Raltegravir–omeprazole

Raltegravir–omeprazole refers to the pharmacological interaction between the HIV-1 integrase inhibitor raltegravir and the proton pump inhibitor omeprazole, rather than a single biological target [1, 2]. Raltegravir is an antiretroviral medication that targets the HIV-1 integrase enzyme, blocking the covalent insertion of the viral genome into the host cell DNA [2, 4]. Omeprazole is a gastric acid-suppressing agent that irreversibly inhibits the H+/K+ ATPase enzyme system, also known as the proton pump, in the parietal cells of the stomach [7, 9]. The interaction between these two drugs is primarily pharmacokinetic; by increasing gastric pH, omeprazole enhances the solubility and absorption of raltegravir, leading to significantly higher plasma levels of the antiviral drug [1, 4]. Although co-administration increases raltegravir exposure, including its area under the curve (AUC) and maximum concentration (Cmax), clinical data suggest this interaction does not necessitate dose adjustments in most patients [3, 5].

Other names

Raltegravir and Omeprazole interactionRaltegravir/Omeprazole co-administrationRaltegravir-PPI interaction

Raltegravir inhibits the HIV-1 integrase enzyme, preventing the covalent insertion of the viral genome into host cell DNA [2, 4]. Omeprazole irreversibly inhibits the gastric H+/K+ ATPase (proton pump), reducing the secretion of hydrochloric acid into the stomach lumen [7, 9]. The interaction between these agents is pharmacokinetic, where omeprazole-induced increases in gastric pH enhance the solubility and bioavailability of raltegravir [1, 4].