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Antibiotics Pharmacology

Damini Sood, Neeraj Kumar, Aarushi Singh, Meena Kishore Sakharkar, Vartika Tomar, Ramesh Chandra
Fluoroquinolone (FQ) antibiotics are an important class of synthetic antibacterial agents. These are the most extensively used drugs for treating bacterial infections in the field of both human and veterinary medicine. Herein, the antibacterial and pharmacological properties of four fluoroquinolones: lomefloxacin, norfloxacin, ciprofloxacin, and ofloxacin have been studied. The objective of this study was to analyze the antibacterial characteristics of the different fluoroquinolones. Also, the pharmacological properties of the compounds including the Lipinski rule of five, absorption, distribution, metabolism, and excretion, LD50, drug likeliness, and toxicity were evaluated...
September 2018: Genomics & Informatics
Fatma Boukattaya, Amal Daoud, Fabien Boeda, Morwenna S M Pearson-Long, Neji Gharsallah, Adel Kadri, Philippe Bertus, Houcine Ammar
BACKGROUND: 2-Aminochromene derivatives display important pharmacological properties, including mainly antibiotic and anticancer activities. OBJECTIVE: The study aims to synthesize new chromene derivatives via a new approach using Grignard reagents, for the evaluation of their antibiotic and antifungal properties. METHOD: A series of novel 3-cyano-4-aminochromene derivatives bearing alkyl substituents at the 4-position was prepared for biological evaluation...
October 9, 2018: Medicinal Chemistry
Ernesto Crisafulli, Enric Barbeta, Antonella Ielpo, Antoni Torres
Background: Patients with chronic obstructive pulmonary disease (COPD) may experience an acute worsening of respiratory symptoms that results in additional therapy; this event is defined as a COPD exacerbation (AECOPD). Hospitalization for AECOPD is accompanied by a rapid decline in health status with a high risk of mortality or other negative outcomes such as need for endotracheal intubation or intensive care unit (ICU) admission. Treatments for AECOPD aim to minimize the negative impact of the current exacerbation and to prevent subsequent events, such as relapse or readmission to hospital...
2018: Multidisciplinary Respiratory Medicine
Witold Rongies, Jacek Bojakowski, Lidia Koktysz, Włodzimierz Dolecki, Agnieszka Olga Lewińska, Antoni Krzeski
The patient with bacterial infection sequelae in the form of damage to cranial nerves (CN) III, IV, and VI was followed-up. He had exhibited clinical and radiographic signs of paranasal sinusitis. Prior to his physiotherapy, the patient received standard treatment with natural and synthetic antibiotics and steroids. After acute signs of infection resolved without any functional improvement, the patient was referred to a rehabilitation unit to undergo neuromuscular re-education of the paralyzed extraocular muscles...
October 8, 2018: American Journal of Physical Medicine & Rehabilitation
Wei Wang, Noémie Van Noten, Jeroen Degroote, Agathe Romeo, Pieter Vermeir, Joris Michiels
Zinc oxide (ZnO) supplied at pharmacological dosage in diets of weaned piglets improves growth performance. However, it causes environmental contamination and induces bacterial antibiotic resistance, yet this practice is debated. The effects on gut microbiota and integrity in weaned piglets of conventional ZnO at nutritional and pharmacological dosage (110 and 2,400 mg/kg Zn, respectively) were compared to an alternative ZnO source at 110 and 220 mg/kg Zn. Each of the four treatments was applied to four pens (two piglets/pen; weaning age, 20 days) for 15 days, and piglets were sampled on day 15 to determine indices of gut integrity...
October 8, 2018: Journal of Animal Physiology and Animal Nutrition
Rosario Cuomo, Martina Cargiolli, Sara Cassarano, Marilia Carabotti, Bruno Annibale
Diverticular disease (DD) is a highly prevalent disease in western industrialized countries that encompasses a complex set of disorders. Because of its complexity and heterogeneity, both from a pathogenic and a clinical point of view, the management of this disease represent a challenge in clinical practice. This review aims to analyze and summarize the most recent evidence on the medical strategies for DD, considering separately the different stages of the disease, from prevention of diverticula formation to treatment of acute diverticulitis and prevention of recurrences...
October 3, 2018: Current Opinion in Pharmacology
Cho R Hong, Gib Bogle, Jingli Wang, Kashyap Patel, Frederik B Pruijn, William R Wilson, Kevin O Hicks
Intra-tumor heterogeneity represents a major barrier to anti-cancer therapies. One strategy to minimize this limitation relies on bystander effects via diffusion of cytotoxins from targeted cells. Hypoxia-activated prodrugs (HAPs) have the potential to exploit hypoxia in this way, but robust methods for measuring bystander effects are lacking. The objective of this study is to develop experimental models (monolayer, multilayer, and multicellular spheroid co-cultures) comprising 'activator' cells with high expression of prodrug-activating reductases and reductase-deficient 'target' cells, and to couple these with agent-based models (ABMs) that describe diffusion and reaction of prodrugs and their active metabolites, and killing probability for each cell...
2018: Frontiers in Pharmacology
Mengxin Geng, Akshaya Ravichandran, Jerome Escano, Leif Smith
Mutacin 1140, a member of the epidermin family of type AI lantibiotics, has a broad spectrum of activity against Gram-positive bacteria. It blocks cell wall synthesis by binding to lipid II. Although it has rapid bactericidal effects and potent activity against Gram-positive pathogens, its rapid clearance and short half-life in vivo limits its development in clinic. In this study, we evaluated the effect of charged and dehydrated residues on the pharmacokinetics of mutacin 1140. The dehydrated residues were determined to contribute to the stability of mutacin 1140, while alanine substitutions of the lysine or arginine residues improved the pharmacological properties of the antibiotic...
October 1, 2018: Antimicrobial Agents and Chemotherapy
Siraj Sundaran, Anjali Udayan, Keerthi Hareendranath, Basil Eliyas, Babu Ganesan, Ashik Hassan, Rajesh Subash, Vishnu Palakkal, Mohammed Saji Salahudeen
Hospital-based adverse drug reaction (ADR) monitoring and reporting programs intend to identify and quantify the risks associated with the use of medicines. To examine the causality, preventability and severity of ADR in a hospital setting; a prospective cohort study on spontaneous ADR reporting was conducted from December 2015 to May 2016. Incidence of ADRs, causality, type, severity and preventability were assessed using necessary assessment scales. The study included 3157 hospitalized individuals, in whom 51 ADRs were detected among 49 patients...
September 29, 2018: Pharmacy (Basel, Switzerland)
Rolf Hirsch, Jochen Wiesner, Alexander Marker, Yvonne Pfeifer, Armin Bauer, Peter E Hammann, Andreas Vilcinskas
Background: The ability of MDR Gram-negative bacteria to evade even antibiotics of last resort is a severe global challenge. The development pipeline for conventional antibiotics cannot address this issue, but antimicrobial peptides (AMPs) offer an alternative solution. Objectives: Two insect-derived AMPs (LS-sarcotoxin and LS-stomoxyn) were profiled to assess their suitability for systemic application in humans. Methods: The peptides were tested against an extended panel of 114 clinical MDR Gram-negative bacterial isolates followed by time-kill analysis, interaction studies and assays to determine the likelihood of emerging resistance...
October 1, 2018: Journal of Antimicrobial Chemotherapy
Syed F A Rizvi, Saleha Tariq, Muhammad Mehdi
OBJECTIVES: Dactinomycin is a well-known antitumor-antibiotic drug isolated from soil bacterium Streptomyces, which exhibits broad-spectrum pharmacological and biochemical effects. In this study, dactinomycin was successfully labeled with technetium-99m for early diagnosis of bacterial infection and to discriminate it from acute inflammation. MATERIALS AND METHODS: Various labeling parameters such as pH, ligand concentration, reducing agent, and stabilizing agent were investigated...
September 25, 2018: Nuclear Medicine Communications
Renata Carolina Alves, Richard Perosa Fernandes, Bruno Fonseca-Santos, Francesca Damiani Victorelli, Marlus Chorilli
Curcumin, a natural compound extracted from turmeric (Curcuma longa), has been extensively studied because of its various pharmacological properties, such as anti-inflammatory, antioxidant, antibiotic, antiprotozoal, immunomodulatory, anti-proliferative, antitumor, and anticarcinogenic effects. However, low solubility in aqueous media has limited its therapeutic applications. To overcome these bioavailability issues, the use of drug delivery systems providing localized or targeted delivery of this drug may represent a more viable therapeutic option...
September 25, 2018: Critical Reviews in Analytical Chemistry
James A D Berry, Dan E Miulli, Benjamin Lam, Christopher Elia, Julia Minasian, Stacey Podkovik, Margaret R S Wacker
Surgically accessing pathological lesions located within the central nervous system (CNS) frequently requires creating an incision in cosmetic regions of the head and neck. The biggest factors of surgical success typically tend to focus on the middle portion of the surgery, but a vast majority of surgical complications tend to happen towards the end of a case, during closure of the surgical site incisions. One of the most difficult complications for a surgeon to deal with is having to take a patient back to the operating room for wound breakdowns and, even worse, wound or CNS infections, which can negate all the positive outcomes from the surgery itself...
September 24, 2018: International Wound Journal
Jennifer Le, John S Bradley
The selection of the right antibiotic and right dose necessitates clinicians understand the contribution of pharmacokinetic variability stemming from age-related physiologic maturation and the pharmacodynamics to optimize drug exposure for clinical response. The complexity of selecting the right dose arises from the multiplicity of pediatric age groups, from premature neonates to adolescents. Body size and age (which relate to organ function) must be incorporated to optimize antibiotic dosing in this vulnerable population...
October 2018: Journal of Clinical Pharmacology
Jasmine Morgan, Matthew Smith, Mark T Mc Auley, J Enrique Salcedo-Sora
Bacteria can survive high doses of antibiotics through stochastic phenotypic diversification. We present initial evidence that folate metabolism could be involved with the formation of persisters. The aberrant expression of the folate enzyme gene fau seems to reduce the incidence of persisters to antibiotics. Folate-impaired bacteria had a lower generation rate for persisters to the antibiotics ampicillin and ofloxacin. Persister bacteria were detectable from the outset of the exponential growth phase in the complex media...
September 24, 2018: Microbiology
E D'Huart, J Vigneron, I Gindre, P Lider, B Demoré
A new function on the international database Stabilis® has been created: a database of research teams involved in stability and compatibility studies of drugs. The first part is descriptive. For each team, the list of publications and of molecules studied can be edited. A search function can extract data by using different criteria like the drug, galenic form, pharmacological class, molecule form (small molecule, monoclonal antibody), country, author and years of publications. The second part of the new function is interactive and allows Stabilis® users to suggest stability studies...
September 19, 2018: Annales Pharmaceutiques Françaises
Yeonwoo Lebovitz, Veronica M Ringel-Scaia, Irving C Allen, Michelle H Theus
From immunology to neuroscience, interactions between the microbiome and host are increasingly appreciated as potent drivers of health and disease. Epidemiological studies previously identified compelling correlations between perinatal microbiome insults and neurobehavioral outcomes, the mechanistic details of which are just beginning to take shape thanks to germ-free and antibiotics-based animal models. This review summarizes parallel developments from clinical and preclinical research that suggest neuroactive roles for gut bacteria and their metabolites...
2018: Frontiers in Immunology
Huisheng Yang, Yanming Xie, Jisheng Ni, Yue Liu, Rui Song, Cen Chen, Yan Zhuang, Yin Zhang
Background: Real world evidence is important for informing healthcare practice and developing medical products and has gained broad interest in healthcare. Compound Kushen Injection (CKI) has been widely applied into treatment of colon carcinoma (CC) in China. Postapproval drug assessment related retrospective studies using electrical medical record (EMR) collected from hospital information system (HIS) is one of the most important categories of real-world study (RWS). Based on HIS EMR, interrelationships of combined medication of CKI in treating CC can be validated in real world settings...
2018: Evidence-based Complementary and Alternative Medicine: ECAM
Andrzej Miskiewicz, Piotr Ceranowicz, Mateusz Szymczak, Krzysztof Bartuś, Paweł Kowalczyk
This review deals with various microbiological activities of ionic liquids, which constitute the first anti-infective defense against multi-drug-resistant bacteria-with a particular emphasis placed on medicine and pharmacology. The quoted data on the biological activity of ionic liquids including their antimicrobial properties (depending on the type of a cation or an anion) and are discussed in view of possible applications in nosocomial infections. Dedicated attention is given to finding infections with the Klebsiella pneumoniae New Delhi strain, Acinetobacter baumannii , and Enterococcus species, which are responsible for the induction of antibiotic resistance in intensive care units...
September 15, 2018: International Journal of Molecular Sciences
Joana Magalhães, Nina Franko, Giannamaria Annunziato, Martin Welch, Stephen K Dolan, Agostino Bruno, Andrea Mozzarelli, Stefano Armao, Aigars Jirgensons, Marco Pieroni, Gabriele Costantino, Barbara Campanini
Several bacteria rely on the reductive sulphur assimilation pathway, absent in mammals, to synthesise cysteine. Reduction of virulence and decrease in antibiotic resistance have already been associated with mutations on the genes that codify cysteine biosynthetic enzymes. Therefore, inhibition of cysteine biosynthesis has emerged as a promising strategy to find new potential agents for the treatment of bacterial infection. Following our previous efforts to explore OASS inhibition and to expand and diversify our library, a scaffold hopping approach was carried out, with the aim of identifying a novel fragment for further development...
December 2018: Journal of Enzyme Inhibition and Medicinal Chemistry
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