Unexpected hepatotoxicity of rifampin and saquinavir/ritonavir in healthy male volunteers

Archives of Drug Information

Volumn 2, Issue 1, 2009, Pages 8-16

  Schmitt, Christophe ^a   Riek, Myriam ^a   Winters, Katie ^b   Schutz, Malte ^c   Grange, Susan ^a  

^a F HOFFMANN LA ROCHE LTD   (Switzerland)

^b ROCHE PRODUCTS LTD   (United Kingdom)

^c HOFFMANN LA ROCHE INC   (United States)

Author keywords

Cytochrome P450; Drug interaction; Hepatotoxicity; Rifampin; Ritonavir; Saquinavir

Indexed keywords

RIFAMPICIN; RITONAVIR; SAQUINAVIR;

ABDOMINAL PAIN; ADULT; ALANINE AMINOTRANSFERASE BLOOD LEVEL; AREA UNDER THE CURVE; ARTICLE; ASPARTATE AMINOTRANSFERASE BLOOD LEVEL; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DRUG BLOOD LEVEL; DRUG CONTRAINDICATION; DRUG ELIMINATION; DRUG HALF LIFE; DRUG TOLERABILITY; DRUG WITHDRAWAL; ELECTROCARDIOGRAPHY; EVENING DOSAGE; HEADACHE; HUMAN; HUMAN EXPERIMENT; LABORATORY TEST; LIVER DISEASE; MALE; MAXIMUM PLASMA CONCENTRATION; MORNING DOSAGE; NAUSEA AND VOMITING; NORMAL HUMAN; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL; SIDE EFFECT; STEADY STATE; TIME TO MAXIMUM PLASMA CONCENTRATION; TREATMENT DURATION; VITAL SIGN; VOLUNTEER;

EID: 70349547034     PISSN: None     EISSN: 17535174     Source Type: Journal    
DOI: 10.1111/j.1753-5174.2009.00017.x     Document Type: Article

References (32)

1. World Health Organization. Global tuberculosis control: Surveillance, planning, financing. World Health Organization Report 2008 [on The Internet]. Geneva: HHO Press. Available at: http://www.who.int/tb/ publications/global_report/2008/pdf/fullreport.pdf (accessed October 9, 2008).
2. Cahn P, Perez H, Ben G, Ochoa C. Tuberculosis and HIV: A partnership against the most vulnerable. J Int Assoc Physicians AIDS Care (Chic Ill) 2003; 2: 106-23.
3. Burman WJ, Gallicano K, Peloquin C. Therapeutic implications of drug interactions in the treatment of human immunodeficiency virus-related tuberculosis. Clin Infect Dis 1999; 28: 419-30.
4. Veldkamp AI, Hoetelmans RMW, Beijnen JH, Mulder JW, Meenhorst PL. Ritonavir enables combined therapy with rifampin and saquinavir. Clin Infect Dis 1999; 29: 1586.
5. Centers for Disease Control and Prevention. Managing drug interactions in the treatment of HIV-related tuberculosis. Available at: http://www.cdc.gov/tb/TB_HIV_Drugs/PDF/tbhiv.pdf (accessed October 9, 2008).
6. Veldkamp AI, van Heeswijk RP, Mulder JW, Meenhorst PL, Schreij G, van der GS, et al. Steady-state pharmacokinetics of twice-daily dosing of saquinavir plus ritonavir in HIV-1-infected individuals. J Acquir Immune Defic Syndr 2001; 27: 344-9.
7. Buss N, Snell P, Bock J, Hsu A, Jorga K. Saquinavir and ritonavir pharmacokinetics following combined ritonavir and saquinavir (soft gelatin capsules) administration. Br J Clin Pharmacol 2001; 52: 255-64.
8. Losso MH, Lourtau LD, Toibaro JJ, Saenz C, González C. The use of saquinavir/ritonavir 1000/100mg twice daily in patients with tuberculosis receiving rifampin. Antiviral Ther 2004; 9: 1031-3.
9. Ribera E, Azuaje C, Lopez RM, Domingo P, Soriano A, Pou L, et al. Once-daily regimen of saquinavir, ritonavir, didanosine, and lamivudine in HIV-infected patients with standard tuberculosis therapy (TBQD Study). J Acquir Immune Defic Syndr 2005; 40: 317-23.
10. Regulatory Compliance Center. Division of AIDS table for grading the severity of adult and pediatric adverse events, December 2004. Available at: http://rcc.tech-res.com/tox_tables.htm (accessed October 9, 2008).
11. American Heart Association. Guideline on cholesterol levels. Available at: http://www.americanheart.org/presenter.jhtml?identifier=4500 (accessed October 9, 2008).
12. Acocella G. Clinical pharmacokinetics of rifampicin. Clin Pharmacokinet 1978; 3: 108-27.
13. Kaeser B, Zhang X, Zandt H, Bour F, Zwanziger E, Schmitt C. Drug-drug interaction study of ketoconazole and ritonavir-boosted saquinavir. Antimicrob Agents Chemother 2009; 53: 609-14.
14. Nijland HMJ, L'homme RFA, Rongen GA, van Uden P, van Crevel R, Boeree MJ, et al. High incidence of adverse events in healthy volunteers receiving rifampicin and adjusted doses of lopinavir/ritonavir tablets. AIDS 2008; 22: 931-5.
15. Ribera E, Azuaje C, Lopez RM, Domingo P, Curran A, Feijoo M, et al. Pharmacokinetic interaction between rifampicin and the once-daily combination of saquinavir and low-dose ritonavir in HIV-infected patients with tuberculosis. Antimicrob Agents Chemother 2007; 59: 690-7.
16. Patel SM, Johnson S, Belknap SM, Chan J, Sha BE, Bennett C. Serious adverse cutaneous and hepatic toxicities associated with nevirapine use by non-HIV-infected individuals. J Acquir Immune Defic Syndr 2004; 35: 120-5.
17. Puro V, Soldani F, De Carli G, Lazarevic Z, Mattioli F, Ippolito G. Drug-induced aminotransferase alterations during antiretroviral HIV post-exposure prophylaxis. AIDS 2003; 17: 1988-90.
18. Centers for Disease Control and Prevention. Serious adverse events attributed to nevirapine regimens for postexposure prophylaxis after HIV exposures-Worldwide, 1997-2000. MMWR Morb Mortal Wkly Rep 2001; 49: 1153-6.
19. Benn PD, Mercey DE, Brink N, Scott G, Williams IG. Prophylaxis with a nevirapine-containing triple regimen after exposure to HIV-1. Lancet 2001; 357: 687-8.
20. Johnson S, Chan J, Bennett CL. Hepatotoxicity after prophylaxis with a nevirapine-containing antiretroviral regimen. Ann Intern Med 2002; 137: 146-7.
21. Stern JO, Robinson PA, Love J, Lanes S, Imperiale MS, Mayers DL. A comprehensive hepatic safety analysis of nevirapine in different populations of HIV infected patients. J Acquir Immune Defic Syndr 2003; 34 (suppl 1): S21-33.
22. Pollard RB, Robinson P, Dransfield K. Safety profile of nevirapine, a nonnucleoside reverse transcriptase inhibitor for the treatment of human immunodeficiency virus infection. Clin Ther 1998; 20: 1071-92.
23. Hamzeh FM, Benson C, Gerber J, Currier J, McCrea J, Deutsch P, et al. Steady-state pharmacokinetic interaction of modified-dose indinavir and rifabutin. Clin Pharmacol Ther 2003; 73: 159-69.
24. Barditch-Crovo P, Trapnell CB, Ette E, Zacur HA, Coresh J, Rocco LE, et al. The effects of rifampin and rifabutin on the pharmacokinetics and pharmacodynamics of a combination oral contraceptive. Clin Pharmacol Ther 1999; 65: 428-38.
25. Apseloff G. Severe neutropenia among healthy volunteers given rifabutin in clinical trials. Clin Pharmacol Ther 2003; 74: 591-2.
26. Hafner R, Bethel J, Standiford HC, Follansbee S, Cohn DL, Polk RE, et al. Tolerance and pharmacokinetic interactions of rifabutin and azithromycin. Antimicrob Agents Chemother 2001; 45: 1572-7.
27. Halsey NA, Coberly JS, Desormeaux J, Losikoff P, Atkinson J, Moulton LH, et al. Randomised trial of isoniazid versus rifampicin and pyrazinamide for prevention of tuberculosis in HIV-1 infection. Lancet 1998; 351: 786-92.
28. Mwinga A, Hosp M, Godfrey-Faussett P, Quigley M, Mwaba P, Mugala BN, et al. Twice weekly tuberculosis preventive therapy in HIV infection in Zambia. AIDS 1998; 12: 2447-57.
29. Gordin FM, Cohn DL, Matts JP, Chaisson RE, O'Brien RJ. 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 2004; 39: 561-5.
30. Jasmer RM, Saukkonen JJ, Blumberg HM, Daley CL, Bernardo J, Vittinghoff E, et al. Short-course rifampin and pyrazinamide compared with isoniazid for latent tuberculosis infection: A multicenter clinical trial. Ann Intern Med 2002; 137: 640-7.
31. McNeill L, Allen M, Estrada C, Cook P. Pyrazinamide and rifampin vs isoniazid for the treatment of latent tuberculosis: Improved completion rates but more hepatotoxicity. Chest 2003; 123: 102-6.
32. Jasmer RM, Daley CL. Rifampin and pyrazinamide for treatment of latent tuberculosis infection: Is it safe? Am J Respir Crit Care Med 2003; 167: 809-10.