Comparative Pharmacology
Head-to-head clinical analysis: CONCERTA versus METHYLIN.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CONCERTA versus METHYLIN.
CONCERTA vs METHYLIN
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.
Methylphenidate is a central nervous system stimulant. It blocks the reuptake of dopamine and norepinephrine into presynaptic neurons, increasing their concentrations in the synaptic cleft.
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.
10 mg orally twice daily, administered 4-6 hours apart; doses may be adjusted in 5-10 mg increments weekly up to 60 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.
2-4 hours (short elimination half-life, requiring multiple daily dosing; immediate-release: 3-4 hours, extended-release: 3-6 hours)
Primarily renal (77%-87% as unchanged drug and metabolites); metabolic elimination accounts for 13%-23%, with minor biliary excretion (<2%).
Renal: 90% (mainly as metabolites, 30-50% as unchanged drug); fecal: <1%
Category C
Category C
CNS Stimulant
CNS Stimulant