What is Acetazolamide tablet?
Acetazolamide, which is an inhibitor of carbonic anhydrase, it is a pale to light yellowish-white crystal with no odor. Powder that is weakly acidic, somewhat water-soluble, and moderately 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: Molecular weight: 222.25
Molecular formula: c4h6n4o3s2 Acetazolamide comes in oral tablets that contain 250 mg and 125 mg of acetazolamide, along with the following inactive ingredients: lactose, corn starch monohydrate, magnesium stearate, providence, and sodium starch glycol ate.
There have been fatalities, but rarely, they are due to serious reactions to sulfonamides such as stevens-johnson syndrome, toxic epidermal necrolysis and agranulocytosis, fulminant hepatic necrosis, or aplastic anemia. Various blood dyscrasias and anaphylaxis the sensitivity may return when the drug is administered again, regardless of the method of administration. If hypersensitivity symptoms or other severe reactions are observed, then stop taking this medication. It is recommended to be cautious for those who are taking high-dose aspirin in conjunction with acetazolamide, as symptoms such as anorexia dysphonia, lurgy metabolic acidosis, coma, and even death have been reported.
Before you take this drug Acetazolamide tablets
Acetazolamide is a powerful carbonic anhydrase inhibitor that is effective in regulating fluid production (e.g., various kinds of glaucoma), treating specific convulsive disorders (e.g., epilepsy), and promoting diuresis when there is irregular fluid retention (e.g., heart edema). Acetazolamide isn't a mercurial diuretic. It is, instead, an bacteriostatic sulfonamide with a chemical structure and pharmacological function that are distinct from the bacteriostatic sulfonamides. Acetazolamide is a steroid inhibitor that specifically affects carbonic anhydrase. It is the enzyme responsible for triggering an irreversible reaction involving the reduction of carbon dioxide as well as the breakdown of carbonic acid. The eye is the target for the acetazolamide inhibitory effect, which reduces the production of aqueous humor. This results in a decrease in intraocular pressure. This is an action that is believed to be desirable in the case of glaucoma or even in some no glaucomatous diseases. The evidence suggests that acetazolamide can be used as an adjuvant to treat specific dysfunctions of the nervous system (e.g., epilepsy). Its inhibition of carbonic acid hydras in this region appears to slow down the abnormal paroxysmal and excessive discharge from central nervous neurons. Acetazolamide's diuretic action results from its actions in the kidney, which is a reversed reaction that involves the hydration of carbon dioxide and the dehydration process of carbonic acid. It results in the elimination of the hco3 ion, which is the one that carries sodium, water, and potassium. The alkalization of urine and diuresis promotion is impaired. Ammonia metabolism is altered because of increased reabsorption of ammonia in the kidney tubules due to the effect of urinary alkalization.
Studies conducted under controlled clinical trials with placebo have proven the prophylactic use of acetazolamide with a dosage of 250 mg once every 8 to 12 hours (or 500 mg in a capsule with controlled release once a day) in the early and middle stages of an ascent that is rapid results in less or no symptoms (such as nausea, headache, shortness of breath, dizziness, as well as fatigue) associated with chronic mountain sickness (ams). The function of the lungs (e.g., minutes of ventilation, expiring vital capacity, as well as peak flow) is higher when acetazolamide is treated, as well as in those with ams as well as asymptomatic patients. Also, climbers treated with acetazolamide had less trouble sleeping.
How to use Acetazolamide tablets?
To treat swelling due to congestive heart failure, drug-induced edema, epilepsies centerencephalic (petit mal, non-localized seizures), persistent simple (open-angle) eye glaucoma, and secondary glaucoma, as well as preoperatively in acute angle-closure glaucoma when delays in surgery are desired for the purpose of lowering the pressure in the eye. Acetazolamide tablets can also be used to prevent or ease the symptoms of acute mountain sickness among those who attempt to climb quickly and for those particularly at risk of developing acute mountain sickness despite slow climbs.
Hypersensitivity to acetazolamide or other excipients that are in the formulation. Because acetazolamide can be a sulfonamide derivative, cross-sensitivity to acetazolamide and sulfonamides, as well as sulfonamide derivatives, can be feasible. Acetazolamide therapy isn't recommended for circumstances where sodium or potassium levels in blood serum are impaired, for instance, in cases that show liver or kidney impairment or disease, suprarenal gland insufficiency, or hyperchloremic acidosis. It's not advised for those suffering from cirrhosis due to the potential for the development of hepatic encephalopathy. Acetazolamide long-term use isn't recommended in people with chronic non-congestive angle-closure glaucoma as it can cause the organic closing of the angle as the worsening of glaucoma gets concealed by decreased intraocular pressure.
Adverse reactions/side effects
All body parts as a whole: headache, malaise, discomfort, fatigue, and flushing at the injection site. Growth slowdown in children, flaccid paralysis, as well as anaphylaxis. Digestive and gastrointestinal issues, including nausea, vomiting, and diarrhea,
Haematological/lymphatic: blood dyscrasias such as aplastic anaemia, agranulocytosis, leukopenia, thrombocytopenia, thrombocytopenic purpura, melena
Hepatobiliary disorders: atypical performance of the liver, jaundiced liver insufficiency, severe hepatic necrosis
Metabolic/nutritional: metabolic acidosis, electrolyte imbalance, including hypokalemia and hypernatremia, osteomalacia with long-term phenytoin therapy, loss of appetite, taste alteration, hyper/hypoglycemia
Nervous: paraesthesia, drowsiness (including a sense of numbness or tingling in the fingers and the face), depression, and confusion dizziness, convulsions
Skin: allergic skin reactions such as photosensitivity, urticarial, stevens-johnson syndrome, and toxic epidermal necrosis
Special senses: hearing disturbances, tinnitus, and transient myopia myopia that is transient occurs as a result of the forward motion of the ciliary organ, leading to the narrowing of the angle.
Urogenital: crystalluria, an increase in likelihood of nephrolithiasis following long-term treatment, hematuria, glycosuria, and renal failure polyuria
Details on dosage.
The glaucoma acetazolamide is recommended in addition to regular treatment. The dosage used in the treatment of simple (open-angle) glaucoma can range from 250 mg up to 5 grams of acetazolamide every 24 hours. Typically, it is in portions for doses greater than 250 mg. It is generally observed that dosages greater than 1 g/24 hours are not a cause for an enhanced result. It is recommended that the dosage be adjusted with particular attention to the symptomatology as well as ocular tension. Continuous supervision from a physician is highly recommended.
For treatment of secondary glaucoma and for the initial treatment of some instances of acutely congestive (closed-angle) eye disease the recommended dosage is 250 mg per hour for 4 hours. However, some cases have shown improvement with 250 mg twice daily for short-term treatments. In certain acute situations, it is beneficial to give an initial dose of 500 mg, followed by either 125 mg or 250 mg once every 4 hours based on the specific situation. The effect of this is observed when acetazolamide is utilized together with meiotic or mydriatics, as required by the situation.
Epilepsy: it's not known for certain if the positive results observed during epilepsy stem from directly inhibiting carbonic anhydrase within the central nervous system or whether they result from the minor amount of acidosis resulting from the dosage divided. Most of the best results have been observed in children with pediatric disorders. Positive results are seen for patients of all ages, adults and pediatrics, with other kinds of seizures like grand malls, mixed seizures, myoclonic jerk patterns, and so on. The daily recommended dose is between 8 and 30 mg/kg, divided into doses. While some patients may respond well to doses that are low, the most effective range seems to be 375–1000 mg per day. Some researchers believe that doses daily in excess of 1 g will not yield superior results to a single gram dosage. If acetazolamide tablets were to be used along with other anticonvulsants, it is recommended to start with a dose of 250 mg daily along with the other medication. The dosage can be increased to the levels indicated in the previous paragraph.
The switch from different medications to acetazolamide must be gradual and consistent with the normal practice of treatment for epilepsy.
Congestive heart failure in the case of diuresis that is caused by chronic heart failure (congestive), the initial dose usually ranges from 250 to 500 mg every day in the early morning (5 mg/kg). After a first reaction, if the patient is unable to stop losing fluid from edema, do not raise the dosage but wait for the kidney to recover by avoiding medications for the duration of the day.
Acetazolamide tablets provide the best diuretic benefits when used over a series of days or over two consecutive days with rest days.
The reason for failures in therapy is over dosage, or taking a dose too often. Acetazolamide therapy doesn't eliminate the need to seek out other therapies such as bed rest, digitalis, and salt reduction.
For oedema caused by drugs, the recommended dose ranges from 250–375 mg of acetazolamide every day for a period of one to two days. Then, alternate with the day off.
The most common form of acute mountain sickness is the dosage ranges from 500 mg to 1000 mg per day in divided doses by taking tablets or capsules that sustain release according to the need. If you are experiencing fast ascents, for example, for rescue or military activities, it is recommended to use a higher dose of 1000 mg. It is recommended to begin dosages between 24 and 24 hours before ascending and then continue to do so for up to 48 hours in high altitude, or as long as is necessary to manage the symptoms.
Be aware that the dosage guidelines for epilepsy and glaucoma differ significantly from the recommendations for congestive heart failure because the two first conditions aren't dependent on carbonic anhydrase inhibitors in the kidneys, which require intermittent doses in order to recuperate from the inhibitory effects of the drug.
Interference with laboratory tests
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 could cause an increased amount of crystals in the urine.
Acetazolamide hinders the hplc method for assaying theophylline. Theophylline testing is affected by acetazolamide, which varies based on the solvent employed during extraction. Acetazolamide does not affect different methods to measure theophylline.
What happens if I over dose?
There is no specific treatment for this. The treatment should be supportive. In the event of an imbalance in electrolytes, an acidotic state and central nervous reactions could be expected to develop. The levels of electrolytes in the blood (particularly potassium) as well as blood ph levels need to be checked regularly. It is essential to take supportive measures to restore electrolyte levels and ph equilibrium. The acidotic condition can generally be rectified by the administration of bicarbonate. Despite its intraerythrocytic concentration and plasma protein binding capabilities, acetazolamide is dialyzable. This can be especially important when it comes to managing the overdose of acetazolamide caused by kidney failure.
What should be avoided while taking this medication
The dose increase does make it less diurnal and can increase the likelihood of paresthesia and/or drowsiness. The increase in dose usually results in a reduction in diuresis. However, in certain instances, extremely large doses are administered in conjunction with diuretics to ensure diuresis even in failure due to refractory disease.
Information for patients
Common adverse reactions to any sulfonamide derivative can occur with fever, anaphylaxis, and eruptions (including stevens-johnson syndrome toxic epidermal neurolysis), as well as crystalluria, bone marrow degeneration, thrombocytopenic purpura anaemia, leukopenia and pancytopenia, and agranulocytosis. It is recommended to be cautious for the rapid detection of these reactions, and the medication should be withdrawn and a suitable treatment implemented. Patients suffering from an obstruction to the lungs or emphysema in which breathing is impaired acetazolamide, which could cause acidosis to worsen or increase, must be used with care. It is advisable to gradually ascend in order to avoid severe mountain sickness. If rapid ascents are planned with acetazolamide tablets, however, be aware that this will not eliminate the need to descend quickly if serious types of high altitude sickness happen, for example, high altitude-related pulmonary edema (hape) and high-altitude cerebral edema. It is recommended to be cautious for those who are taking high-dose aspirin in conjunction with acetazolamide because anorexia, thetahypnea, fatigue, metabolic acidosis, coma, and death have all been observed (see the warnings).
Increases and decreases in blood sugar levels have been observed when patients are treated with acetazolamide. This is something to take into account for patients suffering from an impaired tolerance to glucose or with diabetes mellitus. Acetazolamide treatment can trigger the imbalance of electrolytes to cause hypokalemia, hypernatremia, and metabolic acidosis. So, a regular check of the electrolytes in the serum is suggested. It is especially important to be cautious for patients suffering from conditions that are a result of or may predispose patients to electrolyte or acid-base imbalances. This includes those suffering from impairments in kidney function (including older patients; refer to precautions, geriatric use), patients suffering from diabetes mellitus, and those who suffer from impaired alveolar circulation.Certain adverse reactions associated with acetazolamide can cause fatigue, drowsiness, or myopia, which can hinder the ability to operate and drive. Use machines.
For monitoring for reactions of a hematologic nature that are common to all sulfonamides, it is suggested that the baseline cbc and count of platelets be taken from patients prior to starting the acetazolamide tablets and every few weeks during treatment. If changes are observed that cause concern, rapid discontinuation and the implementation of the appropriate treatment are crucial. Regular monitoring of electrolytes in serum is suggested.
Interaction with other drugs
Acetazolamide tablets affect the metabolism of phenytoin by increasing serum levels of phenytoin. It may also increase or exacerbate osteomalacia's incidence in certain patients who are receiving long-term phenytoin treatment. It is recommended to be cautious with patients who receive chronic therapy in conjunction with it. By reducing the absorption by the gastrointestinal tract of pyrimidine, acetazolamide can reduce the serum levels of pyrimidine as well as its metabolites. There is a possible reduction in its anticonvulsant properties. It is recommended to be cautious when starting, stopping, resuming, or altering the dosage of acetazolamide given to those taking pyrimidine. Due to the possibility of additive effects in the presence of other inhibitors of carbonic anhydrase, it isn't recommended. Acetazolamide could increase the effectiveness of other folic acid antagonists. Acetazolamide could increase or decrease the levels of blood glucose. It is important to consider this for patients who receive antidiuretic medications. Acetazolamide lowers the excretion of amphetamine in urine. It can also increase the duration and intensity of the effects. Acetazolamide decreases the urinary excretion of quinidine. It may also increase its effectiveness. Acetazolamide could block the effect of urinary antiseptic methylamine. Acetazolamide enhances the excretion of lithium, and it is possible that the lithium level will diminish. Acetazolamide in combination with sodium bicarbonate increases the chance of the formation of calculi in the kidney. Acetazolamide may elevate cyclosporine levels.
Carcinogenesis, mutagenesis, and impairment of fertility
Studies on long-term effects in animals for evaluating the potential carcinogenicity of acetazolamide have not been done. A bacterial mutagenicity test was conducted, and acetazolamide wasn't mutagenic in the absence of metabolic activation. The drug was not a factor in fertility when given in the diet to male as well as female rats, with a dose of as much as four times the dosage for humans of 1000 mg for a 50-kg person.
Pregnancy: teratogenicity effect
Acetazolamide, which is administered either by mouth or via parenteral injection, has been proven to cause teratogenic defects (defects of the legs) in rodents, mice, hamsters, and rabbits. There is no evidence of adequate research studies that are well-controlled in pregnant women. Acetazolamide should be considered for pregnant women only if the benefits outweigh the risk for the fetus.
Due to the possibility of severe adverse reactions for infants who are nursing from acetazolamide, it is necessary to decide whether or not to stop nursing or discontinue use of the medication, taking into consideration the significance of the drug for the mother. Acetazolamide is not recommended by women who are nursing when the benefits of using it outweigh the risk for the baby.
The efficacy and safety of acetazolamide among children haven't been proven.
Growing retardation has been observed in children receiving long-term therapies, which is believed to be a result of chronic acidosis.
Metabolic acidosis, which can be serious, can occur among the elderly with diminished kidney function.
The clinical studies on acetazolamide didn't include enough numbers of patients aged 65 or over to know if they react differently to it than younger patients. Some other reported experiences have revealed no difference in the response among older and younger patients. It is generally recommended that dose selection in an older patient be taken with caution, typically starting with the lowest part of the range for dosing, which is indicative of the more frequent occurrence of diminished renal, hepatic, or cardiac function as well as concomitant illness or other treatment.
How are acetazolamide tablets delivered?
Acetazolamide tablets usp 100 mg are round, white, or off-white with a flat face, a beveled edge, and uncoated tablets that have a break line on one side and are embossed with 1238 on the opposite side. The tablets are shipped with the following information:
Ndc 70771-1827-1 is contained in a 100-tablet bottle with a child-proof closure.
Acetazolamide tablets usp 250 mg are round, white or off-white, and flat-faced, with a beveled edge and a quadrisect break line on one side and embossed with '1239' on the other, and supplied with the following information:
Ndc 70771-1828-1 is contained in a bottle of 100 tablets with a child-resistant seal.
Store at 20° to 25°c (68° to 77°f) [see usp controlled room temperature].