Search results for "INHIBITORS"
showing 10 items of 2336 documents
CHF2819: Pharmacological profile of a novel acetylcholinesterase inhibitor
2002
CHF2819 is a novel orally active acetylcholinesterase inhibitor (AChEI) developed for the treatment of Alzheimer's disease (AD). CHF2819 is a selective inhibitor of AChE, it is 115 times more potent against this enzyme than against butyrylcholinesterase (BuChE). Moreover, CHF2819 is more selective for inhibition of central (brain) AChE than peripheral (heart) AChE. In vivo CHF2819, 0.5, 1.5, and 4.5 mg/kg p.o., significantly and in dose-dependent manner increased acetylcholine (ACh) levels in hippocampus of young adult rats. Moreover, aging animals, with lower basal ACh levels than young adult rats, also exhibit a marked increase in hippocampal levels of this neurotransmitter after administ…
Maintenance therapy in gastro-oesophageal reflux disease.
2005
Gastro-oesophageal reflux disease (GORD) is a chronic condition. Symptom control and the maintenance of healing of erosive oesophagitis, if present, are important topics. In patients responding to a proton pump inhibitor (PPI) and showing no treatment symptoms it is appropriate to consider long-term treatment strategies, whether continuous, intermittent or on demand. Maintenance PPI therapy is well tolerated for up to 10 years of continuous use. Furthermore, tachyphylaxis does not occur during long-term maintenance PPI therapy. Previous concerns about risks of long-term PPI therapy in Heliobacter pylori-negative or H. pylori-positive patients have not materialized, while no cases of intesti…
FLT3 as a therapeutic target in AML: still challenging after all these years
2010
Abstract Mutations within the FMS-like tyrosine kinase 3 (FLT3) gene on chromosome 13q12 have been detected in up to 35% of acute myeloid leukemia (AML) patients and represent one of the most frequently identified genetic alterations in AML. Over the last years, FLT3 has emerged as a promising molecular target in therapy of AML. Here, we review results of clinical trials and of correlative laboratory studies using small molecule FLT3 tyrosine kinase inhibitors (TKIs) in AML patients. We also review mechanisms of primary and secondary drug resistance to FLT3-TKI, and from the data currently available we summarize lessons learned from FLT3-TKI monotherapy. Finally, for using FLT3 as a molecul…
Women, thrombosis, and cancer: A gender-specific analysis.
2017
Venous thromboembolism (VTE) is a major common complication in cancer patients. Risk-adapted thromboprophylaxis and antithrombotic therapy for patients diagnosed with VTE can reduce the recurrence of VTE events. Thrombotic risk varies according to cancer type, stage, and comorbidities. The current review analyzes most recent data and provides clinical guidance for the management of women with cancer-associated thrombosis.
Measurement of coagulation factors during rivaroxaban and apixaban treatment: Results from two crossover trials
2018
Abstract Background Prediction models for venous thromboembolism recurrence will likely be improved by adding levels of coagulation factors. Risk assessment is ideally performed during anticoagulant treatment, however, the influence of direct oral anticoagulants on coagulation factors is uncertain. Objective To assess the influence of rivaroxaban and apixaban on several coagulation factor levels. Methods In two crossover trials we assessed the influence of rivaroxaban and apixaban intake on factor (F)VIII, FXI and FXII‐activity and fibrinogen, von Willebrand factor (VWF:Ag), and d‐dimer levels. At three sessions with a washout period in between, blood was taken from 12 healthy male individu…
Intravenous thrombolysis for acute ischaemic stroke in patients on direct oral anticoagulants.
2018
BACKGROUND AND PURPOSE Whereas intravenous thrombolysis (IVT) is allowed for acute ischaemic stroke in patients on vitamin K antagonists with international normalized ratio ≤1.7, there are no similar recommendations for patients on direct oral anticoagulants (DOACs), notably due to the lack of coagulation tests to assess the therapeutic effects. Although the literature is scarce, consisting of small case series and retrospective studies, considering the frequency of this situation the French Vascular Neurology Society and the French Study Group on Haemostasis and Thrombosis have worked on a joint position paper to provide a practical position regarding the emergency management of ischaemic …
Statins decrease all-cause mortality only in CKD patients not requiring dialysis therapy--a meta-analysis of 11 randomized controlled trials involvin…
2013
The available studies have reported the benefits of statins on all-cause and cardiovascular mortality in chronic kidney disease (CKD) patients. However studies in end-stage renal disease patients on dialysis yielded conflicting results. Therefore, we performed a meta-analysis and provide the most reliable trial data to date on the impact of statin therapy on cardiovascular events and death from all causes in CKD patients. Data from PubMed, Web of Science, Cochrane Library, and Scopus for the years 1966 to October 2012 were searched. The final meta-analysis included 11 randomized controlled trials involving 21,295 participants with CKD. Among them 6857 were on dialysis. The use of statins in…
Chronic kidney disease and dyslipidaemia
2016
Chronic kidney disease (CKD) has to be considered as a high, or even very high risk cardiovascular risk condition, since it leads to an increase in cardiovascular mortality that continues to increase as the disease progresses. An early diagnosis of CKD is required, together with an adequate identification of the risk factors, in order to slow down its progression to more severe states, prevent complications, and to delay, whenever possible, the need for renal replacement therapy. Dyslipidaemia is a factor of the progression of CKD that increases the risk in developing atherosclerosis and its complications. Its proper control contributes to reducing the elevated cardiovascular morbidity and …
Impact of Age, Multimorbidity and Frailty on the Prescription of Preventive Antiplatelet Therapy in Older Population
2020
Platelet aggregation inhibitors (PAI) have widely proven their efficiency for the prevention of ischemic cardiovascular events. We aimed to describe PAI prescription in an elderly multimorbid population and to determine the factors that influence their prescription, including the impact of age, comorbidities and frailty, evaluated through a comprehensive geriatric assessment. This cross-sectional study included all patients admitted to the acute geriatric department of a university hospital from November 2016 to January 2017. We included 304 consecutive hospitalized patients aged 88.7 ±
INHIBITION OF CELLULAR GROWTH AND STEROID 11β-HYDROXYLATION INRAS-TRANSFORMED ADRENOCORTICAL CELLS BY THE FUNGAL TOXINS BETICOLINS
1996
Abstract The proliferation of GM16 and 4CDTras-transformed newborn rat adrenocortical (RTAC) cells and Y1 mouse adrenal tumor cells was inhibited by beticolins, the fungal toxins extracted fromCercospora beticola, at submicromolar concentrations in a dose-dependent manner. Inhibitory concentrations for half the maximum inhibition were 150, 75 and 25 n M for beticolin-1 and 230, 150 and 50 n M for beticolin-2 in GM16, 4CDT and Y1 cells respectively. Beticolins strongly inhibited the production of 11β-hydroxysteroids on the second and third days of treatment in a dose-dependent manner between 0.1 and 1 μ M . Beticolins were shown by confocal microscopy to be localized in cytoplasmic organelle…