Lopinavir/ritonavir and Midazolam

Desk tier: Avoid together

Mechanism: strong CYP3A4 inhibition of clearance (↑ exposure)

“KALETRA is contraindicated with drugs that are highly dependent on CYP3A for clearance”

Kaletra (lopinavir/ritonavir), section 4 CONTRAINDICATIONS. DailyMed label

Why this grade

Kaletra (lopinavir/ritonavir) label, Contraindications

The Kaletra (lopinavir/ritonavir) label lists this combination under Contraindications. 4 CONTRAINDICATIONS: "KALETRA is contraindicated with drugs that are highly dependent on CYP3A for clearance" Named in the label: "Sedative/Hypnotics: triazolam, orally administered midazolam" Retrieved from DailyMed 2026-10-02.

Open source

FDA interaction table

FDA's example-interaction table lists Lopinavir/ritonavir as a strong CYP3A inhibitor, and Midazolam as a sensitive CYP3A substrate. FDA grades the roles; the severity tier on this row is the desk's rule. Table content current as of 2026-05-29.

Open source

PMID 7628179

1995 Clin Pharmacol Ther. Oral midazolam is the classic probe for intestinal CYP3A4 knockout.

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Open this pair in the desk

All pairs for Lopinavir/ritonavir · Midazolam

Enzyme behind this pair: CYP3A4

Educational reference only. Not FDA-cleared. The Prescribing Information governs.

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