|
|
|
| Research progress of doxofylline |
| MAO Mingqing1，3 FANG Li′na2 JIA Hui3 HE Wei3 XIA Shuyue3 |
1.Shenyang Medical College, Liaoning Province, Shenyang 110034, China;
2.College of Basic Medical Science, Shenyang Medical College, Liaoning Province, Shenyang 110034, China;
3.Department of Respiratory, the Central Hospital Affiliated to Shenyang Medical College, Liaoning Province, Shenyang 110024, China |
|
|
|
Abstract Doxofylline is a methylxanthine derivative that acts as a new bronchodilator with good pharmacological effects and clinical efficacy in the treatment of chronic obstructive pulmonary disease and asthma. Compared with traditional theophylline, doxofylline has the characteristics of not antagonizing calcium channel receptors, nor affecting calcium influx, and has a weak affinity for adenosine A1 and A2 receptors, so it does not affect heart rate and rhythm, sleep rhythm, central nervous system (CNS) function and gastric secretion, and has good safety and tolerance. This article reviews the research progress of doxofylline in order to provide reference for the majority of medical workers.
|
|
|
|
|
|
[1] Global Initiative for Chronic Obstructive Lung Disease（GOLD）. 2017 Global Strategy for Prevention Diagnosis and Management of COPD [EB/OL]. https：//goldcopd.org/gold-2017-global-strategy-diagnosis-management-prevention-copd/.
[2] Wang C，Xu J，Yang L，et al. Prevalence and risk factors of chronic obstructive pulmonary disease in China （the China Pulmonary Health [CPH] study）：a national cross-sectional study [J]. Lancet，2018，391（10 131）：1706-1717.
[3] Abajobir AA，Abbafati C，Abbas KM，et al. Global，regional，and national age-sex specific mortality for 264 causes of death，1980-2016：a systematic analysis for the Global Burden of Disease Study 2016 [J]. Lancet，2017，390（10 100）：1151-1210.
[4] Collaborators G2CRD. Global regional and national deaths，prevalence，disability-adjusted life years，and years lived with disability for chronic obstructive pulmonary disease and asthma，1990-2015：a systematic analysis for the Global Burden of Disease Study 2015 [J]. Lancet Resp Med，2017，5（9）：691-706.
[5] Dwyer-Lindgren L，Bertozzi-Villa A，Stubbs RW，et al. Trends and Patterns of Differences in Chronic Respiratory Disease Mortality Among US Counties，1980-2014 [J]. Jama，2017，318（12）：1136-1149.
[6] Global Initiative for Asthma（GINA）. Global Strategy for Asthma Management and Prevention Updated 2017 [EB/OL]. http：//www.ginasthma.org.
[7] Peng Y，Wang H，Vos T，et al. A Subnational Analysis of Mortality and Prevalence of COPD in China From 1990 to 2013：Findings From the Global Burden of Disease Study 2013 [J]. Chest，2016，150（6）：1269-1280.
[8] Zafari Z，Sadatsafavi M，Chen W，et al. The projected economic and health burden of sub-optimal asthma control in Canada [J]. Respir Med，2018，138：7-12.
[9] Spina D，Page CP. Xanthines and Phosphodiesterase Inhibitors [J]. Handb Exp Pharmacol，2016，237：63-91.
[10] Mata M，Sarria B，Buenestado A，et al. Phosphodiesterase 4 inhibition decreases MUC5AC expression induced by epidermal growth factor in human airway epithelial cells [J]. Thorax，2005，60（2）：144-152.
[11] Jeon YH，Heo YS，Kim CM，et al. Phosphodiesterase：overview of protein structures，potential therapeutic applications and recent progress in drug development [J]. Cell Mol Life Sci，2005，62（11）：1198-1220.
[12] Houslay MD，Schafer P，Zhang KYJ. Keynote review：Phosphodiesterase-4 as a therapeutic target [J]. Drug Discov Today，2005，10（22）：1503-1519.
[13] Ito K，Lim S，Caramori G，et al. A molecular mechanism of action of theophylline：Induction of histone deacetylase activity to decrease inflammatory gene expression [J]. Proc Natl Acad Sci U S A，2002，99（13）：8921-8926.
[14] Press NJ，Gessi S，Borea PA，et al. Therapeutic potential of adenosine receptor antagonists and agonists [J]. Expert Opin Ther Pa，2007，17（8）：979-991.
[15] Van MJ，Jolas T，Allegra L，et al. The mechanism of action of doxofylline is unrelated to HDAC inhibition，PDE inhibition or adenosine receptor antagonism [J]. Pulm Pharmacol Ther，2012，25（1）：55.
[16] Cruse G，Duffy SM，Brightling CE，et al. Functional KCa3.1 K+ channels are required for human lung mast cell migration [J]. Thorax，2006，61（10）：880-885.
[17] Zhou B，Cai SX，Zou F，et al. Effect of doxofylline on calcium-activated potassium channels in human peripheral blood eosinophils in asthma [J]. Chin J Tubere Respir Dis，2005，28（28）：817-819.
[18] Franzone JS，Cirillo R，Biffignandi P. Doxofylline exerts a prophylactic effect against bronchoconstriction and pleurisy induced by PAF [J]. Eur J Pharmacol，1989，165（2/3）：269-277.
[19] Riffo-Vasquez Y，Man F，Page CP. Doxofylline，a novofylline inhibits lung inflammation induced by lipopolysacharide in the mouse [J]. Pulm Pharmacol Ther，2014，27（2）：170-178.
[20] Cogo R，Castronuovo A. Effects of oral doxofylline on inflammatory changes and altered cell proliferation in chronic obstructive bronchitis [J]. Eur Rev Med Pharmacol Sci， 2000，4（1/2）：15-20.
[21] Patel BS，Kugel MJ，Baehring G，et al. Doxofylline does not increase formoterol-induced cAMP nor MKP-1 expression in ASM cells resulting in lack of anti-inflammatory effect [J]. Pulm Pharmacol Ther，2017，45：34-39.
[22] Franzone JS，Cirillo R，Barone D. Doxofylline and theophylline are xanthines with partly different mechanisms of action in animals [J]. Drug Explt Clin Res，1988，14（7）：479-489.
[23] Franzone JS，Cirillo R，Reboani MC. Doxofylline differs from methylxanthines in its movement of cytosolic calcium [J]. Int J Tissue React，1991，13（3）：131-138.
[24] Rajanandh MG，Nageswari AD，Ilango K. Assessment of montelukast doxofylline and tiotropium with budesonide for the treatment of asthma：which is the best among the second-line treatment？A randomized trial [J]. Clin Ther，2015，37（2）：418-426.
[25] LimS，JatakanonA，Gordon D，et al. Comparison of high dose inhaled steroids，low dose inhaled steroids pluslow dose theophylline，and low dose inhaled steroids alone in chronic asthmain general practice [J]. Thorax，2000，55（10）：837-841.
[26] Goldstein MF，Chervinsky P. Efficacy and safety of doxofylline compared to theophylline in chronic reversible asthma--a double-blind randomized placebo-controlled multicentre clinical trial [J]. Med Sci Monit，2002， 8（4）：297-304.
[27] Margay SM，Farhat S，Kaur S，et al. To study the efficacy and safety of doxophylline and theophylline in bronchial asthma [J]. J Clin Diagn Res，2015，9（4）：5-8.
[28] Lal D，Manocha S，Ray A，et al. Comparative study of the efficacy and safety of theophylline and doxofylline in patients with bronchial asthma and chronic obstructive pulmonary disease [J]. J Basic Clin Physiol Pharmacol，2015， 26（5）：443-451.
[29] Akram MF，Nasiruddin M，Ahmad Z，et al. Comparative evaluation of doxofylline and theophylline in patients of mild bronchial asthma [J]. Ijbcp，2013，2（4）：386.
[30] Akram MF，Nasiruddin M，Ahmad Z，et al. Doxofylline and theophylline：a comparative clinical study [J]. J Clin Diagn Res，2012， 6（10）：1681-1684.
[31] Cravanzola C，Reboani MC，Grosa G，et al. Doxofylline in rat brain in relation to locomotor activity [J]. Drug Metab Dispos Biol Fate Chem，1989，17（4）：437-440.
[32] Sacco C，Braghiroli A，Grossi E，et al. The effects of doxofylline versus theophylline on sleep architecture in COPD patients [J]. Monaldi Arch Chest Dis，1995，50（2）：98-103.
[33] Lazzaroni M，Gross E，Porro GB. The effect of intravenous doxofylline or aminophylline on gastric secretion in duodenal ulcer patients [J]. Aliment Pharmacol Ther，1990，4（6）：643-649.
[34] Bagnato GF. Tolerability of doxofylline in the maintenance therapy of pediatric patients with bronchial asthma [J]. Eur Rev Med Pharmacol Sci，1999，3（6）：255-260.
[35] Guo H，Xu XY，He LY，et al. Preliminary study on the absorption， distribution and excretion of doxophylline in rats [J]. Acta Pharmaceutica Sinica，1997，32（2）：81-84.
[36] Bologna E，Laganà A，Terracino D，et al. Oral and intravenous pharmacokinetic profiles of doxofylline in patients with chronic bronchitis [J]. J Int Med Res，1990，18（4）：282-288.
[37] Gu J，Zhang CY，Cao ZL，et al. The pharmacokinetics of doxofylline in Chinese [J]. Chin J New Drugs，2000，9（6）：396-398.
[38] 杜智敏，张波，刘艳，等.多索茶碱颗粒与口服液在健康人体内的生物利用度和药代动力学[J].中国临床药理学杂志，2003，19（4）：280-283.
[39] Gannu R，Bandari S，Sudke SG，et al. Development and validation of a stability-indicating RP-HPLC method for analysis of doxofylline in human serum. Application of the method to a pharmacokinetic study [J]. Acta Chromatogr，2007，19（19）：149-160.
[40] Lee JH，Namgung HW，Kwon SY，et al. The pharmacokinetic profiles of oral doxofylline and factors influencing the serum level [J]. Eur Res Cong Abstact Book，2007，Poster-2116：350s.
[41] Zhang XR，Chen XY，Hu LD，et al. Evaluation of in-vitro dissolution and in-vivo absorption for two different film-coated pellets of clarithromycin [J]. Arch Pharm Res，2005， 28（8）：977-982.
[42] Huang HF，Lu Y，He HB，et al. Preparation and bioavailability of sustained-release doxofylline pellets in beagle dogs [J]. Drug Dev Ind Pharm，2008，34（7）：676-682.
[43] Franzone JS，Cirillo R，Reboani MC. Pharmacological studies in animals of beta-hydroxyethyltheophylline the major metabolite of doxofylline in humans [J]. Methods Find Exp Clin Pharmacol，1991，13（4）：289-299.
[44] Lentini A，Tabolacci C，Nardi A，et al. Preclinical evaluation of the antineoplastic efficacy of 7-（2-hydroxyethyl）theophylline on melanoma cancer cells [J]. Melanoma Res，2012，22（2）：133-139.
[45] 王金明.氟罗沙星对多索茶碱在人肝微粒体中代谢影响的体外研究[D].杭州：浙江中医药大学，2015.
[46] 蔡灯塔.巴洛沙星对多索茶碱药动学影响的研究[D].郑州：郑州大学，2010. |
|
|
|
