Methylphenidate (MPH; MPD) is a psychostimulant drug approved for treatment of ADHD or attention-deficit hyperactivity disorder, postural orthostatic tachycardia syndrome and narcolepsy. It is better known by its 1948 trademarked name of Ritalin (original owner CIBA, now Novartis Corporation), was first licensed by the FDA in 1955 for treating ADHD, prescribed from 1960, and became heavily prescribed in the 1990s, when ADHD itself became more widely accepted.
ADHD and some other conditions are believed to be linked to sub-performance of the dopamine, norepinephrine, and glutamate processes in the brain responsible for self-regulation functions, leading to self-regulation disorders compromising the sufferer’s attention, self-control, behaviour, motivation, and executive function; methylphenidate primarily works by reducing the reuptake of dopamine and norepinephrine which improves the levels and utility of these neurotransmitters in the brain. Methylphenidate possesses some structural and pharmacological similarities to cocaine, though methylphenidate is less potent and longer in duration.
January 14, 2013
Pfizer Inc. today announced that Quillivant XR™ (methylphenidate hydrochloride) CII for extended-release oral suspension is now available in the U.S. for the treatment of attention deficit hyperactivity disorder (ADHD). Quillivant XR is the first once-daily, extended-release liquid methylphenidate for ADHD and is now available by prescription.
“We also recognize that caring for and treating a child with ADHD goes beyond medication. We look forward to working with mothers and other caregivers of children with ADHD to provide meaningful resources to the ADHD community.”
“In order to effectively treat patients with chronic conditions such as ADHD, it is important to consider individual patient needs, including options for medication administration,” said Ann Childress, M.D., president of the Center for Psychiatry and Behavioral Medicine, Las Vegas, who was an investigator in the Quillivant XR laboratory classroom study. “As the first once-daily, extended-release liquid medication for patients with ADHD, Quillivant XR represents a new alternative to other ADHD treatments.”
Quillivant XR was approved by the U.S. Food and Drug Administration (FDA) on September 27, 2012 for the treatment of ADHD in patients aged 6 years and above. The efficacy of Quillivant XR was evaluated in a randomized, double-blind, placebo-controlled, crossover, multicenter, laboratory classroom study of 45 children with ADHD. Quillivant XR significantly improved ADHD symptoms compared to placebo at the primary endpoint of four hours post-dose, and in a secondary analysis, showed significant improvement at every time point measured, from 45 minutes to 12 hours after dosing.
Four isomers of methylphenidate are known to exist. One pair of threo isomers and one pair of erythro are distinguished, from which only d-threo-methylphenidate exhibits the pharmacologically usually desired effects. When the drug was first introduced it was sold as a 3:1 mixture of erythro:threo diastereomers. The erythro diastereomers are also pressor amines. “TMP” is referring only to the threo product that does not contain any erythro diastereomers. Since the threo isomers are energetically favored, it is easy to epimerize out any of the undesired erythro isomers. The drug that contains only dextrorotary methylphenidate is called d-TMP. A review on the synthesis of enantiomerically pure (2R,2′R)-(+)-threo-methylphenidate hydrochloride has been published.
Methylphenidate preparation according to Jeffrey M. Axten et al. (1998)
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