Comparative Pharmacology
Head-to-head clinical analysis: CONCERTA versus XELSTRYM.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CONCERTA versus XELSTRYM.
CONCERTA vs XELSTRYM
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.
XELSTRYM (dextroamphetamine transdermal system) is a sympathomimetic amine that increases synaptic concentrations of dopamine and norepinephrine by inhibiting their reuptake and promoting their release from presynaptic terminals.
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.
Initial: one 9-mg patch applied to the hip once daily; titrate weekly in 4.5-mg increments to desired effect; maximum dose: 18 mg/day.
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.
Mean terminal elimination half-life of dexmethylphenidate is approximately 2-3 hours in children and adolescents, with no significant accumulation at steady state; clinical effects correlate with plasma concentrations.
Primarily renal (77%-87% as unchanged drug and metabolites); metabolic elimination accounts for 13%-23%, with minor biliary excretion (<2%).
Renal (90% as unchanged drug and metabolites, primarily dehydrodexmethylphenidate and inactive metabolites); minor biliary/fecal elimination (<5%)
Category C
Category C
CNS Stimulant
CNS Stimulant