A magisterial survey of all aspects of the reverse transcriptase inhibitors (RTIs) used to treat HIV/AIDS, including drug discovery, pharmacology, development of drug resistance, toxicity, and prevention of mother-to-child transmission of HIV/AIDS. The authors synthesize our current understanding of the role of reverse transcriptase in the viral life cycle, describe the discovery and development of eight nucleoside and nucleotide analogs that represent milestones in treatment history, and thoroughly discuss the question of toxicity and resistance to this class of drugs. They also address three non-nucleoside RTIs and their pharmacokinetics and comparative clinical efficacy, new RTIs currently under development, and the impact of approved agents on treatment, in general, and on vertical transmission in the developing world.

Includes supplementary material: sn.pub/extras

Texte du rabat
Despite significant pharmacological advances, the backbone of the most highly active antiretroviral therapy regimens for controlling HIV/AIDS is still a combination of reverse transcriptase inhibitors (RTIs) first discovered in the late 1980s. In Reverse Transcriptase Inhibitors in HIV/AIDS Therapy, leading experts in AIDS/HIV drug discovery and development review all aspects of RTIs (nucleosides, nucleotides, and non-nucleosides), including drug discovery, pharmacology, development of drug resistance, toxicity, and prevention of mother-to-child transmission of HIV/AIDS. The authors synthesize our current understanding of the role of reverse transcriptase in the viral life cycle, describe the discovery and development of eight nucleoside and nucleotide analogs that represent milestones in treatment history, and thoroughly discuss the question of toxicity and resistance to this class of drugs. They also address three non-nucleoside RTIs and their pharmacokinetics and comparative clinical efficacy, new RTIs currently under development, and the impact of approved agents on treatment in general, and on vertical transmission in the developing world. Highlights include a thorough discussion of side effects, resistance, and treatment in the third world.
Comprehensive and up-to-date, Reverse Transcriptase Inhibitors in HIIV/AIDS Therapy offers a magisterial survey of the discovery, clinical development, current use, and future possibilities of all drugs that treat HIV/AIDS by inhibiting the viral reverse transcriptase.

Contenu
Structural Studies on HIV Reverse Transcriptase Related to Drug Discovery.- Zidovudine, Lamivudine, and Abacavir.- Stavudine, Didanosine, and Zalcitabine.- Emtricitabine.- Nucleotide Analogs.- Resistance to Nucleoside and Nucleotide Reverse Transcriptase Inhibitors.- Pharmacokinetics of Reverse Transcriptase Inhibitors.- Peripheral Neuropathy Associated With Nucleoside Reverse Transcriptase Inhibitor Therapy.- Mitochondrial Dysfunction and Nucleoside Reverse Transcriptase Inhibitor Therapy.- Mitochondrial Toxicity and Lipodystrophy.- Nevirapine.- Efavirenz.- Delavirdine.- Resistance to Non-Nucleoside Reverse Transcriptase Inhibitors.- Vertical Transmission of HIV and Therapeutic Interventions.- New Reverse Transcriptase Inhibitors in Development.- Antiretroviral Drugs for Millions.