Podcast
Questions and Answers
What is the primary function of Entry Inhibitors in the context of HIV treatment?
What is the primary function of Entry Inhibitors in the context of HIV treatment?
Which drug is classified as a CCR5 coreceptor antagonist?
Which drug is classified as a CCR5 coreceptor antagonist?
Which of the following best describes the mechanism of Ibalizumab?
Which of the following best describes the mechanism of Ibalizumab?
What is the role of gp120 in the HIV entry process?
What is the role of gp120 in the HIV entry process?
Signup and view all the answers
Which class of antiretroviral therapy includes NRTIs?
Which class of antiretroviral therapy includes NRTIs?
Signup and view all the answers
What is the distinguishing feature of Fusion Inhibitors?
What is the distinguishing feature of Fusion Inhibitors?
Signup and view all the answers
Which entry inhibitor binds directly to the HIV virus?
Which entry inhibitor binds directly to the HIV virus?
Signup and view all the answers
In terms of therapeutic classification, which drug is a CD4 receptor blocker?
In terms of therapeutic classification, which drug is a CD4 receptor blocker?
Signup and view all the answers
What is the mechanism of action of Fostemsavir?
What is the mechanism of action of Fostemsavir?
Signup and view all the answers
What type of drug is Fostemsavir classified as?
What type of drug is Fostemsavir classified as?
Signup and view all the answers
What is a critical monitoring parameter for patients on Fostemsavir?
What is a critical monitoring parameter for patients on Fostemsavir?
Signup and view all the answers
Why should Fostemsavir not be used with CYP3A4 inducers?
Why should Fostemsavir not be used with CYP3A4 inducers?
Signup and view all the answers
In which stage of the HIV life cycle does Fostemsavir act?
In which stage of the HIV life cycle does Fostemsavir act?
Signup and view all the answers
Which of the following describes Fostemsavir's formulation?
Which of the following describes Fostemsavir's formulation?
Signup and view all the answers
What conversion occurs before Fostemsavir becomes active?
What conversion occurs before Fostemsavir becomes active?
Signup and view all the answers
What is the primary mechanism of action of nucleoside reverse transcriptase inhibitors (NRTIs)?
What is the primary mechanism of action of nucleoside reverse transcriptase inhibitors (NRTIs)?
Signup and view all the answers
Which characteristic distinguishes NRTIs from natural nucleotides?
Which characteristic distinguishes NRTIs from natural nucleotides?
Signup and view all the answers
Which of the following drugs is classified as a nucleoside reverse transcriptase inhibitor?
Which of the following drugs is classified as a nucleoside reverse transcriptase inhibitor?
Signup and view all the answers
What is a common outcome when NRTIs are incorporated into HIV DNA?
What is a common outcome when NRTIs are incorporated into HIV DNA?
Signup and view all the answers
How do NRTIs affect the translation of HIV RNA?
How do NRTIs affect the translation of HIV RNA?
Signup and view all the answers
Which of the following options best describes the role of triphosphorylated NRTIs?
Which of the following options best describes the role of triphosphorylated NRTIs?
Signup and view all the answers
What is a primary difference between TDF and TAF concerning side effects?
What is a primary difference between TDF and TAF concerning side effects?
Signup and view all the answers
Which combination includes Tenofovir disoproxil fumarate?
Which combination includes Tenofovir disoproxil fumarate?
Signup and view all the answers
Which of the following is true about how TDF and TAF are activated within the body?
Which of the following is true about how TDF and TAF are activated within the body?
Signup and view all the answers
What unique administration route is noted for zidovudine?
What unique administration route is noted for zidovudine?
Signup and view all the answers
What are the recommended monitoring parameters for patients on nucleoside reverse transcriptase inhibitors?
What are the recommended monitoring parameters for patients on nucleoside reverse transcriptase inhibitors?
Signup and view all the answers
Which of the following side effects is associated with nucleoside reverse transcriptase inhibitors?
Which of the following side effects is associated with nucleoside reverse transcriptase inhibitors?
Signup and view all the answers
What distinguishes TAF from TDF in terms of prodrug conversion?
What distinguishes TAF from TDF in terms of prodrug conversion?
Signup and view all the answers
Which nucleoside reverse transcriptase inhibitor combination is used for pre-exposure prophylaxis (PrEP)?
Which nucleoside reverse transcriptase inhibitor combination is used for pre-exposure prophylaxis (PrEP)?
Signup and view all the answers
What role does the HIV integrase enzyme play in the HIV life cycle?
What role does the HIV integrase enzyme play in the HIV life cycle?
Signup and view all the answers
What is the primary function of Integrase Strand Transfer Inhibitors (INSTIs)?
What is the primary function of Integrase Strand Transfer Inhibitors (INSTIs)?
Signup and view all the answers
What happens to HIV DNA when the integrase enzyme is inhibited by an INSTI?
What happens to HIV DNA when the integrase enzyme is inhibited by an INSTI?
Signup and view all the answers
Which of the following statements accurately describes the function of the HIV integrase enzyme?
Which of the following statements accurately describes the function of the HIV integrase enzyme?
Signup and view all the answers
What occurs during the integrase strand transfer step in the HIV life cycle?
What occurs during the integrase strand transfer step in the HIV life cycle?
Signup and view all the answers
How do INSTIs affect the overall replication process of HIV?
How do INSTIs affect the overall replication process of HIV?
Signup and view all the answers
Why is preventing the integration of HIV DNA into host DNA significant in antiretroviral therapy?
Why is preventing the integration of HIV DNA into host DNA significant in antiretroviral therapy?
Signup and view all the answers
What is the result of successful binding of INSTIs to the HIV integrase enzyme?
What is the result of successful binding of INSTIs to the HIV integrase enzyme?
Signup and view all the answers
What is the primary function of protease inhibitors in the treatment of HIV?
What is the primary function of protease inhibitors in the treatment of HIV?
Signup and view all the answers
Which mechanism does Lenacapavir utilize to act as an HIV capsid inhibitor?
Which mechanism does Lenacapavir utilize to act as an HIV capsid inhibitor?
Signup and view all the answers
What type of resistance does the protease inhibitor profile demonstrate?
What type of resistance does the protease inhibitor profile demonstrate?
Signup and view all the answers
What components are encased by the HIV capsid?
What components are encased by the HIV capsid?
Signup and view all the answers
Why are protease inhibitors considered for patients who have failed other anti-retroviral therapies?
Why are protease inhibitors considered for patients who have failed other anti-retroviral therapies?
Signup and view all the answers
Which mutation types are associated with protease inhibitor resistance?
Which mutation types are associated with protease inhibitor resistance?
Signup and view all the answers
What is a consequence of the HIV capsid being disrupted by an inhibitor like Lenacapavir?
What is a consequence of the HIV capsid being disrupted by an inhibitor like Lenacapavir?
Signup and view all the answers
What is a characteristic of the protease enzyme in HIV?
What is a characteristic of the protease enzyme in HIV?
Signup and view all the answers
Study Notes
Presentation Title
- The presentation is titled "Human Immunodeficiency Virus Pharmacology of Anti-Retroviral Therapy"
- The presenter is Akshith Dass, PharmD, BCIDP, BCPS, Assistant Professor of Pharmacy Practice at NEOMED.
- The date of the presentation is December 6th, 2024
- Slide credits are attributed to Bhavin Mistry, PharmD, BCIDP, BCPS
Learning Objectives
- Describe the life cycle of HIV
- Describe the mechanism of action of anti-retroviral agents
- Distinguish the brand and generic names of anti-retroviral agents
- Appraise unique positive and negative attributes of anti-retroviral agents
HIV Anti-Retroviral Therapy Resources
- The presentation includes references to various resources for HIV Anti-Retroviral Therapy, including National HIV Curriculum question banks and relevant textbooks, such as Pharmacotherapy Principles & Practice (6th ed.) and Goodman & Gilman's: The Pharmacological Basis of Therapeutics (14th ed.).
- Specific URLs or website addresses to resources are included
HIV Life Cycle
- The HIV life cycle is described step-by-step in the presentation
- HIV enters a host cell
- The viral RNA is converted to DNA, which then integrates into the host cell's DNA
- New viral RNA and proteins are produced
- The new viral particles bud off from the host cell
- "protease" breaks down proteins
- A diagram illustrating the HIV life cycle is included.
HIV Life Cycle with Anti-Retroviral Therapy
- A diagram illustrates the HIV life cycle and the points at which antiretroviral drugs act.
- Specific drug classes are shown with reference to their points of intervention.
Drug Classes
- Entry inhibitors, Nucleoside/tide Reverse Transcription Inhibitors (NRTIs), Non-Nucleoside Reverse Transcription Inhibitors (NNRTIs), Integrase Inhibitors (INSTIs), Protease Inhibitors (PIs), and Capsid inhibitors are named as drug classes in the presentation.
HIV Entry Inhibitors
- Inhibitors are listed to block the HIV entry process
- Fostemsavir, Ibalizumab, Maraviroc, and Enfuvirtide block different stages of HIV entry.
CD4/gp120 Attachment Inhibitor
- Fostemsavir (Rukobia) is a drug to block HIV attachment
- Mechanism of action: Prodrug converted to temsavir, acting on gp120 to stop interaction with the host CD4 receptor.
CD4-Post Attachment Inhibitor
- Ibalizumab(Trogarzo) intervenes after gp120 binds, preventing structural changes needed for viral entry.
CCR5 Receptor Antagonist: Maraviroc
- Maraviroc (Selzentry) prevents HIV binding by blocking the CCR5 chemokine receptor.
- Maraviroc only works with CCR5 coreceptor.
Fusion Inhibitor: Enfuvirtide
- Enfuvirtide (Fuzeon) is a fusion inhibitor interfering with HIV gp41 function.
Reverse Transcriptase Inhibitors
- The presentation describes the mechanism of nucleoside and non-nucleoside reverse transcriptase inhibitors (NRTIs and NNRTIs), highlighting that they both prevent HIV RNA from being turned into HIV DNA.
Nucleoside Reverse Transcriptase Inhibitors (NRTIs)
- The presentation describes that NRTIs are tri-phosphorylated and mimic human nucleotides, but unlike human nucleotides, they don't have a 3'-hydroxyl group. This prevents reverse transcriptase from adding additional nucleotides to the growing chain, stopping the conversion of HIV RNA to DNA.
- The presentation lists specific drugs, as well as combination drugs, under the category of NRTIs.
Non-Nucleoside Reverse Transcriptase Inhibitors (NNRTIs)
- NNRTIs bind to a pocket near the active site on the reverse transcriptase enzyme preventing HIV RNA to be converted to HIV DNA. They cause a conformational change.
- A series of NNRTI drug names are listed.
INSTI (Integrase Strand Transfer Inhibitors)
- INSTIs block the HIV integrase gene process, preventing HIV DNA from integrating into the host DNA, which is needed to reproduce copies of the virus.
- Various drugs under the INSTI category are named.
HIV Protease Inhibitors (PIs)
- PIs bind to the HIV protease enzyme active site, halting the maturation process of HIV, preventing the infection of healthy cells.
- Atazanavir(Reyataz) and Darunavir (Prezista) are protease inhibitors under discussion.
Boosters or Pharmacokinetic Enhancers
- Ritonavir (Norvir) and Cobicistat (Tybost) are named as boosters for other PIs, enhancing the concentration of other active compounds.
Protease Inhibitor Combinations
- Various protease inhibitor combinations are detailed.
Generalizing the Pl's/NRTIs/NNRTIs/INSTIs
- Presentation covers important general aspects of the drugs. Information includes metabolization by the body and important side effects.
Agent-Specific Toxicity
- Various drugs and their associated toxicities are noted.
INSTI - Resistance
- INSTI resistance is rare.
- In some cases, INSTIs can be used even if HIV resistance to other drugs is present.
HIV Capsid Inhibitor
- This section describes lenacapavir (Sunlenca), a capsid inhibitor that blocks viral capsid structure and function, hindering viral maturation.
HIV Capsid Inhibitor - Lenacapavir Factoids
- The presentation includes information about lenacapavir's administration: two induction regimens, injection sites, and monitoring parameters, like serum creatinine.
Studying That Suits You
Use AI to generate personalized quizzes and flashcards to suit your learning preferences.
Related Documents
Description
Test your knowledge on the different classes of antiretroviral drugs, specifically focusing on entry inhibitors in HIV treatment. The quiz covers critical aspects such as mechanisms of action, drug classifications, and monitoring parameters related to these therapies.
