Acetazolamide 500mg Inj, 1 Vial

Manufacturer X-GEN PHARMACEUTICALS, INC Active Ingredient Acetazolamide Injection Solution(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 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, Agent for altitude sickness
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Pharmacologic Class
Carbonic Anhydrase Inhibitor
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Pregnancy Category
Category C
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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 helps your body get rid of extra fluid, lower pressure in your eyes, or prevent altitude sickness. It works by affecting how your kidneys handle salts and water, and by reducing fluid production in your eyes and brain. It's often used for conditions like glaucoma, swelling, or to help you adjust to high altitudes.
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How to Use This Medicine

To use this medication correctly, follow your doctor's instructions and carefully read all accompanying information. Take this medication exactly as directed, and adhere to all guidelines provided. This drug is administered via intravenous injection.

For storage and disposal, consult with your doctor, nurse, or pharmacist to determine the best approach if you need to keep this medication at home.

If you miss a dose, contact your doctor immediately to receive guidance on the next steps to take.
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Lifestyle & Tips

  • Stay well-hydrated unless otherwise instructed by your doctor, especially when used as a diuretic or for altitude sickness.
  • Avoid excessive alcohol consumption, as it can worsen some side effects.
  • Report any unusual tingling sensations, numbness, or muscle weakness to your doctor.
  • If you have diabetes, monitor your blood sugar levels closely as this medication may affect them.
  • If you are taking this for altitude sickness, start taking it 1-2 days before ascending and continue for 2-4 days after reaching your destination or longer if symptoms persist.

Dosing & Administration

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Adult Dosing

Standard Dose: Varies by indication. For acute angle-closure glaucoma: 500 mg IV stat, then 125-250 mg every 4 hours. For edema: 250-375 mg IV once daily. For acute mountain sickness: 250-500 mg IV every 6-12 hours.
Dose Range: 125 - 1000 mg

Condition-Specific Dosing:

acuteAngleClosureGlaucoma: 500 mg IV stat, then 125-250 mg every 4 hours
edema: 250-375 mg IV once daily
acuteMountainSickness: 250-500 mg IV every 6-12 hours
epilepsyAdjunct: 250-1000 mg/day IV in divided doses
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Pediatric Dosing

Neonatal: Not established for routine use; consult specialist for specific conditions (e.g., hydrocephalus).
Infant: Glaucoma: 5-10 mg/kg/dose IV every 6 hours; Max 1000 mg/day. Edema: 5 mg/kg/dose IV once daily.
Child: Glaucoma: 5-10 mg/kg/dose IV every 6 hours; Max 1000 mg/day. Edema: 5 mg/kg/dose IV once daily. Epilepsy: 8-30 mg/kg/day IV in divided doses; Max 1000 mg/day.
Adolescent: Glaucoma: 5-10 mg/kg/dose IV every 6 hours; Max 1000 mg/day. Edema: 5 mg/kg/dose IV once daily. Epilepsy: 8-30 mg/kg/day IV in divided doses; Max 1000 mg/day.
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Dose Adjustments

Renal Impairment:

Mild: CrCl 30-50 mL/min: Administer every 12 hours.
Moderate: CrCl 10-29 mL/min: Administer every 24 hours.
Severe: CrCl <10 mL/min: Contraindicated or use with extreme caution at reduced frequency (e.g., every 48 hours) if absolutely necessary. Risk of accumulation and toxicity.
Dialysis: Hemodialysis: Acetazolamide is dialyzable. Administer dose after dialysis on dialysis days. Peritoneal Dialysis: Not well studied, use with caution.

Hepatic Impairment:

Mild: No specific dose adjustment, but monitor closely for signs of hepatic encephalopathy.
Moderate: Use with caution; increased risk of hepatic encephalopathy. Consider lower doses and close monitoring.
Severe: Contraindicated in severe hepatic dysfunction or cirrhosis due to risk of hepatic coma.

Pharmacology

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Mechanism of Action

Acetazolamide is a potent carbonic anhydrase inhibitor. It acts on the renal tubule, specifically the proximal convoluted tubule, to inhibit carbonic anhydrase, leading to decreased reabsorption of bicarbonate, sodium, and water. This results in increased excretion of bicarbonate, sodium, potassium, and water, causing diuresis and alkalinization of the urine. In the eye, it reduces the formation of aqueous humor by inhibiting carbonic anhydrase in the ciliary body, thereby lowering intraocular pressure. In the central nervous system, it may inhibit carbonic anhydrase in the brain, which can reduce abnormal neuronal discharge in epilepsy and facilitate acclimatization to high altitudes by increasing ventilation.
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Pharmacokinetics

Absorption:

Bioavailability: 100% (IV)
Tmax: Immediate (IV)
FoodEffect: Not applicable for IV formulation.

Distribution:

Vd: 0.2 L/kg
ProteinBinding: 95% (to plasma proteins and carbonic anhydrase)
CnssPenetration: Limited

Elimination:

HalfLife: 3-6 hours
Clearance: Renal clearance is approximately 0.35 mL/min/kg
ExcretionRoute: Renal (primarily tubular secretion)
Unchanged: 90-100%
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Pharmacodynamics

OnsetOfAction: 2 minutes (IV)
PeakEffect: 15-30 minutes (IV)
DurationOfAction: 4-6 hours (IV)

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 immediately or seek emergency medical attention:

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.
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, pale 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 minor ones, it's essential to discuss any concerns with your doctor. If you experience any of the following side effects, contact your doctor if they bother you or persist:

Diarrhea, nausea, or vomiting.
Changes in taste.
Decreased appetite.
Blurred vision.
Dizziness, sleepiness, tiredness, or weakness.
Headache.
Flushing.
Nervousness or excitability.
Pain at the injection site.

This is not an exhaustive list of possible 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 indicate a serious skin reaction)
  • Unusual bleeding or bruising, persistent sore throat, fever, or signs of infection (could indicate blood problems)
  • Severe fatigue, confusion, or extreme drowsiness (could indicate metabolic acidosis or electrolyte imbalance)
  • Muscle weakness, cramps, or irregular heartbeat (could indicate low potassium)
  • Severe abdominal pain, nausea, vomiting, or dark urine (could indicate liver problems)
  • Flank pain, blood in urine, or painful urination (could indicate kidney stones)
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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.

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

Regularly undergo blood tests and other laboratory examinations as directed by your doctor to monitor your condition.

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 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 growth in 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 taking this medication to ensure the well-being of both you and your baby.
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Overdose Information

Overdose Symptoms:

  • Severe metabolic acidosis
  • Electrolyte imbalances (e.g., hypokalemia, hyponatremia)
  • CNS depression (drowsiness, confusion, lethargy)
  • Dehydration

What to Do:

Seek immediate medical attention. Call 911 or your local emergency number. For poison control, call 1-800-222-1222. Management is primarily supportive, including correction of electrolyte imbalances and metabolic acidosis, and fluid replacement. Hemodialysis may be considered in severe cases as acetazolamide is dialyzable.

Drug Interactions

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Contraindicated Interactions

  • Salicylates (high-dose): Concurrent use can lead to severe metabolic acidosis and CNS toxicity due to displacement of acetazolamide from protein binding sites and inhibition of renal clearance.
  • Methenamine: Acetazolamide alkalinizes urine, which can prevent methenamine from being converted to formaldehyde, rendering it ineffective as a urinary antiseptic.
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Major Interactions

  • Cyclosporine: Acetazolamide may increase cyclosporine levels, increasing risk of nephrotoxicity and neurotoxicity.
  • Lithium: Acetazolamide increases renal excretion of lithium, potentially leading to decreased lithium levels and loss of therapeutic effect.
  • Other diuretics (e.g., loop, thiazide): Additive diuretic and potassium-wasting effects, increasing risk of hypokalemia and metabolic acidosis.
  • Corticosteroids: Increased risk of hypokalemia.
  • Amphotericin B: Increased risk of hypokalemia.
  • Quinidine: Acetazolamide alkalinizes urine, which can decrease renal excretion of quinidine, leading to increased quinidine levels and toxicity.
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Moderate Interactions

  • Anticonvulsants (e.g., phenytoin, carbamazepine): May alter levels of either drug; monitor closely.
  • Oral hypoglycemics: May alter blood glucose control; monitor glucose levels.
  • Sodium bicarbonate: Increased risk of metabolic alkalosis.
  • Topiramate: Increased risk of metabolic acidosis and kidney stone formation.
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Minor Interactions

  • Not available

Monitoring

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Baseline Monitoring

Serum Electrolytes (Sodium, Potassium, Bicarbonate, Chloride)

Rationale: To establish baseline electrolyte status and identify pre-existing imbalances, especially hypokalemia or metabolic acidosis, which can be exacerbated by acetazolamide.

Timing: Prior to initiation of therapy.

Renal Function (BUN, Serum Creatinine)

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

Timing: Prior to initiation of therapy.

Complete Blood Count (CBC) with differential

Rationale: To establish baseline hematologic parameters and monitor for potential rare but serious adverse effects like blood dyscrasias (e.g., agranulocytosis, aplastic anemia).

Timing: Prior to initiation of therapy, especially for long-term use.

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Routine Monitoring

Serum Electrolytes (Potassium, Bicarbonate)

Frequency: Weekly for first few weeks, then monthly or as clinically indicated, especially with concomitant diuretics or corticosteroids.

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 (consider dose reduction or discontinuation if symptomatic metabolic acidosis).

Renal Function (BUN, Serum Creatinine)

Frequency: Monthly or as clinically indicated, especially in patients with pre-existing renal impairment or those on long-term therapy.

Target: Within patient's baseline or normal limits.

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

Intraocular Pressure (for glaucoma patients)

Frequency: As per ophthalmologist's recommendation, typically at follow-up visits.

Target: Individualized target IOP.

Action Threshold: Failure to achieve target IOP or significant fluctuations.

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Symptom Monitoring

  • Paresthesias (tingling sensation in extremities, common but usually benign)
  • Fatigue, lethargy, confusion (signs of metabolic acidosis or electrolyte imbalance)
  • Nausea, vomiting, abdominal pain
  • Rash, fever, sore throat (signs of hypersensitivity or blood dyscrasias)
  • Flank pain, hematuria (signs of kidney stones)
  • Muscle weakness, cramps (signs of hypokalemia)
  • Signs of hepatic encephalopathy (in patients with liver impairment)

Special Patient Groups

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Pregnancy

Category C. Use only if the potential benefit justifies the potential risk to the fetus. Animal studies have shown teratogenic effects (limb defects) at high doses. There are no adequate and well-controlled studies in pregnant women.

Trimester-Specific Risks:

First Trimester: Potential for teratogenicity based on animal data; avoid if possible.
Second Trimester: Limited human data; use with caution.
Third Trimester: Limited human data; use with caution. Risk of metabolic acidosis in the neonate.
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Lactation

L3 (Moderately Safe). Acetazolamide is excreted into breast milk in small amounts. While adverse effects in breastfed infants are generally not expected, monitor the infant for signs of metabolic acidosis (e.g., poor feeding, lethargy) or growth retardation, especially with prolonged use or high doses.

Infant Risk: Low to moderate. Potential for mild metabolic acidosis or electrolyte imbalance in the infant, though unlikely with typical doses.
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Pediatric Use

Dosing is established for specific indications (glaucoma, epilepsy, edema). Use with caution, especially in neonates and infants, due to potential for metabolic acidosis and electrolyte imbalances. Close monitoring of electrolytes and acid-base status is crucial.

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Geriatric Use

Increased susceptibility to adverse effects, particularly electrolyte imbalances (hypokalemia, hyponatremia), metabolic acidosis, and renal impairment. Start with lower doses and titrate slowly. Monitor renal function and electrolytes frequently. Increased risk of falls due to diuretic effect.

Clinical Information

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Clinical Pearls

  • Acetazolamide is a sulfonamide derivative; caution should be exercised in patients with a history of sulfonamide allergy, although cross-reactivity is not absolute.
  • Paresthesias (tingling of fingers, toes, or around the mouth) are a very common side effect, often benign and dose-related, and usually do not require discontinuation.
  • Can cause metabolic acidosis, especially with prolonged use or in patients with renal impairment. Monitor serum bicarbonate levels.
  • May increase the risk of kidney stone formation due to decreased urinary citrate and increased urinary pH.
  • Ensure adequate hydration to prevent kidney stone formation, unless contraindicated for fluid restriction.
  • The IV formulation is preferred for acute situations (e.g., acute angle-closure glaucoma) due to rapid onset of action.
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Alternative Therapies

  • For glaucoma: Topical beta-blockers (e.g., timolol), prostaglandin analogs (e.g., latanoprost), alpha-2 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, levetiracetam, lamotrigine).
  • For altitude sickness: Dexamethasone (for severe symptoms), gradual ascent.
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Cost & Coverage

Average Cost: $10 - $50 per 500mg vial
Generic Available: Yes
Insurance Coverage: Tier 1 or Tier 2 (Generic)
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General Drug Facts

If your symptoms or health problems do not improve or worsen over time, it is essential to contact your doctor for further evaluation and guidance. To ensure safe use, never share your prescription medications with others, and do not take medications that have been prescribed to someone else.

Store all medications in a secure location, out of the reach of children and pets, to prevent accidental ingestion. Proper disposal of unused or expired medications is crucial. Unless instructed otherwise by a healthcare professional or pharmacist, do not dispose of medications by flushing them down the toilet or pouring them down the drain. Instead, consult with your pharmacist to determine the best method for disposal, as some communities may have designated drug take-back programs.

Additionally, some medications may come with a separate patient information leaflet, which can be obtained by consulting with your pharmacist. If you have any questions or concerns about your medication, it is recommended that you discuss them with your doctor, nurse, pharmacist, or other healthcare provider.

In the event of a suspected overdose, immediately contact your local poison control center or seek emergency medical attention. Be prepared to provide information about the medication taken, including the dosage and timing of the incident, to facilitate prompt and effective treatment.