(pharmacology) (CH3CONH)C2N2S(SO2NH2) An odorless, white to faintly yellowish-white, crystalline powder with a melting point of 258°C; slightly soluble in water; used as a diuretic.
Acetazolamide
| Sci-Tech Dictionary: acetazolamide |
(′as·ə·tə′zäl·ə′mīd)
| 5min Related Video: Acetazolamide |
|
Neurological Disorder:
Acetazolamide |
Definition
Acetazolamide (a-set-a-ZOLE-a-mide) is a carbonic anhydrase inhibitor. Carbonic anhydrase is an enzyme that shifts the rate of reaction to favor the conversion of carbon dioxide and water into carbonic acid, bicarbonate ions, and free protons. Carbonic anhydrase activity is key to the regulation of pH and fluid balance in many different reactions throughout the body.
Fluid buildup can alter the shape of the eye and cause pressure on the optic nerve. Clinically, this condition is described as glaucoma. Inhibition of the enzymatic work of carbonic anhydrase activity (e.g., through the action of a carbonic anhydrase inhibitor) can lower fluid pressure in the eye.
Purpose
Acetazolamide is used to treat a number of disorders, including the control of epileptic seizures in those individuals who suffer epilepsy.
Acetazolamide is also used to treat non-neurological disorders such as glaucoma (acetazolamide decreases pressure in the eye), and to reduce the symptoms of edema (an excess storage of water by the body that leads to localized swelling or puffiness) and altitude sickness.
Description
Acetazolamide is prescription medication and is available only with a licensed physician's prescription. Acetazolamide is available in oral form in extended release capsules and tablets. Acetazolamide can also be administered by injection.
Recommended dosage
For both adults and children the recommended dosage for use in epilepsy cases is based upon actual body weight. In all cases, the exact dosage is determined by an experienced physician and/or pharmacist. In the most common cases, the normal recommended dosage is 4.5 mg per pound of body weight (10 mg per kg of body weight) and is administered in multiple (divided) doses delivered in the form of tablets or capsules.
Doses must be taken on a regular schedule but individuals should not double dose to make up for a missed dose.
When used to control anticonvulsive seizures, acetazolamide doses should not be stopped all at once. In most cases, physicians usually curtail (gradually lower) the dose an individual takes over time.
Precautions
As with most prescription medicines, acetazolamide should stored in a safe place—away from the reach of children. Acetazolamide should also be stored in a dry area away from excessive heat or light. Outdated medicine (medicines past their expiration date) should be discarded in a container that is safe from the reach of children.
Women who are pregnant, plan to become pregnant, or who are breast-feeding infants should inform their physician of this fact before taking acetazolamide.
Side effects
Unwanted side effects while taking acetazolamide include drowsiness, fatigue, or a dizzy lightheaded feeling. Individuals who experience these side effects should not operate machinery or drive while experiencing these symptoms. Other common side effects include shortness of breath.
Acetazolamide can also lead to excessive depletion (loss) of potassium from the body. To counter this potential loss, many physicians recommend that patients eat food or drink beverages such as orange juice to replace lost potassium. The loss of potassium does not occur in every case, however, and high levels of potassium can also be dangerous. Individuals who show signs of potassium loss—including, but not limited to, dryness of mouth, increased thirst, or muscle cramps—should alert their physician. Because diet can impact a number of health factors, individuals should only alter their diet after consulting their physician.
Individuals who are diabetic and who take acetazolamide may experience elevated sugar levels in their urine and blood.
Individuals who experience changes in their vision should also consult their physician.
In some rare cases, individuals may suffer depression, pains in the area of the kidneys, and bloody or black tarry stools.
Interactions
Physicians and pharmacists are trained to evaluate the potential for adverse interactions by prescription drugs with other drugs. In the case of acetazolamide physicians evaluate potential adverse reactions with a range of drugs that include—but are not limited to—amphetamines, over-the-counter aspirins, cyclosporine, mood altering drugs (e.g., lithium), drugs used to control mental depression, drugs used to control irregular heartbeats, digoxin, diuretics (also known as water pills), and vitamins.
Resources
PERIODICALS
Varadkar S., J. S. Duncan, and H. Cross. "Acetazolamide and Autosomal Dominant Nocturnal Frontal Lobe Epilepsy." Epilepsia 44 (July 2003): 986.
OTHER
Medline Plus. U.S. National Library of Medicine and the National Institutes of Health. http://www.nlm.nih.gov/medlineplus/druginfo/uspdi/202114.html (May 9, 2004).
ORGANIZATIONS
National Eye Institute. 2020 Vision Place, Bethesda, MD 20892-3655. (301) 496-5248. http://www.nei.nih.gov/.
Paul Arthur
| Drug Info: Acetazolamide |
Brand names: Diamox®
Chemical formula:
- Drug Forms:
- Acetazolamide Oral capsule, extended-release (below)
- Acetazolamide tablets
- Acetazolamide sustained-release capsules
- Acetazolamide Oral tablet
- Acetazolamide Sodium Solution for injection
- Español:
- Acetazolamida, Cápsula oral de liberación prolongada
- Tabletas de acetazolamida
- Cápsulas de liberación prolongada de acetazolamida
- Acetazolamida, Tableta oral
- Acetazolamida Sódica, Solución para inyección
Acetazolamide Oral capsule, extended-release
What is this medicine?
ACETAZOLAMIDE (a set a ZOLE a mide) is used to treat glaucoma. It is also used to treat and to prevent altitude or mountain sickness.
This medicine may be used for other purposes; ask your health care provider or pharmacist if you have questions.
What should I tell my health care provider before I take this medicine?
They need to know if you have any of these conditions:
•diabetes
•kidney disease
•liver disease
•lung disease
•an unusual or allergic reaction to acetazolamide, sulfa drugs, other medicines, foods, dyes, or preservatives
•pregnant or trying to get pregnant
•breast-feeding
How should I use this medicine?
Take this medicine by mouth with a glass of water. Follow the directions on the prescription label. Take with food or on an empty stomach. Do not crush or chew. Take your doses at regular intervals. Do not take your medicine more often than directed. Do not stop taking except on your doctor's advice.
Talk to your pediatrician regarding the use of this medicine in children. Special care may be needed.
Patients over 65 years old may have a stronger reaction and need a smaller dose.
Overdosage: If you think you have taken too much of this medicine contact a poison control center or emergency room at once.
NOTE: This medicine is only for you. Do not share this medicine with others.
What if I miss a dose?
Try not to miss doses. If you miss a dose take the dose as soon as you remember. If it is almost time for the next dose, do not take double doses unless told to by your prescriber or health care professional.What may interact with this medicine?
Do not take this medicine with any of the following medications:
•methazolamide
This medicine may also interact with the following medications:
•aspirin and aspirin-like medicines
•cyclosporine
•lithium
•medicine for diabetes
•methenamine
•other diuretics
•phenytoin
•primidone
•quinidine
•sodium bicarbonate
•stimulant medicines like dextroamphetamine
This list may not describe all possible interactions. Give your health care provider a list of all the medicines, herbs, non-prescription drugs, or dietary supplements you use. Also tell them if you smoke, drink alcohol, or use illegal drugs. Some items may interact with your medicine.
What should I watch for while using this medicine?
Visit your doctor or health care professional for regular checks on your progress. You will need blood work done regularly. If you are diabetic, check your blood sugar as directed.
You may need to be on a special diet while taking this medicine. Ask your doctor. Also, ask how many glasses of fluid you need to drink a day. You must not get dehydrated.
You may get drowsy or dizzy. Do not drive, use machinery, or do anything that needs mental alertness until you know how this medicine affects you. Do not stand or sit up quickly, especially if you are an older patient. This reduces the risk of dizzy or fainting spells.
This medicine can make you more sensitive to the sun. Keep out of the sun. If you cannot avoid being in the sun, wear protective clothing and use sunscreen. Do not use sun lamps or tanning beds/booths.
What side effects may I notice from receiving this medicine?
Side effects that you should report to your doctor or health care professional as soon as possible:
•allergic reactions like skin rash, itching or hives, swelling of the face, lips, or tongue
•breathing problems
•confusion, depression
•dark urine
•fever
•numbness, tingling in hands or feet
•redness, blistering, peeling or loosening of the skin, including inside the mouth
•ringing in the ears
•seizure
•unusually weak or tired
•yellowing of the eyes or skin
Side effects that usually do not require medical attention (report to your doctor or health care professional if they continue or are bothersome):
•change in taste
•diarrhea
•headache
•loss of appetite
•nausea, vomiting
•passing urine more often
This list may not describe all possible side effects. Call your doctor for medical advice about side effects. You may report side effects to FDA at 1-800-FDA-1088.
Where should I keep my medicine?
Keep out of the reach of children.
Store at room temperature between 20 and 25 degrees C (68 and 77 degrees F). Throw away any unused medicine after the expiration date.
Last updated: 7/1/2002
Important Disclaimer: The drug information provided here is for educational purposes only. It is intended to supplement, not substitute for, the diagnosis, treatment and advice of a medical professional. This drug information does not cover all possible uses, precautions, side effects and interactions. It should not be construed to indicate that this or any drug is safe for you. Consult your medical professional for guidance before using any prescription or over the counter drugs.
| Sports Science and Medicine: acetazolamide |
A diuretic drug on the World Anti-Doping Agency's 2005 Prohibited List. Acetazolamide is abused by some athletes to reduce weight artificially and as masking agent. It is also a component of medicines used to treat a number of conditions including oedema and altitude sickness (it is a carbonic anhydrase inhibitor, which probably acts as a respiratory stimulant).
| Veterinary Dictionary: acetazolamide |
A carbonic anhydrase inhibitor used as a diuretic, most commonly to reduce intraocular pressure in the treatment of glaucoma.
| Wikipedia: Acetazolamide |
Not to be confused with acetohexamide.
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| Systematic (IUPAC) name | |
|---|---|
| N-(5-sulfamoyl-1,3,4-thiadiazol-2-yl)acetamide | |
| Identifiers | |
| CAS number | 59-66-5 |
| ATC code | S01EC01 |
| PubChem | 1986 |
| DrugBank | APRD00119 |
| ChemSpider | 1909 |
| Chemical data | |
| Formula | C4H6N4O3S2 |
| Mol. mass | 222.245 g/mol |
| SMILES | eMolecules & PubChem |
| Pharmacokinetic data | |
| Bioavailability | ? |
| Metabolism | None |
| Half life | 3 to 9 hours |
| Excretion | Renal |
| Therapeutic considerations | |
| Pregnancy cat. | |
| Legal status | |
| Routes | Oral, IV |
 (what is this?) (verify) |
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Acetazolamide, sold under the trade name Diamox, is a carbonic anhydrase inhibitor that is used to treat glaucoma, epileptic seizures, benign intracranial hypertension (pseudotumor cerebri), altitude sickness, cystinuria, and dural ectasia. Acetazolamide is available as a generic drug and is also used as a diuretic.
Contents |
Mechanism of action
 |
This section may be confusing or unclear to readers. Please help clarify the article; suggestions may be found on the talk page. (June 2009) |
This drug is a carbonic anhydrase inhibitor.
Carbonic anhydrase (CA) catalyzes the forward motion of molecules in the following equation:
CO2 + H2O >> CA >> H2CO3 >> H+ + HCO3
where CA converts carbon dioxide (CO2) and water (H2O) to carbonic acid (H2CO3), which then dissociates to a hydrogen ion (H+, an acidic proton), and a bicarbonate ion (HCO3-, a basic anion). In some tissues (particularly plants), the equilibrium is such that CA can catalyze the reverse direction of the reaction. Carbonic acid inhibitors, such as acetazolamide, inhibit CA in tissue and fluid, causing less movement of carbonic acid toward CO2 production. In the kidneys, blocking CA leads to bicarbonate wasting in the tubules (alkalizes urine), loss of bicarbonate subsequently leads to a metabolic acidosis. In the meantime, H+ backs up due to acetazolamide CA inhibition in the tubule and enters the cell with Cl-, then passes into the bloodstream, creating a hyperchloremic metabolic acidosis.[1] This effect can also be used for therapeutic correction of respiratory alkalosis.
Uses
Acetazolamide is often used in the treatment of various diseases.
Glaucoma
It has been used for glaucoma sufferers.[2] The drug decreases fluid formation in the eye resulting in lower intraocular pressure.
Neurologic
In epilepsy, its main use is in absence seizures and myoclonic seizures.[3]. It can be used in both episodic ataxia types 1 and 2 (although the mechanisms are presumed to be different between the two).
It is also used to decrease generation of cerebrospinal fluid in idiopathic intracranial hypertension[4] and has shown efficacy in some forms of hyperkalemic periodic paralysis.[5]
Marfan syndrome
It's been demonstrated in drug trials to relieve symptoms associated with dural ectasia in individuals with Marfan Syndrome.[6]
Sleep apnea
Off-label uses include acetazolamide as a conjunction drug to merely assist patients with sleep apnea by lowering blood pH and encourage respiration.[7]
Acute mountain sickness
Acetazolamide is sometimes taken prophylactically, anywhere between 125 milligrams (mg) to 500 mg per day, starting a few days before going to the higher altitude. Such use is recommended for those ascending from sea level to 3000 meters (9800 feet) in one day, or for those ascending more than 600 meters (2000 feet) per day once above an altitude of 2500 meters (8200 feet).[8][9] Also, prophylactic use is recommended for those with a significant history of acute mountain sickness.
The drug forces the kidneys to excrete bicarbonate, the conjugate base of carbonic acid. By increasing the amount of bicarbonate excreted in the urine, the blood becomes more acidic.[9] Acidifying the blood stimulates ventilation, which increases the amount of oxygen in the blood.[10][11]
Note that acetazolamide is not an immediate fix for acute mountain sickness; it speeds up part of the acclimatization process which in turn helps to relieve symptoms.[12][13] This may take up to a day or two, and requires waiting without any further rapid ascent. It is often advisable to descend if even mild acute mountain sickness is experienced. If serious sickness is encountered, descent is considered mandatory unless other circumstances present greater danger.
Side-effects
Common side effects of using this drug include numbness and tingling in the fingers and toes, and taste alterations (parageusia), especially for carbonated drinks. Some may also experience blurred vision but this usually disappears shortly after stopping the medication. Acetazolamide also increases the risk of developing calcium oxalate and calcium phosphate kidney stones. Everyone will experience more frequent urination as a result of using acetazolamide. One should drink more fluids than usual to prevent dehydration and headaches. Acetazolamide prolongs the effects of amphetamines and related drugs. Acetazolamide also causes metabolic acidosis.
Contraindications
Acetazolamide should not be taken by individuals if:
- They have sickle cell anemia
- They are allergic to sulfa medications
- They are allergic to any carbonic anhydrase inhibitor
- They have liver or kidney disease
- They have adrenal gland failure (i.e. Addison's disease)
- They are pregnant or nursing mothers
References
- ^ Renal and Electrolyte Disorders Schrier 1976: page 89
- ^ Kaur IP, Smitha R, Aggarwal D, Kapil M (November 2002). "Acetazolamide: future perspective in topical glaucoma therapeutics". Int J Pharm 248 (1-2): 1–14. doi:. PMID 12429455. http://linkinghub.elsevier.com/retrieve/pii/S0378517302004386.
- ^ "Treatment of Epilepsy | Comprehensive Epilepsy Center | NYU Medical Center, New York, NY". http://www.med.nyu.edu/cec/treatment/medications/side_effects/aceta.html. Retrieved 2008-12-19.
- ^ Celebisoy N, Gökçay F, Sirin H, Akyürekli O (November 2007). "Treatment of idiopathic intracranial hypertension: topiramate vs acetazolamide, an open-label study". Acta Neurol. Scand. 116 (5): 322–7. doi:. PMID 17922725. http://www3.interscience.wiley.com/resolve/openurl?genre=article&sid=nlm:pubmed&issn=0001-6314&date=2007&volume=116&issue=5&spage=322.
- ^ Ptáĉek LJ, Tawil R, Griggs RC, et al. (August 1994). "Sodium channel mutations in acetazolamide-responsive myotonia congenita, paramyotonia congenita, and hyperkalemic periodic paralysis". Neurology 44 (8): 1500–3. PMID 8058156.
- ^ Scoliosis Research Society (2006-11-27). "Dural Ectasia in the Marfan Spine: Symptoms and Treatment.also it's been used in high-altitude mountain sickness". SpineUniverse. http://www.spineuniverse.com/displayarticle.php/article922.html. Retrieved 2007-11-15.
- ^ White DP, Zwillich CW, Pickett CK, Douglas NJ, Findley LJ, Weil JV (October 1982). "Central sleep apnea. Improvement with acetazolamide therapy". Arch. Intern. Med. 142 (10): 1816–9. PMID 6812522.
- ^ Hackett, P.H. & Roach, R.C. (2001). "High-altitude illness". The New England Journal of Medicine 345 (2): 107–114. doi:. PMID 11450659.
- ^ a b Fulco, CS; Ditzler, D; Soares, R; Lammi, E; Muza, SR; Degroot, DW (2002). "Effect of Acetazolamide on Isolated Quadriceps Muscle Endurance Performance at Sea Level and During Acute Altitude Exposure". US Army Research Inst. Of Environmental Medicine Thermal and Mountain Medicine Division Technical Report (USARIEM-TR-T02/9). http://archive.rubicon-foundation.org/7602. Retrieved 2008-09-30.
- ^ "Altitude.org". 2004. http://www.altitude.org. Retrieved 2009-06-05.
- ^ Leaf DE, Goldfarb DS (April 2007). "Mechanisms of action of acetazolamide in the prophylaxis and treatment of acute mountain sickness". J. Appl. Physiol. 102 (4): 1313–22. doi:. PMID 17023566.
- ^ Muza, SR; Fulco, CS; Cymerman, A (2004). "Altitude Acclimatization Guide.". US Army Research Inst. Of Environmental Medicine Thermal and Mountain Medicine Division Technical Report (USARIEM-TN-04-05). http://archive.rubicon-foundation.org/7616. Retrieved 2009-03-05.
- ^ Cymerman, A; Rock, PB. Medical Problems in High Mountain Environments. A Handbook for Medical Officers. USARIEM-TN94-2. US Army Research Inst. of Environmental Medicine Thermal and Mountain Medicine Division Technical Report. http://archive.rubicon-foundation.org/7976. Retrieved 2009-03-05.
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| acetazolamide/acetazolamide sodium |
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