What are the antiretroviral treatments for HIV (Human Immunodeficiency Virus) infection?

Antiretroviral Treatments for HIV Infection

The main classes of antiretroviral treatments for HIV infection are reverse transcriptase inhibitors, protease inhibitors, and integrase inhibitors. These drug classes target different stages of the HIV life cycle and are used in combination to effectively suppress viral replication 1.

Approved Antiretroviral Drug Classes

Reverse Transcriptase Inhibitors

• This class includes two subtypes:
  • Nucleoside/nucleotide reverse transcriptase inhibitors (NRTIs): These drugs act as chain terminators by lacking a 3' hydroxyl group on their ribose moiety 2
  • Non-nucleoside reverse transcriptase inhibitors (NNRTIs): These bind to a hydrophobic pocket near the polymerase active site to inhibit the chemical step of polymerization 2
• Examples include efavirenz (NNRTI), which is indicated for HIV-1 infection treatment in combination with other antiretroviral agents 3

Protease Inhibitors (PIs)

• These drugs target the viral protease enzyme that is essential for viral maturation 1
• Examples include darunavir (boosted with ritonavir or cobicistat), which is recommended as part of combination therapy 1

Integrase Strand Transfer Inhibitors (INSTIs)

• These drugs prevent the integration of viral DNA into the host cell genome 4
• Examples include:
  • Dolutegravir, which is indicated in combination with other antiretroviral agents for HIV-1 infection 5
  • Raltegravir, which is used in combination with other antiretroviral agents 6
  • Other approved INSTIs include elvitegravir, bictegravir, and cabotegravir 4

Other Approved Antiretroviral Drug Classes

Entry/Fusion Inhibitors

• These target the viral entry process by:
  • Blocking attachment to CD4 receptors 7
  • Inhibiting co-receptor binding (CCR5 antagonists) 7, 8
  • Preventing fusion of viral and cellular membranes 7
• Examples include enfuvirtide (fusion inhibitor) and maraviroc (CCR5 antagonist) 7, 8

Current Treatment Recommendations

• Integrase inhibitor-based regimens are generally recommended as first-line therapy due to their high efficacy and favorable side effect profile 1
• Recommended initial regimens typically include:
  • Bictegravir/tenofovir alafenamide/emtricitabine 1
  • Dolutegravir/abacavir/lamivudine 1
  • Dolutegravir plus tenofovir alafenamide/emtricitabine 1
• Alternative regimens may include protease inhibitor-based or NNRTI-based combinations 1

Important Considerations

• Antiretroviral therapy should be initiated as soon as possible after diagnosis to reduce morbidity and mortality 1
• Drug resistance testing should be performed before starting therapy to guide regimen selection 1
• Combination therapy using multiple drug classes is essential to prevent the development of resistance 9, 8
• Treatment selection should consider patient-specific factors such as comorbidities, potential drug interactions, and pregnancy status 1

Answer to Multiple Choice Question

Based on the evidence, the correct antiretroviral treatments for HIV infection are:

• Reverse transcriptase inhibitors 2
• Protease inhibitors 1
• Integrase inhibitors 4

DMARDs (disease-modifying antirheumatic drugs) are not HIV treatments but are used for autoimmune conditions. CCR5 receptor activators do not exist as HIV treatments; instead, CCR5 antagonists (not activators) are used. Protease enhancers are not a recognized class; protease inhibitors are the correct term 1, 7, 9.