title: Pharmacokinetic, safety, and antiviral profiles of oral ganciclovir in persons infected with human immunodeficiency virus: a phase I/II study. AIDS Clinical Trials Group, and Cytomegalovirus Cooperative Study Group.
abstract: A phase I/II study evaluated the pharmacokinetics, tolerability, and antiviral activity of oral ganciclovir in persons infected with human immunodeficiency virus (HIV). Oral bioavailability ranged from 2.6% to 7.3%. The mean maximum serum concentration achieved at 1000 mg every 8 h was 1.11 micrograms/mL, and mean trough level was 0.54 microgram/mL. The time to maximum serum drug concentration was 1.0-2.9 h, with a serum half-life of 3.0-7.3 h, suggesting prolonged oral absorption. Serious adverse events were uncommon. Decreased cytomegalovirus (CMV) shedding was observed from all sites. The median days (by dosage) to retinitis progression assessed by retinal examination after initiation of oral ganciclovir were 62 (1000 mg every 8 h), 148 (500 mg every 3 h), 75 (750 mg every 3 h), 148 (1000 mg every 3 h), and 139 (2000 mg every 8 h). Thus, oral ganciclovir has pharmacokinetic, toxicity, and antiviral profiles that may prove beneficial for both maintenance therapy of CMV retinitis and prevention of CMV disease in HIV-infected persons.
authors.affiliation: Dept. of Pediatrics, University of California, San Diego, La Jolla 92093-0672, USA.
authors.forename: S A
authors.initials: SA
authors.lastname: Spector
authors.forename: D F
authors.initials: DF
authors.lastname: Busch
authors.forename: S
authors.initials: S
authors.lastname: Follansbee
authors.forename: K
authors.initials: K
authors.lastname: Squires
authors.forename: J P
authors.initials: JP
authors.lastname: Lalezari
authors.forename: M A
authors.initials: MA
authors.lastname: Jacobson
authors.forename: J D
authors.initials: JD
authors.lastname: Connor
authors.forename: D
authors.initials: D
authors.lastname: Jung
authors.forename: A
authors.initials: A
authors.lastname: Shadman
authors.forename: B
authors.initials: B
authors.lastname: Mastre
mesh_terms: D000284:Administration, Oral; D000328:Adult; D003586:Cytomegalovirus Infections / Q000188:drug therapy*; D017726:Cytomegalovirus Retinitis / Q000188:drug therapy; D015774:Ganciclovir / Q000008:administration & dosage* / Q000009:adverse effects / Q000493:pharmacokinetics; D015658:HIV Infections / Q000188:drug therapy*; D006801:Humans; D008297:Male
chemical_list: D015774:Ganciclovir