Latest research on Lisdexamfetamine

Lisdexamfetamine (L-lysine-d-amphetamine) is a prodrug of the psychostimulant d-amphetamine coupled with the essential amino acid L-lysine. It was developed so that the amphetamine psychostimulant is released and activated more slowly as the prodrug molecule is hydrolyzed consequently cleaving off the amino acid-during the first pass through the intestines and/or the liver. Amphetamines target the trace amine-associated receptor 1 (TAAR1). Amphetamine is also believed to exert its effects by binding to the monoamine transporters (the dopamine transporter or DAT) and increasing extracellular levels of the biogenic amines dopamine, norepinephrine (noradrenaline) and serotonin.

Latest findings

Specifically, Adderall XR® (Amphetamine mixed salts [MAS-XR]; Shire Canada Inc.), Concerta® (Methylphenidate HCl extended release [OROS-MPH]; Janssen Inc., Toronto, ON, Canada) and generic, Biphentin® (Methylphenidate HCl controlled release [MPH-CR]; Purdue Pharma, Pickering, ON, Canada) and Vyvanse® (Lisdexamfetamine dimesylate [LDX]; Shire Canada Inc.) are available in Canada for the treatment of ADHD [18, 19]. [source, 2016]
Of these, the most common were Humira with 5 unique ads and Cymbalta and Vyvanse with 3 unique ads each. [source, 2016]
Of the 50 (51.5%) participants who were being treated with medication for their ADHD symptoms, 6 received Ritalin, 17 received Concerta, 11 received Vyvanse, 9 received Adderal, 3 received Dexadrine, 3 received Stratterra and 1 received another medication. [source, 2015]
Data from a pooled sample of children and adolescent patients (n = 2357), aged 6–17 years, with a confirmed Statistical Manual of Mental Disorders version IV text revision (DSM-IV-TR) primary diagnosis of ADHD, who participated in one of seven Phase III randomized, double-blind, placebo-controlled trials of Guanfacine hydrochloride extended-release (GXR; Intuniv, Shire US, Inc., Wayne, Pennsylvania, USA) or Lisdexamfetamine dimesylate (Vyvanse, Shire US, Inc.) [27–33]. [source, 2015]
One proof-of-concept trial showed Lisdexamfetamine dimesylate add-on to Escitalopram to be more effective than placebo in treating depressive residual symptoms [83]. [source, 2015]
In contrast to Lisdexamfetamine, the prodrug Phendimetrazine displayed a clockwise hysteresis loop (data reanalyzed from Banks et al., 2013c), which suggests that Phendimetrazine is an active parent drug for an active metabolite. [source, 2015]
Overall, these differential hysteresis effects between the prodrugs Lisdexamfetamine and Phendimetrazine are consistent with the differential onsets of cocaine-appropriate responses produced by these two compounds in the cocaine discrimination procedure. [source, 2015]
Said another way, the cocaine-like discriminative stimulus effects of Lisdexamfetamine are mediated exclusively by the conversion of Lisdexamfetamine to d-amphetamine; in contrast, both the parent drug Phendimetrazine and the active metabolite phenmetrazine contribute to the cocaine-like effects of Phendimetrazine. [source, 2015]
The present study extends these previous findings by showing that chronic 7-day treatment with Lisdexamfetamine also produced a dose-dependent rightward shift in the Cocaine choice dose-effect curve. [source, 2015]
Insofar as reductions in Cocaine choice by chronic d-amphetamine treatment in monkeys are consistent with clinical effectiveness of amphetamine maintenance to reduce Cocaine use (Grabowski et al., 2001; Mariani et al., 2012), these results suggest that Lisdexamfetamine may also be clinically effective to reduce Cocaine use. [source, 2015]