生物活性

• 描述Chlorpheniramine Maleate is potent, less sedative antihistaminic drug, which acts by inhibiting histamine release from mast cells. Chlorpheniramine causes bronchodilation during resting period by acting on the circulating or tissue histamine in asthmatics which contributes to an increase in resting bronchomotor tone^[3]. Chlorpheniramine has a serum half-life of approximately 20 hours in adults, and elimination from the body is primarily by metabolism to monodesmethyl and didesmethyl compounds. Age, dialysis, urinary pH and flow influence the elimination kinetics of chlorpheniramine^[4]. A nasal gel formulation for an antihistaminic drug, Chlorpheniramine maleate (CPM), which suffers from poor oral^[5]. The antihistamine chlorpheniramine maleate (CPM) is also used for symptomatic relief of hypersensitive reactions and in pruritic skin disorders^[6].
• 临床研究

• NCT号	适应症或疾病	临床期	招募状态	预计完成时间	地点
  NCT00000752	HIV Infections ... more >> Sinusitis Collapse <<	Phase 2	Withdrawn	-	United States, California ... more >> Univ of California / San Diego Treatment Ctr San Diego, California, United States, 921036325 Stanford at Kaiser / Kaiser Permanente Med Ctr San Francisco, California, United States, 94115 United States, New York Montefiore Drug Treatment Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10461 Montefiore Family Health Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10461 Samaritan Village Inc / Bronx Municipal Hosp Bronx, New York, United States, 10461 Jack Weiler Hosp / Bronx Municipal Hosp Bronx, New York, United States, 10465 Montefiore Med Ctr / Bronx Municipal Hosp Bronx, New York, United States, 10467 Montefiore Med Ctr Adolescent AIDS Program Bronx, New York, United States, 10467 North Central Bronx Hosp / Bronx Municipal Hosp Bronx, New York, United States, 10467 United States, Pennsylvania Thomas Jefferson Univ Hosp Philadelphia, Pennsylvania, United States, 191075098 Collapse <<
  NCT00377403	Acute Respiratory Infections ... more >> Acute Rhinosinusitis Collapse <<	Phase 4	Completed	-	United States, Missouri ... more >> Washington University in St. Louis St. Louis, Missouri, United States, 63110 Collapse <<
  NCT00857987	Upper Airway Infections	Phase 3	Unknown	December 2011	Brazil ... more >> LAL Clinica Pesquisa e Desenvolvimento Ltda Recruiting Valinhos, SP, Brazil, 13270000 Contact: Karina Guerra, Coordinator    55 19 3829 3822    karina@lalclinica.com.br    Principal Investigator: Alexandre Frederico, Doctor Collapse <<

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• 参考文献

• [1] Medina MA, Garcia de Veas R, et al. Chlorpheniramine inhibits the synthesis of ornithine decarboxylase and the proliferation of human breast cancer cell lines. Breast Cancer Res Treat. 1995 Aug;35(2):187-94.

  [2] Sleevi MC, Cale AD Jr, et al. Optical isomers of rocastine and close analogues: synthesis and H1 antihistaminic activity of its enantiomers and their structural relationship to the classical antihistamines. J Med Chem. 1991 Apr;34(4):1314-28.

  [3] Chugh J, Yadav YR, Kulkarni HS, Maheshwari S. The Effect of Aerosolized Chlorpheniramine Maleate on Exercise Induced Bronchospasm and Gas Exchange in Asthmatics. J Assoc Physicians India. 2020 Apr;68(4):21-25

  [4] Rumore MM. Clinical pharmacokinetics of chlorpheniramine. Drug Intell Clin Pharm. 1984 Sep;18(9):701-7

  [5] Soliman II, Soliman NA, Abdou EM. Formulation and stability study of chlorpheniramine maleate nasal gel. Pharm Dev Technol. 2010 Sep-Oct;15(5):484-91

  [6] Ceschel GC, Maffei P, Gentile M. Design and evaluation of a new transdermal formulation containing chlorpheniramine maleate. Drug Dev Ind Pharm. 1999 Sep;25(9):1035-9

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