Rifampicin (Rifadin / Rimactane)

Rifampicin (Rifadin / Rimactane) is an approved anti-mycobacterial drug that is a standard component of combination regimens for treating tuberculosis. In the United States, it is called rifampin.

Tuberculosis treatment regimens that contain rifampicin are generally more effective than those that do not contain rifampicin. However, rifampicin induces activity of the CYP3A4 enzyme, so has significant interactions with many of the anti-HIV drugs. These interactions mean that rifampicin cannot be used by most HIV-infected people taking antiretroviral therapy: for these patients, rifabutin (Mycobutin) is preferred for the treatment of tuberculosis.

Despite this, rifampicin may be taken by individuals taking the following anti-HIV combinations:

  • Efavirenz (Sustiva) plus two nucleoside reverse transcriptase inhibitors (NRTIs). With this combination, the dose of efavirenz may need to be increased to 800mg a day, although some studies have found that this dose can cause side-effects, and that the standard dose of 600mg is adequate in terms of drug levels and HIV suppression, particularly in patients with low body weight.1 2 3 4 5
  • Full-dose ritonavir (Norvir) plus NRTIs, although this should be used with caution.6

Rifampicin should not be co-administered with any of the other approved non-nucleoside reverse transcriptase inhibitors (NNRTIs) or protease inhibitors, due to alterations in levels of the drugs or side-effects such as liver toxicity.7 8 9 10 11 12 13 14 Rifampicin does not interact with the NRTIs, so triple NRTI combinations may be used by patients taking rifampicin.

Rifampicin interacts with a range of other drugs commonly used in the treatment of HIV and AIDS. Rifampicin dramatically reduces blood levels of the anti-protozoal drug atovaquone (Wellvone), which may be used to treat Pneumocystis pneumonia (PCP) or other opportunistic infections. It also reduces levels of methadone hydrochloride (Methadose), requiring dose increases of up to 50% to avoid withdrawal symptoms.

Rifampicin also increases levels of the meningitis drug fluconazole (Diflucan), although the clinical implications of this remain to be determined.15 In addition, levels of rifampicin may be reduced in people who are taking the anti-fungal drug ketoconazole (Nizoral).

Side-effects of rifampicin can include rash, fever, gastrointestinal disorders and jaundice. Cases of kidney failure and of allergic reaction to rifampicin have also been reported.16 17 To minimise the gastrointestinal effects, rifampicin should not be taken at the same time as food. Orange discoloration of body fluids such as spit and urine, and of soft contact lenses, also occurs. Despite concerns that the combination of rifampicin and the tuberculosis drug pyrazinamide can cause severe liver damage, the incidence of this seems to be low in HIV-positive patients.18

Recent studies have suggested than rifampicin-resistant tuberculosis is becoming more common. For example, 2% of samples from surveys in Botswana and Burundi were found to be resistant to the drug, while tuberculosis resistant to rifampicin and isoniazid is common in eastern Europe, central Asia, China and South Africa.19

There is some evidence that HIV-infected people with tuberculosis or diarrhoea may have low levels of rifampicin in the blood, possibly due to impaired absorption.20 Further studies are in progress to investigate this observation.

Rifampicin may cause a false-positive result in urine tests for opiates, such as heroin and morphine.21

References

  1. Lopez-Cortes LF et al. Pharmacokinetic interactions between rifampin and efavirenz in HIV-infected patients with tuberculosis. Clin Pharmacokinet 41: 681-690, 2002
  2. Pedral-Samapio D et al. Efficacy and safety of efavirenz in HIV patients on rifampicin for tuberculosis. Braz J Infect Dis 8: 211-216, 2004
  3. Patel A et al. Safety and antiretroviral effectiveness of concomitant use of rifampicin and efavirenz for antiretroviral-naive patients in India who are coinfected with tuberculosis and HIV-1. J Acquir Immune Defic Syndr 37: 1166-1169, 2004
  4. Manosuthi W et al. Efavirenz 600 mg/day versus efavirenz 800 mg/day in HIV-infected patients with tuberculosis receiving rifampicin: 48 weeks results. AIDS 20(1): 131-132, 2006
  5. Brennan-Benson P et al. Pharmacokinetic interactions between efavirenz and rifampicin in the treatment of HIV and tuberculosis: one size does not fit all. AIDS 19: 1541-1543, 2005
  6. Moreno S et al. Treatment of tuberculosis in HIV-infected patients: safety and antiretroviral efficacy of the concomitant use of ritonavir and rifampin. AIDS 15: 1185-1187, 2001
  7. Justesen US et al. Pharmacokinetic interaction between rifampin and the combination of indinavir and low-dose ritonavir in HIV-infected patients. Clin Infect Dis 38: 426-429, 2004
  8. Ribera E et al. Pharmacokinetic interaction between nevirapine and rifampicin in HIV-infected patients with tuberculosis. J Acquir Immune Defic Syndr 28: 450-453, 2001
  9. Manosuthi W et al. Plasma nevirapine levels and 24-week efficacy in HIV-infected patients receiving nevirapine-based highly active antiretroviral therapy with or without rifampicin. Clin Infect Dis 43: 253-255, 2006
  10. Jaruratanasirikul S et al. Effect of indinavir on the pharmacokinetics of rifampicin in HIV-infected patients. J Pharm Pharmacol 53: 409-412, 2001
  11. Polk RE et al. Pharmacokinetic interaction between amprenavir and rifabutin or rifampicin in healthy males. Antimicrob Agents Chemother 45: 502-508, 2001
  12. la Porte CJ et al. Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers. Antimicrob Agents Chemother 48: 1553-1560, 2004
  13. Grub S et al. The interaction of saquinavir (soft gelatine capsule) with ketoconazole, erythromycin and rifampicin: comparison of the effect in healthy volunteers and HIV-infected patients. Eur J Clin Pharmacol 57: 115-121, 2001
  14. Ramachandran G et al. Increasing nevirapine dose can overcome reduced bioavailability due to rifampicin coadministration. J Acquir Immune Defic Syndr 42: 36-41, 2006
  15. Panomvana Na Ayudhya D et al. Effect of rifampicin on the pharmacokinetics of fluconazole in patients with AIDS. Clin Pharmacokinet 43: 725-732, 2004
  16. Wen YK et al. Crescentic glomerulonephritis associated with rifampicin in a patient co-infected with tuberculosis and human immunodeficiency virus. Clin Nephrol 65: 284-289, 2006
  17. Buergin S et al. Immediate hypersensitivity to rifampicin in 3 patients: diagnostic procedures and induction of clinical tolerance. Int Arch Allergy Immunol 140: 20-26, 2006
  18. Gordin FM et al. Hepatotoxicity of rifampin and pyrazinamide in the treatment of latent tuberculosis infection in HIV-infected persons: is it different than in HIV-uninfected persons? Clin Infect Dis 39: 561-565, 2004
  19. Sanders M et al. Rifampicin mono-resistant Mycobacetrium tuberculosis in Bujumbura, Burundi: results of a drug resistance survey. Int J Tuberc Lung Dis 10: 178-183, 2006
  20. Perlman DC et al. The clinical pharmacokinetics of rifampin and ethambutol in HIV-infected persons with tuberculosis. Clin Infect Dis 41: 1638-1647, 2005
  21. de Paula M et al. Rifampicin causes false-positive immunoassay results for urine opiates. Clin Chem Lab Med 36: 241-243, 1998

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This content was checked for accuracy at the time it was written. It may have been superseded by more recent developments. NAM recommends checking whether this is the most current information when making decisions that may affect your health.

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