Dexmethylphenidate (Focalin) is central nervous system stimulant drug containing only the pharmacologically effective isomer (d-enantiomer) of racemic methylphenidate (Ritalin, Concerta). Dexmethylphenidate is prescribed for the treatment of ADHD in adults and children over the age of 6. Because dexmethylphenidate contains only the active isomer of methylphenidate its dosage is half that of methylphenidate (Ritalin, Concerta).
Introduction to Dexmethylphenidate
Dexmethylphenidate (Focalin) is central nervous system stimulant drug containing only the pharmacologically effective isomer (d-enantiomer) of racemic methylphenidate (Ritalin, Concerta). Dexmethylphenidate has been shown safe and effective for treatment of ADHD in adults and children over the age of 6 in both immediate release and extended release formulations. [1] [2] Dexmethylphenidate is available as 2.5, 5 and 10mg immediate release (IR) tablets and 5 mg, 10 mg, 15mg, and 20mg extended release (XR) capsules.
Using Dexmethylphenidate
Ways of Administration
Dose
Column 1 Column 2 Threshold mg Light mg Medium mg Strong mg
In patients with ADHD who are not currently receiving methylphenidate, or are receiving other stimulants, treatment with dexmethylphenidate is normally started at 2.5mg twice daily and increased weekly as needed by 2.5 to 5mg increments to a 20mg maximum daily dose.
In patients who are currently receiving methylphenidate, dexmethylphenidate is normally started at a dosage of half that of methylphenidate which can be increased as needed to a maximum of 20 mg/day.Effects of Dexmethylphenidate
Combinations with Dexmethylphenidate
Different Uses for Dexmethylphenidate
Recreational use of Dexmethylphenidate
Using Dexmethylphenidate for ...
Using Dexmethylphenidate for ...
Pharmacology of Dexmethylphenidate
General
Dexmethylphenidate is thought to block dopamine and norepinephrine reuptake into the presynaptic neuron and increase norepinephrine and dopamine release into the extraneuronal space. Dexmethylphenidate is metabolised by de-esterification to its primary metabolite, d-α-phenyl-piperidine acetic acid (d-ritalinic acid), which has negligible pharmacological activity. Dexmethylphenidate did not have an inhibitory effect on cytochrome P450 isoenzymes in in vitro studies. Dexmethylphenidate has a mean elimination half-life of approximately 2.2 hours.Targets, Enzymes, and Transporters
Targets
Enzymes
Transporters
Chemistry of Dexmethylphenidate
Systematic(IUPAC) name: ([alpha]R,2R)-[alpha]-Phenyl-2-piperidine-acetic acid methyl ester Synonyms: Focalin (hydrochloride) Molecular Formula: C14H19NO2 Molar mass: 233.31 g/mol, 269.77 g/mol (hydrochloride) CAS Registry Number: 40431-64-9, 19262-68-1 (hydrochloride) Melting Point: 224-226°C (hydrochloride) Boiling Point: 135-137°C @ 0.6 mmHg Flash Point: no data Solubility: Hydrochloride freely soluble in water, methanol. Soluble in alcohol. Slightly soluble in acetone, chloroform. Additionnal data: pKa 8.9 Notes: Hydrochloride aspect : white to off white powder [/center]
Reagent test results of Dexmethylphenidate
The Dangers of Dexmethylphenidate
General Warnings
Dexmethylphenidate poses a risk of dependence and addiction, especially for people with a history of drug or alcohol dependence or addiction. Abusive use can lead to tolerance and psychological dependence and withdrawal symptoms if use is stopped, particularly abruptly. Careful supervision is required during withdrawal from abusive use, since severe depression may occur.
Side Effects and Interactions
Potential Side Effects
Dexmethylphenidate may aggravate symptoms in patients with marked anxiety, tension, and agitation.
Dexmethylphenidate causes minor side effects including stomach pain, loss of appetite, nausea, vomiting, heartburn, weight loss, dry mouth, difficulty falling or staying asleep, dizziness, drowsiness, nervousness or jitteriness, headache. Tell your doctor if any of these symptoms are severe or do not go away.
Serious side effects are also possible. If you experience any of the following symptoms, call your doctor immediately: fast, pounding, or irregular heartbeat, chest pain, shortness of breath, excessive tiredness, slow or difficult speech, dizziness or faintness, weakness or numbness of an arm or leg, changes in vision or blurred vision, seizures, believing things that are not true, feeling unusually suspicious of others, aggressive behavior, hallucinations (seeing things or hearing voices that do not exist), mood changes, depression, motor tics or verbal tics, swelling of the face, throat, tongue, lips, or eyes, rash, hives, itching, purple blotches under the skin, fever, blistering or peeling skin, joint pain, frequent, painful erections, erection that lasts longer than 4 hours, numbness, pain, or sensitivity to temperature in the fingers or toes, skin color change from pale to blue to red in the fingers or toes, unexplained wounds on the fingers or toes.
Potential Drug Interactions
A dangerous drug interaction can occur between dexmethylphenidate and MAO inhibitors including isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, tranylcypromine, and others. Anyone taking MAO inhibitors or who has taken them in the past 14 days should not take dexmethylphenidate.
Serious side effects and death have occurred with the use of dexmethylphenidate and clonidine.
Methylphenidate has been shown to inhibit the metabolism of tricyclic antidepressants, coumarin anticoagulants and anticonvulsants (for example, phenobarbital, phenytoin, and primidone) so these drugs may interact with dexmethylphenidate in dangerous ways. Anyone taking them must inform their doctor before taking dexmethylphenidate as their dosages may need to be reduced.
Potential Food Interactions
Physical Health Risks
Slowed growth and weight gain in children and teens
Dexmethylphenidate may slow children's growth or weight gain. Your child's doctor will watch his or her growth carefully. Talk to your child's doctor if you have concerns about your child's growth or weight gain while he or she is taking this medication. Talk to your child's doctor about the risks of giving dexmethylphenidate to your child.
Heart and vascular problems
Patients with high blood pressure, serious heart problems, congenital heart defects or peripheral vascular disease such as Raynaud's syndrome can have serious side effects, including fatal ones, from taking stimulant drugs including dexmethylphenidate.
epilepsy or other seizure disorder
Dexmethylphenidate may increase risk of seizure since stimulants including dexmethylphenidate may lower seizure threshold in patients with epilepsy or prior history of seizures and in patients with prior EEG abnormalities in absence of seizures. Seizure threshold may also be lowered in patients with no history of seizures and no prior EEG evidence of seizures, though this is rare.
Increased tics (muscle twitches) or Tourette's syndrome
Patients with Tourette's syndrome or a family history of Tourette's syndrome may have their symptoms worsened and should not take dexmethylphenidate.
Priapism
Prolonged and painful erections, sometimes requiring surgical intervention, have been reported with methylphenidate products in both children and adults. This problem has been reported after some time on the drug often after an increase in dose and has also appeared during a period of drug withdrawal (drug holidays or discontinuation). Patients who develop abnormally sustained or frequent and painful erections should seek immediate medical attention.
Mental Health Risks
Psychosis and aggression
Use of stimulant drugs like dexmethylphenidate at usual doses for ADHD has been reported to induce psychosis in patients without a history of psychotic illness and can worsen pre-existing psychotic disorder by increasing symptoms of behavior disturbance and thought disorder.[3][4] Increased aggression has been reported in patients being treated with normal doses of stimulant medications for ADHD.
New or Worsened Bipolar disorder
Mania can be triggered in patients with bipolar disorder by use of stimulant drugs including dexmethylphenidate.
Induced or worsened depression and suicidal thoughts and attempts
Overdose
Symptoms of overdose include vomiting, agitation, tremors, hyperreflexia, muscle twitching, convulsions (may be followed by coma), euphoria, confusion, hallucinations, delirium, sweating, flushing, headache, hyperpyrexia, tachycardia, palpitations, cardiac arrhythmias, hypertension, mydriasis, and dryness of mucous membranes.
Reported Deaths
Some stimulants including dexmethylphenidate have caused sudden death in children and adults with serious heart problems or congenital heart defects. Tell your doctor if you have heart disease, heart rhythm disorder; coronary artery disease (hardened arteries); or a history of heart attack.
Producing Dexmethylphenidate
Forms of Dexmethylphenidate
Legal Status of Dexmethylphenidate
United Nations
USA
Dexmethylphenidate (Focalin), like other methylphenidate products, is classified as a Schedule II controlled substance by Federal regulation in the USA.
EU
Other Countries
Canadian Legal Status
Controlled Substance - Schedule 3
History of Dexmethylphenidate
Insights for Dexmethylphenidate
Dexmethylphenidate
More Dexmethylphenidate Sections and Information
Posts Tagged With Dexmethylphenidate
Dexmethylphenidate experiences: Post & read experiences with Dexmethylphenidate.
Dexmethylphenidate Forum: Post and read about Dexmethylphenidate.
Research & files about Dexmethylphenidate: Upload and read research & articles on Dexmethylphenidate.
Dexmethylphenidate image Gallery: Post and view pictures of Dexmethylphenidate.
Addiction Calculator: Do this small test to calculate your dependency.
References
- ^Spencer TJ, Adler LA, McGough JJ, et al. (2007) Efficacy and safety of dexmethylphenidate extended-release capsules in adults with attention-deficit/hyperactivity disorder. Biological Psychiatry. 2007;61(12):1380–1387
- ^Silva RR, Muniz R, Pestreich L, et al. Efficacy and duration of effect of extended-release dexmethylphenidate versus placebo in schoolchildren with attention-deficit/hyperactivity disorder (2006) Journal of Child & Adolescent Psychopharmacology. 2006;16(3):239–251.
- ^Randal G. Ross (July 2006), Psychotic and manic-like symptoms during stimulant treatment of attention deficit hyperactivity disorder. American Journal of Psychiatry 163:1149-1152.
- ^Kraemer M, Uekermann J, Wiltfang J, Kis B (July 2010). "Methylphenidate-induced psychosis in adult attention-deficit/hyperactivity disorder: report of 3 new cases and review of the literature". Clinical Neuropharmacology 33 (4): 204–6.
