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Intravenous proton pump inhibitors vs oral potassium competitive acid blockers before endoscopic treatment of bleeding peptic ulcers
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作者 Na Rae Lim Woo Chul Chung 《World Journal of Gastrointestinal Endoscopy》 2025年第6期64-73,共10页
BACKGROUND The use of proton pump inhibitors(PPIs)with the intent of reducing gastric acidity to the desired therapeutic level for treating bleeding peptic ulcer still has several limitations.AIM To compare intravenou... BACKGROUND The use of proton pump inhibitors(PPIs)with the intent of reducing gastric acidity to the desired therapeutic level for treating bleeding peptic ulcer still has several limitations.AIM To compare intravenous PPIs and oral potassium competitive acid blockers(PCABs)administered prior to endoscopic treatment of bleeding peptic ulcers.METHODS This retrospective study involved 105 consecutive patients with non-variceal upper gastrointestinal bleeding(treated August 2023 to February 2024).Prior to emergency endoscopy,patients received either intravenous PPI(pantoprazole 80 mg bolus)or oral PCAB(tegoprazan 50 mg single-dose).Severity of bleeding was assessed using the Glasgow-Blatchford,Rockall,and AIMS65 scoring systems.Patients with severe comorbidities were excluded.Primary outcomes included need for therapeutic endoscopic intervention and occurrence of re-bleeding.Multivariate logistic regression was performed to adjust for potential confounding factors.RESULTS Total of the 105 patients,61 received intravenous PPI injection and 44 received oral PCAB prior to emergency endoscopy.To minimize selection bias,bleeding severity was assessed using the Glasgow-Blatchford,Rockall and AIMS65 scores,with no statistically significant differences observed between the two groups.During emergency endoscopy performed within 48 hours,ulcer bed status was classified according to the Forrest classification.The proportion of lesions graded IIa or higher was significantly lower in the PCAB group(P<0.001),as was the frequency of therapeutic endoscopy intervention(odds ratio=0.272,95%confidence interval:0.111-0.665,P=0.004).The frequency of re-bleeding events was statistically significantly higher in the PPI group(odds ratio=0.141,95%confidence interval:0.024-0.844,P=0.032).CONCLUSION Pre-endoscopic PCAB administration is more effective than PPI injection for upper gastrointestinal bleeding and may reduce ulcer bleeding mortality. 展开更多
关键词 Peptic ulcer Bleeding Proton pump inhibitor Potassium competitive acid blocker Ulcer bleeding
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Treatment of Helicobacter pylori with potassium competitive acid blockers:A systematic review and meta-analysis 被引量:2
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作者 Joseph Edwin Kanu Jonathan Soldera 《World Journal of Gastroenterology》 SCIE CAS 2024年第9期1213-1223,共11页
BACKGROUND Helicobacter pylori(H.pylori)infects over half the global population,causing gastrointestinal diseases like dyspepsia,gastritis,duodenitis,peptic ulcers,GMALT lymphoma,and gastric adenocarcinoma.Eradicating... BACKGROUND Helicobacter pylori(H.pylori)infects over half the global population,causing gastrointestinal diseases like dyspepsia,gastritis,duodenitis,peptic ulcers,GMALT lymphoma,and gastric adenocarcinoma.Eradicating H.pylori is crucial for treating and preventing these conditions.While conventional proton pump inhibitor(PPI)-based triple therapy is effective,there’s growing interest in longer acid suppression therapies.Potassium competitive acid blocker(P-CAB)triple and dual therapy are new regimens for H.pylori eradication.Initially used in Asian populations,vonoprazan(VPZ)has been recently Food and Drug Administration-approved for H.pylori eradication.AIM To assess the efficacy of regimens containing P-CABs in eradicating H.pylori infection.METHODS This study,following PRISMA 2020 guidelines,conducted a systematic review and meta-analysis by searching MEDLINE and Scopus libraries for randomized clinical trials(RCTs)or observational studies with the following command:[("Helicobacter pylori"OR"H pylori")AND("Treatment"OR"Therapy"OR"Eradication")AND("Vonaprazan"OR"Potassium-Competitive Acid Blocker"OR"P-CAB"OR"PCAB"OR"Revaprazan"OR"Linaprazan"OR"Soraprazan"OR"Tegoprazan")].Studies comparing the efficacy of P-CABs-based treatment to classical PPIs in eradicating H.pylori were included.Exclusion criteria included case reports,case series,unpublished trials,or conference abstracts.Data variables encompassed age,diagnosis method,sample sizes,study duration,intervention and control,and H.pylori eradication method were gathered by two independent reviewers.Meta-analysis was performed in R software,and forest plots were generated.RESULTS A total of 256 references were initially retrieved through the search command.Ultimately,fifteen studies(7 RCTs,7 retrospective observational studies,and 1 comparative unique study)were included,comparing P-CAB triple therapy to PPI triple therapy.The intention-to-treat analysis involved 8049 patients,with 4471 in the P-CAB intervention group and 3578 in the PPI control group across these studies.The analysis revealed a significant difference in H.pylori eradication between VPZ triple therapy and PPI triple therapy in both RCTs and observational studies[risk ratio(RR)=1.17,95%confidence interval(CI):1.11-1.22,P<0.0001]and(RR=1.13,95%CI:1.09-1.17,P<0.0001],respectively.However,no significant difference was found between tegoprazan(TPZ)triple therapy and PPI triple therapy in both RCTs and observational studies(RR=1.04,95%CI:0.93-1.16,P=0.5)and(RR=1.03,95%CI:0.97-1.10,P=0.3),respectively.CONCLUSION VPZ-based triple therapy outperformed conventional PPI-based triple therapy in eradicating H.pylori,positioning it as a highly effective first-line regimen.Additionally,TPZ-based triple therapy was non-inferior to classical PPI triple therapy. 展开更多
关键词 Helicobacter pylori infection Potassium competitive acid blockers Proton pump inhibitors Vonoprazan AMOXICILLIN
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A 3D-QSAR Study on a Novel Chromanol Class of I_ (Ks) Potassium Channel Blockers
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作者 杜吕佩 李敏勇 +1 位作者 夏霖 尤启冬 《Journal of Chinese Pharmaceutical Sciences》 CAS 2005年第2期89-94,共6页
Aim and Method A novel three-dimensional quantitative structure-activityrelationship (3D-QSAR) method, self-organizing molecular field analysis (SOMFA) , was used toinvestigate the correlation between the molecular pr... Aim and Method A novel three-dimensional quantitative structure-activityrelationship (3D-QSAR) method, self-organizing molecular field analysis (SOMFA) , was used toinvestigate the correlation between the molecular properties and a class of chromanol analogs asI_(Ks) blockers. Results The cross-validated correlation coefficient q^2 values (0.698) and noncross-validated correlation coefficient r^2 values (0.701) proved a good conventional statisticalcorrelation. Conclusion The final SOMFA model has therefore good predictive activity for the furthermolecular design of chromanol I_(Ks) potassium channel blockers. 展开更多
关键词 quantitative structure-activity relationship self-organizing molecular fieldanalysis I_(Ks) potassium channel blockers chromanol analogs
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Potassium-competitive acid blockers-are they the next generation of proton pump inhibitors? 被引量:5
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作者 Prashanth Rawla Tagore Sunkara +1 位作者 Andrew Ofosu Vinaya Gaduputi 《World Journal of Gastrointestinal Pharmacology and Therapeutics》 CAS 2018年第7期63-68,共6页
The modern lifestyle caters to an increase in the incidence of peptic ulcer disease,gastroesophageal reflux disease and several other acid-related conditions of the gut. The drugs to prevent these conditions work eith... The modern lifestyle caters to an increase in the incidence of peptic ulcer disease,gastroesophageal reflux disease and several other acid-related conditions of the gut. The drugs to prevent these conditions work either through H2 receptor blockade or inhibition of the H^+, K^+ ATPase enzyme. Although proton pump inhibitors have been proven to be efficacious, they have a slow onset of action with limited resolution of symptoms in most patients. Potassium-competitive acid blockers(P-CABs) are novel drugs that bind reversibly to K^+ ions and block the H^+, K^+ ATPase enzyme, thus preventing acid production. P-CABs have a fast onset of action and have dose-dependent effects on acid production. Animal studies exist that differentiate the better results of P-CABs from proton pump inhibitors; further human trials will give a comprehensive picture of the results and will help to elucidate the therapeutic benefits of this new group of drugs. 展开更多
关键词 Potassium-competitive ACID blockers Gastroesophageal reflux DISEASE Proton pump inhibitors PEPTIC ulcer DISEASE Vonoprazan
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Rethinking the role of non-selective beta blockers in patients with cirrhosis and portal hypertension 被引量:3
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作者 Alberto Ferrarese Alberto Zanetto +2 位作者 Giacomo Germani Patrizia Burra Marco Senzolo 《World Journal of Hepatology》 CAS 2016年第24期1012-1018,共7页
Non-selective beta blockers(NSBB) are commonly used to prevent portal hypertensive bleeding in cirrhotics.Nevertheless, in the last years, the use of NSBB in critically decompensated patients, especially in those with... Non-selective beta blockers(NSBB) are commonly used to prevent portal hypertensive bleeding in cirrhotics.Nevertheless, in the last years, the use of NSBB in critically decompensated patients, especially in those with refractory ascites, has been questioned, mainly for an increased risk of mortality and worsening of systemic hemodynamics. Moreover, even if NSBB have been reported to correlate with a higher risk of renal failure and severe infection in patients with advanced liver disease and hypotension, their use has been associated with a reduction of risk of spontaneous bacterial peritonitis, modification of gut permeability and reduction of bacterial translocation. This manuscript systematically reviews the published evidences about harms and benefits of the use of NSBB in patients with decompensated cirrhosis. 展开更多
关键词 Beta blockers ASCITES CIRRHOSIS PORTAL HYPERTENSION
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Potential protective role of ACE-inhibitors and AT1 receptor blockers against levodopa-induced dyskinesias:a retrospective case-control study 被引量:2
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作者 Elena Contaldi Luca Magistrelli +3 位作者 Anna VMilner Marco Cosentino Franca Marino Cristoforo Comi 《Neural Regeneration Research》 SCIE CAS CSCD 2021年第12期2475-2478,共4页
Growing evidence has highlighted that angiotensin-converting enzyme(ACE)-inhibitors(ACEi)/AT1 receptor blockers(ARBs)may influence the complex interplay between dopamine and the renin-angiotensin system in the nigrost... Growing evidence has highlighted that angiotensin-converting enzyme(ACE)-inhibitors(ACEi)/AT1 receptor blockers(ARBs)may influence the complex interplay between dopamine and the renin-angiotensin system in the nigrostriatal pathway,thus affecting the development of levodopa-induced dyskinesia in Parkinson’s disease(PD).In the present study,we analyzed whether the use of this class of medication was associated with a reduced occurrence of levodopa-induced dyskinesia,using electronically-stored information of idiopathic PD patients enrolled at Novara University Hospital“Maggiore della Carità”.We conducted a retrospective case-control study identifying PD patients with dyskinesias(PwD;n=47)as cases.For each PwD we selected a non-dyskinetic control(NoD),nearly perfectly matched according to sex,Unified Parkinson’s Disease Rating Scale(UPDRS)part III score,and duration of antiparkinsonian treatment.Binary logistic regression was used to evaluate whether dyskinesias were associated with ACEi/ARBs use.Ninety-four PD patients were included,aged 72.18±9 years,with an average disease duration of 10.20±4.8 years and 9.04±4.9 years of antiparkinsonian treatment.The mean UPDRS part III score was 18.87±7.6 and the median HY stage was 2.In the NoD group,25(53.2%)were users and 22(46.8%)non-users of ACEi/ARBs.Conversely,in the PwD group,11(23.4%)were users and 36 non-users(76.6%)of this drug class(Pearson chi-square=8.824,P=0.003).Concerning general medication,there were no other statistically significant differences between groups.After controlling for tremor dominant phenotype,levodopa equivalent daily dose,HY 3-4,and disease duration,ACEi/ARBs use was a significant predictor of a lower occurrence of dyskinesia(OR=0.226,95%CI:0.080-0.636,P=0.005).Therefore,our study suggests that ACEi/ARBs may reduce levodopa-induced dyskinesia occurrence and,thanks to good tolerability and easy management,represent a feasible choice when dealing with the treatment of hypertension in PD patients.The study was approved by the Ethics Committee of Novara University Hospital“Maggiore della Carità”(CE 65/16)on July 27,2016. 展开更多
关键词 angiotensin-converting enzyme inhibitors AT1 receptor blockers DYSKINESIAS hypertension LEVODOPA motor complications NEUROINFLAMMATION Parkinson’s disease renin-angiotensin system
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Role of angiotensin-converting enzyme inhibitors and angiotensin receptor blockers in cryoballoon ablation outcomes for paroxysmal atrial fibrillation 被引量:3
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作者 Ibragim Al-Seykal Abhishek Bose +4 位作者 Parag A Chevli Zeba Hashmath Nitish Sharma Ajay K Mishra Douglas Laidlaw 《World Journal of Cardiology》 2022年第10期537-545,共9页
BACKGROUND Cryoballoon ablation(CBA)is recommended for patients with paroxysmal atrial fibrillation(AF)refractory to antiarrhythmic drugs.However,only 80%of patients benefit from initial CBA.There is growing evidence ... BACKGROUND Cryoballoon ablation(CBA)is recommended for patients with paroxysmal atrial fibrillation(AF)refractory to antiarrhythmic drugs.However,only 80%of patients benefit from initial CBA.There is growing evidence that pretreatment with angiotensin-converting enzyme inhibitors(ACEIs)and angiotensin receptor blockers(ARBs)decreases the recurrence of AF postablation,particularly in nonparoxysmal AF undergoing radiofrequency ablation.The role of ACEIs and ARBs in patients with paroxysmal AF in CBA remains unknown.We decided to investigate the role of ACEIs and ARBs in preventing the recurrence of atrial arrhythmia(AA)following CBA for paroxysmal AF.AIM To investigate the role of ACEIs and ARBs in preventing recurrence of AA following CBA for paroxysmal AF.METHODS We followed 103 patients(age 60.6±9.1 years,29%women)with paroxysmal AF undergoing CBA 1-year post procedure.Recurrence was assessed by documented AA on electrocardiogram or any form of long-term cardiac rhythm monitoring.A multivariable Cox proportional hazard model was used to assess if ACEI or ARB treatment predicted the risk of AA recurrence.RESULTS After a 1-year follow-up,19(18.4%)participants developed recurrence of AA.Use of ACEI or ARB therapy was noted in the study population.Patients on ACEI/ARB had a greater prevalence of hypertension and coronary artery disease.On a multivariate model adjusted for baseline demographics and risk factors for AF,ACEI or ARB therapy did not prevent recurrence of AA following CBA(P=0.72).Similarly,on Kaplan–Meier analysis pretreatment with ACEI/ARB did not predict the time to first recurrence of AA(P=0.2173).CONCLUSION In our study population,preablation treatment with an ACEI or ARB had no influence on the recurrence of AA following CBA for paroxysmal AF. 展开更多
关键词 Angiotensin-converting enzyme inhibitors Angiotensin receptor blockers Paroxysmal atrial fibrillation Cryoballoon ablation OUTCOME
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Hyperkalemia of Angiotensin-converting Enzyme Inhibitors or Angiotensin Receptor Blockers in Hemodialysis: A Meta-analysis 被引量:1
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作者 张茜 栾弘 +4 位作者 王艻 张妙 陈艳 吕永曼 马祖福 《Journal of Huazhong University of Science and Technology(Medical Sciences)》 SCIE CAS 2012年第5期785-792,共8页
The safety of angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin receptor blockers (ARBs) used in hemodialysis (HD) patients was evaluated.Medline,Embase,the Cochrane Library,some databases of clinical tr... The safety of angiotensin-converting enzyme inhibitors (ACEIs) or angiotensin receptor blockers (ARBs) used in hemodialysis (HD) patients was evaluated.Medline,Embase,the Cochrane Library,some databases of clinical trial registries,grey literatures,other reference lists of eligible articles and review articles for the randomized clinical trials (RCTs) on comparison of ACEIs/ARBs or placebo in HD patients were retrieved.RCTs reporting the risk of hyperkalemia by using ACEIs/ARBs in HD patients were selected.Eight articles met the eligibility criteria and were subjected to meta-analysis by using the Cochrane Collaboration’s RevMan 4.2 software package.The results showed that there was no significant difference in hyperkalemia in HD patients between ACEIs or ARBs group and control group (ACEIs vs.control:RD=0.03,95% CI=-0.13?0.18,Z=0.34,P=0.73;ARBs vs.control:RD=-0.02,95% CI=-0.07?0.03,Z=0.75,P=0.45).However,there was no significant difference in the serum potassium between ACEIs or ARBs group and control group in HD patients (ACEIs vs.control:WMD=0.10,95% CI=0.06?0.15,Z=4.64,P<0.00001;ARBs vs.control:WMD=-0.24,95% CI=-0.37--0.11,Z=3.58,P=0.0003).The use of ACEIs or ARBs could not cause an increased risk of hyperkalemia in HD patients,however the serum potassium could be increased with use of ACEIs in HD patients.Therefore the serum potassium concentration should still be closely monitored when ACEIs are taken during the maintenance HD. 展开更多
关键词 angiotensin-converting enzyme inhibitors angiotensin receptor blockers HYPERKALEMIA META-ANALYSIS
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Angiotensin converting enzymes inhibitors or angiotensin receptor blockers should be continued in COVID-19 patients with hypertension 被引量:1
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作者 Ci Tian Nan Li +5 位作者 Yi Bai Han Xiao Shu Li Qing-Gang Ge Ning Shen Qing-Bian Ma 《World Journal of Clinical Cases》 SCIE 2021年第1期47-60,共14页
BACKGROUND Recent studies have revealed that sustained ingestion of angiotensin converting enzymes inhibitors or angiotensin receptor blockers(ACEIs/ARBs)had no harmful effects on coronavirus disease 2019(COVID-19)pat... BACKGROUND Recent studies have revealed that sustained ingestion of angiotensin converting enzymes inhibitors or angiotensin receptor blockers(ACEIs/ARBs)had no harmful effects on coronavirus disease 2019(COVID-19)patients complicated with hypertension.AIM To investigate the impact on COVID-19 patients complicated with hypertension who discontinued using ACEIs/ARBs.METHODS All COVID-19 patients complicated with hypertension admitted to our isolated unit were consecutively recruited in this study.Some patients switched from ACEIs/ARBs to calcium channel blocker(CCBs)after admission,while others continued using non-ACEIs/ARBs.We compared characteristics and clinical outcomes between these two groups of patients.RESULTS A total of 53 patients were enrolled,27 patients switched from ACEIs/ARBs to CCBs while 26 patients continued with non-ACEIs/ARBs.After controlling potential confounding factors using the Cox proportional hazards model,hospital stay was longer in patients who discontinued ACEIs/ARBs,with a hazard ratio of 0.424(95%confidence interval:0.187-0.962;P=0.040),upon discharge than patients using other anti-hypertensive drugs.A sub-group analysis showed that the effect of discontinuing use of ACEIs/ARBs was stronger in moderate cases[hazard ratio=0.224(95%confidence interval:0.005-0.998;P=0.0497)].CONCLUSION Patients in the discontinued ACEIs/ARBs group had longer hospital stays.Our findings suggest that COVID-19 patients complicated with hypertension should continue to use ACEIs/ARBs. 展开更多
关键词 COVID-19 HYPERTENSION Angiotensin converting enzymes inhibitors Angiotensin receptor blockers Angiotensin-converting enzyme-2 PROGNOSIS
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Effects of angiotensin receptor blockers and angiotensin-converting enzyme inhibitors on COVID-19 被引量:1
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作者 Xiao-Long Li Tao Li +2 位作者 Qi-Cong Du Li Yang Kun-Lun He 《World Journal of Clinical Cases》 SCIE 2021年第20期5462-5469,共8页
BACKGROUND The World Health Organization reported that 28637952 people worldwide had been infected with severe acute respiratory syndrome coronavirus 2,the causative agent of coronavirus disease 2019(COVID-19),by Sept... BACKGROUND The World Health Organization reported that 28637952 people worldwide had been infected with severe acute respiratory syndrome coronavirus 2,the causative agent of coronavirus disease 2019(COVID-19),by September 13.AIM The aim was to investigate whether long-term use of renin-angiotensin-aldosterone system(RAAS)inhibitors for the treatment of hypertension aggravates the performance of COVID-19 patients with hypertension.METHODS This was a retrospective analysis of lung computed tomography(CT)data and laboratory values of COVID-19 patients with hypertension who were admitted to Huoshenshan Hospital,Wuhan,Hubei Province,between February 18 and March 31,2020.Patients were divided into two groups.Group A included 19 people who were long-term users of RAAS inhibitors for hypertension;and group B included 28 people who were randomly selected from the database and matched with group A by age,sex,basic diseases,and long-term use of other antihypertensive drugs.All patients underwent a series of CT and laboratory tests.We compared the most severe CT images of the two groups and the laboratory examination results within 2 d of the corresponding CT images.RESULTS The time until the most severe CT images from the onset of COVID-19 was 30.37±14.25 d group A and 26.50±11.97 d in group B.The difference between the two groups was not significant(t=1.01,P=0.32).There were no significant differences in blood laboratory values,C-reactive protein,markers of cardiac injury,liver function,or kidney function between the two groups.There was no significant difference in the appearance of the CT images between the two groups.The semiquantitative scores of each involved lobe were 11.84±5.88 in group A and 10.36±6.04 group B.The difference was not significantly different(t=0.84,P=0.41).CONCLUSION Chest CT is an important imaging tool to monitor the characteristics of COVID-19 and the degree of lung injury.Chronic use of RAAS inhibitors is not related to the severity of COVID-19,and it does not worsen the clinical process. 展开更多
关键词 COVID-19 infection Hypertensive patients Angiotensin-converting enzyme inhibitors Angiotensin receptor blockers
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Renin-angiotensin system blockers-SGLT2 inhibitorsmineralocorticoid receptor antagonists in diabetic kidney disease:A tale of the past two decades! 被引量:1
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作者 Awadhesh Kumar Singh Ritu Singh 《World Journal of Diabetes》 SCIE 2022年第7期471-481,共11页
Several pharmacological agents to prevent the progression of diabetic kidney disease(DKD)have been tested in patients with type 2 diabetes mellitus(T2DM)in the past two decades.With the exception of renin-angiotensin ... Several pharmacological agents to prevent the progression of diabetic kidney disease(DKD)have been tested in patients with type 2 diabetes mellitus(T2DM)in the past two decades.With the exception of renin-angiotensin system blockers that have shown a significant reduction in the progression of DKD in 2001,no other pharmacological agent tested in the past two decades have shown any clinically meaningful result.Recently,the sodium-glucose cotransporter-2 inhibitor(SGLT-2i),canagliflozin,has shown a significant reduction in the composite of hard renal and cardiovascular(CV)endpoints including progression of end-stage kidney disease in patients with DKD with T2DM at the top of reninangiotensin system blocker use.Another SGLT-2i,dapagliflozin,has also shown a significant reduction in the composite of renal and CV endpoints including death in patients with chronic kidney disease(CKD),regardless of T2DM status.Similar positive findings on renal outcomes were recently reported as a top-line result of the empagliflozin trial in patients with CKD regardless of T2DM.However,the full results of this trial have not yet been published.While the use of older steroidal mineralocorticoid receptor antagonists(MRAs)such as spironolactone in DKD is associated with a significant reduction in albuminuria outcomes,a novel non-steroidal MRA finerenone has additionally shown a significant reduction in the composite of hard renal and CV endpoints in patients with DKD and T2DM,with reasonably acceptable side effects. 展开更多
关键词 Renin-angiotensin system blockers SGLT-2 inhibitors Mineralocorticoid receptor antagonist Diabetic kidney disease Chronic kidney disease Renal outcomes Cardiovascular outcomes
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THE PROTECTIVE EFFECT OF Na^+ CHANNEL BLOCKERS AGAINST CELL DAMAGE CAUSED BY ISCHEMIA 被引量:1
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作者 Zhu Zhongliang, Li Hui, Fan Xiaoli et al(Department of Physiology, Xi’an Medical University)$$$$ 《Journal of Pharmaceutical Analysis》 CAS 1999年第2期156-156,共1页
In order to observe it blockers of sodium channel obsesses the neuroprotective effect on hippocampal CA 1 pyramidal cell under the condition of transient brain ischemia, the present experiment used 24 male Wistar rat... In order to observe it blockers of sodium channel obsesses the neuroprotective effect on hippocampal CA 1 pyramidal cell under the condition of transient brain ischemia, the present experiment used 24 male Wistar rats aged 9 months and divided them into four groups. Lidocaine and/or furosemide were injected introcerebroventicularlly (I.C.V). Stained with H E and accounted the CA 1 pyramidal cell numbers by computer in each group suggested following findings: Although 5 μl of 2% lidocaine was injected I.C.V, the results indicated lidocaine didn't have any blockade to pyramidal cell injuries in hippocampal CA 1 area (P<0 05). In the group medicated with 2 5μl of both 2% lidocaine and 2% furosemide, the results showed that the combined approach had a blockade to injuries of pyramidal cells compared with control group (P<0 01). The present experiment indicates that the combined blockade of lidocaine and furosemide injected I.C.V. to Na + channel can prevent the injuries from hippocampal neurons owing to ischemia. 展开更多
关键词 THE PROTECTIVE EFFECT OF Na AGAINST CELL DAMAGE CAUSED BY ISCHEMIA CHANNEL blockers
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Effect of voltage-gated sodium channels blockers on motility and viability of human spermin vitro
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作者 Hammad Ahmad Gakhar Ishrat Waheed +1 位作者 Taseer Ahmad Naeem-ur-rahman 《Asian pacific Journal of Reproduction》 2018年第2期62-71,共10页
Objective:To test the effect of voltage-gated sodium channels (VGSCs) blockers on the motility and viability of human spermin-vitro and to evaluate the tested compounds as potential contact spermicidal.Methods: Sperm ... Objective:To test the effect of voltage-gated sodium channels (VGSCs) blockers on the motility and viability of human spermin-vitro and to evaluate the tested compounds as potential contact spermicidal.Methods: Sperm samples were obtained from healthy non-smoking volunteers of age 25-30 years who had not taken any drug 3 months before and during the course of the study. The effect of VGSCs blockers evaluated from two pharmacological classes including antiarrhythmic (amiodarone, procainamide and disopyramide) and antiepileptic (carbamazepine, oxcarbazepine, phenytoin, and lamotrigine) drugs. They were tested on thein-vitro motility and viability of human sperm using Computer Assisted Semen Analyzer.Results:All tested drugs except oxcarbazepine showed dose dependent inhibition of total motility with significant reduction (P<0.05) at the maximum concentration of 200 μM when compared with the control. The concentrations of drugs that reduced total sperm motility to 50% of control (half maximal inhibitory concentration) were 2.76, 14.16 and 20.29 μM for phenytoin, lamotrigine and carbamazepine, respectively;and 2.53, 5.32 and 0.37 μM for amiodarone, procainamide and disopyramide, respectively. The anti-motility effects were reversible to various degrees. There was statistically insignificant difference in the inhibition of sperm viability among amiodarone, procainamide and disopyramide. Phenytoin demonstrated the most potent spermicidal action.Conclusions:VGSCs blockers have significant adverse effects onin-vitro motility of human spermatozoa. Soin-vivo studies are required to determine their potential toxicological effects on human semen quality, which is an important factor regarding fertility. Moreover, these drugs have the potential to be developed into contact spermicidal. 展开更多
关键词 Human sperm VGSCs blockers AMIODARONE PROCAINAMIDE and DISOPYRAMIDE Carbamazepine OXCARBAZEPINE PHENYTOIN
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Calcium Channel Blockers《钙离子阻断剂》
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作者 苏定冯 《中国药理学通报》 CAS CSCD 北大核心 2005年第2期140-140,共1页
关键词 阻断剂 钙通道 对抗药 慢通道 凝血因子Ⅳ 钙离子 Calcium Channel blockers
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Voltage-gated Sodium Channels and Blockers:An Overview and Where Will They Go?
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作者 Zhi-mei LI Li-xia CHEN Hua LI 《Current Medical Science》 SCIE CAS 2019年第6期863-873,共11页
Voltage-gated sodium(Nav)channels are critical players in the generation and propagation of action potentials by triggering membrane depolarization.Mutations in Nav channels are associated with a variety of channelopa... Voltage-gated sodium(Nav)channels are critical players in the generation and propagation of action potentials by triggering membrane depolarization.Mutations in Nav channels are associated with a variety of channelopathies,which makes them relevant targets for pharmaceutical intervention.Sofar,the cryoelectron microscopic structure of the human Nav 1.2,Nav 1.4,and Nav 1.7 has been reported,which sheds light on the molecular basis of functional mechanism of Nav channels and provides a path toward structure-based drug discovery.In this review,we focus on the recent advances in the structure,molecular mechanism and modulation of Nav channels,and state updated sodium channel blockers for the treatment of pathophysiology disorders and briefly discuss where the blockers may be developed in the future. 展开更多
关键词 voltage-gated sodium channels blockers Nav channel structures CHANNELOPATHIES
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Impact of angiotensin-converting enzyme inhibitors or angiotensin receptor blockers on the mortality in sepsis: A meta-analysis
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作者 Deng-Can Yang Jian Xu +1 位作者 Li Jian Yi Yu 《World Journal of Clinical Cases》 SCIE 2023年第36期8498-8506,共9页
BACKGROUND The effect of angiotensin-converting enzyme inhibitors(ACEIs)or angiotensin receptor blockers(ARBs)on the mortality of patients with sepsis is not well characterized.AIM To elucidate the association between... BACKGROUND The effect of angiotensin-converting enzyme inhibitors(ACEIs)or angiotensin receptor blockers(ARBs)on the mortality of patients with sepsis is not well characterized.AIM To elucidate the association between prior ACEI or ARB exposure and mortality in sepsis.METHODS The PubMed,EMBASE,Web of Science,and Cochrane Library databases were searched for all studies of premorbid ACEI or ARB use and sepsis mortality until November 302019.Two reviewers independently assessed,selected,and ab-stracted data from studies reporting ACEIs or ARBs,sepsis,and mortality.The primary extracted data consisted of premorbid ACEI or ARB exposure,mortality,and general patient data.Two reviewers independently assessed the risk of bias and quality of evidence.RESULTS A total of six studies comprising 281238 patients with sepsis,including 49799 cases with premorbid ACEI or ARB exposure were eligible for analysis.Pre-morbid ACEIs or ARBs exposure decreased the 30-d mortality in patients with sepsis.Moreover,the use of ACEIs or ARBs was associated with approximately a 6%decreased risk of 30-d mortality.CONCLUSION The results of this systematic review suggest that ACEI or ARB exposure prior to sepsis may be associated with reduced mortality.Further high-quality cohort studies and molecular mechanism experiments are required to confirm our results. 展开更多
关键词 SEPSIS MORTALITY Angiotensin-converting enzyme inhibitors Angiotensin receptor blockers
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Beta Blockers Use in Cardiac Failure: Does the Current Prescribing Practice at a Large Urban Hospital in Zimbabwe Exhibit Evidence Based Care and Offer Optimal Therapy for Cardiac Failure Patients?
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作者 Patrick Rutendo Matowa 《Pharmacology & Pharmacy》 2015年第5期267-279,共13页
Background: Cardiac failure treatment largely focused on symptomatic relief at the expense of the address of the underlying disease process of cardiac remodelling. This old wisdom of practice has been turned around by... Background: Cardiac failure treatment largely focused on symptomatic relief at the expense of the address of the underlying disease process of cardiac remodelling. This old wisdom of practice has been turned around by clinical research findings that have shown that there are agents that reverse cardiac remodelling and offer long-term benefits to cardiac failure patients. This has led to the recommendation of evidence-based practice in chronic heart failure management using reverse modelling agents such as beta blockers. Objectives: To ascertain the prescribing patterns of beta blockers in cardiac failure patients by doctors in a public hospital setting and determine the prevalence of cardiac failure hospitalisation and the age groups involved. Study design: A retrospective medical records review observational study. Methodology: A sample size of 385 cardiac failure cases was used. Data on cardiac failure patients who were once hospitalised at the hospital of study were abstracted from the patients’ medical records files using data collection forms. Results: There were 36 (9.4%) patients who were prescribed beta blockers, 7 patients had their beta blocker substituted for another. Atenolol was prescribed to 30 (7.8%) patients, propranolol to 7 (1.8%) and carvedilol to 6 (1.6%) patients. Metoprolol and bisoprolol were not prescribed at all. There were more females (57.9%) than males (42.1%) and the mean age was 41.9 (standard deviation 24.0) years. The prevalence of cardiac failure hospitalisation was 1.54%. Conclusion: The rate of beta blocker prescribing was low. There is need for emphasis on evidence-based treatment options in the management of cardiac failure in Zimbabwe. 展开更多
关键词 CARDIAC Failure Beta blockers PRESCRIBING Patterns
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Mechanism and reversal strategies of immune checkpoint blockers drug resistance
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作者 Xiao-Hui Liu 《Precision Medicine Research》 2019年第4期121-124,共4页
Recent years,the immune checkpoint blockers(ICBs)become more and more important in tumor therapy with the development of tumor immunology and achieved significant clinical effects in various solid tumors.ICBs is a typ... Recent years,the immune checkpoint blockers(ICBs)become more and more important in tumor therapy with the development of tumor immunology and achieved significant clinical effects in various solid tumors.ICBs is a type of tumor immunotherapy method which controls and clears tumor by activating the autoimmune system and restoring the body's normal anti-tumor immune response.However,the resistance of ICBs cannot be ignored and still faces many challenges.The mechanism and the solution of ICBs resistance need to be further research. 展开更多
关键词 Tumor immunotherapy PD-1/PD-L1 IMMUNE CHECKPOINT blockers Drug resistance Combined therapy
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Evaluation of Anti-inflammatory Effects of Angiotensin Receptor Blockers in an Experimental Model of Acute Inflammation in Rats
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作者 Prasad Pandit Pratiksha Chandrakant Mainkar Sanket Subhash Sawant 《Journal of Pharmacy and Pharmacology》 2014年第3期185-193,共9页
There is a renewed interest in ARBs (angiotensin receptor blockers) for their effects on inflammation, as they are commonly used in the elderly suffering from disorders like arthritis, atherosclerosis which may have... There is a renewed interest in ARBs (angiotensin receptor blockers) for their effects on inflammation, as they are commonly used in the elderly suffering from disorders like arthritis, atherosclerosis which may have a potential inflammatory etiology. But there have been conflicting reports on the effect of ARBs on inflammation. The present study was aimed to evaluate the anti-inflammatory effect of ARBs in rat model of acute inflammation. Albino Wistar rats were randomly assigned to seven groups, i.e., Control (1% CMC (carboxy methyl cellulose)), Aspirin, Losartan, Telmisartan, Valsartan, Candesartan and Irbesartan groups. Rats were orally pretreated with drugs for three consecutive days. On the 3rd day, rats were challenged by a subcutaneous injection of 0.05 mL of 1% carrageenan into the plantar side of right hind paw, 30 min after drug administration. Paw edema was measured using a mercury plethysmograph and paw diameter by micrometer screw-gauge at 0, 3, 6 and 24 h after carrageenan challenge. Percentage inhibition of edema was also calculated. All the ARBs showed a significant anti-inflammatory effect at 3, 6 and 24 h as compared to control, although not comparable to that of aspirin. This anti-inflammatory effect, although not comparable to a known anti-inflammatory agent like aspirin, would perhaps prove beneficial in elderly patients routinely treated with these drugs. 展开更多
关键词 Angiotensin receptor blockers INFLAMMATION CARRAGEENAN paw edema.
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Long-term Effects of Nicorandil Combined with Dihydropyridine Calcium Channel Blockers on Cardiovascular Outcomes in Patients with Coronary Heart Disease: A Real-world Observational Study
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作者 Jia Cheng Zixuan Zhang +5 位作者 Hongyang Shu Weijian Hang Qingqing Zhao Jinzhao Zhao Zhichao Xiao Ning Zhou 《Cardiovascular Innovations and Applications》 2023年第1期633-644,共12页
Objective:This study was aimed at investigating whether the addition of nicorandil to a dihydropyridine calcium channel blocker(DHP-CCB)regimen might decrease the occurrence of major adverse cardiovascular events(MACE... Objective:This study was aimed at investigating whether the addition of nicorandil to a dihydropyridine calcium channel blocker(DHP-CCB)regimen might decrease the occurrence of major adverse cardiovascular events(MACE)in patients with coronary heart disease(CHD).Methods:A multicenter,retrospective,real-world study was conducted.Between August 2002 and March 2020,7413 eligible patients with CHD were divided into DHP-CCB plus nicorandil combination(n=1843)and DHP-CCB(n=5570)treatment groups.The primary outcome was MACE,defined as a composite of myocardial infarction,stroke,and all-cause mortality.Propensity score matching was used to adjust for confounding factors.Results:After propensity score matching,combination therapy,compared with DHP-CCBs alone,was associated with a lower risk of MACE(HR:0.80,95%CI:0.67–0.97).The combination group also had a lower risk of stroke(HR:0.55,95%CI:0.44–0.69),but not myocardial infarction(HR:1.21,95%CI:0.91–1.61)or all-cause mortality(HR:1.24,95%CI:0.63–2.44).Subgroup analysis revealed more prominent benefits of the combined treatment on MACE in patients with than without diabetes.Conclusions:The combination of nicorandil and DHP-CCBs may be more beneficial than DHP-CCBs alone in decreasing long-term risks of MACE and stroke in patients with CHD. 展开更多
关键词 coronary heart disease ANGINA NICORANDIL calcium channel blockers major adverse cardiovascular events
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