Acetazolamide (250mg)

May 01, 2023

Introduction

ATZOLSMILE 250 contains Acetazolamide 250 mg, a potent carbonic anhydrase inhibitor used to treat various medical conditions, including glaucoma, altitude sickness, epilepsy, diuretic-related disorders, and metabolic alkalosis. It exerts its action primarily by modulating bicarbonate and sodium transport, reducing fluid buildup and pressure in various body tissues.

Acetazolamide Tablets IP 250 mg Uses

ATZOLSMILE 250 is indicated in the treatment and prevention of:

  • Glaucoma (chronic open-angle and secondary)

  • Acute mountain sickness (altitude sickness)

  • Epilepsy (as adjunctive therapy)

  • Edema associated with congestive heart failure or drug-induced fluid retention

  • Metabolic alkalosis

  • Periodic paralysis

 It helps relieve pressure in the eye and brain and reduces fluid retention in the body.

Mechanism of Action of Acetazolamide

Acetazolamide Mechanism of Action (MOA):

Acetazolamide is a carbonic anhydrase (CA) inhibitor, which blocks the enzyme carbonic anhydrase in the proximal renal tubule, ciliary body of the eye, choroid plexus of the brain, and other tissues.

Key Steps in MOA:

  • Inhibits carbonic anhydrase, reducing the conversion of carbon dioxide and water to carbonic acid.

  • Leads to decreased reabsorption of bicarbonate (HCO₃⁻) in the kidney.

  • Results in alkaline diuresis, causing increased excretion of bicarbonate, sodium, potassium, and water.

  • In the eye, it reduces the production of aqueous humor, lowering intraocular pressure.

  • In the CNS, it alters the pH of cerebrospinal fluid, which may help control seizures.

The net effect is diuretic, anticonvulsant, and pressure-reducing.

Synthesis of Acetazolamide (Brief Overview)

Acetazolamide is a sulfonamide derivative synthesized through a multi-step process:

  1. Starting compound: Acetamide.

  2. Introduction of a thiadiazole ring to form 5-acetamido-1,3,4-thiadiazole-2-sulfonamide.

  3. The sulfonamide group is essential for its inhibitory action on carbonic anhydrase.

  4. Purification and crystallization yield Acetazolamide in its final form.

 Note: The actual industrial synthesis may involve more complex chemical pathways and protective group chemistry for large-scale production.

Dosage and Administration of Acetazolamide 250 mg

Indication Recommended Adult Dose
Glaucoma 250–1000 mg/day in divided doses
Acute Mountain Sickness 500–1000 mg/day (starting 1–2 days before ascent)
Epilepsy 250–1000 mg/day in divided doses
Edema 250–375 mg once daily in the morning
Metabolic Alkalosis 250–375 mg once or twice daily

 

  • Take with or after food to reduce gastrointestinal discomfort.

  • Always follow physician guidance for dosage adjustment in renal or hepatic impairment.

Side Effects of Acetazolamide Tablets IP 250 mg

Common Side Effects:

  • Tingling sensation (paresthesia)

  • Increased urination (diuresis)

  • Fatigue or drowsiness

  • Taste alterations

  • Nausea or vomiting

Serious Side Effects:

  • Electrolyte imbalance (hypokalemia, hyponatremia)

  • Metabolic acidosis

  • Blood disorders (aplastic anemia, leukopenia)

  • Kidney stones

  • Allergic reactions (rash, Stevens-Johnson syndrome)

If you notice signs of serious allergic reaction, electrolyte imbalance, or unusual bleeding—seek medical help immediately.

Contraindications and Precautions

Contraindications:

  • Known hypersensitivity to sulfonamides or acetazolamide

  • Severe hepatic or renal dysfunction

  • Adrenal gland failure

  • Hyponatremia or hypokalemia

  • Pregnancy (especially in the first trimester)

Use with Caution In:

  • Elderly patients

  • Patients with diabetes mellitus

  • Those at risk of metabolic acidosis

Drug Interactions

  • May enhance the effects of salicylates and methotrexate

  • Can decrease the effect of antiepileptics if used improperly

  • Increases risk of hypokalemia when used with diuretics like furosemide

  • May affect lithium levels

Storage Instructions

  • Store in a dry, cool place below 30°C

  • Protect from light and moisture

  • Keep out of reach of children

FAQs – Acetazolamide Tablets IP 250 mg (ATZOLSMILE 250)

Q1: What is Acetazolamide 250 mg used for?

A: It is used to treat glaucoma, epilepsy, altitude sickness, edema, and metabolic alkalosis.

Q2: How does Acetazolamide work in the body?

A: It inhibits carbonic anhydrase, reducing fluid buildup and controlling pressure in the eye, brain, and kidneys.

Q3: Is Acetazolamide a diuretic?

A: Yes, it causes mild diuresis by promoting the excretion of sodium, bicarbonate, and water.

Q4: When should Acetazolamide be taken for altitude sickness?

A: Start 1–2 days before ascent and continue during your stay at high altitude.

Q5: Can I use Acetazolamide in pregnancy?

A: It is not recommended during pregnancy unless prescribed under strict medical supervision.

Q6: Does Acetazolamide affect potassium levels?

A: Yes, it can lower potassium levels; monitoring and supplementation may be required.

Conclusion

ATZOLSMILE 250 (Acetazolamide Tablets IP 250 mg) by Steris Healthcare Pvt. Ltd. is a reliable, multipurpose carbonic anhydrase inhibitor that plays a critical role in managing fluid pressure-related conditions such as glaucoma, altitude sickness, and edema. With a well-established mechanism, versatile uses, and a tolerable side effect profile, it remains an important tool in both neurology and ophthalmology.

About The Author

STERIS HEALTHCARE PVT LTD

Steris Healthcare Pvt Ltd, known as Sterispharma, was founded in February 2018 by a team of experienced professionals in the pharmaceutical industry. Headquartered in Navi Mumbai, the company holds certifications from WHO, GMP, and ISO, reflecting its dedication to maintaining high standards of quality and safety. Sterispharma’s mission is to provide affordable, high-quality medications across India, strictly adhering to WHO guidelines. With the convenience of an online pharmacy, customers can easily order medicines with home delivery options.

For further information 

Email: info@sterispharma.com / contact@sterispharma.com

Call/WhatsApp: 8209542042 , 8824175417

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