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Current Drug Metabolism

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https://www.readbyqxmd.com/read/28413976/laboratory-monitoring-or-measurement-of-direct-oral-anticoagulants-doacs-advantages-limitations-and-future-challenges
#1
Emmanuel J Favaloro, Leonardo Pasalic, Jennifer Curnow, Giuseppe Lippi
BACKGROUND: The Direct Oral Anticoagulants (DOACs) represent a new generation of antithrombotic agents, providing direct inhibition of either thrombin (factor IIa; FIIa) or activated factor X (FXa). Around the globe, their use is progressively rising, as these new agents replace the historical anticoagulants (heparin and vitamin K antagonists including warfarin) for various clinical conditions in medical practice. Other acronyms used to designate DOACs include TSOAC (target specific oral anticoagulants) and NOAC (novel; or non-vitamin K antagonist oral anticoagulants)...
April 17, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28412908/news-in-the-indications-of-non-vitamin-k-oral-anticoagulants-according-to-the-guidelines-of-the-american-college-of-chest-physicians-2016
#2
Gabriela Cesarman Maus, Guillermo Jose Ruiz Argüelles
Antithrombotic guidelines published by the Chest Journal, the official publication of the American College of Chest Physicians (ACCP), are continuously updated as clinically relevant information accumulates. The Evidence-Based Clinical Practice Guidelines on antithrombotic therapy and prevention of thrombosis were published in 2012. This year, the topic that has been updated pertains to antithrombotic therapy, specifically addressing prophylaxis and treatment of venous thromboembolic (VTE) disease. In this paper, I focus on these guidelines regarding the indications or lack thereof for the use of Non-vitamin K-antagonist Oral Anticoagulants (NOACS), also referred to as Direct-acting Oral Anticoagulants (DOACS)...
April 13, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28412907/review-of-the-pharmacology-of-the-emerging-possibilities-of-the-direct-oral-anticoagulants-reversal
#3
Matej Samos, Lucia Stanciakova, Ingrid Skornova, Tomas Bolek, Frantisek Kovar, Jan Stasko, Peter Galajda, Marian Mokan, Peter Kubisz
BACKGROUND: Direct oral anticoagulants (DOACs) offer consistent and predictable anticoagulation, oral administration with good patient compliance and a good safety profile. Dabigatran - a direct thrombin inhibitor, apixaban and rivaroxaban - direct factor Xa inhibitors are now largely used for anticoagulation in patients with non-valvular atrial fibrillation and in patients with venous thromboembolism. These agents have emerged as an expediential clinical choice in long-term anticoagulation for an increasing number of patients...
April 13, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28382862/inflammatory-bowel-disease-new-therapeutic-options-in-the-post-anti-tnf%C3%AE-era
#4
Miguel Jiménez Pérez, Raúl V Olmedo Martín, Víctor M Amo Trillo, Rocío González Gande
Inflammatory bowel diseasesare chronic bowel disorders the causes of which have not been fully elucidated,though they all sharean immunological basis. They have an important impact on both quality of life of the patient and on healthcare services. The incorporation of biological agents against tumour necrosis factor (TNF) alpha some 15 years ago represented a revolution in the management of patients with disease that did not respond to conventional treatment, enabling an overall improvement in the quality of life of many of these patients...
April 6, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28382861/metabolism-of-drugs-used-in-the-therapy-of-seizures-an-analytical-point-of-view-part-1
#5
Roberto Mandrioli, Laura Mercolini
BACKGROUND: Seizures are aetiologically and clinically heterogeneous neurological disorders that are currently treated using a wide array of drugs, belonging to equally heterogeneous chemical classes. Some of them are known as "antiepileptic drugs" (AEDs), due to their main field of use, while others (such as benzodiazepines) are frequently used for other conditions as well as for seizures. Due to their different chemical properties and mechanisms of activity, the metabolic characteristics of anti-seizure drugs can vary widely, also producing big differences in terms of safety, efficacy and therapeutic suitability...
April 6, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28322159/towards-predicting-the-cytochrome-p450-modulation-from-qsar-to-proteochemometric-modeling
#6
Watshara Shoombuatong, Philip Prathipati, Veda Prachayasittikul, Nalini Schaduangrat, Aijaz Ahmad Malik, Reny Pratiwi, Sompon Wanwimolruk, Jarl E S Wikberg, Matthew Paul Gleeson, Ola Spjuth, Chanin Nantasenamat
Drug metabolism determines the fate of a drug when it enters the human body and is a critical factor in defining their absorption, distribution, metabolism, excretion and toxicity (ADMET) characteristics. Among the various drug metabolizing enzymes, cytochrome P450s (CYP450) constitute an important protein family that aside from functioning in xenobiotic metabolism is also responsible for a diverse array of other roles encompassing steroid and cholesterol biosynthesis, fatty acid metabolism, calcium homeostasis, neuroendocrine functions and growth regulation...
March 20, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28302029/in-silico-adme-studies-for-new-drug-discovery-from-chemical-compounds-to-chinese-herbal-medicines
#7
Guojun Yan, Xiaobing Wang, Zhou Chen, Xianhui Wu, Jinhuo Pan, Yushen Huang, Gang Wan, Zhaogang Yang
Nowadays, in-silico tools are widely used to provide the potential structure of the metabolites formed depending on the site of metabolism. These methods can also highlight the molecular moieties that help to direct the molecule into the cytochrome cavity so that the site of metabolism is in proximity to the catalytic center. In this mini-review, we summarized three aspects of the in-silico methods in the application of prediction the ADME (absorption, distribution, metabolism and excretion) properties of compounds: structure-based approaches for predicting molecular modeling of drug metabolizing enzymes; in-silico metabolite prediction; and pharmacophore models for analysis substrate specificity...
March 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28302028/quantum-mechanical-qm-calculations-applied-to-admet-drug-prediction-a-review
#8
Edeildo F Silva-Júnior, J X Araújo-Júnior, T M Aquino
The discovery of new drugs is generally considered a long and expensive process, which often leads to molecules with low efficacy and high toxicity, which in many cases can be related to metabolism. In an attempt to reduce these failures and the production costs of a new drug, in silico studies have been used to obtain important information about the behavior of these compounds in the metabolism phases: absorption, distribution, metabolism (or biotransformation) and elimination (or excretion). Quantum Mechanical (QM) calculations are based on Schrödinger's equation can be used to develop models and theoretical parameters able to explain properties observed experimentally...
March 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28302027/in-silico-design-and-admet-studies-of-natural-compounds-as-inhibitors-of-xanthine-oxidase-xo-enzyme
#9
Neelam Malik, Priyanka Dhiman, Anurag Khatkar
BACKGROUND: Xanthine oxidase a ubiquitous enzyme has been found to be involved in various pathological disorders including gout, hyperuricemia, inflammation, oxidative stress and cardiovascular diseases. Inhibitors of xanthine oxidase thus find a crucial role in the therapeutic treatment of these deadly diseases. OBJECTIVE: Considering the side effects of today's treatment regimen here we choose nature based compounds to act as xanthine oxidase inhibitors. In the present work, we performed in-silico docking of natural compounds to reveal the underlying mechanism of inhibition of xanthine oxidase...
March 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28302026/drug-metabolism-in-preclinical-drug-development-a-survey-of-the-discovery-process-toxicology-and-computational-tools
#10
Naiem T Issa, Henri Wathieu, Abiola Ojo, Stephen W Byers, Sivanesan Dakshanamurthy
Increased R & D spending and high failure rates exist in drug development, due in part to inadequate prediction of drug metabolism and its consequences in the human body. Hence, there is a need for computational methods to supplement and complement current biological assessment strategies. In this review, we provide an overview of drug metabolism in pharmacology, and discuss the current in vitro and in vivo strategies for assessing drug metabolism in preclinical drug development. We highlight computational tools available to the scientific community for the in silico prediction of drug metabolism, and examine how these tools have been implemented to produce drug-target signatures relevant to metabolic routes...
March 15, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28266274/dermatokinetics-as-an-important-tool-to-assess-the-bioavailability-of-drugs-by-topical-nanocarriers
#11
O P Katare, Kaisar Raza, Sheetu Wadhwa, Pramod Kumar, Nagarani Thotakura
Now-a-days, numerous nanocarrier-based drug products for topical applications are present in market and a huge number of similar products are being researched. To estimate the amount of drug delivery to skin, the scientists have now established techniques for separation of skin layers for the determination of drug concentrations. This forms the basis of pharmacokinetics of drug(s) in skin, i.e., dermatokinetics. However, dermatokinetic modeling of topical products is still a colossal challenge for scientists...
March 5, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28266273/nanosystems-for-skin-delivery-from-drugs-to-cosmetics
#12
Catarina P Reis, Patrícia Rijo, Paula Pereira, Ana F Antunes
Skin delivery is an exciting and challenging area. There are numerous skin delivery systems currently available on the market. However, this market still remains limited to a narrow range of substances. Thus, several strategies have been developed to improve the performance of those substances, including the development of nanosystems. The aim of this review is to elucidate the nanosystems applied to the skin. In order to contextualize this subject, anatomy and physiology of the skin will be first briefly described and then general concepts and the various examples of these nanosystems, both cosmetic and pharmaceutical field, will be also accessed...
March 5, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28260515/in-silico-and-in-vivo-toxicological-evaluation-of-cissampelos-sympodialis-secondary-metabolites-in-rattus-norvegicus
#13
Luciana Scotti
Cissampelos sympodialis is a plant to northeastern Brazil region used by populace for treating diseases respiratory. Several studies have shown that the ethanol extract of the leaves have immunomodulatory and anti-inflammatory activities. The infusion is an ancient popular technique widely used in traditional medicine using as extracting means just hot water. This study aims to investigate the acute toxicological potential administering a dose of 2000mg/kg in Rattus norvegicus combined with in silico study of 117 alkaloids present in Cissampelos genre...
March 1, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28260514/coral-software-analysis-of-impacts-of-pharmaceutical-agents-upon-metabolism-via-the-optimal-descriptors
#14
Alla P Toporova
Optimal descriptors, which are aimed to predict values of endpoints with apparent influence upon metabolism are crytically compared in aspect of their robustness and heuristic potential. Arguments which are confirming the necessity of reformulation of basics of quantitative structure - property / activity relationships (QSPRs/QSARs) are listed. The arguments are the following: (i) each QSAR model is the stochastic experiment. The result of this experiment is defined by distribution into the training set and validation set; (ii) real predictive potential of a model should be checked up with a group of different splits into the training and validation sets; and (iii) only model stochastically stable for a defined group of the above splits can be estimated as a reliable tool for the prediction of the examined endpoint...
February 28, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228079/lipid-based-nanoparticles-as-carriers-for-dermal-delivery-of-antioxidants
#15
Lucia Montenegro
The skin, being the outermost layer of our body, is constantly exposed to oxidative stress induced by UV-radiation, pollutants, smoke and xenobiotics. To counteract the deleterious effects of such exposure, the skin is equipped with a complex anti-oxidation system, involving both exogenous and endogenous antioxidants. As low molecular weight antioxidants undergo depletion in counteracting oxidative stress occurring in the skin, topical supplementation with these agents is regarded as a suitable strategy to restore skin oxidative balance...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228078/nanocarriers-mediated-topical-drug-delivery-for-psoriasis-treatment
#16
Sevgi Güngör, Meriem Rezigue
BACKGROUND: Psoriasis is a chronic autoimmune inflammatory skin disease affecting 2 to 3% of people worldwide. Topical therapy as first option in the management of psoriasis is an attractive strategy by delivering drugs efficiently into target sites of disease, minimizing systemic side effects of drugs and ensuring high patient compliance. However, the delivery of antipsoriatic agents via conventional topical formulations is limited due to their poor percutaneous penetration and targeting into deeper layers of the skin...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228077/antioxidant-nanoplatforms-for-dermal-delivery-melatonin
#17
Aroha Belen Sánchez Milán, Ana C Calpena Campmany, Beatriz Clares Naveros
Melatonin (MLT) is emerging as a promising therapeutic agent, mainly due to its role as antioxidant. Substantial evidences show that melatonin is potentially effective on a variety of diseases as cancer, inflammation and neurodegenerative diseases. The excellent antioxidant capacity with pharmacokinetics characteristics and the emerging search for new pharmaceutical nanotechnology based systems, make it particularly attractive to elaborate nanoplatforms based on MLT for biomedical or cosmetic dermal applications...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228076/transdermal-drug-delivery-opportunities-and-challenges-for-controlled-delivery-of-therapeutic-agents-using-nanocarriers
#18
Balak Das Kurmi, Pawan Tekchandani, Rishi Paliwal, Shivani Rai Paliwal
BACKGROUND: Transdermal drug delivery represents an extremely attractive and innovative route across the skin owing to the possibility for achieving systemic effect of drugs. Present scenario demands a special focus on developing safe medicine with minimize toxic adverse effects related to most of the pharmacologically active agents. Transdermal drug delivery would be a focal paradigm which provides patient convenience, first-pass hepatic metabolism avoidance, local targeting and reduction in toxic effect related to various categories of drugs like, analgesics, anti-inflammatory, antibiotics, antiviral, anaesthetic, anticancer etc...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228075/challenges-in-dermal-delivery-of-therapeutic-antimicrobial-protein-and-peptides
#19
Rohan Aminbhai Lalani, Ambikanandan Misra, Jitendra Amrutiya, Hinal Patel, Priyanka Bhatt, Vivek Patel
BACKGROUND: Protein and peptides in biological system form an important part of innate immune system and are being explored for potential use in various diseases as therapeutics. Importance of proteins and peptides as a new class of antimicrobial agents have boosted research in the field of biotechnology as potential alternative to antibiotic agents. OBJECTIVE: Protein and peptides antimicrobial as a therapeutics class are structurally diverse and exhibit potent activity against microbes by various mechanisms...
February 22, 2017: Current Drug Metabolism
https://www.readbyqxmd.com/read/28228080/marine-drugs-a-hidden-wealth-and-a-new-epoch-for-cancer-management
#20
Eram Shakeel, Deepika Arora, Qazi Mohammad Sajid Jamal, Salman Akhtar, Mohd Kalim Ahmad Khan, Mohammad A Kamal, Mohd Haris Siddiqui, Mohtashim Lohani, Jamal M Arif
Malignant tumors are the leading cause of death in humans. Due to tedious efforts and investigation made in the field of marine drug discovery, there is now a scientific bridge between marine and pharmaceutical sciences. However, at present only few marine drugs have been paved towards anticancer management, yet many more to be established. Marine organisms are profuse manufacturer of structurally inimitable bioactive metabolites that have unusual mechanisms of action and diverse biosynthetic pathways. Some of the compounds derived from marine organisms have antioxidant property and anticancer activities, but they are largely unexplored...
February 20, 2017: Current Drug Metabolism
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