Comparative Pharmacology
Head-to-head clinical analysis: CONCERTA versus CYLERT.
Peer-Reviewed Evidence
Head-to-head clinical analysis: CONCERTA versus CYLERT.
CONCERTA vs CYLERT
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.
CNS stimulant; increases extracellular dopamine and norepinephrine levels by blocking their reuptake and enhancing release.
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.
37.5 mg orally once daily in the morning; may increase by 18.75 mg weekly to a maximum of 112.5 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 is 12-30 hours in children (mean 19 hours) and 8-14 hours in adults; the long half-life supports once-daily dosing, but accumulation can occur with repeated dosing
Primarily renal (77%-87% as unchanged drug and metabolites); metabolic elimination accounts for 13%-23%, with minor biliary excretion (<2%).
Primarily renal (80-90% as unchanged drug and metabolites, with 50-60% as unchanged pemoline), minor biliary/fecal elimination (<10%)
Category C
Category C
CNS Stimulant
CNS Stimulant