Ogedengbe Oluwatosin O, Naidu Edwin C S, Azu Onyemaechi O
Discipline of Clinical Anatomy, Nelson R. Mandela School of Medicine, University of Kwazulu-Natal, Durban, South Africa.
Department of Anatomy, College of Medicine and Health Sciences, Afe Babalola University, Ado Ekiti, Nigeria.
Eur J Drug Metab Pharmacokinet. 2018 Apr;43(2):121-135. doi: 10.1007/s13318-017-0438-6.
The prevalence of alcohol use among HIV-infected patients undergoing antiretroviral (ARV) treatments has raised several concerns related to key therapeutic indices. These include drug interactions, compliance, efficacy and toxicity with the possibility of accelerated disease progression. Interaction of ARVs with alcohol can result in therapeutic failures or place patients at significant risk for toxicities. Research findings in this particular area are, however, limited and sometimes conflicting. This review focuses on alcohol and ARV interactions affecting testicular and spermatogenic indices. Antiretroviral drugs are known to negatively impact testicular functions via altered mitochondrial DNA and oxidative stress mechanisms. Interaction with alcohol can significantly affect seminal fluid concentration of ARVs. Habitual consumption of alcohol causes testicular hypofunction with potential for lowered fertility. Concomitant use of ARVs appears to act synergistically to exacerbate this toxicity. Alcohol also induces cytochrome P450 (CYPs) microsomal enzymes, which in turn affect ARVs metabolized by these enzymes. In the presence of ARVs with strong inhibitory activity, increased bioavailability with toxicities predominates. In addition, alcohol and ARVs have pronounced effects on membrane-associated drug transporters. Alcohol alters the properties of the lipid bilayer by changing membrane permeability and protein distribution. Since drug transporters critical to pharmacokinetics are integral membrane proteins, alcohol tends to diminish the activity of both the efflux and influx transporters. While excessive alcohol precipitates accelerated hypogonadism, future research needs to be directed to quantifying these effects of alcohol and ARVs in human testicular tissue.
接受抗逆转录病毒(ARV)治疗的HIV感染患者中酒精使用的流行率引发了一些与关键治疗指标相关的担忧。这些包括药物相互作用、依从性、疗效和毒性,以及疾病加速进展的可能性。抗逆转录病毒药物与酒精的相互作用可能导致治疗失败或使患者面临显著的毒性风险。然而,这一特定领域的研究结果有限,有时还相互矛盾。本综述聚焦于影响睾丸和生精指标的酒精与抗逆转录病毒药物的相互作用。已知抗逆转录病毒药物会通过改变线粒体DNA和氧化应激机制对睾丸功能产生负面影响。与酒精的相互作用会显著影响抗逆转录病毒药物在精液中的浓度。习惯性饮酒会导致睾丸功能减退,有可能降低生育能力。同时使用抗逆转录病毒药物似乎会协同作用加剧这种毒性。酒精还会诱导细胞色素P450(CYPs)微粒体酶,进而影响由这些酶代谢的抗逆转录病毒药物。在存在具有强抑制活性的抗逆转录病毒药物时,生物利用度增加且毒性占主导。此外,酒精和抗逆转录病毒药物对膜相关药物转运体有显著影响。酒精通过改变膜通透性和蛋白质分布来改变脂质双层的性质。由于对药代动力学至关重要的药物转运体是整合膜蛋白,酒精往往会降低外排和内流转运体的活性。虽然过量饮酒会加速性腺功能减退,但未来的研究需要致力于量化酒精和抗逆转录病毒药物在人类睾丸组织中的这些影响。