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Shuaibing Liu, Xiangfen Shi, Xin Tian, Xiaojian Zhang, Zhiyong Sun, Liyan Miao
Ticagrelor is the first reversible, direct-acting, potent P2Y12 receptor antagonist in management of acute coronary syndromes. It is rapidly absorbed and extensively metabolized. AR-C124910XX, the major active metabolite, antagonizes the P2Y12 receptor at approximately equal potency. The metabolism of ticagrelor to AR-C124910XX involves CYP3A4 and CYP3A5. CYP3A polymorphisms have been well documented, and CYP3A4(∗)1G (g.20230G>A, rs2242480) and CYP3A5(∗)3 (g.6986A>G, rs776746) are the most important single nucleotide polymorphisms in Chinese...
2017: Frontiers in Pharmacology
Chad A Bousman, Malcolm Forbes, Mahesh Jayaram, Harris Eyre, Charles F Reynolds, Michael Berk, Malcolm Hopwood, Chee Ng
About half of people who take antidepressants do not respond and many experience adverse effects. These detrimental outcomes are in part a result of the impact of an individual's genetic profile on pharmacokinetics and pharmcodynamics. If known and made available to clinicians, this could improve decision-making and antidepressant therapy outcomes. This has spurred the development of numerous pharmacogenetic-based decision support tools. In this article, we provide an overview of pharmacogenetic decision support tools, with particular focus on tools relevant to antidepressants...
February 8, 2017: BMC Psychiatry
Dorothee Kasteleijn-Nolst Trenite
No abstract text is available yet for this article.
November 27, 2016: Epilepsy Research
Jing-Yang Liou, Mei-Yung Tsou, Chien-Kun Ting
Drug interaction is fundamental in performing anesthesia. A response surface model (RSM) is a very useful tool for investigating drug interactions. The methodology appeared many decades ago, but did not receive attention in the field of anesthesia until the 1990s. Drug investigations typically start with pharmacokinetics, but it is the effects on the body clinical anesthesiologists really care about. Typically, drug interactions are divided into additive, synergistic, or infra-additive. Traditional isobolographic analysis or concentration-effect curve shifts are limited to a single endpoint...
December 2015: Acta Anaesthesiologica Taiwanica: Official Journal of the Taiwan Society of Anesthesiologists
Xiaotian Xie, Huijun Zhao, Dawei Qin, Xiaohong Qiao
OBJECTIVE: To compare the pharmacokinetics and pharmacodynamics of antithymocyte globulins (ATGs) produced by two companies in the treatment of children with aplastic anemia (AA). METHODS: Six children with acquired AA were divided into two groups. The patients in each group were treated with either R-ATG or F-ATG for 5 consecutive days. Venous blood samples were collected at time points of 0 h, 4 h, 8 h after infusion of ATGs on day 1, at the end of the infusion on day 2-5, and on d7, d21, d35, d60, d90...
2015: International Journal of Clinical and Experimental Medicine
Nobuharu Goto, Masayuki Suzuki
The premise of the implementation of eligible pharmacodynamic biomarkers (PD markers) in clinical development of drugs is based on their qualification and understanding of human disease networks on a molecular level, which may be relevant to risk factors, pathogenesis, prognosis, and relapse/remission. Especially, information on PD markers characterized with drug exposure in target tissues, drug binding to target molecules, and linkage to clinical endpoints in early drug development stage can be critical for GO/NO GO decision for the next late clinical stages...
2014: Yakugaku Zasshi: Journal of the Pharmaceutical Society of Japan
Anshumali Awasthi, Mohtashim Lohani, Manoj K Singh, Anu T Singh, Manu Jaggi
To develop naphthyridine derivatives as anticancer candidates, pharmacokinetic (PK) evaluations of 10 novel derivatives of 1,4-dihydro-4-oxo-1-proparagyl-1,8-naphthyridine-3-carboxamide, with potent anticancer activity were done using in vitro ADME (absorption, distribution, metabolism, excretion) and pharmacokinetic--pharmcodynamic (PK/PD) assays. Only derivatives 5, 6, 9 and 10 showed better metabolic stability, solubility, permeability, partition coefficient and cytochrome P450 (CYP) inhibition values. PK of derivatives 5, 6, 9 and 10 in rat showed comparable PK profile for derivative 5 (C0 = 6...
October 2014: Journal of Enzyme Inhibition and Medicinal Chemistry
A D Pranger, J W C Alffenaar, R E Aarnoutse
Fluoroquinolones (FQs) are important drugs to treat drug-resistant tuberculosis. In this review we integrated pharmacokinetic properties (PK) and microbiological susceptibility against M. tuberculosis and eventually evaluated the pharmcodynamic (PD) properties, as well as the influence of co-administered agents on these characteristics, for the currently used FQs (ciprofloxacin, ofloxacin, levofloxacin, gatifloxacin and moxifloxacin) in TB treatment. Future FQs that are being developed may overcome the problems with FQs that are used in daily practice...
2011: Current Pharmaceutical Design
Mei Yang, Jian-Feng Ge, Chika Arai, Isamu Itoh, Qiang Fu, Masataka Ihara
In vivo antimalarial drug candidates screening test was carried out on a series of water-soluble 3,7-bis(dialkylamino)phenoxazin-5-ium derivatives. Among them, 3-(diethylamino)-7-(piperidin-1-yl)phenoxazin-5-ium chloride (SSJ-206) showing highest efficacy was chosen for further pharmcodynamics and pharmacokinetics study. It was supported from these data that the phenoxazinium salts, SSJ-206, would be one of hopeful candidates as an oral antimalarial drug.
February 15, 2009: Bioorganic & Medicinal Chemistry
Frederick J Stoddard, Craigan T Usher, Annah N Abrams
Psychopharmacologic treatment in pediatric critical care requires a careful child or adolescent psychiatric evaluation, including a thorough review of the history of present illness or injury, any current or pre-existing psychiatric disorder, past history, and laboratory studies. Although there is limited evidence to guide psychopharmacologic practice in this setting, psychopharmacologic treatment is increasing in critical care, with known indications for treatment, benefits, and risks; initial dosing guidelines; and best practices...
July 2006: Child and Adolescent Psychiatric Clinics of North America
Qiaoyun Chen, Nan Wang, Feng Yao, Xiaohe Lu
Since the introduction of the phosphodiesterase type 5 (PDE-5) inhibitor sildenafil in 1998, there has been a fundamental change in the treatment of erectile dysfunction (ED). Sildenafil has already been used by over 20 million men in over 100 countries, with a death rate similar to that of general population. The success rate of sildenafil amounts to an average of over 80%, and sildenafil has become the first choice for patients with ED. The development of two new PDE-5 inhibitors, vardenafil and tadalafil, has added to the options for the treatment of ED...
April 2004: Zhonghua Nan Ke Xue, National Journal of Andrology
H G Zapotoczky, C A Simhandl
An overview is presented of interactions of currently frequently used antidepressants with various other drugs. The effects of interactions of tricyclic antidepressants, tetracyclics, monoamine oxidase (MAO) inhibitors, lithium and carbamazepine are comparatively well documented, their pharmcodynamic and pharmacokinetic characteristics extensively researched and well known to the practitioner. These interactions concern synergic effects, enzyme inhibition, enzyme induction in the liver, competitive inhibition of absorption and reciprocal effects on the receptor...
1995: Wiener Klinische Wochenschrift
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