title: Lisdexamfetamine Dimesylate: Prodrug Delivery, Amphetamine Exposure and Duration of Efficacy.
abstract: Lisdexamfetamine dimesylate (LDX) is a long-acting d-amphetamine prodrug used to treat attention-deficit/hyperactivity disorder (ADHD) in children, adolescents and adults. LDX is hydrolysed in the blood to yield d-amphetamine, and the pharmacokinetic profile of d-amphetamine following oral administration of LDX has a lower maximum plasma concentration (Cmax), extended time to Cmax (Tmax) and lower inter- and intra-individual variability in exposure compared with the pharmacokinetic profile of an equivalent dose of immediate-release (IR) d-amphetamine. The therapeutic action of LDX extends to at least 13 h post-dose in children and 14 h post-dose in adults, longer than that reported for any other long-acting formulation. Drug-liking scores for LDX are lower than for an equivalent dose of IR d-amphetamine, which may result from the reduced euphorigenic potential associated with its pharmacokinetic profile. These pharmacokinetic and pharmacodynamic characteristics of LDX may be beneficial in the management of symptoms in children, adolescents and adults with ADHD.
authors.affiliation: Shire, Wayne, PA, USA.
authors.forename: James C
authors.initials: JC
authors.lastname: Ermer
authors.affiliation: Shire, Basingstoke, UK. mike.pennick@hotmail.com.|University of Dundee, Dundee, UK. mike.pennick@hotmail.com.
authors.forename: Michael
authors.initials: M
authors.lastname: Pennick
authors.affiliation: Shire, Wayne, PA, USA.
authors.forename: Glen
authors.initials: G
authors.lastname: Frick
mesh_terms: D000284:Administration, Oral; D000293:Adolescent; D000328:Adult; D000661:Amphetamine / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D001289:Attention Deficit Disorder with Hyperactivity / Q000097:blood / Q000188:drug therapy; D000697:Central Nervous System Stimulants / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D002648:Child; D016503:Drug Delivery Systems / Q000379:methods*; D006801:Humans; D000069478:Lisdexamfetamine Dimesylate / Q000008:administration & dosage* / Q000097:blood / Q000737:chemistry; D008297:Male; D011355:Prodrugs / Q000008:administration & dosage* / Q000737:chemistry / Q000378:metabolism; D016896:Treatment Outcome
chemical_list: D000697:Central Nervous System Stimulants; D011355:Prodrugs; D000661:Amphetamine; D000069478:Lisdexamfetamine Dimesylate