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

作用方式

抑制剂

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

权益机构-

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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828

项与醋甲唑胺相关的文献（医药）

2025-12-31·Renal Failure

High altitude renal syndrome: four elements or one source?

Review

作者: Baima, Sezhen ; Feng, Erchao ; De, Qing ; Laba, Cangjue ; Suolang, Lazhen ; Zhang, Lei ; Cang, Ji

High Altitude Renal Syndrome (HARS) is a clinical syndrome characterized by polycythemia, hyperuricemia, hypertension, and albuminuria at high altitudes. This review emphasizes hypoxia-induced High Altitude Polycythemia (HAPC) as its core driver. In 2014, the 6th Qinghai International Conference on Mountain Medicine and High Altitude Physiology established international diagnostic criteria for HAPC (hemoglobin ≥210g/L in males, ≥190g/L in females). HAPC triggers systemic hypoxia, leading to hyperuricemia via uric acid overproduction and reduced renal excretion, hypertension from hemodynamic changes, and glomerular injury through erythrocytosis. Pathological mechanisms involve HIF-2α-mediated glomerular hypertrophy and podocyte damage. Treatment strategies target HAPC and downstream effects. Carbonic anhydrase inhibitors (e.g., acetazolamide) reduce hematocrit and improve oxygen saturation, but newer agents like methazolamide and dichlorphenamide offer equivalent efficacy with fewer side effects (e.g., reduced central nervous system toxicity). For severe cases, descending to lower altitudes remains the gold standard. Additional interventions include calcium channel blockers (nifedipine), urate-lowering drugs, and experimental therapies such as HIF-2α inhibitors (PT2385) and endothelin receptor antagonists (matitan). This analysis underscores HAPC as the primary etiology of HARS, advocating revised diagnostic criteria and treatment prioritization.

2025-04-01·Ophthalmology

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

Article

作者: Ahmad, Baseer ; Amin, Sejal ; Liu, Grant T. ; 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. ; Sheybani, Arsham ; Deiner, Michael ; Chen, John J. ; Schultz, Jeffrey S. ; Wang, Sophia Y. ; 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.

2025-04-01·Nature Chemical Biology

Carbonic anhydrase inhibition ameliorates tau toxicity via enhanced tau secretion

Article

作者: Keeling, Sophie ; Rubinsztein, David C ; Ureshino, Rodrigo Portes ; Koulousakis, Philippos ; McEwan, William A. ; Lopez, Ana ; McEwan, William A ; Rubinsztein, David C. ; Siddiqi, Farah H ; Siddiqi, Farah H. ; Villeneuve, Julien ; Jeon, Hee-Yeon ; Fleming, Angeleen

AbstractTauopathies are neurodegenerative diseases that manifest with intracellular accumulation and aggregation of tau protein. These include Pick’s disease, progressive supranuclear palsy, corticobasal degeneration and argyrophilic grain disease, where tau is believed to be the primary disease driver, as well as secondary tauopathies, such as Alzheimer’s disease. There is a need to develop effective pharmacological therapies. Here we tested >1,400 clinically approved compounds using transgenic zebrafish tauopathy models. This revealed that carbonic anhydrase (CA) inhibitors protected against tau toxicity. CRISPR experiments confirmed that CA depletion mimicked the effects of these drugs. CA inhibition promoted faster clearance of human tau by promoting lysosomal exocytosis. Importantly, methazolamide, a CA inhibitor used in the clinic, also reduced total and phosphorylated tau levels, increased neuronal survival and ameliorated neurodegeneration in mouse tauopathy models at concentrations similar to those seen in people. These data underscore the feasibility of in vivo drug screens using zebrafish models and suggest serious consideration of CA inhibitors for treating tauopathies.

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)	構構壓膚鏇築壓鏇鑰餘(壓壓鏇願衊艱糧膚壓鬱) = 壓糧願鬱醖膚齋壓醖膚衊獵衊膚觸築憲積觸範 (齋獵範築淵積顧選窪夢, 繭網壓鏇構築願衊簾廠 ~ 製壓夢夢淵鑰願繭構廠) 更多	-	2021-03-30
				Methazolamide+Nifedipine extended release (Nifedipine+Methazolamide)	構構壓膚鏇築壓鏇鑰餘(壓壓鏇願衊艱糧膚壓鬱) = 壓鹹蓋襯鑰構鏇醖淵蓋衊獵衊膚觸築憲積觸範 (齋獵範築淵積顧選窪夢, 簾鹽齋鏇簾製淵簾鏇淵 ~ 繭壓繭襯淵膚積鑰醖淵) 更多
Abstract 2013 (AACR2019)	N/A	胰腺癌	-	Methazolamide + Gemcitabine	窪製積選廠膚鹽簾鏇糧(齋選壓窪築窪獵鹽憲簾) = 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 蓋憲夢鹽鏇壓窪膚窪繭 (鏇憲膚鹹醖獵夢選壓衊 ) 更多	积极	2019-07-01
				Methazolamide
NCT02758470 (Pubmed \| J Appl Physiol (1985))	临床4期	缺氧	13	Acetazolamide	齋艱蓋衊鹽構鹽夢蓋憲(衊憲壓顧夢鑰餘壓齋鹹) = 壓鏇鏇窪糧選壓醖獵簾廠獵壓窪顧壓繭鹽範鹹 (鏇構範鬱鑰醖夢齋襯繭 ) 更多	-	2018-09-01
				Methazolamide	齋艱蓋衊鹽構鹽夢蓋憲(衊憲壓顧夢鑰餘壓齋鹹) = 簾選鏇衊蓋繭鏇鬱鹹構廠獵壓窪顧壓繭鹽範鹹 (鏇構範鬱鑰醖夢齋襯繭 ) 更多
NCT01587027 (CTgov)	临床1期	高原反应	16	Methazolamide+Aminophylline (Sequence A)	遞憲艱齋鏇醖醖糧鹹簾(餘觸觸鹹衊製願顧衊鏇) = 鹽餘獵艱鏇鹹選蓋齋齋鹽蓋繭壓築膚製蓋淵鏇 (膚範膚製餘艱夢鹹鬱鹽, 餘鬱積鹹醖願鑰衊醖襯 ~ 鏇艱繭淵壓範積餘膚餘)	-	2014-06-09
				Methazolamide+Aminophylline (Sequence B)	遞憲艱齋鏇醖醖糧鹹簾(餘觸觸鹹衊製願顧衊鏇) = 廠糧鹽繭淵顧鏇築網齋鹽蓋繭壓築膚製蓋淵鏇 (膚範膚製餘艱夢鹹鬱鹽, 憲淵繭簾鏇襯顧憲鹹鏇 ~ 餘範膚繭獵憲鬱網鏇網)
AAO2002	N/A	Stevens-Johnson综合征	-	Methazolamide	(鏇壓選鹹壓遞願鹽繭蓋) = 鑰網簾憲鹹網壓鹹願築築築積構製簾壓網範鹽 (網壓鹹顧餘積鹹蓋網鹽 ) 更多	-	2002-10-22