Acetazolamide 125mg Tablets

Manufacturer HERITAGE PHARMACEUTICALS Active Ingredient Acetazolamide Tablets(a set a ZOLE a mide) Pronunciation a-set-a-ZOLE-a-mide
It is used to get rid of extra fluid. It is used to treat or prevent altitude sickness.It is used to help control certain kinds of seizures. It is used to treat glaucoma.It may be given to you for other reasons. Talk with the doctor.
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Drug Class
Carbonic Anhydrase Inhibitor; Diuretic; Antiglaucoma Agent; Anticonvulsant
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Pharmacologic Class
Carbonic Anhydrase Inhibitor
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Pregnancy Category
C
FDA Approved
Jul 1954
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DEA Schedule
Not Controlled

Overview

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What is this medicine?

Acetazolamide is a medication that works by affecting how your kidneys handle salts and water, and how your eyes produce fluid. It's used to treat conditions like glaucoma (high pressure in the eye), swelling (edema), certain types of seizures, and to help prevent or treat altitude sickness.
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How to Use This Medicine

Taking Your Medication

To get the most benefit from your medication, follow your doctor's instructions carefully. Read all the information provided with your prescription and follow the instructions closely. You can take this medication with or without food, but if it causes stomach upset, taking it with food may help. Be aware that this medication may increase the frequency of urination, so try to avoid taking it too close to bedtime to minimize sleep disruptions.

Storing and Disposing of Your Medication

Store your medication at room temperature in a dry place, avoiding the bathroom. Keep all medications in a safe location, out of the reach of children and pets. When disposing of unused or expired medication, do not flush it down the toilet or pour it down the drain unless instructed to do so. Instead, check with your pharmacist for guidance on the best disposal method or inquire about potential drug take-back programs in your area.

Missing a Dose

If you miss a dose, take it as soon as you remember. However, if it's close to the time for your next scheduled dose, skip the missed dose and resume your regular dosing schedule. Do not take two doses at the same time or take extra doses to make up for a missed one.
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Lifestyle & Tips

  • Stay well-hydrated, especially when taking this medication, to help prevent kidney stones.
  • Report any unusual tingling sensations (paresthesias) in your fingers or toes, as this is a common side effect.
  • Avoid excessive sun exposure and use sunscreen, as this medication can increase sensitivity to sunlight.
  • If you have diabetes, monitor your blood sugar closely as this medication may affect it.
  • Do not stop taking this medication suddenly, especially if you are taking it for epilepsy, without consulting your doctor.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication. For glaucoma (open-angle): 250 mg to 1 g per 24 hours, usually in divided doses. For edema: 250-375 mg once daily in the morning. For acute mountain sickness: 125-250 mg every 8-12 hours.
Dose Range: 125 - 1000 mg

Condition-Specific Dosing:

glaucoma_open_angle: 250 mg to 1 g per 24 hours, usually in divided doses (e.g., 250 mg 1-4 times daily or 500 mg sustained-release capsule twice daily).
glaucoma_acute_angle_closure: 250 mg every 4 hours or 500 mg initially, followed by 125-250 mg every 4 hours.
edema: 250-375 mg once daily in the morning, or 5 mg/kg once daily.
epilepsy: 8-30 mg/kg/day in divided doses. Initial dose 250 mg once daily, increasing to 250 mg 2-4 times daily. Max 1 g/day.
acute_mountain_sickness: 125-250 mg every 8-12 hours, starting 24-48 hours before ascent and continuing for 48 hours or longer after reaching altitude.
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Pediatric Dosing

Neonatal: Not established for routine use. Limited data for hydrocephalus: 5 mg/kg/day initially, increasing to 20-30 mg/kg/day in divided doses.
Infant: Not established for routine use. For hydrocephalus: 5 mg/kg/day initially, increasing to 20-30 mg/kg/day in divided doses.
Child: For glaucoma: 8-30 mg/kg/day in divided doses. For epilepsy: 8-30 mg/kg/day in divided doses. For edema: 5 mg/kg once daily in the morning.
Adolescent: Same as adult dosing for most indications.
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Dose Adjustments

Renal Impairment:

Mild: No specific adjustment usually needed (CrCl >50 mL/min).
Moderate: Reduce dose by 50% or extend dosing interval (CrCl 10-50 mL/min). For example, administer every 12-24 hours.
Severe: Contraindicated (CrCl <10 mL/min) due to risk of accumulation and toxicity.
Dialysis: Contraindicated. Not significantly dialyzable. Risk of accumulation and toxicity.

Hepatic Impairment:

Mild: No specific adjustment.
Moderate: Use with caution. May exacerbate hepatic encephalopathy.
Severe: Contraindicated in severe hepatic dysfunction (e.g., cirrhosis) due to risk of precipitating hepatic coma.

Pharmacology

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Mechanism of Action

Acetazolamide is a potent carbonic anhydrase inhibitor. Carbonic anhydrase is an enzyme found in various tissues, including the renal tubules, ciliary body of the eye, and central nervous system. By inhibiting this enzyme, acetazolamide decreases the reabsorption of bicarbonate, sodium, and water in the proximal renal tubule, leading to increased excretion of these ions and diuresis. In the eye, it reduces the formation of aqueous humor, thereby lowering intraocular pressure. In the CNS, it may inhibit carbonic anhydrase in the brain, which can reduce abnormal neuronal discharge in epilepsy and facilitate bicarbonate excretion at high altitudes, aiding acclimatization.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 100% (oral)
Tmax: Tablets: 2-4 hours; Sustained-release capsules: 8-12 hours
FoodEffect: Food may delay absorption but does not significantly affect the extent of absorption.

Distribution:

Vd: 0.2 L/kg
ProteinBinding: 95% (primarily to carbonic anhydrase in red blood cells and plasma proteins)
CnssPenetration: Limited, but sufficient to exert effects on CSF production and neuronal activity.

Elimination:

HalfLife: 2.4-5.8 hours (normal renal function)
Clearance: Renal clearance is approximately 100 mL/min
ExcretionRoute: Renal (primarily by tubular secretion and passive reabsorption)
Unchanged: Approximately 90% excreted unchanged in urine within 24 hours.
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Pharmacodynamics

OnsetOfAction: Oral: 1-1.5 hours; IV: 2 minutes
PeakEffect: Oral: 2-4 hours; IV: 15 minutes
DurationOfAction: Oral (tablets): 8-12 hours; Oral (sustained-release): 18-24 hours; IV: 4-6 hours

Safety & Warnings

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Side Effects

Urgent Side Effects: Seek Medical Help Right Away

Although rare, some people may experience severe and potentially life-threatening side effects while taking this medication. If you notice any of the following symptoms, contact your doctor or seek medical attention immediately:

Signs of an allergic reaction: rash, hives, itching, red, swollen, blistered, or peeling skin (with or without fever), wheezing, tightness in the chest or throat, difficulty breathing, swallowing, or talking, unusual hoarseness, or swelling of the mouth, face, lips, tongue, or throat.
Signs of acidosis (too much acid in the blood): confusion, rapid breathing, rapid heartbeat, irregular heartbeat, severe stomach pain, nausea, vomiting, excessive sleepiness, shortness of breath, or feeling extremely tired or weak.
Signs of electrolyte problems: mood changes, confusion, muscle pain, cramps, or spasms, weakness, shakiness, balance disturbances, abnormal heartbeat, seizures, loss of appetite, or severe nausea and vomiting.
Signs of high or low blood sugar: fruity breath odor, dizziness, rapid breathing, rapid heartbeat, confusion, sleepiness, weakness, flushing, headache, unusual thirst or hunger, frequent urination, shaking, or sweating.
Changes in vision, eye pain, or severe eye irritation.
Changes in hearing.
Ringing in the ears.
Abnormal burning, numbness, or tingling sensations.
Painful urination or blood in the urine.
Difficulty urinating or changes in urine output.
Muscle weakness.
Balance disturbances.
Mobility problems.
Depression.
Confusion.
Seizures.

Rare but Serious Side Effects

In rare cases, sulfa drugs can cause severe and potentially life-threatening effects, including liver problems, blood disorders, and severe skin reactions (Stevens-Johnson syndrome/toxic epidermal necrolysis). If you experience any of the following symptoms, contact your doctor immediately:

Rash or red, swollen, blistered, or peeling skin.
Red or irritated eyes.
Sores in the mouth, throat, nose, or eyes.
Fever, chills, or sore throat.
New or worsening cough.
Extreme fatigue or weakness.
Bruising or bleeding.
Signs of liver problems: dark urine, fatigue, decreased appetite, nausea, stomach pain, light-colored stools, vomiting, or yellow skin and eyes.

Other Possible Side Effects

Like all medications, this drug can cause side effects. While many people may not experience any side effects or only mild ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor or seek medical attention if they bother you or persist:

Diarrhea, nausea, or vomiting.
Changes in taste.
Decreased appetite.
Blurred vision.
Dizziness, drowsiness, fatigue, or weakness.
Headache.
Flushing.
Feeling nervous or excitable.

Reporting Side Effects

This list is not exhaustive, and you may experience other side effects. If you have questions or concerns, contact your doctor. You can also report side effects to the FDA at 1-800-332-1088 or online at https://www.fda.gov/medwatch.
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Seek Immediate Medical Attention If You Experience:

  • Severe skin rash, blistering, or peeling (could be a sign of a serious skin reaction)
  • Unusual bleeding or bruising, persistent sore throat, fever, or unusual tiredness (could be signs of blood problems)
  • Severe muscle weakness or cramps, irregular heartbeat (signs of electrolyte imbalance, especially low potassium)
  • Confusion, disorientation, severe drowsiness (signs of metabolic acidosis or hepatic encephalopathy)
  • Flank pain, blood in urine, difficulty urinating (signs of kidney stones)
  • Yellowing of skin or eyes (jaundice), dark urine, light-colored stools (signs of liver problems)
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Before Using This Medicine

Before Taking This Medication: Important Information to Share with Your Doctor

It is essential to inform your doctor about the following:

Any allergies you have, including allergies to this medication, its components, or other substances, such as foods or drugs. Be sure to describe the allergic reaction and its symptoms.
A known sulfa allergy.
Certain health conditions, including:
+ Acidic blood problems
+ Kidney disease
+ Liver disease
+ Low potassium levels (hypokalemia)
+ Low sodium levels (hyponatremia)
+ Poor adrenal function
If you are currently taking methazolamide.

This list is not exhaustive, and it is crucial to discuss all your medications, including prescription and over-the-counter drugs, natural products, and vitamins, with your doctor and pharmacist. They will help you determine if it is safe to take this medication with your existing treatments and health conditions.

Remember, do not start, stop, or change the dose of any medication without first consulting your doctor to ensure your safety.
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Precautions & Cautions

It is essential to inform all your healthcare providers, including doctors, nurses, pharmacists, and dentists, that you are taking this medication.

Until you understand how this drug affects you, avoid operating a vehicle or engaging in any activities that require alertness and clear vision.

Regularly monitor your blood work and other laboratory tests as instructed by your doctor.

If you have diabetes (high blood sugar), it is crucial to closely monitor your blood sugar levels, as this medication may impact them. Additionally, notify all your healthcare providers and laboratory personnel that you are taking this drug, as it may influence the results of certain lab tests.

Be cautious when exposed to the sun, as this medication may increase your susceptibility to sunburn. If you experience easy sunburning while taking this drug, inform your doctor.

If you are also taking aspirin, consult with your doctor, as high doses of aspirin combined with this medication have been associated with severe side effects, including loss of appetite, rapid breathing, lethargy, coma, and even death.

If you are 65 years or older, exercise caution when using this medication, as you may be more prone to experiencing side effects.

In some cases, this drug may affect the growth of children and teenagers. Regular growth checks may be necessary, so discuss this with your doctor.

If you are pregnant, planning to become pregnant, or breastfeeding, consult your doctor to weigh the benefits and risks of this medication to both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe electrolyte imbalance (e.g., hypokalemia, hyperchloremic metabolic acidosis)
  • Dehydration
  • CNS depression (drowsiness, confusion, stupor, coma)
  • Anorexia, nausea, vomiting
  • Paresthesias, tremor

What to Do:

Call 911 or your local poison control center (e.g., 1-800-222-1222 in the US) immediately. Treatment is supportive and symptomatic, focusing on correcting electrolyte and acid-base imbalances. Gastric lavage may be considered if ingestion is recent. Acetazolamide is not significantly dialyzable.

Drug Interactions

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Contraindicated Interactions

  • Methenamine (risk of crystalluria and reduced efficacy of methenamine)
  • Severe renal impairment (CrCl <10 mL/min)
  • Severe hepatic dysfunction (risk of hepatic coma)
  • Adrenal insufficiency
  • Hyperchloremic acidosis
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Major Interactions

  • High-dose salicylates (increased risk of metabolic acidosis and CNS toxicity, including anorexia, tachypnea, lethargy, coma, and death)
  • Cyclosporine (increased cyclosporine levels, leading to nephrotoxicity and neurotoxicity)
  • Lithium (increased lithium excretion, leading to decreased lithium levels)
  • Other carbonic anhydrase inhibitors (additive toxicity)
  • Topiramate, Zonisamide (increased risk of metabolic acidosis and kidney stones)
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Moderate Interactions

  • Amphetamines, Quinidine, Procainamide (decreased excretion due to alkaline urine, leading to increased levels and toxicity)
  • Antidiabetics (may alter blood glucose levels)
  • Diuretics (additive diuretic and potassium-wasting effects)
  • Corticosteroids (increased risk of hypokalemia)
  • Folic acid antagonists (e.g., methotrexate, pyrimethamine) (may potentiate toxicity due to altered pH)
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Minor Interactions

  • Sodium bicarbonate (may increase risk of kidney stones)

Monitoring

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Baseline Monitoring

Serum Electrolytes (Sodium, Potassium, Bicarbonate, Chloride)

Rationale: To establish baseline levels and identify pre-existing imbalances (e.g., hypokalemia, metabolic acidosis) that could be exacerbated.

Timing: Prior to initiation of therapy.

Renal Function (BUN, Creatinine)

Rationale: To assess kidney function, as acetazolamide is primarily renally eliminated and contraindicated in severe renal impairment.

Timing: Prior to initiation of therapy.

Complete Blood Count (CBC) with differential

Rationale: To establish baseline and monitor for potential hematologic adverse effects (e.g., aplastic anemia, agranulocytosis, thrombocytopenia) which are rare but serious sulfonamide-related reactions.

Timing: Prior to initiation of therapy.

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Routine Monitoring

Serum Electrolytes (Potassium, Bicarbonate)

Frequency: Weekly for the first few weeks, then monthly or as clinically indicated, especially during dose titration or in patients at risk for electrolyte imbalance.

Target: Potassium: 3.5-5.0 mEq/L; Bicarbonate: 22-29 mEq/L

Action Threshold: Potassium <3.0 mEq/L (consider supplementation); Bicarbonate <20 mEq/L (monitor for acidosis symptoms, consider dose reduction or discontinuation).

Renal Function (BUN, Creatinine)

Frequency: Periodically, especially in elderly patients or those with pre-existing renal impairment.

Target: Within normal limits for age/baseline.

Action Threshold: Significant increase in BUN/Creatinine (consider dose adjustment or discontinuation).

Intraocular Pressure (IOP)

Frequency: As per ophthalmologist's recommendation for glaucoma patients (e.g., every 3-6 months).

Target: Individualized target IOP.

Action Threshold: IOP above target range (consider dose adjustment or additional therapy).

CBC with differential

Frequency: Periodically, especially if therapy is prolonged or if symptoms suggestive of hematologic toxicity occur.

Target: Within normal limits.

Action Threshold: Significant decrease in cell counts (e.g., WBC <3000/mm³, Platelets <100,000/mm³) (discontinue immediately).

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Symptom Monitoring

  • Paresthesias (tingling sensation in extremities, common)
  • Fatigue, lethargy, malaise
  • Nausea, vomiting, diarrhea, anorexia
  • Polyuria, polydipsia
  • Signs of metabolic acidosis (e.g., hyperventilation, confusion, stupor)
  • Signs of electrolyte imbalance (e.g., muscle weakness, cramps, irregular heartbeat)
  • Skin rash, fever, sore throat (signs of hypersensitivity or hematologic reaction)
  • Flank pain, hematuria (signs of kidney stones)
  • Vision changes (rare, but possible with severe acidosis or idiosyncratic reaction)

Special Patient Groups

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Pregnancy

Acetazolamide is Pregnancy Category C. Animal studies have shown teratogenic effects (limb defects) at doses higher than human therapeutic doses. There are no adequate and well-controlled studies in pregnant women. Use during pregnancy only if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for teratogenic effects based on animal data. Avoid if possible, especially during organogenesis.
Second Trimester: Less data on specific risks, but continued use should be carefully weighed against benefits.
Third Trimester: Risk of metabolic acidosis in the mother and fetus, potentially leading to fetal distress or neonatal acidosis. May also inhibit fetal growth.
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Lactation

Acetazolamide is excreted in breast milk in small amounts. The American Academy of Pediatrics considers it compatible with breastfeeding. However, monitor the infant for potential adverse effects such as metabolic acidosis, growth inhibition, or rash. Use with caution, especially in premature or jaundiced infants.

Infant Risk: L3 (Moderate risk). Low levels in milk, but theoretical risk of metabolic acidosis or sulfonamide-related reactions in the infant. Monitor for irritability, poor feeding, or rash.
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Pediatric Use

Dosing is weight-based for most indications. Use with caution in infants and young children due to increased risk of metabolic acidosis. Long-term use may affect growth. Monitor electrolytes and acid-base status closely.

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Geriatric Use

Elderly patients may be more susceptible to adverse effects, particularly electrolyte imbalances (hypokalemia, metabolic acidosis) and renal impairment. Start with lower doses and titrate slowly. Monitor renal function and electrolytes closely.

Clinical Information

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Clinical Pearls

  • Acetazolamide is a sulfonamide derivative; inquire about sulfa allergies before administration. Cross-reactivity with non-antibiotic sulfonamides is low but possible.
  • Paresthesias (tingling of extremities) are a very common and usually benign side effect, often dose-related. Patients should be counseled about this.
  • Administer in the morning for diuretic effect to avoid nocturia.
  • Ensure adequate hydration to minimize the risk of kidney stone formation.
  • Long-term use requires regular monitoring of serum electrolytes (especially potassium and bicarbonate) and renal function.
  • Can cause metabolic acidosis, which may be symptomatic (e.g., hyperventilation, fatigue, confusion).
  • Not effective in patients with severe renal impairment (CrCl <10 mL/min) and is contraindicated due to accumulation risk.
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Alternative Therapies

  • For Glaucoma: Beta-blockers (e.g., timolol), prostaglandin analogs (e.g., latanoprost), alpha-adrenergic agonists (e.g., brimonidine), miotics (e.g., pilocarpine), other carbonic anhydrase inhibitors (e.g., dorzolamide, brinzolamide - topical).
  • For Edema: Loop diuretics (e.g., furosemide), thiazide diuretics (e.g., hydrochlorothiazide), potassium-sparing diuretics (e.g., spironolactone).
  • For Epilepsy: Other anticonvulsants (e.g., valproic acid, carbamazepine, lamotrigine, levetiracetam).
  • For Acute Mountain Sickness: Dexamethasone (for treatment), gradual ascent (for prevention).
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Cost & Coverage

Average Cost: Varies, typically $15-$50 per 30 tablets (125mg)
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic)
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General Drug Facts

If your symptoms or health issues persist or worsen, it's essential to contact your doctor for further guidance. To ensure your safety, never share your medication with others or take someone else's medication. Some medications may come with an additional patient information leaflet, so be sure to check with your pharmacist for more information. If you have any questions or concerns about this medication, don't hesitate to reach out to your doctor, nurse, pharmacist, or other healthcare provider. In the event of a suspected overdose, immediately call your local poison control center or seek medical attention. When seeking help, be prepared to provide details about the medication, including the amount taken and the time it happened, to ensure you receive the best possible care.