Lisdexamfetamine
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Lisdexamfetamine (dimesylate)
Vyvanse, Elvanse (EU)
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Summary
Common uses
Attention-deficit/hyperactivity disorder (FDA, ages 6+ and adult)0, Binge-eating disorder in adults (FDA)0
Pharmacy
Starting dose
ADHD: 30 mg PO once daily in the morning; titrate by 10-20 mg weekly to clinical effect. Binge-eating disorder: 30 mg/day, titrate to 50-70 mg/day
Preparations
Capsules 10, 20, 30, 40, 50, 60, 70 mg; chewable tablets 10, 20, 30, 40, 50, 60 mg
US FDA Max
70 mg/day
Pharmacology
Routes
Oral
Onset
1-2 hours (slower than immediate-release amphetamine because activation requires enzymatic cleavage in red blood cells)
Duration
10-12 hours (smoother profile than immediate-release amphetamine salts)
Half-life
Parent lisdexamfetamine <1 hour; dextroamphetamine 10-12 hours after release[1]
Bioavailability
~96% after red blood cell hydrolytic cleavage releases dextroamphetamine[1]
Pregnancy
Limited human data; the amphetamine class is associated with intrauterine growth restriction and neonatal withdrawal symptoms.[citation needed]
Legal status
Purported mechanism
Lisdexamfetamine is an inactive lysine-conjugated parent compound that requires enzymatic cleavage by red blood cell hydrolases to release active dextroamphetamine. The red-blood-cell-dependent conversion provides a slower, smoother release profile than immediate-release amphetamine salts, and is the basis of the abuse-deterrent design: IV administration bypasses the necessary RBC cleavage and produces no peak effect, and intranasal misuse offers little kinetic advantage over oral administration.0 Once converted, dextroamphetamine acts by displacing dopamine and norepinephrine from presynaptic vesicles via VMAT-2 and reversing DAT and NET transport, the shared mechanism of all amphetamine-class agents[1].
References
- ↑ 1.0 1.1 1.2 1.3 FDA Prescribing Information, Vyvanse (lisdexamfetamine dimesylate), Takeda/Shire, current revision. https://www.accessdata.fda.gov/drugsatfda_docs/label/2017/021977s045lbl.pdf