Lopinavir/ritonavir pharmacokinetics in a substitution of high-dose soft-gelatin capsule to tablet formulation

Journal of Clinical Pharmacology

Volumn 49, Issue 2, 2009, Pages 155-161

  Hull, Mark W ^a,b   Harris, Marianne ^a   Lima, Viviane ^b,c   Guillemi, Silvia ^b,c   Harrigan, P Richard ^b,c   Montaner, Julio S G ^a,b,c  

^a Canadian HIV Trials Network   (Canada)

^b BRITISH COLUMBIA CENTRE FOR EXCELLENCE IN HIV AIDS   (Canada)

^c UNIVERSITY OF BRITISH COLUMBIA   (Canada)

Author keywords

Cytochrome P450 inducers; Lopinavir ritonavir; Pharmacokinetics

Indexed keywords

AMPRENAVIR PHOSPHATE; ATAZANAVIR; CYTOCHROME P450 3A4; DIDANOSINE; EFAVIRENZ; EMTRICITABINE; ENFUVIRTIDE; LAMIVUDINE; LOPINAVIR PLUS RITONAVIR; NEVIRAPINE; SAQUINAVIR; STAVUDINE; TENOFOVIR; ZIDOVUDINE;

ADULT; ARTICLE; CD4 LYMPHOCYTE COUNT; CLINICAL ARTICLE; CLINICAL TRIAL; DEMOGRAPHY; DRUG BLOOD LEVEL; DRUG CAPSULE; DRUG DOSAGE FORM COMPARISON; DRUG DOSE INCREASE; DRUG MEGADOSE; DRUG TOLERABILITY; FEMALE; HIGH PERFORMANCE LIQUID CHROMATOGRAPHY; HIGHLY ACTIVE ANTIRETROVIRAL THERAPY; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; INDIVIDUALIZATION; INTERPATIENT VARIABILITY; MALE; MAXIMUM PLASMA CONCENTRATION; OPEN STUDY; PATIENT COMPLIANCE; RASH; SIDE EFFECT; SOFT GELATIN CAPSULE; TABLET FORMULATION; TANDEM MASS SPECTROMETRY; TRIACYLGLYCEROL BLOOD LEVEL; VIRUS LOAD;

ANTI-HIV AGENTS; ANTIRETROVIRAL THERAPY, HIGHLY ACTIVE; CAPSULES; CYTOCHROME P-450 CYP3A; DRUG COMBINATIONS; DRUG THERAPY, COMBINATION; ENZYME INDUCTION; FEMALE; GELATIN; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HUMANS; MALE; MIDDLE AGED; PYRIMIDINONES; RITONAVIR; TABLETS;

EID: 58849110616     PISSN: 00912700     EISSN: 15524604     Source Type: Journal    
DOI: 10.1177/0091270008329550     Document Type: Article

References (21)

1. Cvetkovic RS, Goa KL Lopinavir/ritonavir: a review of its use in the management of HIV infection. Drugs. 2003 ; 63: 769-802.
2. Doherty MM, Charman WN The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism ? Clin Pharmacokinet. 2002 ; 41: 235-253.
3. Walmsley S., Bernstein B., King M., et al. Lopinavir-ritonavir versus nelfinavir for the initial treatment of HIV infection. N Engl J Med. 2002 ; 346: 2039-2046.
4. Hicks C., King MS, Gulick RM, et al. Long-term safety and durable antiretroviral activity of lopinavir/ritonavir in treatment-naive patients: 4 year follow-up study. AIDS. 2004 ; 18: 775-779.
5. Bongiovanni M., Bini T., Capetti A., et al. Long-term antiretroviral efficacy and safety of lopinavir/ritonavir in HAART-experienced subjects: 4 year follow-up study. AIDS. 2005 ; 19: 1934-1936.
6. Eron JJ, Feinberg J., Kessler HA, et al. Once-daily versus twice-daily lopinavir/ritonavir in antiretroviral-naive HIV-positive patients: a 48-week randomized clinical trial. J Infect Dis. 2004 ; 189: 265-272.
7. van der Leur MR, Burger DM, la Porte CJ, Koopmans PP A retrospective TDM database analysis of interpatient variability in the pharmacokinetics of lopinavir in HIV-infected adults. Ther Drug Monit. 2006 ; 28: 650-653.
8. Breilh D., Pellegrin I., Rouzes A., et al. Virological, intracellular and plasma pharmacological parameters predicting response to lopinavir/ritonavir (KALEPHAR study). AIDS. 2004 ; 18: 1305-1310.
9. Gonzalez de Requena D., Gallego O., Valer L., Jimenez-Nacher I., Soriano V. Prediction of virological response to lopinavir/ritonavir using the genotypic inhibitory quotient. AIDS Res Hum Retroviruses. 2004 ; 20: 275-278.
10. Boffito M., Arnaudo I., Raiteri R., et al. Clinical use of lopinavir/ ritonavir in a salvage therapy setting: pharmacokinetics and pharmacodynamics. AIDS. 2002 ; 16: 2081-2083.
11. Hsu A., Isaacson J., Brun S., et al. Pharmacokinetic-pharmacodynamic analysis of lopinavir-ritonavir in combination with efavirenz and two nucleoside reverse transcriptase inhibitors in extensively pretreated human immunodeficiency virus-infected patients. Antimicrob Agents Chemother. 2003 ; 47: 350-359.
12. Dailly E., Reliquet V., Raffi F., Jolliet P. A population approach to study the influence of nevirapine administration on lopinavir pharmacokinetics in HIV-1 infected patients. Eur J Clin Pharmacol. 2005 ; 61: 153-156.
13. Mauss S., Schmutz G., Kuschak D. Unfavourable interaction of amprenavir and lopinavir in combination with ritonavir ? AIDS. 2002 ; 16: 296-297.
14. Klein CE, Chiu YL, Awni W., et al. The tablet formulation of lopinavir/ritonavir provides similar bioavailability to the soft-gelatin capsule formulation with less pharmacokinetic variability and diminished food effect. J Acquir Immune Defic Syndr. 2007 ; 44: 401-410.
15. la Porte CJ, Colbers EP, Bertz R., et al. Pharmacokinetics of adjusted-dose lopinavir-ritonavir combined with rifampin in healthy volunteers. Antimicrob Agents Chemother. 2004 ; 48: 1553-1560.
16. Alexander CS, Montaner JS, Asselin JJ, et al. Simplification of therapeutic drug monitoring for twice-daily regimens of lopinavir/ ritonavir for HIV infection. Ther Drug Monit. 2004 ; 26: 516-523.
17. Solas C., Poizot-Martin I., Drogoul MP, et al. Therapeutic drug monitoring of lopinavir/ritonavir given alone or with a non-nucleoside reverse transcriptase inhibitor. Br J Clin Pharmacol. 2004 ; 57: 436-440.
18. Gutierrez F., Padilla S., Navarro A., et al. Lopinavir plasma concentrations and changes in lipid levels during salvage therapy with lopinavir/ritonavir-containing regimens. J Acquir Immune Defic Syndr. 2003 ; 33: 594-600.
19. Gonzalez de Requena D., Blanco F., Garcia-Benayas T., et al. Correlation between lopinavir plasma levels and lipid abnormalities in patients taking lopinavir/ritonavir. AIDS Patient Care STDS. 2003 ; 17: 443-445.
20. Nettles RE, Kieffer TL, Parsons T., et al. Marked intraindividual variability in antiretroviral concentrations may limit the utility of therapeutic drug monitoring. Clin Infect Dis. 2006 ; 42: 1189-1196.
21. Boffito M., Back DJ, Hoggard PG, et al. Intra-individual variability in lopinavir plasma trough concentrations supports therapeutic drug monitoring. AIDS. 2003 ; 17: 1107-1108.