Methazolamide (Neptazane) - Uses, Dose, Side effects, MOA, Brands

Like acetazolamide, methazolamide (Neptazane) is a carbonic anhydrase inhibitor that raises the urinary volume and modifies blood and urine PH. Patients with persistent open-angle glaucoma are treated with it.

Methazolamide Uses:

  • Glaucoma:
    • It is used for the management of secondary or chronic open-angle glaucoma.
    • It is also used for the short-term treatment of acute angle-closure glaucoma before surgery.

Methazolamide (Neptazane) Dose in Adults:

Methazolamide (Neptazane) Dose in the treatment of Glaucoma:

  • For glaucoma treatment, the dose is usually 50 to 100 mg taken by mouth 2 to 3 times a day.

Use in Children:

Not indicated.


Pregnancy Risk Factor C

  • Tests on animals showed that the medicine might cause problems during pregnancy.

Use of methazolamide while breastfeeding

  • We don't know if methazolamide passes into breast milk.
  • Since it might harm a breastfeeding baby, moms have to decide whether to stop breastfeeding or stop taking the medicine.

Methazolamide Dose in Kidney Disease:

In cases of severe renal failure, it is not advised.

Methazolamide Dose in Liver disease:

In cases of severe liver failure, it is not advised.


Side effects of Methazolamide (Neptazane):

  • Renal:
    • Nephrolithiasis
    • Polyuria
  • Central Nervous System:
    • Paresthesia
    • Seizure
    • Fatigue
    • Flaccid Paralysis
    • Confusion
    • Drowsiness
    • Malaise
  • Miscellaneous:
    • Fever
  • Dermatologic:
    • Skin Rash
    • Stevens-Johnson Syndrome
    • Erythema Multiforme
    • Skin Photosensitivity
    • Toxic Epidermal Necrolysis
    • Urticaria
  • Endocrine & Metabolic:
    • Electrolyte Disturbance
    • Metabolic Acidosis
    • Glycosuria
  • Gastrointestinal:
    • Dysgeusia
    • Melena
    • Decreased Appetite
    • Diarrhea
    • Nausea
    • Vomiting
  • Genitourinary:
    • Crystalluria
    • Hematuria
  • Hematologic & Oncologic:
    • Leukopenia
    • Pancytopenia
    • Bone Marrow Depression
    • Hemolytic Anemia
    • Agranulocytosis
    • Aplastic Anemia
    • Immune Thrombocytopenia
  • Hypersensitivity:
    • Anaphylaxis
    • Hypersensitivity Reaction
  • Hepatic:
    • Fulminant Hepatic Necrosis
    • Hepatic Insufficiency
  • Ophthalmic:
    • Myopia
  • Otic:
    • Auditory Disturbance
    • Tinnitus

Contraindications to Methazolamide (Neptazane):

Methazolamide might not be safe for people with:

  • Major kidney or liver problems.
  • Broken adrenal glands (glands above your kidneys).
  • Severe liver disease.
  • A specific acid imbalance in the blood.
  • Low salt or potassium in the blood.
  • A certain type of glaucoma if treated for a long time.

Warnings and precautions

CNS effects

  • This medicine might affect your brain, making you less alert or coordinated.
  • Be careful, especially when doing tasks like driving.

Electrolyte disturbance:

  • The medicine might change the balance of certain minerals in your body, especially potassium.
  • If you're at risk, you need regular checks for low potassium levels and its signs.

Allergy to sulfonamide ("sulfa")

  • Some medications contain a chemical called sulfonamide, and some people are allergic to it.
  • In the past, there were concerns that if you were allergic to one sulfonamide medication, you might react to all of them.
  • But now, we know that the risk of reacting to other sulfonamide medicines, especially non-antibiotic ones, is very low.
  • Severe reactions are rare, but if you had a severe reaction before, some doctors may still avoid giving you medicines with sulfonamides.

Diabetes:

  • If you have early-stage diabetes or full-blown diabetes, be careful when using this medicine.
  • It might affect your blood sugar levels.

Hepatic impairment

  • If you have liver problems, be careful with this medicine.
  • It might make a liver condition called hepatic encephalopathy worse.
  • Don't use it if you have severe liver issues or cirrhosis.

Respiratory disease

  • If you have lung diseases like emphysema or blocked airways, be careful with this medicine.
  • It might make a breathing-related condition called respiratory acidosis worse.

Methazolamide: Drug Interaction

Risk Factor C (Monitor therapy)

Alpha-/Beta-Agonists (Indirect-Acting)

Carbonic Anhydrase Inhibitors may raise its serum levels.

Amantadine

Carbonic Anhydrase Inhibitors may raise its serum levels.

Amphetamines

Carbonic Anhydrase Inhibitors may lower its excretion.

CarBAMazepine

Carbonic Anhydrase Inhibitors may raise its serum levels.

Diacerein

might make diuretics' therapeutic effects stronger. Particularly, there may be a higher chance of hypokalemia or dehydration. 

Flecainide

Flecainide's serum levels may rise in response to carbonic anhydrase inhibitors. 

Fosphenytoin-Phenytoin

Fosphenytoin-Phenytoin may have a more negative or hazardous impact when taken with carbonic anhydrase inhibitors. In particular, there may be a higher risk for rickets or osteomalacia.

Lithium

Lithium levels in the blood may drop after using carbonic anhydrase inhibitors.

Memantine

When carbonic anhydrase inhibitors are used, memantine serum levels may increase.

MetFORMIN

When used with carbonic anhydrase inhibitors, metFORMIN may have a more adverse or dangerous effect. An increased risk of developing lactic acidosis is one such possibility.

Opioid Agonists

can intensify the negative or toxic effects of diuretics. Opioid antagonists may lessen the therapeutic effect of diuretics.

Primidone

Primidone's harmful or poisonous effects may be exacerbated by carbonic anhydrase inhibitors. Specifically, rickets and osteomalacia. Primidone serum levels may be decreased by carbonic anhydrase inhibitors.

QuiNIDine

QuiNIDine excretion could be decreased by carbonic anhydrase inhibitors.

Trientine

Trientine's serum levels could be lowered by diuretics that inhibit carbonic anhydrase.

Risk Factor D (Consider therapy modification)

Methenamine

Methenamine's ability to treat illness may be lessened by carbonic anhydrase inhibitors. Management: Take into account avoiding this pairing. If you use a carbonic anhydrase inhibitor at the same time as methenamine, keep an eye out for any diminished therapeutic benefits. 

Salicylates

might intensify the hazardous or harmful effects of carbonic anhydrase inhibitors. This identical combination may increase salicylate toxicity. Management: Whenever you can, stay away from these pairings. The use of dichlorphenamide with aspirin at high doses is not advised. If a different combination is used, patients should be closely watched for side effects. There have been reports of tachypnea, anorexia, lethargy, and coma.

Sodium Phosphates

It's possible that diuretics will worsen sodium phosphates' nephrotoxic effects. Particularly, acute phosphate nephropathy may be at elevated risk. The best course of action is to temporarily cease taking diuretics or hunt for a different oral sodium phosphate bowel preparation. Drink plenty of water and monitor your kidney and fluid levels if you must avoid the combo.

Risk Factor X (Avoid combination)

Carbonic Anhydrase Inhibitors

Other carbonic anhydrase inhibitors may have more adverse or dangerous consequences. Combining the use of oral and ophthalmic carbonic anhydrase inhibitors has been linked to reports of acid-base imbalances. Management: Avoid taking many carbonic anhydrase inhibitors at once, if at all possible. The degree of metabolic acidosis and the potential development of kidney stones should be closely monitored in patients.

Monitoring parameters:

CBC (Complete Blood Count)

  • When: At the start and then every so often.
  • Why: To check the health of your blood cells.

Platelet Count

  • When: At the start and then every so often.
  • Why: To see if you have enough platelets, which help blood clot.

Serum Electrolytes

  • When: Every so often.
  • Why: To check the balance of minerals in your blood.

How to administer methazolamide (Neptazane)?

It is administered orally without regard to meals.


Mechanism of action of Methazolamide (Neptazane):

  • Methazolamide slows down an enzyme called carbonic anhydrase, which is mainly found on the edge of cells in a part of the kidney called the proximal tubule.
  • When this enzyme is slowed down, more urine is produced, and it becomes more basic (alkaline).
  • As a result, less acid and ammonia get removed from the body through the urine.

Start Working:

  • Takes 2-4 hours to start working, which is slower than a similar drug called acetazolamide.

Strongest Effect:

  • Felt around 6-8 hours after taking.

Lasts:

  • The effects last between 10-18 hours.

Getting into the Body:

  • It enters the body slowly.

Spread in the Body:

  • It spreads through a volume of 17-23 liters in the body.

Binding:

  • About 55% of it sticks to proteins in the blood.

Breaking Down:

  • It's broken down slowly in the stomach and intestines.

How Long in Body:

  • Half of it is gone from the body in about 14 hours.

Leaving the Body:

  • It's removed from the body through urine, and about 25% leaves the body without changing.Top of Form

International Brands of Methazolamide:

  • Neptazane
  • Glaumetax
  • Mezomine

Methazolamide Brands Names in Pakistan:

Not Available.