetirizine compared with diphenhydramine in the prevention of chemotherapy-related infusion reactions.

scholarly journals Role of holter monitoring in the new russian guidelines for arrhythmias and conduction disturbances

2020 ◽  
Vol 27 (3) ◽  
pp. 58-67
Author(s):  
Yu. V. Shubik ◽  
M. M. Medvedev ◽  
M. A. Baturova ◽  
A. E. Rivin
Keyword(s):  
Cardiac Arrhythmias ◽  
Treatment Efficacy ◽  
Safety Monitoring ◽  
Holter Monitoring ◽  
Efficacy And Safety ◽  
Conduction Disturbances ◽  
Diagnostic Approaches ◽  
Management Algorithms

The indications for Holter monitoring, which are included in the new Russian guidelines on cardiac arrhythmias and conduction disturbances, are considered. Possibilities of the diagnostic approaches of arrhythmias, management algorithms and treatment efficacy and safety monitoring are discussed.

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