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Acetazolamide

 

 
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Acetazolamide
 
 
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Acetazolamide, sold under the trade name Diamox, is a carbonic anhydrase inhibitor that is used to treat glaucoma
Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
, epileptic seizures, benign intracranial hypertension (pseudotumor cerebri), altitude sickness
Altitude sickness

Altitude sickness, also known as acute mountain sickness , altitude illness, or soroche, is a pathological condition that is caused by acute exposure to low air pressure ....
, cystinuria
Cystinuria

Cystinuria is an inherited autosome dominance metabolic disorder that is characterized by the formation of cystine stones in the kidneys, ureter, and Urinary bladder....
, and dural ectasia
Dural ectasia

Dural ectasia is a widening or ballooning of the dura_mater sac surrounding the spinal cord usually at the lumbosacral level. It is one of the major manifestations of Marfan syndrome....
. Acetazolamide is available as a generic drug
Generic drug

A generic drug is a medication which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
 and is also used as a diuretic
Diuretic

A diuretic is any drug that elevates the rate of urination and thus provides a means of forced diuresis. There are several categories of diuretics....
.

drug is a carbonic anhydrase inhibitor. Carbonic anhydrase
Carbonic anhydrase

The carbonic anhydrases form a family of enzymes that catalyst the rapid conversion of carbon dioxide to bicarbonate and Hydronium ions, a reaction that occurs rather slowly in the absence of a catalyst....
 creates H+ and HCO3- from CO2 and H2O.






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Acetazolamide, sold under the trade name Diamox, is a carbonic anhydrase inhibitor that is used to treat glaucoma
Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
, epileptic seizures, benign intracranial hypertension (pseudotumor cerebri), altitude sickness
Altitude sickness

Altitude sickness, also known as acute mountain sickness , altitude illness, or soroche, is a pathological condition that is caused by acute exposure to low air pressure ....
, cystinuria
Cystinuria

Cystinuria is an inherited autosome dominance metabolic disorder that is characterized by the formation of cystine stones in the kidneys, ureter, and Urinary bladder....
, and dural ectasia
Dural ectasia

Dural ectasia is a widening or ballooning of the dura_mater sac surrounding the spinal cord usually at the lumbosacral level. It is one of the major manifestations of Marfan syndrome....
. Acetazolamide is available as a generic drug
Generic drug

A generic drug is a medication which isproduced and distributed without patent protection. The generic drug may still have a patent on the formulation but not on the active ingredient....
 and is also used as a diuretic
Diuretic

A diuretic is any drug that elevates the rate of urination and thus provides a means of forced diuresis. There are several categories of diuretics....
.

Mechanism of Action

This drug is a carbonic anhydrase inhibitor. Carbonic anhydrase
Carbonic anhydrase

The carbonic anhydrases form a family of enzymes that catalyst the rapid conversion of carbon dioxide to bicarbonate and Hydronium ions, a reaction that occurs rather slowly in the absence of a catalyst....
 creates H+ and HCO3- from CO2 and H2O. The H+ is then excreted in exchange for Na+ on the renal luminal membrane while the HCO3- is co-reabsorbed with Na+ on the basolateral membrane. Acetazolamide blocks the action of carbonic anhydrase II and IV, which results in increasing amounts of HCO3- and Na+ (and therefore water) in the urine. Indirectly, it will block the Na/H exchanger in the renal proximal convoluted tubule and therefore, there is a natriuretic/diuretic action in addition to the "washing away" of bicarbonate in the urine. The excess luminal water and sodium leads to an increased flow rate that can further disrupt other transporters in the tubule from functioning properly.

Uses

Acetazolamide is often used in the treatment of various diseases.

Glaucoma

It has been used for glaucoma
Glaucoma

Glaucoma is a group of diseases of the optic nerve involving loss of ganglion cell in a characteristic pattern of optic atrophy. Raised intraocular pressure is a significant risk factor for developing glaucoma ....
 sufferers. The drug decreases fluid formation in the eye
Eye

Eyes are Organ that detect light, and send signals along the optic nerve to the visual system and other areas of the brain. Complex optical systems with resolving power have come in ten fundamentally different forms, and 96% of animal species possess a complex optical system....
 resulting in lower intraocular pressure.

Neurologic

In epilepsy, its main use is in absence seizure
Absence seizure

Absence seizures are one of several kinds of seizures. These seizures are sometimes referred to as petit mal seizures .In absence seizures, the person may appear to be staring into space with or without jerking or Muscle contraction movements of the eye muscles....
s and myoclonic seizures.

It is also used to decrease generation of cerebrospinal fluid
Cerebrospinal fluid

Cerebrospinal fluid , Liquor cerebrospinalis, is a clear bodily fluid that occupies the subarachnoid space and the ventricular system around and inside the brain....
 in benign intracranial hypertension and has shown efficacy in autosomal dominant hyperkalemic periodic paralysis
Hyperkalemic periodic paralysis

Hyperkalemic periodic paralysis , also known as Impressive Syndrome, is an genetic disease autosomal dominance relationship disorder which affects ion channelss in muscle cells and the ability to regulate potassium levels in the blood....
.

Marfan syndrome

It's been demonstrated in drug trials to relieve symptoms associated with dural ectasia in indivduals with Marfan Syndrome
Marfan syndrome

Marfan syndrome is a genetic disorder of the connective tissue.It is sometimes inherited as a Autosomal dominant trait. It is carried by a gene called FBN1, which encodes a connective protein called fibrillin-1....
.

Sleep apnea

Off-label uses include acetazolamide as a conjunction drug to merely assist patients with sleep apnea
Sleep apnea

Sleep apnea is a sleep disorder characterized by pauses in breathing during sleep. Each episode, called an apnea , lasts long enough so that one or more breaths are missed, and such episodes occur repeatedly throughout sleep....
 by lowering blood pH and encourage respiration.

Acute mountain sickness

Acetazolamide is sometimes taken prophylactically
Prophylaxis

Prophylaxis is any medical or public health procedure whose purpose is to prevent, rather than treat or cure a disease. Roughly, prophylactic measures are divided between primary prophylaxis and secondary prophylaxis ....
, 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). Also, prophylactic use is recommended for those with a significant history of acute mountain sickness.

The drug forces the kidney
Kidney

The kidneys are Organ that have numerous biological roles. Their primary role is to maintain the homeostasis balance of bodily fluids by filtering and secreting Metabolomics#Metabolitess and minerals from the blood and excreting them, along with water , as urine....
s to excrete bicarbonate
Bicarbonate

In inorganic chemistry, bicarbonate is an intermediate form in the deprotonation of carbonic acid. Its chemical formula is HCO3−....
, the conjugate base of carbonic acid
Carbonic acid

Carbonic acid has the Molecular formula H2CO3. It is also a name sometimes given to solutions of carbon dioxide in water , which contain small amounts of H2CO3....
. By increasing the amount of bicarbonate excreted in the urine, the blood becomes more acidic. Acidifying the blood stimulates ventilation, which is beneficial during acclimatization.

Note that acetazolamide is not an immediate fix for acute mountain sickness; it speeds up acclimatization
Acclimatization

Acclimatization is the process of an organism adjusting to chronic change in its Ecosystem, often involving temperature, moisture, food, often relating to seasonal climate changes....
 which in turn helps to relieve symptoms. 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
Adverse drug reaction

An adverse drug reaction or adverse drug event is an expression that describes the unwanted, negative consequences associated with the use of given medications....
 of using this drug include numbness and tingling
Paresthesia

Paresthesia is a sensation of tingling, pricking, or numbness of a person's skin with no apparent long-term physical effect. It is more generally known as the feeling of "pins and needles" or of a human limb being "asleep" ....
 in the fingers and toes, and taste
Taste

Sorry, no overview for this topic
 alterations (parageusia
Parageusia

Parageusia is the medical term for a bad taste in the mouth.One common form of parageusia is a metallic taste of food. This can be a Adverse effect of several medications, such as acetazolamide, eszopiclone, metronidazole, or etoposide....
), especially for carbonated drinks. Some may also experience blurred vision
Visual perception

Visual perception is the ability to interpret information from visible light reaching the eye. The resulting perception is also known as eyesight, sight or 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
Urination

Urination, also known as micturition, voiding, and, more rarely, emiction, is the process of disposing urine from the urinary bladder through the urethra to the outside of the body....
 as a result of using acetazolamide. One should drink more fluids than usual to prevent dehydration
Dehydration

Dehydration is the removal of water from an object. In Physiology terms, it entails a relative deficiency of water molecules in relation to other dissolved solutes....
 and headache
Headache

In medicine a headache or wiktionary:cephalalgia is a symptom of a number of different conditions of the head and sometimes neck. Some of the causes are benign while others are medical emergencies....
s. Acetazolamide prolongs the effects of amphetamines and related drugs.

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
    Liver

    The liver is a vital organ present in vertebrates and some other animals; it has a wide range of functions, a few of which are detoxification, protein synthesis, and production of biochemicals necessary for digestion....
     or kidney
    Kidney

    The kidneys are Organ that have numerous biological roles. Their primary role is to maintain the homeostasis balance of bodily fluids by filtering and secreting Metabolomics#Metabolitess and minerals from the blood and excreting them, along with water , as urine....
     disease
  • They have adrenal gland
    Adrenal gland

    In mammals, the adrenal glands are the star-shaped endocrine glands that sit on top of the kidneys; their name indicates that position . They are chiefly responsible for regulating the stress response through the biosynthesis of corticosteroids and catecholamines, including cortisol and adrenaline, respectively....
     failure (i.e. Addison's disease
    Addison's disease

    Addison's disease is a rare endocrine disorder in which the adrenal gland doesn't produce enough steroid hormones . It may develop in children and adults, and may occur as the result many underlying causes....
    )
  • They have diabetes
  • They are pregnant or nursing mothers


Footnotes