拉替拉韦治疗艾滋病的药学机制、临床疗效与不良反应研究

Study on the Pharmaceutical Mechanism,Clinical Efficacy and Adverse Reactions of Raltegravir in the Treatment of AIDS

拉替拉韦是一种临床上较为常用的抗病毒药物,其为一种整合酶链转移抑制剂,并已获得美国FDA批准用于HIV的治疗.拉替拉韦主要作用为抗逆转录病毒复制,它主要通过尿苷二磷酸葡萄糖醛酸转移酶1A1代谢,并具有单一的无活性葡萄糖醛酸代谢产物.拉替拉韦并不受到细胞色素P450酶的影响,因而表现出较低的药物间相互作用.然而,强尿苷二磷酸葡萄糖醛酸转移酶1A1抑制剂或诱导剂可参与拉替拉韦体内的代谢、分布和排泄过程,因而可改变拉替拉韦的体内药代动力学特征.现有的证据表明,拉替拉韦具有良好的临床疗效和耐受性,能够有效抑制HIV病毒复制的同时鲜有严重不良反应报道.最常见的轻微不良反应包括头痛、恶心和腹泻,但严重不良反应较为少见.目前已报道的拉替拉韦有关的严重不良反应包括横纹肌溶解和严重的皮肤和超敏反应.本文对拉替拉韦治疗艾滋病的药学机制、临床疗效与不良反应相关文献进行了复习和总结,为拉替拉韦在艾滋病的临床应用提供参考.

Raltegravir an integrase chain transfer inhibitor,is a commonly used antiviral drug in clinical practice and has been approved by FDA for the treatment of HIV.Raltegravir acts primarily on antiretroviral replication and is metabolized by uridine diphosphate glucuronic transferase 1Al with a single inactive glucuronic acid metabolite.Raltegravir is not affected by noncytochrome P450 enzymes and thus exhibits low drug interaction.However,inhibitors or inducers of strong uridine diphosphate glucuronic transferase 1A1 May be involved in the metabolism,distribution,and excretion of Raltegravir in vivo,thus changing the pharmacokinetic profile of Raltegravir in vivo.The available evidence shows that Raltegravir has good clinical efficacy and tolerability,and can effectively inhibit HIV replication while serious adverse reactions have been reported.The most common mild adverse events include headache,nausea,and diarrhea,but severe adverse events are less common.Serious adverse events associated with Raltegravir that have been reported to date include rhabdomyolysis and severe skin and hypersensitivity reactions.In this paper,literature on the pharmaceutical mechanism,clinical efficacy and adverse reactions of Lativir in the treatment of AIDS was reviewed and summarized,so as to provide reference for the clinical application of Lativir in AIDS.