Mechanism and Pharmacokinetics of Concerta

Mechanism of Action and Pharmacokinetic Profile

The American Academy of Neurology and other medical societies support the fact that, by enhancing dopamine and norepinephrine signaling, methylphenidate increases the efficiency of prefrontal cortex activity and optimizes executive and attentional function 1
Additional mechanisms of Concerta include agonist activity at the serotonin type 1A receptor and redistribution of the vesicular monoamine transporter 2 1

The American Academy of Pediatrics and other medical organizations note that Concerta provides 10 to 12 hours of continuous symptom control after a single morning dose, with the 18 mg dose being approximately equivalent to methylphenidate 5 mg three times daily 2
For patients requiring coverage beyond 12 hours, short-acting stimulant boosters can be added in late afternoon, though timing is critical to avoid insomnia 2
Individual response to methylphenidate formulations is idiosyncratic, with approximately 40% of patients responding to both methylphenidate and amphetamine, and 40% responding to only one 2