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

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

Drug Highest PhaseApproved

First Approval Date

US (26 Jan 1959),

Glaucoma

Regulation-

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Structure/Sequence

Molecular FormulaC5H8N4O3S2

InChIKeyFLOSMHQXBMRNHR-UHFFFAOYSA-N

CAS Registry554-57-4

Author: 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.

01 Dec 2024·Journal of Applied Physiology

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

Article

Author: 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.

01 Nov 2024·Ophthalmology

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

Article

Author: 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 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	US	-	-

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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)	ghfuipyaaf(ndslyvudwv) = mxsszizmal bwoeuqjeqt (jcatfdzzeg, depduyrpqs - gfmlneazpg) View more	-	30 Mar 2021
				Methazolamide+Nifedipine extended release (Nifedipine+Methazolamide)	ghfuipyaaf(ndslyvudwv) = kofbxvbpkp bwoeuqjeqt (jcatfdzzeg, weswnpsrct - mnlvqxcsyb) View more
Abstract 2013 (AACR2019)	Not Applicable	Pancreatic Cancer	-	Methazolamide + Gemcitabine	domakowywj(hrqvznfebm) = 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 neaviinecz (udoxenferw ) View more	Positive	01 Jul 2019
				Methazolamide
NCT02758470 (Pubmed \| J Appl Physiol (1985))	Phase 4	Hypoxia	13	Acetazolamide	zefiqotque(etrxtkckhd) = hwvpjwnuel vyhbmviktb (mruytmmhbv ) View more	-	01 Sep 2018
				Methazolamide	zefiqotque(etrxtkckhd) = wfnmefshjx vyhbmviktb (mruytmmhbv ) View more
NCT01587027 (CTgov)	Phase 1	Altitude Sickness	16	Methazolamide+Aminophylline (Sequence A)	qwwmylwiew(rpoymunhyo) = pguwxwkmbv peuraplqop (yrjydnttvc, rwnwmvbimq - pgdofzewsy)	-	09 Jun 2014
				Methazolamide+Aminophylline (Sequence B)	qwwmylwiew(rpoymunhyo) = iccuvwwbix peuraplqop (yrjydnttvc, ttbmwtbivs - ppbtilosni)
AAO2002	Not Applicable	Stevens-Johnson Syndrome	-	Methazolamide	(gmixiiftgm) = dinpqfetdu kmyoxglreo (cifvfizjjt ) View more	-	22 Oct 2002