Acetin Cap 25 mg 3×10’s (Acetazolamide)-Potential Overview

Generic Information

• Brand Name: Acetin Cap
• Generic Name: Acetazolamide
• Strength: 25 mg per capsule
• Pack Size: 30 capsules (3×10’s)
• Pharmaceutical Class:
  • Class: Carbonic Anhydrase Inhibitor
  • Type: Diuretic, Anticonvulsant

Indications for Use

Acetin (Acetazolamide) is used for the treatment of:

1. Glaucoma:
   • Reduces intraocular pressure in patients with open-angle or secondary glaucoma.
2. Edema:
   • Treatment of edema associated with heart failure, renal disease, or drug-induced edema.
3. Epilepsy:
   • Adjunct treatment for certain types of epilepsy (e.g., generalized tonic-clonic seizures).
4. Acute Mountain Sickness (AMS):
   • Used as a prophylactic treatment for altitude sickness in climbers.
5. Hypercalciuria:
   • Used to treat excessive calcium in the urine.
6. Idiopathic Intracranial Hypertension (IIH):
   • Reduces intracranial pressure in conditions like pseudotumor cerebri.

Common Side Effects

• Gastrointestinal:
  • Nausea, vomiting, loss of appetite, dry mouth, taste alterations.
• Central Nervous System:
  • Drowsiness, dizziness, headache, fatigue.
• Urinary:
  • Increased urination, polyuria.
• Skin Reactions:
  • Rash, itching, photosensitivity.

Serious Side Effects (Less Common)

• Electrolyte Imbalance:
  • Hypokalemia (low potassium), hyponatremia (low sodium), metabolic acidosis.
• Blood Disorders:
  • Thrombocytopenia (low platelet count), leukopenia (low white blood cell count), aplastic anemia.
• Kidney:
  • Renal stones, nephrolithiasis (kidney stones), kidney dysfunction.
• Liver Toxicity:
  • Hepatitis, jaundice, and liver damage.
• Severe Allergic Reactions:
  • Anaphylaxis, difficulty breathing, swelling of the throat or lips.

Dosage and Usage Instructions

1. For Adults:
   • Glaucoma:
     • 250 mg (1 tablet) twice daily. Dosage may be adjusted based on the patient’s response.
   • Edema:
     • Initial dose of 250 mg to 500 mg daily. May be adjusted as needed.
   • Acute Mountain Sickness (AMS):
     • 125-250 mg twice daily starting 1 day before ascent and continuing for the first 48 hours at high altitude.
   • Epilepsy:
     • Start with 250 mg once or twice daily, and increase gradually based on response.
   • Idiopathic Intracranial Hypertension:
     • 250 mg twice daily. Dosage adjustment may be necessary.
2. Dosage Instructions:
   • Take Acetin capsules with food to minimize gastrointestinal upset.
   • Swallow whole with a full glass of water.
   • Missed Dose: If a dose is missed, take it as soon as remembered unless it is almost time for the next dose. Do not double the dose.

Drug Interactions

1. With Food:
   • No significant interaction with food, but taking with food may reduce stomach irritation.
2. With Other Medications:
   • Other Diuretics (e.g., Furosemide): Increased risk of dehydration, electrolyte imbalance.
   • Corticosteroids (e.g., Prednisone): Increased risk of hypokalemia (low potassium).
   • Salicylates (e.g., Aspirin): Increased risk of metabolic acidosis.
   • Anticonvulsants (e.g., Phenytoin, Carbamazepine): Increased risk of metabolic acidosis and reduced effectiveness of anticonvulsant drugs.
   • Carbonic Anhydrase Inhibitors (e.g., Methazolamide): Avoid concomitant use due to additive effects on carbonic anhydrase inhibition.
   • Lithium: Increased lithium toxicity due to renal effects.
   • Digoxin: Risk of digoxin toxicity due to electrolyte imbalances (e.g., hypokalemia).
3. Other Interactions:
   • Alcohol: Use with caution; alcohol may increase the risk of side effects like dizziness or drowsiness.
   • Xanthines (e.g., Theophylline): Potential increase in theophylline toxicity due to renal function changes.

Regulatory Approval and Manufacturer

• Regulatory Approval:
  • Acetazolamide is approved in various countries, including the U.S., India, and Europe, for its uses in glaucoma, edema, epilepsy, and acute mountain sickness.
• Manufacturer:
  • Manufactured by various pharmaceutical companies across the globe, including companies like Mylan, Cipla, and others.

Pharmacist-Related Data

Drug Name and Chemical Details

• Generic Name: Acetazolamide
• Chemical Formula: C4H6N4O3S2
• CAS Number: 59-66-5
• Molecular Weight: 222.2 g/mol

Pharmacodynamics

1. Mechanism of Action:
   • Acetazolamide is a carbonic anhydrase inhibitor. It works by inhibiting the enzyme carbonic anhydrase, which catalyzes the conversion of carbon dioxide and water to carbonic acid. This inhibition leads to reduced bicarbonate reabsorption in the kidneys, resulting in increased urine output (diuresis) and correction of fluid and electrolyte imbalances. It also reduces the production of aqueous humor in the eye, lowering intraocular pressure.
2. Therapeutic Effects:
   • Diuretic: Promotes fluid excretion, thus reducing edema.
   • Antiglaucoma: Lowers intraocular pressure in patients with glaucoma.
   • Anticonvulsant: Used as an adjunct for certain types of epilepsy.
   • Altitude Sickness Prevention: Reduces symptoms of acute mountain sickness by correcting metabolic alkalosis and promoting fluid balance.

Pharmacokinetics

1. Absorption:
   • Acetazolamide is well absorbed from the gastrointestinal tract, with peak plasma concentrations occurring within 2-4 hours after oral administration.
2. Distribution:
   • It is widely distributed throughout the body, including the eyes, brain, and kidneys, where its action is most pronounced. It has a moderate protein-binding capacity (about 40-50%).
3. Metabolism:
   • Acetazolamide is minimally metabolized in the liver and is primarily excreted unchanged in the urine.
4. Excretion:
   • Excreted mainly by the kidneys, with a significant amount of the drug excreted in the urine.
5. Half-Life:
   • The elimination half-life of acetazolamide is approximately 3 to 5 hours, which supports its frequent dosing.

Drug Interactions

1. With Food:
   • There is no significant interaction between food and acetazolamide, although it may help reduce gastrointestinal discomfort if taken with food.
2. With Other Medications:
   • Other Diuretics: Caution with other diuretics to avoid excessive fluid loss and dehydration.
   • Lithium: Increased risk of lithium toxicity due to impaired renal clearance.
   • Corticosteroids: Increased risk of electrolyte disturbances (e.g., hypokalemia) when used together.
   • Salicylates: Increases the risk of acidosis and should be used cautiously together.
3. Other Interactions:
   • Alcohol: Use with caution as alcohol may exacerbate side effects like dizziness, drowsiness, and confusion.

Clinical Considerations

1. Pregnancy Category:
   • Category C: Acetazolamide should be used during pregnancy only if the potential benefit justifies the potential risk to the fetus. It is contraindicated during the first trimester unless absolutely necessary.
2. Lactation:
   • Acetazolamide is excreted in breast milk. While it is generally considered safe for short-term use, it is recommended to avoid its use during breastfeeding, especially in high doses.
3. Pediatric Use:
   • Safety and efficacy in children have not been established. Acetazolamide is generally not recommended for pediatric use unless prescribed by a physician.
4. Geriatric Use:
   • Elderly patients may be more susceptible to side effects like electrolyte imbalances and kidney dysfunction. Use with caution and monitor renal function.
5. Other Considerations:
   • Renal and Hepatic Impairment: Use with caution in patients with pre-existing renal or liver dysfunction, and monitor renal and hepatic function regularly.
   • Electrolyte Imbalance: Monitor for signs of electrolyte disturbances (e.g., hypokalemia, hyponatremia) during therapy.