Simultaneous determination of rifampicin and efavirenz in plasma.

Complex drug interactions involving antiretroviral agents and drugs for the management of opportunistic infections demand the monitoring of plasma drug concentrations to prevent treatment failure. The high occurrence of tuberculosis in HIV-infected subjects makes the management of HIV treatment complex. Rifampicin, a potent inducer of the cytochrome P 450 metabolic pathway, is a very active antituberculosis drug that accelerates the metabolism of protease inhibitors. Regimens containing efavirenz, a non-nucleoside reverse transcription inhibitor, could be an alternative, but efavirenz plasma concentrations may be altered after the coadministration of rifampicin. Efavirenz is also a cytochrome P 450 inducer and may alter rifampicin plasma levels. Due to the increasing need to monitor plasma concentrations in HIV patients with tuberculosis, a high-performance liquid chromatographic (HPLC) method has been developed to measure rifampicin and efavirenz at the same time in a small amount of sample. This HPLC method is highly sensitive and precise, suitable for pharmacokinetic studies or routine clinical monitoring of rifampicin and efavirenz simultaneously in HIV patients with tuberculosis.
AuthorsMarta Boffito, John Tija, Helen E Reynolds, Patrick G Hoggard, Stefano Bonora, Giovanni Di Perri, David J Back
JournalTherapeutic drug monitoring (Ther Drug Monit) Vol. 24 Issue 5 Pg. 670-4 (Oct 2002) ISSN: 0163-4356 [Print] United States
PMID12352941 (Publication Type: Journal Article)
Chemical References
  • Benzoxazines
  • Oxazines
  • efavirenz
  • Rifampin
  • Adult
  • Antiretroviral Therapy, Highly Active (methods)
  • Benzoxazines
  • Chromatography, High Pressure Liquid (methods)
  • HIV Infections (blood, drug therapy)
  • Humans
  • Male
  • Middle Aged
  • Oxazines (blood, therapeutic use)
  • Rifampin (blood, therapeutic use)
  • Tuberculosis (blood, drug therapy)

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