Methazolamide
Editor-In-Chief: C. Michael Gibson, M.S., M.D. [1]; Associate Editor(s)-in-Chief: Gerald Chi
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Overview
Methazolamide is a carbonic anhydrase inhibitor that is FDA approved for the {{{indicationType}}} 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. Common adverse reactions include diarrhea, taste alterations, loss of appetite, nausea, vomiting, confusion, paresthesia, somnolence, polyuria, fatigue, and malaise.
Adult Indications and Dosage
FDA-Labeled Indications and Dosage (Adult)
Glaucoma
- Dosing Information
- 50–100 mg two or three times daily
Off-Label Use and Dosage (Adult)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Methazolamide in adult patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Methazolamide in adult patients.
Pediatric Indications and Dosage
FDA-Labeled Indications and Dosage (Pediatric)
- The safety and effectiveness of methazolamide in children have not been established.
Off-Label Use and Dosage (Pediatric)
Guideline-Supported Use
There is limited information regarding Off-Label Guideline-Supported Use of Methazolamide in pediatric patients.
Non–Guideline-Supported Use
There is limited information regarding Off-Label Non–Guideline-Supported Use of Methazolamide in pediatric patients.
Contraindications
- 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.
- Long-term administration of methazolamide is contraindicated in patients with angle-closure glaucoma, since organic closure of the angle may occur in spite of lowered intraocular pressure.
Warnings
- 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. 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.
Precautions
- Potassium excretion is increased initially upon administration of methazolamide and in patients with cirrhosis or hepatic insufficiency could precipitate a hepatic coma.
- In patients with pulmonary obstruction or emphysema, where alveolar ventilation may be impaired, methazolamide should be used with caution because it may precipitate or aggravate acidosis.
Laboratory Tests
- To monitor for hematologic reactions common to all sulfonamides, it is recommended that a baseline CBC and platelet count be obtained on patients prior to initiating methazolamide therapy and at regular intervals during therapy. If significant changes occur, early discontinuance and institution of appropriate therapy are important. Periodic monitoring of serum electrolytes is also recommended.
Adverse Reactions
Clinical Trials Experience
There is limited information regarding Clinical Trial Experience of Methazolamide in the drug label.
Central Nervous System
Cardiovascular
Respiratory
Gastrointestinal
Hypersensitivity
Miscellaneous
Postmarketing Experience
There is limited information regarding Postmarketing Experience of Methazolamide in the drug label.
Central Nervous System
Cardiovascular
Respiratory
Gastrointestinal
Hypersensitivity
Miscellaneous
Drug Interactions
- Methazolamide should be used with caution in patients on steroid therapy because of the potential for developing hypokalemia.
- 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.
Use in Specific Populations
Pregnancy
- Pregnancy Category
- Australian Drug Evaluation Committee (ADEC) Pregnancy Category
There is no Australian Drug Evaluation Committee (ADEC) guidance on usage of Methazolamide in women who are pregnant.
Labor and Delivery
There is no FDA guidance on use of Methazolamide during labor and delivery.
Nursing Mothers
There is no FDA guidance on the use of Methazolamide with respect to nursing mothers.
Pediatric Use
There is no FDA guidance on the use of Methazolamide with respect to pediatric patients.
Geriatic Use
There is no FDA guidance on the use of Methazolamide with respect to geriatric patients.
Gender
There is no FDA guidance on the use of Methazolamide with respect to specific gender populations.
Race
There is no FDA guidance on the use of Methazolamide with respect to specific racial populations.
Renal Impairment
There is no FDA guidance on the use of Methazolamide in patients with renal impairment.
Hepatic Impairment
There is no FDA guidance on the use of Methazolamide in patients with hepatic impairment.
Females of Reproductive Potential and Males
There is no FDA guidance on the use of Methazolamide in women of reproductive potentials and males.
Immunocompromised Patients
There is no FDA guidance one the use of Methazolamide in patients who are immunocompromised.
Administration and Monitoring
Administration
- Oral
- Intravenous
Monitoring
There is limited information regarding Monitoring of Methazolamide in the drug label.
Condition1
- Description
IV Compatibility
There is limited information regarding IV Compatibility of Methazolamide in the drug label.
Overdosage
Acute Overdose
Signs and Symptoms
- Description
Management
- Description
Chronic Overdose
There is limited information regarding Chronic Overdose of Methazolamide in the drug label.
Pharmacology
Methazolamide
| |
Systematic (IUPAC) name | |
N-(3-methyl-5-sulfamoyl-3H- 1,3,4-thiadiazol-2-ylidene) ethanamide | |
Identifiers | |
CAS number | |
ATC code | S01 |
PubChem | |
DrugBank | |
Chemical data | |
Formula | Template:OrganicBox atomTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox atomTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBoxTemplate:OrganicBox |
Mol. mass | 236.274 g/mol |
Pharmacokinetic data | |
Bioavailability | ? |
Protein binding | 55% |
Metabolism | ? |
Half life | 14 hours |
Excretion | ? |
Therapeutic considerations | |
Pregnancy cat. |
C(US) |
Legal status |
[[Prescription drug|Template:Unicode-only]](US) |
Routes | Oral |
Mechanism of Action
Structure
Pharmacodynamics
There is limited information regarding Pharmacodynamics of Methazolamide in the drug label.
Pharmacokinetics
There is limited information regarding Pharmacokinetics of Methazolamide in the drug label.
Nonclinical Toxicology
There is limited information regarding Nonclinical Toxicology of Methazolamide in the drug label.
Clinical Studies
There is limited information regarding Clinical Studies of Methazolamide in the drug label.
Condition1
- Description
How Supplied
Storage
There is limited information regarding Methazolamide Storage in the drug label.
Images
Drug Images
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Package and Label Display Panel
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Patient Counseling Information
There is limited information regarding Patient Counseling Information of Methazolamide in the drug label.
Precautions with Alcohol
- Alcohol-Methazolamide interaction has not been established. Talk to your doctor about the effects of taking alcohol with this medication.
Brand Names
- Neptazane®
- Glauctabs®[1]
Look-Alike Drug Names
- A® — B®[2]
Drug Shortage Status
Price
References
The contents of this FDA label are provided by the National Library of Medicine.
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