Methazolamide

SENSORY ORGANS

Key facts

Methazolamide is an ofp drug catalogued in DrugCentral. It was first approved by the FDA in 1959. DrugCentral lists 34 molecular targets, including CA3, CA7 and CA5A|CA5B. Recorded indications include Angle-closure glaucoma, Open-angle glaucoma and Secondary glaucoma.

• Approval status: ofp (first approved 1959 by the FDA).
• Molecular targets: CA3, CA7, CA5A|CA5B and CA12 (34 listed in DrugCentral).
• Indications: Angle-closure glaucoma, Open-angle glaucoma and Secondary glaucoma.
• ATC code: S01EC05 (Carbonic anhydrase inhibitors).
• Molecular formula: C5H8N4O3S2; molecular weight 236.26 g/mol.

Indications & contraindications

Drug–disease relationships curated by DrugCentral (OMOP / SNOMED concepts).

Indications (3)

• Angle-closure glaucoma
• Open-angle glaucoma
• Secondary glaucoma

Off-label uses (1)

• Malignant glaucoma

Contraindications (17)

• Acute nephropathy
• Decreased respiratory function
• Diabetes mellitus type 1
• Diabetes mellitus type 2
• Disease of blood AND/OR blood-forming organ
• Disease of liver
• Disorder of electrolytes
• Gout
• Hepatic failure
• Hyperkalemia
• Hyponatremia
• Kidney disease
• Metabolic acidosis, normal anion gap, acidifying salts
• Primary adrenocortical insufficiency
• Recurrent Calcium Renal Calculi
• Renal tubular acidosis
• Respiratory acidosis

Mechanism & targets

Molecular targets (34)

Target	Gene	Action	Activity
Carbonic anhydrase 3	CA3	unknown	Ki 8.96
Carbonic anhydrase 7	CA7	inhibitor	Ki 8.68
Carbonic anhydrase V	CA5A|CA5B	unknown	Ki 8.60
Carbonic anhydrase 12	CA12	unknown	Ki 8.47
Carbonate dehydratase	—	unknown	Ki 8.09
Carbonic anhydrase 2	CA2	inhibitor	Ki 8.05
Carbonic anhydrase 6	CA6	unknown	Ki 8.00
Carbonic anhydrase	NCE103	unknown	Ki 7.85
Carbonic anhydrase 1	CA1	inhibitor	Ki 7.85
Carbonic anhydrase 13	CA13	unknown	Ki 7.72
Carbonic anhydrase 13	Ca13	unknown	Ki 7.72
Carbonic anhydrase	CA12|CA1|CA2|CA3|CA4|CA6|CA5A|CA7|CA9|CA13|CA14|CA5B	unknown	IC50 7.70
Alpha carbonic anhydrase	CA	unknown	Ki 7.67
Carbonic anhydrase, alpha family	—	unknown	Ki 7.58
Carbonic anhydrase 9	CA9	unknown	Ki 7.57
Carbonic anhydrase 4	CA4	unknown	Ki 7.44
Carbonic anhydrase 14	CA14	unknown	Ki 7.37
Carbonic anhydrase 5B, mitochondrial	CA5B	unknown	Ki 7.21
Carbonic anhydrase 2	CAN2	unknown	Ki 7.20
Carbonic anhydrase 5A, mitochondrial	CA5A	unknown	Ki 7.19

Regulatory approvals (1)

Date	Agency	Marketed as	Applicant	Orphan
1959-01-26	FDA	—	LEDERLE

ATC classification

ATC code	Therapeutic hierarchy
S01EC05	SENSORY ORGANS › OPHTHALMOLOGICALS › ANTIGLAUCOMA PREPARATIONS AND MIOTICS › Carbonic anhydrase inhibitors

Reported adverse-event signals

Strongest FDA FAERS disproportionality signals (log-likelihood ratio). A signal is a statistical association in spontaneous reports, not proof that the drug causes the event.

MedDRA term	LLR
Nerve degeneration	92.7
Renal neoplasm	64.5
Abdominal rigidity	61.0
Renal mass	59.6
Middle insomnia	48.9
Metastasis	48.6

Chemical structure

• Molecular formula: C₅H₈N₄O₃S₂
• Molecular weight: 236.26 g/mol
• CAS number: 554-57-4
• InChIKey: FLOSMHQXBMRNHR-UHFFFAOYSA-N
• PubChem CID: 4100

CN1N=C(SC1=NC(C)=O)S(N)(=O)=O

Frequently asked questions

Answers are generated from the structured data on this page, not written by hand.

What is Methazolamide used for?

DrugCentral lists the following indications for Methazolamide: Angle-closure glaucoma, Open-angle glaucoma and Secondary glaucoma.

How does Methazolamide work?

Its molecular targets in DrugCentral include CA3, CA7 (inhibitor), CA5A|CA5B and CA12.

When was Methazolamide first approved?

Methazolamide was first approved by the FDA in 1959.

What is the chemical formula of Methazolamide?

Methazolamide has the molecular formula C5H8N4O3S2 and a molecular weight of 236.26 g/mol.

Sources

• DrugCentral drug card 1741 — structure, indications, targets, approvals, pharmacologic classes (CC BY-SA 4.0)
• ChEMBL CHEMBL19 — compound record and bioactivity
• PubChem CID 4100 — chemical identifiers
• DrugBank DB00703 — drug record
• FDA UNII W733B0S9SD — substance identity
• DailyMed: FDA labels for Methazolamide — current prescribing information (label search)
• UniProt P07451 (CA3) — target protein
• UniProt P43166 (CA7) — target protein
• UniProt O43570 (CA12) — target protein
• UniProt P00918 (CA2) — target protein
• UniProt P23280 (CA6) — target protein
• UniProt P00915 (CA1) — target protein
• FDA Adverse Event Reporting System (openFDA FAERS) — adverse-event signals, as aggregated by DrugCentral

How this page is built: methodology · editorial policy & corrections.