title: The steady-state pharmacokinetics of efavirenz and nevirapine when used in combination in human immunodeficiency virus type 1-infected persons.
abstract: The steady-state pharmacokinetics of efavirenz and nevirapine, when used in combination to treat human immunodeficiency virus type 1 (HIV-1)-infected subjects, were investigated. HIV-1-infected persons who had used efavirenz (600 mg once daily) for > or =2 weeks were eligible for study inclusion. The plasma pharmacokinetics of efavirenz were determined over 24 h. Subsequently, nevirapine (400 mg once daily) was added to the regimen. After 4 weeks, the pharmacokinetics of efavirenz and nevirapine were assessed over 24 h. The differences between the pharmacokinetic parameters of efavirenz with and without nevirapine were analyzed, and the pharmacokinetics of nevirapine were compared with those in historical control patients. The exposure to efavirenz when combined with nevirapine was significantly decreased by 22% (area under the plasma concentration vs. time curve), 36% (minimum plasma concentration), and 17% (maximum plasma concentration). Nevirapine pharmacokinetics appear to be unaffected by coadministration of efavirenz, compared with data from historical control patients.
authors.affiliation: Department of Pharmacy and Pharmacology, Slotervaart Hospital, 1066 EC Amsterdam, The Netherlands. apabg@slz.nl
authors.forename: A I
authors.initials: AI
authors.lastname: Veldkamp
authors.forename: M
authors.initials: M
authors.lastname: Harris
authors.forename: J S
authors.initials: JS
authors.lastname: Montaner
authors.forename: G
authors.initials: G
authors.lastname: Moyle
authors.forename: B
authors.initials: B
authors.lastname: Gazzard
authors.forename: M
authors.initials: M
authors.lastname: Youle
authors.forename: M
authors.initials: M
authors.lastname: Johnson
authors.forename: M O
authors.initials: MO
authors.lastname: Kwakkelstein
authors.forename: H
authors.initials: H
authors.lastname: Carlier
authors.forename: R
authors.initials: R
authors.lastname: van Leeuwen
authors.forename: J H
authors.initials: JH
authors.lastname: Beijnen
authors.forename: J M
authors.initials: JM
authors.lastname: Lange
authors.forename: P
authors.initials: P
authors.lastname: Reiss
authors.forename: R M
authors.initials: RM
authors.lastname: Hoetelmans
mesh_terms: D000328:Adult; D000480:Alkynes; D019380:Anti-HIV Agents / Q000008:administration & dosage / Q000493:pharmacokinetics*; D048588:Benzoxazines; D003521:Cyclopropanes; D004334:Drug Administration Schedule; D004359:Drug Therapy, Combination; D015658:HIV Infections / Q000097:blood* / Q000188:drug therapy; D015497:HIV-1; D006207:Half-Life; D006801:Humans; D008297:Male; D019829:Nevirapine / Q000008:administration & dosage / Q000493:pharmacokinetics*; D010078:Oxazines / Q000008:administration & dosage / Q000493:pharmacokinetics*; D018894:Reverse Transcriptase Inhibitors / Q000008:administration & dosage / Q000493:pharmacokinetics*; D019562:Viral Load
chemical_list: D000480:Alkynes; D019380:Anti-HIV Agents; D048588:Benzoxazines; D003521:Cyclopropanes; D010078:Oxazines; D018894:Reverse Transcriptase Inhibitors; D019829:Nevirapine; C098320:efavirenz