比托特羅

化合物

比托特羅INN:bitolterol)是一種短效β2腎上腺素受體激動劑,用於緩解哮喘[1][2]慢性阻塞性肺病等疾病的支氣管痙攣。[3][4][5]在這些疾病中,負責將空氣輸送到肺部的氣道(支氣管及其分支)會變窄。支氣管內的肌肉痙攣和炎症加劇了這種變窄。比托特羅通過放鬆持續存在於支氣管和支氣管細支周圍的平滑肌,有助於空氣順暢通過。

比托特羅
臨床資料
AHFS/Drugs.comMicromedex詳細消費者藥物信息
MedlinePlusa601236
ATC碼
識別資訊
  • (RS)-[4-(1-Hydroxy-2-tert-butylamino-ethyl)-2-(4-methylbenzoyl)oxy-phenyl] 4-methylbenzoate
CAS號30392-40-6
30392-41-7  checkY
PubChem CID
DrugBank
ChemSpider
UNII
ChEMBL
CompTox Dashboard英語CompTox Chemicals Dashboard (EPA)
化學資訊
化學式C28H31NO5
摩爾質量461.56 g·mol−1
3D模型(JSmol英語JSmol
手性外消旋混合物
  • O=C(Oc2cc(ccc2OC(=O)c1ccc(cc1)C)C(O)CNC(C)(C)C)c3ccc(cc3)C
可爾特羅

比托特羅是可爾特羅的前藥。[6][7]它起效迅速(2至5分鐘),可持續長達6至8小時。[8]該藥單獨或與茶鹼合用,不顯示心臟毒性作用。[9]

美國食品和藥物管理局於1984年12月批准了比托特羅。該藥物於2001年被Élan製藥英語Élan從市場上撤回。

參考資料

  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. June 1986, 56 (6): 494–499. PMID 3717716. 
  2. ^ Nathan RA, Bernstein IL, Bronsky EA, Bush RK, Chervinsky P, Condemi JJ, et al. Comparison of the bronchodilator effects of nebulized bitolterol mesylate and isoproterenol hydrochloride in steroid-dependent asthma. The Journal of Allergy and Clinical Immunology. May 1987, 79 (5): 822–829. PMID 3571773. doi:10.1016/0091-6749(87)90216-8 . 
  3. ^ Friedel HA, Brogden RN. Bitolterol. A preliminary review of its pharmacological properties and therapeutic efficacy in reversible obstructive airways disease. Drugs. January 1988, 35 (1): 22–41. PMID 3278878. S2CID 218471864. doi:10.2165/00003495-198835010-00002. (原始內容存檔於2012-12-23). 
  4. ^ Early Career Awards for 1978 (John Robert Anderson, Philip M. Groves, Gary E. Schwartz). The American Psychologist. January 1979, 34 (1): 69–79. PMID 396832. doi:10.1037/h0078247. 
  5. ^ Petty TL, Scoggin CH, Rollins DR, Repsher LH. Bitolterol compared to isoproterenol in advanced chronic obstructive pulmonary disease. Chest. September 1984, 86 (3): 404–408. PMID 6380974. doi: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. 6 May 1985, 5 (3): 127–137. PMID 3895171. S2CID 29431526. doi:10.1002/j.1875-9114.1985.tb03410.x. 
  7. ^ ChEBI: Bitolterol. Chemical Entities of Biological Interest. Wellcome Genome Campus, Hinxton, Cambridgeshire, CB10 1SD, UK. [27 March 2016]. (原始內容存檔於2024-03-28). 
  8. ^ Kass I, Mingo TS. Bitolterol mesylate (WIN 32784) aerosol. A new long-acting bronchodilator with reduced chronotropic effects. Chest. August 1980, 78 (2): 283–287. PMID 6995040. doi: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. January 1984, 73 (1 Pt 1): 32–43. PMID 6693665. doi:10.1016/0091-6749(84)90481-0 .