Once-daily treatment with saquinavir mesylate (2000 mg) and ritonavir (100 mg) together with a fixed-dose combination of abacavir/lamivudine (600/300 mg) or tenofovir/emtricitabine (245/200 mg) in HIV-1-infected patients.
J Antimicrob Chemother
; 64(6): 1260-4, 2009 Dec.
Article
em En
| MEDLINE
| ID: mdl-19776037
ABSTRACT
OBJECTIVES:
To investigate the feasibility and pharmacokinetics of a once-daily regimen of 2000 mg saquinavir mesylate boosted with 100 mg ritonavir. PATIENTS ANDMETHODS:
Patients successfully treated with 1000 mg saquinavir boosted with 100 mg ritonavir twice daily together with two nucleoside or nucleotide reverse transcriptase inhibitors [N(t)RTIs] who were switched to 2000 mg saquinavir with 100 mg ritonavir once daily with unchanged N(t)RTI therapy were analysed. CD4 cells, HIV-RNA PCR and metabolic parameters were compared between baseline and 3, 6, 9 and 12 months after the switch. Saquinavir and ritonavir drug levels were measured before and a median of 3 weeks after switching from twice to once daily at 0, 1, 2, 4, 6, 9, 12 and 24 h after intake of the medication. The area under the serum concentration-time curve from 0 to 24 h (AUC(0-24)) was calculated using the trapezoidal rule.RESULTS:
Eighteen patients (16 males, median age of 41 years) with a median CD4 cell count of 464 cells/mm(3) were analysed. HIV-RNA PCR remained <500 copies/mL for all patients. After switching from 100 mg twice daily to 100 mg once daily, the AUC(0-24) for ritonavir decreased significantly [21 874 to 10 267 ng.h/mL, geometric mean ratio (GMR) = 0.47; P < 0.001], whereas the AUC(0-24) for saquinavir decreased only marginally from 35 000 to 34 490 ng.h/mL (GMR = 0.99; P = 0.426). The CD4 cell count and the fasting metabolic parameters remained unchanged.CONCLUSIONS:
Once-daily treatment with ritonavir-boosted saquinavir was well tolerated and resulted in similar saquinavir drug exposure despite much lower ritonavir concentrations when compared with a twice-daily dosing schedule.
Texto completo:
1
Coleções:
01-internacional
Base de dados:
MEDLINE
Assunto principal:
Adenina
/
Infecções por HIV
/
Ritonavir
/
Saquinavir
/
Lamivudina
/
Fármacos Anti-HIV
/
Desoxicitidina
/
Organofosfonatos
Tipo de estudo:
Prognostic_studies
Idioma:
En
Revista:
J Antimicrob Chemother
Ano de publicação:
2009
Tipo de documento:
Article
País de afiliação:
Alemanha