title: The pharmacokinetic profile of raltegravir-containing antiretroviral therapy in HIV-infected individuals over 60 years of age.
abstract: Antiretroviral safety and efficacy and may differ in older versus younger HIV-infected patients. The objective of this study was to assess the pharmacokinetic (PK) profile in older HIV-infected subjects (>60 years) switching combination antiretroviral therapy (cART) to a raltegravir (RAL) containing regimen.
  
  
  
  Nineteen HIV-infected patients over 60 years of age on effective cART (HIV-RNA < 50 copies/ml) were enrolled in this prospective 24-week study. On day 1, patients switched to tenofovir/emtricitabine (245/200 mg once daily) and RAL (400 mg twice daily). On day 28, intensive PK sampling was undertaken in a fasted state and RAL plasma concentrations determined. Neurocognitive function was assessed at baseline and week 24 using a neuropsychological battery. RAL PK parameters were compared to those of two younger historical HIV-infected control groups that received twice-daily RAL co-administered with darunavir/ritonavir (DRV/r) 800/100 once daily by nonlinear mixed effects modelling.
  
  
  
  In HIV-infected subjects over the age of 60 (mean ± SD age: 66 ± 3.4 years, n = 19) switching to a RAL containing regimen, we observed no safety concerns, no plasma virological rebounds, and no differences in RAL apparent oral clearance when compared to younger HIV-infected populations (mean ± SD age: 41 ± 9.2 years, n = 38) based on population pharmacokinetic analysis. After 24 weeks of study therapy a decline in cognitive function was observed [change in (SD) global score of (0.91 (1.3), P = 0.018].
  
  
  
  No significant changes in RAL exposure associated with age were observed.
authors.forename: Jaime H
authors.initials: JH
authors.lastname: Vera
authors.forename: Akil
authors.initials: A
authors.lastname: Jackson
authors.forename: Laura
authors.initials: L
authors.lastname: Dickinson
authors.forename: Laura
authors.initials: L
authors.lastname: Else
authors.forename: Tristan
authors.initials: T
authors.lastname: Barber
authors.forename: Borja
authors.initials: B
authors.lastname: Mora-Peris
authors.forename: David
authors.initials: D
authors.lastname: Back
authors.forename: Marta
authors.initials: M
authors.lastname: Boffito
authors.forename: Alan
authors.initials: A
authors.lastname: Winston
mesh_terms: D000328:Adult; D019380:Anti-HIV Agents / Q000493:pharmacokinetics* / Q000494:pharmacology; D019540:Area Under Curve; D018791:CD4 Lymphocyte Count; D004359:Drug Therapy, Combination; D000068679:Emtricitabine / Q000493:pharmacokinetics* / Q000494:pharmacology; D005260:Female; D015658:HIV Infections / Q000188:drug therapy* / Q000821:virology; D015497:HIV-1 / Q000187:drug effects; D006801:Humans; D008297:Male; D000073216:Mental Status and Dementia Tests; D008875:Middle Aged; D011446:Prospective Studies; D000068898:Raltegravir Potassium / Q000493:pharmacokinetics* / Q000494:pharmacology; D000068698:Tenofovir / Q000493:pharmacokinetics* / Q000494:pharmacology; D006113:United Kingdom; D019562:Viral Load / Q000187:drug effects
chemical_list: D019380:Anti-HIV Agents; D000068898:Raltegravir Potassium; D000068698:Tenofovir; D000068679:Emtricitabine
keywords: Aging; Pharmacokinetics,; Raltegravir,