Drug intelligence / Profile preview

rifapentine + midazolam

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

Overview

Rifapentine + midazolam is a combination of two pharmaceutical agents with distinct mechanisms and indications. Rifapentine is an antibiotic in the antimycobacterial class used primarily for the treatment of active and latent tuberculosis, often in combination with other antitubercular drugs. It acts by inhibiting bacterial RNA synthesis through binding to the beta subunit of DNA-dependent RNA polymerase, thereby killing or preventing the growth of Mycobacterium tuberculosis[2][8]. Midazolam is a short-acting benzodiazepine used as a sedative, anxiolytic, muscle relaxant, anticonvulsant, and hypnotic agent. Its primary mechanism involves positive allosteric modulation of GABA-A receptors in the central nervous system to enhance inhibitory neurotransmission[1][3][4]. Notably, co-administration can result in significant drug-drug interactions; rifapentine (like its analog rifampin) induces CYP3A4 enzymes that metabolize midazolam—markedly reducing plasma concentrations and pharmacodynamic effects of midazolam[5].

02

Targets

CYP3A4 (Cytochrome P450 3A4)rpoB (DNA-directed RNA polymerase subunit beta)GABA-A receptor α1β2γ2 (GABA_A receptor α1β2γ2 – N-methyllaurotetanine)

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