A combined-formulation tablet of lamivudine/nevirapine/stavudine: Bioequivalence compared with concurrent administration of lamivudine, nevirapine, and stavudine in healthy Indian subjects

Journal of Clinical Pharmacology

Volumn 45, Issue 3, 2005, Pages 265-274

  Narang, Vishal S ^a   Lulla, Amar ^a   Malhotra, Geena ^a   Purandare, Shrinivas ^a  

^a CIPLA LTD   (India)

Author keywords

Bioequivalence; Lamivudine; Nevirapine; Pharmacokinetics; Stavudine

Indexed keywords

ANTIRETROVIRUS AGENT; LAMIVUDINE; NEVIRAPINE; RNA DIRECTED DNA POLYMERASE INHIBITOR; STAVUDINE;

ADULT; AREA UNDER THE CURVE; ARTICLE; BIOEQUIVALENCE; CLINICAL TRIAL; CONTROLLED CLINICAL TRIAL; CONTROLLED STUDY; DIZZINESS; DRUG BLOOD LEVEL; DRUG DOSE REGIMEN; DRUG FORMULATION; DRUG TOLERABILITY; ETHNIC GROUP; HEADACHE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; MALE; NORMAL HUMAN; RANDOMIZED CONTROLLED TRIAL; RASH; TABLET FORMULATION; TANDEM MASS SPECTROMETRY;

ADULT; ANTI-HIV AGENTS; CROSS-OVER STUDIES; DRUG COMBINATIONS; DRUG THERAPY, COMBINATION; HUMANS; INDIA; LAMIVUDINE; MALE; NEVIRAPINE; REVERSE TRANSCRIPTASE INHIBITORS; STAVUDINE; TABLETS; THERAPEUTIC EQUIVALENCY;

EID: 16844379765     PISSN: 00912700     EISSN: None     Source Type: Journal    
DOI: 10.1177/0091270004273343     Document Type: Article

References (40)

1. UNAIDS: The Joint United Nations Programme on HIV/AIDS Web site. Available at: http://www.unaids.org/Unaids/EN/Resources/Epidemiology/ epidemicupdateslides.asp. Accessed on August 17,2004.
2. U.S. Department of Health and Human Services (DHHS). HIV/AIDS medical practice guidelines. Available at: http://www.aidsinfo.nih.gov/guidelines/. Accessed on August 17, 2004.
3. Nolan D. Metabolic complications associated with HIV protease inhibitor therapy. Drugs. 2003;63:2555-2574.
4. Van Leeuwen R, Katlama C, Murphy RL, et al. A randomized trial to study first-line combination therapy with or without a protease inhibitor in HIV-1-infected patients. AZDS. 2003;17:987-999.
5. Staszewski S, Morales-Ramirez J, Tashima KT, et al. Efavirenz plus zidovudine and lamivudine, efavirenz plus indinavir, and indinavir plus zidovudine and lamivudine in the treatment of HIV-1 infection in adults. Study 006 Team. N Engl J Med. 1999;341:1865-1873.
6. Yozviak JL, Doerfler RE, Woodward WC. Effectiveness and tolerability of nevirapine, stavudine, and lamivudine in clinical practice. HIV Clin Trials. 2001;2:474-476.
7. Laurent C, Kouanfack C, Koulla-Shiro S, et al. Effectiveness and safety of a generic fixed-dose combination of nevirapine, stavudine, and lamivudine in HTV-1-infected adults in Cameroon: open-label multicentre trial. Lancet. 2004;364:29-34.
8. van Leth F, Phanuphak P, Ruxrungtham K, Baraldi E, Miller S, Gazzard B. Comparison of first-line antiretroviral therapy with regimens including nevirapine, efavirenz, or both drugs, plus stavudine and lamivudine: a randomised open-label trial, the 2NN Study. Lancet. 2004;363:1253-1263.
9. Katlama C, Valantin MA, Matheron S, et al. Efficacy and tolerability of stavudine plus lamivudine in treatment-naive and treatment-experienced patients with HIV-1 infection. Ann Intern Med. 1998;129:525-531.
10. Merrill DP, Moonis M, Chou TC, Hirsch MS. Lamivudine or stavudine in two- and three-drug combinations against human immunodeficiency virus type 1 replication in vitro. J Infect Dis. 1996;173:355-364.
11. Furman PA, Fyfe JA, St Clair MH, et al. Phosphorylation of 3′-azido-3′-deoxythymidine and selective interaction of the 5′-triphosphate with human immunodeficiency virus reverse transcriptase. Proc Natl Acad Sci USA. 1986;83:8333-8337.
12. Moore KH, Barrett JE, Shaw S, et al. The pharmacokinetics of lamivudine phosphorylation in peripheral blood mononuclear cells from patients infected with HIV-1. AZDS. 1999;13:2239-2250.
13. Becher F, Landman R, Mboup S, et al. Monitoring of didanosine and stavudine intracellular trisphosphorylated anabolite concentrations in HIV-infected patients. AIDS. 2004;18:181-187.
14. Floridia M, Bucciaidini R, Ricciaidulli D, et al. A randomized, double-blind trial on the use of a triple combination including nevirapine, a nonnucleoside reverse transcriptase HIV inhibitor, in antiretroviral-naive patients with advanced disease. J Acquir Immune Defic Syndr Hum Retrovirol. 1999;20:11-19.
15. Grob PM, Wu JC, Cohen KA, et al. Nonnucleoside inhibitors of HIV-1 reverse transcriptase: nevirapine as a prototype drug. AIDS Res Hum Retroviruses. 1992;8:145-152.
16. Perry CM, Faulds D. Lamivudine: a review of its antiviral activity, PK properties and therapeutic efficacy in the management of HIV infection. Drugs. 1997;53:657-680.
17. Escobar Y, Venturelli CR, Escobar-Islas E, Hoyo-Vadillo C. Pharmacokinetics of stavudine by oral administration to healthy Mexican volunteers. Proc West Pharmacol Soc. 2003;46:109-110.
18. Lamson MJ, Sabo JP, MacGregor TR, et al. Single dose pharmacokinetics and bioavailability of nevirapine in healthy volunteers. Biopharm Drug Dispos. 1999;20:285-291.
19. Cheeseman SH, Hattox SE, McLaughlin MM, et al. Pharmacokinetics of nevirapine: initial single-rising-dose study in humans. Antimicrob Agents Chemother. 1993;37:178-182.
20. Johnson MA, Moore KH, Yuen GJ, Bye A, Pakes GE. Clinical pharmacokinetics of lamivudine. Clin Pharmacokinet. 1999;36:41-66.
21. Horton CM, Dudley MN, Kaul S, et al. Population pharmacokinetics of stavudine (d4T) in patients with AIDS or advanced AIDS-related complex. Antimicrob Agents Chemother. 1995;39:2309-2315.
22. Viramune (nevirapine) [product information]. Ridgefield, Conn: Boehringer Ingelheim Pharmaceuticals; 1999.
23. Schaad HJ, Petty BG, Grasela DM, Christofalo B, Raymond R, Stewart M. Pharmacokinetics and safety of a single dose of stavudine (d4T) in patients with severe hepatic impairment. Antimicrob Agents Chemother. 1997;41:2793-2796.
24. Moore KH, Shaw S, Laurent AL, et al. Lamivudine/zidovudine as a combined formulation tablet: bioequivalence compared with lamivudine and zidovudine administered concurrently and the effect of food on absorption. J Clin Pharmacol. 1999;39:593-605.
25. Yuen GJ, Lou Y, Thompson NF, et al. Abacavir/lamivudine/zidovudine as a combined formulation tablet: bioequivalence compared with each component administered concurrently and the effect of food on absorption. J Clin Pharmacol. 2001;41:277-288.
26. Azoulay S, Nevers MC, Creminon C, et al. Sensitive enzyme immunoassay for measuring plasma and intracellular nevirapine levels in human immunodeficiency virus-infected patients. Antimicrob Agents Chemother. 2004;48:104-109.
27. Yuen GJ, Lou Y, Bumgarner NF, et al. Equivalent steady-state pharmacokinetics of lamivudine in plasma and lamivudine triphosphate within cells following administration of lamivudine at 300 milligrams once daily and 150 milligrams twice daily. Antimicrob Agents Chemother. 2004;48:176-182.
28. van Leeuwen R, Lange JM, Hussey EK, et al. The safety and pharmacokinetics of a reverse transcriptase inhibitor, 3TC, in patients with HIV infection: a phase I study. AIDS. 1992;6:1471-1475.
29. Havlir D, Cheeseman SH, McLaughlin M, et al. High-dose nevirapine: safety, pharmacokinetics, and antiviral effect in patients with human immunodeficiency virus infection. J Infect Dis. 1995;171:537-545.
30. Sabo JP, Lamson MJ, Leitz G, Yong CL, MacGregor TR. Pharmacokinetics of nevirapine and lamivudine in patients with HIV-1 infection. AAPS PharmSci. 2000;2:E1.
31. Skowron G, Leoung G, Hall DB, Robinson P, Lewis R, Grosso R. Pharmacokinetic evaluation and short-term activity of stavudine, nevirapine, and nelfinavir therapy in HIV-1-infected adults. J Acquir Immune Defic Syndr. 2004;35:351-358.
32. Dudley MN, Graham KK, Kaul S, Geletko S, Dunkle L, Browne M. Pharmacokinetics of stavudine in patients with AIDS or AIDS-related complex. J Infect Dis. 1992;166:480-485.
33. Pluda JM, Cooley TP, Montaner JS, et al. A phase I/II study of 2′-deoxy-3′-thiacytidine (lamivudine) in patients with advanced human immunodeficiency virus infection. J Infect Dis. 1995;171:1438-1447.
34. Narang VS, Lulla A, Malhotra G, Purandare S. Bioequivalence evaluation of two marketed brands of stavudine 40 mg capsules in healthy human South African volunteers. Pharmacol Res. 2004;50:511-516.
35. Moore KH, Yuen GJ, Hussey EK, Pakes GE, Eron JJ Jr, Bartlett JA. Population pharmacokinetics of lamivudine in adult human immunodeficiency virus-infected patients enrolled in two phase III clinical trials. Antimicrob Agents Chemother. 1999;43:3025-3029.
36. de Maat MM, Nellen JF, Huitema AD, et al. Race is not associated with nevirapine pharmacokinetics. Ther Drug Monit. 2004;26:456-458.
37. Peytavin G, Laurent C, Boukobza S, et al. Quality of a generic fixed dose combination and pharmacokinetics of nevirapine, stavudine and lamivudine after its administration to HIV-1 infected patients in a prospective ANRS study in Cameroon. In: 44th Interscience Conference on Antimicrobial Agents and Chemotherapy (ICAAC); October 30-November 2, 2004; Washington, DC. Abstract H-867.
38. Kaul S, Mummaneni V, Barbhaiya RH. Dose proportionality of stavudine in HIV seropositive asymptomatic subjects: application to bioequivalence assessment of various capsule formulations. Biopharm Drug Dispos. 1995;16:125-136.
39. 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-S33.
40. Oyugi JH, Byakika-Tusiime J, Charlebois ED, et al. Multiple validated measures of adherence indicate high levels of adherence to generic HIV antiretroviral therapy in a resource-limited setting. J Acquir Immune Defic Syndr. 2004;36:1100-1102.