A phase i, randomized, open-label, crossover study of the single-dose pharmacokinetic properties of guanfacine extended-release 1-, 2-, and 4-mg tablets in healthy adults

Population Pharmacokinetic Modeling of Guanfacine in Pediatric Patients

“…The typical population PK parameters (CL/F and V/F) from the final model, following allometric scaling to 70 kg, were similar, though slightly higher than the mean parameters in adult patients reported in the literature [20]. The The values from this analysis were higher than those found in the adult literature.…”

A Review of the Rationale and Clinical Utilization of α2-Adrenoceptor Agonists for the Treatment of Attention-Deficit/Hyperactivity and Related Disorders

“…For GXR, increases in C max and AUC were proportional to dose, but lower compared with GUAN-IR (e.g., the relative bioavailability of GXR compared with GUAN-IR is 57%) (PDR Network and Staff 2011). Importantly GXR also exhibits a longer T max than GUAN-IR (Kiechel 1980;Swearingen et al 2007;Newcorn et al 2011a;PDR Network and Staff 2011;). In both children and adolescents, GXR T max is 5 hours with dose-related increases in maximum concentration (C max ) (Boellner et al 2007).…”

“…Subsequent pharmacokinetic studies of GXR demonstrated a large differences from GUAN-IR for maximal concentration (C max ), time to maximal concentration (T max ), and total systemic exposure (area under the curve [AUC]) (Swearingen et al 2007). For GXR, increases in C max and AUC were proportional to dose, but lower compared with GUAN-IR (e.g., the relative bioavailability of GXR compared with GUAN-IR is 57%) (PDR Network and Staff 2011).…”

“…GXR GXR (Intuniv Ò , Shire Development LLC, Wayne, PA) is FDAapproved for once-daily administration for the treatment of ADHD (Boellner et al 2007;Intuniv 2011;Shojaei et al 2006;Swearingen et al 2007). Two short-term (8-and 9-week) pivotal studies (Table 1) (Biederman et al 2008b;Sallee et al 2009b) were conducted using GXR as monotherapy.…”

Profile of guanfacine extended release and its potential in the treatment of attention-deficit hyperactivity disorder

“…27,33 Conversely, GXR exhibits a time to C max twice as long as GIR, reaching a time to C max 6 hours after GXR dosing compared with 3 hours after dosing with GIR. 41,43 The pharmacokinetics of GXR do not seem to change with dose, but are significantly affected by food intake. When administered with a high-fat meal, exposure to guanfacine from GXR is increased significantly, with approximately a 40% increase in AUC and a 75% increase in C max compared to dosing in a fasted state.…”