Small molecule
PubChem CID 4158
Methylphenidate
Concerta
- Mechanism of action
- CNS stimulant, blocks dopamine and norepinephrine reuptake
- In plain language
- Blocks the tiny transporters in the brain that normally reabsorb dopamine and norepinephrine, leaving more of these focus-and-alertness chemicals active between nerve cells, which helps improve attention and reduce hyperactivity in ADHD.
- How it works
- Methylphenidate (Concerta) is a central nervous system (CNS) stimulant. Per the FDA label, methylphenidate blocks the reuptake of norepinephrine and dopamine into the presynaptic neuron and increases the release of these monoamines into the extraneuronal space; the mode of therapeutic action in the treatment of ADHD is not known. Concerta uses an osmotic extended-release delivery system that produces an ascending plasma methylphenidate concentration profile over roughly 6 to 10 hours after an initial peak, minimizing the peak-to-trough fluctuations seen with immediate-release methylphenidate dosed three times daily.
- Therapeutic applications
- Methylphenidate (Concerta) is FDA-indicated for the treatment of attention deficit hyperactivity disorder (ADHD) in patients aged 6 to 65 years old; its use is not recommended in pediatric patients younger than 6 years of age, who showed higher plasma exposure and a higher incidence of adverse reactions at the same dosage. It carries a boxed warning: Concerta contains methylphenidate, a Schedule II controlled substance with a high potential for abuse and misuse that can lead to a substance use disorder, including addiction, and misuse or abuse of CNS stimulants can result in overdose and death.
- Class
- Small molecule
- Therapeutic area
- CNS / Psychiatric
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