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Bitolterol

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Title: Bitolterol  
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Bitolterol

Bitolterol
Systematic (IUPAC) name
(RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate
Clinical data
AHFS/Drugs.com
MedlinePlus
Identifiers
CAS Registry Number
ATC code R03
PubChem CID:
DrugBank
ChemSpider
UNII  Y
ChEMBL  Y
Chemical data
Formula C28H31NO5
Molecular mass 461.549 g/mol

Bitolterol mesylate (Tornalate) is a 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 get worse this narrowing. Bitolterol relaxes the smooth muscles present continuously around the bronchi and bronchioles facilitating the flow of air through them.

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

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 The drug was withdrawn from the market by Élan Pharmaceuticals in 2001.

References

  1. ^ Nathan RA, Bodman SF, Storms WW, Mingo TS (June 1986). "Bitolterol mesylate aerosol in adults with steroid-dependent asthma: a comparison with isoproterenol hydrochloride aerosol". Ann Allergy 56 (6): 494–9.  
  2. ^ Nathan RA, Bernstein IL, Bronsky EA, Bush RK, Chervinsky P, Condemi JJ, Dockhorn RJ, Pinnas JL, Repsher LH (May 1987). "Comparison of the bronchodilator effects of nebulized bitolterol mesylate and isoproterenol hydrochloride in steroid-dependent asthma". J. Allergy Clin. Immunol. 79 (5): 822–9.  
  3. ^ Friedel HA; Brogden RN (1988). "Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease". Drugs 35: 22–41.  
  4. ^ Anderson, JR.; Groves, PM.; Schwartz, GE. (Jan 1979). "Early Career Awards for 1978 (John Robert Anderson, Philip M. Groves, Gary E. Schwartz).". Am Psychol 34 (1): 69–79.  
  5. ^ Petty, TL.; Scoggin, CH.; Rollins, DR.; Repsher, LH. (Sep 1984). "Bitolterol compared to isoproterenol in advanced chronic obstructive pulmonary disease.". Chest 86 (3): 404–8.  
  6. ^ Kass, I.; Mingo, TS. (Aug 1980). "Bitolterol mesylate (WIN 32784) aerosol. A new long-acting bronchodilator with reduced chronotropic effects.". Chest 78 (2): 283–7.  
  7. ^ Kemp, JP.; Chervinsky, P.; Orgel, HA.; Meltzer, EO.; Noyes, JH.; Mingo, TS. (Jan 1984). "Concomitant bitolterol mesylate aerosol and theophylline for asthma therapy, with 24 hr electrocardiographic monitoring.". J Allergy Clin Immunol 73 (1 Pt 1): 32–43.  
Adrenergics, inhalants
Short acting β2-agonists
Long acting β2-agonists (LABA)
other
Glucocorticoids
Anticholinergics/
muscarinic antagonist
Mast cell stabilizers
Xanthines
Eicosanoid inhibition
Leukotriene antagonists
Arachidonate 5-lipoxygenase inhibitors
Thromboxane receptor antagonists
Non-xanthine PDE4 inhibitors
Others/unknown
Combination products
Index of the respiratory system
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