Carbonic anhydrase inhibition with acetazolamide. Medical search. Frequent questions

Hydrochloric acid (HCl) and carbonic anhydrase inhibitors may be used in some acute situations. (medscape.com)
The method is suitable for estimating the activity of carbonic anhydrase inhibitors and for their determination in biological material. (aspetjournals.org)
Carbonic anhydrase inhibitors are a class of pharmaceuticals that suppress the activity of carbonic anhydrase. (wikipedia.org)
Carbonic anhydrase inhibitors are primarily used for the treatment of glaucoma. (wikipedia.org)
Other examples are: Dorzolamide Methazolamide Brinzolamide Dichlorphenamide Carbonic anhydrase inhibitors may be used to reduce the production of cerebrospinal fluid (CSF) in the brain. (wikipedia.org)
A more immediate treatment is carbonic anhydrase inhibitors, which prevent bicarbonate uptake in the kidney and help correct the alkalosis. (wikipedia.org)
Carbonic anhydrase inhibitors have also been shown to improve chronic mountain sickness. (wikipedia.org)
The p-toluensulfonate, the methylsulfonate, and the chlorhydrate monohydrate salts of Hats were evaluated as carbonic anhydrase (CA, EC 4.2.1.1) inhibitors (CAIs) and as anticonvulsants and diuretics, since many CAIs are clinically used as pharmacological agents. (conicet.gov.ar)
This agrees with our recent observations when we were the first to report the inhibition of hCAII by STS inhibitors. (ox.ac.uk)
Similarly, the binding affinities of compound ( 2 ) are higher with the receptor proteins (-87.76, -86.20 and -92.12 kcal/mol with PDE, urease and carbonic anhydrase, respectively) than the standard inhibitors (-80.77 (EDTA), -69.61 (thiourea) and -49.25 kcal/mol (Acetazolamide). (innspub.net)
and carbonic anhydrase inhibitors, including acetazolamide and methazolamide. (aspetjournals.org)
One of the carbonic anhydrase inhibitors that is sometimes effective against absence seizures. (pharmfair.com)
Carbonic anhydrase inhibitors (CAIs) have been used to treat glaucoma since 1954, when Becker 1 first demonstrated the clinical efficacy of systemically administered acetazolamide. (entokey.com)
Ozgun, Synthesis and bioactivities of pyrazoline benzensulfonamides as carbonic anhydrase and acetylcholinesterase inhibitors with low cytotoxicity, Bioorg. (dntb.gov.ua)
Istrefi, Sulfonamides incorporating ketene N,S-acetal bioisosteres as potent carbonic anhydrase and acetylcholinesterase inhibitors, Arch. (dntb.gov.ua)
Sever, Thiazolyl-pyrazoline derivatives: In vitro and in silico evaluation as potential acetylcholinesterase and carbonic anhydrase inhibitors, Int. J. Biol. (dntb.gov.ua)
The concomitant administration of brinzolamide and oral carbonic anhydrase inhibitors is not recommended. (ncats.io)
Plus, in patients treated with oral carbonic anhydrase inhibitors, rare instances of acid-base alterations have occurred with high-dose salicylate therapy. (ncats.io)
Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. (medscape.com)
Dr. Maren then returned to industry at the chemotherapy division of the American Cyanamid Company, where he began studying carbonic anhydrase and its inhibitors. (ufl.edu)
In the mid-1970s, Dr. Maren returned to his early work on glaucoma medication, convinced that carbonic anhydrase inhibitors could be applied topically to the eye. (ufl.edu)
The catalytic and inhibition mechanisms of these enzymes are understood in detail, and this helped the design of potent inhibitors, some of which possess important clinical applications. (rhea-db.org)

In the eye, this inhibitory action of acetazolamide decreases the secretion of aqueous humor and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain non-glaucomatous conditions. (nih.gov)
In the eye this inhibitory action of acetazolamide decreases the secretion of aqueous humour and results in a drop in intraocular pressure, a reaction considered desirable in cases of glaucoma and even in certain nonglaucomatous conditions. (myvmc.com)
These compounds therefore have a similar CAII inhibitory potency to that of acetazolamide (IC(50)=25 nM), a known hCAII inhibitor. (ox.ac.uk)
In general, sulfonamides and their derivatives are researched for their inhibitory effects on carbonic anhydrase isoenzymes (CAs). (gazi.edu.tr)
In the eye, the inhibitory activity of acetazolamide reduces the secretion of aqueous humor resulting in a reduction in intraocular pressure, which is beneficial for glaucoma. (statpearls.com)
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. (pharmfair.com)
Sağlık, Synthesis, molecular docking analysis and carbonic anhydrase I-II inhibitory evaluation of new sulfonamide derivatives, Bioorg. (dntb.gov.ua)

In rare cases, the inhibition of carbonic anhydrase may be strong enough to cause metabolic acidosis of clinical importance. (wikipedia.org)

Urine volume increases with enzyme inhibition (proximal tubule reabsorption of water is reduced by approximately one third), which promotes an alkaline pH. (medscape.com)
citation needed] Some diuretics inhibit the activity of carbonic anhydrase in proximal convoluted tubules and prevent reabsorption of bicarbonates from renal tubules. (wikipedia.org)
Since sodium and bicarbonate reabsorption are coupled, we postulated that the molecules involved in their reabsorption [NHE3 and carbonic anhydrase II (CAII)] might physically and functionally interact. (bvsalud.org)
Carbonic anhydrase plays an important role in bicarbonate reabsorption from the proximal tubule ( Ives, 2001 ). (aspetjournals.org)

For the reduction of intraocular pressure (IOP), acetazolamide inactivates carbonic anhydrase and interferes with the sodium pump, which decreases aqueous humor formation and thus lowers IOP. (wikipedia.org)
citation needed] Brinzolamide (trade name Azopt) is a carbonic anhydrase inhibitor used to lower intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (wikipedia.org)
Long-term administration of acetaZOLAMIDE is contraindicated in patients with chronic non-congestive angle-closure glaucoma since it may permit organic closure of the angle to occur while the worsening glaucoma is masked by lowered intraocular pressure. (drugcite.com)
Brinzolamide is a carbonic anhydrase inhibitor that is FDA approved for the treatment of elevated intraocular pressure in patients with ocular hypertension or open-angle glaucoma. (ncats.io)
INDICATIONS & USAGE SECTION SIMBRINZA† (brinzolamide/brimonidine tartrate ophthalmic suspension) 1%/0.2% is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure (IOP) in patients with open-angle glaucoma or ocular hypertension. (ncats.io)
SIMBRINZA is a fixed combination of a carbonic anhydrase inhibitor and an alpha 2 adrenergic receptor agonist indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (ncats.io)
His early work contributed to the first effective oral diuretic, Diamox (acetazolamide), a carbonic anhydrase inhibitor, which also happened to lower intraocular pressure. (ufl.edu)

The classical CA inhibitor, acetazolamide, showed an inhibition constant of 84.1 nM. (biomedcentral.com)
Carbonic anhydrase inhibitor acetazolamide affects the delicate equilibrium among CO2, H+, and HCO3- in the neurons and modulates the activity of ligand-gated ion channels at the neuronal level, such as GABA-A signaling. (statpearls.com)
In contrast, infusion of the CA inhibitor acetazolamide resulted in a respiratory acidosis in the blood of recovering lampreys. (researcher.life)
Inside a transwell assay (Fig.?2a), both anti-CAIX mAbs G37 and G119 showed inhibition of RCC cell migration much like that seen using the CA inhibitor acetazolamide. (monossabios.com)
more specifically a carbonic anhydrase (CA) inhibitor, acetazolamide predominantly acts within the proximal convoluted tubule of the nephron (De Marchi and Cecchin 1990). (ukessays.com)

Acetazolamide extended-release capsules provide prolonged action to inhibit aqueous humor secretion for 18 to 24 hours after each dose, whereas tablets act for only eight to 12 hours. (nih.gov)
Acetazolamide, in a dose sufficient to inhibit the erythrocyte carbonic anhydrase (EC 4.2.1.1), thus induced a rapid and marked increase in CBF, leaving CMRO2 unchanged. (nih.gov)
We also demonstrate these anti-CAIX mAbs inhibit migration of RCC cells including tumor infiltration of NK cells and activation of T cells, leading to inhibition of CAIX+ tumor development. (monossabios.com)
Likewise, both mAbs demonstrated a capability to inhibit RCC development in wound curing assays (Fig.?2b) that mirrored inhibition seen with acetazolamide treatment [29]. (monossabios.com)
These drugs inhibit carbonic anhydrase (CA), one of the enzymes that regulate aqueous humor formation. (entokey.com)

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. (nih.gov)
The prolonged continuous effect of acetazolamide permits a reduction in dosage frequency. (nih.gov)
The aim of this study was to evaluate the effect of acetazolamide on cerebral blood flow (CBF) and cerebral metabolic rate for oxygen (CMRO2). (nih.gov)
This effect of acetazolamide on CBF is probably explained by a decrease in brain pH rather than by brain tissue hypoxia due to inhibition of oxygen unloading in the brain capillaries. (nih.gov)
Becker's demonstration of the marked ocular hypotensive effect of acetazolamide in glaucoma patients led to the widespread clinical use of oral CAIs for the treatment of glaucoma and to numerous clinical and laboratory evaluations of acetazolamide and other CAIs. (entokey.com)
The discovery of the substantial effect of acetazolamide on IOP encouraged Maren to extensively research the chemistry, physiology, and pharmacology of CAIs. (entokey.com)

Acetazolamide is a potent carbonic anhydrase inhibitor, effective in the control of fluid secretion (e.g., some types of glaucoma), in the treatment of certain convulsive disorders (e.g., epilepsy) and in the promotion of diuresis in instances of abnormal fluid retention (e.g., cardiac edema). (nih.gov)

Since acetazolamide is a sulfonamide derivative, cross sensitivity between acetazolamide, sulfonamides and other sulfonamide derivatives is possible. (nih.gov)
The nature of carbonic anhydrase inhibition by aromatic sulfonamides is briefly discussed, as it may relate to certain variables in the analytical method. (aspetjournals.org)
In order to test the principle that a CA IX inhibitor could be used for targeting PET or SPECT metallic radioisotopes to tumours we have prepared a number of conjugates involving aryl-sulfonamides or an acetazolamide derivative linked to a range of copper, indium, rhenium, 99m-technetium and zinc complexes. (bath.ac.uk)
Among tested compounds, bis-(5-nitro-2 furaldehydemethanesulfonylhydrazone) copper(II) chloride was found to be the most active complex on CA I isoenzyme with IC50 value of 7.03 x 10(-5) M. The enzyme inhibition trends of copper(II) sulfonamides on CA I isoenzyme were also investigated by CV and differential pulse voltammetry (DPV) techniques, qualitatively. (gazi.edu.tr)

Their mechanism of action is unknown but may involve inhibition of cyclooxygenase activity and prostaglandin synthesis. (medscape.com)
Other mechanisms may also play a role, such as inhibition of leukotriene synthesis, lysosomal enzyme release, lipoxygenase activity, neutrophil aggregation, and various cell membrane functions. (medscape.com)
Under the direction of Richard Roblin at the American Cyanamid Company, Maren 5 was searching for a CAI to use as an oral diuretic agent and was involved in the synthesis of acetazolamide in 1954. (entokey.com)
Aydin, Synthesis of N-alkylated pyrazolo [3, 4-d] pyrimidine analogs and evaluation of acetylcholinesterase and carbonic anhydrase inhibition properties, Arch. (dntb.gov.ua)
Akin, Synthesis of 1, 2, 4-triazole-5-on derivatives and determination of carbonic anhydrase II isoenzyme inhibition effects, Bioorg. (dntb.gov.ua)
Singh, Synthesis and carbonic anhydrase inhibition studies of sulfonamide based indole-1, 2, 3-triazole chalcone hybrids, Bioorg. (dntb.gov.ua)

Inhibition of various human carbonic anhydrase isoforms (I, II, IX and XII) was tested with the 'cold', non-radiolabelled complexes, and compared with an acetazolamide standard (AZA). (bath.ac.uk)
At least 14 different carbonic anhydrase (CA, EC 4.2.1.1) isoforms were isolated in higher vertebrates, where these zinc enzymes play crucial physiological roles. (rhea-db.org)

Acetazolamide may be used in loop or thiazide diuretic−induced metabolic alkalosis, especially in edematous states. (medscape.com)

Acetazolamide is a classic treatment option for glaucoma as it causes a reduction in aqueous humor. (statpearls.com)
he elected to evaluate acetazolamide as an ocular hypotensive agent in glaucoma patients. (entokey.com)

Acetazolamide extended-release capsules are an inhibitor of the enzyme carbonic anhydrase. (nih.gov)
Acetazolamide is an enzyme inhibitor that acts specifically on carbonic anhydrase, the enzyme that catalyzes the reversible reaction involving the hydration of carbon dioxide and the dehydration of carbonic acid. (nih.gov)
The major pharmacologic action of agents in this class is noncompetitive inhibition of the enzyme carbonic anhydrase. (medscape.com)
The electrochemical studies showed that when the concentration of the inhibitor was increased, the reduction peak current of PNP produced by the hydrolysis of PNPA was decreased by enzyme inhibition. (gazi.edu.tr)
AcetaZOLAMIDE, an inhibitor of the enzyme carbonic anhydrase, is a white to faintly yellowish white crystalline, odorless powder, weakly acidic, very slightly soluble in water and slightly soluble in alcohol. (drugcite.com)

Carbonic anhydrase is found in the proximal tubule of the nephron and red blood cells. (statpearls.com)

Inhibition of carbonic anhydrase II in the ciliary processes of the eye decreases aqueous humor secretion, presumably by slowing the formation of bicarbonate ions with subsequent reduction in sodium and fluid transport. (wikipedia.org)
Acetazolamide reduces the rate of CSF formation and decreases cerebral spinal fluid pH. (blogspot.com)
The anticonvulsant activity of Acetazolamide may depend on a direct inhibition of carbonic anhydrase in the CNS, which decreases carbon dioxide tension in the pulmonary alveoli, thus increasing arterial oxygen tension. (pharmfair.com)

The active ingredient in Diamox is acetazolamide. (myvmc.com)

Methazolamide is also a carbonic anhydrase inhibitor. (wikipedia.org)
We recently showed that the carbonic anhydrase inhibitor (CAI) methazolamide (MTZ) prevents amyloid β (Aβ)-mediated onset of apoptosis in the mouse brain. (peixotolab.org)

Zonisamide is another sulfur containing antiseizure drug that weakly inhibits carbonic anhydrase. (wikipedia.org)
Acetazolamide is also used in treating idiopathic intracranial hypertension, as it inhibits enzymes in the choroid plexus and reduces the production of CSF, resulting in a decrease in intracranial pressure(ICP). (statpearls.com)

Plasma concentrations of acetazolamide peak from three to six hours after administration of acetazolamide extended-release capsules, compared to one to four hours with tablets. (nih.gov)
Placebo-controlled clinical trials have shown that prophylactic administration of acetazolamide at a dose of 250 mg every eight to 12 hours (or a 500 mg controlled-release capsule once daily) before and during rapid ascent to altitude results in fewer and/or less severe symptoms of acute mountain sickness (AMS) such as headache, nausea, shortness of breath, dizziness, drowsiness, and fatigue. (nih.gov)

In vivo experiments were carried out to determine the relative effects of carbonic anhydrase (CA) infusion or inhibition on carbon dioxide (CO2) transport and acid-base status in the arterial and venous blood of sea lampreys recovering from exhaustive exercise. (researcher.life)
The calculated arterial and venous partial pressure of carbon dioxide (PCO2) and the total CO2 concentration in whole blood (CCO2wb) and red blood cells (CCO2rbc) during recovery in the acetazolamide-infused lampreys were also significantly greater than those values in the saline-infused control lampreys. (researcher.life)
CA catalyzes the reversible reaction in which carbon dioxide (CO 2 ) is hydrated (H 2 O) to form carbonic acid (H 2 CO 3 ) (i.e. (entokey.com)

The entire process of excretion inhibited by carbonic anhydrase is essentially working to acidify the urine and reabsorb bicarbonate. (statpearls.com)
and PAH inhibition of furosemide excretion in the rabbit ( Bidiville and Roch-Ramel, 1986 ). (aspetjournals.org)
Some diuretics, such as acetazolamide , help to make the urine more alkaline and are helpful in increasing excretion of substances such as aspirin in cases of overdose or poisoning. (wikidoc.org)

The mechanism is thought to involve inhibition of carbonic anhydrase (CA) within the choroidal epithelial cells, reducing the production of protons which are necessary for the osmotic transport of water and ions which constitute CSF. (wikipedia.org)

It has a longer elimination half-life than acetazolamide and is less associated with adverse effects to the kidney. (wikipedia.org)

Evidence seems to indicate that acetazolamide has utility as an adjuvant in treatment of certain dysfunctions of the central nervous system (e.g., epilepsy). (nih.gov)
In epilepsy, inhibition of carbonic anhydrase by acetazolamide seems to retard abnormal, excessive, paroxysmal electrical discharge from neurons. (statpearls.com)

The diuretic effect depends on the inhibition of carbonic anhydrase, causing a reduction in the availability of hydrogen ions for active transport in the renal tubule lumen. (pharmfair.com)
Background Carbonic anhydrase (CA) IX is normally a surface-expressed protein that's upregulated from the hypoxia inducible factor (HIF) and represents a prototypic tumor-associated antigen that's overexpressed about renal cell carcinoma (RCC). (monossabios.com)

Acetazolamide therapy is contraindicated in situations in which sodium and/or potassium blood serum levels are depressed, in cases of marked kidney and liver disease or dysfunction, in suprarenal gland failure, and in hyperchloremic acidosis. (nih.gov)
Carbonic anhydrase II binds to and increases the activity of the epithelial sodium-proton exchanger, NHE3. (bvsalud.org)
Acetazolamide will derange the whole process by increasing sodium in the urine and increasing bicarbonate which alkalinizes the urine. (statpearls.com)
Acetazolamide, a major carbonic anhydrase inhibitor, blocks the re-absorption of sodium bicarbonate, resulting in an alkaline diuresis with loss of sodium and bicarbonate in the urine. (aspetjournals.org)

The Mechanism of Action of Acetazolamide in the Treatment of Acute Mountain Sickness. (ukessays.com)

That means this drug works to cause an accumulation of carbonic acid by preventing its breakdown. (statpearls.com)
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. (statpearls.com)
He studied carbonic anhydrase and other methods of acid secretion and bicarbonate resorption in many marine animals every summer in Maine for 40 years. (ufl.edu)

Inhibition of carbonic anhydrase in this area appears to retard abnormal, paroxysmal, excessive discharge from central nervous system neurons. (nih.gov)

After coming to UF, Dr. Maren continued his work on carbonic anhydrase. (ufl.edu)

Dorzolamide is a sulfonamide and topical carbonic anhydrase II inhibitor. (wikipedia.org)

Comparative physiology gave him particular insight into the roles of carbonic anhydrase in humans, especially the secretion of cerebrospinal fluid. (ufl.edu)

The acetazolamide treated climbers also had less difficulty in sleeping. (nih.gov)
AcetaZOLAMIDE is also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness in climbers attempting rapid ascent and in those who are very susceptible to acute mountain sickness despite gradual ascent. (drugcite.com)

Carbonic anhydrases rapidly decrease or increase H+ and HCO3 − in the neurons. (statpearls.com)

However, many questions remain regarding the efficacy of acetazolamide, CSF shunting procedures and cerebral transverse venous sinus stenting. (bmj.com)

Through network analysis of the compound-target pathway, we identified hub molecular targets within these pathways including carbonic anhydrase II (CA2), peroxisome proliferator activated receptor γ (PPAR γ ), retinoid X receptor α (RXRA), and vitamin D receptor (VDR). (hindawi.com)

Acetazolamide is a diuretic and carbonic anhydrase inhibitor medication used to treat several illnesses, as summarized below. (statpearls.com)

Acetazolamide extended-release capsules are also indicated for the prevention or amelioration of symptoms associated with acute mountain sickness despite gradual ascent. (nih.gov)

Whether carbonic anhydrase inhibition contributes to its clinical activity is not known. (wikipedia.org)

Food does not affect bioavailability of acetazolamide extended-release capsules. (nih.gov)

Tubular secretion of acetazolamide was demonstrated to be important for the elimination of this drug in the study using the isolated rat perfused kidney ( Taft and Sweeney, 1995 ). (aspetjournals.org)

The GDPSP/C was dependent on the availability of bicarbonate, but not on interstitial or intrapyramidal carbonic anhydrase activity. (jneurosci.org)
Inhibition of endogenous CAII activity with acetazolamide significantly decreased NHE3 activity, indicating that CAII activates NHE3. (bvsalud.org)
Using a 96-well plate assay, oestrone-3-O-sulphamate (EMATE) and two coumarin-based sulphamate drugs (667 COUMATE and STX 118) were found to have IC(50) values of 25-59 nM for the inhibition of hCAII activity. (ox.ac.uk)
Similarly, both the compounds showed significant activity against urease with IC 50 values equal to 45 ± 1.45 and 67 ± 6.23 µM, respectively, while thiourea was used as standard for urease inhibition assay with IC 50 value of 21 ± 0.12 µM. (innspub.net)
Acetazolamide modulates the abnormal GABA-A-mediated depolarization that generates epileptic waves and has been shown to block epileptiform activity by inhibiting HCO3 -efflux. (statpearls.com)

Diseases1

Chemicals and Drugs14

Phenomena and Processes1

Inhibitors22

Inhibitory7

Metabolic acidosis1

Reabsorption4

Intraocular pressure7

Inhibitor acetazolamide5

Inhibit5

Effect of acetazolamide6

Potent carbonic anhydrase1

Sulfonamides4

Synthesis6

Isoforms2

Induced metabolic1

Glaucoma2

Enzyme5

Proximal tubule of the nephron1

Decreases3

Diamox1

Methazolamide2

Inhibits2

Administration of acetazolamide2

Carbon dioxide3

Excretion3

Involve inhibition1

Adverse effects1

Epilepsy2

Renal2

Sodium4

Mechanism1

Acid3

Retard abnormal1

Maren1

Dorzolamide1

Physiology1

Climbers2

Neurons1

Cerebral1

Molecular1

Medication1

Acute1

Clinical1

Extended-release capsules1

Tubular1

Activity5