Acetazolamide

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Generic Name of Acetazolamide - Learn More

Acetazolamide

Acetazolamide Precaution - What You Need to Know

- Pregnancy and Breastfeeding: Acetazolamide is classified as a Category C drug by the FDA for pregnancy. This means that while animal studies have shown adverse effects, no well-controlled studies are available in humans. It should only be used during pregnancy if the potential benefits outweigh the risks. Acetazolamide is excreted in breast milk; therefore, its use is generally not recommended during breastfeeding unless absolutely necessary. If used, the infant should be closely monitored for potential side effects, such as drowsiness or altered electrolyte levels.
- Renal and Hepatic Impairment: Patients with pre-existing kidney or liver conditions should be closely monitored. Acetazolamide is primarily excreted by the kidneys, and impaired renal function could lead to the drug accumulating in the body, increasing the risk of side effects. In cases of severe renal impairment, its use may be contraindicated. Liver impairment may affect drug metabolism, so careful consideration and dose adjustments are necessary.
- Monitoring Parameters: Regular monitoring of electrolyte levels (especially potassium, sodium, and bicarbonate) is important due to the potential for disturbances caused by acetazolamide. Additionally, renal function should be assessed periodically through serum creatinine and blood urea nitrogen (BUN) levels. Patients should also be monitored for signs of acidosis, dehydration, and altered mental status.
- Misuse or Dependency: Acetazolamide is not known to carry a high potential for abuse or dependency. However, improper use or overuse may lead to serious electrolyte imbalances and renal complications. It should only be used as prescribed and under the guidance of a healthcare professional.

Acetazolamide Indication - Uses and Benefits

Acetazolamide is primarily indicated for the treatment of conditions such as:
- Glaucoma: It is used to lower intraocular pressure in patients with open-angle or angle-closure glaucoma, often when other medications are not effective or contraindicated.
- Edema: In cases of edema associated with heart failure or renal dysfunction, acetazolamide helps in reducing fluid retention by promoting diuresis.
- Acute Mountain Sickness (AMS): Acetazolamide is often used for prophylaxis and treatment of AMS, as it can help increase the respiratory rate and improve oxygenation at high altitudes.
- Seizures: It is occasionally used as an adjunct in the treatment of certain types of seizures, especially in patients with drug-resistant epilepsy.
Off-label uses include treatment for idiopathic intracranial hypertension (pseudotumor cerebri) and urinary alkalinization. In cases of pseudotumor cerebri, acetazolamide helps reduce intracranial pressure. The use of acetazolamide in these conditions is supported by clinical evidence, but they are not FDA-approved indications.

Acetazolamide Contraindications - Important Warnings

Acetazolamide should not be used in patients with the following conditions:
- Hypersensitivity: Known hypersensitivity to acetazolamide or other sulfonamides contraindicates its use, as it may trigger allergic reactions, including Stevens-Johnson syndrome or anaphylaxis.
- Severe Renal or Hepatic Impairment: As acetazolamide is excreted via the kidneys and metabolized by the liver, patients with severe renal or hepatic dysfunction are at increased risk for drug accumulation and toxicity.
- Adrenal Insufficiency (Addison’s Disease): Acetazolamide can increase the risk of developing metabolic acidosis in patients with adrenal insufficiency, making it unsafe for this group.
- Low Serum Electrolytes: Patients with pre-existing low levels of sodium, potassium, or bicarbonate should not use acetazolamide, as it can exacerbate electrolyte imbalances.
- Age Considerations: It is contraindicated in infants and young children with severe renal or hepatic impairment due to the potential risk of serious adverse effects. Acetazolamide should also be used cautiously in elderly patients due to the increased likelihood of renal and electrolyte disturbances.

Acetazolamide Side Effects - What to Expect

The side effects of acetazolamide can be categorized by their frequency and severity:
- Common and Mild Side Effects:
- Drowsiness and fatigue: Can interfere with normal daily activities and may be exacerbated by alcohol or sedative medications.
- Tingling or numbness in the fingers or toes (paresthesia) is often observed and is generally benign but can be bothersome.
- Dizziness or light-headedness, especially when standing up quickly.
- Serious Side Effects:
- Electrolyte Imbalances: Hypokalemia, hyponatremia, and metabolic acidosis are potential risks, particularly in patients with pre-existing conditions or those on concurrent diuretics.
- Kidney Stones: Acetazolamide can increase the urinary excretion of calcium, leading to an increased risk of kidney stone formation.
- Renal Failure: Rare but serious, particularly in patients with pre-existing renal conditions.
- Severe Allergic Reactions: Symptoms such as skin rash, difficulty breathing, or swelling of the face or throat may indicate an allergic reaction and require immediate medical attention.
- Mitigation: To minimize side effects, it is recommended to stay well-hydrated, monitor electrolyte levels regularly, and avoid activities requiring full alertness (like driving) if drowsiness occurs.

Acetazolamide Pregnancy Category ID - Safety Information

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Acetazolamide Mode of Action - How It Works

Acetazolamide is a carbonic anhydrase inhibitor, which works by inhibiting the enzyme carbonic anhydrase. This enzyme plays a key role in the reversible conversion of carbon dioxide and water to bicarbonate and hydrogen ions. By inhibiting this enzyme, acetazolamide reduces bicarbonate reabsorption in the kidneys, leading to increased bicarbonate excretion in the urine. This results in a mild metabolic acidosis, which decreases intraocular pressure in glaucoma and helps with fluid management in conditions like edema or high-altitude sickness. Additionally, the increased renal excretion of bicarbonate and sodium promotes diuresis, which is beneficial in conditions such as heart failure and edema. At the cellular level, acetazolamide’s effects extend beyond fluid balance regulation, influencing respiratory rates and acid-base homeostasis.

Acetazolamide Drug Interactions - What to Avoid

Acetazolamide has significant interactions with several other drugs:
- Diuretics (e.g., furosemide, thiazides): When used together, acetazolamide may enhance the diuretic effects of these drugs, increasing the risk of dehydration and electrolyte imbalances, particularly hypokalemia and hyponatremia. Monitoring of electrolytes is essential when combining these medications.
- Carbonic Anhydrase Inhibitors: Concurrent use with other carbonic anhydrase inhibitors (e.g., methazolamide) can exacerbate side effects such as metabolic acidosis and renal dysfunction.
- Aminoglycosides (e.g., gentamicin): The combination of acetazolamide with aminoglycosides may increase the risk of nephrotoxicity and ototoxicity. Caution and close monitoring are required.
- Salicylates (e.g., aspirin): Acetazolamide may enhance the toxic effects of high-dose salicylates, potentially leading to salicylate toxicity, especially in patients with renal impairment.
- Alcohol: Acetazolamide can enhance the effects of alcohol on the central nervous system, leading to increased drowsiness, dizziness, or confusion. Patients should be advised to avoid alcohol while taking this medication.
- Food Interactions: There are no major food interactions with acetazolamide; however, maintaining adequate hydration is essential, especially since the drug increases urine output and can lead to dehydration.

Acetazolamide Adult Dose - Recommended Dosage

- Glaucoma: The typical adult dose is 250 mg orally twice a day, with potential increases up to 1 gram per day if needed. In cases of acute glaucoma, higher doses may be used initially.
- Edema: Acetazolamide is usually started at 250 mg orally 1 to 2 times daily. The dose may be adjusted based on the clinical response and electrolyte levels.
- Acute Mountain Sickness (AMS): For prophylaxis, the recommended dose is 125–250 mg orally every 12 hours, starting 24–48 hours before ascending to high altitudes.
- Seizures: When used as an adjunct in seizure treatment, the typical starting dose is 250 mg once daily, with gradual titration upwards based on efficacy and tolerance.
The maximum recommended dose for adults is 1,000 mg per day, with the dose being tailored based on the severity of the condition and response to treatment.

Acetazolamide Child Dose - Dosage for Children

For children, acetazolamide dosing is based on weight and age:
- For Glaucoma: The typical pediatric dose ranges from 5–10 mg/kg/day in divided doses, not exceeding 375 mg per day.
- For Edema or Mountain Sickness: Children can receive 5 mg/kg/dose every 12 hours, with adjustments made based on clinical response.
Dosing in children under the age of 2 is generally not recommended due to the increased risk of side effects and lack of sufficient safety data. As with adults, pediatric patients require close monitoring of electrolyte levels, renal function, and overall clinical status during treatment.

Acetazolamide Renal Dose - Dosage for Kidney Conditions

Acetazolamide requires dose adjustments in patients with renal impairment:
- Mild to Moderate Renal Dysfunction: For patients with creatinine clearance (CrCl) between 30 and 60 mL/min, the usual starting dose is 250 mg daily, with careful monitoring of renal function and electrolytes.
- Severe Renal Dysfunction: Acetazolamide should be avoided or used with extreme caution in patients with CrCl less than 30 mL/min due to the risk of drug accumulation and toxicity. If necessary, the dose should be reduced and patients closely monitored.
- Monitoring: Renal function (serum creatinine, BUN) and electrolytes (potassium, bicarbonate) should be monitored frequently during therapy, particularly in patients with renal impairment or those on other medications that affect renal function.