Antiretroviral Agents: Drug Classes and Key Drugs

Vocabulary flashcards covering major antiretroviral drug classes and representative agents mentioned in the video notes.

Nucleoside reverse transcriptase inhibitors (NRTIs)

A class of antiretroviral drugs that are nucleoside analogs; after phosphorylation they inhibit HIV reverse transcriptase and terminate DNA synthesis.

Nucleotide reverse transcriptase inhibitors (NtRTIs)

A class of RT inhibitors that are nucleotides; require fewer phosphorylation steps and inhibit RT (example: tenofovir).

Emtricitabine (FTC)

An NRTI used to inhibit HIV reverse transcriptase; commonly part of combination regimens.

Lamivudine (3TC)

An NRTI that inhibits HIV reverse transcriptase; often used in combination therapies.

Abacavir

An NRTI used in HIV treatment; associated with hypersensitivity reactions in certain HLA-B*57:01 carriers.

Tenofovir

A nucleotide reverse transcriptase inhibitor (NtRTI); active against HIV and hepatitis B; available as TDF or TAF prodrugs.

Non-nucleoside reverse transcriptase inhibitors (NNRTIs)

A class of RT inhibitors that bind RT at an allosteric site, causing a conformational change and inhibition.

Nevirapine

An NNRTI used in various HIV regimens; resistance and safety considerations apply.

Etravirine

A second-generation NNRTI with activity against some resistant HIV strains.

Rilpivirine

An NNRTI with a long half-life; used in several single-pill regimens.

Doravirine

A newer NNRTI with activity against common NNRTI-resistant HIV strains.

Protease inhibitors (PIs)

Inhibit HIV protease, preventing maturation of viral particles; often boosted with ritonavir or cobicistat.

Ritonavir

A protease inhibitor used primarily as a pharmacokinetic booster to raise levels of other PIs; has limited direct ARV activity at boosting doses.

Darunavir

A potent PI commonly boosted with ritonavir or cobicistat in regimens.

Atazanavir

A protease inhibitor often boosted; may cause hyperbilirubinemia and other metabolic effects.

Fusion inhibitors

Block the fusion of HIV with host cells to prevent entry.

Enfuvirtide

A peptide fusion inhibitor that prevents viral membrane fusion; administered by subcutaneous injection.

Attachment inhibitors

Block HIV from attaching to the host cell by targeting gp120 or CD4 interaction.

Fostemsavir

An attachment inhibitor (gp120 blocker) used to prevent HIV entry.

Post-attachment inhibitors

Block HIV after attachment to the CD4 receptor; ibalizumab is the clinical example.

Ibalizumab

A monoclonal antibody that acts as a post-attachment inhibitor by binding CD4 and blocking HIV entry.

CCR5 coreceptor antagonists

Block the CCR5 co-receptor to prevent CCR5-tropic HIV from entering cells; maraviroc is a primary example.

Maraviroc

A CCR5 antagonist used to prevent HIV entry in CCR5-tropic infections.

Integrase strand transfer inhibitors (INSTIs)

Inhibit HIV integrase, preventing integration of viral DNA into the host genome.

Raltegravir

The first approved INSTI; inhibits integrase to block viral DNA integration.

Dolutegravir

A high-barrier INSTI commonly used in first-line regimens.

Elvitegravir

An INSTI often given with cobicistat as a single-tablet regimens booster.

Cabotegravir

A long-acting INSTI used for maintenance therapy in injectable form.

Lenacapavir

A capsid inhibitor that disrupts HIV replication by targeting the viral capsid.

Capsid inhibitors

A newer class targeting the HIV capsid; lenacapavir is a key example.

Pharmacokinetic boosters

Agents that increase ARV drug levels (e.g., ritonavir, cobicistat) to boost other drugs; they provide boosting rather than direct ARV activity.

Cobicistat

A pharmacokinetic booster used to enhance levels of certain PIs and INSTIs; has no direct ARV activity.