Comparative Pharmacology
Head-to-head clinical analysis: CONCERTA versus DEXAMPEX.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CONCERTA versus DEXAMPEX.
CONCERTA vs DEXAMPEX
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.
Dextroamphetamine is a central nervous system stimulant that increases extracellular dopamine and norepinephrine levels by blocking their reuptake and promoting 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.
5-10 mg orally once daily in the morning, maximum 20 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.
Terminal elimination half-life 10–13 hours in adults (7–8 hours in children). Longer in alkaline urine (up to 20 hours) due to reduced renal tubular reabsorption.
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 deaminated metabolites); fecal/biliary <2%.
Category C
Category C
CNS Stimulant
CNS Stimulant