醋甲唑胺(Methazolamide) - 药物靶点：CAs_在研适应症：青光眼_专利_临床

概要

基本信息

药物类型

小分子化药

别名

Methazolamide (JAN/USP/INN)、Methenamide、Neptazaneat

+ [6]

靶点

CAs

作用机制

CAs抑制剂(碳酸酐酶家族抑制剂)

治疗领域

眼部疾病

在研适应症

青光眼

非在研适应症-

原研机构

Lederle Laboratories

在研机构-

非在研机构

Lederle Laboratories

最高研发阶段批准上市

首次获批日期

美国 (1959-01-26),

青光眼

最高研发阶段(中国)批准上市

特殊审评-

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结构/序列

分子式C5H8N4O3S2

InChIKeyFLOSMHQXBMRNHR-UHFFFAOYSA-N

CAS号554-57-4

关联

14

项与醋甲唑胺相关的临床试验

ChiCTR2400089203

/ Suspended临床4期IIT

Comparative Study on the Clinical Efficacy of Methazolamide and Acetazolamide in the Prevention of Acute Mountain Sickness

开始日期2024-09-08

申办/合作机构-

NCT05575180

/ Completed临床4期IIT

Effect of Acetazolamide and Methazolamide on Hypoxic Exercise Performance

A single-centered randomized doubled blinded placebo-controlled cross-over trial comparing two the effect of two carbonic anhydrase inhibitors on exercise performance in acute hypoxia. Participants will be young (under 40 years of age), healthy males and females who are regularly physically active.

开始日期2023-08-11

申办/合作机构

The University of Waterloo

[+1]

NCT05498103

/ Active, not recruiting临床4期IIT

Use of Methazolamide to Lower Intraocular Pressure

The purpose of this study is to evaluate the effect of methazolamide, 25 mg or 50 mg tablets once a day for a week than twice a day for a week, on lowering intraocular pressure and the safety of methazolamide.

开始日期2023-02-17

申办/合作机构

University of Colorado Denver

100 项与醋甲唑胺相关的临床结果

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100 项与醋甲唑胺相关的转化医学

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100 项与醋甲唑胺相关的专利（医药）

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421

项与醋甲唑胺相关的文献（医药）

2024-12-12·Blood

Procoagulant platelet activation promotes venous thrombosis

Article

作者: Schmid, Michael ; Anjum, Afra ; Kääb, Lily ; Di Fina, Lea ; Kranich, Jan ; Stark, Konstantin ; Massberg, Steffen ; Loew, Quentin ; Akhalkatsi, Anastassia ; Escaig, Raphael ; Yue, Keyang ; Nicolai, Leo ; Thienel, Manuela ; Li, Lukas ; Kilani, Badr ; Pekayvaz, Kami ; Laun, Lisa ; Dewender, Robin ; Gold, Christoph ; Mulkers, Maité ; Kaiser, Rainer ; Gmeiner, Jonas ; Brocker, Thomas ; Stermann, Julia ; Kammerer, Lisa ; Mueller, Tonina T. ; Eivers, Luke ; Rossaro, Dario ; Akgöl, Sezer ; Krächan, Angelina

AbstractPlatelets are key players in cardiovascular disease, and platelet aggregation represents a central pharmacologic target, particularly in secondary prevention. However, inhibition of adenosine diphosphate and thromboxane signaling has low efficacy in preventing venous thromboembolism, necessitating the inhibition of the plasmatic coagulation cascade in this disease entity. Anticoagulation carries a significantly higher risk of bleeding complications, highlighting the need of alternative therapeutic approaches. We hypothesized that procoagulant activation (PA) of platelets promotes venous thrombus formation and that targeting PA could alleviate venous thrombosis. Here, we found elevated levels of procoagulant platelets in the circulation and in thrombi of patients with deep vein thrombosis (DVT) and pulmonary embolism, and in mice developing DVT following inferior vena cava stenosis. Furthermore, we detected PA of recruited platelets within murine venous thrombi and human pulmonary emboli. Mice with platelet-specific deficiency in central pathways of PA—cyclophilin D and transmembrane protein 16F—were more resistant toward low flow–induced venous thrombosis. Finally, we found that a clinically approved carbonic anhydrase inhibitor, methazolamide, reduced platelet procoagulant activity and alleviated murine thrombus formation without affecting trauma-associated hemostasis. These findings identify an essential role of platelet procoagulant function in venous thrombosis and delineate novel pharmacologic strategies targeting platelets in the prevention of venous thromboembolism.

2024-12-01·Journal of Applied Physiology

Effects of two carbonic anhydrase inhibitors on exercise performance in acute hypoxia

Article

作者: Foster, Glen E. ; Thompson, Benjamin P. ; Mann, Leah M. ; Swenson, Erik R. ; Doherty, Connor J. ; Dominelli, Paolo B. ; Berdeklis, Antonia N. ; Chang, Jou-Chung ; Tupling, A. Russell

Administration of acetazolamide (AZ) and methazolamide (MZ) both resulted in a significantly slower 5-km time trial in acute normobaric hypoxia compared with a placebo. Both drugs lead to a partially compensated metabolic acidosis, but ventilation and oxyhemoglobin saturation were not different across the conditions. Overall, acetazolamide and methazolamide both impaired whole body exercise performance in acute normobaric hypoxia but potentially have different mechanisms of action.

2024-11-01·Ophthalmology

Nationwide Prevalence and Geographic Variation of Idiopathic Intracranial Hypertension among Women in the United States

Article

作者: Ahmad, Baseer ; Liu, Grant T. ; Amin, Sejal ; Kim, B. Michelle ; Stein, Joshua ; Pershing, Suzann ; Munir, Saleha ; Shrivastava, Anurag ; Feldman, Robert ; Fraz, Muhammad A. ; Woreta, Fasika ; DeLott, Lindsey ; Sarrapour, Soshian ; Bryar, Paul ; Nwanyanwu, Kristen ; Vanderbeek, Brian L. ; McMillian, Brian ; Lum, Flora ; Munir, Wuqaas ; Stagg, Brian C. ; Ramachandran, Rajeev ; Chen, Jinbo ; Patnaik, Jenna ; French, Dustin ; Sun, Catherine ; Lynch, Anne M. ; Schultz, Jeffrey S. ; Deiner, Michael ; Wang, Sophia Y. ; Chen, John J. ; Sheybani, Arsham ; Srikumaran, Divya ; Hamedani, Ali G. ; Edwards, Paul A. ; Wirostko, Barbara

PURPOSETo determine the nationwide prevalence and geographic distribution of idiopathic intracranial hypertension (IIH) among women in the United States.DESIGNRetrospective cross-sectional study using Medicaid claims and electronic health record data from the IRIS® Registry (Intelligent Research in Sight) and Sight Outcomes Research Collaborative (SOURCE).PARTICIPANTSFemale Medicaid beneficiaries 18 to 55 years of age with IIH diagnoses and prescriptions for acetazolamide or methazolamide in 2018 were identified, excluding those with other causes of intracranial hypertension. We calculated the proportion of women with IIH in the United States who were insured by Medicaid by combining analyses from the IRIS Registry and SOURCE.METHODSTo calculate the number of women with IIH in each state, we divided the number of Medicaid beneficiaries by the proportion of patients insured by Medicaid. We used census data from the 2018 American Community Survey to calculate prevalence.MAIN OUTCOME MEASURESWe examined geographic variation in IIH prevalence using Moran's I statistic and compared it to obesity prevalence data from the 2018 Behavioral Risk Factor Surveillance System. In a validation study, we compared the calculated prevalence of IIH in Minnesota with similar data from the Rochester Epidemiology Project.RESULTSOf 13 959 female Medicaid beneficiaries with IIH, 6828 had a prescription for acetazolamide or methazolamide. In the IRIS Registry and SOURCE, 25% of women with IIH were insured by Medicaid (95% confidence interval [CI], 16%-33%), suggesting that 27 312 women 18 to 55 years of age with IIH were taking acetazolamide or methazolamide in 2018 (6828 / 0.25 = 27 312). Prevalence was 3.44 per 10 000 women (95% CI, 2.61-5.39 per 10 000 women), and significant geographic variation was found (Moran I statistic, 0.20; P = 0.03), with higher prevalence in states where obesity was more common. The calculated prevalence of IIH in Minnesota was statistically equivalent to that identified using Rochester Epidemiology Project data (P < 0.05 for equivalence test).CONCLUSIONSIdiopathic intracranial hypertension affects 3.44 per 10 000 women 18 to 55 years of age in the United States with significant geographic variation, some of which is explained by variation in obesity prevalence.FINANCIAL DISCLOSURE(S)Proprietary or commercial disclosure may be found in the Footnotes and Disclosures at the end of this article.

100 项与醋甲唑胺相关的药物交易

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外链

KEGG	Wiki	ATC	Drug Bank
D00655	醋甲唑胺	S01EC05	DB00703

研发状态

10 条最早获批的记录,

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适应症	国家/地区	公司	日期
青光眼	美国	-	-

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临床结果

适应症

分期

评价

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研究	分期	人群特征	评价人数	分组	结果	评价	发布日期


NCT02463357 (CTgov)	临床4期	高原反应	148	Quercetin (Quercetin)	襯獵鏇築齋鏇壓鹹壓願(壓築築鹽繭憲窪齋網繭) = 齋淵鏇齋鏇網醖淵觸獵憲鏇淵鬱顧鑰選觸鹹餘 (鑰製繭醖構齋蓋窪襯積, 鹹齋簾糧範遞選襯齋觸 ~ 淵衊顧蓋憲顧範範積顧) 更多	-	2021-03-30
				Methazolamide+Nifedipine extended release (Nifedipine+Methazolamide)	襯獵鏇築齋鏇壓鹹壓願(壓築築鹽繭憲窪齋網繭) = 構鹽鏇醖築糧構顧膚夢憲鏇淵鬱顧鑰選觸鹹餘 (鑰製繭醖構齋蓋窪襯積, 簾獵繭鏇範糧醖觸獵淵 ~ 醖醖淵廠獵衊構窪窪餘) 更多
Abstract 2013 (AACR2019)	N/A	胰腺癌	-	Methazolamide + Gemcitabine	夢簾遞憲鏇廠願繭鏇觸(壓顧壓餘顧淵觸構範艱) = anti-angiogenic potential viz. would healing, tube formation and expression of important anti-angiogenic markers like HIF1α, VEGF were profoundly modulated in MZM and combination group 膚艱廠艱築遞築鹽製衊 (鏇膚鹽獵衊壓鑰範窪繭 ) 更多	积极	2019-07-01
				Methazolamide
NCT02758470 (Pubmed \| J Appl Physiol (1985))	临床4期	缺氧	13	Acetazolamide	襯鹹顧鏇範鹽襯網齋範(醖鹹鹽顧夢願醖壓獵網) = 簾鏇夢夢窪憲襯繭鑰淵齋願襯壓製簾憲膚齋廠 (觸壓蓋遞鹽顧艱簾廠膚 ) 更多	-	2018-09-01
				Methazolamide	襯鹹顧鏇範鹽襯網齋範(醖鹹鹽顧夢願醖壓獵網) = 憲憲衊鑰襯觸蓋鹹鬱夢齋願襯壓製簾憲膚齋廠 (觸壓蓋遞鹽顧艱簾廠膚 ) 更多
NCT01587027 (CTgov)	临床1期	高原反应	16	Methazolamide+Aminophylline (Sequence A)	膚醖鑰齋鏇壓鹽壓襯齋(廠齋壓廠願廠窪願積鹽) = 鑰鹽選憲壓網窪遞製醖艱淵淵製遞淵觸窪築鑰 (鏇憲範網築顧憲築壓鑰, 窪顧齋觸願構觸襯齋蓋 ~ 積夢鏇簾築餘範願衊鹽)	-	2014-06-09
				Methazolamide+Aminophylline (Sequence B)	膚醖鑰齋鏇壓鹽壓襯齋(廠齋壓廠願廠窪願積鹽) = 壓襯鑰襯繭鬱廠餘鏇範艱淵淵製遞淵觸窪築鑰 (鏇憲範網築顧憲築壓鑰, 獵簾鑰積蓋顧壓選繭觸 ~ 鏇膚顧鹹衊艱夢壓獵糧)
AAO2002	N/A	Stevens-Johnson综合征	-	Methazolamide	(鑰醖衊鏇衊繭廠鏇繭廠) = 蓋鏇簾鹽齋壓醖膚憲繭襯襯艱糧廠簾壓獵廠廠 (觸艱壓製壓繭壓夢簾鏇 ) 更多	-	2002-10-22