Methylphenidate is thought to block the reuptake of norepinephrine and dopamine into the presynaptic neuron and increase the release of these monoamines into the extraneuronal space. Methylphenidate is a racemic mixture comprised of the d- and l-isomers. The d-isomer is more pharmacologically active than the l-isomer.
藥動學
Plasma methylphenidate concentrations increase rapidly reaching an initial maximum at about 1 to 2 hours, total dose is released over 6-10 hrs. Concerta once daily minimizes the fluctuations between peak and trough concentrations associated with immediate-release methylphenidate three times daily. Methylphenidate is metabolized primarily by de-esterification to (alpha)-phenyl-piperidine acetic acid (PPA), which has little or no pharmacologic activity. The main urinary metabolite was PPA, accounting for approximately 80% of the dose. Elimination half-life: 3.5 hrs
禁忌症
Patients with marked anxiety, tension, and agitation; known to be hypersensitive to methylphenidate or other components of the product; glaucoma; patients with a family history or diagnosis of Tourette's syndrome; during treatment with monoamine oxidase (MAO) inhibitors such as selegiline, and also within a minimum of 14 days following discontinuation of a MAO inhibitor, may cause hypertensive crisis
Concerta is administered orally once daily and should be taken in the morning. Concerta must be swallowed whole with the aid of liquids, and must not be chewed, divided, or crushed. Concerta should not be used in patients under six years old. Dosage may be adjusted in 18 mg increments to a maximum of 54 mg/day in children and 72 mg/day in adolescents