A-Carbonic anhydrases

If a carbonic anhydrase inhibitor is being given for absence or nonlocalized epileptic seizures, the nurse assesses the patient at frequent intervals for the occurrence of seizures, especially early in therapy and in patients known to experience seizures at frequent intervals. If a seizure does occur, the nurse records a description of the seizure in the patient s chart, including time of onset and duration. Accurate descriptions of the pattern and the number of seizures occurring each day helps the primary health care provider plan future therapy and adjust drug dosages as needed. 

Bertini, /., Luchinat, C., Scozzafava, A. Carbonic Anhydrase An Insight into the Zinc Binding Site and into the Active Cavity Through Metal Substitution. Vol. 48, pp. 45-91. 

Figure 14.4 Gel image of proteins extracted from a mixed carbonic anhydrase lysozyme tissue surrogate. Lane M, molecular weight marker lane 1, a 1 2 mol ratio mixture of native, non-formalin-treated carbonic anhydrase and lysozyme lane 2, mixed surrogate with 1 2 mol ratio carbonic anhydrase lysozyme, solubilized and retrieved in 20mM Tris-HCl, pH 4.0, with 2% SDS lane 3, mixed surrogate with 1 2 mol ratio carbonic anhydrase lysozyme, solubilized and retrieved in 20mM Tris-HCl, pH 6.0, with 2% SDS. Protein bands corresponding to lysozyme monomer (a), carbonic anhydrase monomer (b), and the putative lysozyme-carbonic anhydrase heterodimer (c) are indicated. For more detail, see Reference 25.

The answer is c. (Hardman, pp 6917 693 J Acetazolamide is a carbonic anhydrase inhibitor with its primary site of action at the proximal tubule of the nephron. Acetazolamide promotes a urinary excretion of Na, K, and bicarbonate There is a decrease in loss of Cl ions The increased excretion of bicarbonate makes the urine alkaline and may produce metabolic acidosis as a consequence of the loss of bicarbonate from the blood. None of the other diuretic drugs promote a reduction in the excretion of the Cl ion... 

Figure 9. A dynamic combinatorial chemistry library used to identify a carbonic anhydrase inhibitor.

Kisker, C., Schindelin, H., Alber, B. E., Ferry, J. G., and Rees, D. C. (1996). A left-hand beta-helix revealed by the crystal structure of a carbonic anhydrase from the archaeon Methanosarcina thermophila. EMBO J. 15, 2323-2330. 

Aromatic sulfonamides are specific inhibitors of carbonic anhydrase (E). The apparent second-order rate constants for association of p-nitrobenzenesulfonamide with (a) carbonic anhydrase-B and (b) the carboxymethylated derivative of the enzyme are shown against pH in Figure 1.14. Estimate using equations (1.225) and (1.226) the values for pAig, and k and he two possible schemes shown for both carbonic... 

Acetazolamide is a carbonic anhydrase inhibitor that reduces aqueous humour production and is therefore indicated in glaucoma to reduce the intraocular pressure. Salbutamol is a selective, short-acting beta2-agonist used as a bronchodilator in asthma. Tolbutamide is a short-acting sulphonylurea used in type 2 (non-insulin dependent) diabetes mellitus. Chlorpromazine is an aliphatic neuroleptic antipsychotic drug used in schizophrenia. Zafirlukast is a leukotriene-receptor antagonist that is indicated in the prophylaxis of asthma but should not be used to relieve acute severe asthma. 

Acetazolamide is a carbonic anhydrase inhibitor, used primarily in glaucoma to reduce aqueous humour production. Acetazolamide may cause blood disorders including agranulocytosis (deficiency of neutrophils) as a side-effect. 

Acetazolamide is a carbonic anhydrase inhibitor, which reduces intraocular pressure by reducing aqueous humour production. It is used in the treatment of glaucoma. Acetazolamide is administered systemically. Recently newer carbonic anhydrase inhibitors have been developed, which are available as topical agents (for example, dorzolamide). 

Acetazolamide is a carbonic anhydrase inhibitor that is administered orally for the treatment of glaucoma. Topical carbonic anhydrase inhibitors include dorzolamide and brinzolamide. Carbonic anhydrase inhibitors reduce the production of aqueous humour, thereby reducing intraocular pressure. They can be used alone or in addition to beta-blocker therapy in glaucoma patients. 

Acetazolamide is an aromatic sulfonamide used as a carbonic anhydrase inhibitor. It facilitates production of alkahne urine with an elevated biocarbonate, sodium, and potassium ion concentrations. By inhibiting carbonic anhydrase, the drug suppresses reabsorption of sodium ions in exchange for hydrogen ions, increases reflux of bicarbonate and sodium ions and reduces reflux of chloride ions. During this process, chloride ions are kept in the kidneys to cover of insufficiency of bicarbonate ions, and for keeping an ion balance. Electrolytic contents of fluid secreted by the kidneys in patients taking carbonic anhydrase inhibitors are characterized by elevated levels of sodium, potassium, and bicarbonate ions and a moderate increase in water level. Urine becomes basic, and the concentration of bicarbonate in the plasma is reduced. 

W.M. Grant and I.H. Leopold, Antiglaucoma Drugs Problems with a Carbonic Anhydrase Inhibition , in Symposium on Ocular Therapy, C.V. Mosby, ed., St. Louis, 1973, pp. 19-38. 

Mechanism of Action A carbonic anhydrase inhibitor that reduces formation of hydrogen and bicarbonate ions from carbon dioxide and water by inhibiting, in proximal renal tubule, the enzyme carbonic anhydrase, thereby promoting renal excretion of sodium, potassium, bicarbonate, and water. Ocular Reduces rate of aqueous humor formation, lowers intraocular pressure. Therapeutic Effect Produces anticonvulsant activity. 

Acetazolamide (a carbonic anhydrase inhibitor) used as diuretic by increasing bicarbonate excretion and thus acidosis occur as side effect which is related to its pharmacological action. 

Alprazolam may also relieve tremor at doses of 0.75 to 3 mg/day (357). Because chronic use can lead to habituation or dependence, alprazolam is best used episodically for patients who require only intermittent tremor reduction to prevent social embarrassment or occupational interference. Methazolamide, a carbonic anhydrase inhibitor, has been reported to reduce hand tremor (at doses of 50 to 300 mg/day) in several open studies ( 358, 359). A controlled trial, however, could not confirm the efficacy of this agent in the treatment of tremor but did report that side effects such as paresthesias, sedation, headache, and gastrointestinal symptoms were common (77, 356). 

FIGURE 7-27. Shown here is an icon of topiramate s pharmacologic actions. By interfering with calcium channels and sodium channels, topiramate is thought both to enhance the inhibitory actions of gamma aminobutyric acid (GABA) and to reduce the excitatory actions of glutamate. Topiramate is also a carbonic anhydrase inhibitor (CAI) and as such has independent anticonvulsant actions. 

Reduction of the sulfur-containing cyclic ketones A and B with (R,R)-39 gives the R alcohols C and D with 99% ee and 98% ee, respectively (Scheme 1.84) [321 ]. The chiral products are important intermediates in the synthesis of MK-0417, which is a carbonic anhydrase inhibitor [325],... 

Carbonic anhydrase inhibitors such as dorzo-lamide (Trusopt) and dichlorphenamide (Daranide) are used to treat glaucoma patients and altitude sickness. Acetazolamide (Diamox), a carbonic anhydrase... 

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