Pharmacology of HIV/AIDS Drugs PDF

Pharmacology of HIV/AIDS Drugs Exploring the pharmacological properties and mechanisms of action of the various drug classes used to treat HIV/AIDS, a devastating global pandemic. by Molecular Biology Molecular Simulation Introduction to HIV/AIDS 1 HIV: Human 2 AID...

Pharmacology of HIV/AIDS Drugs Exploring the pharmacological properties and mechanisms of action of the various drug classes used to treat HIV/AIDS, a devastating global pandemic. by Molecular Biology Molecular Simulation Introduction to HIV/AIDS 1 HIV: Human 2 AIDS: Acquired 3 Global Impact Immunodeficiency Virus Immunodeficiency HIV/AIDS remains a major public A retrovirus that attacks the Syndrome health concern worldwide, with immune system, leading to AIDS if The advanced stage of HIV millions of people affected. left untreated. infection, marked by the development of opportunistic infections. Overview of HIV Life Cycle 1 Entry HIV binds to and fuses with the host cell, injecting its genetic material. 2 Replication The viral genome is integrated into the host cell's DNA, and new viral particles are produced. 3 Release The newly formed virus particles bud from the host cell, ready to infect other cells. Antiretroviral Drug Classes NRTIs NNRTIs PIs Nucleoside/Nucleotide Reverse Non-Nucleoside Reverse Transcriptase Protease Inhibitors Transcriptase Inhibitors Inhibitors Disrupt the processing of viral proteins, Interfere with the reverse transcription Bind directly to the reverse preventing the formation of mature, process, preventing viral DNA transcriptase enzyme, blocking its infectious viral particles. synthesis. activity. Mechanism of Action of NRTIs Structural Similarity Chain Termination NRTIs mimic the structure of Once incorporated, NRTIs lack natural nucleosides, allowing the necessary 3' hydroxyl them to be incorporated into the group, preventing further DNA growing viral DNA chain. synthesis and halting viral replication. Competitive Inhibition NRTIs compete with natural nucleosides for binding to the reverse transcriptase enzyme, further disrupting viral DNA synthesis. Mechanism of Action of NNRTIs 1 2 3 Binding to Reverse Conformational Changes Inhibition of DNA Synthesis Transcriptase This binding induces conformational By inhibiting the reverse transcriptase NNRTIs bind to a specific pocket in the changes in the enzyme, disrupting its enzyme, NNRTIs prevent the synthesis reverse transcriptase enzyme, distinct catalytic activity. of viral DNA, halting viral replication. from the active site. Mechanism of Action of PIs Protease Inhibition Immature Viral Particles Disruption of Viral Replication PIs target the HIV protease enzyme, By inhibiting protease, PIs prevent the The production of functional viral which is essential for processing viral maturation of viral particles, rendering proteins is disrupted, ultimately inhibiting proteins. them non-infectious. the overall viral replication cycle. Mechanism of Action of INSTIs Integrase Inhibition INSTIs target the HIV integrase enzyme, which is responsible for inserting the viral genome into the host cell's DNA. Blocking Integration By inhibiting the integrase enzyme, INSTIs prevent the integration of viral DNA, halting the viral replication cycle. Preventing Proviral Formation Without successful integration, the viral genome cannot be incorporated into the host cell's DNA, preventing the formation of the latent proviral reservoir. Combination Antiretroviral Therapy 1 Synergistic Effects Using multiple antiretroviral drugs with different mechanisms of action enhances the suppression of viral replication. 2 Delayed Resistance Combination therapy makes it more difficult for the virus to develop resistance, improving long-term treatment efficacy. 3 Improved Outcomes Combination therapy has led to significant advancements in the management of HIV/AIDS, reducing morbidity and mortality. Adverse Effects and Drug Interactions 1 Metabolic 2 Hepatotoxicity Complications Certain antiretroviral drugs Antiretroviral drugs can lead can cause liver damage, to metabolic changes, such requiring close monitoring as lipodystrophy, and management. dyslipidemia, and insulin resistance. 3 Drug Interactions Antiretrovirals may interact with other medications, necessitating careful consideration of potential side effects and adjustments in dosing.