Database : MEDLINE
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PMID:27681773
Author:Ibrahim F; Sharaf El-Din MK; El-Deen AK; Shimizu K
Address:Department of Pharmaceutical Analytical Chemistry, Faculty of Pharmacy, Mansoura University, Mansoura 35516, Egypt.
Title:Micellar HPLC Method for Simultaneous Determination of Ethamsylate and Mefenamic Acid in Presence of Their Main Impurities and Degradation Products.
Source:J Chromatogr Sci; 55(1):23-29, 2017 01.
ISSN:1945-239X
Country of publication:United States
Language:eng
Abstract:An eco-friendly sensitive, rapid and less hazardous micellar liquid chromatographic method was developed and validated for the simultaneous analysis of ethamsylate (ETM) and mefenamic acid (MFA) in the presence of hydroquinone (HQ) and 2,3-dimethylaniline (DMA) the main impurities of ETM and MFA, respectively. Good chromatographic separation was attained using Eclipse XDB-C8 column (150 mm × 4.6 mm, 5 µm particle size) adopting UV detection at 300 nm with micellar mobile phase consisting of 0.12 M sodium dodecyl sulfate, 0.3% triethylamine and 15% 2-propanol in 0.02 M orthophosphoric acid (pH 7.0) at 1.0 mL/min. The analytes were well resolved in <6.0 min, ETM (t = 1.55 min), HQ (t = 1.95 min), MFA (t = 4.55 min) and DMA (t = 5.80 min). Different validation parameters were examined as recommended by international conference on harmonization (ICH) guidelines. The method was linear over the concentration ranges of 0.5-18.0, 0.5-20.0, 0.01-0.5 and 0.02-0.2 µg/mL with limits of detection of 0.118, 0.159, 0.005 and 0.005 µg/mL and limits of quantification of 0.358, 0.482, 0.014 and 0.015 µg/mL for ETM, MFA, HQ and DMA, respectively. The suggested method was successfully applied for the determination of the two drugs in their bulk powder, laboratory-prepared mixtures, single-ingredient and co-formulated tablets. The obtained results were in accordance with those of the comparison method. The method can also detect trace amounts of HQ and DMA as the main impurities of ETM and MFA, respectively, within the BP limit (0.1%) for both impurities. Furthermore, it is a stability-indicating one for the determination of ETM in its pure form, single-component tablet and co-formulated tablets with other drugs.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Micelles); 24YL531VOH (Ethamsylate); 367589PJ2C (Mefenamic Acid)


  2 / 179 MEDLINE  
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PMID:27171802
Author:Jian-Hua W; Jie C; Lan-Fang T
Title:A 7-Year-Old Girl with Hemoptysis for 3 Days.
Source:Pediatr Ann; 45(5):e162-4, 2016 May 01.
ISSN:1938-2359
Country of publication:United States
Language:eng
Publication type:CASE REPORTS; JOURNAL ARTICLE
Name of substance:0 (Hemostatics); 24YL531VOH (Ethamsylate); YKH834O4BH (Epinephrine)


  3 / 179 MEDLINE  
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PMID:27137123
Author:Fan H; Chen K; Duan L; Wang YZ; Ju G
Address:Institute of Neurosciences, Key Laboratory of Spinal Cord Injury and Repair, Fourth Military Medical University, Xi'an, China.
Title:Beneficial effects of early hemostasis on spinal cord injury in the rat.
Source:Spinal Cord; 54(11):924-932, 2016 Nov.
ISSN:1476-5624
Country of publication:England
Language:eng
Abstract:STUDY DESIGN: Experimental study. OBJECTIVES: To investigate the effect of early hemostasis on spinal cord injury (SCI). SETTING: Fourth Military Medical University, Xi'an, China. METHODS: Sprague Dawley rats were used. Hematoxylin and eosin (HE) staining was performed to observe hemorrhage at different time points (2, 6, 12, 24 and 48 h) after SCI to determine the time window of hemostatic drug administration (n=3 per time point). Three different concentrations of Etamsylate (0.025, 0.05 and 0.1 g kg ) were administered immediately and 5 and 10 h after SCI to evaluate the effective dosage (n=6 per group). Another 82 rats were then randomly divided into two groups, Etamsylate group (0.1 g kg , n=41) and glucose control group (n=41). Nissl staining was performed to observe neurons at 10 days post injury. Immunohistochemistry, western blot and quantitative real-time PCR were performed to detect tissue necrosis at 7 d.p.i., the activation of astrocytes and microglia/macrophages and lesion cavity at 10 d.p.i. Basso-Beattie-Bresnahan scoring and rump height index assay were used to examine locomotion recovery. RESULTS: Early hemostasis reduced the lesion area and tissue necrosis, enhanced neuronal survival, alleviated the activation of microglia/macrophages and astrocytes and facilitated functional recovery after spinal cord contusion in rats. Early hemostasis decreased hemorrhage area and lesion area after spinal cord transection in rats. CONCLUSION: The present study demonstrated that early hemostasis has beneficial effects on SCI in the rat. It has the potential to be translated into clinical practice.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Aif1 protein, rat); 0 (Calcium-Binding Proteins); 0 (Glial Fibrillary Acidic Protein); 0 (Hemostatics); 0 (Microfilament Proteins); 24YL531VOH (Ethamsylate); EC 2.7.11.1 (Receptor-Interacting Protein Serine-Threonine Kinases); EC 2.7.11.1 (receptor-interacting protein 3, rat); EC 2.7.11.25 (MAP Kinase Kinase Kinases); EC 2.7.11.25 (Map3k9 protein, rat)


  4 / 179 MEDLINE  
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PMID:26643109
Author:Iwamura H; Koie T; Soma O; Matsumoto T; Imai A; Hatakeyama S; Yoneyama T; Hashimoto Y; Ohyama C
Address:Department of Urology, Hirosaki University Graduate School of Medicine, 5 Zaifucho, Hirosaki, Aomori, 036-8562, Japan. hiro_hiro388@yahoo.co.jp.
Title:Eviprostat has an identical effect compared to pollen extract (Cernilton) in patients with chronic prostatitis/chronic pelvic pain syndrome: a randomized, prospective study.
Source:BMC Urol; 15:120, 2015 Dec 07.
ISSN:1471-2490
Country of publication:England
Language:eng
Abstract:BACKGROUND: Previously reported results of a prospective, randomized placebo-controlled study showed that the pollen extract (Cernilton) significantly improved total symptoms, pain, and quality of life in patients with inflammatory prostatitis/chronic pelvic pain syndrome (CP/CPPS) without severe side effects. A phytotherapeutic agent, Eviprostat, is reportedly effective in a rat model of nonbacterial prostatitis. The aim of the present study was to compare the efficacy and safety of Eviprostat to that of the pollen extract in the management of CP/CPPS. METHODS: The patients with category III CP/CPPS were randomized to receive either oral capsules of Eviprostat (two capsules, q 8 h) or the pollen extract (two capsules, q 8 h) for 8 weeks. The primary endpoint of the study was symptomatic improvement in the NIH Chronic Prostatitis Symptom Index (NIH-CPSI). Participants were evaluated using the NIH-CPSI and the International Prostate Symptom Score (IPSS) at baseline and after 4 and 8 weeks. RESULTS: In the intention-to-treat analysis, 100 men were randomly allocated to Eviprostat (n = 50) or the pollen extract (n = 50). Response (defined as a decrease in the NIH-CPSI total score by at least 25 %) in the Eviprostat group and the pollen extract group was 88.2 and 78.1 %, respectively. There was no significant difference in the total, pain, urinary, and quality of life (QOL) scores of the NIH-CPSI between the two groups at 8 weeks. This was also the case with the total, voiding, and storage symptoms of the IPSS. There were no severe adverse events observed in any patients in this study. CONCLUSION: Both the pollen extract and Eviprostat significantly reduced the symptoms of category III CP/CPPS without any adverse events. Eviprostat may have an identical effect on category III CP/CPPS compared the pollen extract. TRIAL REGISTRATION: The study was registered with the University Hospital Medical Information Network Clinical Trials Registry in Japan (UMIN000019618); registration date: 3 November 2015.
Publication type:JOURNAL ARTICLE; RANDOMIZED CONTROLLED TRIAL
Name of substance:0 (Drug Combinations); 0 (Plant Extracts); 24YL531VOH (Ethamsylate); 59738-67-9 (eviprostat); 8054-43-1 (cernilton)


  5 / 179 MEDLINE  
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PMID:26291043
Author:Zawrotniak M; Kozik A; Rapala-Kozik M
Address:Department of Analytical Biochemistry, Faculty of Biochemistry, Biophysics and Biotechnology, Jagiellonian University in Kraków, Kraków, Poland.
Title:Selected mucolytic, anti-inflammatory and cardiovascular drugs change the ability of neutrophils to form extracellular traps (NETs).
Source:Acta Biochim Pol; 62(3):465-73, 2015.
ISSN:1734-154X
Country of publication:Poland
Language:eng
Abstract:Neutrophils form the first line of host defense against infections that combat pathogens using two major mechanisms, the phagocytosis or the release of neutrophil extracellular traps (NETs). The netosis (NET formation) exerts additional, unfavorable effects on the fitness of host cells and is also involved at the sites of lung infection, increasing the mucus viscosity and in the circulatory system where it can influence the intravascular clot formation. Although molecular mechanisms underlying the netosis are still incompletely understood, a role of NADPH oxidase that activates the production of reactive oxygen species (ROS) during the initiation of NETs has been well documented. Since several commonly used drugs can affects the netosis, our current study was aimed to determine the effects of selected mucolytic, anti-inflammatory and cardiovascular drugs on NET formation, with a special emphasis on ROS production and NADPH oxidase activity. The treatment of neutrophils with N-acetylcysteine, ketoprofen and ethamsylate reduced the production of ROS by these cells in a dose-dependent manner. NET formation was also modulated by selected drugs. N-acetylcysteine inhibited the netosis but in the presence of H2O2 this neutrophil ability was restored, indicating that N-acetylcysteine may influence the NET formation by modulating ROS productivity. The administration of ethamsylate led to a significant reduction in NET formation and this effect was not restored by H2O2 or S. aureus, suggesting the unexpected additional side effects of this drug. Ketoprofen seemed to promote ROS-independent NET release, simultaneously inhibiting ROS production. The results, obtained in this study strongly suggest that the therapeutic strategies applied in many neutrophil-mediated diseases should take into account the NET-associated effects.
Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Name of substance:0 (Anti-Inflammatory Agents); 0 (Cardiovascular Agents); 0 (Reactive Oxygen Species); 24YL531VOH (Ethamsylate); 90Y4QC304K (Ketoprofen); 95QN29S1ID (Clemastine); BBX060AN9V (Hydrogen Peroxide); EC 1.6.3.- (NADPH Oxidases); WYQ7N0BPYC (Acetylcysteine)


  6 / 179 MEDLINE  
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PMID:23968273
Author:Kuperman AA; Brenner B; Kenet G
Address:a Pediatric Hematology Clinic, Thrombosis and Hemostasis Service, Institute of Hematology, Western Galilee Hospital , Naharriya , Israel .
Title:Intraventricular haemorrhage in preterm infants--can we improve outcome by addressing coagulation?
Source:J Matern Fetal Neonatal Med; 28 Suppl 1:2265-7, 2015 Nov.
ISSN:1476-4954
Country of publication:England
Language:eng
Abstract:During the last few decades, the survival of preterm infants has increased dramatically. Nevertheless, with the increasing number of very young and extremely low birth weight infants, morbidity is still a major problem. Intraventricular Haemorrhage (IVH) is a major complication of preterm birth, and large haemorrhages or haemorrhages associated with parenchymal brain lesions may yield a high rate of future disability. IVH is a complex, multi-factorial disorder. Prematurity and low birth weight remain as its most important risk factors, affecting vulnerability of the germinal matrix as well as the coagulation system. Approximately 80% of IVHs occur by 72 h after birth, but a considerable proportion of IVH is already visible on the first cranial ultrasound scan within a few hours of birth. The hypothesis that a severe coagulation deficiency in the premature newborn could be a major contributing factor to IVH has been suggested, and small open label interventional studies targeting the premature coagulation system have been conducted with ethamsylate, vitamin K, fresh frozen plasma, recombinant activated factor VII and prothrombin complex concentrate. The outcome of these studies will be reviewed.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Blood Coagulation Factors); 0 (Hemostatics); 0 (Recombinant Proteins); 12001-79-5 (Vitamin K); 24YL531VOH (Ethamsylate); 37224-63-8 (prothrombin complex concentrates); AC71R787OV (recombinant FVIIa); EC 3.4.21.21 (Factor VIIa)


  7 / 179 MEDLINE  
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PMID:25589317
Author:Kaplunov OA; Mikhin IV; Biriukov SN
Title:[Blood loss during total knee-joint replacement: a combination of anticoagulant and hemostatic techniques].
Source:Khirurgiia (Mosk); (12):41-5, 2014.
ISSN:0023-1207
Country of publication:Russia (Federation)
Language:rus
Publication type:JOURNAL ARTICLE
Name of substance:0 (Anticoagulants); 0 (Antifibrinolytic Agents); 0 (Hemostatics); 24YL531VOH (Ethamsylate); 6T84R30KC1 (Tranexamic Acid)


  8 / 179 MEDLINE  
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PMID:25185424
Author:Dastych M; Wiewiorka O; Benovská M
Title:Ethamsylate (Dicynone) interference in determination of serum creatinine, uric acid, triglycerides, and cholesterol in assays involving the Trinder reaction; in vivo and in vitro.
Source:Clin Lab; 60(8):1373-6, 2014.
ISSN:1433-6510
Country of publication:Germany
Language:eng
Abstract:BACKGROUND: The aim of our research was the quantification of interfering properties of the haemostatic drug Dicynone (ethamsylate) in serum creatinine, uric acid, cholesterol, and triglyceride assays using the Trinder reaction. METHODS: Blood from patients was collected before and 15 minutes after administration of 500 mg Dicynone dose i.v. and the above mentioned analytes were quantified using Roche assays (Cobas 8000). In our in vitro experiment, we measured concentrations of the analytes in pooled serum aliquots with final concentrations of Dicynone additions 0, 30, 60, 150, and 300 mg/L. Aliquots with 60 mg/L Dicynone were also measured at 2, 6, and 8 hours after initial measurement when stored in 22 degrees C and 4 degrees C for comparison. RESULTS: Concentrations of the measured analytes in samples from patients administered with a 500 mg dose of Dicynone were lower in all cases (n = 10) when compared to values in samples taken immediately before treatment. The in vitro samples showed that considerable negative interference occurred even with the low concentrations of Dicynone additions (30 and 60 mg/L), showing the strongest negative interference in creatinine values, followed by uric acid, triglycerides, and cholesterol. Using in vitro samples, we showed strong time and temperature dependence on Dicynone interference. CONCLUSIONS: We found and proved significant negative interference of the drug Dicynone (ethamsylate) in the clinical analysis of blood using in vivo and in vitro experiments. Furthermore, we observed a change of this effect in serum matrix over time and at different storage temperatures.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Triglycerides); 24YL531VOH (Ethamsylate); 268B43MJ25 (Uric Acid); 97C5T2UQ7J (Cholesterol); AYI8EX34EU (Creatinine)


  9 / 179 MEDLINE  
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PMID:24581515
Author:Shibuya S; Xia Z; Sugimoto M; Ueda N; Haba R; Kakehi Y
Address:Department of Diagnostic Pathology, Faculty of Medicine, Kagawa University, Kagawa, Japan.
Title:The phytotherapeutic agent, eviprostat, suppresses stromal proliferation and inflammation even after establishment of nonbacterial prostatitis in the rat prostate.
Source:Urology; 83(3):528-34, 2014 Mar.
ISSN:1527-9995
Country of publication:United States
Language:eng
Abstract:OBJECTIVE: To evaluate the effect of phytotherapeutic agent, Eviprostat, administered after the establishment of nonbacterial prostatitis (NBP) on the stroma-to-epithelium ratio (S/E ratio), inflammatory scores, tissue macrophage infiltration, and cytokines and chemokines levels in prostate tissue and urine. MATERIALS AND METHODS: Ten-month-old male Wistar rats were castrated and exposed to 17-beta-isomer of estradiol for 30 days to induce NBP. Twenty-five NBP rats were divided into 5 groups: (1) NBP (0) rats sacrificed immediately after the establishment of NBP; (2,3) NBP (30)/control (CTL) and NBP (30)/Eviprostat (EVI) rats fed without or with 0.1% Eviprostat under estradiol-free for 30 days, respectively; and (4,5) NBP (60)/CTL and NBP (60)/EVI rats fed without or with 0.1% Eviprostat under estradiol-free for 60 days, respectively. The S/E ratio, inflammatory scores, and the number of macrophage infiltration in the prostate were assessed. Concentrations of cytokines and chemokines in prostatic tissue and urine were measured by enzyme-linked immunosorbent assay. RESULTS: The S/E ratio was significantly increased with time until 60 days under estradiol-free condition (P <.001). The S/E ratio and the inflammatory scores in NBP (60)/EVI was significantly lower than that of NBP (60)/CTL (P <.001, and P = .022, respectively). The mean tissue concentration of chemokine ligand 2 (CCL2)/monocyte chemoattractant protein-1 (MCP-1) in NBP (60)/CTL was significantly higher than that in NBP (0) (P = .016), whereas, there was no difference between NBP (60)/EVI and NBP (0). Furthermore, urinary CCL2/MCP-1 was significantly decreased in NBP (60)/EVI as compared with NBP (0) (P = .028). CONCLUSION: Eviprostat suppresses the stromal proliferation and inflammation in the rat prostate after the establishment of NBP at least partly owing to inhibitory effect on CCL2/MCP-1 production in the prostate.
Publication type:JOURNAL ARTICLE
Name of substance:0 (Chemokine CCL2); 0 (Chemokine CCL3); 0 (Chemokine CXCL1); 0 (Chemokines); 0 (Drug Combinations); 0 (Interleukin-1beta); 0 (Plant Extracts); 0 (Urological Agents); 24YL531VOH (Ethamsylate); 4TI98Z838E (Estradiol); 59738-67-9 (eviprostat)


  10 / 179 MEDLINE  
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PMID:24352866
Author:Rao H; Zhang J; Li J
Address:College of Chemistry, Chemical Engineering & Materials Science, Soochow University, Suzhou, 215123, China; The Key Lab of Health Chemistry & Molecular Diagnosis of Suzhou, Suzhou, 215123, China.
Title:Highly sensitive electrochemiluminescence determination of etamsylate using a low-cost electrochemical flow-through cell based on a tris(2, 2'-bipyridyl)ruthenium(II)-Nafion-modified carbon paste electrode.
Source:Luminescence; 29(7):784-90, 2014 Nov.
ISSN:1522-7243
Country of publication:England
Language:eng
Abstract:A simple and sensitive electrochemiluminescence (ECL) method for the determination of etamsylate has been developed by coupling an electrochemical flow-through cell with a tris(2,2'-bipyridyl)ruthenium(II) (Ru(bpy)3(2+))-Nafion-modified carbon electrode. It is based on the oxidized Ru(bpy)3(2+) on the electrode surface reacting with etamsylate and producing an excellent ECL signal. Under optimized experimental conditions, the proposed method allows the measurement of etamsylate over the range of 8-1000 ng/mL with a correlation coefficient of r = 0.9997 (n = 7) and a limit of detection of 1.57 ng/mL (3σ), the relative standard deviation (RSD) for 1000 ng/mL etamsylate (n = 7) is 0.96%. The immobilized Ru(bpy)3(2+) carbon paste electrode shows good electrochemical and photochemical stability. This method is rapid, simple, sensitive and has good reproducibility. It has been successfully applied to the determination of the studied etamsylate in pharmaceutical preparations with satisfactory results. The possible ECL reaction mechanism has also been discussed.
Publication type:JOURNAL ARTICLE; RESEARCH SUPPORT, NON-U.S. GOV'T
Name of substance:0 (Fluorocarbon Polymers); 0 (Organometallic Compounds); 0 (tris(2,2'-bipyridyl)ruthenium(II)); 24YL531VOH (Ethamsylate); 39464-59-0 (perfluorosulfonic acid); 7440-44-0 (Carbon)



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