Of the three classes of bronchodilators (2-adrenergicreceptoragonists, methylxanthines, and anticholinergic agents), the2-adrenergicreceptor agonists produce the greatest bronchodilationin patients with bronchial asthma.12-Adrenergic agonists aregenerally preferred both for the relief of acute symptoms2,3and for the prevention of exercise-induced bronchospasm.4 Therecent introduction of long-acting inhaled 2-adrenergic agonistshas overcome the principal shortcoming of the previously availabledrugs of this class, their limited duration of action. However,the possibility of adverse effects with regular use of 2-adrenergicagonists has been raised.5,6,7 In this article I shall reviewthe pharmacology of the 2-adrenergic agonists, examine potentialadverse . . . [Full Text of this Article]
The 2-Adrenergic Receptor
Classes of 2-Adrenergic Agonists
Routes of Administration
Non-Bronchodilator Actions of the 2-Adrenergic Agonists
Potential Adverse Reactions to 2-Adrenergic Agonists
Side Effects Due to Pharmacologic Actions of the Drugs
Side Effects That May Occur with Long-Term Administration
Tolerance of 2-Adrenergic Agonists
Loss of Protection against Bronchoconstrictive Stimuli
Bronchial Hyperresponsiveness
Possible Mechanisms of the Adverse Effects of 2-Adrenergic Agonists
Clinical Problems Associated with 2-Adrenergic Agonists
Overview of Therapy
Regular Use of 2-Adrenergic Agonists
Long-Acting 2-Adrenergic Bronchodilators
Special Considerations in the Clinical Use of 2-Adrenergic Agonists
Conclusions
Source Information
From the Department of Medicine, National Jewish Center for Immunology and Respiratory Medicine, 1400 Jackson St., Denver, CO 80206, where reprint requests should be addressed to Dr. Nelson.
References
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Montuschi, P., Pagliari, G., Fuso, L.
(2009). Pharmacotherapy of asthma: regular treatment or on demand?. Ther Adv Respir Dis
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[Abstract]
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(2009). Asthma. NEJM
360: 1002-1014
[Full Text]
Beasley, R., Martinez, F. D., Hackshaw, A., Rabe, K. F., Sterk, P. J., Djukanovic, R.
(2009). Safety of long-acting {beta}-agonists: urgent need to clear the air remains. Eur Respir J
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[Full Text]
Metzger, N. L, Kockler, D. R, Gravatt, L. A. H.
(2008). Confirmed {beta}16 Arg/Arg Polymorphism in a Patient with Uncontrolled Asthma. The Annals of Pharmacotherapy
42: 874-881
[Abstract][Full Text]
Choudhry, S., Seibold, M. A., Borrell, L. N., Tang, H., Serebrisky, D., Chapela, R., Rodriguez-Santana, J. R., Avila, P. C., Ziv, E., Rodriguez-Cintron, W., Risch, N. J., Burchard, E. G.
(2007). Dissecting Complex Diseases in Complex Populations: Asthma in Latino Americans. Proc Am Thorac Soc
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[Abstract][Full Text]
Wechsler, M. E., Lehman, E., Lazarus, S. C., Lemanske, R. F. Jr., Boushey, H. A., Deykin, A., Fahy, J. V., Sorkness, C. A., Chinchilli, V. M., Craig, T. J., DiMango, E., Kraft, M., Leone, F., Martin, R. J., Peters, S. P., Szefler, S. J., Liu, W., Israel, E., for the National Heart Lung and Blood Institute's,
(2006). beta-Adrenergic Receptor Polymorphisms and Response to Salmeterol. Am. J. Respir. Crit. Care Med.
173: 519-526
[Abstract][Full Text]
Spooner, L. M, Olin, J. L
(2005). Paradoxical Bronchoconstriction with Albuterol Administered by Metered-Dose Inhaler and Nebulizer Solution. The Annals of Pharmacotherapy
39: 1924-1927
[Abstract][Full Text]
Choudhry, S., Ung, N., Avila, P. C., Ziv, E., Nazario, S., Casal, J., Torres, A., Gorman, J. D., Salari, K., Rodriguez-Santana, J. R., Toscano, M., Sylvia, J. S., Alioto, M., Castro, R. A., Salazar, M., Gomez, I., Fagan, J. K., Salas, J., Clark, S., Lilly, C., Matallana, H., Selman, M., Chapela, R., Sheppard, D., Weiss, S. T., Ford, J. G., Boushey, H. A., Drazen, J. M., Rodriguez-Cintron, W., Silverman, E. K., Burchard, E. G., on behalf of the Genetics of Asthma in Latino Amer,
(2005). Pharmacogenetic Differences in Response to Albuterol between Puerto Ricans and Mexicans with Asthma. Am. J. Respir. Crit. Care Med.
171: 563-570
[Abstract][Full Text]
Harvey, J. S., Howe, J. R., Lynch, A. M., Rees, R. W.
(2005). The results of five coded compounds: genistein, metaproterenol, rotenone, p-anisidine and resorcinol tested in the pH 6.7 Syrian hamster embryo cell morphological transformation assay. Mutagenesis
20: 51-56
[Abstract][Full Text]
Whitsett, J. A., Bachurski, C. J., Barnes, K. C., Bunn, P. A. Jr., Case, L. M., Cook, D. N., Crooks, D., Duncan, M. W., Dwyer-Nield, L., Elston, R. C., Fessler, M. B., Franklin, W. A., Friedman, N., Garcia, J. G. N., Geraci, M. W., Glasgow, C., Glasser, S. W., Hardie, W. D., Henning, L. M., Johnson, G. L., Kawkitinarong, K., Keith, R. L., Korfhagen, T. R., Leikauf, G. D., Liggett, S. B., Malcolm, K. C., Malkinson, A. M., Mariani, T. J., McDowell, S. A., McGraw, D. W., Medvedovic, M., Moss, J., Nogee, L. M., Nonas, S., Pacheco-Rodriguez, G., Palmer, L. J., Peters, D. G., Prows, D. R., Redline, S., Regev, A., Sartor, M. A., Schwartz, D. A., Silverman, E. K., Steagall, W. K., Stearman, R. S., Taveira-DaSilva, A., Tichelaar, J. W., Tomlinson, C. R., Tsukada, K., Weaver, T. E., Wert, S. E., Wesselkamper, S. C., Worthen, G. S., Xu, Y., Zerbe, L., Zhang, Y., Zhang, Y., Choi, A. M. K., Kaminski, N.
(2004). Functional Genomics of Lung Disease. Am. J. Respir. Cell Mol. Bio.
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101: 4948-4953
[Abstract][Full Text]
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(2004). Lower Bronchodilator Responsiveness in Puerto Rican than in Mexican Subjects with Asthma. Am. J. Respir. Crit. Care Med.
169: 386-392
[Abstract][Full Text]
Jenkins, C.
(2003). Formoterol as relief medication in asthma: the jury is still out. Eur Respir J
22: 723-724
[Full Text]
Green, R H, Brightling, C E, Pavord, I D, Wardlaw, A J
(2003). Management of asthma in adults: current therapy and future directions. Postgrad. Med. J.
79: 259-267
[Abstract][Full Text]
Prieto, L., Gutierrez, V., Torres, V., Uixera, S., Marin, J.
(2002). Effect of Salmeterol on Seasonal Changes in Airway Responsiveness and Exhaled Nitric Oxide in Pollen-Sensitive Asthmatic Subjects*. Chest
122: 798-805
[Abstract][Full Text]
Hanania, N. A., Sharafkhaneh, A., Barber, R., Dickey, B. F.
(2002). {beta}-Agonist Intrinsic Efficacy: Measurement and Clinical Significance. Am. J. Respir. Crit. Care Med.
165: 1353-1358
[Full Text]
Nightingale, J. A., Rogers, D. F., Barnes, P. J.
(2002). Comparison of the Effects of Salmeterol and Formoterol in Patients With Severe Asthma*. Chest
121: 1401-1406
[Abstract][Full Text]
Kelly, H. W.
(2001). The Management of Acute Severe Asthma. Journal of Pharmacy Practice
14: 91-107
[Abstract]
Grootendorst, D.C., Sterk, P.J., Heijerman, H.G.M.
(2001). Effect of oral prednisolone on the bronchoprotective effect of formoterol in patients with persistent asthma. Eur Respir J
17: 374-379
[Abstract][Full Text]
NIU, T., ROGUS, J. J., CHEN, C., WANG, B., YANG, J., FANG, Z., WEISS, S. T., XU, X.
(2000). Familial Aggregation of Bronchodilator Response . A Community-Based Study. Am. J. Respir. Crit. Care Med.
162: 1833-1837
[Abstract][Full Text]
ISRAEL, E., DRAZEN, J. M., LIGGETT, S. B., BOUSHEY, H. A., CHERNIACK, R. M., CHINCHILLI, V. M., COOPER, D. M., FAHY, J. V., FISH, J. E., FORD, J. G., KRAFT, M., KUNSELMAN, S., LAZARUS, S. C., LEMANSKE, R. F. Jr., MARTIN, R. J., MCLEAN, D. E., PETERS, S. P., SILVERMAN, E. K., SORKNESS, C. A., SZEFLER, S. J., WEISS, S. T., YANDAVA, C. N.
(2000). The Effect of Polymorphisms of the beta 2-Adrenergic Receptor on the Response to Regular Use of Albuterol in Asthma. Am. J. Respir. Crit. Care Med.
162: 75-80
[Abstract][Full Text]
BOUSQUET, J., JEFFERY, P. K., BUSSE, W. W., JOHNSON, M., VIGNOLA, A. M.
(2000). Asthma . From Bronchoconstriction to Airways Inflammation and Remodeling. Am. J. Respir. Crit. Care Med.
161: 1720-1745
[Full Text]
Milgrom, H., Taussig, L. M.
(1999). Keeping Children With Exercise-induced Asthma Active. Pediatrics
104
: e38-e38
[Abstract][Full Text]
Groeben, H., Emala, C.
(1999). Is {beta}-Adrenergic-Mediated Airway Relaxation of Salmeterol Antagonized by Its Solvent Xinafoic Acid?. Chest
115: 1678-1683
[Abstract][Full Text]
NIGHTINGALE, J. A., ROGERS, D. F., BARNES, P. J.
(1999). Differential Effect of Formoterol on Adenosine Monophosphate and Histamine Reactivity in Asthma. Am. J. Respir. Crit. Care Med.
159: 1786-1790
[Abstract][Full Text]
SZCZEKLIK, A., DWORSKI, R., MASTALERZ, L., PROKOP, A., SHELLER, J. R., NIZANKOWSKA, E., CMIEL, A., OATES, J. A.
(1998). Salmeterol Prevents Aspirin-induced Attacks of Asthma and Interferes with Eicosanoid Metabolism. Am. J. Respir. Crit. Care Med.
158: 1168-1172
[Abstract][Full Text]
CHEUNG, D., WEVER, A. M. J., de GOEIJ, J. A., de GRAAFF, C. S., STEEN, H., STERK, P. J.
(1998). Effects of Theophylline on Tolerance to the Bronchoprotective Actions of Salmeterol in Asthmatics In Vivo. Am. J. Respir. Crit. Care Med.
158: 792-796
[Abstract][Full Text]
Martin, R. M, Dunn, N. R, Freemantle, S. N, Mann, R. D
(1998). Risk of non-fatal cardiac failure and ischaemic heart disease with long acting beta 2 agonists. Thorax
53: 558-562
[Abstract][Full Text]
Peebles, R. S. Jr., Permutt, S., Togias, A.
(1998). Rapid reversibility of the allergen-induced pulmonary late-phase reaction by an intravenous beta 2-agonist. J. Appl. Physiol.
84: 1500-1505
[Abstract][Full Text]
Ferris, T. G., Saglam, D., Stafford, R. S., Causino, N., Starfield, B., Culpepper, L., Blumenthal, D.
(1998). Changes in the Daily Practice of Primary Care for Children. Arch Pediatr Adolesc Med
152: 227-233
[Abstract][Full Text]
Lemanske, R. F. Jr, Busse, W. W.
(1997). Asthma. JAMA
278: 1855-1873
[Abstract]
Taylor, D., Jensen, M., Aikman, S., Harris, J., Barnes, P., O'Connor, B.
(1997). Comparison of salmeterol and albuterol-induced bronchoprotection against adenosine monophosphate and histamine in mild asthma. Am. J. Respir. Crit. Care Med.
156: 1731-1737
[Abstract][Full Text]
YATES, D. H., WORSDELL, M., BARNES, P. J.
(1997). Effect of Regular Salmeterol Treatment on Albuterol-induced Bronchoprotection in Mild Asthma. Am. J. Respir. Crit. Care Med.
156: 988-991
[Abstract][Full Text]
Carlstedt, B. C.
(1997). Pharmacotherapy of Asthma. Journal of Pharmacy Practice
10: 147-164
[Abstract]
Drazen, J. M., Israel, E., Boushey, H. A., Chinchilli, V. M., Fahy, J. V., Fish, J. E., Lazarus, S. C., Lemanske, R. F., Martin, R. J., Peters, S. P., Sorkness, C., Szefler, S. J., The National Heart Lung andBlood Institute's Asthm,
(1996). Comparison of Regularly Scheduled with As-Needed Use of Albuterol in Mild Asthma. NEJM
335: 841-847
[Abstract][Full Text]