期刊目次

加入编委

期刊订阅

添加您的邮件地址以接收即将发行期刊数据:

Open Access Article

International Medical Research Frontier. 2024; 8: (1) ; 35-41 ; DOI: 10.12208/j.imrf.20240009.

Progress for clinical pharmacology and application of bupropion
安非他酮临床药理及应用新进展

作者: 黄璐璐1,2,3, 于洋4, 韩晓雨1,2,3, 肖云1,2,3, 张永杰5, 刘方兰2, 何佳珂1,2,5,6 *

1 南昌大学第二附属医院药学部 江西南昌
2 南昌大学临床药理研究所 江西南昌
3 南昌大学药学院 江西南昌

4 南昌大学第二附属医院医务处 江西南昌

5 中国药科大学基础医学院和临床药学院 江苏南京

6 南昌县人民医院药剂科 江西南昌

*通讯作者: 何佳珂,单位: 南昌县人民医院药剂科 江西南昌;

发布时间: 2024-06-29 总浏览量: 124

摘要

作为新型氨基酮类抗抑郁药,安非他酮通过阻滞多巴胺和去甲肾上腺素再摄取以发挥疗效。安非他酮体内过程复杂,CYP2B6、羰基还原酶、UGT2B7和UGT1A等参与其体内立体选择性代谢,影响临床疗效的发挥。该文通过查阅国内外相关文献,就安非他酮药理作用机制、体内过程、相互作用、抗抑郁、戒除烟瘾以及减肥治疗的有效性和安全性做一综述,以期为临床安全、合理、有效用药提供参考。

关键词: 安非他酮;作用机制;体内过程;抗抑郁;减肥;戒烟

Abstract

Bupropion is an aminoketone antidepressant, which exerts its effects mainly by inhibiting dopamine and norepinephrine. Bupropion is stereoselective metabolized by CYP2B6, carbonyl reductase, UGT2B7 and UGT1A in vivo which affect its clinical efficacy. Based on published researches, a systematic review was conducted focusing mainly on the pharmacological mechanisms, in-vivo disposition, drug-drug interaction, safety, and effectiveness of bupropion in antidepressant therapy, weight loss and smoking cessation, providing guidelines for clinical practice.

Key words: Bupropion; Mechanism; ADME; Antidepressant; Weight loss; Smoking cessation

参考文献 References

[1] Wilkes S. Bupropion[J]. Drugs Today (Barc), 2006, 42(10): 671-681.

[2] Lakshmi NY, Sidney HK, Sagar VParikh, et al. Canadian Network for Mood and Anxiety Treatments (CANMAT) and International Society for Bipolar Disorders (ISBD) 2018 guidelines for the management of patients with bipolar disorder[J]. Bipolar Disord, 2018, 20(2): 97–170. 

[3] Greig SL, Keating GM. Naltrexone ER/Bupropion ER: A Review in Obesity Management[J]. Drugs, 2015, 75(11): 1269-1280.

[4] 朱谦. 多巴胺/去甲肾上腺素再摄取抑制剂安非他酮治疗神经病理性疼痛的脊髓机制研究[D].北京协和医学院,2022,58(3):1-58.

[5] Khan SR, Berendt RT, Ellison CD, et al. Bupropion Hydrochloride[J]. Profiles Drug Subst Excip Relat Methodol, 2016, 41: 1-30.

[6] Shepherd G, Velez LI, Keyes DC. Intentional bupropion overdoses[J]. J Emerg Med, 2004, 27(2): 147-151.

[7] Stassinos GL, Klein-Schwartz W. Bupropion "Abuse" Reported to US Poison Centers[J]. J Addict Med, 2016, 10(5): 357-362.

[8] 喻东山. 安非他酮的不良反应[J]. 临床精神医学杂志, 2016, 26(6): 427-428.

[9] 盐酸安非他酮片药品说明书[Z]. 2012年6月14日版.

[10] 英国警示安非他酮及其联合使用其他5-羟色胺类药物的血清素综合征风险[J].中国药物评价,2020,37(6):421.

[11] Stahl SM, Pradko JF, Haight BR, et al. A Review of the Neuropharmacology of Bupropion, a Dual Norepinephrine and Dopamine Reuptake Inhibitor[J]. Prim Care Companion J Clin Psychiatry, 2004, 6(4): 159-166.

[12] Evan DK, Amanda C. Common polymorphisms of CYP2B6 influence stereoselective bupropion disposition[J]. Clin Pharmacol Ther, 2019, 105(1): 142-152. 

[13] Ma H, Zhang WP, Yang XY, et al. effects of Genetic Polymorphisms of CYP2B6 on the Pharmacokinetics of Bupropion and Hydroxybupropion in Healthy Chinese Subjects[J]. Med Sci Monit, 2018, 24: 2158-2163.

[14] Jefferson JW, Pradko JF, Muir KT. Bupropion for major depressive disorder: Pharmacokinetic and formulation considerations[J]. Clin Ther. 2005 ,27(11):1685-95. 

[15] Gufford BT, Lu JB, Metzger IF, et al. Stereoselective Glucuronidation of Bupropion Metabolites In Vitro and In Vivo[J]. Drug Metab Dispos, 2016, 44(4): 544-553.

[16] Ranjeet PD, Rana R, Nuggehally RS,et al. Chirality and neuropsychiatric drugs: an update on stereoselective disposition and clinical pharmacokinetics of bupropion[J]. Xenobiotica, 2018, 48(9):945-957.

[17] Andrea RM, Brandon TG, Jessica BLL, et al. Chiral Plasma Pharmacokinetics and Urinary Excretion of Bupropion and Metabolites in Healthy Volunteers[J]. J Pharmacol Exp Ther,2016,358(2):230-238.

[18] Farid NA, Small DS, Li YG, et al. Effect of Prasugrel, a Novel Thienopyridine, on CYP2B6 Activity in Healthy Subjects as Determined by Bupropion Hydroxylation[c]. 14th ISSX meeting.

[19] Park J, Vousden M,Brittain C, et al. Dose-related reduction in bupropion plasma concentrations by ritonavir[J]. J Clin Pharmacol, 2010, 50(10):1180-1187.

[20] Kristine H, Marianne A, Espen M, et al. Dose-Dependent Inhibition of CYP2D6 by Bupropion in Patients With Depression[J]. J Clin Psychopharmacol, 2021, 41(3):281-285.

[21] 于洋,何佳珂,熊爱珍,等.UPLC-MS/MS法同时测定大鼠血浆中安非他酮及其活性代谢产物的浓度[J].南昌大学学报·医学版,2019,59(1):1-6,12.

[22] Farid NA, Small DS, Li YG, et al. Effect of Prasugrel, a Novel Thienopyridine, on CYP2B6 Activity in Healthy Subjects as Determined by Bupropion Hydroxylation[c]. 14th ISSX meeting.

[23] Park J, Vousden M, Brittain C, et al. Dose-related reduction in bupropion plasma concentrations by ritonavir[J]. J Clin Pharmacol, 2010, 50(10):1180-1187.

[24] Hogeland GW, Swindells S, McNabb JC, et al. Lopinavir/ritonavir reduces bupropion plasma concentrations in healthy subjects[J]. Clin Pharmacol Ther, 2007,81(1):69-75.

[25] Reese MJ, Wurm RM, Muir KT, et al. An in vitro mechanistic study to elucidate the desipramine/bupropion clinical drug-drug interaction[J]. Drug Metab Dispos,2008,36(7): 1198-1201.

[26] Molden E, Spigset O. Interaksjoner mellom metoprolol og antidepressive legemidler [Interactions between metoprolol and antidepressants[J]. Tidsskr Nor Laegeforen. 2011 Sep 20;131(18):1777-9. Norwegian.

[27] Spina E, Trifirò G, Caraci F. Clinically significant drug interactions with newer antidepressants[J]. CNS Drugs. 2012 Jan 1;26(1):39-67. 

[28] Kirby BJ, Collier AC, Kharasch ED, et al. Complex drug interactions of the HIV protease inhibitors 3: effect of simultaneous or staggered dosing of digoxin and ritonavir, nelfinavir, rifampin, or bupropion[J]. Drug Metab Dispos, 2012, 40(3): 610-616.

[29] He JK, Yu Y, Prasad B, et al. Mechanism of an unusual, but clinically significant, digoxin-bupropion drug interaction[J]. Biopharm Drug Dispos, 2014, 35(5): 253-263.

[30] Shen Y, Yu Y, Lai W, et al. Evaluation of a potential clinical significant drug-drug interaction between digoxin and bupropion in cynomolgus monkeys[J]. Pharm Res, 2018,36 (1):1.

[31] Andrea C, Toshi AF, Georgia S, et al. Comparative efficacy and acceptability of 21 antidepressant drugs for the acute treatment of adults with major depressive disorder: a systematic review and network meta-analysis[J]. Lancet,2018,391(10128):1357-1366. 

[32] Clayton AH, Croft HA, Horrigan JP, et al. Bupropion extended release compared with escitalopram: effects on sexual functioning and antidepressant efficacy in 2 randomized, double-blind, placebo-controlled studies[J]. J Clin Psychiatry, 2006, 67(5): 736-746.

[33] Yuen-Siang A, Roselinde K, Thilo D, et al. Pretreatment reward sensitivity and frontostriatal resting-state functional connectivity are associated with response to bupropion after sertraline non-response[J]. Biol Psychiatry, 2020, 88(8): 657–667.

[34] Rosso G, Rigardetto S, Bogetto F, et al. A randomized, single-blind, comparison of duloxetine with bupropion in the treatment of SSRI-resistant major depression. J Affect Disord. 2012 Jan;136(1-2):172-176.

[35] Rush A, Trivedi M, Carmody T, et al. Response in relation to baseline anxiety levels in majordepressive disorder treated with bupropion sustainedrelease or sertraline [J]. Neuropsychopharmacology, 2001, 25(1): 131-138.

[36] Rush A, Trivedi M, Wisniewski S, et al. Bupropion-SR, sertraline, or venlafaxine-XR after failure of SSRIs for depression[J]. N Engl J Med, 2006, 354(12): 1231-1242.

[37] Feighner J, Gardner E, Johnston J, et al. Double-blind comparison of bupropion and fluoxetine in depressed outpatients[J]. J Clin Psychiatry, 1991, 52(8): 329-335.

[38] Coleman CC, King BR, Bolden-Watson C, et al. A placebo-controlled comparison of the effects on sexual functioning of bupropion sustained release and fluoxetine[J]. Clin Ther, 2001 Jul, 23(7):1040-1058.

[39] Hewett K, Chrzanowski W, Schmitz M, et al. Eight-week, placebo-controlled, double-blind comparison of the antidepressant efficacy and tolerability of bupropion XR and venlafaxine XR[J]. J Psychopharmacol, 2010, 24(8):1209-1216.

[40] Sean W, Lilian R, Kristin JS, et al. Medications that cause weight gain and alternatives in Canada: a narrative review[J]. Diabetes Metab Syndr Obes, 2018, 11:427-438.

[41] Zuilhof Z, Norris S, Blondeau C, et al. Optimized regimens of combined medications for the treatment of major depressive disorder: a double-blind, randomized-controlled trial[J]. Neuropsychiatr Dis Treat. 2018 Nov 22; 14:3209-3218. 

[42] Iosifescu DV, Jones A, O'Gorman C, Streicher C, Feliz S, Fava M, Tabuteau H. Efficacy and Safety of AXS-05 (Dextromethorphan-Bupropion) in Patients With Major Depressive Disorder: A Phase 3 Randomized Clinical Trial (GEMINI) [J]. J Clin Psychiatry. 2022 May 30;83(4):21m14345. 

[43] Greenway FL, Fujioka K, Plodkowski RA, et al. Effect of naltrexone plus bupropion on weight loss in overweight and obese adults (COR-I): a multicentre, randomised, double-blind, placebo-controlled, phase 3 trial[J]. Lancet, 2010, 376(9741): 595-605.

[44] Apovian CM, Aronne L, Rubino D, et al. A randomized, phase 3 trial of naltrexone SR/bupropion SR on weight and obesity-related risk factors (COR-II)[J].Obesity, 2013, 21(5): 935-943.

[45] Wadden TA, Foreyt JP, Foster GD, et al. Weight loss with naltrexone SR/bupropion SR combination therapy as an adjunct to behavior modification: the COR-BMOD trial[J]. Obesity, 2011, 19(1): 110-120.

[46] Hollander P, Gupta AK, Plodkowski R, et al. Effects of naltrexone sustained-release/ bupropion sustained-release combination therapy on body weight and glycemic parameters in overweight and obese patients with type 2 diabetes[J]. Diabetes Care, 2013, 36(12): 4022-4029.

[47] Carbone EA, Caroleo M, Rania M, et al. An open-label trial on the efficacy and tolerability of naltrexone/bupropion SR for treating altered eating behaviours and weight loss in binge eating disorder[J]. Eat Weight Disord. 2021 Apr;26(3):779-788.

[48] Weizman S, Shelef A, Bloemhof Bris E, Stryjer R. A Double-Blind, Placebo-Controlled Trial of Bupropion Add-on to Olanzapine or Risperidone in Overweight Individuals With Schizophrenia[J]. J Clin Psychopharmacol. 2021 Nov-Dec 01;41(6):629-631.

[49] Zyban®[Z]. Research Triangle Park, NC: GlaxoSmithKline LLC, 2017.

[50] Rafaela C, Nuno GO, Ricardo JD. Pharmacokinetic and pharmacodynamic of bupropion: integrative overview of relevant clinical and forensic aspects[J]. Drug Metab Rev,2019, 51(3):293-313.

[51] Giulietti F, Filipponi A, Rosettani G, et al. Pharmacological Approach to Smoking Cessation: An Updated Review for Daily Clinical Practice[J]. High Blood Press Cardiovasc Prev. 2020 Oct;27(5):349-362.

[52] 张锦, 何智余, 杨琳,等. 安非他酮戒除心血管疾病吸烟患者烟瘾有效性与安全性的Meta分析[J]. 中国循证医学杂志, 2014, 14(3): 292-298.

[53] Mills EJ, Thorlund K, Eapen S, et al. Cardiovascular events associated with smoking cessation pharmacotherapies: a network meta-analysis[J]. Circulation, 2014, 129(1): 28-41.

[54] Hughes JR, Stead LF, Hartmann-Boyce J, et al. Antidepressants for smoking cessation[J]. Cochrane Database Syst Rev, 2014, (1): CD000031.

[55] Vogeler T, McClain C, Evoy KE. Combination bupropion SR and varenicline for smoking cessation: a systematic review[J]. Am J Drug Alcohol Abuse, 2016, 42(2): 129-139.

[56] Daniel K, Colin S, Wolfgang V, et al. Cardiovascular and neuropsychiatric safety of varenicline and bupropion compared with nicotine replacement therapy for smoking cessation: study protocol of a retrospective cohort study using the QResearch general practice database[J]. BMJ Open, 2014, 4(8): e005281.

[57] Yan T, Goldman RD. Bupropion for smoking cessation in adolescents[J]. Can Fam Physician. 2021 Oct;67(10):743-745.

[58] Piper ME, Smith SS, Schlam TR, et al. A randomized placebo-controlled clinical trial of 5 smoking cessation pharmacotherapies[J]. Arch Gen Psychiatry. 2009;66(11):1253–62.

[59] Howes S, Hartmann-Boyce J, Livingstone-Banks J, et al. Antidepressants for smoking cessation[J]. Cochrane Database Syst Rev. 2020 Apr 22;4(4):CD000031.

[60] Australian Government Department of Health. Therapeutic Goods Administration. Bupropion and serious cardiovascular adverse events[J]. Medicines Safety Update, 2014, 5(5): 168.

引用本文

黄璐璐, 于洋, 韩晓雨, 肖云, 张永杰, 刘方兰, 何佳珂, 安非他酮临床药理及应用新进展[J]. 国际医药研究前沿, 2024; 8: (1) : 35-41.