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Chemical Compound Review

Aerolate     1,3-dimethyl-7H-purine-2,6- dione

Synonyms: Afonilum, Sustaire, Theolair, Theonite, Theospan, ...
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Disease relevance of Bronkodyl

  • To determine the role of liver dysfunction in theophylline toxicity, we administered single intravenous doses of the drug to nine patients with cirrhosis and observed its disposition over a period of 24 to 48 hours [1].
  • To assess the effects of theophylline in chronic obstructive pulmonary disease, we conducted a randomized, placebo-controlled, double-blind, crossover trial in 60 patients with severe but stable disease [2].
  • CONCLUSIONS: In patients with stable heart failure, oral theophylline therapy reduced the number of episodes of apnea and hypopnea and the duration of arterial oxyhemoglobin desaturation during sleep [3].
  • Dosage of theophylline in bronchial asthma [4].
  • METHODS: In a double-blind, placebo-controlled trial, we randomly assigned 62 patients to receive either 400 microg of inhaled budesonide (low-dose budesonide) with 250 or 375 mg of theophylline (depending on body weight) or 800 microg of inhaled budesonide (high-dose budesonide) [5].

Psychiatry related information on Bronkodyl


High impact information on Bronkodyl


Chemical compound and disease context of Bronkodyl


Biological context of Bronkodyl


Anatomical context of Bronkodyl


Associations of Bronkodyl with other chemical compounds


Gene context of Bronkodyl

  • Whereas T beta RI levels remained relatively constant, T beta RII expression was strongly induced in TPA-treated skins, prior to the induction of the growth inhibitory response to TGF-beta 1, and its level of expression correlated with growth sensitivity to TGF-beta 1 in vivo and in vitro [30].
  • Nevertheless, cAMP and prostaglandins of the E series in the presence of theophylline induce transcription of the IL-6 promoter more strongly than LPS, suggesting distinctive effects of cAMP and LPS on posttranscriptional events [31].
  • Caffeine and theophylline also inhibit the intrinsic protein kinase activity of the class IA PI3Ks and DNA-dependent protein kinase, although with a much lower potency than that for the lipid kinase (IC(50) approximately 10 mm for p110 alpha, 3 mm for p110 beta, and 10 mm for DNA-dependent protein kinase) [32].
  • Theophylline owes a significant portion of its metabolism to CYP1A2 and can cause gastric acid reflux that calls for concurrent use of proton pump inhibitors [33].
  • The study compared the pharmacokinetics of lansoprazole and theophylline in five white extensive metabolizers, six Korean extensive metabolizers, and seven poor metabolizers of CYP2C19 [33].

Analytical, diagnostic and therapeutic context of Bronkodyl


  1. Theophylline disposition in patients with hepatic cirrhosis. Piafsky, K.M., Sitar, D.S., Rangno, R.E., Ogilvie, R.I. N. Engl. J. Med. (1977) [Pubmed]
  2. A randomized, controlled trial of theophylline in patients with severe chronic obstructive pulmonary disease. Murciano, D., Auclair, M.H., Pariente, R., Aubier, M. N. Engl. J. Med. (1989) [Pubmed]
  3. Effect of theophylline on sleep-disordered breathing in heart failure. Javaheri, S., Parker, T.J., Wexler, L., Liming, J.D., Lindower, P., Roselle, G.A. N. Engl. J. Med. (1996) [Pubmed]
  4. Dosage of theophylline in bronchial asthma. Piafsky, K.M., Ogilvie, R.I. N. Engl. J. Med. (1975) [Pubmed]
  5. A comparison of low-dose inhaled budesonide plus theophylline and high-dose inhaled budesonide for moderate asthma. Evans, D.J., Taylor, D.A., Zetterstrom, O., Chung, K.F., O'Connor, B.J., Barnes, P.J. N. Engl. J. Med. (1997) [Pubmed]
  6. Adenosine receptors and behavioral actions of methylxanthines. Snyder, S.H., Katims, J.J., Annau, Z., Bruns, R.F., Daly, J.W. Proc. Natl. Acad. Sci. U.S.A. (1981) [Pubmed]
  7. Methylxanthine therapy and reversible airway obstruction. McFadden, E.R. Am. J. Med. (1985) [Pubmed]
  8. Concurrent use of theophylline and lithium in a patient with chronic obstructive lung disease and bipolar disorder. Sierles, F.S., Ossowski, M.G. The American journal of psychiatry. (1982) [Pubmed]
  9. Alterations in state in apneic pre-term infants receiving theophylline. Dietrich, J., Krauss, A.N., Reidenberg, M., Drayer, D.E., Auld, P.A. Clin. Pharmacol. Ther. (1978) [Pubmed]
  10. Inhaled salmeterol or oral theophylline in nocturnal asthma? Selby, C., Engleman, H.M., Fitzpatrick, M.F., Sime, P.M., Mackay, T.W., Douglas, N.J. Am. J. Respir. Crit. Care Med. (1997) [Pubmed]
  11. Theophylline and sleep-disordered breathing in heart failure. Goggins, M. N. Engl. J. Med. (1997) [Pubmed]
  12. Effects of theophylline on erythropoietin production in normal subjects and in patients with erythrocytosis after renal transplantation. Bakris, G.L., Sauter, E.R., Hussey, J.L., Fisher, J.W., Gaber, A.O., Winsett, R. N. Engl. J. Med. (1990) [Pubmed]
  13. Ephedrine therapy in asthmatic children. Clinical tolerance and absence of side effects. Tinkelman, D.G., Avner, S.E. JAMA (1977) [Pubmed]
  14. Fluoroquinolones and theophylline toxicity: norfloxacin. Green, L., Clark, J. JAMA (1989) [Pubmed]
  15. Exercise-induced asthma. Pharmacological assessment of single drugs and drug combinations. Bierman, C.W., Pierson, W.E., Shapiro, G.G. JAMA (1975) [Pubmed]
  16. Endotoxin administration to humans inhibits hepatic cytochrome P450-mediated drug metabolism. Shedlofsky, S.I., Israel, B.C., McClain, C.J., Hill, D.B., Blouin, R.A. J. Clin. Invest. (1994) [Pubmed]
  17. Selective killing of oncogenic human cells cocultivated with normal human fibroblasts. Warrington, R.C. J. Natl. Cancer Inst. (1978) [Pubmed]
  18. Pharmacokinetic aspects of theophylline in premature newborns. Aranda, J.V., Sitar, D.S., Parsons, W.D., Loughnan, P.M., Neims, A.H. N. Engl. J. Med. (1976) [Pubmed]
  19. The relation of product formulation to absorption of oral theophylline. Weinberger, M., Hendeles, L., Bighley, L. N. Engl. J. Med. (1978) [Pubmed]
  20. Cyclic AMP-mediated control of lipogenic enzyme synthesis during adipose differentiation of 3T3 cells. Spiegelman, B.M., Green, H. Cell (1981) [Pubmed]
  21. The value of maintenance theophylline in steroid-dependent asthma. Nassif, E.G., Weinberger, M., Thompson, R., Huntley, W. N. Engl. J. Med. (1981) [Pubmed]
  22. Identification of two serum components regulating the expression of T-lymphocyte function in childhood myasthenia gravis. Shore, A., Limatibul, S., Dosch, H.M., Gelfand, E.W. N. Engl. J. Med. (1979) [Pubmed]
  23. Theophylline-induced changes in ion transport and conductance in human small intestinal mucosa. Corbett, C.L., Isaacs, P.E., Hawker, P.C., Turnberg, L.A. Nature (1977) [Pubmed]
  24. Metabolism of theophylline to caffeine in human fetal liver. Aranda, J.V., Louridas, A.T., Vitullo, B.B., Thom, P., Aldridge, A., Haber, R. Science (1979) [Pubmed]
  25. Theophylline restores histone deacetylase activity and steroid responses in COPD macrophages. Cosio, B.G., Tsaprouni, L., Ito, K., Jazrawi, E., Adcock, I.M., Barnes, P.J. J. Exp. Med. (2004) [Pubmed]
  26. Defective beta adrenergic response of cystic fibrosis sweat glands in vivo and in vitro. Sato, K., Sato, F. J. Clin. Invest. (1984) [Pubmed]
  27. Theophylline accelerates human granulocyte apoptosis not via phosphodiesterase inhibition. Yasui, K., Hu, B., Nakazawa, T., Agematsu, K., Komiyama, A. J. Clin. Invest. (1997) [Pubmed]
  28. Adenosine A2b receptors evoke interleukin-8 secretion in human mast cells. An enprofylline-sensitive mechanism with implications for asthma. Feoktistov, I., Biaggioni, I. J. Clin. Invest. (1995) [Pubmed]
  29. Inhibition of vasopressin-stimulated prostaglandin E biosynthesis by chlorpropamide in the toad urinary bladder. Mechanism of enhancement of vasopressin-stimulated water flow. Zusman, R.M., Keiser, H.R., Handler, J.S. J. Clin. Invest. (1977) [Pubmed]
  30. Concerted action of TGF-beta 1 and its type II receptor in control of epidermal homeostasis in transgenic mice. Cui, W., Fowlis, D.J., Cousins, F.M., Duffie, E., Bryson, S., Balmain, A., Akhurst, R.J. Genes Dev. (1995) [Pubmed]
  31. Multiple regulatory elements in the interleukin-6 gene mediate induction by prostaglandins, cyclic AMP, and lipopolysaccharide. Dendorfer, U., Oettgen, P., Libermann, T.A. Mol. Cell. Biol. (1994) [Pubmed]
  32. Direct effects of caffeine and theophylline on p110 delta and other phosphoinositide 3-kinases. Differential effects on lipid kinase and protein kinase activities. Foukas, L.C., Daniele, N., Ktori, C., Anderson, K.E., Jensen, J., Shepherd, P.R. J. Biol. Chem. (2002) [Pubmed]
  33. Theophylline pharmacokinetics are not altered by lansoprazole in CYP2C19 poor metabolizers. Ko, J.W., Jang, I.J., Shin, J.G., Nam, S.K., Shin, S.G., Flockhart, D.A. Clin. Pharmacol. Ther. (1999) [Pubmed]
  34. Management of theophylline intoxication with charcoal-column hemoperfusion. Russo, M.E. N. Engl. J. Med. (1979) [Pubmed]
  35. Effects of theophylline on diaphragmatic strength and fatigue in patients with chronic obstructive pulmonary disease. Murciano, D., Aubier, M., Lecocguic, Y., Pariente, R. N. Engl. J. Med. (1984) [Pubmed]
  36. Theophylline for erythrocytosis after renal transplantation. Beach, R.S., Donlon, D., Escoto, D., McCarthy, J., Napolitano, A., Sosa, R. N. Engl. J. Med. (1990) [Pubmed]
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