Methazolamide
/api/v1/drug/methazolamideMechanism of action
Sourced from openFDAMechanism-of-action class: Carbonic Anhydrase Inhibitors.
Indications
Sourced from openFDA- Methazolamide Tablets are indicated in the treatment of ocular conditions where lowering intraocular pressure is likely to be of therapeutic benefit, such as chronic open-angle glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where lowering the intraocular pressure is desired before surgery.ICD-10: H40.9
Contraindications
Sourced from openFDA- Methazolamide therapy is contraindicated in situations in which sodium and/or potassium serum levels are depressed, in cases of marked kidney or liver disease or dysfunction, in adrenal gland failure, and in hyperchloremic acidosis. In patients with cirrhosis, use may precipitate the development of hepatic encephalopathy.contraindicated
Dosage & administration
Sourced from openFDAThe effective therapeutic dose administered varies from 50 mg to 100 mg two or three times daily. The drug may be used concomitantly with miotic and osmotic agents.
Warnings & precautions
Sourced from openFDAFatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias. Hypersensitivity reactions may recur when a sulfonamide is readministered, irrespective of the route of administration. If hypersensitivity or other serious reactions occur, the use of this drug should be discontinued. Caution is advised for patients receiving high-dose aspirin and methazolamide concomitantly, as anorexia, tachypnea, lethargy, coma, and death have been reported with concomitant use of high-dose aspirin and carbonic anhydrase inhibitors.
Adverse reactions
Sourced from openFDAAdverse reactions, occurring most often early in therapy, include paresthesias, particularly a “tingling” feeling in the extremities; hearing dysfunction or tinnitus; fatigue; malaise; loss of appetite; taste alteration; gastrointestinal disturbances such as nausea, vomiting, and diarrhea; polyuria; and occasional instances of drowsiness and confusion. Metabolic acidosis and electrolyte imbalance may occur. Transient myopia has been reported. This condition invariably subsides upon diminution or discontinuance of the medication. Other occasional adverse reactions include urticaria, melena, hematuria, glycosuria, hepatic insufficiency, flaccid paralysis, photosensitivity, convulsions, and, rarely, crystalluria and renal calculi. Also see PRECAUTIONS: Information for Patients for possible reactions common to sulfonamide derivatives. Fatalities have occurred, although rarely, due to severe reactions to sulfonamides including Stevens-Johnson syndrome, toxic epidermal necrolysis, fulminant hepatic necrosis, agranulocytosis, aplastic anemia, and other blood dyscrasias (see WARNINGS ). To report SUSPECTED ADVERSE REACTIONS, contact NorthStar Rx LLC at 1-800-206-7821 or FDA at 1-800-FDA-1088 or www.fda.gov/medwatch.
Use in specific populations
Sourced from openFDAPregnancy Teratogenic effects Methazolamide has been shown to be teratogenic (skeletal anomalies) in rats when given in doses approximately 40 times the human dose. There are no adequate and well controlled studies in pregnant women. Methazolamide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus.
Overdosage
Sourced from openFDANo data are available regarding methazolamide overdosage in humans as no cases of acute poisoning with this drug have been reported. Animal data suggest that even a high dose of methazolamide is nontoxic. No specific antidote is known. Treatment should be symptomatic and supportive. Electrolyte imbalance, development of an acidotic state, and central nervous system effects might be expected to occur. Serum electrolyte levels (particularly potassium) and blood pH levels should be monitored. Supportive measures may be required to restore electrolyte and pH balance.
Approval history
Sourced from openFDA- Jun 30, 1993ANDAANDA040001Ani Pharms
- Jan 27, 1994ANDAANDA040062Anda Repository
- Oct 5, 2018ANDAANDA207438Bausch And Lomb Inc
- Oct 18, 2022ANDAANDA215615Tagi
- Feb 9, 2026ANDAANDA217408Ajanta Pharma Ltd
FAERS reports
- 1Drug Ineffective4012%
- 2Fatigue3611%
- 3Dizziness299.0%
- 4Headache288.6%
- 5Dyspnoea268.0%
- 6Off Label Use247.4%
- 7Blood Pressure Increased226.8%
- 8Asthenia216.5%
- 9Anxiety206.2%
- 10Death206.2%
- 11Pain In Extremity206.2%
- 12Fall185.6%
- 13Malaise185.6%
- 14Nasopharyngitis185.6%
- 15Arthralgia175.2%
Literature
Recent PubMed references pinned to Methazolamide as a MeSH major topic. Citations link to pubmed.ncbi.nlm.nih.gov.
- Efficient quantification of methazolamide in rat plasma using UHPLC-Q-Orbitrap MS for pharmacokinetic analysis.Analytical methods : advancing methods and applications · 2026 · Wang X, Zou QLPMID 41586802DOI 10.1039/d5ay00276a
- Cerebral proteome adaptations to amyloid angiopathy are prevented by carbonic anhydrase inhibitors.Alzheimer's & dementia : the journal of the Alzheimer's Association · 2025 · Carlsen J, Fossati S, Østergaard L, et al.PMID 40285374DOI 10.1002/alz.70122
- Role of intermittent hypoxic training combined with methazolamide in the prevention of high-altitude cerebral edema in rats.Scientific reports · 2024 · Peng W, Ma H, Zhao R, et al.PMID 39632926DOI 10.1038/s41598-024-81226-z
- Effects of two carbonic anhydrase inhibitors on exercise performance in acute hypoxia.Journal of applied physiology (Bethesda, Md. : 1985) · 2024 · Chang JC, Thompson BP, Doherty CJ, et al.PMID 39480272DOI 10.1152/japplphysiol.00589.2024
- Methazolamide Reduces the AQP5 mRNA Expression and Immune Cell Migration-A New Potential Drug in Sepsis Therapy?International journal of molecular sciences · 2024 · Rump K, Koos B, Ziehe D, et al.PMID 38203778DOI 10.3390/ijms25010610
- Revealing mechanism of Methazolamide for treatment of ankylosing spondylitis based on network pharmacology and GSEA.Scientific reports · 2023 · Sun T, Wang M, Liang W, et al.PMID 37717047DOI 10.1038/s41598-023-42721-x
- Association of HLA-C*01:02 with methazolamide-induced toxic epidermal necrolysis.BMJ case reports · 2022 · Qiumei G, Zhengju C, Xuefei H, et al.PMID 36572447DOI 10.1136/bcr-2022-250048
- Detection, identification, characterization, and high-performance liquid chromatography quantification of five impurities from a methazolamide product.Journal of separation science · 2022 · Shen Q, He Q, Pan Y, et al.PMID 35691018DOI 10.1002/jssc.202200122
Clinical trials
The 10 most recently updated of 11 ClinicalTrials.gov registrations naming Methazolamide as an intervention. Registration is not evidence of efficacy or safety — reference crosswalk only.
- Stop Retinal Ganglion Cell Dysfunction StudyTerminated · Phase 3 · Interventional · 28 enrolled · University of MiamiNCT02390284updated 2025-08-26
- Acamprosate and Methazolamide for Essential TremorWithdrawn · Phase 2 · Interventional · 0 enrolled · Henry Ford Health SystemNCT06312800updated 2024-09-25
- Effect of Acetazolamide and Methazolamide on Hypoxic Exercise PerformanceCompleted · Phase 4 · Interventional · 15 enrolled · University of WaterlooNCT05575180updated 2024-03-12
- Use of Methazolamide to Lower Intraocular PressureActive not recruiting · Phase 4 · Interventional · 30 enrolled · University of Colorado, DenverNCT05498103updated 2024-02-06
- Three New Ideas to Protect Special Forces From the Stress of High AltitudeCompleted · Phase 4 · Interventional · 148 enrolled · University of Colorado, DenverNCT02463357updated 2021-03-30
- Comparison of Two Different Sedation Protocols During Transvaginal Oocyte RetrievalTerminated · Observational · 80 enrolled · Attikon HospitalNCT03362021updated 2020-09-22
- Improving Tumor Oxygenation in Cervical CancerWithdrawn · Phase 2 · Interventional · 0 enrolled · University of California, IrvineNCT00257829updated 2018-12-03
- Muscle Fatigue and Carbonic Anhydrase InhibitorsCompleted · Phase 4 · Interventional · 13 enrolled · University of British ColumbiaNCT02758470updated 2018-09-25
- Safety Evaluation of Aminophylline and MethazolamideCompleted · Phase 1 · Interventional · 16 enrolled · Poudre Valley Health SystemNCT01587027updated 2017-02-10
- AZ, MZ, and the Pulmonary System Response to HypoxiaCompleted · Phase 4 · Interventional · 14 enrolled · University of British ColumbiaNCT02760121updated 2016-10-19
Pharmacogenomics
CPIC-curated drug–gene pairs for Methazolamide. Levels describe the strength of curated evidence and guideline status — never a recommendation to test or to adjust therapy.
- HLA-BCPIC C (provisional)ClinPGx 2A
- HLA-CCPIC C (provisional)ClinPGx 2B
Frequently asked questions
- How does Methazolamide work?
- Mechanism-of-action class: Carbonic Anhydrase Inhibitors.
- What is Methazolamide used for?
- According to FDA labeling, Methazolamide carries indications including: Methazolamide Tablets are indicated in the treatment of ocular conditions where lowering intraocular pressure is likely to be of therapeutic benefit, such as chronic open-angle glaucoma, secondary glaucoma, and preoperatively in acute angle-closure glaucoma where lowering the intraocular pressure is desired before surgery.. This is a reference summary of labeled uses, not medical advice or a treatment recommendation.
- What class of drug is Methazolamide?
- Methazolamide is classified as Carbonic anhydrase inhibitors, Carbonic Anhydrase Inhibitors, Decreased Intraocular Fluid Pressure, Increased Proximal Tubule Cl- Excretion, Increased Proximal Tubule HCO3- Excretion, Increased Proximal Tubule K+ Excretion, Increased Proximal Tubule Na+ Excretion.
- What are the contraindications for Methazolamide?
- Methazolamide labeling lists contraindications including: Methazolamide therapy is contraindicated in situations in which sodium and/or potassium serum levels are depressed, in cases of marked kidney or liver disease or dysfunction, in adrenal gland failure, and in hyperchloremic acidosis. In patients with cirrhosis, use may precipitate the development of hepatic encephalopathy.. Always consult the full prescribing information and a clinician.
methazolamide is illustrative MVP content compiled from public sources. pharmacopeia is for educational and informational use only and is not a substitute for professional medical advice.