IngentaConnect Extended-Release Methylphenidate (Ritalin LA)

Abstract:

utrif An extended-release formulation of methylphenidate (Ritalin® LA), a CNS stimulant that inhibits dopamine and noradrenaline (norepinephrine) reuptake into presynaptic neurons, has been developed for use in patients with attention deficit/hyperactivity disorder (ADHD).

utrif In children with ADHD and healthy male adults, extended-release methylphenidate 20mg was rapidly absorbed and demonstrated two distinct peak plasma concentrations 4 hours apart. The absorption pharmacokinetics of extended-release methylphenidate 20mg, which closely mimics those of immediate-release methylphenidate 10mg given in two doses 4 hours apart, permits once-daily administration.

utrif In a 2-week randomised, double-blind, placebo-controlled trial in 134 evaluable children aged 6 to 12 years with ADHD, symptoms improved to a significantly greater extent with extended-release methylphenidate 10 to 40mg once daily than with placebo.

utrif Extended-release methylphenidate improved both inattention and hyperactivity symptoms and was effective in children with combined- (inattentive and hyperactive/impulsive) type or predominantly inattentive-type ADHD.

utrif In clinical trials, the safety and tolerability profiles of extended-release methylphenidate were consistent with that of the immediate-release formulation.

Children with attention deficit/hyperactivity disorder (ADHD), the most extensively studied neurobehavioural disorder of childhood, show symptoms that include inattention, underperformance, hyperactivity and impulsiveness.This disorder, which presents in childhood and may continue through adolescence and adult life, may result in functional problems such as poor interpersonal relationships, difficulties in school and underachievement in careers. ADHD is effectively treated with stimulant medication (e.g. methylphenidate) and/or behaviour therapy. However, the short duration of action of immediate-release methylphenidate results in the drug often being administered two to three times daily, which may present problems with administration of the midday dose during school hours.

A number of formulations of extended-release methylphenidate are available; this review examines the use of a novel once-daily extended-release formulation of methylphenidate (Ritalin LA), hereafter referred to as extended-release methylphenidate, in the treatment of ADHD. This formulation uses a spheroidal oral drug absorption system (SODAS), which allows 50% of the drug (formulated as immediate-release beads) to be released immediately providing a rapid onset, and 50% (formulated as enteric-coated delayed-release beads) to be released 4 hours after administration. This mimics the twice-daily administration of immediate-release methylphenidate.