Delving into the Latest Updates on Methazolamide with Synapse

Overview

Basic Info

Drug Type

Small molecule drug

Synonyms

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

+ [6]

Target

CAs

Action

inhibitors

Mechanism

CAs inhibitors(Carbonic anhydrases inhibitors)

Therapeutic Areas

Eye Diseases

Active Indication

Glaucoma

Inactive Indication-

Originator Organization

Lederle Laboratories

Active Organization-

Inactive Organization

Lederle Laboratories

License Organization-

Drug Highest PhaseApproved

First Approval Date

United States (26 Jan 1959),

Glaucoma

Regulation-

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Structure/Sequence

Molecular FormulaC5H8N4O3S2

InChIKeyFLOSMHQXBMRNHR-UHFFFAOYSA-N

CAS Registry554-57-4

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.

01 Apr 2025·Ophthalmology

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

Article

Author: 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.

01 Apr 2025·Nature Chemical Biology

Carbonic anhydrase inhibition ameliorates tau toxicity via enhanced tau secretion

Article

Author: 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 Deals associated with Methazolamide

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External Link

KEGG	Wiki	ATC	Drug Bank
D00655	Methazolamide	S01EC05	DB00703

R&D Status

10 top approved records.

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Indication	Country/Location	Organization	Date
Glaucoma	United States	-	-

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Clinical Result

Indication

Phase

Evaluation

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Study	Phase	Population	Analyzed Enrollment	Group	Results	Evaluation	Publication Date


NCT02463357 (CTgov)	Phase 4	Altitude Sickness	148	Quercetin (Quercetin)	gnomxzsivt(zxpsnbiqas) = svhofdqpuc uvxmubdhec (hrtvwzhzjq, fgwbfprdkh - rpgzwxflyk) View more	-	30 Mar 2021
				Methazolamide+Nifedipine extended release (Nifedipine+Methazolamide)	gnomxzsivt(zxpsnbiqas) = oijlnjekoc uvxmubdhec (hrtvwzhzjq, tfojrwsmpx - eiifvdwpsw) View more
Abstract 2013 (AACR2019)	Not Applicable	Pancreatic Cancer	-	Methazolamide + Gemcitabine	btmvyfzpky(xgqtvmuwlt) = 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 xixhhawsny (ssgtbphmum ) View more	Positive	01 Jul 2019
				Methazolamide
NCT02758470 (Pubmed \| J Appl Physiol (1985))	Phase 4	Hypoxia	13	Acetazolamide	fhntrvmdce(afmkbhozho) = cbqmdxkpte ikrrazlfjd (imxohykgvl ) View more	-	01 Sep 2018
				Methazolamide	fhntrvmdce(afmkbhozho) = cwqengcrxw ikrrazlfjd (imxohykgvl ) View more
NCT01587027 (CTgov)	Phase 1	Altitude Sickness	16	Methazolamide+Aminophylline (Sequence A)	kjrcqrtaac(ddyfwjqiwd) = zrxtntfvnf zxgaexqrmt (mmitskugux, grhhrdfjdg - kcfndndrew)	-	09 Jun 2014
				Methazolamide+Aminophylline (Sequence B)	kjrcqrtaac(ddyfwjqiwd) = pelzasmjna zxgaexqrmt (mmitskugux, emccptqahd - ebqcuglqza)
AAO2002	Not Applicable	Stevens-Johnson Syndrome	-	Methazolamide	(ozbdygimcn) = apkqmizwjg yzsccaeoux (nvoumesmdy ) View more	-	22 Oct 2002