TY - JOUR
T1 - Sildenafil and bosentan plasma concentrations in a human immunodeficiency virus-infected patient with pulmonary arterial hypertension treated with ritonavir-boosted protease inhibitor
AU - Chinello, Pierangelo
AU - Cicalini, Stefania
AU - Pichini, Simona
AU - Pacifici, Roberta
AU - Tempestilli, Massimo
AU - Cicini, Maria P.
AU - Pucillo, Leopoldo P.
AU - Petrosillo, Nicola
PY - 2015
Y1 - 2015
N2 - Sildenafil and bosentan are increasingly used for the treatment of pulmonary arterial hypertension (PAH) in HIV-infected patients. However, concerns exist about pharmacokinetic interactions among sildenafil, bosentan and antiretroviral drugs, including protease inhibitors (PI). We describe here the case of an HIV-infected patient with PAH, who was co-administered bosentan 125 mg twice daily and sildenafil 40 mg three times per day, together with a ritonavir-boosted PI-based antiretroviral therapy; plasma levels of bosentan, sildenafil, N-desmethylsildenafil, and PI were measured. The patient had a sildenafil Cthrough and Cmax of 276.94 ng/mL and 1733.19 ng/mL, respectively. The Cthrough and the Cmax of bosentan were 1546.53 ng/mL and 3365.99 ng/mL, respectively. The patient was able to tolerate as high sildenafil blood concentrations as 10 times those usually requested and did not report any significant adverse reaction to sildenafil during the follow-up period. Therapeutic drug monitoring should be considered during sildenafil therapy in patients concomitantly treated with ritonavir-boosted PI.
AB - Sildenafil and bosentan are increasingly used for the treatment of pulmonary arterial hypertension (PAH) in HIV-infected patients. However, concerns exist about pharmacokinetic interactions among sildenafil, bosentan and antiretroviral drugs, including protease inhibitors (PI). We describe here the case of an HIV-infected patient with PAH, who was co-administered bosentan 125 mg twice daily and sildenafil 40 mg three times per day, together with a ritonavir-boosted PI-based antiretroviral therapy; plasma levels of bosentan, sildenafil, N-desmethylsildenafil, and PI were measured. The patient had a sildenafil Cthrough and Cmax of 276.94 ng/mL and 1733.19 ng/mL, respectively. The Cthrough and the Cmax of bosentan were 1546.53 ng/mL and 3365.99 ng/mL, respectively. The patient was able to tolerate as high sildenafil blood concentrations as 10 times those usually requested and did not report any significant adverse reaction to sildenafil during the follow-up period. Therapeutic drug monitoring should be considered during sildenafil therapy in patients concomitantly treated with ritonavir-boosted PI.
KW - Bosentan
KW - Human immunodeficiency virus
KW - Protease inhibitors
KW - Pulmonary arterial hypertension
KW - Sildenafil
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UR - http://www.scopus.com/inward/citedby.url?scp=84928719348&partnerID=8YFLogxK
U2 - 10.4081/idr.2015.5822
DO - 10.4081/idr.2015.5822
M3 - Article
AN - SCOPUS:84928719348
VL - 7
JO - Infectious Disease Reports
JF - Infectious Disease Reports
SN - 2036-7430
IS - 1
M1 - 5822
ER -