metricas
covid
Buscar en
Enfermedades Infecciosas y Microbiología Clínica
Toda la web
Inicio Enfermedades Infecciosas y Microbiología Clínica Interacciones medicamentosas de darunavir
Journal Information
Vol. 26. Issue S10.
Darunavir
Pages 43-50 (October 2008)
Share
Share
Download PDF
More article options
Vol. 26. Issue S10.
Darunavir
Pages 43-50 (October 2008)
Full text access
Interacciones medicamentosas de darunavir
Pharmacological interactions with darunavir
Visits
4980
José Moltóa,b,
Corresponding author
jmolto.fls.gezmanstrias@gencat.cat

Correspondencia: Fundació Lluita contra la Sida. Unidad VIH. Hospital Universitari Germans Trias i Pujol. Carretera del Canyet, s/n. 08916 Badalona. Barcelona. España.
, Marta Valleb,c, Bonaventura Clotetb,d
a Fundación Lluita contra la Sida. Hospital Universitari Germans Trias i Pujol. Badalona. Barcelona. España
b Centre d’Investigació del Medicament. Institut de Recerca. Hospital de la Santa Creu i Sant Pau. Universitat Autónoma de Barcelona. Barcelona. España
c Centre d’Investigació del Medicament. Institut de Recerca. Hospital de la Santa Creu i Sant Pau. Barcelona. España
d Fundación IrsiCaixa. Hospital Universitari Germans Trias i Pujol. Badalona. Barcelona. España
This item has received
Article information

Darunavir es un nuevo inhibidor de la proteasa del virus de la inmunodeficiencia humana (VIH) que ha demostrado tener una gran utilidad en el tratamiento de los pacientes infectados por el VIH. Darunavir se metaboliza por el citocromo P450 hepático, por lo que su administración con dosis bajas de ritonavir resulta en un marcado incremento en la exposición a éste y permite reducir el número de comprimidos y de dosis diarias. Tanto darunavir como ritonavir actúan como inhibidores a la vez que sustratos del citocromo CYP3A4, por lo que son susceptibles de presentar interacciones medicamentosas con un amplio número de fármacos comúnmente usados en los pacientes infectados por el VIH. El objetivo de esta revisión es el de resumir los principales estudios llevados a cabo para evaluar dichas interacciones y servir de guía para el manejo del tratamiento con darunavir/ritonavir en la práctica clínica.

Palabras clave:
Darunavir
Interacciones medicamentosas

Darunavir is a new HIV protease inhibitor that has been shown to be highly useful in HIV-infected patients. This drug is primarily metabolized by the liver through the cytochrome P450 3A4 (CYP3A4) isozyme and consequently coadministration with low doses of ritonavir markedly increases exposure and allows both daily doses and pill burden to be reduced. Both darunavir and ritonavir act as inhibitors and substrates of CYP3A4 and may therefore present pharmacological interactions with a large number of drugs commonly used in HIV-infected patients. The present review aims to summarize the main studies that have evaluated drug interactions and to provide recommendations on treatment with darunavir/ritonavir in clinical practice.

Key words:
Darunavir
Drug-drug interactions
Full text is only aviable in PDF
Bibliografía
[1.]
S. De Meyer, H. Azijn, D. Surleraux, et al.
TMC114, a novel human immunodeficiency virus type 1 protease inhibitor active against protease inhibitorresistant viruses, including a broad range of clinical isolates.
Antimicrob Agents Chemother, 49 (2005), pp. 2314-2321
[2.]
B. Clotet, N. Bellos, J.M. Molina, et al.
Efficacy and safety of darunavir-ritonavir at week 48 in treatment-experienced patients with HIV-1 infection in POWER 1 and 2: a pooled subgroup analysis of data from two randomised trials.
Lancet, 369 (2007), pp. 1169-1178
[3.]
J.V. Madruga, D. Berger, M. McMurchie, et al.
Efficacy and safety of darunavir-ritonavir compared with that of lopinavir-ritonavir at 48 weeks in treatment-experienced, HIV-infected patients in TITAN: a randomised controlled phase III trial.
[4.]
R. Ortiz, E. DeJesus, H. Khanlou, E. Veronin, J. Van Lunzen, J. Andrade-Villanueva, et al.
Efficacy and safety of darunavir/ritonavir versus lopinavir/ritonavir in treatment-naïve HIV-1-infected patients at week 48.
[5.]
PREZISTA® (darunavir) Ficha técnica. Disponible en: http://www.emea.europa.eu/humandocs/Humans/EPAR/prezista/prezista.htm
[6.]
V. Sekar, S. Spinosa-Guzmán, E. Lefebvre, et al.
Cinical Pharmacology of TMC114 – a new HIV protease inhibitor.
16th Internacional AIDS Conference,
[7.]
V. Sekar, S. De Meyer, T. Vangeneudgden, et al.
Pharmacokinetic/pharmacodynamic (PK/PD) analyses of TMC114 in the POWER 1 and POWER 2 trials in treatment-experienced HIV-infected patients.
13th Conference on Retroviruses and Opportunistic Infections,
[8.]
V. Sekar, E. Lefebvre, S. Spinosa-Guzmán, et al.
Pharmacokinetic interaction between the HIV protease inhibitors TMC114 and saquinavir, in the presence of low-dose of ritonavir.
44th Annual Meeting of the Infectious Diseases Society of America,
[9.]
V. Sekar, E. Lefebvre, G. Boogaerts, et al.
Pharmacokinetic interaction between the protease inhibitors TMC114 and lopinavir/ritonavir.
46th Interscience Conference on Antimicrobial Agents and Chemotherapy,
[10.]
V. Sekar, T. De Marez, S. Spinosa-Guzmán, et al.
Pharmacokinetic interaction between TMC114/ritonavir and atazanavir in healthy volunteers.
10th European AIDS Conference,
[11.]
V. Sekar, M. De Pauwn, K. Marien, et al.
Pharmacokinetic interaction between TMC114/r and efavirenz in healthy volunteers.
Antivir Ther, 12 (2007), pp. 509-514
[12.]
V. Sekar, E. Lefevbre, K. Marien, et al.
Pharmacokinetic interaction between the antirretroviral agents TMC114 and nevirapine, in the presence of low-dose ritonavir.
44th Annual Meeting of the Infectious Diseases Society of America,
[13.]
M. Boffito, A. Winston, C. Fletcher, et al.
Pharmacokinetics (PK) and antiretroviral (ARV) response to TMC114/r and TMC125 combination in patients with high level viral resistance.
13th Conference on Retroviruses and Opportunistic Infections,
[14.]
R. Hoetelmans, K. Mariën, M. De Pauw, et al.
Pharmacokinetic interaction between TMC114/ritonavir and tenofovir disoproxil fumarate in healthy volunteers.
Br J Clin Pharmacol, 64 (2007), pp. 655-661
[15.]
V. Sekar, S. Spinosa-Guzmán, E. De Paepe, et al.
Pharmacokinetic interaction trial between darunavir in combination with low-dose of ritonavir and didanosine.
4th IAS Conference on HIV Patogénesis, Treatment and Prevention,
[16.]
V. Sekar, E. De Paepe, T. Vangeneugden, et al.
Absence of an interaction between the potent HIV protease inhibitor TMC114 and the fusion inhibitor enfuvirtide in the POWER 3 analysis.
7th International Workshop on Clinical Pharmacology of HIV Therapy,
[17.]
S. Abel, G. Ridgeway, J. Hamlin, et al.
An open, randomised, 2-way crossover study to investigate the effect of darunavir/ritonavir on the pharmacokinetics of Maraviroc in healthy subjects 8th International Workshop on Clinical Pharmacology of HIV Therapy,
[18.]
A. Mathias, G. Shen, J. Enejosa, et al.
Lack of pharmacokinetic interaction between ritonavir-boosted GS-9137(elvitegravir) and darunavir/r.
4th IAS Conference on HIV Pathogenesis and Treatment,
[19.]
V. Sekar, S. Guzmán, M. De Pauwn, et al.
The pharmacokinetic interaction between clarithromycin and TMC114/ritonavir in healthy subjects.
The 2006 Annual Meeting of the American Society for Clinical Pharmacology and Therapeutics,
[20.]
V. Sekar, E. Lefevbre, M. De Pauwn, et al.
Pharmacokinetic interaction between TMC114 and ketoconazole, in the absence and presence of low-dose ritonavir.
44th Annual Meeting of the Infectious Diseases Society of America,
[21.]
V.J. Sekar, S. Spinosa-Guzmán, K. Marien, et al.
Pharmacokinetic drug-drug interaction between the new HIV protease inhibitor darunavir (TMC114) and the lipid-lowering agent pravastatin.
8th International Workshop on Pharmacology of HIV Therapy,
[22.]
R. Hoetelmans, A. Lasure, A. Koester, et al.
The effect of TMC114, a potent next-generation HIV protease inhibitor, with low-dose ritonavir on atorvastatin pharmacokinetics.
44th Interscience Conference on Antimicrobial Agents and Chemotherapy,
[23.]
V. Sekar, E. Lefebvre, S. Spinosa-Guzmán, et al.
Pharmacokinetic interaction between ethinyl estradiol, norethindrone and TMC114, a new protease inhibitor.
46th Interscience Conference on Antimicrobial Agents and Chemotherapy,
[24.]
V. Sekar, E. Lefebvre, E. De Paepe, et al.
Pharmacokinetic interaction of darunavir boosted with ritonavir and omeprazole or ranitidine in human immunodeficiency virus-negative healthy volunteers.
Antimicrob Agents Chemother, 51 (2007), pp. 958-961
[25.]
V. Sekar, M. Malt, E. De Paepe, et al.
Pharmacokinetic interaction between darunavir (TMC114), a new protease inhibitor, and methadone.
8th International Congress on Drug Therapy in HIV Infection,
[26.]
V. Sekar, E. Lefebvre, T. De Marez, et al.
Pharmacokinetic interaction between TMC114, a new protease inhibitor and sildenafil.
46th Interscience Conference on Antimicrobial Agents and Chemotherapy,
[27.]
V. Sekar, E. De Paepe, T. De Marez, et al.
Pharmacokinetic interaction between darunavir (TMC114), a new protease inhibitor, and the selective serotonin reuptake inhibitors (SSRIs), paroxetine and sertraline.
8th Internacional Congress on Drug Therapy in HIV Infection,
Copyright © 2008. Elsevier España S.L.. Todos los derechos reservados
Download PDF
Article options
es en pt

¿Es usted profesional sanitario apto para prescribir o dispensar medicamentos?

Are you a health professional able to prescribe or dispense drugs?

Você é um profissional de saúde habilitado a prescrever ou dispensar medicamentos