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Proton pump inhibitors therapy vs H_2 receptor antagonists therapy for upper gastrointestinal bleeding after endoscopy: A meta-analysis 被引量:14
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作者 Ying-Shi Zhang Qing Li +2 位作者 Bo-Sai He Ran Liu Zuo-Jing Li 《World Journal of Gastroenterology》 SCIE CAS 2015年第20期6341-6351,共11页
AIM: To compare the therapeutic effects of proton pump inhibitors vs H2 receptor antagonists for upper gastrointestinal bleeding in patients after successful endoscopy.METHODS: We searched the Cochrane library, MEDLIN... AIM: To compare the therapeutic effects of proton pump inhibitors vs H2 receptor antagonists for upper gastrointestinal bleeding in patients after successful endoscopy.METHODS: We searched the Cochrane library, MEDLINE, EMBASE and Pub Med for randomized controlled trials until July 2014 for this study. The risk of bias was evaluated by the Cochrane Collaboration's tool and all of the studies had acceptable quality. The main outcomes included mortality, re-bleeding, received surgery rate, blood transfusion units and hospital stay time. These outcomes were estimated using odds ratios(OR) and mean difference with 95% confidence interval(CI). Rev Man 5.3.3 software and Stata 12.0 software were used for data analyses. RESULTS: Ten randomized controlled trials involving 1283 patients were included in this review; 678 subjects were in the proton pump inhibitors(PPI) group and the remaining 605 subjects were in the H2 receptor antagonists(H2RA) group. The meta-analysis results revealed that after successful endoscopic therapy, compared with H2 RA, PPI therapy had statistically significantly decreased the recurrent bleeding rate(OR = 0.36; 95%CI: 0.25-0.51) and receiving surgery rate(OR = 0.29; 95%CI: 0.09-0.96). There were no statistically significant differences in mortality(OR = 0.46; 95%CI: 0.17-1.23). However, significant heterogeneity was present in both the numbers of patients requiring blood transfusion after treatment [weighted mean difference(WMD),-0.70 unit; 95%CI:-1.64- 0.25] and the time that patients remained hospitalized [WMD,-0.77 d; 95%CI:-1.87- 0.34]. The Begg's test(P = 0.283) and Egger's test(P = 0.339) demonstrated that there was no publication bias in our meta-analysis.CONCLUSION: In patients with upper gastrointestinal bleeding after successful endoscopic therapy, compared with H2 RA, PPI may be a more effective therapy. 展开更多
关键词 H2 receptor antagonist Proton pump inhibitor Upper GASTROINTESTINAL BLEEDING Randomized controlledtrial META-ANALYSIS
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Medical therapy for clinical benign prostatic hyperplasia:α1 Antagonists,5α reductase inhibitors and their combination 被引量:4
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作者 Cheuk Fan Shum Weida Lau Chang Peng Colin Teo 《Asian Journal of Urology》 2017年第3期185-190,共6页
Medical therapy for clinical benign prostatic hyperplasia(BPH)has advanced significantly in the last 2 decades.Many new a1 antagonists and 5a reductase inhibitors(5ARi)are now commercially available.The practicing uro... Medical therapy for clinical benign prostatic hyperplasia(BPH)has advanced significantly in the last 2 decades.Many new a1 antagonists and 5a reductase inhibitors(5ARi)are now commercially available.The practicing urologist must decide on the most appropriate medication for his patients,taking into consideration various factors like efficacy,dosing regime,adverse effects,cost,patient’s socioeconomic background,expectations,drug availability and his own clinical experience.The use of combination therapy added further to the complexity in clinical judgment when prescribing.We highlight some of the key points in prescribing a1 antagonists,5ARi and their combination,based on our viewpoints and experience as urologists in an Asian clinical setting. 展开更多
关键词 5αReductase inhibitors Adrenergicα1 receptor antagonists Drug therapy COMBINATION Prostatic hyperplasia
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Head-to-head comparison of H_2-receptor antagonists and proton pump inhibitors in the treatment of erosive esophagitis: A meta-analysis 被引量:1
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作者 Wei-HongWang Jia-QingHuang +4 位作者 Ge-FanZheng HarryHua-XiangXia Wai-ManWong Shiu-KumLam BenjaminChun-YuWong 《World Journal of Gastroenterology》 SCIE CAS CSCD 2005年第26期4067-4077,共11页
AIM: To systematically evaluate the efficacy of H2-receptor antagonists (H2RAs) and proton pump inhibitors in healing erosive esophagitis (EE).METHODS: A meta-analysis was performed. A literature search was conducted ... AIM: To systematically evaluate the efficacy of H2-receptor antagonists (H2RAs) and proton pump inhibitors in healing erosive esophagitis (EE).METHODS: A meta-analysis was performed. A literature search was conducted in PubMed, Medline, Embase, and Cochrane databases to include randomized controlled head-to-head comparative trials evaluating the efficacy of H2RAs or proton pump inhibitors in healing EE. Relative risk (RR) and 95% confidence interval (CI) were calculated under a random-effects model.RESULTS: RRs of cumulative healing rates for each comparison at 8 wk were: high dose vs standard dose H2RAs,1.17 (95%CI, 1.02-1.33); standard dose proton pump inhibitors vsstandard dose H2RAs, 1.59 (95%CI, 1.44-1.75);standard dose other proton pump inhibitors vs standard dose omeprazole, 1.06 (95%CI, 0.98-1.06). Proton pump inhibitors produced consistently greater healing rates than H2RAs of all doses across all grades of esophagitis, including patients refractory to H2RAs. Healing rates achieved with standard dose omeprazole were similar to those with other proton pump inhibitors in all grades of esophagitis.CONCLUSION: H2RAS are less effective for treating patients with erosive esophagitis, especially in those with severe forms of esophagitis. Standard dose proton pump inhibitors are significantly more effective than H2RAs in healing esophagitis of all grades. Proton pump inhibitors given at the recommended dose are equally effective for healing esophagitis. 展开更多
关键词 H2-受体 质子泵抑制剂 溃疡性食道炎 治疗方法
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Renin-angiotensin system blockers-SGLT2 inhibitorsmineralocorticoid receptor antagonists in diabetic kidney disease:A tale of the past two decades!
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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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Comparison of PPIs and H_2-receptor antagonists plus prokinetics for dysmotility-like dyspepsia 被引量:9
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作者 Masahiro Sakaguchi Miyuki Takao +14 位作者 Yasuo Ohyama Hiroshi Oka Hiroshi Yamashita Takumi Fukuchi Kiyoshi Ashida Masahiro Murotani Masuyo Murotani Kazuo Majima Hiroshi Morikawa Takashi Hashimoto Keisuke Kiyota Hirohiko Esaki Kanji Amemoto Gouhei Isowa Fumiyuki Takao 《World Journal of Gastroenterology》 SCIE CAS CSCD 2012年第13期1517-1524,共8页
AIM:To compare efficacy of proton pump inhibitors(PPIs)with H2-receptor antagonists(H2RAs)plus prokinetics(Proks)for dysmotility-like symptoms in functional dyspepsia(FD).METHODS:Subjects were randomized to receive op... AIM:To compare efficacy of proton pump inhibitors(PPIs)with H2-receptor antagonists(H2RAs)plus prokinetics(Proks)for dysmotility-like symptoms in functional dyspepsia(FD).METHODS:Subjects were randomized to receive openlabel treatment with either rabeprazole 10 mg od(n= 57)or famotidine 10 mg bid plus mosapride 5 mg tid(n=57)for 4 wk.The primary efficacy endpoint was change(%)from baseline in total dysmotility-like dyspepsia symptom score.The secondary efficacy endpoint was patient satisfaction with treatment.RESULTS:The improvement in dysmotility-like dyspep-sia symptom score on day 28 was significantly greater in the rabeprazole group(22.5%±29.2%of baseline) than the famotidine+mosapride group(53.2%± 58.6%of baseline,P<0.0001).The superior benefit of rabeprazole treatment after 28 d was consistent regardless of Helicobacter pylori status.Significantly more subjects in the rabeprazole group were satisfied or very satisfied with treatment on day 28 than in the famotidine+mosapride group(87.7%vs 59.6%,P= 0.0012).Rabeprazole therapy was the only significant predictor of treatment response(P<0.0001),defined as a total symptom score improvement≥50%.CONCLUSION:PPI monotherapy improves dysmotility-like symptoms significantly better than H2RAs plus Proks,and should be the treatment of first choice for Japanese FD. 展开更多
关键词 H2受体拮抗剂 消化不良 功能障碍 指数和 生产者 配合治疗 不良症状 运动
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The use of antimuscarinics,phosphodiesterase type Ⅴ inhibitors and phytotherapy for lower urinary tract symptoms in men 被引量:2
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作者 Kok Kit Ng Foo Cheong Ng 《Asian Journal of Urology》 2017年第3期191-194,共4页
Besides the mainstay of α-blockers and 5α-reductase inhibitors,other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms(LUTS)in men.These treatments can target speci... Besides the mainstay of α-blockers and 5α-reductase inhibitors,other forms of medical therapy complete the armamentarium in the treatment of lower urinary tract symptoms(LUTS)in men.These treatments can target specific symptoms as well as associated symptoms that would affect the quality of life of the patients.Many patients are bothered by storage symptoms,more so than the voiding symptoms.Antimuscarinics are efficacious and safe,provided the patients do not have high post void residual urine.Many patients with LUTS also have erectile dysfunction,and phosphodiesterase type Ⅴ inhibitors are effective in relieving both LUTS as well as erectile dysfunction for such patients.Phytotherapy provides a popular and safe treatment for LUTS,however,the efficacy of the treatment has not been proven in well conducted prospective randomized controlled studies. 展开更多
关键词 Benign prostatic hyperplasia Erectile dysfunction Lower urinary tract symptoms Muscarinic antagonists Phosphodiesterase 5 inhibitors PHYTOTHERAPY
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Stronger inhibition of gastric acid secretion by lafutidine, a novel H_2 receptor antagonist, than by the proton pump inhibitor lansoprazole 被引量:3
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作者 Hatsushi Yamagishi Tomoyuki Koike +10 位作者 Shuichi Ohara Toru Horii Ryousuke Kikuchi Shigeyuki Kobayashi Yasuhiko Abe Katsunori Iijima Akira Imatani Kaori Suzuki Takanori Hishinuma Junichi Goto Tooru Shimosegawa 《World Journal of Gastroenterology》 SCIE CAS CSCD 2008年第15期2406-2410,共5页
AIM: To compare the antisecretory activity and plasma drug concentrations of a single oral dose of 10 mg lafutidine, a novel H2 receptor antagonist, with those of the proton pump inhibitor lansoprazole (LPZ) 30 mg. ME... AIM: To compare the antisecretory activity and plasma drug concentrations of a single oral dose of 10 mg lafutidine, a novel H2 receptor antagonist, with those of the proton pump inhibitor lansoprazole (LPZ) 30 mg. METHODS: Ten volunteers without H pylori infection participated in this crossover study comparing lafutidine 10 mg with LPZ 30 mg. Intragastric pH was monitored for 6 h in all participants, and blood samples were collected from four randomly selected individuals after single-dose administration of each drug. RESULTS: The median intragastric pH was significantly higher in individuals who received lafutidine 10 mg than in those who received LPZ 30 mg 2, 3, 4, 5, and 6 h after administration. Maximal plasma drug concentration was reached more promptly with lafutidine 10 mg than with LPZ 30 mg. CONCLUSION: In H pylori-negative individuals, gastric acid secretion is more markedly inhibited by lafutidinethan by LPZ. 展开更多
关键词 胃病 胃酸分泌物 抑制剂 拮抗体
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Affinity Crosslinking of Y1036 to Nerve Growth Factor Identifies Pharmacological Targeting Domain for Small Molecule Neurotrophin Antagonists
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作者 Joseph K. Eibl Zouleika Abdallah +2 位作者 Allison E. Kennedy John A. Scott Gregory M. Ross 《Neuroscience & Medicine》 2013年第4期290-298,共9页
Classically, small molecule antagonists have targeted membrane bound receptors and intracellular enzyme targets. While this drug discovery strategy is extremely successful, the number of new chemical entities in the p... Classically, small molecule antagonists have targeted membrane bound receptors and intracellular enzyme targets. While this drug discovery strategy is extremely successful, the number of new chemical entities in the pharmaceutical pipeline is diminishing and complementary strategies are in need. A particularly attractive therapeutic strategy is to neutralize soluble signalling proteins using small molecules. Small molecule-based technologies have the potential to sufficiently alter the molecular topology of a given ligand and inhibit ligand/receptor interactions—effectively neutralizing the ligand’s signalling capacity. Recent technical advances in the field of structural biology have enabled the elucidation of ligand/receptor complexes at atomic resolution enabling a detailed appreciation of the molecular interactions governing ligand-mediated receptor activation. Exploiting molecular modeling techniques to study these signalling complexes allows for a paradigm shift from “receptorcentric” to “ligandcentric” screening strategies. Nerve growth factor (NGF) is a prototypical protein signalling ligand, which binds two receptors, TrkA and p75NTR. We first explore the molecular landscape governing the ligand/receptor interactions of NGF/TrkA and NGF/p75 structures. Next, we use the recently reported NGF neutralizing small-molecule, Y1036, as an affinity probe to determine residues in proximity to the pharmacological targeting domain of NGF and perform theoretical docking experiments to predict the residues which comprise distinct pharmacological targeting domains on the surface of NGF. Exploiting such strategies may facilitate “ligandcentric” drug discovery and could further the development of a trophic-factor-selective compound such as a BDNF-selective antagonist. 展开更多
关键词 NGF BDNF inhibitor antagonist Pain
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心力衰竭药物治疗相关高钾血症防治专家共识
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作者 中国医师协会心血管内科医师分会 中国老年医学学会心电与心功能分会 +6 位作者 周京敏 杨杰孚 陈牧雷 李萍 孙志军 徐东杰 徐亚妹 《中国循环杂志》 CSCD 北大核心 2024年第6期537-546,共10页
肾素-血管紧张素系统抑制剂(RASi)、血管紧张素受体脑啡肽酶抑制剂(ARNI)、盐皮质激素受体拮抗剂(MRA)等是心力衰竭治疗的基石药物,也是诱发高钾血症的重要原因。发生高钾血症的心力衰竭患者死亡风险和再住院风险显著增加,而减少或停用... 肾素-血管紧张素系统抑制剂(RASi)、血管紧张素受体脑啡肽酶抑制剂(ARNI)、盐皮质激素受体拮抗剂(MRA)等是心力衰竭治疗的基石药物,也是诱发高钾血症的重要原因。发生高钾血症的心力衰竭患者死亡风险和再住院风险显著增加,而减少或停用这些药物对心力衰竭患者预后的危害超过高钾血症带来的风险。为了更好地降低心力衰竭人群中高钾血症的发生风险并规范管理,由中国医师协会心血管内科医师分会、中国老年医学学会心电与心功能分会组织相关专家,参考国内外最新高钾血症管理指南/共识意见及临床研究结果,结合我国国情和临床实践制定了本共识,主要内容包括心力衰竭患者中高钾血症的流行病学,心力衰竭治疗药物的规范应用,心力衰竭患者合并高钾血症高危人群的识别、监测、随访及预防,降钾用药策略等,以期为临床医师早期预防和管理心力衰竭药物治疗相关高钾血症提供临床依据。 展开更多
关键词 心力衰竭 肾素-血管紧张素系统抑制剂 盐皮质激素受体拮抗剂 药物治疗 高钾血症 共识
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ACEI和ARB对慢性肾脏病患者预后的影响分析
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作者 王秀莲 高真真 +1 位作者 段海玲 耿明亮 《中国实用医药》 2024年第5期33-36,共4页
目的 研讨血管紧张素转化酶抑制剂(ACEI)和血管紧张素Ⅱ受体拮抗剂(ARB)对慢性肾脏病(CKD)患者预后的影响。方法 选取88例慢性肾脏病患者,随机分成对照组、观察组,各44例。对照组采用ACEI治疗,观察组采用ARB治疗。比较两组的治疗效果、... 目的 研讨血管紧张素转化酶抑制剂(ACEI)和血管紧张素Ⅱ受体拮抗剂(ARB)对慢性肾脏病(CKD)患者预后的影响。方法 选取88例慢性肾脏病患者,随机分成对照组、观察组,各44例。对照组采用ACEI治疗,观察组采用ARB治疗。比较两组的治疗效果、肾功能相关指标、心功能指标、生活质量评分、不良反应发生情况。结果 两组的治疗总有效率均较高(P>0.05)。观察组治疗后的尿素氮(9.25±1.05)mmol/L、血肌酐(142.56±32.08)μmol/L均低于对照组的(12.56±5.25)mmol/L、(252.26±55.16)μmol/L,血肌酐清除率(96.41±2.08)ml/min高于对照组的(88.56±8.25)ml/min(P<0.05)。观察组治疗后的左室收缩末期内径(LVESD)(46.25±1.06)mm、左室舒张末期内径(LVEDD)(50.26±0.36)mm小于对照组的(49.26±5.26)、(57.15±2.56)mm,左室射血分数(LVEF)(44.89±1.08)%高于对照组的(41.26±5.62)%(P<0.05)。观察组治疗后的活力状况、生理职能、情感职能、社会功能评分分别为(68.44±1.54)、(64.99±2.10)、(68.48±2.15)、(62.48±1.08)分,均高于对照组的(59.48±6.50)、(58.48±8.10)、(59.48±8.41)、(59.71±0.36)分(P<0.05)。两组的不良反应发生率均较低(P>0.05)。结论 ACEI和ARB治疗慢性肾脏病均有一定疗效,但ARB更能显著改善患者的肾功能指标与心功能指标,更有助于提升生活质量。 展开更多
关键词 血管紧张素转化酶抑制剂 血管紧张素Ⅱ受体拮抗剂 慢性肾脏病 肾功能
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射血分数减低型心力衰竭的病情进展机制与治疗
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作者 孟霄 李峰 《心血管康复医学杂志》 CAS 2024年第1期104-107,共4页
临床上,射血分数减低型心力衰竭(HFrEF)的病情以进行性心功能下降为特征,伴随着患者反复住院、症状加重、生活质量显著恶化,并给患者家庭带来巨大的经济负担。并且随着时间的推移,以前被用来改善患者预后的药物疗效逐渐下降。即使采用... 临床上,射血分数减低型心力衰竭(HFrEF)的病情以进行性心功能下降为特征,伴随着患者反复住院、症状加重、生活质量显著恶化,并给患者家庭带来巨大的经济负担。并且随着时间的推移,以前被用来改善患者预后的药物疗效逐渐下降。即使采用当前最先进的医疗手段,患者的死亡率仍呈上升趋势。临床上,HFrEF患者更容易出现对神经激素药物的不耐受,以及对利尿剂高需求量和利尿剂抵抗的心肾综合征,神经激素激活可能是其进展的主要决定因素。本文就HFrEF的病情进展的机制及治疗方案作一综述。 展开更多
关键词 心力衰竭 血管紧张素转换酶抑制药 肾上腺素能Β受体拮抗剂
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ACEI/ARB对新型冠状病毒肺炎合并高血压病人预后的影响 被引量:1
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作者 李超 史宏涛 韩清华 《中西医结合心脑血管病杂志》 2023年第3期474-479,共6页
目的:分析血管紧张素Ⅱ受体拮抗剂(ARB)/血管紧张素转换酶抑制剂(ACEI)类药物对新型冠状病毒肺炎(COVID-19)合并高血压病人各项临床指标及预后的影响,并探讨其临床应用价值。方法:选取2020年1月14日—2020年2月18日山西省各地区医院确诊... 目的:分析血管紧张素Ⅱ受体拮抗剂(ARB)/血管紧张素转换酶抑制剂(ACEI)类药物对新型冠状病毒肺炎(COVID-19)合并高血压病人各项临床指标及预后的影响,并探讨其临床应用价值。方法:选取2020年1月14日—2020年2月18日山西省各地区医院确诊COVID-19病人76例,根据是否合并高血压分为高血压组(21例)和非高血压组(55例);根据高血压病人是否长期服用ACEI/ARB类药物分为使用ACEI/ARB组(11例)和使用其他药物组(10例)。记录并比较病人相关病史及入院后一般生命体征、血常规、降钙素原(PCT)、C反应蛋白(CRP)、肝功能、肾功能、心肌损伤标志物等。比较病人出院后1个月、6个月、12个月的随访指标。结果:与非高血压组比较,高血压组病人年龄较大,体质指数(BMI)值较高,收缩压(SBP)、舒张压(DBP)增高,白细胞及中性粒细胞增多(P<0.05);使用其他药物组与使用ACEI/ARB组病人一般资料比较,差异均无统计学意义(P>0.05);使用ACEI/ARB组和使用其他药物组各指标随访结果比较,差异均无统计学意义(P>0.05)。结论:ACEI/ARB类药物并未对COVID-19合并高血压病人各项临床指标产生明显影响,且不影响该类病人的预后,可以考虑继续服用ACEI/ARB进行临床治疗。 展开更多
关键词 高血压 新型冠状病毒肺炎 COVID-19 血管紧张素转换酶抑制剂 血管紧张素Ⅱ受体拮抗剂
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IgA肾病治疗研究进展及展望 被引量:1
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作者 王冰心 李贞琼 《中外医学研究》 2023年第15期163-168,共6页
IgA肾病是全球最常见的原发性肾小球疾病,其是一种缓慢进展的疾病,目前尚无特异性治疗方法,且糖皮质激素和免疫抑制剂的治疗作用一直存在争议。随着生物科学和医学技术进步,肠道黏膜免疫、补体系统、内皮素(ET)受体及B细胞活化因子(B ce... IgA肾病是全球最常见的原发性肾小球疾病,其是一种缓慢进展的疾病,目前尚无特异性治疗方法,且糖皮质激素和免疫抑制剂的治疗作用一直存在争议。随着生物科学和医学技术进步,肠道黏膜免疫、补体系统、内皮素(ET)受体及B细胞活化因子(B cell activating factor,BAFF)/增殖诱导配体(a proliferation-inducing ligand,APRIL)系统等被证实在IgA肾病发生发展中发挥重要作用。这些新进展为推测发病机制提供了理论依据,也为研发新型药物提供了方向。本文主要对IgA肾病药物治疗现状及其存在的问题进行综述。 展开更多
关键词 IGA肾病 钠-葡萄糖共转运蛋白2 抑制剂 内皮素受体拮抗剂 补体抑制剂
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Advances in Medical Treatment of Primary Aldosteronism 被引量:1
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作者 Ying-Jie Li Zhi-Gang Ji Jin Wen 《Chinese Medical Sciences Journal》 CAS CSCD 2023年第1期49-56,共8页
Primary aldosteronism(PA)is the most common form of secondary hypertension,with its main manifestations including hypertension and hypokalemia.Early identification of PA is extremely important as PA patients can easil... Primary aldosteronism(PA)is the most common form of secondary hypertension,with its main manifestations including hypertension and hypokalemia.Early identification of PA is extremely important as PA patients can easily develop cardiovascular complications such as atrial fibrillation,stroke,and myocardial infarction.The past decade has witnessed the rapid advances in the genetics of PA,which has shed new light on PA treatment.While surgery is the first choice for unilateral diseases,bilateral lesions can be treated with mineralocorticoid receptor antagonists(MRAs).The next-generation non-steroidal MRAs are under investigations.New medications including calcium channel blockers,macrophage antibiotics,and aldosterone synthase inhibitors have provided a new perspective for the medical treatment of PA. 展开更多
关键词 primary aldosteronism mineralocorticoid receptor antagonists calcium channel blockers macrolide antibiotics aldosterone synthase inhibitors
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防治心力衰竭新药临床应用及研究进展 被引量:1
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作者 唐尚仪 张晓静 +2 位作者 郭宝剑 胡靖渝 王书林 《河北医药》 CAS 2023年第13期2041-2045,共5页
心力衰竭(heart failure,HF)是全球的公共卫生问题,是多种心血管疾病的终末阶段,HF患者面临着高死亡率的威胁,且因反复住院及活动耐受差,严重影响生活质量。一线药物如利尿剂、肾素血管紧张素醛固酮系统(renin-angiotensin-aldosterone ... 心力衰竭(heart failure,HF)是全球的公共卫生问题,是多种心血管疾病的终末阶段,HF患者面临着高死亡率的威胁,且因反复住院及活动耐受差,严重影响生活质量。一线药物如利尿剂、肾素血管紧张素醛固酮系统(renin-angiotensin-aldosterone system,RAAS)抑制剂和β受体拮抗剂(beta-receptor blockers,BB)等使各类HF患者获益,但临床应用时产生的电解质紊乱、干咳、血管性水肿、心律失常和肾功能损伤等不良反应时有发生;同时药物种类的局限为心力衰竭药物治疗带来桎梏。因此,国内外围绕HF的新药研发一直在开展。本文就近5年在中国上市的防治HF新药临床应用及其在各期临床研究取得的进展进行综述,旨在明确HF新药临床应用价值与前景,为临床HF药物治疗提供新的思路。 展开更多
关键词 心力衰竭 临床新进展 ARNI SGLT-2抑制剂 新型MRA 维利西呱 omecamtiv mecarbil
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Targeting the“undruggable”cancer driver genes:Ras,myc,and tp53
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作者 XINGBO WU DAN PAN +1 位作者 SHOUYI TANG YINGQIANG SHEN 《BIOCELL》 SCIE 2023年第7期1459-1472,共14页
The term“undruggable”is to describe molecules that are not targetable or at least hard to target pharmacologically.Unfortunately,some targets with potent oncogenic activity fall into this category,and currently litt... The term“undruggable”is to describe molecules that are not targetable or at least hard to target pharmacologically.Unfortunately,some targets with potent oncogenic activity fall into this category,and currently little is known about how to solve this problem,which largely hampered drug research on human cancers.Ras,as one of the most common oncogenes,was previously considered“undruggable”,but in recent years,a few small molecules like Sotorasib(AMG-510)have emerged and proved their targeted anti-cancer effects.Further,myc,as one of the most studied oncogenes,and tp53,being the most common tumor suppressor genes,are both considered“undruggable”.Many attempts have been made to target these“undruggable”targets,but little progress has been made yet.This article summarizes the current progress of direct and indirect targeting approaches for ras,myc,two oncogenes,and tp53,a tumor suppressor gene.These are potential therapeutic targets but are considered“undruggable”.We conclude with some emerging research approaches like proteolysis targeting chimeras(PROTACs),cancer vaccines,and artificial intelligence(AI)-based drug discovery,which might provide new cues for cancer intervention.Therefore,this review sets out to clarify the current status of targeted anti-cancer drug research,and the insights gained from this review may be of assistance to learn from experience and find new ideas in developing new chemicals that directly target such“undruggable”molecules. 展开更多
关键词 RAS MYC TP53 Antineoplastic agents PHARMACOLOGY Oncogene proteins antagonists and inhibitors
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青藤碱对环氧化酶2活性的选择性抑制作用 被引量:64
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作者 王文君 王培训 《广州中医药大学学报》 CAS 2002年第1期46-47,51,共3页
【目的】探讨中药青风藤的单体生物碱提取物青藤碱的抗炎作用机理。[方法]应用体外酶反应实验体系,观察青藤碱对离体环氧化酶-1(COX-1)和COX-2纯酶活性的影响。[结果]一定浓度的青藤碱对COX-2所致前列腺素E2(PGE... 【目的】探讨中药青风藤的单体生物碱提取物青藤碱的抗炎作用机理。[方法]应用体外酶反应实验体系,观察青藤碱对离体环氧化酶-1(COX-1)和COX-2纯酶活性的影响。[结果]一定浓度的青藤碱对COX-2所致前列腺素E2(PGE2)合成表现出较强的抑制作用,且有良好的量效关系。[结论]提示青藤碱选择性抑制COX-2的活性,可能是其抗炎镇痛作用较强而胃肠副作用小的主要机制之一。 展开更多
关键词 青藤碱 环氧化酶2 活性 选择性抑制作用 抗炎作用 药理学
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快速起效抗抑郁药物的研究进展 被引量:17
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作者 薛瑞 张有志 邹莉波 《中国药理学通报》 CAS CSCD 北大核心 2008年第12期1558-1561,共4页
目前临床使用的抗抑郁药物存在起效延迟的不足,这不仅降低了病人的依从性,还增加了其自杀的危险性。因此,如何研制出高效低毒且快速起效的抗抑郁药物成为研发热点。研究表明,选择性5-HT1A、α2自身受体拮抗剂及5-HT2A受体拮抗剂可加快5... 目前临床使用的抗抑郁药物存在起效延迟的不足,这不仅降低了病人的依从性,还增加了其自杀的危险性。因此,如何研制出高效低毒且快速起效的抗抑郁药物成为研发热点。研究表明,选择性5-HT1A、α2自身受体拮抗剂及5-HT2A受体拮抗剂可加快5-羟色胺重摄取抑制剂及去甲肾上腺素重摄取抑制剂等抗抑郁药物的起效速度。此外,5-HT/NE双重重摄取抑制剂及5-HT/NE/DA三重重摄取抑制剂起效时间也缩短。该文将重点围绕单胺系统对抗抑郁药物起效延迟的原因及快速起效抗抑郁药物的研究进展作一综述。 展开更多
关键词 抗抑郁药物 起效时间 5-HT1A受体拮抗剂 5-HT2A 受体拮抗剂 α2受体拮抗剂 双重/三重摄取抑制剂
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二烯丙基二硫对人胃癌细胞裸鼠移植瘤的抗肿瘤作用 被引量:10
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作者 向姝霖 肖晓岚 +4 位作者 凌晖 廖前进 周秀田 董琳 苏琦 《癌症》 SCIE CAS CSCD 北大核心 2005年第8期940-944,共5页
背景与目的:既往研究发现二烯丙基二硫(diallyldisulfide,DADS)在体外可抑制多种肿瘤细胞生长,但在体内抗肿瘤作用的研究报道较少。本实验旨在探讨DADS对人胃癌细胞移植瘤在BALB/C裸鼠体内生长的影响。方法:未经药物处理和经30mg/LDADS... 背景与目的:既往研究发现二烯丙基二硫(diallyldisulfide,DADS)在体外可抑制多种肿瘤细胞生长,但在体内抗肿瘤作用的研究报道较少。本实验旨在探讨DADS对人胃癌细胞移植瘤在BALB/C裸鼠体内生长的影响。方法:未经药物处理和经30mg/LDADS处理1天的胃癌细胞MGC803接种于裸鼠皮下;观察体外DADS处理MGC803细胞裸鼠移植瘤的成瘤情况和未处理MGC803细胞移植瘤成瘤后腹腔注射DADS对胃癌移植瘤在BALB/c裸鼠体内生长情况的影响。Westernblot检测瘤组织中增殖细胞核抗原(proliferatingcellnuclearantigen,PCNA)的表达情况。结果:30mg/LDADS处理的MGC803细胞移植裸鼠体内无一成瘤。荷瘤裸鼠腹腔注射DADS剂量为50、100和200mg/kg时的抑瘤率分别为27.8%、66.1%和73.0%,同时可抑制移植瘤癌细胞PCNA的表达。结论:DADS可明显降低胃癌细胞裸鼠移植瘤的成瘤性,并对移植瘤生长有明显抑制作用。 展开更多
关键词 胃癌细胞 移植瘤 药理学 二烯丙基二硫/拮抗剂和抑制剂 小鼠
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治疗糖尿病并发症药物的研究进展 被引量:8
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作者 申升 刘宏飞 +1 位作者 徐希明 余江南 《中国药事》 CAS 2012年第8期906-910,共5页
目的探讨防治糖尿病并发症药物的研究概况。方法参阅近年来国内外文献资料,并进行整理、综述。结果概述了治疗糖尿病并发症的药物开发与研究进展,主要包括醛糖还原酶抑制剂、血管紧张素转换酶抑制剂、血管紧张素Ⅱ受体拮抗剂、内皮素受... 目的探讨防治糖尿病并发症药物的研究概况。方法参阅近年来国内外文献资料,并进行整理、综述。结果概述了治疗糖尿病并发症的药物开发与研究进展,主要包括醛糖还原酶抑制剂、血管紧张素转换酶抑制剂、血管紧张素Ⅱ受体拮抗剂、内皮素受体拮抗剂、他汀类降脂药、抗氧剂、抗血小板药、钙拮抗剂等,简述了其作用机制、临床效果及应用前景。结论开发治疗糖尿病并发症的药物对提高糖尿病患者的生命质量具有重要意义。 展开更多
关键词 糖尿病并发症 醛糖还原酶抑制剂 血管紧张素转换酶抑制剂 内皮素受体拮抗剂 钙拮抗剂
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