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Drugs 2002Dexmethylphenidate comprises only the d-enantiomer (the pharmacologically effective isomer) of racemic methylphenidate and is indicated for the treatment of patients... (Review)
Review
Dexmethylphenidate comprises only the d-enantiomer (the pharmacologically effective isomer) of racemic methylphenidate and is indicated for the treatment of patients aged > or =6 years with attention deficit hyperactivity disorder (ADHD). In a 4-week, double-blind trial in 132 children with ADHD, significantly greater improvements from baseline in teacher-rated Swanson, Nolan and Pelham (SNAP)-ADHD scores were seen in dexmethylphenidate and methylphenidate recipients, compared with placebo recipients. In addition, significantly more dexmethylphenidate and methylphenidate recipients, compared with placebo recipients, were much improved or very much improved according to Clinical Global Impression-Improvement of Illness scale scores. In the same study, parent-rated SNAP-ADHD scores had decreased by a significantly greater extent in dexmethylphenidate recipients at 3pm and 6pm and in methylphenidate recipients at 3pm, compared with placebo recipients. Significantly fewer dexmethylphenidate than placebo recipients failed treatment in a double-blind, treatment-withdrawal trial in 75 children with ADHD (17.1 vs 61.5%). In a noncomparative study in 22 children with ADHD, symptoms of ADHD, as assessed by teachers and parents, were controlled during the entire school day in 68 and 86% of dexmethylphenidate recipients, respectively, with a median duration of effect of 6.3 and 7.5 hours, respectively. Dexmethylphenidate was generally well tolerated in children with ADHD; adverse events were consistent with those known to be associated with agents containing methylphenidate.
Topics: Absorption; Attention Deficit Disorder with Hyperactivity; Child; Dexmethylphenidate Hydrochloride; Dopamine Uptake Inhibitors; Female; Humans; Male; Methylphenidate; Randomized Controlled Trials as Topic; Stereoisomerism; Treatment Outcome
PubMed: 12215063
DOI: 10.2165/00003495-200262130-00009 -
Expert Review of Neurotherapeutics Jul 2005Medications for attention deficit hyperactivity disorder (ADHD) currently represent the ninth largest segment of the CNS market by sales, with 2.4 billion USD spent... (Review)
Review
Medications for attention deficit hyperactivity disorder (ADHD) currently represent the ninth largest segment of the CNS market by sales, with 2.4 billion USD spent annually on this condition and 40% annual growth. Stimulant medications remain the most effective ADHD therapies and provide robust improvement in ADHD symptoms in both youth and adults. Current prescribing practices favor extended release preparations due to increased convenience, compliance and tolerability with once-daily dosing. Dexmethylphenidate extended release is a long-acting preparation of the ADHD medication Focalin (dexmethylphenidate immediate release) and was approved for marketing by the US Food and Drug administration in June 2005. Dexmethylphenidate consists of the single dextro-isomer form of d,l-methylphenidate commonly marketed as Ritalin. Dexmethylphenidate extended release utilizes spheroidal oral drug absorption system technology to achieve a 50% immediate medication delivery and 50% delayed release of dexmethylphenidate approximately 4 h after ingestion. Placebo-controlled, clinical trials in children and adults with ADHD have demonstrated efficacy for behavioral and academic ratings, with an analog classroom study showing medication effects up to 12 h after dosing. Dexmethylphenidate extended release was generally well tolerated with a side-effect profile similar to other stimulants. The most common reported side effects include diminished appetite and insomnia. Given its duration of effect, favorable tolerability and flexibility in dosing, dexmethylphenidate extended release is likely to gain considerable use as an ADHD treatment.
Topics: Animals; Attention Deficit Disorder with Hyperactivity; Capsules; Delayed-Action Preparations; Dexmethylphenidate Hydrochloride; Humans; Methylphenidate
PubMed: 16026226
DOI: 10.1586/14737175.5.4.437 -
Expert Opinion on Pharmacotherapy 2023Attention deficit/hyperactivity disorder (ADHD) is a common behavioral disorder which is best treated through a combination of medication and behavioral therapy, with... (Review)
Review
INTRODUCTION
Attention deficit/hyperactivity disorder (ADHD) is a common behavioral disorder which is best treated through a combination of medication and behavioral therapy, with stimulant medications serving as a first-line treatment approach. Serdexmethylphenidate (SDX), a prodrug of dexmethylphenidate (d-MPH), a commonly utilized stimulant medication, has recently received approval and is marketed in the U.S.A.
AREAS COVERED
This review summarizes peer-reviewed literature on SDX published between 2021-2023 and a review of data available from ClinicalTrials.gov.
EXPERT OPINION
SDX represents a new option for treatment for ADHD. It is unique in its prodrug design and achieves a relatively extended duration of action in comparison to other stimulant formulations. Although the research is relatively limited thus far, early data suggests it to be a safe medication to consider with side effects being similar to other stimulant medications. Its prodrug design is useful in potentially serving as a deterrent to intentional parenteral abuse and its ability to be opened and sprinkled makes it an option for those individuals with ADHD who might be unable to swallow pills.
Topics: Humans; Attention Deficit Disorder with Hyperactivity; Central Nervous System Stimulants; Dexmethylphenidate Hydrochloride; Prodrugs; Methylphenidate
PubMed: 37226489
DOI: 10.1080/14656566.2023.2218544 -
American Journal of Health-system... Jul 2014Current literature on the safety and efficacy of various intermediate- and long-acting preparations of methylphenidate and dexmethylphenidate for pediatric... (Review)
Review
PURPOSE
Current literature on the safety and efficacy of various intermediate- and long-acting preparations of methylphenidate and dexmethylphenidate for pediatric attention-deficit/hyperactivity disorder (ADHD) is reviewed.
SUMMARY
The efficacy of methylphenidate in controlling ADHD symptoms is firmly established. Given the drug's relatively short half-life in pediatric patients (about 2.5 hours), a number of intermediate- and long-acting products have been developed; these extended-release methylphenidate products provide the same efficacy as immediate-release (IR) formulations, with the convenience of less frequent dosing. Intermediate-acting methylphenidate preparations have effects lasting as long as 8 hours, but peak concentrations are not attained for up to 5 hours, and many patients may require twice-daily dosing. Long-acting methylphenidate products developed to address these challenges include a controlled-release tablet and bimodal-delivery capsules containing mixtures of IR and extended-release beads (durations of effect, 8-12 hours). Options for patients with difficulty swallowing tablets or capsules include a once-daily transdermal delivery system and a once-daily liquid formulation. Dexmethylphenidate (the more pharmacologically active d-isomer of racemic methylphenidate) can provide efficacy comparable to that of IR methylphenidate at half the dose; an extended-release form of dexmethylphenidate can provide less fluctuation in peak and trough concentrations than the IR form. Methylphenidate and dexmethylphenidate products in capsule form can be opened and sprinkled on applesauce.
CONCLUSION
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. All are equally efficacious in controlling ADHD symptoms.
Topics: Attention Deficit Disorder with Hyperactivity; Capsules; Central Nervous System Stimulants; Child; Delayed-Action Preparations; Dexmethylphenidate Hydrochloride; Humans; Methylphenidate; Tablets
PubMed: 24973373
DOI: 10.2146/ajhp130638 -
CNS Drugs Dec 2009Dexmethylphenidate extended release (XR) [Focalin XR] is a CNS stimulant indicated for the treatment of attention-deficit hyperactivity disorder (ADHD) in patients aged... (Review)
Review
Dexmethylphenidate extended release (XR) [Focalin XR] is a CNS stimulant indicated for the treatment of attention-deficit hyperactivity disorder (ADHD) in patients aged > or = 6 years. Dexmethylphenidate contains the d-threo-enantiomer of methylphenidate. Dexmethylphenidate XR capsules have a bimodal release profile, which mimics two doses of dexmethylphenidate immediate release (IR) given 4 hours apart, and allows once-daily administration. Once-daily dexmethylphenidate XR was effective and generally well tolerated in the treatment of ADHD in children, adolescents and adults in placebo-controlled trials. Improvements in ADHD symptoms were significantly greater for dexmethylphenidate XR versus placebo throughout the day, from as early as 0.5 hours after drug administration up to 11-12 hours after administration. Furthermore, dexmethylphenidate XR showed greater efficacy than osmotic release oral system (OROS) methylphenidate over the first half of the laboratory classroom day in crossover trials; however, assessments late in the day (10-12 hours post-dose) favoured OROS methylphenidate. The once-daily administration regimen with dexmethylphenidate XR avoids the need for a midday dose to be administered at school; administration options are extended in that the contents of the dexmethylphenidate XR capsule can be sprinkled on apple sauce for patients unable to swallow the capsule whole. Although dexmethylphenidate XR is a controlled substance in the US, this formulation appears to have a low risk of abuse or misuse. Thus, dexmethylphenidate XR extends the range of first-line pharmacological treatment options for children, adolescents or adults with ADHD, particularly for patients who require a rapid onset and prolonged duration of action, including children who require a reduction in ADHD symptoms throughout the school day.
Topics: Adolescent; Adult; Attention Deficit Disorder with Hyperactivity; Central Nervous System Stimulants; Child; Clinical Trials as Topic; Delayed-Action Preparations; Dexmethylphenidate Hydrochloride; Dose-Response Relationship, Drug; Drug Interactions; Humans; Methylphenidate; Psychiatric Status Rating Scales; Severity of Illness Index
PubMed: 19958043
DOI: 10.2165/11201140-000000000-00000 -
The Medical Letter on Drugs and... Oct 2021
Topics: Attention Deficit Disorder with Hyperactivity; Central Nervous System Stimulants; Child; Double-Blind Method; Drug Approval; Drug Combinations; Drug Interactions; Humans; Methylphenidate; Randomized Controlled Trials as Topic; United States; United States Food and Drug Administration
PubMed: 34550957
DOI: No ID Found -
Frontiers in Psychiatry 2023Sleep-related problems are common in children with attention-deficit/hyperactivity disorder (ADHD). Sleep disorders are also side effects of all stimulant ADHD...
INTRODUCTION
Sleep-related problems are common in children with attention-deficit/hyperactivity disorder (ADHD). Sleep disorders are also side effects of all stimulant ADHD medications. Serdexmethylphenidate/dexmethylphenidate (SDX/d-MPH) is a once-daily treatment approved for patients age 6 years and older with ADHD. In this analysis, sleep behavior was assessed during SDX/d-MPH treatment in children with ADHD.
METHODS
In a 12-month, dose-optimized, open-label safety study in 6- to 12-year-old participants (NCT03460652), a secondary endpoint was assessment of sleep behavior based on the Children's Sleep Habits Questionnaire (CSHQ) consisting of 8 sleep domains (bedtime resistance, sleep onset delay, sleep duration, sleep anxiety, night wakings, parasomnias, sleep-disordered breathing, and daytime sleepiness). This analysis examined the individual sleep domains in the 12-month safety study.
RESULTS
Of 282 participants enrolled, 238 were included in the sleep analysis. At baseline, mean (SD) CSHQ total sleep disturbance score was 53.4 (5.9). After 1 month of treatment, the mean (SD) CSHQ total score significantly decreased to 50.5 (5.4); least-squares mean change from baseline was -2.9 (95% CI: -3.5 to -2.4; < 0.0001) and remained decreased up to 12 months. Mean sleep-score improvements from baseline to 12 months were statistically significant ( < 0.0001) for 5 of 8 sleep domains, including bedtime resistance, sleep anxiety, night wakings, parasomnias, and daytime sleepiness. Parasomnias and daytime sleepiness sleep domains showed the greatest mean improvement from baseline to 12 months. Sleep onset delay and sleep duration scores increased from baseline to 12 months. No statistically significant worsening occurred from baseline in sleep duration and sleep-disordered breathing domains; however, worsening of sleep onset delay was statistically significant.
CONCLUSION
In this analysis of children taking SDX/d-MPH for ADHD, sleep problems did not worsen based on the mean CSHQ total sleep disturbance score. Statistically significant improvements in most CSHQ sleep domains were observed after 1 month and lasted for up to 12 months of treatment.
PubMed: 37426086
DOI: 10.3389/fpsyt.2023.1193455 -
Cureus Aug 2022Rhabdomyolysis secondary to prescription drug-drug interactions can be an overlooked life-threatening emergency. Amphetamines and similar substances have been...
Rhabdomyolysis secondary to prescription drug-drug interactions can be an overlooked life-threatening emergency. Amphetamines and similar substances have been associated with muscle lysis secondary to increased sympathetic activity that can cause myotoxicity, hyperthermia, and increased muscular activity. Anabolic steroids may also be a predisposing factor in developing rhabdomyolysis. A high index of suspicion for drug-induced rhabdomyolysis in a patient presenting with atraumatic extremity pain can facilitate rapid diagnosis and treatment. We present a case of drug-induced rhabdomyolysis likely secondary to a previously unreported medication interaction.
PubMed: 36134084
DOI: 10.7759/cureus.27988 -
Drugs in R&D 2002Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin].... (Review)
Review
Celgene has developed a chirally pure form of methylphenidate (Ritalin), called dexmethylphenidate [d-methylphenidate, d-methylphenidate hydrochloride, d-MPH; Focalin]. The drug has been launched in the USA and is undergoing registration in Canada for the treatment of children with attention-deficit hyperactivity disorder (ADHD). Dexmethylphenidate is the single isomer version of racemic methylphenidate (Ritalin), which contains the active d isomer of Ritalin. Dexmethylphenidate acts via the inhibition of reuptake of norepinephrine and dopamine. Research is ongoing to further clarify the mode of therapeutic action in ADHD. Dexmethylphenidate was developed with the aim of reducing drug load, adverse events and drug interactions. Dexmethylphenidate provides effective management of attention-deficit hyperactivity disorder at half the dose of Ritalin. In April 2000, worldwide rights (excluding Canada) to dexmethylphenidate were granted to Novartis. Celgene has also granted Novartis rights to all related intellectual properties and patents. Novartis will fund all remaining development and marketing expenses required for regulatory approval and commercialisation of dexmethylphenidate. Crystaal Corporation, the marketing division of Biovail Corporation International, has exclusive Canadian marketing rights for all formulations of dexmethylphenidate. Novartis launched dexmethylphenidate (Focalin) in the USA during Q1 2002. It is available as a D-shaped tablet (2.5, 5 and 10 mg doses). Novartis had planned to use the tradename Ritadex, however the FDA recommended an alternative name due to potential prescribing errors with Ritalin. The finalized tradename to be used is Focalin. In July 2001, a new drug submission was filed with Canada's Therapeutic Products Programme for dexmethylphenidate in the treatment of attention-deficit disorder and attention-deficit hyperactivity disorder. Novartis is also developing an extended-release version of chirally pure dexmethylphenidate. Dexmethylphenidate has been found to be effective and well tolerated in clinical trials, involving a total of 684 children with ADHD and in 15 healthy adult volunteers. Dexmethylphenidate is a schedule II drug.
Topics: Attention Deficit Disorder with Hyperactivity; Clinical Trials as Topic; Dexmethylphenidate Hydrochloride; Dopamine Uptake Inhibitors; Humans; Methylphenidate; Norepinephrine
PubMed: 12455205
DOI: 10.2165/00126839-200203040-00010