title: Novel Antiretroviral Drugs in Patients with Renal Impairment: Clinical and Pharmacokinetic Considerations.
abstract: Highly active antiretroviral therapy (HAART) has dramatically increased the survival of HIV-infected patients from Western countries reducing the incidence of opportunistic infections and AIDS-related malignancies, and improving the patients' quality of life compared with the pre-HAART era. HIV is thus now considered in the West as a chronic disease, with the majority of HIV-infected patients successfully reaching an optimal immune and virological outcome a few months after starting HAART. However, this switch from acute to chronic disease has been accompanied by an increased incidence of chronic kidney disease (CKD), reported in up to 60% of HIV-infected patients. Tenofovir disoproxil fumarate (TDF) is considered to play a significant role in the development of CKD in these patients. It has been proposed that tenofovir alafenamide (TAF), a prodrug formulation able to providing lower systemic and renal drug exposure, could potentially contribute to reduce the development of CKD in HAART-treated patients. On the other hand, the pharmacokinetics of some components of HAART can be significantly altered in HIV-infected patients developing CKD. TDF- or TAF-based antiretroviral regimens should be avoided in patients with a creatinine clearance of less than 50 or 30 mL/min, respectively. This review focuses on the pharmacokinetic changes of novel antiretroviral drugs in HIV-infected patients with renal impairment or requiring renal replacement therapy, and provides some suggestions on how to change drug doses in these clinical settings.
authors.affiliation: Unit of Clinical Pharmacology, Department of Laboratory Medicine, ASST Fatebenefratelli Sacco University Hospital, Via GB Grassi 74, 20157, Milan, Italy. dario.cattaneo@asst-fbf-sacco.it.
authors.forename: Dario
authors.initials: D
authors.lastname: Cattaneo
authors.affiliation: III Division of Infectious Diseases, Department of Infectious Diseases, ASST Fatebenefratelli Sacco University Hospital, Milan, Italy.
authors.forename: Cristina
authors.initials: C
authors.lastname: Gervasoni
mesh_terms: D044966:Anti-Retroviral Agents / Q000009:adverse effects / Q000493:pharmacokinetics* / Q000627:therapeutic use; D023241:Antiretroviral Therapy, Highly Active; D016903:Drug Monitoring; D015658:HIV Infections / Q000150:complications / Q000188:drug therapy / Q000378:metabolism*; D006801:Humans; D007677:Kidney Function Tests; D051436:Renal Insufficiency, Chronic / Q000150:complications / Q000188:drug therapy / Q000378:metabolism*
chemical_list: D044966:Anti-Retroviral Agents