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Chemical Compound Review

Diacarb     N-(5-sulfamoyl-1,3,4- thiadiazol-2...

Synonyms: Diuramide, Glauconox, Glaupax, Acetazolam, Diamox, ...
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Disease relevance of Diacarb


Psychiatry related information on Diacarb


High impact information on Diacarb


Chemical compound and disease context of Diacarb


Biological context of Diacarb


Anatomical context of Diacarb

  • Acetazolamide, in a dose sufficient to inhibit the erythrocyte carbonic anhydrase (EC, thus induced a rapid and marked increase in CBF, leaving CMRO2 unchanged [23].
  • 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 [23].
  • Absolute reabsorption of bicarbonate was also significantly higher in superficial than in juxtamedullary nephrons after administration of acetazolamide (727 +/- 82 vs. 346 +/- 126 pmol/min; P less than 0.05) [24].
  • Bicarbonate reabsorption that was insensitive to acetazolamide occurred in the superficial and deep loop of Henle and between the distal tubule and base collecting duct [25].
  • Blocking the carbonic anhydrase with acetazolamide (100 mg/kg) completely prevented the protective effect of a 1 M HCO3- infusion, and 6 out of 8 stomachs ulcerated [26].

Associations of Diacarb with other chemical compounds

  • Thus, acetazolamide caused either inhibition or stimulation of Na+ uptake depending on the conditions with respect to pH and HCO3- gradients [27].
  • Furthermore, an outwardly directed bicarbonate concentration gradient from the deep loop of Henle to vasa recta was demonstrated during acetazolamide (delta tCO2 = 20.9 +/- 3.3 mM), but was abolished during combined mannitol and acetazolamide administration (delta tCO2 = 3.5 +/- 0.9 mM) [25].
  • In addition, acetazolamide may potentiate the phosphaturic effect of parathyroid hormone by promoting accumulation of cyclic AMP in tissue [28].
  • Addition of forskolin stimulated an increase in short-circuit current that was likely a result of bicarbonate secretion because it was inhibited by a HCO3(-)-free solution, by addition of the carbonic anhydrase inhibitor, acetazolamide, or by mucosal addition of the anion channel blocker, diphenylamine 2-carboxylate [29].
  • The reaction depends upon the trapping of OH ions produced during gastric stimulation and is blocked by the benzimidazole, Hassle 149/94, which inhibits the K+ + H+-ATPase and by acetazolamide, an inhibitor of carbonic anhydrase activity [30].

Gene context of Diacarb

  • Some remarkable clinical features were observed in a large hypoPP family carrying an SCN4A mutation: a complete penetrance in men and women, an early age at onset, postcritic myalgias and an increased number and severity of attacks induced by acetazolamide [31].
  • Similar to CA VA, CA VB is a "low activity" enzyme with a sensitivity to acetazolamide [32].
  • The valproyl derivative of acetazolamide (5-valproylamido-1,3,4-thiadiazole-2-sulfonamide, 6M) was one of the best hCA I and hCA II inhibitor in the series and exhibited very strong anticonvulsant properties in an MES test in mice [33].
  • The isoenzyme CA III, which is resistant to inhibition by sulfonamides, did not appear to be present in these ocular tissues, since the histochemical staining of enzyme activity was completely abolished by 10(-6) M acetazolamide [34].
  • Cerebral perfusion reserve was obtained from 6 patients (3 MELAS, 1 MERRF, 1 KSS, 1 CCOD) for a comparative analysis using the split-dose 123I-IMP SPECT method before and after the injection of acetazolamide [35].

Analytical, diagnostic and therapeutic context of Diacarb


  1. Effect of acetazolamide on hypoxemia during sleep at high altitude. Sutton, J.R., Houston, C.S., Mansell, A.L., McFadden, M.D., Hackett, P.M., Rigg, J.R., Powles, A.C. N. Engl. J. Med. (1979) [Pubmed]
  2. Letter: Anticonvulsants, acetazolamide and osteomalacia. Mallette, L.E. N. Engl. J. Med. (1975) [Pubmed]
  3. Acute mountain sickness and acetazolamide. Clinical efficacy and effect on ventilation. Larson, E.B., Roach, R.C., Schoene, R.B., Hornbein, T.F. JAMA (1982) [Pubmed]
  4. Acute metabolic alkalosis perpetuating hypercarbia. A role for acetazolamide in chronic obstructive pulmonary disease. Miller, P.D., Berns, A.S. JAMA (1977) [Pubmed]
  5. Responses to hypercarbia induced by acetazolamide in panic disorder patients. Mathew, R.J., Wilson, W.H., Tant, S. The American journal of psychiatry. (1989) [Pubmed]
  6. Cerebral hemodynamics in CADASIL before and after acetazolamide challenge assessed with MRI bolus tracking. Chabriat, H., Pappata, S., Ostergaard, L., Clark, C.A., Pachot-Clouard, M., Vahedi, K., Jobert, A., Le Bihan, D., Bousser, M.G. Stroke (2000) [Pubmed]
  7. Toxic interaction between acetazolamide and salicylate: case reports and a pharmacokinetic explanation. Sweeney, K.R., Chapron, D.J., Brandt, J.L., Gomolin, I.H., Feig, P.U., Kramer, P.A. Clin. Pharmacol. Ther. (1986) [Pubmed]
  8. The effect of acetazolamide on essential tremor: an open-label trial. Busenbark, K., Pahwa, R., Hubble, J., Koller, W. Neurology (1992) [Pubmed]
  9. Resting and acetazolamide-challenged technetium-99m-ECD SPECT in transient global amnesia. Takeuchi, R., Yonekura, Y., Matsuda, H., Nishimura, Y., Tanaka, H., Ohta, H., Sakahara, H., Konishi, J. J. Nucl. Med. (1998) [Pubmed]
  10. Sacrococcygeal teratoma in a neonate. Association with maternal use of acetazolamide. Worsham, F., Beckman, E.N., Mitchell, E.H. JAMA (1978) [Pubmed]
  11. A mouse model of episodic ataxia type-1. Herson, P.S., Virk, M., Rustay, N.R., Bond, C.T., Crabbe, J.C., Adelman, J.P., Maylie, J. Nat. Neurosci. (2003) [Pubmed]
  12. Luminal vasopressin modulates transport in the rabbit cortical collecting duct. Ando, Y., Tabei, K., Asano, Y. J. Clin. Invest. (1991) [Pubmed]
  13. Variations of gastric transmucosal potential difference and lesion formation during hemorrhagic shock in the rat. Takeuchi, K., Ohno, T., Okabe, S. Gastroenterology (1986) [Pubmed]
  14. The effect of acetazolamide on ventilation in panic disorder patients. Gorman, J.M., Papp, L.A., Coplan, J., Martinez, J., Liebowitz, M.R., Klein, D.F. The American journal of psychiatry. (1993) [Pubmed]
  15. A randomized trial of dexamethasone and acetazolamide for acute mountain sickness prophylaxis. Ellsworth, A.J., Larson, E.B., Strickland, D. Am. J. Med. (1987) [Pubmed]
  16. Is impaired cerebral vasomotor reactivity a predictive factor of stroke in asymptomatic patients? Gur, A.Y., Bova, I., Bornstein, N.M. Stroke (1996) [Pubmed]
  17. The effect of ergotamine and dihydroergotamine on cerebral blood flow in man. Andersen, A.R., Tfelt-Hansen, P., Lassen, N.A. Stroke (1987) [Pubmed]
  18. Acetazolamide in the treatment of acute mountain sickness: clinical efficacy and effect on gas exchange. Grissom, C.K., Roach, R.C., Sarnquist, F.H., Hackett, P.H. Ann. Intern. Med. (1992) [Pubmed]
  19. Mapping the gene for acetazolamide responsive hereditary paryoxysmal cerebellar ataxia to chromosome 19p. von Brederlow, B., Hahn, A.F., Koopman, W.J., Ebers, G.C., Bulman, D.E. Hum. Mol. Genet. (1995) [Pubmed]
  20. Acetazolamide opens the muscular KCa2+ channel: a novel mechanism of action that may explain the therapeutic effect of the drug in hypokalemic periodic paralysis. Tricarico, D., Barbieri, M., Camerino, D.C. Ann. Neurol. (2000) [Pubmed]
  21. Active transport of methotrexate from cerebrospinal fluid in humans. Bode, U., Magrath, I.T., Bleyer, W.A., Poplack, D.G., Glaubiger, D.L. Cancer Res. (1980) [Pubmed]
  22. The esterase activity of bovine carbonic anhydrase B above pH 9. Reversible and cooalent inhibition by acetozolamide. Wells, J.W., Kandel, S.I., Kandel, M., Gornall, A.G. J. Biol. Chem. (1975) [Pubmed]
  23. Effect of acetazolamide on cerebral blood flow and cerebral metabolic rate for oxygen. Vorstrup, S., Henriksen, L., Paulson, O.B. J. Clin. Invest. (1984) [Pubmed]
  24. Internephron heterogeneity for carbonic anhydrase-independent bicarbonate reabsorption in the rat. Frommer, J.P., Laski, M.E., Wesson, D.E., Kurtzman, N.A. J. Clin. Invest. (1984) [Pubmed]
  25. Effect of carbonic anhydrase inhibition on superficial and deep nephron bicarbonate reabsorption in the rat. DuBose, T.D., Lucci, M.S. J. Clin. Invest. (1983) [Pubmed]
  26. The relative importance of HCO3- and blood flow in the protection of rat gastric mucosa during shock. Starlinger, M., Jakesz, R., Matthews, J.B., Yoon, C., Schiessel, R. Gastroenterology (1981) [Pubmed]
  27. Effects of acetazolamide on Na+-HCO-3 cotransport in basolateral membrane vesicles isolated from rabbit renal cortex. Soleimani, M., Aronson, P.S. J. Clin. Invest. (1989) [Pubmed]
  28. Mechanism of resistance to the phosphaturic effect of the parathyroid hormone in the hamster. Knox, F.G., Preiss, J., Kim, J.K., Dousa, T.P. J. Clin. Invest. (1977) [Pubmed]
  29. cAMP stimulates bicarbonate secretion across normal, but not cystic fibrosis airway epithelia. Smith, J.J., Welsh, M.J. J. Clin. Invest. (1992) [Pubmed]
  30. Action of gastrin in guinea pig oxyntic cells. Studies using quantitative cytochemistry. Heldsinger, A.A., Vinik, A.I. J. Clin. Invest. (1984) [Pubmed]
  31. Hypokalaemic periodic paralysis type 2 caused by mutations at codon 672 in the muscle sodium channel gene SCN4A. Sternberg, D., Maisonobe, T., Jurkat-Rott, K., Nicole, S., Launay, E., Chauveau, D., Tabti, N., Lehmann-Horn, F., Hainque, B., Fontaine, B. Brain (2001) [Pubmed]
  32. Human mitochondrial carbonic anhydrase VB. cDNA cloning, mRNA expression, subcellular localization, and mapping to chromosome x. Fujikawa-Adachi, K., Nishimori, I., Taguchi, T., Onishi, S. J. Biol. Chem. (1999) [Pubmed]
  33. Carbonic anhydrase inhibitors: anticonvulsant sulfonamides incorporating valproyl and other lipophilic moieties. Masereel, B., Rolin, S., Abbate, F., Scozzafava, A., Supuran, C.T. J. Med. Chem. (2002) [Pubmed]
  34. Carbonic anhydrase isoenzymes CA I and CA II in the human eye. Wistrand, P.J., Schenholm, M., Lönnerholm, G. Invest. Ophthalmol. Vis. Sci. (1986) [Pubmed]
  35. SPECT findings in mitochondrial encephalomyopathy. Watanabe, Y., Hashikawa, K., Moriwaki, H., Oku, N., Seike, Y., Kodaka, R., Ono, J., Uehara, T., Kusuoka, H., Nishimura, T. J. Nucl. Med. (1998) [Pubmed]
  36. Distal tubule bicarbonate accumulation in vivo. Effect of flow and transtubular bicarbonate gradients. Iacovitti, M., Nash, L., Peterson, L.N., Rochon, J., Levine, D.Z. J. Clin. Invest. (1986) [Pubmed]
  37. Effects of carbonic anhydrase inhibition on ventilation-perfusion matching in the dog lung. Swenson, E.R., Robertson, H.T., Hlastala, M.P. J. Clin. Invest. (1993) [Pubmed]
  38. Effect of acute hypercapnia on renal and proximal tubular total carbon dioxide reabsorption in the acetazolamide-treated rat. Winaver, J., Walker, K.A., Kunau, R.T. J. Clin. Invest. (1986) [Pubmed]
  39. The incidence, importance, and prophylaxis of acute mountain sickness. Hackett, P.H., Rennie, D. Lancet (1976) [Pubmed]
  40. Noninvasive evaluation of intrarenal oxygenation with BOLD MRI. Prasad, P.V., Edelman, R.R., Epstein, F.H. Circulation (1996) [Pubmed]
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