Bitolterol Explained

Bitolterol mesylate (Tornalate) is a short-acting β2 adrenergic receptor agonist used for the relief of bronchospasm in conditions such as asthma[1] [2] and COPD.[3] [4] [5] In these disorders there is a narrowing of the airways (bronchi and their ramifications) that carry air to the lungs. Muscle spasm and inflammation within the bronchi worsen this narrowing. Bitolterol relaxes the smooth muscles present continuously around the bronchi and bronchioles facilitating the flow of air through them.

Bitolterol is a prodrug of colterol.[6] [7] It has a rapid onset of action (2 - 5 minutes) and may last up to 6 - 8 hours.[8] The drug, alone or in co-administration with theophylline, doesn't show cardiotoxic effect.[9]

The U.S. Food and Drug Administration (FDA) approved bitolterol in December 1984. The drug was withdrawn from the market by Élan Pharmaceuticals in 2001.

References

See main article: other.

Notes and References

  1. Nathan RA, Bodman SF, Storms WW, Mingo TS . Bitolterol mesylate aerosol in adults with steroid-dependent asthma: a comparison with isoproterenol hydrochloride aerosol . Annals of Allergy . 56 . 6 . 494–499 . June 1986 . 3717716 .
  2. Nathan RA, Bernstein IL, Bronsky EA, Bush RK, Chervinsky P, Condemi JJ, Dockhorn RJ, Pinnas JL, Repsher LH . 6 . Comparison of the bronchodilator effects of nebulized bitolterol mesylate and isoproterenol hydrochloride in steroid-dependent asthma . The Journal of Allergy and Clinical Immunology . 79 . 5 . 822–829 . May 1987 . 3571773 . 10.1016/0091-6749(87)90216-8 . free .
  3. Friedel HA, Brogden RN . Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease . Drugs . 35 . 1 . 22–41 . January 1988 . 3278878 . 10.2165/00003495-198835010-00002 . dead . 218471864 . https://archive.today/20121223091149/http://ukpmc.ac.uk/abstract/MED/3278878/reload=0;jsessionid=c0HU7QxJoemJjpllzd68.24 . 2012-12-23 .
  4. Early Career Awards for 1978 (John Robert Anderson, Philip M. Groves, Gary E. Schwartz) . The American Psychologist . 34 . 1 . 69–79 . January 1979 . 396832 . 10.1037/h0078247 .
  5. Petty TL, Scoggin CH, Rollins DR, Repsher LH . Bitolterol compared to isoproterenol in advanced chronic obstructive pulmonary disease . Chest . 86 . 3 . 404–408 . September 1984 . 6380974 . 10.1378/chest.86.3.404 .
  6. Walker SB, Kradjan WA, Bierman CW . Bitolterol mesylate: a beta-adrenergic agent. Chemistry, pharmacokinetics, pharmacodynamics, adverse effects and clinical efficacy in asthma . Pharmacotherapy . 5 . 3 . 127–137 . 6 May 1985 . 3895171 . 10.1002/j.1875-9114.1985.tb03410.x . 29431526 .
  7. Web site: ChEBI: Bitolterol. Chemical Entities of Biological Interest. Wellcome Genome Campus, Hinxton, Cambridgeshire, CB10 1SD, UK. 27 March 2016.
  8. Kass I, Mingo TS . Bitolterol mesylate (WIN 32784) aerosol. A new long-acting bronchodilator with reduced chronotropic effects . Chest . 78 . 2 . 283–287 . August 1980 . 6995040 . 10.1378/chest.78.2.283 .
  9. Kemp JP, Chervinsky P, Orgel HA, Meltzer EO, Noyes JH, Mingo TS . Concomitant bitolterol mesylate aerosol and theophylline for asthma therapy, with 24 hr electrocardiographic monitoring . The Journal of Allergy and Clinical Immunology . 73 . 1 Pt 1 . 32–43 . January 1984 . 6693665 . 10.1016/0091-6749(84)90481-0 . free .

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