ketoconazole + sufentanil

Ketoconazole + sufentanil is a combination of two pharmaceutical agents with distinct mechanisms of action. Ketoconazole is an imidazole antifungal agent that inhibits fungal ergosterol synthesis by blocking the cytochrome P450-dependent enzyme lanosterol 14α-demethylase. It is also a potent inhibitor of CYP3A4 in humans, which can significantly increase the systemic exposure to drugs metabolized by this enzyme, such as sufentanil. Sufentanil is a synthetic opioid analgesic and anesthetic that acts as a highly selective full agonist at μ-opioid receptors in the central nervous system, producing profound analgesia and sedation. The combination may be clinically relevant due to pharmacokinetic interactions; co-administration with ketoconazole can increase plasma concentrations of sufentanil by inhibiting its metabolism via CYP3A4[6]. This interaction increases both efficacy and risk for adverse effects such as respiratory depression.

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