Acetazolamide (Diamox) is used to treat glaucoma, edema due to drugs or heart failure, seizures and prevention and treatment of high altitude sickness.

It is also used as a respiratory stimulant in stable COPD patients who are hypercapnic and in the treatment of metabolic alkalosis.

Acetazolamide use in migraine Aura status:

• Acetazolamide has shown promise in treating a condition called migraine aura status, which affects up to 30% of migraine sufferers.
• This condition involves experiencing frequent or consecutive episodes of aura without the accompanying headache.
• Aura can manifest as visual disturbances, sensory changes, or other symptoms like tinnitus.
• While acetazolamide doesn't stop migraines from happening or relieve headache pain, it has been observed to help with migraine aura status, making it less bothersome for those affected.
• Additionally, it has shown some effectiveness in managing migraine with aura in individuals with CADASIL, a condition characterized by certain types of brain damage.
• However, acetazolamide isn't typically used to prevent migraines or to stop a migraine attack once it's started, unlike medications like Sumatriptan and zolmitriptan.

Acetazolamide for hereditary paroxysmal ataxia:

• Acetazolamide has been found to be effective in treating patients with hereditary paroxysmal ataxia, a condition characterized by sudden episodes of ataxia (loss of muscle control), dysarthria (difficulty speaking), and nystagmus (involuntary eye movements).
• These individuals experience sudden, intermittent attacks of these symptoms.
• Acetazolamide has shown promise in alleviating these symptoms and improving the overall quality of life for those affected by this condition.

Acetazolamide for sleep apnea:

• Acetazolamide has been explored as a potential treatment for certain types of sleep apnea, such as central sleep apnea, chronic obstructive airway disease, and obesity hypoventilation syndrome.
• This medication works by making the blood more acidic, which stimulates the respiratory center in the brain, leading to increased breathing.
• As a result, patients may experience improvements in their symptoms, including reduced episodes of sleep apnea.
• In fact, one study found a significant 69% reduction in sleep apnea episodes with acetazolamide therapy.
• This suggests that acetazolamide could be a beneficial option for managing sleep apnea in certain individuals, particularly those with conditions characterized by abnormal breathing patterns during sleep.

Acetazolamide in patients with hydrocephalus:

• Acetazolamide has demonstrated effectiveness in treating hydrocephalus in animal studies by reducing the production of cerebrospinal fluid (CSF), thus lowering ventricular pressure.
• However, its efficacy in humans, particularly in children with hydrocephalus, is uncertain, with one study showing negligible therapeutic effects.
• In adults, acetazolamide has been found to be beneficial in certain cases, particularly in patients with idiopathic intracranial hypertension, also known as pseudotumor cerebri, where it can help reduce CSF production and alleviate symptoms.
• While acetazolamide may have a limited role in managing hydrocephalus in adults with specific conditions, further research is needed to determine its overall efficacy in this population.

Acetazolamide for Altitude sickness:

• Immediate-release tablets at a dose of 500-1000 mg per day, divided into two to three doses.
• Extended-release capsules can be given at a similar dosage of 500-1000 mg per day, either once daily or split into two doses.

Acetazolamide for the Prevention of altitude sickness:

• Acetazolamide is typically prescribed at a dose of 125 mg every twelve hours.
• It's recommended to start taking acetazolamide at least a day before ascending to higher elevations.
• After spending 2 to 3 days at the same altitude, you can discontinue the medication.

Note:

• In situations where rapid ascent is unavoidable, a higher dose of 1000 mg per day is recommended, along with dexamethasone.
• Additionally, dexamethasone should be administered to patients who develop cerebral edema, a serious complication of altitude sickness.

Acetazolamide dose for the treatment of Edema: 

• Whether administered orally or intravenously, the typical dose of acetazolamide ranges from 250 to 375 mg once daily.
• This medication works by reducing the production of fluids in the body, helping to alleviate swelling caused by conditions such as heart failure, liver disease, or kidney disorders.

Acetazolamide Does in seizures and epilepsy: 

• The typical oral dosage of acetazolamide ranges from 8 to 30 mg per kg per day, divided into multiple doses.
• The maximum recommended dose is 30 mg/kg/day or 1 g/day.

Note: 

• It's important to note that minimal additional benefit is observed with doses exceeding 16 mg/kg/day.
• Additionally, the extended-release capsule formulation of acetazolamide is not recommended for the treatment of epilepsy.

Acetazolamide does in Glaucoma:

• Secondary or acute (closed-angle) glaucoma:
  • Initial dose: 250-500 mg
  • Maintenance dose: Take 125 to 250 mg every four hours
  • Some patients may find 250 mg every 12 hours effective for short-term treatment
• Chronic simple (open-angle) glaucoma:
  • Acetazolamide 250 mg tablets can be taken once to four times a day
  • Alternatively, Diamox 500 mg extended-release capsules can be taken twice daily.

Acetazolamide dose in Metabolic alkalosis:

• A single dose of acetazolamide, typically in the form of Diamox 500 mg tablets, may be administered intravenously.

Acetazolamide dose as a respiratory stimulant in stable hypercapnic COPD:

• The typical dosage is acetazolamide 250 mg tablets taken orally twice daily.

Acetazolamide dose in Children:

Acetazolamide dosage for altitude sickness prophylaxis:

• The recommended dosage of acetazolamide is 2.5 mg per kg per dose every 12 hours.
• It's typically advised to start taking the medication three days after reaching the same height, ideally beginning either a day before or at least on the day of ascent to higher altitudes.

Acetazolamide altitude sickness pediatric dose (Treatment dose):

• The recommended dosage of acetazolamide is 2.5 mg per kg per dose, administered every 8 to 12 hours, with a maximum dose of 250 mg per dose.

Pregnancy Risk Factor C 

• Indeed, studies on animals have indicated potential teratogenic effects of acetazolamide, making it advisable to avoid its use in pregnant women.
• Additionally, acetazolamide has been detected in breast milk, suggesting caution during lactation.

Acetazolamide dose in kidney failure:

• While significant renal impairment is generally considered a contraindication for acetazolamide use, there isn't a well-defined threshold creatinine clearance level established for its contraindication.

• In individuals with creatinine clearance (ClCr) less than 10 mL per minute, it's generally recommended to avoid the use of acetazolamide due to the risk of accumulation and potential adverse effects.
• For those with ClCr between 10 and 50 mL per minute, acetazolamide can be administered but typically at a reduced frequency, such as every 12 hours, to account for decreased renal clearance.
• In patients undergoing hemodialysis, acetazolamide is considered moderately dialyzable, with 20% to 50% removed during dialysis sessions.

Acetazolamide Dose in Liver disease:

• Acetazolamide shouldn't be used by patients with severe liver problems or cirrhosis.

Acetazolamide Side effects:

• Miscellaneous:
  • Anaphylaxis
• Ophthalmologic:
  • burning,
  • corneal disorders,
  • ocular stinging,
  • pain at the injection site.
  • dry eyes,
  • erythema,
  • Anaphylaxis,
  • blepharoconjunctivitis,
  • itching,
• Endocrine & metabolic:
  • metabolic acidosis
  • hyperglycemia,
  • Electrolyte imbalance,
  • hypoglycemia,
  • hypokalemia,
  • growth retardation (children),
  • hyponatremia,
• Neurologic side effects:
  • drowsiness,
  • excitement,
  • convulsions,
  • fever,
  • headache,
  • depression,
  • Flushing,
  • ataxia,
  • confusion,
  • dizziness,
  • fatigue,
  • malaise

• Gastrointestinal adverse effects:
  • taste alteration,
  • Appetite decreased,
  • melena,
  • nausea,
  • diarrhea,
  • vomiting
• Dermatologic:
  • Allergic skin reactions,
  • Stevens-Johnson syndrome,
  • toxic epidermal necrolysis,
  • photosensitivity,
  • urticaria
• Genitourinary effects:
  • Crystalluria,
  • hematuria,
  • polyuria,
  • glycosuria,
  • renal failure
• Ear problems:
  • Hearing disturbance,
  • tinnitus
• Hematologic effects:
  • aplastic anemia,
  • thrombocytopenia,
  • Agranulocytosis,
  • leukopenia,
  • thrombocytopenic purpura
• Neuromuscular & skeletal:
  • Flaccid paralysis,
  • paresthesia
• Hepatic adverse effects:
  • hepatic insufficiency,
  • fulminant hepatic necrosis,
  • Abnormal liver function tests
  • Cholestatic jaundice,

 Acetazolamide Contraindications: 

• Acetazolamide should be avoided in patients with severe allergic reactions to acetazolamide or sulfonamides, advanced liver or kidney disease, severe hyponatremia, hypokalemia, adrenal insufficiency, and noncongestive angle-closure glaucoma, especially with long-term usage.

Monitor:

• Monitoring fluid and electrolyte levels, liver function tests, and renal function is important for patients taking acetazolamide.
• This helps ensure that the medication is being tolerated well and that any potential adverse effects are identified early.

How to take Acetazolamide?

• Acetazolamide oral formulations can be taken with or without meals, but be aware that it may alter the taste, especially in carbonated beverages.
• To minimize the bitter taste, short-acting tablets can be crushed and mixed with 10 ml of hot water and 10 ml of honey or chocolate syrup; however, avoid mixing with fruit juices.
• Intramuscular administration is not recommended due to severe pain.
• Acetazolamide can be mixed with almost any type of intravenous fluid solution, ensuring compatibility.

Mechanism of Action of Acetazolamide:

• Acetazolamide works by slowing down a specific enzyme in the body, leading to the removal of salt, potassium, and bicarbonate.
• This helps reduce the production of fluid in the eye and lowers certain acids in the brain, which can calm down abnormal and excessive nerve activity.

The onset of action:

• Oral formulations: It takes about 2 hours for the medication to start working after taking it by mouth.
• Intravenous formulation: When given through a vein, the effects can begin in just 5 to 10 minutes.

Excretion of Acetazolamide:

• The body gets rid of acetazolamide mainly through urine.
• Around 70% to 100% of the drug is excreted unchanged in the urine.

Time to Peak:

• Extended-release capsule: It takes about 3 to 6 hours for the medication to reach its highest levels in the body when taken in extended-release capsule form.
• Tablet: When taking the tablet form, it typically peaks in the bloodstream within 1 to 4 hours after ingestion.

Acetazolamide International Brands:

• Apo-Acetazolamide
• Azol
• Carbinib
• Acetadiazol
• Acetak
• Albox
• Glaupax
• Glauseta
• Huma-Zolamide
• Cetamid
• Diacarb
• Diluran
• Diural
• Diuramid
• Evamox
• Fonurit
• Diamox
• Diamox Sustets
• Diazomid
• Glaucomed
• Glaumox
• Odemin
• Renamid
• Stazol
• Synomax
• Uramox
• Ledamox
• Medene
• Oculten
• Zolmide

Acetazolamide brands in Pakistan:

Acemox (Vega pharmaceruticalsLTD)

Tablets: 250mg:

30 tablets pack: Rs.30

AZM (Ethical laboratories (PVT) LTD)

Tablets: 250mg:

30 tablets pack: Rs.34

Diamox (Pfizer laboratories LTD)

Tablets: 250mg:

30 tablets pack: Rs.34.43

Evamox (Don valley pharmaceuticals (PVT) LTD)

Tablets: 250mg:

30 tablets pack: Rs.27

Setacar (Remington pharmaceuticals industries (PVT) LTD)

  Tablets: 250mg:

30 tablets pack: Rs.33.48