Drug intelligence / Profile preview

ritonavir + midazolam

Development stage
Unknown
Lead developer
Abbott
Modality
Small Molecules
Administration
Oral, Intravenous, Intramuscular, Intranasal, Buccal
01

Overview

**Ritonavir + midazolam** is a combination of two pharmaceutical drugs, each with distinct mechanisms and clinical uses. Ritonavir is an HIV protease inhibitor primarily used as part of antiretroviral therapy for HIV infection and as a pharmacokinetic enhancer due to its potent inhibition of cytochrome P450 3A4 (CYP3A4). Midazolam is a short-acting benzodiazepine with anxiolytic, sedative, hypnotic, muscle relaxant, anticonvulsant, and amnesic properties; it acts by enhancing the effect of the inhibitory neurotransmitter gamma-aminobutyric acid (GABA) at the GABA-A receptor[5][8]. When co-administered, ritonavir dramatically increases plasma concentrations of midazolam by inhibiting its CYP3A4-mediated metabolism. This can result in extreme sedation or respiratory depression; therefore, oral co-administration is contraindicated and parenteral use requires close monitoring[1][2]. The combination does not represent a therapeutic product but rather describes a clinically significant drug-drug interaction.

Brand names
KaletraBuccolam
Other names
RTV (for ritonavir)Versed (for midazolam)
02

Targets

CYP3A4 (Cytochrome P450 3A4)GABRR (GABA-A receptor subunit rho)PR (Progesterone receptor)

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