Population pharmacokinetics of lopinavir in combination with ritonavir in HIV-1-infected patients

British Journal of Clinical Pharmacology

Volumn 60, Issue 4, 2005, Pages 378-389

  Crommentuyn, K M L ^a   Kappelhoff, B S ^a   Mulder, J W ^a   Mairuhu, A T A ^a   Van Gorp, E C M ^a   Meenhorst, P L ^a   Huitema, A D R ^a   Beijnen, J H ^a,b  

^a SLOTERVAART HOSPITAL   (Netherlands)

^b UTRECHT UNIVERSITY   (Netherlands)

Author keywords

HIV; Lopinavir ritonavir; Population pharmacokinetics

Indexed keywords

EFAVIRENZ; LOPINAVIR; NEVIRAPINE; RITONAVIR; RNA DIRECTED DNA POLYMERASE INHIBITOR;

ADULT; ARTICLE; BAYES THEOREM; CONTROLLED STUDY; DRUG ABSORPTION; DRUG BLOOD LEVEL; DRUG CLEARANCE; DRUG DISTRIBUTION; DRUG EFFECT; DRUG EXPOSURE; FEMALE; HUMAN; HUMAN IMMUNODEFICIENCY VIRUS 1; HUMAN IMMUNODEFICIENCY VIRUS INFECTION; MAJOR CLINICAL STUDY; MALE; PHARMACOGENETICS; POPULATION MODEL; PRIORITY JOURNAL;

ADULT; ANTI-HIV AGENTS; CAPSULES; DRUG COMBINATIONS; FEMALE; HIV INFECTIONS; HIV PROTEASE INHIBITORS; HIV-1; HUMANS; MALE; MIDDLE AGED; MODELS, CHEMICAL; PYRIMIDINONES; RETROSPECTIVE STUDIES; RITONAVIR;

EID: 26444450453     PISSN: 03065251     EISSN: None     Source Type: Journal    
DOI: 10.1111/j.1365-2125.2005.02455.x     Document Type: Article

References (39)

1. Cvetkovic RS, Goa KL. Lopinavir/ritonavir. a review of its use in the management of HIV infection. Drugs 2003; 63: 769-802.
2. Abbott Laboratories. Kaletra Product Monograph. http 2004,// http://www.rxabbott.com/PDF/kaletrapi.pdf.6-8-.
3. Crommentuyn KML, Mulder JW, Mairuhu ATA, van Corp ECM, Meenhorst PL, Huitema ADR, Beijnen JH. The plasma and intracellular steady-state pharmacokinetics of lopinavir/ritonavir in HIV-1-infected patients. Antivir Ther 2004; 9: 779-85.
4. Doherty MM, Charman WN. The mucosa of the small intestine: how clinically relevant as an organ of drug metabolism? Clin Pharmacokinet 2002; 41: 235-53.
5. Lee CG, Gottesman MM, Cardarelli CO, Ramachandra M, Jeang KT, Ambudkar SV, Pastan I, Dey S. HIV-1 protease inhibitors are Substrates for the MDR1 multidrug transporter. Biochemistry 1998; 37: 3594-601.
6. Huisman MT, Smit JW, Wiltshire HR, Hoetelmans RMW, Beijnen JH, Schinkel AH. P-glycoprotein limits oral availability, brain, and fetal penetration of saquinavir even with high doses of ritonavir. Mol Pharmacol 2001; 59: 806-13.
7. Drewe J, Gutmann H, Fricker G, Torok M, Beglinger C, Huwyler J. HIV protease inhibitor ritonavir. a more potent inhibitor of P-glycoprotein than the cyclosporine analog SDZ PSC 833. Biochem Pharmacol 1999; 57: 1147-52.
8. Gutmann H, Fricker G, Drewe J, Toeroek M, Miller DS. Interactions of HIV protease inhibitors with ATP-dependent drug export proteins. Mol Pharmacol 1999; 56: 383-9.
9. Sham HL, Kempf DJ, Molla A, Marsh KC, Kumar GN, Chen CM, Kati W, Stewart K, Lal R, Hsu A, Betebenner D, Korneyeva M, Vasavanonda S, Mcdonald E, Salvidar A, Wideburg N, Chen X, Niu P, Park C, Jayanti V, Grabowski B, Granneman GR, Sun E, Japour AJ, Leonard JM, Plattner JJ, Norbeck DW. ABT-378, a highly potent inhibitor of the human immunodeficiency virus protease. Antimicrob Agents Chemother 1998; 42: 3218-24.
10. Solas C, Poizot-Martin I, Drogoul MP, Ravaux I, Dhiver C, Lafeuillade A, Allegre T, Mokhtari M, Moreau J, Lepeu G, Petit N, Durand A, Lacarelle B. Therapeutic drug monitoring of lopinavir/ ritonavir given alone or with a non-nucleoside reverse transcriptase inhibitor. Br J Clin Pharmacol 2004; 57: 436-40.
11. Hsu A, Isaacson J, Brun S, Bernstein B, Lam W, Bertz R, Foit C, Rynkiewicz K, Richards B, King M, Rode R, Kempf DJ, Granneman GR, Sun E. 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: 350-9.
12. Smith PF, Dicenzo R, Morse GD. Clinical pharmacokinetics of nonnucleoside reverse transcriptase inhibitors. Clin Pharmacokinet 2001; 40: 893-905.
13. Gibbons S, Robinson L, Davies G, Back DJ, Khoo SH. Is there evidence for weight-adjusted dosing of Kaletra? 10th Anniversary Conference of the British HIV Association, Cardiff, UK. Abstract P75.
14. Eron JJ, Feinberg J, Kessler HA, Horowitz HW, Witt MD, Carpio FF, Wheeler D, Ruane P, Mildvan D, Yangco BG, Bertz R, Bernstein B, King MS, Sun E. Once-daily versus twice-daily lopinavir/ritonavir in antiretroviral-naive HIV-positive patients: a 48-week randomized clinical trial. J Infect Dis 2004; 189: 265-72.
15. Crommentuyn KML, Mulder JW, Sparidans RW, Huitema ADR, Schellens JHM, Beijnen JH. Drug-drug interaction between itraconazole and the antiretroviral drug lopinavir/ritonavir in an HIV-1-infected patient with disseminated histoplasmosis. Clin Infect Dis 2004; 38: e73-e75.
16. Crommentuyn KML, Rosing H, Nan-Offeringa LG, Hillebrand MJX, Huitema ADR, Beijnen JH. Rapid quantification of HIV protease inhibitors in human plasma by high-performance liquid chromatography coupled with electrospray ionization tandem mass spectrometry. J Mass Spectrom 2003; 38: 157-66.
17. Beat SL, Sheiner LB. NONMEM, User's Guides. NONMEM Project Group. University of California at San Francisco 1998.
18. Johnsson EN, Karlsson MO. Xpose - an S-Plus based population pharmacokinetic-pharmacodynamic model building aid for NONMEM. Comp Meth Prog Biomed 1998; 58: 51-64.
19. Kappelhoff BS, Huitema ADR, Crommentuyn KML, Mulder JW, Meenhorst PL, van Gorp ECM, Mairuhu ATA, Beijnen JH. Development and validation of a population pharmacokinetic model for ritonavir used as a booster or as an antiviral agent in HIV-1-infected patients. Br J Clin Pharmacol 2005; 59: 174-82.
20. Huitema ADR, Mathôt RAA, Tibben MM, Rodenhuis S, Beijnen JH. A mechanism-based pharmacokinetic model for the cytochrome P450 drug-drug interaction between cyclophosphamide and thioTEPA and the autoinduction of cyclophosphamide. J Pharmacokinet Pharmacodyn 2001; 28: 211-30.
21. Karlsson MO, Sheiner LB. The importance of modeling interoccasion variability in population pharmacokinetic analyses. J Pharmacokinet Biopharm 1993; 21: 735-50.
22. Lee WM. Hepatitis B virus infection. N Engl J Med 1997; 337: 1733-45.
23. Sharara Al, Hunt CM, Hamilton JD. Hepatitis C. Ann Intern Med 1996; 125: 658-68.
24. Parke J, Holford NH, Charles BG. A procedure for generating bootstrap samples for the validation of nonlinear mixed-effects population models. Comput Meth Programs Biomed 1999; 59: 19-29.
25. Hurst M, Faulds D. Lopinavir. Drugs 2000; 60: 1371-9.
26. Best B, Haubrich R, Miller C, Witt M, Kemper C, Squires K, Diamond C, Heseltine P, Hellman N, Mccutchan JA, Capparelli E. Population pharmacokinetics of lopinavir/ritonavir in experienced patients. 10th Conference on Retroviruses and Opportunistic Infections 10-14 February, 2003, Boston, MA, USA, Abstract 527.
27. Takanaga H, Ohnishi A, Murakami H, Matsuo H, Higuchi S, Urae A, Irie S, Furuie H, Matsukuma K, Kimura M, Kawano K, Orii Y, Tanaka T, Sawada Y. Relationship between time after intake of grapefruit juice and the effect on pharmacokinetics and pharmacodynamics of nisoldipine in healthy subjects. Clin Pharmacol Ther 2000; 67: 201-14.
28. Takanaga H, Ohnishi A, Matsuo H, Murakami H, Sata H, Kuroda K, Urae A, Higuchi S, Sawada Y. Pharmacokinetic analysis of felodipine-grapefruit juice interaction based on an irreversible enzyme inhibition model. Br J Clin Pharmacol 2000; 49: 49-58.
29. Lamba JK, Lin YS, Schuetz EG, Thummel KE. Genetic contribution to variable human CYP3A-mediated metabolism. Adv Drug Deliv Rev 2002; 54: 1271-94.
30. Hsu A, Granneman GR, Bertz RJ. Ritonavir. Clinical pharmacokinetics and interactions with other anti-HIV agents. Clin Pharmacokinet 1998; 35: 275-91.
31. Breilh D, Pellegrin I, Rouzés A, Berthoin K, Xuereb F, Budzinski H, Munck M, Fleury HJA, Saux MC, Pellegrin JL. Virological, intracellular and plasma pharmacological parameters predicting response to lopinavir/ritonavir (KALEPHAR Study). AIDS 2004; 18: 1305-10.
32. Lal R, Hsu A, Bertz R, Lam W, Jennings J, Brooks R, Bryan P, Sun E, Granneman GR, Japour A. Evaluation of the pharmacokinetics if the concurrent administration of ABT-378/ritonavir and nevirapine. 7th European Conference on Clinical Aspects and Treatment of HIV-Infection 23-27 October, 1999, Lisbon, Portugal, Abstract 782.
33. Hsu A, Bertz R, Renz C, Lam W, Rode R, Deetz C, Schweitzer SM, Bernstein B, Brun S, Granneman GR, Sun E. Assessment of the pharmacokinetic interaction between lopinavir/ritonavir and nevirapine in HIV-infected pediatric subjects. 5th International Congress on Drug Therapy in HIV Infection 22-26 October, 2000, Glasgow, UK, P 292.
34. Bertz R, Foit C, Burt D, Grebner K, Marsh T, Bernstein B, Brun S, Chiu YL, King M, Hsu A, Granneman GR, Sun E. Assessment of the effect of nevirapine on the pharmacokinetics of lopinavir/ ritonavir (Kaletra®) after multiple dosing in HIV-infected adults. XIV. International AIDS Conference.: Barcelona, Spain. TuPeB4565.
35. Taburet AM, Piketty C, Chazallon C, Vincent I, Gerard L, Calvez V, Clavel F, Aboulker JP, Girard PM. Interactions between atazanavir-ritonavir and tenofovir in heavily pretreated human immunodeficiency virus-infected patients. Antimicrob Agents Chemother 2004; 48: 2091-6.
36. Scarsi K, Postelnick M, Murphy R. Comparison of lopinavir/r plasma levels with and without tenofovir as part of HAART in HIV-1-infected patients. 5th International Workshop on Clinical Pharmacology of HIV Therapy 1-3 April, 2004, Rome, Italy. Abstract 4.14.
37. Stephan C, Hentig N, Kourbeti I, Dauer B, Mosch M, Lutz T, Klauke S, Harder S, Kurowski M, Staszewski S. Saquinavir drug exposure is not impaired by the boosted double protease inhibitor combination of lopinavir/ritonavir. AIDS 2004; 18: 503-8.
38. De Luca A, Baldini F, Cingolani A, Di Giambenedetto S, Hoetelmans RMW, Cauda R. Deep salvage with amprenavir and lopinavir/ritonavir: Correlation of pharmacokinetics and drug resistance with pharmacodynamics. J Acquir Immune Defic Syndr 2004; 35: 359-66.
39. Taburet AM, Raguin G, Le Tiec C, Droz C, Barrail A, Vincent I, Morand-Joubert L, Chêne G, Clavel F, Girard PM. Interactions between amprenavir and the lopinavir-ritonavir combination in heavily pretreated patients infected with human immunodeficiency virus. Clin Pharmacol Ther 2004; 75: 310-23.