Comparative Pharmacology
Head-to-head clinical analysis: CONCERTA versus LISDEXAMFETAMINE DIMESYLATE.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CONCERTA versus LISDEXAMFETAMINE DIMESYLATE.
CONCERTA vs LISDEXAMFETAMINE DIMESYLATE
Comparing the clinical profiles, pharmacokinetic behaviors, and safety indices of these two therapeutic agents.
Methylphenidate is a central nervous system (CNS) stimulant. It blocks the reuptake of norepinephrine and dopamine into presynaptic neurons, increasing their levels in the synaptic cleft. It also acts as a dopamine agonist by stimulating the release of dopamine from storage sites.
Lisdexamfetamine is a prodrug of dextroamphetamine, which blocks the reuptake of norepinephrine and dopamine from the synaptic cleft and increases their release into the extraneuronal space.
18-72 mg orally once daily in the morning, starting at 18-36 mg/day and titrating in 18 mg increments weekly; maximum 72 mg/day.
30–70 mg orally once daily in the morning.
None Documented
None Documented
Terminal elimination half-life of methylphenidate from CONCERTA is approximately 3.5 hours (range 2.5-5.5 hours) in adults; in children, mean half-life is 3-4 hours. The extended-release formulation provides a prolonged clinical effect due to the OROS delivery system, not prolonged half-life.
Terminal elimination half-life of lisdexamfetamine is approximately 1 hour (prodrug conversion), while dextroamphetamine (active moiety) has a half-life of 10-12 hours in adults. In children, half-life is slightly shorter (9-11 hours). Clinically, once-daily dosing provides symptom control for ADHD.
Primarily renal (77%-87% as unchanged drug and metabolites); metabolic elimination accounts for 13%-23%, with minor biliary excretion (<2%).
Primarily renal: approximately 95% of the dose is excreted in urine, with about 70% as intact lisdexamfetamine, 20% as dextroamphetamine and its metabolites (hippuric acid, benzoic acid), and minimal biliary/fecal elimination (<5%).
Category C
Category C
CNS Stimulant
CNS Stimulant