Rifampin and rifabutin drug interactions: an update

Arch Intern Med. 2002 May 13;162(9):985-92. doi: 10.1001/archinte.162.9.985.

Abstract

Rifampin is a potent inducer of cytochrome P-450 oxidative enzymes. A few examples of well-documented clinically significant interactions include interactions with warfarin, oral contraceptives, cyclosporine, glucocorticoids, ketoconazole or itraconazole, theophylline, quinidine sulfate, digitoxin or digoxin, verapamil hydrochloride, human immunodeficiency virus-related protease inhibitors, zidovudine, delavirdine mesylate, nifedipine, and midazolam. Recent reports have demonstrated clinically relevant interactions with numerous other drugs, such as buspirone hydrochloride, zolpidem tartrate, simvastatin, propafenone hydrochloride, tacrolimus, ondansetron hydrochloride, and opiates. Rifabutin reduces serum concentrations of antiretroviral agents, but less so than rifampin. To avoid a reduced therapeutic response, therapeutic failure, or toxic reactions when rifampin is added to or discontinued from medication regimens, clinicians need to be cognizant of these interactions. Enhanced knowledge of known interactions will continue to develop, including research on the induction of specific cytochrome P-450 isoenzymes and on the importance of the P-glycoprotein transport system. New rifampin and rifabutin interactions will be discovered with further investigations.

Publication types

  • Research Support, Non-U.S. Gov't
  • Review

MeSH terms

  • AIDS-Related Opportunistic Infections / drug therapy
  • ATP Binding Cassette Transporter, Subfamily B, Member 1 / metabolism
  • Anti-Bacterial Agents* / pharmacology
  • Anti-HIV Agents / pharmacology
  • Antibiotics, Antitubercular / pharmacology
  • Antiemetics / pharmacology
  • Cardiovascular Agents / pharmacology
  • Cytochrome P-450 Enzyme System / biosynthesis
  • Drug Interactions
  • Enzyme Induction
  • Enzyme Inhibitors / pharmacology
  • Humans
  • Immunosuppressive Agents / pharmacology
  • Narcotics / pharmacology
  • Psychotropic Drugs / pharmacology
  • Rifabutin* / pharmacology
  • Rifampin* / pharmacology

Substances

  • ATP Binding Cassette Transporter, Subfamily B, Member 1
  • Anti-Bacterial Agents
  • Anti-HIV Agents
  • Antibiotics, Antitubercular
  • Antiemetics
  • Cardiovascular Agents
  • Enzyme Inhibitors
  • Immunosuppressive Agents
  • Narcotics
  • Psychotropic Drugs
  • Rifabutin
  • Cytochrome P-450 Enzyme System
  • Rifampin