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https://www.readbyqxmd.com/read/28730460/impact-of-safety-warnings-on-domperidone-prescribing-in-ireland
#1
M Teeling, M J MacAvin, K Bennett
AIM: This study aimed to investigate the impact of the 2014 safety warnings on use of domperidone, on subsequent prescribing patterns in Ireland. METHODS: The Irish HSE-PCRS pharmacy claims database was used to identify the study cohort (aged 18+), prescribed domperidone from Jan 2014 to Oct 2015. Dosage was available for each claim; concomitant prescription with the following drug classes was identified and calculated as a percentage of the total number of claims: anti-arrhythmics, macrolide antimicrobials and the selective serotonin receptor inhibitors (SSRIs) citalopram and escitalopram...
July 20, 2017: Irish Journal of Medical Science
https://www.readbyqxmd.com/read/28728494/the-clinical-significance-of-qt-prolongation-associated-with-tamoxifen-a-review-of-the-literature
#2
Katherine Fung, Julia Imeson, Frances Cusano
Objective To review the literature discussing QT prolongation associated with the use of tamoxifen in order to evaluate the clinical significance. Data sources A search of PubMed (1946 to 2017), MEDLINE (1946 to 2017) and EMBASE (1947 to 2017) was performed using a combination of the following search terms: tamoxifen, estrogen antagonist, selective estrogen receptor modulator, QT prolongation, QT interval, long QT syndrome and torsades de pointes. All searches were limited to human subjects. Reference lists of the literature found were also reviewed but did not reveal any further articles...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28714380/loperamide-and-cardiac-events-is-high-dose-use-still-safe-for-chemotherapy-induced-diarrhea
#3
Mário L de Lemos, Jolene Guenter, Victoria Kletas
High-dose loperamide is often used for the acute management of chemotherapy-induced diarrhea, with a maximum daily dosing of up to 24 mg. Recently, the US Food and Drug Administration has issued a warning that loperamide can cause rare serious cardiac events, including QT prolongation, torsades de pointes, cardiac arrest and death. Most events were reported in patients taking very high doses for an extended period of time. Daily intake ranged from 64 mg to 1600 mg, often continuously for weeks or months...
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28713157/population-pharmacokinetics-of-moxifloxacin-and-its-concentration-qt-interval-relationship-modeling-in-chinese-healthy-volunteers
#4
Feng-Yan Xu, Ji-Han Huang, Ying-Chun He, Li-Yu Liang, Lu-Jin Li, Juan Yang, Fang Yin, Ling Xu, Qing-Shan Zheng, Kun Wang
Moxifloxacin (MX) is an 8-methoxyquinolone antimicrobial drug, which is often used as a positive control in thorough QT (TQT) studies. In the present study we established the population pharmacokinetics model of MX and the relationship of MX concentrations with the QT and various corrected QT (QTc) intervals, and compared the results with other ethnicities. The MX data used for modeling were obtained from a published TQT interval prolongation study of antofloxacin with MX as the positive control. In this four-period crossover study, 24 adult Chinese healthy volunteers received either 200 or 400 mg of oral antofloxacin once daily, 400 mg of MX, or a placebo...
July 17, 2017: Acta Pharmacologica Sinica
https://www.readbyqxmd.com/read/28711156/towards-a-structural-view-of-drug-binding-to-herg-k-channels
#5
REVIEW
Jamie I Vandenberg, Eduardo Perozo, Toby W Allen
The human ether-a-go-go-related gene (hERG) K(+) channel is of great medical and pharmaceutical relevance. Inherited mutations in hERG result in congenital long-QT syndrome which is associated with a markedly increased risk of cardiac arrhythmia and sudden death. hERG K(+) channels are also remarkably susceptible to block by a wide range of drugs, which in turn can cause drug-induced long-QT syndrome and an increased risk of sudden death. The recent determination of the near-atomic resolution structure of the hERG K(+) channel, using single-particle cryo-electron microscopy (cryo-EM), provides tremendous insights into how these channels work...
July 12, 2017: Trends in Pharmacological Sciences
https://www.readbyqxmd.com/read/28711067/pa-6-inhibits-inward-rectifier-currents-carried-by-v93i-and-d172n-gain-of-function-kir2-1-channels-but-increases-channel-protein-expression
#6
Yuan Ji, Marlieke G Veldhuis, Jantien Zandvoort, Fee L Romunde, Marien J C Houtman, Karen Duran, Gijs van Haaften, Eva-Maria Zangerl-Plessl, Hiroki Takanari, Anna Stary-Weinzinger, Marcel A G van der Heyden
BACKGROUND: The inward rectifier potassium current IK1 contributes to a stable resting membrane potential and phase 3 repolarization of the cardiac action potential. KCNJ2 gain-of-function mutations V93I and D172N associate with increased IK1, short QT syndrome type 3 and congenital atrial fibrillation. Pentamidine-Analogue 6 (PA-6) is an efficient (IC50 = 14 nM with inside-out patch clamp methodology) and specific IK1 inhibitor that interacts with the cytoplasmic pore region of the KIR2...
July 15, 2017: Journal of Biomedical Science
https://www.readbyqxmd.com/read/28703360/model-averaging-for-robust-assessment-of-qt-prolongation-by-concentration-response-analysis
#7
A G Dosne, M Bergstrand, M O Karlsson, D Renard, G Heimann
Assessing the QT prolongation potential of a drug is typically done based on pivotal safety studies called thorough QT studies. Model-based estimation of the drug-induced QT prolongation at the estimated mean maximum drug concentration could increase efficiency over the currently used intersection-union test. However, robustness against model misspecification needs to be guaranteed in pivotal settings. The objective of this work was to develop an efficient, fully prespecified model-based inference method for thorough QT studies, which controls the type I error and provides satisfactory test power...
July 13, 2017: Statistics in Medicine
https://www.readbyqxmd.com/read/28699784/cancer-drugs-and-qt-prolongation-weighing-risk-against-benefit
#8
Pierantonio Menna, Emanuela Salvatorelli, G Minotti
No abstract text is available yet for this article.
July 12, 2017: Expert Opinion on Drug Safety
https://www.readbyqxmd.com/read/28695570/population-pharmacokinetics-and-electrocardiographic-effects-of-dihydroartemisinin-piperaquine-in-healthy-volunteers
#9
Palang Chotsiri, Thanaporn Wattanakul, Richard Hoglund, Borimas Hanboonkunupakarn, Sasithon Pukrittayakamee, Daniel Blessborn, Podjanee Jittamala, Nicholas J White, Nicholas P J Day, Joel Tarning
AIMS: The aims of the presented study were to evaluate the pharmacokinetic properties of dihydroartemisinin and piperaquine, potential drug-drug interactions with concomitant primaquine treatment, and piperaquine effects on the electrocardiogram in healthy volunteers. METHODS: Population pharmacokinetic properties of dihydroartemisinin and piperaquine were assessed in 16 in healthy Thai adults using an open-label randomized crossover study. Drug concentration-time data and electrocardiographic measurements were evaluated with nonlinear mixed-effects modelling...
July 11, 2017: British Journal of Clinical Pharmacology
https://www.readbyqxmd.com/read/28687226/acquired-long-qt-syndrome-and-phosphoinositide-3-kinase
#10
REVIEW
Ira S Cohen, Richard Z Lin, Lisa M Ballou
While it is well known that mutation of several different ion channels can cause congenital long QT syndrome, block of IKr is widely thought to be responsible for most cases of drug-induced acquired long QT syndrome (aLQTS). In this article, we review evidence supporting another cause of aLQTS due to inhibition of phosphoinositide 3-kinase (PI3K) signaling. Inhibition of PI3K affects multiple plateau currents, reducing IKr, IKs, and ICaL while increasing the persistent sodium current (INaP). The effects of PI3K inhibitors develop slowly, requiring hours to days to reach steady state...
May 17, 2017: Trends in Cardiovascular Medicine
https://www.readbyqxmd.com/read/28685701/the-role-of-quinidine-in-the-pharmacological-therapy-of-ventricular-arrhythmias-quinidine
#11
Bojana Bozic, Teodora Vidonja Uzelac, Aleksandra Kezic, Milica Bajcetic
BACKGROUND: Historically, quinidine was the first medicine used in the therapy of heart arrhythmias. Studies in the early 20th century identified quinidine, a diastereomer of the antimalarial quinine, as the most potent of the antiarrhythmic substances extracted from the cinchona plant. Quinidine is used by the 1920s, as an antiarrhythmic agent to maintain sinus rhythm after conversion from atrial flutter or atrial fibrillation and to prevent recurrence of ventricular tachycardia or ventricular fibrillation...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28685698/medical-therapy-for-long-qt-syndrome
#12
George Adamos, Nicoletta Iacovidou, Theodoros Xanthos
Long QT syndrome (LQTS) is an arrhythmogenic disorder characterized by repolarization abnormalities with a propensity to cause life threatening cardiac events. The first manifestation of the syndrome may be sudden death, therefore, early diagnosis and therapy is of great importance. LQTS can be both congenital and acquired. The latter is most commonly seen in hospitalized patients and such individuals have an easily recognizable and reversible precipitating factor (electrolyte disturbances, certain drugs etc...
July 7, 2017: Mini Reviews in Medicinal Chemistry
https://www.readbyqxmd.com/read/28682150/drug-drug-interaction-related-to-the-use-of-pipamperon-and-ondansetron-in-a-child-treated-for-leukemia
#13
Tiene Bauters, Sarah Buts, Victoria Bordon, Geneviève Laureys
Pipamperon is a potent neuroleptic drug with many side effects, including prolongation of the QT interval. We report a case of a child treated for leukemia in which prolongation of the QT interval was observed. Physicians and pharmacists should be cautious for drug-drug interactions when pipamperon is prescribed, especially in combination with other QT-prolongating agents. Alternative strategies should be used whenever possible.
January 1, 2017: Journal of Oncology Pharmacy Practice
https://www.readbyqxmd.com/read/28675269/-new-therapeutics
#14
Adriana Iacob Popescu, Liz Coronado, Aikaterini Efstathopoulou, Daniele Frisone, Gian-Marco Stamm, Javier Torralvo, Luc Barberini, Pierre-Auguste Petignat
Daily medical practice triggers reflexes in the use of drugs which must nevertheless always be adapted to new knowledge. Physician assistants and residents in the clinical ward of Internal Medicine of Sion Hospital summarize six recently published clinical treatments to which primary care physicians or in hospital-based internal medicine have to pay a particular attention. Quinolones are widely used but associated with QT interval widening, morphine delays and attenuate ticagrelor action in patients with myocardial infarction, evolocumab, a monoclonal antibody impact in reducing lipids and cardiovascular events, impact of statins on influenza vaccine effectiveness, vitamin D treatment for the prevention of functional decline, high dose dexamethasone for the treatment of immune thrombocytopenia...
September 7, 2016: Revue Médicale Suisse
https://www.readbyqxmd.com/read/28674475/drug-induced-qt-prolongation-and-torsades-de-pointes
#15
Matthew Li, Liz G Ramos
Torsades de pointes (TdP)-an uncommon but life-threatening polymorphic ventricular tachycardia-is almost always drug induced. The authors describe the causes, risk factors, symptoms, diagnosis, and treatment of TdP.
July 2017: P & T: a Peer-reviewed Journal for Formulary Management
https://www.readbyqxmd.com/read/28673607/nanoparticle-formulations-to-enhance-tumor-targeting-of-poorly-soluble-polyphenols-with-potential-anticancer-properties
#16
REVIEW
Maria Cristina Bonferoni, Silvia Rossi, Giuseppina Sandri, Franca Ferrari
Polyphenols have been extensively studied for their relevant anticancer activity. Quite often however their instability, extensive metabolization, low bioavailability and poor solubility limit their application in cancer prevention and therapy. Formulation in nanoparticles has been widely proposed as a means to overcome these limits, maximize localization and specific activity at tumor site. The present review is intended as an update of literature regarding nanoparticulate carriers aimed to deliver polyphenols to the cancer site...
June 30, 2017: Seminars in Cancer Biology
https://www.readbyqxmd.com/read/28673509/discovery-of-a-new-mexiletine-derived-agonist-of-the-herg-k-channel
#17
Roberta Gualdani, Maria Maddalena Cavalluzzi, Francesco Tadini-Buoninsegni, Giovanni Lentini
The human Ether-a-go-go Related Gene (hERG) potassium channel plays a central role in the rapid component (IKr) of cardiac action potential repolarization phase. A large number of structurally different compounds block hERG and cause a high risk of arrhythmias. Among the drugs that block hERG channel, a few compounds have been identified as hERG channel activators. Such compounds may be useful, at least in theory, for the treatment of long term QT syndrome. Here we describe a new activator of hERG channel, named MC450...
June 19, 2017: Biophysical Chemistry
https://www.readbyqxmd.com/read/28668627/vigabatrin-lacks-proarrhythmic-potential-results-from-a-thorough-qt-qtc-study-in-healthy-volunteers
#18
Dwain Tolbert, Susan Reid, Stuart Harris, Ihor Bekersky
PURPOSE: A thorough QT study was performed to assess the proarrhythmic potential of vigabatrin, an antiepileptic drug approved in the United States for the treatment of infantile spasms and refractory complex partial seizures. METHODS: In this Phase I, randomized, double-blind, placebo- and active-controlled (moxifloxacin), 4-sequence, crossover study conducted at a single center, healthy participants received 1 of 4 randomly assigned treatments: 3.0g vigabatrin solution (therapeutic dose) and 1 moxifloxacin placebo tablet; 6...
June 28, 2017: Clinical Therapeutics
https://www.readbyqxmd.com/read/28665790/effects-of-quinine-on-gastric-ulcer-healing-in-wistar-rats
#19
Olasupo Stephen Adeniyi, Olubiyi Vincent Makinde, Emmanuel Titus Friday, Samuel Babafemi Olaleye
Background Quinine (QT) is an important anti-malarial drug; however, there is little information about its effects on the gut. Therefore, this study aimed to investigate the effects of a therapeutic dose of QT on the healing of gastric ulcer in rats. Methods Male Wistar rats weighing 150-200 g were divided into three groups: control rats without ulcer (group 1), ulcerated rats treated with 1 mL/kg (p.o.) normal saline (NS) (group 2), and ulcerated rats treated with 10 mg/kg (p.o.) QT (group 3). Ulcers were induced by serosal application of 80 % acetic acid to the stomach of rats anaesthetized with 50 mg/kg thiopentone sodium and treatment was given three times daily...
June 29, 2017: Journal of Complementary & Integrative Medicine
https://www.readbyqxmd.com/read/28658794/a-comparative-study-on-clinical-and-biochemical-parameters-in-amlodipine-and-cilnidipine-treated-hypertensive-patients
#20
Kiran Shetty, Ranjan Shetty, Lakshminarayana Bairy, Pragna Rao, Amruth Kiran, Manjunath Shetty, Deepak, Vidya Nayak
INTRODUCTION: Hypertension is a major health issue worldwide. Calcium Channel Blockers (CCBs) are the most commonly used antihypertensive agents. CCBs act on voltage-dependent calcium channels and they were categorized into two subclasses, Dihydropyridine (DHP) and non-Dihydropyridine (non-DHP) derivative. Amlodipine is a third generation L-type of DHP and Cilnidipine is a novel L/N-type of DHP CCB, both drugs have excellent pharmacological profiles with the unique actions. AIM: To study the clinical and biochemical profile in Amlodipine and Cilnidipine treated mild to moderate hypertensive patients...
May 2017: Journal of Clinical and Diagnostic Research: JCDR
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