Acetazolamide 250mg Tablets

Manufacturer STRIDES PHARMA 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
Antiglaucoma Agent; Diuretic; Anticonvulsant
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Pharmacologic Class
Carbonic Anhydrase Inhibitor
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Pregnancy Category
D
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FDA Approved
Jul 1953
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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 body handles certain chemicals, particularly in your kidneys and eyes. It's often used to reduce pressure in the eyes (for glaucoma), to help your body get rid of extra fluid (as a diuretic), or to help prevent altitude sickness. It can also be used as an add-on treatment for certain types of seizures.
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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. To minimize sleep disturbances, try to avoid taking it too close to bedtime.

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. Dispose of unused or expired medications properly. Do not flush them down the toilet or pour them down the drain unless instructed to do so. If you have questions about disposing of your medication, consult your pharmacist. You may also want to check if there are drug take-back programs available 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 continue with 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.
  • Avoid excessive sun exposure as this medication may increase sensitivity to sunlight.
  • Report any unusual tingling or numbness in your fingers or toes, as this is a common side effect.
  • Avoid driving or operating machinery until you know how this medication affects you, as it can cause drowsiness or dizziness.
  • If you are taking this for altitude sickness, start taking it 24-48 hours before ascending and continue for a few days after reaching your destination.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication. For glaucoma: 250 mg to 1 g per day in divided doses. For edema: 250-375 mg once daily. For acute mountain sickness: 125-250 mg every 8-12 hours.
Dose Range: 125 - 1000 mg

Condition-Specific Dosing:

openAngleGlaucoma: 250 mg to 1 g per day in divided doses (e.g., 250 mg 1-4 times daily)
secondaryGlaucoma: 250 mg every 4 hours or 250 mg twice daily
edema: 250-375 mg once daily, or every other day, or for 2 days followed by a rest day
acuteMountainSickness: 125-250 mg every 8-12 hours, starting 24-48 hours before ascent
epilepsyAdjunct: 8-30 mg/kg/day in divided doses, typically 250-1000 mg/day
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Pediatric Dosing

Neonatal: Not established for routine use; limited data for hydrocephalus (5 mg/kg/day initially, increasing to 20-100 mg/kg/day in 2-3 divided doses)
Infant: For hydrocephalus: 5 mg/kg/day initially, increasing to 20-100 mg/kg/day in 2-3 divided doses. For glaucoma: 10-15 mg/kg/day in 2-3 divided doses.
Child: For glaucoma: 10-15 mg/kg/day in 2-3 divided doses. For epilepsy: 8-30 mg/kg/day in divided doses, max 1000 mg/day.
Adolescent: Dosing similar to adult for specific indications, adjusted by weight if necessary.
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Dose Adjustments

Renal Impairment:

Mild: CrCl 50-80 mL/min: Administer 50% of usual dose.
Moderate: CrCl 10-50 mL/min: Administer 25% of usual dose.
Severe: CrCl < 10 mL/min: Contraindicated due to risk of accumulation and toxicity.
Dialysis: Not dialyzable. Contraindicated in severe renal disease. If used in patients on dialysis, administer after dialysis and monitor closely for adverse effects.

Hepatic Impairment:

Mild: Use with caution; monitor for signs of hepatic encephalopathy.
Moderate: Use with caution; monitor for signs of hepatic encephalopathy. Consider dose reduction.
Severe: Contraindicated 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 formation of bicarbonate and hydrogen ions. In the kidney, this leads to increased excretion of bicarbonate, sodium, potassium, and water, resulting in diuresis. In the eye, it reduces the formation of aqueous humor, thereby lowering intraocular pressure. In the CNS, it may affect neuronal excitability by altering CO2 and bicarbonate levels.
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Pharmacokinetics

Absorption:

Bioavailability: Approximately 90-100%
Tmax: 2-4 hours (oral tablet)
FoodEffect: Food may delay absorption but does not significantly affect the extent of absorption.

Distribution:

Vd: Approximately 0.2 L/kg
ProteinBinding: Approximately 95% (to plasma proteins and carbonic anhydrase)
CnssPenetration: Limited, but sufficient to exert effects on CNS (e.g., anticonvulsant activity, effect on altitude sickness).

Elimination:

HalfLife: 2.4-5.8 hours
Clearance: Primarily renal clearance
ExcretionRoute: Renal (primarily unchanged drug)
Unchanged: Approximately 90% of the administered dose is excreted unchanged in the urine within 24 hours.
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Pharmacodynamics

OnsetOfAction: Oral: 1-1.5 hours
PeakEffect: Oral: 2-4 hours
DurationOfAction: Oral: 8-12 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 immediate medical attention:

Signs of an allergic reaction, such as:
+ 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
+ Swelling of the mouth, face, lips, tongue, or throat
Signs of acidosis (too much acid in the blood), such as:
+ Confusion
+ Rapid breathing
+ Rapid heartbeat
+ Abnormal heartbeat
+ Severe stomach pain, nausea, or vomiting
+ Excessive sleepiness
+ Shortness of breath
+ Feeling extremely tired or weak
Signs of electrolyte problems, such as:
+ Mood changes
+ Confusion
+ Muscle pain, cramps, or spasms
+ Weakness
+ Shakiness
+ Balance changes
+ Abnormal heartbeat
+ Seizures
+ Loss of appetite
+ Severe nausea or vomiting
Signs of high or low blood sugar, such as:
+ Fruity-smelling breath
+ Dizziness
+ Rapid breathing
+ Rapid heartbeat
+ Confusion
+ Sleepiness
+ Weakness
+ Flushing
+ Headache
+ Unusual thirst or hunger
+ Frequent urination
+ Shaking
+ 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 changes
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
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, such as:
+ Dark urine
+ Fatigue
+ Decreased appetite
+ Nausea or stomach pain
+ Light-colored stools
+ Vomiting
+ Yellow skin or 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 minor 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
Sleepiness
Fatigue
Weakness
Headache
Flushing
* Nervousness or excitability

Reporting Side Effects

If you have questions or concerns about side effects, 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 extreme tiredness (could indicate a blood problem)
  • Severe muscle weakness or cramps, irregular heartbeat (signs of electrolyte imbalance)
  • Confusion, disorientation, or severe drowsiness (especially in patients with liver problems)
  • Flank pain, blood in urine, or difficulty urinating (signs of kidney stones)
  • Persistent nausea, vomiting, or loss of appetite
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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 you experienced, including any symptoms that occurred.
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.

Additionally, provide your doctor and pharmacist with a comprehensive list of all your medications, including:
Prescription and over-the-counter (OTC) drugs
Natural products
* Vitamins

This will help ensure that it is safe to take this medication with your other medications and health conditions. Never start, stop, or change the dose of any medication without first consulting your doctor.
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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. Before engaging in activities that require alertness or clear vision, such as driving, wait until you understand how this drug affects you.

Regular blood tests and other laboratory evaluations should be conducted as directed 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 sunlight, 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 combining high doses of aspirin with this medication has led to 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 side effects. In some cases, this drug may affect growth in children and teenagers, necessitating regular growth assessments. Discuss this with your doctor.

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

Overdose Symptoms:

  • Severe electrolyte imbalance (e.g., hypokalemia, metabolic acidosis)
  • Drowsiness, confusion, lethargy
  • Anorexia, nausea, vomiting
  • Paresthesias
  • Tachypnea (rapid breathing)

What to Do:

Seek immediate medical attention. Treatment is primarily supportive and symptomatic. Correct electrolyte imbalances (e.g., administer potassium, bicarbonate). Gastric lavage or emesis may be considered if ingestion is recent. Acetazolamide is not significantly dialyzable. Call 1-800-222-1222 (Poison Control).

Drug Interactions

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Contraindicated Interactions

  • High-dose salicylates (risk of severe metabolic acidosis and CNS toxicity)
  • Methenamine (risk of crystalluria and decreased efficacy of methenamine)
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Major Interactions

  • Cyclosporine (increased cyclosporine levels)
  • Lithium (increased lithium excretion, decreased lithium levels)
  • Quinidine (decreased quinidine excretion, increased quinidine levels)
  • Other carbonic anhydrase inhibitors (additive toxicity)
  • Topiramate, Zonisamide (increased risk of metabolic acidosis)
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Moderate Interactions

  • Corticosteroids (increased risk of hypokalemia)
  • Digoxin (increased risk of digoxin toxicity due to hypokalemia)
  • Amphetamines, tricyclic antidepressants (decreased excretion, increased effects)
  • Oral anticoagulants (potential for altered anticoagulant effect, monitor INR)
  • Diuretics (additive diuretic and potassium-wasting effects)
  • Folic acid antagonists (e.g., methotrexate, pyrimethamine) (potential for increased toxicity)
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Minor Interactions

  • Sodium bicarbonate (may reduce acetazolamide efficacy)

Monitoring

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Baseline Monitoring

Complete Blood Count (CBC) with differential

Rationale: To establish baseline and monitor for blood dyscrasias (e.g., aplastic anemia, agranulocytosis, thrombocytopenia) which are rare but serious adverse effects.

Timing: Prior to initiation of therapy.

Serum Electrolytes (Sodium, Potassium, Bicarbonate, Chloride)

Rationale: To establish baseline and monitor for electrolyte imbalances, particularly hypokalemia and metabolic acidosis.

Timing: Prior to initiation of therapy.

Renal Function (BUN, Creatinine)

Rationale: To assess baseline renal function, as the drug is primarily renally eliminated and dose adjustments are required in renal impairment.

Timing: Prior to initiation of therapy.

Intraocular Pressure (IOP)

Rationale: For patients treated for glaucoma, to establish baseline and monitor therapeutic efficacy.

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 (normal range, monitor for decrease)

Action Threshold: Potassium < 3.0 mEq/L (consider supplementation); Bicarbonate < 18 mEq/L (consider discontinuation or bicarbonate supplementation if symptomatic acidosis).

Complete Blood Count (CBC)

Frequency: Every 3-6 months, or more frequently if signs of blood dyscrasias develop.

Target: Within normal limits for age and sex.

Action Threshold: Significant decrease in WBC, RBC, or platelet counts (investigate immediately, consider discontinuation).

Renal Function (BUN, Creatinine)

Frequency: Every 3-6 months, or as clinically indicated, especially in elderly or those with pre-existing renal impairment.

Target: Within normal limits; stable.

Action Threshold: Significant increase in BUN/Creatinine (re-evaluate dose, consider discontinuation).

Intraocular Pressure (IOP)

Frequency: As per glaucoma management guidelines (e.g., every 3-6 months or more frequently if uncontrolled).

Target: Individualized target IOP.

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

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Symptom Monitoring

  • Paresthesias (tingling/numbness in extremities, common but usually benign)
  • Fatigue, malaise, drowsiness
  • Nausea, vomiting, diarrhea, anorexia
  • Polyuria (increased urination)
  • Signs of metabolic acidosis (e.g., hyperventilation, confusion, lethargy)
  • Signs of electrolyte imbalance (e.g., muscle weakness, cramps, irregular heartbeat)
  • Signs of blood dyscrasias (e.g., fever, sore throat, unusual bleeding/bruising, pallor)
  • Skin rash, Stevens-Johnson syndrome (rare but serious)
  • Vision changes (e.g., transient myopia)
  • Flank pain, hematuria (signs of renal calculi)

Special Patient Groups

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Pregnancy

Acetazolamide is classified as Pregnancy Category D. This means there is positive evidence of human fetal risk based on adverse reaction data from investigational or marketing experience or studies in humans, but potential benefits may warrant use of the drug in pregnant women despite potential risks. Animal studies have shown teratogenic effects (e.g., limb defects, growth retardation). Use during pregnancy should only be considered if the potential benefit justifies the potential risk to the fetus.

Trimester-Specific Risks:

First Trimester: Potential for teratogenic effects, particularly limb defects, observed in animal studies. Avoid if possible.
Second Trimester: Risk of fetal growth retardation and electrolyte disturbances. Use with caution.
Third Trimester: Risk of fetal growth retardation, electrolyte disturbances, and potential for neonatal metabolic acidosis. Use with caution.
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Lactation

Acetazolamide is excreted into 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, diarrhea, or rash. The risk to the infant is generally considered low, but caution is advised, especially in premature infants or those with underlying conditions.

Infant Risk: Low risk (L3 - Moderately Safe)
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Pediatric Use

Used in pediatric patients for glaucoma, epilepsy, and hydrocephalus. Dosing is weight-based. Children may be more susceptible to metabolic acidosis and electrolyte imbalances. Close monitoring of electrolytes and acid-base status is crucial.

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Geriatric Use

Elderly patients may be more susceptible to adverse effects, particularly electrolyte imbalances (hypokalemia, metabolic acidosis), dehydration, and central nervous system effects (drowsiness, confusion). Renal function often declines with age, necessitating careful dose adjustment and monitoring. Start with lower doses and titrate slowly.

Clinical Information

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Clinical Pearls

  • Paresthesias (tingling sensation) are a very common and usually benign side effect, often occurring in the extremities. Patients should be counseled about this.
  • Acetazolamide is a sulfonamide derivative; therefore, patients with a history of sulfonamide allergy should be monitored closely for hypersensitivity reactions, although cross-reactivity is not absolute.
  • Long-term use can lead to metabolic acidosis, which may require bicarbonate supplementation or discontinuation of the drug.
  • Patients should be advised to maintain adequate fluid intake to prevent the formation of renal calculi (kidney stones), a known side effect.
  • The diuretic effect of acetazolamide tends to diminish with prolonged use due to the development of metabolic acidosis.
  • For acute mountain sickness, acetazolamide helps with acclimatization by increasing bicarbonate excretion, which acidifies the blood and stimulates respiration.
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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).
  • For Edema: Loop diuretics (e.g., furosemide), thiazide diuretics (e.g., hydrochlorothiazide), potassium-sparing diuretics (e.g., spironolactone).
  • For Epilepsy: Various other anticonvulsants (e.g., valproic acid, carbamazepine, lamotrigine, levetiracetam).
  • For Altitude Sickness: Dexamethasone (for severe symptoms), gradual ascent.
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Cost & Coverage

Average Cost: $15 - $50 per 30 tablets (250mg)
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 your 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 emergency medical attention. When seeking help, be prepared to provide details about the medication taken, the amount, and the time it occurred.