| 词条 | Bitolterol |
| 释义 |
| IUPAC_name = (RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate | image = Bitolterol.svg | width = 240 | chirality = Racemic mixture | tradename = | Drugs.com = {{drugs.com|CONS|bitolterol}} | MedlinePlus = a601236 | pregnancy_category = | legal_status = | routes_of_administration = | bioavailability = | protein_bound = | metabolism = | elimination_half-life = | CAS_number = 30392-41-7 | ATC_prefix = R03 | ATC_suffix = AC17 | ATC_supplemental = | PubChem = 35330 | DrugBank = DB00901 | ChemSpiderID = 32525 | UNII_Ref = {{fdacite|correct|FDA}} | UNII = 9KY0QXD6LI | ChEMBL_Ref = {{ebicite|correct|EBI}} | ChEMBL = 1201295 | C=28 | H=31 | N=1 | O=5 | molecular_weight = 461.549 g/mol | smiles = O=C(Oc2cc(ccc2OC(=O)c1ccc(cc1)C)C(O)CNC(C)(C)C)c3ccc(cc3)C }} 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 get worse 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 The drug was withdrawn from the market by Élan Pharmaceuticals in 2001. {{clear left}}References1. ^{{cite journal |vauthors=Nathan RA, Bodman SF, Storms WW, Mingo TS |title=Bitolterol mesylate aerosol in adults with steroid-dependent asthma: a comparison with isoproterenol hydrochloride aerosol |journal=Ann Allergy |volume=56 |issue=6 |pages=494–9 |date=June 1986 |pmid=3717716 |doi= |url=}} {{Adrenergic agonists}}{{Asthma_and_copd_rx}}{{main other|2. ^{{cite journal |vauthors=Nathan RA, Bernstein IL, Bronsky EA, Bush RK, Chervinsky P, Condemi JJ, Dockhorn RJ, Pinnas JL, Repsher LH |title=Comparison of the bronchodilator effects of nebulized bitolterol mesylate and isoproterenol hydrochloride in steroid-dependent asthma |journal=J. Allergy Clin. Immunol. |volume=79 |issue=5 |pages=822–9 |date=May 1987 |pmid=3571773 |doi= 10.1016/0091-6749(87)90216-8|url=}} 3. ^{{cite journal|author1=Friedel HA |author2=Brogden RN |title=Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease|journal= Drugs |year =1988 |volume = 35 |pages = 22–41 |url = http://ukpmc.ac.uk/abstract/MED/3278878/reload=0;jsessionid=c0HU7QxJoemJjpllzd68.24 |doi=10.2165/00003495-198835010-00002}} 4. ^{{Cite journal | last1 = Anderson | first1 = JR. | last2 = Groves | first2 = PM. | last3 = Schwartz | first3 = GE. | title = Early Career Awards for 1978 (John Robert Anderson, Philip M. Groves, Gary E. Schwartz). | journal = Am Psychol | volume = 34 | issue = 1 | pages = 69–79 |date=Jan 1979 | doi = | PMID = 396832 }} 5. ^{{Cite journal | last1 = Petty | first1 = TL. | last2 = Scoggin | first2 = CH. | last3 = Rollins | first3 = DR. | last4 = Repsher | first4 = LH. | title = Bitolterol compared to isoproterenol in advanced chronic obstructive pulmonary disease. | journal = Chest | volume = 86 | issue = 3 | pages = 404–8 |date=Sep 1984 | doi = 10.1378/chest.86.3.404| PMID = 6380974 }} 6. ^{{cite journal|last1=Walker|first1=Susannah B.|last2=Kradjan|first2=Wayne A.|last3=Bierman|first3=C. Warren|title=Bitolterol Mesylate: A Beta-adrenergic Agent; Chemistry, Pharmacokinetics, Pharmacodynamics, Adverse Effects and Clinical Efficacy in Asthma|journal=Pharmacotherapy|date=6 May 1985|volume=5|issue=3|pages=127–137|doi=10.1002/j.1875-9114.1985.tb03410.x|pmid=3895171}} 7. ^{{cite web|title=ChEBI: Bitolterol|url=http://www.ebi.ac.uk/chebi/searchId.do?chebiId=3133|website=Chemical Entities of Biological Interest|publisher=Wellcome Genome Campus, Hinxton, Cambridgeshire, CB10 1SD, UK|accessdate=27 March 2016}} 8. ^{{Cite journal | last1 = Kass | first1 = I. | last2 = Mingo | first2 = TS. | title = Bitolterol mesylate (WIN 32784) aerosol. A new long-acting bronchodilator with reduced chronotropic effects. | journal = Chest | volume = 78 | issue = 2 | pages = 283–7 |date=Aug 1980 | doi = 10.1378/chest.78.2.283| PMID = 6995040 }} 9. ^{{Cite journal | last1 = Kemp | first1 = JP. | last2 = Chervinsky | first2 = P. | last3 = Orgel | first3 = HA. | last4 = Meltzer | first4 = EO. | last5 = Noyes | first5 = JH. | last6 = Mingo | first6 = TS. | title = Concomitant bitolterol mesylate aerosol and theophylline for asthma therapy, with 24 hr electrocardiographic monitoring. | journal = J Allergy Clin Immunol | volume = 73 | issue = 1 Pt 1 | pages = 32–43 |date=Jan 1984 | doi = 10.1016/0091-6749(84)90481-0| PMID = 6693665 }} }}{{respiratory-system-drug-stub}} 5 : Beta2-adrenergic agonists|Benzoates|Prodrugs|Withdrawn drugs|Tert-butyl compounds |
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