What conditions does acetazolamide treat?
Acetazolamide is a prescription medication used to treat the symptoms of Glaucoma, Acute Altitude Sickness, Congestive Heart Failure, Seizure, Drug-induced Edema, and Epilepsy. Learn about side effects, dosages, interactions, and warnings.
What is the purpose of acetazolamide?
Acetazolamide is a carbonic anhydrase (CA) inhibitor sometimes used as a respiratory stimulant for patients with chronic obstructive pulmonary disease (COPD) with the goal of improving oxygenation, reducing carbon dioxide retention, and aiding liberation from mechanical ventilation and/or attempting to correct a metabolic alkalosis.
What is acetazolamide used for?
What is Acetazolamide and how is it used? Acetazolamide is a prescription medicine used to treat the symptoms of Epilepsy, seizures, drug-induced Edema, acute altitude sickness, and Glaucoma. Acetazolamide may be used alone or with other medications.
Is acetazolamide a diuretic?
Acetazolamide is in the diuretic and carbonic anhydrase inhibitor families of medication. It works by decreasing the formation of hydrogen ions and bicarbonate from carbon dioxide and water. Acetazolamide came into medical use in 1952. It is on the World Health Organization's List of Essential Medicines.
What is the main function of acetazolamide?
Acetazolamide is used to treat glaucoma, a condition in which increased pressure in the eye can lead to gradual loss of vision. Acetazolamide decreases the pressure in the eye.
How does acetazolamide work as a diuretic?
a potent carbonic anhydrase inhibitor. The diuretic effect of acetazolamide is due to its action in the kidney on the reversible reaction involving hydration of carbon dioxide and dehydration of carbonic acid. The result is renal loss of bicarbonate (HCO3 ion), which carries out sodium, water, and potassium.
What type of diuretic is acetazolamide?
Acetazolamide is the only carbonic anhydrase inhibitor with significant diuretic effects. It is readily absorbed and undergoes renal elimination by tubular secretion. Its administration is ordinarily marked by a brisk alkaline diuresis.
What is the mechanism of action of carbonic anhydrase?
Mechanism of Action The intracellular carbonic anhydrase enzyme converts water and carbon dioxide back to carbonic acid, which dissociates into H+ and bicarbonate.
How does acetazolamide lower potassium?
Carbonic anhydrase inhibitors, such as acetazolamide, decrease proximal tubular reabsorption of HCO3− in the kidneys by noncompetitive inhibition of luminal and cellular carbonic anhydrase. Hypokalemia is caused by increased sodium delivery to the distal nephron and its reabsorption there in exchange for potassium.
Why acetazolamide is a weak diuretic?
Carbonic anhydrase inhibitors. Carbonic anhydrase inhibitors such as acetazolamide (Diamox) are weak diuretics. They decrease the secretion of hydrogen ions by the proximal renal tubule, with increased loss of bicarbonate and hence of sodium.
What is the most severe adverse effect of acetazolamide?
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
What is another name for acetazolamide?
Acetazolamide (Brand Name: Diamox) is a "water pill" (diuretic) used to prevent and reduce the symptoms of altitude sickness. Acetazolamide is also used with other medications to treat a certain type of eye problem (open-angle glaucoma).
What drug class is acetazolamide?
Acetazolamide belongs to a class of drugs called Anticonvulsants, Other; Antiglaucoma, Carbonic Anhydrase Inhibitors.
Does acetazolamide lower blood pressure?
Acetazolamide showed a clear orthostatic effect by significantly decreasing the standing systolic blood pressure (BP), while propranolol, at the doses used, had no obvious reducing effect on BP.
How quickly does acetazolamide work?
It's often used along with other antiseizure medications. How long does acetazolamide take to work? The immediate-release pills can work within 1 to 2 hours. The extended-release pills are released more slowly in the body than the immediate-release pills.
Who should not use acetazolamide?
Before taking this medicine You should not use acetazolamide if you are allergic to it, or if you have: severe liver disease, or cirrhosis; severe kidney disease; an electrolyte imbalance (such as acidosis or low levels of potassium or sodium in your blood);
How quickly does acetazolamide work?
It's often used along with other antiseizure medications. How long does acetazolamide take to work? The immediate-release pills can work within 1 to 2 hours. The extended-release pills are released more slowly in the body than the immediate-release pills.
What is the most severe adverse effect of acetazolamide?
A very serious allergic reaction to this drug is rare. However, get medical help right away if you notice any symptoms of a serious allergic reaction, including: rash, itching/swelling (especially of the face/tongue/throat), severe dizziness, trouble breathing.
Where does acetazolamide work in the nephron?
Carbonic anhydrase is found in the proximal tubule of the nephron and red blood cells. It works to reabsorb sodium, bicarbonate, and chloride. Once acetazolamide inhibits carbonic anhydrase, sodium, bicarbonate, and chloride get excreted rather than reabsorbed; this also leads to the excretion of excess water.
Is acetazolamide a loop diuretic?
Carbonic anhydrase inhibitor Acetazolamide has been used in HF patients with edema and metabolic alkalosis, where the increased proximal tubular reabsorption of sodium results in decreased distal sodium delivery, hence rendering loop diuretics ineffective.
What is acetazolamide used for?
Acetazolamide, a potent carbonic anhydrase (CA) inhibitor, is the most commonly used and best-studied agent for the amelioration of acute mountain sickness (AMS).
Does acetazolamide cause bicarbonaturia?
Traditionally, acetazolamide's efficacy has been attributed to inhibition of CA in the kidneys, resulting in bicarbonaturia and metabolic acidosis. The result is offsetting hyperventilation-induced respiratory alkalosis and allowance of chemoreceptors to respond more fully to hypoxic stimuli at altitude.
Is acetazolamide a CA inhibitor?
Traditionally, acetazolamide's efficacy ha …. Acetazolamide, a potent carbonic anhydrase (CA) inhibitor, is the most commonly used and best-studied agent for the amelioration of acute mountain sickness (AMS). The actual mechanisms by which acetazolamide reduces symptoms of AMS, however, remain unclear. Traditionally, acetazolamide's efficacy ha ….
What is acetazolamide used for?
Acetazolamide is a diuretic and carbonic anhydrase inhibitor medication that is used to treat several illnesses. [1]
How does acetazolamide help with glaucoma?
Acetazolamide is a classic treatment option for glaucoma as it causes a reduction in the aqueous humor. As well, it is useful for the treatment of altitude sickness, because of its underlying mechanism of action. The medication works to excrete bicarbonate. By doing so, it alkalizes the urine as there is greater bicarbonate in the urine. As a result, the blood is more acidic, given that the bicarbonate has been excreted out. Some mechanisms equate the carbon dioxide concentrations in the body to the degree of acidity, resulting in an artificial compensatory mechanism to what the body believes to be excess carbon dioxide. This compensation results in faster and deeper breathing. The outcome of that is higher concentrations of oxygen in the body, which improves the ability of the body to adjust itself to the higher altitude levels. [3]
Is acetazolamide a diuretic?
Acetazolamide is a diuretic and carbonic anhydrase inhibitor medication that is used to treat several illnesses. FDA-approved indications include glaucoma, idiopathic intracranial hypertension, congestive heart failure, altitude sickness, periodic paralysis, and epilepsy. This activity outlines the indications, contraindications, interactions, monitoring, and other therapeutic information pertinent to members of an interprofessional team in the care of patients with conditions requiring the use of acetazolamide.
Can you take acetazolamide with food?
Patients take acetazolamide with or without food, and the patient should drink plenty of fluids with the medication. Available dosages are 125 mg, 250 mg, and 500 mg tablets.[5] These are also available in instant-release and extended-release drug dosage forms.
Can acetazolamide cause hypokalemia?
Acetazolamide can induce electrolyte abnormalities. As such, those with hypokalemia or hyponatremia should not use it. Similarly, it can decrease kidney function, and clinicians should avoid using it with anyone with kidney disease or decreased kidney function.
Can you take acetazolamide with hyperchloremic acidosis?
Patients with hyperchloremic acidosis should not use acetazolamide. [9]
Does acetazolamide cause acidic blood?
Acetazolamide is a carbonic anhydrase inhibitor. That means this drug works to cause an accumulation of carbonic acid by preventing its breakdown. The result is lower blood pH (i.e., more acidic), given the increased carbonic acid, which has a reversible reaction into bicarbonate and a hydrogen ion.
What is acetazolamide used for?
It has also been used in the treatment of altitude sickness, Ménière's disease, increased intracranial pressure and neuromuscular disorders. In epilepsy, the main use of acetazolamide is in menstrual-related epilepsy and as an add on to other treatments in refractory epilepsy.
What is the effect of acetazolamide on blood pH?
Carbonic anhydrase is an enzyme found in red blood cells and many other tissues that catalyses the following reaction: hence lowering blood pH, by means of the following reaction that carbonic acid undergoes: which has a pK a of 6.3.
What enzyme is responsible for reabsorption of sodium and chloride?
The enzyme carbonic anhydrase is found here, allowing the reabsorption of bicarbonate, sodium, and chloride. By inhibiting this enzyme, these ions are excreted, along with excess water, lowering blood pressure, intracranial pressure, and intraocular pressure.
Is acetazolamide a diuretic?
Common side effects include numbness, ringing in the ears, loss of appetite, vomiting, and sleepiness. It is not recommended in those with significant kidney problems, liver problems, or who are allergic to sulfonamides. Acetazolamide is in the diuretic and carbonic anhydrase inhibitor families of medication.
Is acetazolamide safe for pregnancy?
Pregnancy and lactation. Acetazolamide is pregnancy category B3 in Australia, which means that studies in rats, mice and rabbits in which acetazola mide was given intravenously or orally caused an increased risk of fetal malformations, including defects of the limbs.
Can acetazolamide be used for dural ectasia?
Though various websites on the internet report that acetazolamide can be used to treat dural ectasia in individuals with Marfan Syndrome, the only supporting evidence for this assertion exists from a small study of 14 patients which was not peer-reviewed or submitted for publication.
Does acetazolamide cause liver disease?
Marked liver disease or impairment of liver function, including cirrhosis because of the risk of development of hepatic encep halopathy. Acetazolamide decreases ammonia clearance.
What is the hypersensitivity to acetazolamide?
Hypersensitivity to acetazolamide, sulfonamides, or any component of the formulation; marked hepatic disease or insufficiency; decreased sodium and/or potassium levels; adrenocortical insufficiency; cirrhosis; hyperchloremic acidosis; severe renal disease or dysfunction; long-term use in noncongestive angle-closure glaucoma
What enzyme is inhibited by reversible inhibition?
Reversible inhibition of the enzyme carbonic anhydrase resulting in reduction of hydrogen ion secretion at renal tubule and an increased renal excretion of sodium, potassium, bicarbonate, and water. Decreases production of aqueous humor and inhibits carbonic anhydrase in central nervous system to retard abnormal and excessive discharge ...
Does acetazolamide help with hypokalemic paralysis?
Familial periodic paralysisc. Limited data from controlled trials and case reports suggest that acetazolamide may have some benefits in the treatment of hypokalemic and hyperkalemic periodic paralysis. Studies have shown that acetazolamide improves muscle strength in patients with hypokalemic periodic paralysis.
Does acetazolamide help with urinary alkalinization?
Data from a limited number of patients in a retrospective review suggest that acetazolamide may have some benefits as adjunctive therapy for urinary alkalinization in the prevention of cystine renal calculi formation in patients who are recalcitrant to potassium citrate therapy.
Does acetazolamide help with gait?
Data from a limited number of patients in a retrospective review suggest that low-dose acetazolamide can reduce periventricular hyperintensities leading to gait improvement in patients with normal pressure hydrocephalus Alperin 2014. Additional data may be necessary to further define the role of acetazolamide in this condition.
Is sulfonamide contraindicated?
Note: Although the FDA approved product labeling states this medication is contraindicated with other sulfonamide-containing drug classes, the scientific basis of this statement has been challenged. See “Warnings/Precautions” for more detail.
Is acetazolamide a stimulant?
Data from a randomized, double-blind, crossover study supports the use of acetazolamide as a respiratory stimulant in the treatment of stable hypercapnic COPD Wagenaar 2003. Additional trials may be necessary to further define the role of acetazolamide in this condition.
What is thiadiazole sulfonamide?
This compound belongs to the class of organic compounds known as thiadiazole sulfonamides. These are heterocyclic compounds containing a thiazole ring substituted by at least one sulfonamide group.
What is the name of the enzyme that is used to treat edema?
Enzymes (1) Transporters (1) Acetazolamide. Identification. Summary. Acetazolamideis a carbonic anhydrase inhibitor used to treat edema from heart failure or medications, certain types of epilepsy, and glaucoma. Generic Name.
Is carbonic anhydrase inhibitor effective against absence seizures?
One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle.
Is carbonic anhydrase inhibitor effective?
One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. It is sometimes useful also as an adjunct in the treatment of tonic-clonic, myoclonic, and atonic seizures, particularly in women whose seizures occur or are exacerbated at specific times in the menstrual cycle. However, its usefulness is transient often because of rapid development of tolerance. Its antiepileptic effect may be due to its inhibitory effect on brain carbonic anhydrase, which leads to an increased transneuronal chloride gradient, increased chloride current, and increased inhibition. (From Smith and Reynard, Textbook of Pharmacology, 1991, p337)
Is acetazolamide a mercurial diuretic?
Acetazolamide is not a mercurial diuretic.
Does acetazolamide increase potassium perchlorate?
Potassium perchlorate. Acetazolamide may increase the excretion rate of Potassium perchlorate which could result in a lower serum level and potentially a reduction in efficacy. Potassium sulfate. The risk or severity of adverse effects can be increased when Acetazolamide is combined with Potassium sulfate.
Does acetazolamide lower potassium cation?
Acetazolamide may increase the excretion rate of Potassium cation which could result in a lower serum level and potentially a re duction in efficacy. Potassium chloride. Acetazolamide may increase the excretion rate of Po tassium chloride which could result in a lower serum level and potentially a re duction in efficacy.
What is acetazolamide?
Acetazolamide reduces the activity of a protein in your body called carbonic anhydrase. Blocking this protein can help reduce the build-up of certain fluids in the body.
What are the side effects of acetazolamide?
Acetazolamide side effects. Get emergency medical help if you have signs of an allergic reaction: hives; difficult breathing; swelling of your face, lips, tongue, or throat. Call your doctor at once if you have: blood in urine or stools; a seizure (convulsions); loss of movement in any part of your body;
What should I avoid while taking acetazolamide?
acetazolamide may impair your thinking or reactions. Be careful if you drive or do anything that requires you to be alert.
Can you skip acetazolamide?
Your dose of this medicine will depend on the condition you are treating. If you take acetazolamide for congestive heart failure, your doctor may tell you to skip your medication for a day. Follow your doctor's dosing instructions very carefully. Take this medicine with a full glass of water.
Is acetazolamide a complete treatment?
Acetazolamide may be only part of a complete treatment program that may also include other medications. Follow your doctor's instructions very closely.
Can you take acetazolamide if you have cirrhosis?
You should not use acetazolamide if you have cirrhosis, severe liver or kidney disease, an electrolyte imbalance, adrenal gland failure, or an allergy to acetazolamide or sulfa drugs.
Can acetazolamide be taken with other medications?
Other drugs may interact with acetazolamide, including prescription and over-the- counter medicines, vitamins, and herbal products. Tell each of your health care providers about all medicines you use now and any medicine you start or stop using.
What is sulfonamide derivative?
It is a sulfonamide derivative of carbonic anhydrase enzyme inhibitor. It exerts it`s diuretic, anti glaucomal, anti convulsant, anti altitude sickness actions by non competitively and reversibly inhibiting carbonic anhydrase in renal proximal tubules, ciliary body of eye, brain, lungs and tissues etc.#N#Diuretic action: The inhibition of carbonic anhydrase at proximal renal tubules resulting in slowing of hydration of carbon dioxide which leads to decreased availability of H+ to exchange with luminal sodium. Inhibition of brush border carbonic anhydrase retards dehydration of carbonic acid in the tubular fluid so that less carbon dioxide diffuses back in to the cells. Thus inhibits bicarbonate and Na+ reabsorption in proximal tubules. It also inhibits secretion of H+ in collecting duct and distal tubule. K+ is also lost in excess due to Na+ exchange in distal tubule takes place only with potassium. The drug promotes excretion of bicarbonate, sodium, potassium and water.#N#Anti glaucomal action: By inhibiting carbonic anhydrase in ciliary body of eye it reduces aqueous formation by limiting generation of bicarbonate in the ciliary epithelium lowers intraocular tension.#N#Anticonvulsant action: By inhibiting carbonic anhydrase in the brain it increases the carbon dioxide levels in brain which leads to increased acidity and raising seizure threshold.#N#Vertigo: Diuretics are used in vertigo in assumption that vertigo is due to endolymphatic hydrops. They reduce labyrinthine fluid pressure.#N#Anti altitude sickness agent: It shortens the period of high altitude acclimatization by preventing conversion of carbon dioxide in to bicarbonate it increase carbon dioxide tension in tissues and decreases it in lungs
What is the difference between metabolization and absorption?
Absorption: Well absorbed orally, Distribution: Widely distributed in to the body tissues. Metabolism: Not metabolized in the body. Excretion: Excreted unchanged in urine.
How to treat acidosis?
Treatment is supportive and symptomatic. Drug is removed by induced emesis or gastric lavage. Monitor & support serum electrolyte level and blood acidosis. Acidotic state can be corrected by administration of bicarbonate. Perform dialysis if required in conditions such as renal failure.
Is acetazolamide a generic?
Acetazolamide is a generic medicine name and there are several brands available for it. Some of the brands for acetazolamide might be better known than acetazolamide itself. If the pharmacy that's willing to deliver medicines to your home doesn't have acetazolamide in stock, you can ask for one of the branded alternatives for acetazolamide.
Does India sell acetazolamide?
Medicine India is just a publishing medium for medicine related information and does not provide services or sales of medicines including acetazolamide.
Can you take acetazolamide without a prescription?
Please be aware that you should take acetazolamide only if a doctor has recommended or prescribed it. Some or all pharmacies who provide a home delivery service for medicines might insist on a prescription for acetazolamide before they complete the sale. You can get this information while placing the order for acetazolamide with the pharmacy.
Overview
Mechanism of action
Acetazolamide is a carbonic anhydrase inhibitor, hence causing the accumulation of carbonic acid. Carbonic anhydrase is an enzyme found in red blood cells and many other tissues that catalyses the following reaction:
H2CO3 ⇌ H2O + CO2
hence lowering blood pH, by means of the following reaction that carbonic aci…
Medical uses
It is used in the treatment of glaucoma, drug-induced edema, heart failure-induced edema, epilepsy and in reducing intraocular pressure after surgery. It has also been used in the treatment of altitude sickness, Ménière's disease, increased intracranial pressure and neuromuscular disorders.
In epilepsy, the main use of acetazolamide is in menstrual-related epilepsy and as an add on to other treatments in refractory epilepsy. Though various websites on the internet report that acet…
Side effects
Common adverse effects of acetazolamide include the following: paraesthesia, fatigue, drowsiness, depression, decreased libido, bitter or metallic taste, nausea, vomiting, abdominal cramps, diarrhea, black stool, polyuria, kidney stones, metabolic acidosis and electrolyte changes (hypokalemia, hyponatremia). Whereas less common adverse effects include Stevens–Johnson syndrome, anaphylaxis and blood dyscrasias.
Interactions
It is possible that it might interact with:
• Amphetamines, because it increases the pH of the renal tubular urine, hence reducing the clearance of amphetamines.
• Other carbonic anhydrase inhibitors — potential for additive inhibitory effects on carbonic anhydrase and hence potential for toxicity.
History
An early description of this compound (as 2-acetylamino-1,3,4-thiadiazole-5-sulfonamide) and its synthesis has been patented.
Research
Smaller clinical trials have also shown promising results in the treatment of normal pressure hydrocephalus (NPH).
External links
• "Acetazolamide". Drug Information Portal. U.S. National Library of Medicine.