Which antifungal agent is known for its ability to penetrate the blood-brain barrier?

Fluconazole is recognized for its ability to effectively penetrate the blood-brain barrier, which is critical for treating central nervous system infections caused by fungi, particularly in cases of cryptococcal meningitis. This characteristic is attributed to its small molecular size and high water solubility, which allow it to achieve therapeutic concentrations in the cerebrospinal fluid.

In contrast, while other antifungal agents like amphotericin B may penetrate the blood-brain barrier to some extent, their efficacy is often limited due to potential toxicity and the formulation challenges associated with delivering these agents effectively to the central nervous system. Ketoconazole and caspofungin have more restricted penetrative capacities regarding the blood-brain barrier, making them less suitable for targeting fungal infections in the brain. This underlines the importance of selecting fluconazole in scenarios where central nervous system involvement is suspected or confirmed.