Pharmacokinetic interaction between amprenavir and clarithromycin in healthy male volunteers

Antimicrobial Agents and Chemotherapy

Volumn 44, Issue 4, 2000, Pages 978-984

  Brophy, Donald F ^a   Israel, Debra S ^b   Pastor, Antonio ^a   Gillotin, Catherine ^c   Chittick, Greg E ^d   Symonds, William T ^e   Lou, Yu ^e   Sadler, Brian M ^e   Polk, Ron E ^a,f  

^a VIRGINIA COMMONWEALTH UNIVERSITY SCHOOL OF MEDICINE   (United States)

^b HOFFMANN LA ROCHE INC   (United States)

^c GLAXOSMITHKLINE   (United Kingdom)

^d Triangle Pharmaceuticals   (United States)

^e GLAXOSMITHKLINE   (United States)

^f VIRGINIA COMMONWEALTH UNIVERSITY   (United States)

Author keywords

[No Author keywords available]

Indexed keywords

14 HYDROXYCLARITHROMYCIN; AMPRENAVIR; CLARITHROMYCIN; CYTOCHROME P450 3A4; ERYTHROMYCIN; INDINAVIR; RITONAVIR; SAQUINAVIR;

ADULT; AREA UNDER THE CURVE; ARTICLE; BREATH ANALYSIS; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; CROSSOVER PROCEDURE; DOSE RESPONSE; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG METABOLISM; DRUG URINE LEVEL; HUMAN; HUMAN EXPERIMENT; MALE; NORMAL HUMAN; PHASE 1 CLINICAL TRIAL; PRIORITY JOURNAL; RANDOMIZED CONTROLLED TRIAL;

ADOLESCENT; ADULT; ANTI-BACTERIAL AGENTS; ANTI-HIV AGENTS; AREA UNDER CURVE; BIOTRANSFORMATION; BREATH TESTS; CARBAMATES; CLARITHROMYCIN; CROSS-OVER STUDIES; CYTOCHROME P-450 ENZYME SYSTEM; DRUG COMBINATIONS; DRUG INTERACTIONS; ENZYME INHIBITORS; ERYTHROMYCIN; HALF-LIFE; HUMANS; LIVER FUNCTION TESTS; MALE; MIXED FUNCTION OXYGENASES; SULFONAMIDES;

EID: 0034062934     PISSN: 00664804     EISSN: None     Source Type: Journal    
DOI: 10.1128/AAC.44.4.978-984.2000     Document Type: Article

References (27)

1. Adkins, J. C., and D. Faulds. Amprenavir. 1998. Drugs 55:837-842.
2. Cheng, C. L., D. E. Smith, P. L. Carver, S. R. Cox, P. B. Watkins, D. S. Blake, C. A. Kauffman, K. M. Meyer, G. L. Amidon, and P. L. Stetson. 1997. Steady-state pharmacokinetics of delavirdine in HIV-positive patients: effect on erythromycin breath test. Clin. Pharmacol. Ther. 61:531-543.
3. Chu, S., D. S. Wilson, R. L. Deaton, A. V. Mackenthun, C. N. Eason, and J. H. Cavanaugh. 1993. Single- and multiple-dose pharmacokinetics of clarithromycin, a new macrolide antimicrobial. J. Clin. Pharmacol. 33:719-726.
4. Decker, C. J., L. M. Laitinen, G. W. Bridson, S. A. Raybuck, R. D. Tung, and P. R. Chaturvedi. 1998. Metabolism of amprenavir in liver microsomes: role of CYP3A4 inhibition for drug interactions. J. Pharm. Sci. 87:803-807.
5. Flexner, C. HIV-protease inhibitors. 1998. N. Engl. J. Med. 338:1281-1292.
6. Gorski, J. C., D. R. Jones, B. D. Haehner-Daniels, M. A. Hamman, E. M. O'Mara, and S. D. Hall. 1998. The contribution of intestinal and hepatic CYP3A to the interaction between midazolam and clarithromycin. Clin. Pharmacol. Ther. 64:133-143.
7. Hall, S. D., K. E. Thummel, P. B. Watkins, K. S. Lown, L. Z. Benet, M. F. Paine, R. R. Mayo, D. K. Turgeon, D. G. Bailey, R. J. Fontana, and S. A. Wrighton. 1999. Molecular and physical mechanisms of first-pass extraction. Drug. Metab. Dispos. 27:161-166.
8. Hoover, W. W., M. S. Barrett, and R. N. Jones. 1992. Clarithromycin in vitro activity enhanced by its major metabolite, 14-hydroxyclarithromycin. Diagn. Microbiol. Infect. Dis. 15:259-266.
9. Hsu, A., G. R. Granneman, G. Cao, L. Carothers, T. El-Shourbagy, P. Baroldi, K. Erdman, F. Brown, E. Sun, and J. Leonard. 1998. Pharmacokinetic interactions between two human immunodeficiency virus protease inhibitors, ritonavir and saquinavir. Clin. Pharmacol. Ther. 63:453-464.
10. Hsu, A., G. R. Granneman, G. Cao, L. Carothers, A. Japour, T. El-Shourbagy, S. Dennis, J. Berg, K. Erdman, J. Leonard, and E. Sun. 1998. Pharmacokinetic interaction between ritonavir and indinavir in healthy volunteers. Antimicrob. Agents Chemother. 42:2784-2791.
11. Kempf, D. J., K. C. Marsh, G. Kumar, A. D. Rodrigues, J. F. Denissen, E. McDonald, M. J. Kukulka, A. Hsu, G. R. Granneman, P. A. Baroldi, E. Sun, D. Pazzuti, J. J. Plattner, D. W. Norbeck, and J. M. Leonard. 1997. Pharmacokinetic enhancement of inhibitors of the human immunodeficiency virus protease by coadministration with ritonavir. Antimicrob. Agents Chemother. 41:654-660.
12. Kim, R. B., M. F. Fromm, C. Wandell, B. Leake, A. J. Wood, D. Roden, and G. R. Wilkinson. 1998. The drug transporter P-glycoprotein limits oral absorption and brain entry of HIV-1 protease inhibitors. J. Clin. Investig. 101: 289-294.
13. Langtry, H. D., and R. N. Brogden. 1997. Clarithromycin: a review of its efficacy in the treatment of respiratory tract infections in immunocompetent patients. Drugs 53:973-1004.
14. Murphy, R. L., R. M. Gulick, V. DeGruttola, R. T. D'Aquila, J. J. Eron, J. P. Sommadossi, J. S. Currier, L. Smeaton, I. Frank, A. M. Caliendo, J. G. Gerber, R. Tung, and D. R. Kuritzkes. 1999. Treatment with amprenavir alone or amprenavir with zidovudine and lamivudine in adults with human immunodeficiency virus infection. AIDS Clinical Trials Group 347 Study Team. J. Infect. Dis. 179:808-816.
15. Ouellet, D., A. Shu, G. R. Granneman, G. Carlson, J. Cavanaugh, H. Guenther, and J. M. Leonard. 1998. Pharmacokinetic interaction between ritonavir and clarithromycin. Clin. Pharm. Ther. 64:355-362.
16. Polk, R. E., M, Crouch, D. S. Israel, A. Pastor, B. M. Sadler, G. E. Chittick, B. T. Symonds, W. Gouldin, and Y. Lou. 1999. Pharmacokinetic interaction between ketoconazole and amprenavir after single dose administration to healthy male subjects. Pharmacotherapy 19:1378-1384.
17. Polli, J. W., J. L. Jarrett, S. D. Studenberg, J. E. Humpreys, S. W. Dennis, K. R. Brouwer, and J. L. Wooley. 1999. Role of P-glycoprotein in the CNS penetration of amprenavir (141W94), an HIV protease inhibitor. Pharm. Res. 16:1206-1212.
18. Rodrigues, A. D., E. M. Roberts, D. J. Mulford, Y. Yao, and D. Ouellet. 1997. Oxidative metabolism of clarithromycin in the presence of human liver microsomes. Major role for the cytochrome P4503A subfamily. Drug Metab. Dispos. 25:623-630.
19. Sadler, B. M., C. D. Hanson, G. E. Chittick, W. T. Symonds, and N. S. Roskell. 1999. Safety and pharmacokinetics of amprenavir (141W92), a human immunodeficiency virus (HIV) type 1 protease inhibitor, following oral administration of single doses to HIV-infected adults. Antimicrob. Agents Chemother. 43:1686-1692.
20. Singh, R., L. C. Taylor, and S. Y. Chang. 1996. In vitro metabolism of a potent HIV-protease inhibitor (141W94) using rat, monkey and human liver S9. Rapid Commun. Mass Spectrom. 10:1019-1026.
21. St. Clair, M. H., J. Millard, J. Rooney, M. Tisdale, N. Perry, B. M. Sadler, M. R. Blum, and G. Painter. 1996. In vitro antiviral activity of 141W94 (VX-478) in combination with other antiretroviral agents. Antiviral Res. 29: 53-56.
22. U. S. Public Health Service (USPHS) and Infectious Diseases Society of America (IDSA). 1999. 1999 USPHS/IDSA guidelines for the prevention of opportunistic infections in persons infected with human immunodeficiency virus. Morbid. Mortal. Weekly Rep. 48:1-59.
23. Wagner, D. 1998. CYP3A4 and the erythromycin breath test. Clin. Pharmacol. Ther. 64:129.
24. Wakasugi, H., I. Yano, T. Ito, T. Hashida, T. Futami, R. Nohara, S. Sasayama, and K. Inui. 1998. Effect of clarithromycin on renal excretion of digoxin: interaction with P-glycoprotein. Clin. Pharmacol. Ther. 64:123-128.
25. Washington, C. B., G. E. Duran, M. C. Man, B. I. Sikic, and T. Blaschke. 1998. Interaction of anti-HIV protease inhibitors with the multidrug transporter P-glycoprotein (P-gp) in human cultured cells. J. Acquir. Immune Defic. Syndr. Hum. Retrovirol. 19:203-209.
26. Watkins, P. B. 1994. Non-invasive tests of CYP3A enzymes. Pharmacogenetics 4:171-184.
27. 14C]-amprenavir in human volunteers. Pharm. Sci. 1(Suppl.):2044. (Abstract.)