New methylphenidate formulations for the treatment of attention-deficit/hyperactivity disorder

  title={New methylphenidate formulations for the treatment of attention-deficit/hyperactivity disorder},
  author={Kennerly Sexton Patrick and Mario A. Gonz{\'a}lez and Arthur B. Straughn and John Seth Markowitz},
  journal={Expert Opinion on Drug Delivery},
  pages={121 - 143}
dl-Methylphenidate (MPH) remains the most widely used pharmacological agent in the treatment of attention-deficit/hyperactivity disorder (ADHD). The predominantly dopaminergic mechanism of the psychostimulant actions has become more clearly defined. Neuroimaging and genetic studies are revealing the underlying neuropathology in ADHD. Novel extended-release (ER) MPH formulations now offer drug delivery options to overcome both the short-term actions of immediate-release (IR) MPH and the acute… 

Comparison of the pharmacokinetics and clinical efficacy of new extended-release formulations of methylphenidate

  • R. Maldonado
  • Medicine, Biology
    Expert opinion on drug metabolism & toxicology
  • 2013
This review focuses on the pharmacokinetics of ER MPH formulations (Concerta, Equasym XL/Metadate CD, Medikinet Retard and Ritalin LA) and attempts to align the properties of each agent with available clinical findings in children/adolescents with ADHD.

OROS methylphenidate for the treatment of adults with attention-deficit/hyperactivity disorder

Evidence from various clinical studies assessing the efficacy and safety of OROS-MPH in different clinical samples of adults with ADHD, including samples with the most common comorbidities found in ADHD patients are summarized.

Dexmethylphenidate hydrochloride in the treatment of attention deficit hyperactivity disorder

This paper reviews and summarizes the available research literature on d-MPH regarding pharmacodynamic, pharmacokinetic, chemical structure, receptor binding, toxicology, and clinical perspectives and potentially may offer some advantages in the realms of absorption and duration of action compared with its racemic counterpart.

Methylphenidate for attention-deficit/hyperactivity disorder in adults: a narrative review

There is substantial body of evidence to suggest that MPH is an effective and safe treatment option for adults with ADHD.

Methylphenidate and dexmethylphenidate formulations for children with attention-deficit/hyperactivity disorder.

  • D. SugrueR. BognerM. Ehret
  • Medicine
    American journal of health-system pharmacy : AJHP : official journal of the American Society of Health-System Pharmacists
  • 2014
The various formulations of IR and intermediate- and extended-release methylphenidate and dexmethylphenidate can be useful options in satisfying patients' individual needs in the management of ADHD.

Stimulants and Other Non-stimulants for Attention-Deficit/Hyperactivity Disorder (ADHD)

The pharmacodynamic benefits and adverse effects of methylphenidate, amphetamines, and atomoxetine may be linked to their pharmacokinetic profiles.

Isopropylphenidate: an ester homolog of methylphenidate with sustained and selective dopaminergic activity and reduced drug interaction liability.

IPH displayed unique pharmacological characteristics including greater DAT than NET binding and cellular uptake activity, and greater resistance to hydrolysis and transesterification via carboxylesterase 1 relative to MPH.

An update on the pharmacokinetic considerations in the treatment of ADHD with long-acting methylphenidate and amphetamine formulations

Since there are no reliable biomarkers that can predict individualized response to long-acting stimulants, clinicians need to consider their distinctive pharmacokinetic properties, including the pharmacokinetics profile, rate and extent of absorption, variability, dose proportionality, bioequivalence and potential for accumulation.

Cognitive and behavioral effects of multilayer-release methylphenidate in the treatment of children with attention-deficit/hyperactivity disorder.

MLR MPH given once daily produces equivalent improvements in behavioral and cognitive measures, and has a duration of effect at least as long as that of IR MPH given twice daily.

Differential pharmacokinetics and pharmacodynamics of methylphenidate enantiomers: does chirality matter?

Data from in vitro, animal, and human studies support the premise that the d-enantiomer of MPH mediates the neurophysiological actions of MPH and therefore likely mediates its clinical efficacy.



Advances in the Pharmacotherapy of Attention‐Deficit‐Hyperactivity Disorder: Focus on Methylphenidate Formulations

The psychostimulant dl‐methylphenidate (MPH) remains the most common drug therapy in child and adolescent psychiatry for the treatment of attention‐deficit‐hyperactivity disorder (ADHD). Evidence of

Pharmacokinetic Considerations in the Treatment of Attention-Deficit Hyperactivity Disorder with Methylphenidate

The difficulties in administering methylphenidate multiple times a day, particularly during the school day, have been alleviated in the past few years by the development of extended-release preparations with varying behavioural effects lasting 8–12 hours.

Pharmacology of methylphenidate, amphetamine enantiomers and pemoline in attention‐deficit hyperactivity disorder

Methylphenidate appears to produce psychostimulation by inhibiting the presynaptic uptake of impulse‐released dopamine, and pemoline appears to both release and block the uptake of dopamine.

Mechanism of action of methylphenidate: Insights from PET imaging studies

It is postulate that MPH-induced increases In DA could improve attention and decrease distractibility; and that since DA modulates motivation, the increases in DA would also enhance the saliency of the task facilitating the “interest it elicits” and thus improving performance.

A comparison of once-daily extended-release methylphenidate formulations in children with attention-deficit/hyperactivity disorder in the laboratory school (the Comacs Study).

Large, statistically significant main effects for the within-subject factor of treatment for all 3 outcome measures (deportment, attention, and permanent product) were revealed and clinical superiority is expected at any point in time for the formulation with the highest MPH plasma concentration.

Variables that affect the clinical use and abuse of methylphenidate in the treatment of ADHD.

The characteristics of clinical use (low doses administered orally and titrated for therapeutic effects) constrain methylphenidate's abuse.

Comparative Efficacy of Adderall and Methylphenidate in Attention-deficit/Hyperactivity Disorder: A Meta-Analysis

Data from the four available studies suggest that Adderall has a small but statistically significant advantage over the standard-release form of methylphenidate.

Pharmacokinetic and pharmacodynamic properties of stimulants: implications for the design of new treatments for ADHD

Psychopharmacology of attention deficit disorder: pharmacokinetic, neuroendocrine, and behavioral measures following acute and chronic treatment with methylphenidate.

The concentration of MPH in single "spot" samples obtained at two to three hours after administration of medication were significantly correlated with the percentage of improvement in the abbreviated Conners rating scale, indicating a relationship between plasma MPH concentration and clinical response.

Sustained release methylphenidate: pharmacokinetic studies in ADDH males.

Comparisons of the two sets of plasma concentration curves suggest that MPH-SR has a longer Tmax, but that it does not reach the same Cmax as an identical dose of standard MPH.