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Acetazolamide capsules 

Dosage Format: Capsule, Extended Release.
Classes of Drugs: Carbonic Anhydrase Inhibitors for Anticonvulsants, Carbonic Anhydrase Inhibitors.

What is Acetazolamide Capsule?

Acetazolamide extended-release capsules act as inhibitors of the carbonic enzyme anhydrase. Acetazolamide is a light to slightly yellowish white crystalline inert, odorless, and moderately acidic compound that is soluble in water and a little soluble in alcohol. The chemical name for acetazolamide is n-(5-sulfamoyl-1,3,4-thiadiazol-2-yl) acetamide and has the following chemical structure: The extended-release acetazolamide capsule designed for oral use includes 500 mg of acetazolamide. Additionally, every capsule has the following inactive ingredients: ammonia methacrylate copolymer dispersion types b and a, microcrystalline cellulose, gelatin, sodium lauryl, sodium sulphate, and titanium dioxide. The capsule is printed using black pharmaceutical ink that has the black oxide of iron as an agent for coloring.


The possibility of death has been reported, however rarely, because of severe reactions to sulfonamides, including stevens-johnson syndrome, toxic epidermal necrolysis, anaphylaxis, fulminant liver necrosis, agranulocytosis, aplastic anaemia, and other blood dyscrasias. It is possible that sensitization will recur if a drug is administered again, regardless of the route used to administer it. If symptoms of hypersensitivity or other severe reactions are observed, then stop taking this medication. A cautious approach is suggested for patients who are taking high-dose aspirin in conjunction with acetazolamide, as symptoms such as anorexia dysphoria, lethargy, tachypnea acidosis, coma, and even death have been documented.

Prior to Using this Drug

Acetazolamide is an effective carbonic anhydrase inhibitor, which is efficient in controlling the secretion of fluids (e.g., various forms of glaucoma) as well as for the treatment of specific convulsive disorders (e.g., epilepsy), as well as in stimulating diuresis in situations of abnormal retention of fluid (e.g., cardiac oedema). Acetazolamide isn't a diuretic that is mercurial. It is, instead, a sulfonamide that is non-bacteriostatic and has a chemical structure as well as pharmacological properties that are distinct in comparison to the bacteriostatic sulfonamides. Acetazolamide is an inhibitor of enzymes that specifically targets carbonic anhydrase. It is the enzyme responsible for triggering an irreversible reaction that results in the reduction of carbon dioxide and the removal of carbonic acid. Within the eye, the acetazolamide inhibitory effect reduces the production of aqueous humor. This results in a decrease in intraocular pressure. This is what is considered beneficial in the case of glaucoma or even for certain conditions that are not glaucomatous. The evidence suggests that acetazolamide can be used as an adjuvant to treat certain disorders of the central nervous system (e.g., epilepsy). Its inhibition of carbonic acid hydrase in this region appears to reduce abnormal, paroxysmal, and excessive discharges from central nervous system neurons. Acetazolamide's diuretic effects result from its actions in the kidney on the irreversible processes of hydration of carbon dioxide and dehydration of carbonic acid. This results in renal reduction of the hco3 ion, which transports sodium, water, and potassium. The alkalinization of urine and diuresis promotion are impaired. Ammonia metabolism is altered as a result of the increased absorption of ammonia in the kidney tubules due to the alkalinization of urine. Acetazolamide extended-release capsules offer extended action that inhibits the secretion of aqueous humor for between 18 and 24 hours after the dose. Tablets are only effective for eight or 12 hours. Because of the long-lasting, continuous effects of extended-release acetazolamide capsules, an increase in the frequency of doses is possible. Acetazolamide concentrations in plasma peak between three and six hours after taking extended-release acetazolamide capsules, as opposed to between one and four hours when taking tablets. Food intake does not impact the absorption of acetazolamide extended-release capsules. Clinical trials that have been controlled by placebos have demonstrated that the prophylactic use of acetazolamide with a dose of 250 mg daily for eight or twelve hours (or 500 mg capsule controlled release every day) in the early and middle stages of the rapid ascent of altitude results in fewer or no manifestations of the acute illness (ams) like nausea, headaches, shortness of breath, fatigue, dizziness, and fatigue. The function of the lungs (e.g., the ability to breathe, minute respiration, exhausted vital capacity, or peak flow) is higher in the group treated with acetazolamide as well as in those with ams and in asymptomatic individuals. Climbers treated with acetazolamide also experienced fewer sleep difficulties.

How to take Acetazolamide Capsules?

It is a adjunctive treatment for persistent simple (open-angle) glaucoma secondary glaucoma and surgically for acute angle closure glaucoma, where delaying surgical intervention is required for the purpose of lowering the pressure in the eye. Acetazolamide extended-release capsules are used for the alleviation or reduction of signs and symptoms that are associated with acute mountain sickness in spite of the gradual rise.


Hypersensitivity to acetazolamide and excipients used in the formulation. Since acetazolamide can be viewed as a sulfonamide derivative, cross-sensitivity between acetazolamide, sulfonamides, and other sulfonamide derivatives could be feasible. Acetazolamide treatment isn't recommended for situations where sodium or potassium blood serum levels are low, for instances of kidney or liver disease or malfunction, suprarenal dysfunction, or in the presence of hyperchloremic acidosis. It's not advised for those who suffer from cirrhosis due to the potential for the development of hepatic encephalopathy. Acetazolamide long-term use is not recommended for patients suffering from chronic glaucoma that is not congestive because it could cause organic closure of the angle as the glaucoma worsens and is hidden by lower intraocular pressure.

What should be avoided?


Increased doses do make it less diurnal and could increase the risk of paresthesia and drowsiness. In most cases, increasing the dose will result in a reduction in diuresis. However, in certain instances, extremely large doses are administered in conjunction with diuretics to maintain diuresis during refractory failure.

Information for patients

Common adverse reactions to the sulfonamide derivatives can be seen with fever, anaphylaxis, and eruptions (including stevens-johnson syndrome neurotoxic epidermal necrosis), crystalluria, bone marrow degeneration, and thrombocytopenic purpura. They can also cause hemolytic anaemia, leukopenia, pancytopenia, and granulocytosis. Beware of rapid detection of these reactions. The drug must be stopped, and appropriate treatment must be implemented.

Patients suffering from an obstruction to the lungs or with emphysema, in which breathing through the alveoli is impaired, must be administered with caution. Acetazolamide, which can cause or worsen acidosis, must be administered with caution.

A gradual ascent is recommended in order to prevent the acute symptoms of mountain sickness. If rapid ascents are undertaken with acetazolamide, it is important to note that this doesn't eliminate the necessity for rapid descent in the event that severe symptoms of high altitude illness are observed, i.e., high altitude respiratory ooedema (hape) or cerebral ooedema at high altitude.

It is recommended to be cautious for those who are taking high-dose aspirin in conjunction with acetazolamide, as symptoms such as anorexia, thetahypnea, fatigue, metabolic acidosis, coma, and even death have been documented

The increase and decrease in blood glucose levels were reported in patients being treated with acetazolamide. This is something to take into account for patients suffering from an impaired tolerance to glucose or with diabetes mellitus.

Acetazolamide therapy can cause an imbalance in electrolytes, such as hypokalemia and hyponatremia, and metabolic acidosis. So, periodic examination of the levels of electrolytes in serum is suggested. It is especially important to be cautious when patients suffer from ailments that are associated with or may predispose someone to an imbalance in acid or electrolytes, for example, patients suffering from impairments in kidney function , patients suffering from diabetes mellitus, or patients suffering from a lack of alveolar ventricle.

Certain adverse reactions associated with acetazolamide, including drowsiness, fatigue, or myopia, can hinder the ability to operate and drive. Control equipment.

Laboratory tests

For monitoring for reactions to hematologic causes that are common to all sulfonamides, it is suggested to have the baseline cbc along with a count of platelets taken on patients before initiating treatment with acetazolamide and also at regular intervals throughout therapy. If there are significant changes, prompt discontinuation and implementation of appropriate therapy are essential. Monitoring the electrolyte levels in the serum regularly is advised.

Details on dosage of Acetazolamide capsules


The suggested dosage is one capsule (500 mg) twice a day. It is common to take one capsule at the beginning of the day and one capsule in the evening. It is possible to modify the dosage; however, it is generally discovered that an amount in excess of two capsules (1 gramme) is not a cause for an increase in the result. Dosage should be adjusted according to individual considerations for symptoms and intraocular pressure. Constant surveillance by a medical professional is always recommended.

If there are rare circumstances where sufficient control cannot be achieved with the daily administration twice a day of extended-release acetazolamide capsules, the required control can be achieved through acetazolamide (tablets or via parenteral). Tablets or parenteral are used following the dose schedules with more frequency that are recommended for these dosage types, like 250 mg every 4 hours, an initial dose of 500 mg that is followed with 250 mg, or 125 mg once every four hours, according to the specific situation.

Acute mountain sickness

Dosage ranges from 500 mg to 1,000 mg per day, taken in divided doses by taking tablets or capsules that extend-release according to the need. If you are experiencing high altitude, like for rescue or military activities at high altitude, a dose higher than 1,000 mg is advised. It is recommended to begin doses 24 to 48 hours prior to ascent and continue them for a period of an additional 48 hours when at higher altitudes, or as long as it is necessary to manage symptoms.

What happens if I over dose?

A specific remedy is not available. Treatment must be both symptomatic and helpful. In the event of an electrolyte imbalance, an acidotic state as well as central nervous system reactions could be expected to develop. The levels of electrolytes in the blood (particularly potassium) as well as blood ph levels need to be closely monitored. In order to support the patient, it is essential to restore ph and electrolyte equilibrium. The acidotic condition can generally be resolved through the use of bicarbonate.

In spite of its extensive intraerythrocytic circulation and its plasma protein binding capabilities, acetazolamide is able to be dialyzed. This is particularly relevant for the treatment of an overdose of acetazolamide when it is accompanied by kidney failure.

Adverse Reactions/Side effects.

The whole body:

Headache, malaise, fatigue, fever, pain at the injection site, flushing, growth retardation in children, flaccid paralysis, anaphylaxis


Gastrointestinal disorders like vomiting, nausea, and diarrhoea


The blood dyscrasias include aplastic anaemia, agranulocytosis, or leukopenia, as well as thrombocytopenic purpura and melena.

Hepato-biliary disorders:

Anomaly in the liver hepatic necrosis of the liver and fulminant hepatic insufficiency


Electrolyte imbalance, metabolic acidosis such as hyponatremia, hypokalemia, and osteomalacia that is cured by prolonged phenytoin treatment, weight loss, changes in taste, or hyper/hypoglycemia


Paresthesia, drowsiness (including sensory numbness, tingling, and swelling of the face and extremities), as well as excitement, depression, and confusion convulsions or confusion; dizziness


Allergies to skin, including urticaria and stevens-johnson syndrome, chronic epidermal necrosis

Special senses:

Hearing disturbances, tinnitus, and transient myopia transient myopia results from the forward motion of the ciliary organ, leading to a decrease in the angle.


Crystalluria is associated with an increased likelihood of nephrolithiasis following prolonged therapy, hematuria, glycosuria, and renal failure polyuria.

For information on suspected adverse results, to report suspected adverse reactions, please contact chartwell rx, llc. At 1-845-232-1683 or the fda at 1-800-fda-1088 or

Process to make it available.

Acetazolamide extended release capsules 500 mg. Are white to off-white pellets packed inside empty capsules of hard gelatin with a transparent orange cap that is imprinted in black with "ep" in black ink and a white opaque body stamped in black with "107" in black ink and supplied in the following manner:

ndc 62135-612-60 is contained in a bottle of 60 capsules.

store at 20° to 25°c (68° to 77°f) [see usp controlled room temperature].
Make sure to store the liquid in tightly sealed containers that are well sealed.

Interaction with other Drugs.

Acetazolamide alters the metabolism of phenytoin, resulting in an increase in the levels of phenytoin in the serum. It may also increase the incidence of osteomalacia among patients taking chronic therapy with phenytoin. It is recommended to be cautious with patients who receive chronic therapy. In reducing the absorption by the stomach of pyrimidine, acetazolamide could reduce the serum levels of pyrimidine as well as its metabolites, resulting in a diminution of the effects of anticonvulsants. It is recommended to be cautious when beginning, stopping, or modifying the dosage of acetazolamide for patients taking pyrimidine. In light of the potential additive effect in the presence of other inhibitors of carbonic anhydrase, it isn't advised. Acetazolamide can increase the effect of other antagonists of folic acid. Acetazolamide lowers urinary excretion of amphetamine and can increase the intensity and duration of its effects. Acetazolamide decreases the urinary excretion of quinidine and can improve its effects. Acetazolamide could block the antiseptic effects of urine methylamine. Acetazolamide enhances the excretion of lithium, and lithium excretion may decrease. Acetazolamide and sodium bicarbonate taken together increase the chance of the formation of calculus in the kidney. Acetazolamide may elevate cyclosporine levels.

Tests for drug and laboratory test interactions

Sulfonamides may give false negative or decreased values for urinary phenolsulfonphthalein and phenol red elimination values for urinary protein, serum non-protein, and serum uric acid. Acetazolamide can cause an increase in the concentration of crystals in urine.

Acetazolamide is a problem with the hplc method for assaying theophylline. Theophylline testing is affected by acetazolamide, which varies based on the solvent utilized for extraction. Acetazolamide is not likely to interfere with different methods to measure theophylline.

Carcinogenesis, mutagenesis, and impairment of fertility

Studies on long-term effects in animals for evaluating the potential carcinogenicity of acetazolamide were not done. In a mutagenicity test on bacterial cells, it was found that acetazolamide is not mutagenic in the absence of metabolic activation.

The drug did not have any effect on fertility when it was administered to the diet of male and female rats with a daily dose of as much as four times the dosage of 1000 mg per 50 kg person.

Pregnancy and Teratogenicity Effects

Acetazolamide is a drug that can be administered parenteral or orally and is known to cause teratogenicity defects (defects of the legs) in rats, mice, hamsters, and rabbits. There is no evidence of adequate research studies that are well-controlled in pregnant women. Acetazolamide is recommended to be taken by pregnant women only if the benefits outweigh the risk for the fetus.

Nursing mothers

Given the risk of grave adverse reactions among infants who are nursing from acetazolamide, a decision must be made when deciding whether or not to stop nursing or stop using the drug based on the significance of the drug for the mother. Acetazolamide should only be used by mothers who nurse in cases where the possible benefit outweighs any risk that could be posed to the infant.

Pediatric use

The efficacy and safety of extended-release capsules containing acetazolamide in children under the age of 12 have not been proven. There have been reports of a slowing in growth for children who are receiving long-term therapy that is believed to be a result of chronic acidosis.

Geriatric use

Metabolic acidosis, which can be very severe, is a possibility among the elderly with diminished kidney function.

The general rule is that the selection of doses in the elderly patient needs to be considered with caution, typically starting in the lower limit of dosing due to the higher incidence of diminished hepatic or renal functioning as well as the concomitant illness or other treatment.

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