恩曲他滨的药理和临床应用

据世界卫生组织报道,自1981年发现和报告艾滋病以来,全球感染者已累计6900万人,其中死亡人数占40%,每年约新增500多万HIV(人类免疫缺陷病毒)感染病例,目前HIV/AIDS(获得性免疫缺陷综合征)患者总数达4200多万人,若不能有效的预防控制,预计20年后HIV感染者将达2亿人。从地域上看,在撒哈拉以南的非洲地区患者占70%,而病死率已达八成;在拉丁美洲和加勒比地区流行率也较高,60%感染者失去生命,而亚洲也已呈现出快速蔓延的趋势。随着HIV在全球的快速蔓延,抗HIV药物的发展已成为目前研究的热点。恩曲他滨(emtricitabine)是由美国Gilead Sci…     

替诺福韦抗病毒感染最新研究进展

替诺福韦是一种核苷酸类逆转录酶抑制剂,对人免疫缺陷病毒（HIV）和乙型肝炎病毒（HBV）均有良好的抑制作用,临床应用广泛。本文综述替诺福韦在HIV抗逆转录病毒治疗、暴露前预防和HBV治疗领域的最新研究成果,旨在为临床诊疗提供参考。     

妊娠期和哺乳期抗乙肝病毒药物治疗的安全性

乙型肝炎病毒（HBV）感染呈世界性流行,母婴传播是我国HBV感染的主要传播途径,育龄期女性常常面对妊娠期和哺乳期的抗病毒治疗问题。本文通过检索国内外数据库文献,综述了目前我国所有批准用于抗乙肝病毒感染药物（包括干扰素α、拉米夫定、替比夫定、替诺福韦酯、恩替卡韦、阿德福韦酯和恩曲他滨）在妊娠期和哺乳期使用的安全性数据和经验,依次从胎盘转运、动物生殖毒性和致畸性研究、人类妊娠期使用经验、药物乳汁分泌及人类哺乳期使用经验4方面进行阐述。其中替诺福韦和替比夫定研究资料相对较多,动物研究未发现致畸性,人类妊娠期使用也未见出生缺陷发生率增加,可作为妊娠期抗HBV治疗的选择。拉米夫定在妊娠期应用广泛（HIV治疗）,未发现出生缺陷发生率增加,故也可作为妊娠期抗HBV治疗的选择之一。     

日本上市两种抗HIV药物

由日本烟草产业株式会社生产的抗HIV药物恩曲他滨(emtricitabine)的胶囊(商品名：Emtriva)以及恩曲他滨(200mg)与替诺福韦(300mg)的复方片剂(商品名：Truvada)于3月23日获得日本厚生劳动省的批准,4月19日上市销售。它们的用药剂量都是一天口服1次,价格分别为1750．90日元/粒和3862．80日元/片。     

人类免疫缺陷病毒感染与冠心病

自从抗逆转录病毒治疗问世以后,获得性免疫缺陷综合征患者的寿命延长。获得性免疫缺陷综合征患者冠心病和心肌梗死的危险性高于一般人群。其病因与这些患者冠心病危险因素增加、人类免疫缺陷病毒感染本身及抗逆转录病毒治疗等有关。慢性炎症和免疫激活也在冠心病的病理生理中发挥重要作用。     

高载药量的恩曲他滨替诺福韦片处方优化研究

目的 研究一种高载药量的恩曲他滨替诺福韦复方片处方,优化其处方配伍方案。 方法 在对国外上市制剂的处方工艺进行分析的基础上,进行稳定剂、填充剂、崩解剂、黏合剂的筛选和最终处方的放大验证,确定合理可行的处方工艺。结果 以处方解析确定的高风险因素为考察指标,确定了高载药量的恩曲他滨替诺福韦片的处方:每片含恩曲他滨200 mg,富马酸替诺福韦二吡呋酯300 mg,预胶化淀粉60 mg,微晶纤维素100 mg,交联羧甲基纤维素钠30 mg,硬脂酸镁5 mg,95%乙醇为黏合剂。自制片与对照片质量比对结果一致。结论 筛选的恩曲他滨替诺福韦复方片处方工艺合理可行,产品重现性和稳定性好。     

免疫缺陷综合征儿童的特点与护理

美国自1983年发现第一例儿童获得性免疫缺陷综合征（AIDS）患者以来，到20世纪90年代，人类获得性免疫缺陷病毒（HIV）已成为引起1～4岁儿童死亡的十大原因之一。截至1994年，美国有7500名儿童发展为AIDS患儿，在随后的10年里，至少有125000名儿童成为这一流行病的孤儿。迄今为止，AIDS已经吞噬了全球300万儿童的生命，现今还有100万儿童感染HIV，在新感染者中占l／10。     

HIV感染/艾滋病患者富马酸替诺福韦二吡呋酯相关范可尼综合征临床特征分析

目的探讨HIV感染/艾滋病(HIV/AIDS)患者富马酸替诺福韦二吡呋酯(TDF)相关范可尼综合征(FS)的临床特征。方法检索医院信息系统, 收集2017年12月至2021年2月在云南省传染病医院住院且采用含TDF的抗反转录病毒治疗(ART)并诊断为FS的HIV/AIDS患者的病历资料, 包括性别、年龄、体重、体重指数(BMI)、ART治疗方案和时间、诊断FS时间、主要临床表现、入院及出院实验室检查结果, 双能X射线骨密度检查结果以及干预和转归等信息, 进行回顾性分析。结果设定时段内诊断为TDF相关FS的HIV/AIDS患者共16例, 其中完全型FS 6例, 不完全型FS 10例;7例合并慢性丙型肝炎、高血压病、肝癌和抑郁症等慢性疾病;16例患者接受含TDF的ART治疗时间最短20个月, 最长168个月, 平均68个月;FS的初始症状多为骨痛、乏力、恶心、纳差、多饮、多尿, 体重下降等, 从出现初始症状至确诊FS的时间最短2周, 最长24周, 平均7周。实验室检查结果显示, 16例患者在血糖正常情况下尿葡萄糖均为阳性, 14例尿蛋白阳性, 低尿磷、低尿钙、低尿钾和低尿钠者分别为11、1...     

恩曲他滨与替诺福韦的专利保护现状与市场应用前景分析

笔者通过检索中国专利检索系统文摘数据库（CPRSABS）,对1992–2013年间治疗获得性免疫缺陷综合征（AIDS）的核苷类逆转录酶抑制剂恩曲他滨、替诺福韦及两者的复方制剂在中国的专利保护现状进行分析,为中国企业和研究机构提供专利预警和应对建议,使其在药物研发、专利保护方面更加有针对性,更准确地把握临床应用趋势,赢得市场。     

抗人类免疫缺陷病毒感染的药物治疗进展

近年来 ,抗HIV感染药物的研究取得了巨大的进步 ,对艾磁病的控制和治疗具有重大意义。本文综述了国内外抗HIV感染的研究情况 ,从机制、应用与注意事项几个方面分别作介绍。     

Immunotherapy of human immunodeficiency virus infection

HIV infection results in the destruction of the thymus-dependent cellular immune system and death due to opportunistic infection and malignancy. Immunosuppressive influences (other sexually or blood-transmitted viruses, HIV-derived peptides, semen, poor nutrition, drugs, etc.) favor the progression of the disease. Although immunorestorative agents may be expected to delay progression of the disease, John Hadden argues that no agent has yet proven useful in reversing the immunodeficiency in full-blown AIDS. However, two thymomimetic drugs, isoprinosine and diethyldithiocarbamate, inhibit the development of infections in patients with pre-AIDS in large multicenter trials, and preliminary data from trials with two thymomimetic peptides, thymopentin and ImReg-1, in pre-AIDS patients are encouraging.     

Safety of single-dose nevirapine for prevention of vertical transmission of human immunodeficiency virus infection

Introduction:

Nevirapine administered as a single dose each to the mother and child within 72 h after birth is used to prevent vertical transmission of human immunodeficiency virus (HIV) under the prevention of parent to child transmission of HIV program (PPTCT). The efficacy of nevirapine in this regard has been proved beyond doubt, but there are unresolved questions about its safety. Hence, the primary objective of this study was to evaluate the safety of this regime.

Materials and Methods:

HIV-positive pregnant women who consented to participate in the study received a single oral dose of 200 mg nevirapine at the onset of labor followed by administration of 2 mg/kg of nevirapine syrup to the newborn within 72 h of birth. Both mother and child were followed up for 1 week postpartum to note the occurrence of any adverse reactions.

Results:

The mother and child followed up for 1 week postpartum did not show any serious adverse reactions in the present study. Mothers reported adverse reactions like nausea, vomiting, and headache which were self-limiting and did not require any intervention.

Conclusion:

The present study substantiates the safety of nevirapine.     

Immunology of the human immunodeficiency virus infection

From the beginning of the AIDS epidemic it was realized, that the immune system is the major target of the disease. After isolation of the ethiological agent -named the human immunodeficiency virus became clear that there is a dual relationship between the immune system and HIV, i.e. HIV attaques the immune system and the immune system attaques the HIV. The present communication gives a brief review of both aspects of the HIV infection. It is emphasised that both aspects of the relationship have inherent complexities illustrated on the one hand by the findings that the immunodeficiency cannot be explained solely by the established pathogenetic mechanism of lysis of the CD4+ T lymphocytes with ultimate depletion of the cells, and on the other hand by the fact that the virus manage to establish itself as a relentlessly progressing infection in seemingly all infected humans in spite of a vigorous anti-HIV directed immune response.     

围产期母婴人免疫缺陷病毒感染的药物治疗

15岁以下儿童人免疫缺陷病毒(HIV)感染的最主要途径是母婴传播,采取剖宫产、人工喂养和早期使用抗病毒药物等综合干预手段可以明显降低母婴传播率.对围产期感染HIV的母婴进行早期合理的抗病毒药物干预,可以有效地保障母婴健康.本文综述围产期母婴HIV感染的药物治疗时机、用药方案及药物不良反应等.     

Atazanavir for the treatment of human immunodeficiency virus infection

Atazanavir is the first once-daily protease inhibitor for the treatment of human immunodeficiency virus type 1 infection and should be used only in combination therapy, as part of a highly active antiretroviral therapy (HAART) regimen. In addition to being the most potent protease inhibitor in vitro, atazanavir has a distinct cross-resistance profile that does not confer resistance to other protease inhibitors. However, resistance to other protease inhibitors often confers clinically relevant resistance to atazanavir. Currently, atazanavir is not a preferred protease inhibitor for initial HAART regimens. In treatment-naive patients, atazanavir can be given as 400 mg/day. However, atazanavir should be pharmacologically boosted with ritonavir in treatment-experienced patients or when coadministered with either tenofovir or efavirenz. Patients who receive atazanavir experience similar rates of adverse events compared with patients receiving comparator regimens. An exception is an increased risk of asymptomatic hyperbilirubinemia, which is due to competitive inhibition of uridine diphosphate-glucuronosyltransferase 1A1. Although hyperbilirubinemia is a common adverse drug reaction of atazanavir therapy (22-47%), fewer than 2% of patients discontinue atazanavir therapy because of this adverse effect. Common adverse effects reported with atazanavir include infection, nausea, vomiting, diarrhea, abdominal pain, headache, peripheral neuropathy, and rash. Of significance, fewer abnormalities have been observed in plasma lipid profiles in patients treated with atazanavir compared with other protease inhibitor-containing regimens. As with other protease inhibitors, atazanavir is also a substrate and moderate inhibitor of the cytochrome P450 (CYP) system, in particular CYP3A4 and CYP2C9. Clinically significant drug interactions include (but are not limited to) antacids, proton pump inhibitors, histamine type 2 receptor antagonists, tenofovir, diltiazem, irinotecan, simvastatin, lovastatin, St. John's wort, and warfarin. We conclude that atazanavir is a distinctively characteristic protease inhibitor owing to its in vitro potency, once-daily dosing, distinct initial resistance pattern, and infrequent association with metabolic abnormalities.     

Serological survey of human immunodeficiency virus infection in Ethiopia

A serological survey was conducted on 1754 people in various parts of Ethiopia from 1982-1987, with no HIV positive findings until 1984. The problem of Aids reached epidemic proportion in North America and Central Africa in the early 1980s. The reasons for delayed appearance and the source of HIV infection in Ethiopia are not clear. There were 4 groups of subjects tested. The 1st from 1982-83 consisted of 500 patients: 100 each from Asmara, Harar, Addis Ababa, Yirga Alem, and Nekemte; the 2nd in 1983 consisted of 459 volunteer blood donors in Addis Ababa; the 3rd in 1984 consisted of 167 patients with Bell's palsy, and 100 others; the 4th from 1985-87 consisted of 528 patients of the liver clinic of Tikur Anbessa Hospital. The 1st 2 HIV positive sera appeared in group 3 during 1984, and since then 13 patients examined for liver and gastrointestinal conditions were found to be positive. It may be speculated that the new and delayed introduction of HIV infection into Ethiopia is part of the transcontinental spread, caused by migration of refugees, frequent visits to existing harbors by sailors, and the influx of many international organizations to Addis Ababa where prostitution is common. Considering the high prevalence of HIV infection among prostitutes, promiscuity might be the major mode of transmission in this population. The multiple use of inadequately sterilized hypodermics and blood transfusions without screening also contribute to the spread of HIV infection.