Which antiretroviral drug class requires separation from antacids due to chelation with polyvalent cations?

Integrase inhibitors are a class of antiretroviral drugs that are important in the treatment of HIV. They work by inhibiting the integrase enzyme, which is crucial for the viral DNA to be integrated into the host cell’s DNA. One significant pharmacokinetic consideration with integrase inhibitors, such as raltegravir and dolutegravir, is their interaction with polyvalent cations found in antacids.

When integrase inhibitors are taken simultaneously with antacids containing metals like magnesium, aluminum, or calcium, a chelation reaction can occur. This reaction results in the formation of insoluble complexes that significantly reduce the absorption and bioavailability of the integrase inhibitors. Therefore, a separation of administration times—usually by at least two hours before or six hours after taking antacids—is necessary to ensure the effectiveness of the integrase inhibitor therapy.

This consideration is specific to integrase inhibitors and not to other classes such as nonnucleoside reverse transcriptase inhibitors, protease inhibitors, or entry inhibitors, which do not share this particular interaction with antacids. Thus, understanding the unique properties and interactions of integrase inhibitors is essential for proper patient management and to optimize therapeutic outcomes.