Carbonic Anhydrase Inhibitors
Carbonic Anhydrase II
Carbonic Anhydrase III
Carbonic Anhydrase I
Carbonic Anhydrase V
Does gill boundary layer carbonic anhydrase contribute to carbon dioxide excretion: a comparison between dogfish (Squalus acanthias) and rainbow trout (Oncorhynchus mykiss). (1/420)In vivo experiments were conducted on spiny dogfish (Squalus acanthias) and rainbow trout (Oncorhynchus mykiss) in sea water to determine the potential role of externally oriented or gill boundary layer carbonic anhydrase in carbon dioxide excretion. This was accomplished by assessing pH changes in expired water using a stopped-flow apparatus. In dogfish, expired water was in acid-base disequilibrium as indicated by a pronounced acidification (delta pH=-0.11+/-0.01; N=22; mean +/- s.e.m.) during the period of stopped flow; inspired water, however, was in acid-base equilibrium (delta pH=-0.002+/-0.01; N=22). The acid-base disequilibrium in expired water was abolished (delta pH=-0.005+/-0.01; N=6) by the addition of bovine carbonic anhydrase (5 mg l-1) to the external medium. Addition of the carbonic anhydrase inhibitor acetazolamide (1 mmol l-1) to the water significantly reduced the magnitude of the pH disequilibrium (from -0.133+/-0.03 to -0.063+/-0.02; N=4). However, after correcting for the increased buffering capacity of the water caused by acetazolamide, the acid-base disequilibrium during stopped flow was unaffected by this treatment (control delta [H+]=99.8+/-22.8 micromol l-1; acetazolamide delta [H+]=81.3+/-21.5 micromol l-1). In rainbow trout, expired water displayed an acid-base disequilibrium (delta pH=0.09+/-0.01; N=6) that also was abolished by the application of external carbonic anhydrase (delta pH=0.02+/-0.01). The origin of the expired water acid-base disequilibrium was investigated further in dogfish. Intravascular injection of acetazolamide (40 mg kg-1) to inhibit internal carbonic anhydrase activity non-specifically and thus CO2 excretion significantly diminished the extent of the expired water disequilibrium pH after 30 min (from -0.123+/-0.01 to -0.065+/-0.01; N=6). Selective inhibition of extracellular carbonic anhydrase activity using a low intravascular dose (1.3 mg kg-1) of the inhibitor benzolamide caused a significant reduction in the acid-base disequilibrium after 5 min (from -0.11+/-0.01 to -0.07+/-0. 01; N=14). These results demonstrate that the expired water acid-base disequilibrium originates, at least in part, from excretory CO2 and that extracellular carbonic anhydrase in dogfish may have a significant role in carbon dioxide excretion. However, externally oriented carbonic anhydrase (if present in dogfish) plays no role in catalysing the hydration of the excretory CO2 in water flowing over the gills and thus is unlikely to facilitate CO2 excretion. (+info)
Synaptic activation of GABAA receptors induces neuronal uptake of Ca2+ in adult rat hippocampal slices. (2/420)Synaptically evoked transmembrane movements of Ca2+ in the adult CNS have almost exclusively been attributed to activation of glutamate receptor channels and the consequent triggering of voltage-gated calcium channels (VGCCs). Using microelectrodes for measuring free extracellular Ca2+ ([Ca2+]o) and extracellular space (ECS) volume, we show here for the first time that synaptic stimulation of gamma-aminobutyric acid-A (GABAA) receptors can result in a decrease in [Ca2+]o in adult rat hippocampal slices. High-frequency stimulation (100-200 Hz, 0.4-0.5 s) applied in stratum radiatum close (+info)
Modulation of chloride, potassium and bicarbonate transport by muscarinic receptors in a human adenocarcinoma cell line. (3/420)1. Short-circuit current (I(SC)) responses to carbachol (CCh) were investigated in Colony 1 epithelia, a subpopulation of the HCA-7 adenocarcinoma cell line. In Krebs-Henseleit (KH) buffer, CCh responses consisted of three I(SC) components: an unusual rapid decrease (the 10 s spike) followed by an upward spike at 30 s and a slower transient increase (the 2 min peak). This response was not potentiated by forskolin; rather, CCh inhibited cyclic AMP-stimulated I(SC). 2. In HCO3- free buffer, the decrease in forskolin-elevated I(SC) after CCh was reduced, although the interactions between CCh and forskolin remained at best additive rather than synergistic. When Cl- anions were replaced by gluconate, both Ca2+- and cyclic AMP-mediated electrogenic responses were significantly inhibited. 3. Basolateral Ba2+ (1-10 mM) and 293B (10 microM) selectively inhibited forskolin stimulation of I(SC), without altering the effects of CCh. Under Ba2+- or 293B-treated conditions, CCh responses were potentiated by pretreatment with forskolin. 4. Basolateral charybdotoxin (50 nM) significantly increased the size of the 10 s spike of CCh responses in both KH and HCO3- free medium, without affecting the 2 min peak. The enhanced 10 s spike was inhibited by prior addition of 5 mM apical Ba2+. Charybdotoxin did not affect forskolin responses. 5. In epithelial layers prestimulated with forskolin, the muscarinic antagonists atropine and 4-diphenylacetoxy-N-methylpiperidine methiodide (4-DAMP, both at 100 nM) abolished subsequent 10 microM CCh responses. Following addition of p-fluoro hexahydro-sila-difenidol (pF-HHSiD, 10 microM) or pirenzepine (1 microM), qualitative changes in the CCh response time-profile also indicated a rightward shift of the agonist concentration-response curve; however, 1 microM gallamine had no effect. These results suggest that a single M3-like receptor subtype mediates the secretory response to CCh. 6. It is concluded that CCh and forskolin activate discrete populations of basolateral K+ channels gated by either Ca2+ or cyclic AMP, but that the Cl- permeability of the apical membrane may limit their combined effects on electrogenic Cl- secretion. In addition, CCh activates a Ba2+-sensitive apical K+ conductance leading to electrogenic K+ transport. Both agents may also modulate HCO3- secretion through a mechanism at least partially dependent on carbonic anhydrase. (+info)
Effects of maternal acetazolamide treatment on body weights and incisor development of the fetal rat. (4/420)The incisor development of fetal rats on gestation day 19 was well correlated with their fetal weights. The number of odontoblasts in the mandibular incisors, an index of incisor development, increased more than that of the maxillary incisors with increase in fetal body weights. Maternal acetazolamide treatments were observed to suppress the mean fetal weight and to retard incisor development. A smaller incisor size, a thinner predentin layer, and fewer odontoblasts were characteristic of the acetazolamide group. There was also a good correlation between the fetal weights and the number of odontoblasts in the acetazolamide group. From these results, we postulated that the retarded incisor development of the fetal rats caused by the maternal acetazolamide treatment was related to their suppressed fetal weights. However, the regression coefficient of the fetal weights and the number of odontoblasts in the acetazolamide group was smaller than that of the vehicle control group. It may indicate that retarded incisor development in response to maternal acetazolamide treatment is to some extent independent of suppressed fetal weight. (+info)
Endogenous pH shifts facilitate spreading depression by effect on NMDA receptors. (5/420)Rapid extracellular alkalinizations accompany normal neuronal activity and have been implicated in the modulation of N-methyl-D-aspartate (NMDA) receptors. Particularly large alkaline transients also occur at the onset of spreading depression (SD). To test whether these endogenous pH shifts can modulate SD, the alkaline shift was amplified using benzolamide, a poorly permeant inhibitor of interstitial carbonic anhydrase. SD was evoked by microinjection of 1.2 M KCl into the CA1 stratum radiatum of rat hippocampal slices and recorded by a proximal double-barreled pH microelectrode and a distal potential electrode. In Ringer solution of pH 7.1 containing picrotoxin (but not at a bath pH of 7.4), addition of 10 microM benzolamide increased the SD alkaline shift from 0.20 +/- 0.07 to 0.38 +/- 0.17 unit pH (means +/- SE). This was correlated with a significant shortening of the latency and an increase in the conduction velocity by 26 +/- 16%. In the presence of the NMDA receptor antagonist DL-2-amino-5-phosphonovaleric acid (APV), benzolamide still amplified the alkaline transient, however, its effect on the SD latency and propagation velocity was abolished. The intrinsic modulation of SD by its alkaline transient may play an important role under focal ischemic conditions by removing the proton block of NMDA receptors where interstitial acidosis would otherwise limit NMDA receptor activity. (+info)
Inhibition of carbonic anhydrase accounts for the direct vascular effects of hydrochlorothiazide. (6/420)Hydrochlorothiazide has been shown to exert direct vasodilator effects by activation of calcium-activated potassium (KCa) channels in human and guinea pig isolated resistance arteries. Since hydrochlorothiazide binds to and inhibits the enzyme carbonic anhydrase and because KCa channel activation is pH sensitive, we investigated the role of intracellular and extracellular carbonic anhydrase in the vascular effects of thiazide diuretics. Small arteries were isolated from guinea pig mesentery and studied by use of a microvascular myograph technique. In some experiments, tone and intracellular pH (pHi) were measured simultaneously with 2', 7'-bis(2-carboxyethyl)-5(6)'-carboxyfluorescein (BCECF-AM). Bendroflumethiazide, a thiazide diuretic with minimal inhibitory effects on carbonic anhydrase, had little effect on noradrenaline-induced tone (16+/-8% relaxation) compared with hydrochlorothiazide (74+/-12% relaxation). In contrast to hydrochlorothiazide, the action of bendroflumethiazide was unaffected by 100 nmol/L charybdotoxin, a selective blocker of KCa channels. All inhibitors of carbonic anhydrase relaxed noradrenaline-induced tone in a concentration-dependent manner, and this effect was blocked by charybdotoxin. Hydrochlorothiazide and the inhibitors of carbonic anhydrase failed to relax tone induced by a depolarizing potassium solution. Acetazolamide and hydrochlorothiazide increased pHi by 0.27+/-0.07 and 0.21+/-0.04, respectively, whereas bendroflumethiazide had a much smaller effect: 0.06+/-0.03. The rise in pHi induced by any agent was not inhibited by charybdotoxin. The vasorelaxant effect of hydrochlorothiazide is shared by other inhibitors of carbonic anhydrase. Inhibitors of carbonic anhydrase, but not bendroflumethiazide, cause intracellular alkalinization, which is associated with KCa channel opening. These data suggest that the vasodilator effect of thiazide diuretics results primarily from inhibition of vascular smooth muscle cell carbonic anhydrase, which results in a rise in pHI, leading to KCa channel activation and vasorelaxation. (+info)
Topical therapies for glaucoma: what family physicians need to know. (7/420)Medication classes historically used in the management of glaucoma include beta blockers, miotics, sympathomimetics and carbonic anhydrase inhibitors. Because topically applied medications are more site specific, they are preferred in the treatment of glaucoma. Compared with oral medications, topical agents are associated with a decreased incidence of systemic side effects. With topical administration, conjunctival and localized skin allergic reactions are relatively common, whereas severe reactions, including death, are rare. Recently introduced topical agents for glaucoma therapy include dorzolamide and brinzolamide, the first topical carbonic anhydrase inhibitors; brimonidine and apraclonidine, more ocular-specific alpha agonists; and latanoprost, a prostaglandin analog, which is a new class of glaucoma medication. Latanoprost has the unique side effect of increasing iris pigmentation. Like their predecessors, the newer agents lower intraocular pressure by a statistically significant degree. Preservation of visual field, the more substantial patient-oriented end point, continues to be studied. (+info)
VCO2 and VE kinetics during moderate- and heavy-intensity exercise after acetazolamide administration. (8/420)The effect of carbonic anhydrase inhibition with acetazolamide (Acz) on CO2 output (VCO2) and ventilation (VE) kinetics was examined during moderate- and heavy-intensity exercise. Seven men [24 +/- 1 (SE) yr] performed cycling exercise during control (Con) and Acz (10 mg/kg body wt iv) sessions. Each subject performed step transitions (6 min) in work rate from 0 to 100 W [below ventilatory threshold (
Carbonic anhydrase inhibitors (CAIs) are a class of drugs that are used to treat a variety of medical conditions, including glaucoma, altitude sickness, and certain types of epilepsy. These drugs work by inhibiting the activity of an enzyme called carbonic anhydrase, which is involved in the production of bicarbonate ions in the body. By inhibiting this enzyme, CAIs can help to lower the production of bicarbonate ions, which can help to reduce the pressure inside the eye in the case of glaucoma, or help to reduce the symptoms of altitude sickness by reducing the body's production of carbon dioxide. CAIs are also sometimes used to treat certain types of epilepsy by reducing the frequency and severity of seizures.
Acetazolamide is a medication that is used to treat a variety of medical conditions, including: 1. High altitude sickness: Acetazolamide is used to prevent and treat altitude sickness, which occurs when a person is exposed to high altitudes and experiences symptoms such as headache, nausea, and dizziness. 2. Glaucoma: Acetazolamide is used to lower the pressure inside the eye in people with glaucoma, a condition in which the pressure inside the eye is too high and can damage the optic nerve. 3. Epilepsy: Acetazolamide is sometimes used as an adjunctive therapy to treat certain types of epilepsy, such as Lennox-Gastaut syndrome. 4. Fluid retention: Acetazolamide is used to treat fluid retention, which can occur in people with heart failure, kidney disease, or other conditions. 5. Acute mountain sickness: Acetazolamide is used to treat acute mountain sickness, which is a condition that occurs when a person is exposed to high altitudes and experiences symptoms such as headache, nausea, and dizziness. Acetazolamide is usually taken by mouth, although it can also be given intravenously in some cases. It works by decreasing the amount of bicarbonate ions in the body, which helps to lower the pressure inside the eye and reduce fluid retention.
Carbonic anhydrases (CAs) are a family of metalloenzymes that catalyze the reversible hydration of carbon dioxide (CO2) to bicarbonate (HCO3-) and a proton (H+). These enzymes are found in a wide variety of organisms, including bacteria, plants, and animals, and play important roles in many physiological processes. In the medical field, CAs are of particular interest because they are involved in several important physiological processes, including respiration, pH regulation, and ion transport. For example, CAs are important in the regulation of blood pH, as they help to maintain the balance of bicarbonate and carbon dioxide in the blood. They are also involved in the transport of ions across cell membranes, and play a role in the formation of certain acids and bases. In addition to their physiological roles, CAs have also been the subject of extensive research in the medical field, as they have been implicated in a number of diseases and conditions, including respiratory acidosis, metabolic acidosis, and certain types of cancer. As a result, CAs have become important targets for the development of new drugs and therapies for these conditions.
Methazolamide is a medication that is used to treat glaucoma, a condition that can cause damage to the optic nerve and lead to vision loss. It is also used to treat fluid buildup in the brain, which can cause swelling and pressure. Methazolamide works by decreasing the production of fluid in the eye or brain, which helps to lower pressure and reduce symptoms. It is usually taken by mouth, but it can also be given as an injection or applied as eye drops. Side effects of methazolamide may include headache, dizziness, nausea, and ringing in the ears. It is important to follow the instructions of your healthcare provider when taking this medication.
Dichlorphenamide is a medication that is used to treat primary polydipsia (excessive thirst) and primary polyuria (excessive urination) in people with central diabetes insipidus. It works by increasing the amount of antidiuretic hormone (ADH) in the body, which helps to regulate the amount of water that is reabsorbed by the kidneys and reduces the amount of urine that is produced. It is usually taken once or twice a day, with or without food.
Ethoxzolamide is a medication that is used to treat glaucoma, a condition in which there is increased pressure in the eye that can damage the optic nerve and lead to vision loss. It is a type of diuretic called a carbonic anhydrase inhibitor, which works by reducing the production of aqueous humor, the clear fluid that fills the space inside the eye. This helps to lower the pressure inside the eye and prevent further damage to the optic nerve. Ethoxzolamide is usually taken by mouth, but it can also be given as an eye drop. It is generally well-tolerated, but like all medications, it can cause side effects, such as dizziness, nausea, and stomach pain.
Benzolamide is a medication that is used to treat glaucoma, a condition that can lead to vision loss and blindness. It works by decreasing the production of aqueous humor, a clear fluid that fills the front part of the eye and helps to maintain its shape. By reducing the production of aqueous humor, benzolamide helps to lower the pressure inside the eye, which can help to prevent further damage to the optic nerve and preserve vision. Benzolamide is available as a prescription medication and is typically taken once or twice a day, either by mouth or as a gel applied to the eye. It is generally well-tolerated, but like all medications, it can cause side effects. Common side effects of benzolamide include headache, dizziness, and dry mouth. More serious side effects are rare, but may include allergic reactions, changes in blood pressure, and difficulty breathing. As with any medication, it is important to talk to your doctor about the potential risks and benefits of benzolamide before starting to take it.
Carbonic anhydrase II (CA II) is an enzyme that plays a crucial role in the body's metabolism of carbon dioxide (CO2) and bicarbonate (HCO3-). It is primarily found in the red blood cells, where it helps to regulate the pH of the blood by converting CO2 into bicarbonate and protons (H+). This process is essential for maintaining the proper balance of acids and bases in the body, which is necessary for the proper functioning of many physiological processes. In addition to its role in regulating blood pH, CA II also plays a role in the transport of CO2 from the tissues to the lungs, where it is exhaled. It does this by converting bicarbonate back into CO2, which can then be transported in the blood to the lungs and exhaled. CA II is also involved in the regulation of fluid balance in the body, as bicarbonate is an important ion that helps to maintain the proper concentration of electrolytes in the blood. It is also involved in the metabolism of other substances, such as ammonia and sulfates. In the medical field, CA II is often studied as a potential target for the treatment of a variety of conditions, including metabolic acidosis, respiratory acidosis, and certain types of cancer. It is also used as a diagnostic marker for certain diseases, such as renal disease and liver disease.
Bicarbonates, also known as bicarbonate ions or HCO3-, are a type of ion found in the blood and other body fluids. They play an important role in regulating the acid-base balance of the body and maintaining the proper pH of the blood. In the medical field, bicarbonate levels are often measured as part of a routine blood test. Abnormal levels of bicarbonate can indicate a variety of medical conditions, including metabolic acidosis (a condition in which the body produces too much acid), metabolic alkalosis (a condition in which the body produces too little acid), and respiratory acidosis (a condition in which the body is not able to remove enough carbon dioxide from the blood). Bicarbonate is also used in medicine to treat certain conditions, such as metabolic acidosis and respiratory acidosis. It is given intravenously (through a vein) or by mouth in the form of a salt, such as sodium bicarbonate.
Thiophenes are a class of organic compounds that contain a five-membered ring with one sulfur atom and two carbon atoms. They are commonly found in a variety of natural and synthetic compounds, including some pharmaceuticals and pesticides. In the medical field, thiophenes are sometimes used as ingredients in drugs to treat a variety of conditions. For example, some thiophene-containing drugs are used to treat high blood pressure, while others are used to treat depression and anxiety. Some thiophenes have also been studied for their potential use in treating cancer. It is important to note that thiophenes can have potential side effects, and their use in medicine is carefully regulated by regulatory agencies such as the U.S. Food and Drug Administration (FDA).
Sulfonamides are a class of synthetic antimicrobial drugs that were first discovered in the 1930s. They are commonly used to treat a variety of bacterial infections, including urinary tract infections, respiratory infections, and skin infections. Sulfonamides work by inhibiting the production of folic acid by bacteria, which is essential for their growth and reproduction. They are often used in combination with other antibiotics to increase their effectiveness. Sulfonamides are generally well-tolerated, but can cause side effects such as nausea, vomiting, and allergic reactions in some people.
Thiadiazoles are a class of heterocyclic compounds that contain a sulfur atom and two nitrogen atoms in a six-membered ring. They are commonly used in the medical field as pharmaceuticals, particularly as antihypertensive agents, diuretics, and antipsychotic drugs. Some examples of drugs containing thiadiazoles include thiazide diuretics (such as hydrochlorothiazide), thiazolidinediones (such as pioglitazone), and atypical antipsychotics (such as clozapine). These drugs have a variety of mechanisms of action and are used to treat a range of conditions, including high blood pressure, diabetes, and schizophrenia.
Carbonic anhydrase III (CA III) is an enzyme that is primarily found in the heart, skeletal muscles, and red blood cells. It plays a crucial role in the regulation of acid-base balance in the body by catalyzing the conversion of carbon dioxide (CO2) to bicarbonate (HCO3-) and protons (H+). This reaction helps to maintain the proper pH levels in the blood and tissues. In the heart, CA III is involved in the regulation of cardiac contractility and the maintenance of the normal electrical activity of the heart. In skeletal muscles, it helps to regulate the pH levels during exercise and helps to maintain the proper function of the muscles. In red blood cells, CA III is involved in the transport of CO2 from the tissues to the lungs for exhalation. Abnormal levels of CA III can be associated with various medical conditions, including muscle disorders, heart disease, and respiratory disorders. In some cases, CA III levels may be used as a diagnostic marker for these conditions.
In the medical field, carbon dioxide (CO2) is a gas that is produced as a byproduct of cellular respiration and is exhaled by the body. It is also used in medical applications such as carbon dioxide insufflation during colonoscopy and laparoscopic surgery, and as a component of medical gases used in anesthesia and respiratory therapy. High levels of CO2 in the blood (hypercapnia) can be a sign of respiratory or metabolic disorders, while low levels (hypocapnia) can be caused by respiratory failure or metabolic alkalosis.
Carbonic anhydrase I (CA I) is an enzyme that catalyzes the reversible hydration of carbon dioxide (CO2) to bicarbonate (HCO3-) and a proton (H+). It is primarily found in red blood cells, where it plays a crucial role in the transport of CO2 from tissues to the lungs for exhalation. In the medical field, CA I is often measured as a biomarker for various diseases and conditions, including renal disease, liver disease, and cancer. Abnormal levels of CA I can indicate impaired kidney function, liver damage, or the presence of certain types of cancer. Additionally, CA I inhibitors are being developed as potential treatments for certain types of cancer and other diseases.
Carbonic Anhydrase IV (CA IV) is an enzyme that is primarily found in the lungs and kidneys. It plays a crucial role in the body's respiratory and excretory systems by catalyzing the conversion of carbon dioxide (CO2) to bicarbonate (HCO3-) and protons (H+). This process is essential for maintaining acid-base balance in the body and facilitating the removal of excess CO2 from the bloodstream. In the lungs, CA IV helps to regulate the pH of the airways and prevent the buildup of excess CO2. In the kidneys, it helps to regulate the pH of the blood and facilitate the excretion of H+ ions. CA IV has also been found to play a role in several other physiological processes, including the regulation of blood pressure, the maintenance of electrolyte balance, and the regulation of fluid balance in the body. In the medical field, CA IV has been studied as a potential therapeutic target for a variety of conditions, including respiratory diseases, kidney disorders, and cardiovascular diseases. For example, drugs that inhibit CA IV have been shown to be effective in treating high blood pressure and other cardiovascular conditions.
Aqueous humor is a clear, colorless fluid that is produced by the ciliary body of the eye. It is a component of the anterior chamber of the eye and plays an important role in maintaining the shape and pressure of the eye. The aqueous humor is constantly being produced and drained from the eye, and its production and drainage are regulated by a number of factors, including the level of light, the amount of physical activity, and the overall health of the eye. Abnormalities in the production or drainage of aqueous humor can lead to a number of eye conditions, including glaucoma.
Timolol is a medication that belongs to a class of drugs called beta blockers. It is primarily used to treat high blood pressure, chest pain (angina), and tremors caused by certain neurological disorders. Timolol works by blocking the effects of adrenaline on the heart and blood vessels, which helps to lower blood pressure and reduce the workload on the heart. It can also slow down the heart rate and reduce the severity and frequency of angina attacks. Timolol is available in both oral and topical forms, and it is generally well-tolerated by most people. However, it may cause side effects such as dizziness, fatigue, and difficulty breathing in some individuals.
Chlorides are a type of anion that are commonly found in the human body. They are produced when chlorine combines with other elements, such as sodium or potassium, to form compounds. In the body, chlorides are primarily found in the fluid that surrounds cells, known as extracellular fluid, and in the fluid that fills the lungs and other cavities, known as intracellular fluid. Chlorides play an important role in maintaining the balance of fluids in the body and in regulating the pH of the blood. They also help to transport nutrients and waste products throughout the body. Chlorides are an essential component of many bodily functions, including the production of hydrochloric acid in the stomach, which aids in the digestion of food. In the medical field, chlorides are often measured as part of a routine blood test to assess the overall health of the body. Abnormal levels of chlorides in the blood can be a sign of a variety of medical conditions, including kidney disease, liver disease, and respiratory disorders.
Glaucoma is a group of eye diseases that damage the optic nerve, which is responsible for transmitting visual information from the eye to the brain. This damage can lead to gradual vision loss and, in severe cases, blindness. There are several types of glaucoma, including open-angle glaucoma, closed-angle glaucoma, and normal-tension glaucoma. Open-angle glaucoma is the most common type and typically affects both eyes. It occurs when the drainage system in the eye becomes blocked, causing increased pressure inside the eye. Closed-angle glaucoma is less common and occurs when the iris blocks the drainage system, causing a sudden increase in eye pressure. Normal-tension glaucoma occurs when the eye pressure is within the normal range, but the optic nerve is still damaged. Symptoms of glaucoma may include blurred vision, eye pain, redness, and sensitivity to light. However, many people with glaucoma have no symptoms until the disease is advanced. That's why regular eye exams are important for early detection and treatment. Treatment for glaucoma typically involves lowering eye pressure with medication, laser therapy, or surgery. The goal of treatment is to slow or stop the progression of the disease and preserve vision.
Sodium is an essential mineral that plays a crucial role in various bodily functions. In the medical field, sodium is often measured in the blood and urine to assess its levels and monitor its balance in the body. Sodium is primarily responsible for regulating the body's fluid balance, which is essential for maintaining blood pressure and proper functioning of the heart, kidneys, and other organs. Sodium is also involved in nerve impulse transmission, muscle contraction, and the production of stomach acid. Abnormal levels of sodium in the body can lead to various medical conditions, including hyponatremia (low sodium levels), hypernatremia (high sodium levels), and dehydration. Sodium levels can be affected by various factors, including diet, medications, and underlying medical conditions. In the medical field, sodium levels are typically measured using a blood test called a serum sodium test or a urine test called a urine sodium test. These tests can help diagnose and monitor various medical conditions related to sodium levels, such as kidney disease, heart failure, and electrolyte imbalances.
Biological transport refers to the movement of molecules, such as nutrients, waste products, and signaling molecules, across cell membranes and through the body's various transport systems. This process is essential for maintaining homeostasis, which is the body's ability to maintain a stable internal environment despite changes in the external environment. There are several mechanisms of biological transport, including passive transport, active transport, facilitated diffusion, and endocytosis. Passive transport occurs when molecules move down a concentration gradient, from an area of high concentration to an area of low concentration. Active transport, on the other hand, requires energy to move molecules against a concentration gradient. Facilitated diffusion involves the use of transport proteins to move molecules across the cell membrane. Endocytosis is a process by which cells take in molecules from the extracellular environment by engulfing them in vesicles. In the medical field, understanding the mechanisms of biological transport is important for understanding how drugs and other therapeutic agents are absorbed, distributed, metabolized, and excreted by the body. This knowledge can be used to design drugs that are more effective and have fewer side effects. It is also important for understanding how diseases, such as cancer and diabetes, affect the body's transport systems and how this can be targeted for treatment.
Carbonic anhydrase V (CA5) is an enzyme that is primarily found in the red blood cells of mammals. It catalyzes the reversible hydration of carbon dioxide (CO2) to bicarbonate (HCO3-) and a proton (H+), which is an important step in the regulation of blood pH and the transport of CO2 from tissues to the lungs for exhalation. CA5 is also involved in the metabolism of ammonia and the regulation of intracellular pH in certain cell types. In the medical field, CA5 has been studied as a potential target for the treatment of various diseases, including respiratory disorders, metabolic acidosis, and certain types of cancer.
Carbonic anhydrase inhibitor
Carbonic anhydrase 9
Carbonic anhydrase 7
Carbonyl sulfide hydrolase
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- Carbonic anhydrase inhibitors (eg, acetazolamide) and loop diuretics (eg, furosemide) are thought to exert their effect on ICP by reducing cerebrospinal fluid (CSF) production at the choroid plexus. (medscape.com)
- Acetazolamide is a nonbacteriostatic sulfonamide and a potent CA inhibitor that is effective in diminishing fluid secretion. (medscape.com)
- Acetazolamide is a carbonic anhydrase (CA) IX inhibitor with an IC50 of 30 nM. (abmole.com)
- In this work we have investigated the effect of 17β-estradiol, an ER activator, and ferulic acid, a carbonic anhydrase inhibitor, as well as ER activator, in the absence and in the presence of the carbonic anhydrase inhibitor acetazolamide on the metabolism of MCF7 cells and MCF7 cells, stably transfected to express HER2 (MCF7HER2). (canada.ca)
- However, the carbonic anhydrase inhibitor acetazolamide had the largest effect on the profile of lipophilic metabolites. (canada.ca)
- Acetazolamide (ACZ) is a carbonic anhydrase inhibitor prescribed for the treatment of various pathologies. (unicam.it)
- Acetazolamide belongs to a class of drugs known as carbonic anhydrase inhibitors. (webmd.com)
- Acetazolamide extended-release capsules are an inhibitor of the enzyme carbonic anhydrase. (nih.gov)
- 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)
- 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 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)
- however, an oral carbonic anhydrase inhibitor such as acetazolamide might be used in patients who exhibit continued intraocular pressure elevation despite topical treatment. (pharmacology2000.com)
- People who have swelling of the retina (macular edema) are given drugs called carbonic anhydrase inhibitors (usually acetazolamide or dorzolamide ) by mouth or as eye drops. (msdmanuals.com)
- 2 We hypothesized that 1) IOPs would differ between fish species, 2) the ophthalmic carbonic anhydrase inhibitor dorzolamide (Trusopt®) would reduce intraocular pressure in normal eyes, and 3) IOPs of exophthalmic eyes would differ from normal eyes. (vin.com)
- Dorzolamide HCl is a water-soluble, potent inhibitor of human carbonic anhydrase II and IV with Ki of 1.9 nM and 31 nM, respectively, used as anti-glaucoma agent. (abmole.com)
- the sulfonamide coxibs (celecoxib, valdecoxib and paricoxib), or the protein kinase inhibitors pazopanib, imatinib and nilotinib, also show significant inhibition of many pharmacologically relevant CA isoforms. (pharmadvances.com)
- This polypharmacology of the CA inhibitors (CAIs) thus affords for novel applications for these drugs, such as for example the antiobesity action of topiramate and zonisamide (thought to be due to inhibition of two mitochondrial CA isoforms) or the antitumor activity of most sulfonamides and also coxibs and kinase inhibitors, which strongly inhibit the tumor-associated isoforms CA IX and XII. (pharmadvances.com)
- Dichlorphenamide is a sulfonamide and a carbonic anhydrase inhibitor of the meta-Disulfamoylbenzene class. (abmole.com)
- All currently used inhibitors anhydrase inhibitors contain a sulfonamide or a sulfamate moiety connected to so-called 'ring structure' which is usually a 5- or 6-membered aromatic ring or conjugated ring system containing nitrogen, oxygen, and/or sulfur heteroatoms. (imtm.cz)
- U-104 is a potent carbonic anhydrase (CA) inhibitor for CA IX and CA XII with K i of 45.1 nM and 4.5 nM, respectively, very low inhibition for CA I and CA II. (abmole.com)
- Inhibition of carbonic anhydrase in this area appears to retard abnormal, paroxysmal, excessive discharge from central nervous system neurons. (nih.gov)
- A class of compounds that reduces the secretion of H+ ions by the proximal kidney tubule through inhibition of CARBONIC ANHYDRASES. (bvsalud.org)
- Comment: Carbonic anhydrase inhibitors (CAIs) and salicylates inhibit each other's renal tubular secretion, resulting in increased plasma levels. (medscape.com)
- There are four types of RTA: classic distal RTA (type I), proximal RTA (type II), hyperkalemic distal RTA (type IV), and a rare combination of proximal and distal RTA caused by carbonic anhydrase II deficiency and carbonic anhydrase inhibitors blocking the metabolism of bicarbonate and carbonic acid (type III). (bmj.com)
- EMAC10101d is a potent and selective toward hCA II inhibitor, with a Ki of 8.1 nM. (abmole.com)
- Girentuximab (G250) is a chimeric monoclonal antibody that binds carbonic anhydrase IX (CAIX), a cell surface glycoprotein ubiquitously expressed in clear cell renal cell carcinoma (ccRCC). (abmole.com)
- We have developed selective CAIX inhibitors with anticancer properties based on carborane scaffold to the structure-assisted design of novel and original inhibitors targeting therapeutically relevant isoenzymes of human carbonic anhydrase. (imtm.cz)
- Selected sulfamides incorporate cluster with inhibitory effects toward CAs (IC50 values in the submicromolar and nanomolar range, some of the inhibitors being more than 50-times more selective toward the tumor-specific CAIX than for CAII abundantly present in normal tissues). (imtm.cz)
- It catalyzes a reversible reaction whereby carbon dioxide becomes hydrated and carbonic acid becomes dehydrated. (medscape.com)
- Carbonic anhydrase (CA) is an enzyme found in many tissues. (medscape.com)
- Risk factors for metformin-associated lactic acidosis include renal impairment, concomitant use of certain drugs (eg, carbonic anhydrase inhibitors such as topiramate ), age 65 years old or greater, having a radiological study with contrast, surgery and other procedures, hypoxic states (eg, acute congestive heart failure), excessive alcohol intake, and hepatic impairment. (medscape.com)
- Epilepsy and belongs to the drug class carbonic anhydrase inhibitor anticonvulsants . (drugs.com)
- One mechanism by which carbonic anhydrase inhibitors could cause adverse effects in fish is by inducing plasma electrolyte imbalances, as has been reported in alewife. (vin.com)
- A single application of the carbonic anhydrase inhibitor did not reduce IOP at either 4 h or 24 h, but neither were any adverse effects of treatment noted by visual examination or plasma electrolytes. (vin.com)
- Cardiovascular Drugs / Antilipemic Agents / HMG-CoA Reductase Inhibitors (i.e. (tevausa.com)
- Carbonic anhydrase inhibitors have been proposed as a potential treatment for gaseous exophthalmia in fish by modifying gas exchange between the pseudobranch and the eye. (vin.com)
- Estrogen receptor (ER) activity has a profound effect on breast cancer cell growth through a number of metabolic changes driven by its effect on transcription of several enzymes, including carbonic anhydrases, Stearoyl-CoA desaturase-1, and oncogenes including HER2. (canada.ca)
- Acetazolamide and methazolamide are carbonic anhydrase inhibitors used as diuretics and in the therapy of glaucoma. (nih.gov)
- The carbonic anhydrase inhibitors methazolamide and acetazolamide have different effects on the hypoxic ventilatory response in the anaesthetized cat. (nih.gov)
- however, an oral carbonic anhydrase inhibitor such as acetazolamide might be used in patients who exhibit continued intraocular pressure elevation despite topical treatment. (pharmacology2000.com)
- 4 Acetazolamide (ACZ) is a carbonic anhydrase inhibitor. (drug-dev.com)
- People who have swelling of the retina (macular edema) are given drugs called carbonic anhydrase inhibitors (usually acetazolamide or dorzolamide ) by mouth or as eye drops. (msdmanuals.com)
- Simbrinza (brimonidine and brinzolamide) is a fixed combination of an alpha 2 adrenergic receptor agonist and a carbonic anhydrase inhibitor indicated for the reduction of elevated intraocular pressure in patients with open-angle glaucoma or ocular hypertension. (drugs.com)
- Intraocular pressure effects of carbonic anhydrase inhibitors in primary open-angle glaucoma. (nih.gov)
- Drug interaction considerations in the therapeutic use of carbonic anhydrase inhibitors. (nih.gov)
- If additional medication is needed to control eye pressure, carbonic anhydrase inhibitors are also prescribed in oral or pill forms. (aphconnectcenter.org)
- Carbonic anhydrase inhibitors reduce the body's uptake of bicarbonate ions and decrease salt absorption, which lowers fluid levels in the body. (aphconnectcenter.org)
- Concomitant administration of oral carbonic anhydrase inhibitors. (who.int)
- Common side effects experienced with carbonic anhydrase inhibitor (CAI) eye drop include burning, a bitter taste, eyelid reactions and eye redness. (allaboutvision.com)
- The results revealed that the inhibitors bind to distinct regions of Mpro COVID-19, with variations in RMSD values from 1.325 to 1.962 Å and binding free energy of -5.2 to -4.3 kcal/mol. (bvsalud.org)
- In hyperkalemic PP, kaliopenic effect of CA inhibitors may be beneficial. (medscape.com)