Disposition of amodiaquine and desethylamodiaquine in HIV-infected Nigerian subjects on nevirapine-containing antiretroviral therapy.
Disposition of amodiaquine and desethylamodiaquine in HIV-infected Nigerian subjects on nevirapine-containing antiretroviral therapy.
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在接受奈韦拉平抗逆转录病毒治疗的艾滋病毒感染尼日利亚受试者中阿莫地喹和去乙基阿莫地喹的处置。
DOI：
10.1093/jac/dkt513
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发表时间：
2014
期刊：
影响因子：
--
通讯作者：
Murphy,Robert
中科院分区：
文献类型：
--
作者：
Scarsi,KimberlyK;Fehintola,FataiA;Ma,Qing;Aweeka,FrancescaT;Darin,KristinM;Morse,GeneD;Akinola,IbrahimTemitope;Adedeji,WaheedA;Lindegardh,Niklas;Tarning,Joel;Ojengbede,Oladosu;Adewole,IsaacF;Taiwo,Babafemi;Murphy,Robert
目的青蒿琥酯加阿莫地喹用于艾滋病重叠流行地区的疟疾治疗。青蒿琥酯/阿莫地喹与抗逆转录病毒治疗（ART）联合给药可能导致药物相互作用，但数据很少。本研究评估了奈韦拉平为基础的ART，含有骨架的齐多夫定和拉米夫定，阿莫地喹及其活性代谢产物，去乙基阿莫地喹（DEAQ）的处置的影响。MethodsThis是一个开放标签，平行组之间的HIV感染，成人受试者接受稳态奈韦拉平为基础的ART（n= 10）和ART初治受试者（对照组，n= 11）的药代动力学比较。 所有受试者每天接受青蒿琥酯/阿莫地喹（200/600 mg）的松散制剂，持续3天，在青蒿琥酯/阿莫地喹末次给药后96 h内进行系列药代动力学采样。采用经验证的HPLC法和UV检测对阿莫地喹和DEAQ进行定量。结果与对照组相比，以奈韦拉平为基础的ART组阿莫地喹和DEAQ的暴露量均显著降低（阿莫地喹AUC 0 -24145与204 ng·h/mL，P= 0.02; DEAQ AUC 0 -9614 571与21648 ng·h/mL，P<0.01）。 AUCDEAQ/AUCamodiaquineratio组间无差异（ART组116与对照组102，P= 0.67）。 因此，这可能会对青蒿琥酯/阿莫地喹在艾滋病毒感染者中对这种抗逆转录病毒疗法组合的有效性产生负面影响。
ObjectivesArtesunate plus amodiaquine is used for malaria treatment in regions with overlapping HIV endemicity. Co-administration of artesunate/amodiaquine with antiretroviral therapy (ART) may result in drug–drug interactions, but minimal data exist. This study evaluated the impact of nevirapine-based ART, containing a backbone of zidovudine and lamivudine, on the disposition of amodiaquine and its active metabolite, desethylamodiaquine (DEAQ).MethodsThis was an open-label, parallel-group pharmacokinetic comparison between HIV-infected, adult subjects receiving steady-state nevirapine-based ART (n= 10) and ART-naive subjects (control group,n= 11). All subjects received a loose formulation of artesunate/amodiaquine (200/600 mg) daily for 3 days, with serial pharmacokinetic sampling over 96 h following the final dose of artesunate/amodiaquine. Amodiaquine and DEAQ were quantified using a validated HPLC method with UV detection. Pharmacokinetic parameters were determined using standard non-compartmental methods.ResultsExposures to both amodiaquine and DEAQ were significantly lower in the nevirapine-based ART group compared with the control group (amodiaquine AUC0–24145 versus 204 ng·h/mL,P= 0.02; DEAQ AUC0–9614 571 versus 21 648 ng·h/mL,P< 0.01). The AUCDEAQ/AUCamodiaquineratio was not different between groups (ART group 116 versus control group 102,P= 0.67).ConclusionsSubjects on nevirapine-based ART had lower exposure to both amodiaquine and DEAQ (28.9% and 32.7%, respectively). Consequently, this may negatively impact the effectiveness of artesunate/amodiaquine in HIV-infected individuals on this ART combination.
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影响因子：
6.7
作者：
通讯作者：
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青蒿素衍生物和用于以青蒿素为基础的联合疗法治疗儿童恶性疟原虫疟疾的伴随药物的药代动力学特征
影响因子：
4.5
作者：
S. Pawluk;K. Wilby;M. H. Ensom
通讯作者：
M. H. Ensom
DOI：
10.1086/503423
发表时间：
2006-06-01
期刊：
Clinical infectious diseases : an official publication of the Infectious Diseases Society of America
影响因子：
--
作者：
Price RN;Uhlemann AC;van Vugt M;Brockman A;Hutagalung R;Nair S;Nash D;Singhasivanon P;Anderson TJ;Krishna S;White NJ;Nosten F
通讯作者：
Nosten F
阿莫地喹导致致命的急性肝炎。
影响因子：
2.9
作者：
Raymond Jm;F. Dumas;C. Baldit;P. Couzigou;C. Bĕraud;M. Amouretti
通讯作者：
M. Amouretti
影响因子：
2.1
作者：
Xu C;Desta Z
通讯作者：
Desta Z