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Drug Comparisons


Oral Beta-2 Agonists

Like inhaled beta-2 agonists, oral beta-2 agonists activate certain receptors in the lungs. Receptors are specialized places on cells that recognize and attract specific substances that activate the receptors. Activating beta-2 receptors relaxes muscles in the bronchial tubes (airways) and lets more air enter the lungs.

For patients with mild asthma, inhaled beta-2 agonists are typically first-line agents. Short-acting inhaled beta-2 agonists are used more frequently than oral forms of beta-2 agonists because the inhaled products generally provide faster relief, they usually have fewer adverse effects, and they typically are more effective. However, oral beta-2 agonists can be prescribed for patients who cannot use an inhaler or who need prolonged symptom relief (such as during the night).

Drugs in this Class
Albuterol Oral Syrup
Albuterol Oral Tablets
Metaproterenol Tablets
Terbutaline Tablets

Summarizing the Evidence

  • Only a few small studies have compared oral forms of albuterol, metaproterenol, and terbutaline with each other. Mostly conducted several years ago, the studies do not reach firm conclusions about which oral beta-2 agonist may be better than the others. In general, all oral beta-2 agonists are about equally as effective in treating asthma symptoms.
  • One study showed that oral metaproterenol was quicker to provide relief of asthma symptoms, but that oral albuterol and oral terbutaline controlled asthma symptoms for longer periods.
  • Metaproterenol is used less often than albuterol because albuterol is more selective for beta-2 receptors and may be less likely to cause cardiac side effects than metaproterenol.
  • Because they are absorbed systemically (through the bloodstream) rather than going directly to the lungs like inhaled beta-2 agonists do, oral beta-2 agonists have more side effects than inhaled beta-2 agonists.
  • Generally, oral beta-2 agonists have not been as effective as extended-release theophylline for controlling nocturnal (nighttime) asthma symptoms.

Dosing and Administration

  • Albuterol, metaproterenol, and terbutaline are available in immediate-release (short-acting) formulations. Albuterol is also available in an extended-release (long-acting) preparation.
  • Short-acting oral beta-2 agonists can be used for relief of acute asthma symptoms.
  • Compared to inhaled beta-2 agonists, the doses of oral beta-2 agonists needed to control asthma symptoms are relatively higher.
  • Short-acting oral albuterol and metaproterenol are available as tablets or syrup, commonly taken three times or four times daily. Oral terbutaline comes in tablets that usually are taken three times daily.
  • Long-acting formulations of albuterol (marketed as the brand-name products Proventil Repetabs, Volmax, and VoSpire) come as tablets to be taken twice a day. They cannot be used for immediate relief of asthma symptoms. Typically, they are used for long-term prevention of symptoms, especially asthma symptoms that occur at night.

Generic Availability

  • Short-acting albuterol, metaproterenol, and terbutaline are all available as generics.
  • Long-acting albuterol is also available as a generic.

Drug Interactions

Some interactions between medications can be more severe than others. The best way for you to avoid harmful interactions is to tell your doctor and/or pharmacist what medications you are currently taking, including any over-the-counter products, vitamins, and herbals. For specific information on how the drugs interact and the severity of the interaction, please use our Drug Interactions Checker.

Side Effects

To view specific side effect information, please use our Side Effect Checker.

Additional Information

References

Drug Facts & Comparisons. Facts and Comparisons. St. Louis, MO. 2002.

Drugdex Database. In: Gelman CJ, Rumack BH, editors. Denver: Micromedex Inc. 2000.

Grossman J, Morris RJ, White KD, et al. Improved stability in oral delivery of albuterol provides less variability in bronchodilation in adults with asthma. Ann Allergy. 1991;66:324-327.

Heins M, Kurtin L, Oellerich M, Maes R, Sybrecht GW. Nocturnal asthma: slow-release terbutaline versus slow-release theophylline therapy. Eur Respir J. 1988;1(4):306-310.

Hussey EK, Donn KH, Powell JR. Albuterol extended-release products: a comparison of steady-state pharmacokinetics. Pharmacotherapy. 1991;11:131-135.

Kemp JP, Meltzer EO. Beta 2 adrenergic agonists--oral or aerosol for the treatment of asthma? J Asthma. 1990;27(3):149-157.

Legge JS, Gaddie J, Palmer KN. Comparison of two oral selective beta2-adrenergic stimulant drugs in bronchial asthma. British Medical Journal. 1971;1(750):637-639.

Milroy R, Carter R, Carlyle D, Boyd G. Clinical and pharmacologic study of a novel controlled release reparation. Br J Clin Pharm. 1990; 29(5):578-580.

Nathan RA. Beta 2 agonist therapy: oral versus inhaled delivery. J Asthma. 1992;29(1):49-54.

Shaw RJ, Waller JF, Hetzel MR, Clark TJ. Do oral and inhaled terbutaline have different effects on the lung? Br J Dis Chest. 1982;76(2):171-176.

Stewart IC, Rhind GB, Power JT, Flenley DC, Douglas NJ. Effect of sustained release terbutaline on symptoms and sleep quality in patients with nocturnal asthma. Thorax. 1987;42(10):797-800.

U.S. National Institutes of Health. National Heart, Lung, and Blood Institute. Global Initiative for Asthma. Global strategy for asthma management and prevention. Revised 2002. NIH Publication No. 02-3659. February 2002.

Van Keimpema AR, Ariaansz M, Raaijmakers JA, Nauta JJ, Postmus PE. Treatment of nocturnal asthma by addition of oral slow-release albuterol to standard treatment in stable asthma patients. J Asthma. 1996;33(2):119-124.

Webb J, Rees J, Clark TJ. A comparison of the effects of different methods of administration of beta-2-sympathomimetics in patients with asthma. Br J Dis Chest. 1982;76(4):351-357.

Wilkens JH, Wilkens H, Heins M, Kurtin L, Oellerich M, Sybrecht GW. Treatment of nocturnal asthma: the role of sustained-release theophylline and oral beta-2-mimetics. Chronobiol Int. 1987;4(3):387-396.

Wolfe JD, Shapiro GG, Ratner PH. Comparison of albuterol and metaproterenol syrup in the treatment of childhood asthma. Pediatrics. 1991;88(2):312-319.

Wolfe JD, Yamate M, Biedermann AA, Chu TJ. Comparison of the acute cardiopulmonary effects of oral albuterol, metaproterenol, and terbutaline in asthmatics. Journal of the American Medical Association. 1985;253(14):2068-2072.

Last Updated: September 2008
This content was created by members of the DrugDigest team of experts and is solely under DrugDigest's editorial control.


Note: The above information is intended to supplement, not substitute for, the expertise and judgment of your physician, pharmacist, or other healthcare professional. It should not be construed to indicate that the use of the product is safe, appropriate, or effective for you. Consult your healthcare professional before taking any medication.



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