What class of drugs, such as Ketoconazole, interacts with Amlodipine via CYP3A4 inhibition?
Azole Antifungals
Azole Antifungals, including specific compounds like ketoconazole or itraconazole, are characterized as potent inhibitors of the CYP3A4 enzyme system in the liver. Since amlodipine is metabolized by this identical enzyme, the presence of these antifungals severely hampers the body's ability to break down the calcium channel blocker. This strong inhibition leads directly to elevated concentrations of amlodipine remaining active in the patient's systemic circulation. Similar to the interaction caused by grapefruit juice, this unintended high level of amlodipine increases the risk of adverse effects, most notably hypotension, resulting in dizziness or fainting. Antivirals, such as ritonavir, which is sometimes used in combination therapies like Paxlovid, can exert an analogous inhibitory effect via the same metabolic pathway.
