title: Pharmacokinetics and safety of the lopinavir/ritonavir tablet 500/125 mg twice daily coadministered with efavirenz in healthy adult participants.
abstract: A study was conducted in healthy adults (n = 19) to evaluate the pharmacokinetics of lopinavir/ritonavir when coadministered with efavirenz. Participants were administered lopinavir/ritonavir 400/100 mg alone twice daily (bid) from the morning of day 1 through the morning of day 10, and then lopinavir/ritonavir 500/125 mg bid was coadministered with efavirenz 600 mg every evening (qhs) from the evening of day 10 through day 20. Lopinavir and ritonavir exposures when administered alone versus with efavirenz were determined on days 10 and 20 and compared using point estimates and 90% confidence intervals. The point estimates for the ratios of lopinavir maximum observed plasma concentration (C(max)), plasma concentration prior to morning dosing (C(trough)), and area under the plasma concentration-time curve over a dosing interval (AUC(12)) were 1.121, 0.954, and 1.060, respectively. The lopinavir/ritonavir dose of 500/125 mg bid administered with efavirenz most closely approximates the pharmacokinetic exposure of lopinavir/ritonavir 400/100 mg bid administered alone.
authors: Abbott Laboratories, Abbott Park, IL, USA. Juki.Ng@abbott.com
authors: Juki
authors: J
authors: Ng
authors: Yi-Lin
authors: YL
authors: Chiu
authors: Walid
authors: W
authors: Awni
authors: Barry
authors: B
authors: Bernstein
authors: Sonja J
authors: SJ
authors: Causemaker
authors: Cheri E
authors: CE
authors: Klein
mesh_terms: D000293:Adolescent; D000328:Adult; D000480:Alkynes; D048588:Benzoxazines / Q000008:administration & dosage / Q000009:adverse effects / Q000493:pharmacokinetics; D003521:Cyclopropanes; D004334:Drug Administration Schedule; D004347:Drug Interactions; D004359:Drug Therapy, Combination / Q000009:adverse effects* / Q000379:methods; D005260:Female; D006801:Humans; D061466:Lopinavir / Q000008:administration & dosage / Q000009:adverse effects* / Q000097:blood / Q000493:pharmacokinetics*; D008297:Male; D008875:Middle Aged; D019438:Ritonavir / Q000008:administration & dosage* / Q000009:adverse effects* / Q000493:pharmacokinetics*; D013607:Tablets / Q000008:administration & dosage* / Q000009:adverse effects* / Q000493:pharmacokinetics*; D055815:Young Adult
chemical_list: D000480:Alkynes; D048588:Benzoxazines; D003521:Cyclopropanes; D013607:Tablets; D061466:Lopinavir; C098320:efavirenz; D019438:Ritonavir