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Methazolamide: Drug information

Methazolamide: Drug information
(For additional information see "Methazolamide: Patient drug information")

For abbreviations, symbols, and age group definitions used in Lexicomp (show table)
Pharmacologic Category
  • Carbonic Anhydrase Inhibitor;
  • Diuretic, Carbonic Anhydrase Inhibitor;
  • Ophthalmic Agent, Antiglaucoma
Dosing: Adult
Glaucoma

Glaucoma: Oral: 50 to 100 mg 2 to 3 times daily.

Dosing: Kidney Impairment: Adult

Contraindicated in marked renal dysfunction.

Dosing: Hepatic Impairment: Adult

Contraindicated in marked hepatic dysfunction.

Dosing: Older Adult

Refer to adult dosing.

Adverse Reactions

The following adverse drug reactions and incidences are derived from product labeling unless otherwise specified. Frequency not defined.

Central nervous system: Confusion, drowsiness, fatigue, flaccid paralysis, malaise, paresthesia, seizure

Dermatologic: Erythema multiforme, skin photosensitivity, skin rash, Stevens-Johnson syndrome, toxic epidermal necrolysis, urticaria

Endocrine & metabolic: Electrolyte disturbance, glycosuria, metabolic acidosis

Gastrointestinal: Decreased appetite, diarrhea, dysgeusia, melena, nausea, vomiting

Genitourinary: Crystalluria, hematuria

Hematologic & oncologic: Agranulocytosis, aplastic anemia, bone marrow depression, hemolytic anemia, immune thrombocytopenia, leukopenia, pancytopenia

Hepatic: Fulminant hepatic necrosis, hepatic insufficiency

Hypersensitivity: Anaphylaxis, hypersensitivity reaction

Ophthalmic: Myopia

Otic: Auditory disturbance, tinnitus

Renal: Nephrolithiasis, polyuria

Miscellaneous: Fever

Contraindications

Marked kidney or liver dysfunction; adrenal gland failure; cirrhosis; hyperchloremic acidosis; hyponatremia; hypokalemia; long-term treatment of angle-closure glaucoma

Warnings/Precautions

Concerns related to adverse effects:

• CNS effects: May impair mental alertness and/or physical coordination.

• Electrolyte disturbance: Initially, potassium excretion may be increased; periodically monitor serum electrolytes and signs of hypokalemia in at risk patients.

• Sulfonamide (“sulfa”) allergy: The FDA-approved product labeling for many medications containing a sulfonamide chemical group includes a broad contraindication in patients with a prior allergic reaction to sulfonamides. There is a potential for cross-reactivity between members of a specific class (eg, two antibiotic sulfonamides). However, concerns for cross-reactivity have previously extended to all compounds containing the sulfonamide structure (SO2NH2). An expanded understanding of allergic mechanisms indicates cross-reactivity between antibiotic sulfonamides and nonantibiotic sulfonamides may not occur or at the very least this potential is extremely low (Brackett 2004; Johnson 2005; Slatore 2004; Tornero 2004). In particular, mechanisms of cross-reaction due to antibody production (anaphylaxis) are unlikely to occur with nonantibiotic sulfonamides. T-cell-mediated (type IV) reactions (eg, maculopapular rash) are less well understood and it is not possible to completely exclude this potential based on current insights. In cases where prior reactions were severe (Stevens-Johnson syndrome/TEN), some clinicians choose to avoid exposure to these classes.

Disease-related concerns:

• Diabetes: Use with caution in patients with prediabetes or diabetes mellitus; may see a change in glucose control.

• Hepatic impairment: Use with caution in patients with hepatic impairment; may precipitate hepatic encephalopathy. Use is contraindicated in patients with marked liver impairment or cirrhosis.

• Respiratory disease: Use with caution in patients with respiratory disease such as emphysema or pulmonary obstruction; may precipitate or aggravate respiratory acidosis.

Dosage Forms: US

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Generic: 25 mg, 50 mg

Generic Equivalent Available: US

Yes

Pricing: US

Tablets (methazolAMIDE Oral)

25 mg (per each): $2.76 - $5.11

50 mg (per each): $5.52 - $10.22

Disclaimer: A representative AWP (Average Wholesale Price) price or price range is provided as reference price only. A range is provided when more than one manufacturer's AWP price is available and uses the low and high price reported by the manufacturers to determine the range. The pricing data should be used for benchmarking purposes only, and as such should not be used alone to set or adjudicate any prices for reimbursement or purchasing functions or considered to be an exact price for a single product and/or manufacturer. Medi-Span expressly disclaims all warranties of any kind or nature, whether express or implied, and assumes no liability with respect to accuracy of price or price range data published in its solutions. In no event shall Medi-Span be liable for special, indirect, incidental, or consequential damages arising from use of price or price range data. Pricing data is updated monthly.

Dosage Forms: Canada

Excipient information presented when available (limited, particularly for generics); consult specific product labeling.

Tablet, Oral:

Generic: 50 mg

Administration: Adult

Oral: May administer without regard to food.

Use: Labeled Indications

Glaucoma: Treatment of chronic open-angle or secondary glaucoma; short-term therapy of acute angle-closure glaucoma prior to surgery

Medication Safety Issues
Sound-alike/look-alike issues:

MethazolAMIDE may be confused with methenamine, methIMAzole, metOLazone

Neptazane may be confused with Nesacaine

Metabolism/Transport Effects

None known.

Drug Interactions

Note: Interacting drugs may not be individually listed below if they are part of a group interaction (eg, individual drugs within “CYP3A4 Inducers [Strong]” are NOT listed). For a complete list of drug interactions by individual drug name and detailed management recommendations, use the Lexicomp drug interactions program by clicking on the “Launch drug interactions program” link above.

Alpha-/Beta-Agonists (Indirect-Acting): Carbonic Anhydrase Inhibitors may increase the serum concentration of Alpha-/Beta-Agonists (Indirect-Acting). Risk C: Monitor therapy

Amantadine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Amantadine. Risk C: Monitor therapy

Amphetamines: Carbonic Anhydrase Inhibitors may decrease the excretion of Amphetamines. Risk C: Monitor therapy

Carbonic Anhydrase Inhibitors: May enhance the adverse/toxic effect of other Carbonic Anhydrase Inhibitors. The development of acid-base disorders with concurrent use of ophthalmic and oral carbonic anhydrase inhibitors has been reported. Management: Avoid concurrent use of different carbonic anhydrase inhibitors if possible. Monitor patients closely for the occurrence of kidney stones and with regards to severity of metabolic acidosis. Risk X: Avoid combination

Desmopressin: Hyponatremia-Associated Agents may enhance the hyponatremic effect of Desmopressin. Risk C: Monitor therapy

Diacerein: May enhance the therapeutic effect of Diuretics. Specifically, the risk for dehydration or hypokalemia may be increased. Risk C: Monitor therapy

Flecainide: Carbonic Anhydrase Inhibitors may decrease the excretion of Flecainide. Risk C: Monitor therapy

Fosphenytoin-Phenytoin: Carbonic Anhydrase Inhibitors may enhance the adverse/toxic effect of Fosphenytoin-Phenytoin. Specifically, the risk for osteomalacia or rickets may be increased. Risk C: Monitor therapy

Lithium: Carbonic Anhydrase Inhibitors may decrease the serum concentration of Lithium. Risk C: Monitor therapy

Memantine: Carbonic Anhydrase Inhibitors may increase the serum concentration of Memantine. Risk C: Monitor therapy

MetFORMIN: Carbonic Anhydrase Inhibitors may enhance the adverse/toxic effect of MetFORMIN. Specifically, the risk of developing lactic acidosis may be increased. Risk C: Monitor therapy

Methenamine: Carbonic Anhydrase Inhibitors may diminish the therapeutic effect of Methenamine. Management: Consider avoiding the concomitant use of medications that alkalinize the urine, such as carbonic anhydrase inhibitors, and methenamine. Monitor for decreased therapeutic effects of methenamine if used concomitant with a carbonic anhydrase inhibitor. Risk D: Consider therapy modification

Opioid Agonists: May enhance the adverse/toxic effect of Diuretics. Opioid Agonists may diminish the therapeutic effect of Diuretics. Risk C: Monitor therapy

Polyethylene Glycol-Electrolyte Solution: Diuretics may enhance the nephrotoxic effect of Polyethylene Glycol-Electrolyte Solution. Risk C: Monitor therapy

Salicylates: May enhance the adverse/toxic effect of Carbonic Anhydrase Inhibitors. Salicylate toxicity might be enhanced by this same combination. Management: Avoid these combinations when possible.Dichlorphenamide use with high-dose aspirin as contraindicated. If another combination is used, monitor patients closely for adverse effects. Tachypnea, anorexia, lethargy, and coma have been reported. Risk D: Consider therapy modification

Sodium Phosphates: Diuretics may enhance the nephrotoxic effect of Sodium Phosphates. Specifically, the risk of acute phosphate nephropathy may be enhanced. Risk C: Monitor therapy

Pregnancy Considerations

Adverse events were observed in animal reproduction studies.

Breastfeeding Considerations

It is not known if methazolamide is excreted in breast milk. Due to the potential for serious adverse reactions in the nursing infant, a decision should be made whether to discontinue nursing or to discontinue the drug, taking into account the importance of treatment to the mother.

Monitoring Parameters

CBC and platelet count (baseline and periodically), serum electrolytes (periodically)

Mechanism of Action

Noncompetitive inhibition of the enzyme carbonic anhydrase; thought that carbonic anhydrase is located at the luminal border of cells of the proximal tubule. When the enzyme is inhibited, there is an increase in urine volume and a change to an alkaline pH with a subsequent decrease in the excretion of titratable acid and ammonia.

Pharmacokinetics (Adult Data Unless Noted)

Onset of action: Slow in comparison with acetazolamide (2 to 4 hours).

Peak effect: 6 to 8 hours.

Duration: 10 to 18 hours.

Absorption: Slow.

Distribution: Vd: 17 to 23 L.

Protein binding: ~55%.

Metabolism: Slowly from GI tract.

Half-life elimination: ~14 hours.

Excretion: Urine (~25% as unchanged drug).

Brand Names: International
International Brand Names by Country
For country code abbreviations (show table)

  • (AR) Argentina: Glaumetax;
  • (CN) China: Nearmox | Ni mu ke si;
  • (FR) France: Neptazane;
  • (IL) Israel: Neptazane;
  • (JP) Japan: Neptazane;
  • (KR) Korea, Republic of: Methazone | Mezomine | Neptazane;
  • (NO) Norway: Methazolamide wyeth lederle;
  • (PR) Puerto Rico: Glauctabs | Neptazane;
  • (TH) Thailand: Neptazane
  1. Brackett CC, Singh H, Block JH. Likelihood and mechanisms of cross-allergenicity between sulfonamide antibiotics and other drugs containing a sulfonamide functional group. Pharmacotherapy. 2004;24(7):856-870. [PubMed 15303450]
  2. Funder JW, Carey RM, Mantero F, et al. The management of primary aldosteronism: case detection, diagnosis, and treatment: an Endocrine Society Clinical Practice Guideline. J Clin Endocrinol Metab. 2016;101(5):1889-1916. doi:10.1210/jc.2015-4061 [PubMed 26934393]
  3. Johnson KK, Green DL, Rife JP, Limon L. Sulfonamide cross-reactivity: fact or fiction? Ann Pharmacother. 2005;39(2):290-301. [PubMed 15644481]
  4. Methazolamide tablets [prescribing information]. Bridgewater, NJ: Oceanside Pharmaceuticals; April 2020.
  5. Slatore CG, Tilles SA. Sulfonamide hypersensitivity. Immunol Allergy Clin North Am. 2004;24(3):477-490. [PubMed 15242722]
  6. Tornero P, De Barrio M, Baeza ML, Herrero T. Cross-reactivity among p-amino group compounds in sulfonamide fixed drug eruption: diagnostic value of patch testing. Contact Dermatitis. 2004;51(2):57-62. [PubMed 15373844]
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