Drug intelligence / Profile preview

buprenorphine + rifampin

Development stage
Unknown
Lead developer
Indivior
Modality
Small Molecules
Administration
Oral, Intravenous, Sublingual, Buccal, Transdermal, Intramuscular, Subcutaneous
01

Overview

Buprenorphine + rifampin is a combination of two pharmaceutical agents used together, typically in patients who require both opioid dependence treatment or pain management (buprenorphine) and tuberculosis therapy (rifampin). Buprenorphine is a partial agonist at the μ-opioid receptor, providing analgesia and reducing opioid withdrawal symptoms. Rifampin is an antibiotic that inhibits bacterial DNA-dependent RNA polymerase, primarily used to treat tuberculosis. When co-administered, rifampin induces cytochrome P450 3A4 enzymes, significantly increasing the metabolism of buprenorphine. This interaction can lead to reduced plasma concentrations of buprenorphine and may precipitate opioid withdrawal or reduce analgesic efficacy[1][2][4]. Dose adjustments or alternative therapies may be required when these drugs are used together.

02

Targets

DOR (Opioid Receptor Delta 1)MOR (Mu opioid receptor)RNAP (Bacterial dna-dependent RNA polymerase)KOR (Kappa opioid receptor)CYP3A4 (Cytochrome P450 3A4)

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