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*Efficacy and safety of stimulant therapy for attention deficit hyperactivity disorder (ADHD) has been well established.
*Major side effects of methylphenidate (MPH) therapy in ADHD are appetite disturbance, dizziness, stomach ache, headache and insomnia.
*Mild growth suppression appears to occur in continuous MPH use, although the ultimate effect on adult height is unknown.
*MPH therapy during childhood may be associated with decreased substance abuse in adolescence.
*MPH therapy is well tolerated in the epilepsy and Tourette syndrome populations.
*The formulations of MPH differ in the delivery pattern of the drug.
*The dopamine transporter 1, D4 dopamine receptor and intraneuronal vesicular trafficking of dopamine are all mechanisms through which MPH appears to exert a therapeutic effect.
*The body of extant and emerging literature supports stimulant therapy as a first-line treatment for ADHD.
Figure 1. Methylphenidate.
(Figure omitted. See article PDF.)
Attention deficit hyperactivity disorder (ADHD) remains the most prevalent neuro-psychiatric disorder diagnosed in children. Major impairment in multiple areas of life, a high incidence of psychiatric comorbidities and the persistence of symptoms into adulthood spur ongoing research into the mechanism and application of stimulant therapy, the most widely used modality for the treatment of this disorder. The efficacy of stimulant medication, including long-acting preparations, for children with ADHD in terms of classroom performance, social behavior and continuous performance tasks has been established for some time [1].
The efficacy and safety of long-acting stimulant formulations in the treatment of ADHD have been demonstrated, and the emergence of new delivery systems of methylphenidate (MPH), as well as extended release (ER) amphetamine products in recent years, has led to widespread use of these drugs in clinical practice. The use of newer formulations of MPH, including the isolated d -isomer, is expected to increase as greater experience is gained with the appropriate evaluation of ADHD, efficacy and dosing of medication, and management of side effects.
Chemical properties
MPH (α-phenyl-2-piperidineacetic acid) has a molecular weight of 233.31 and molecular formula of C14H19NO2 (Figure 1). MPH contains two chiral centers, resulting in two racemic pairs of four separate isomers, a D,L-erythro-MPH pair and a D,L-threo-MPH pair. The erythro racemate does not have a significant stimulant effect and has been linked to a higher incidence of adverse effects [2]. Most current commercial...