Drug information of Dexmethylphenidate

Dexmethylphenidate is the more active, d-threo-enantiomer, of racemic methylphenidate. It is a CNS stimulant; blocks the reuptake of norepinephrine and dopamine, and increases their release into the extraneuronal space.

Absorption

Immediate release: Rapid; Extended release: Bimodal (with 2 peak concentrations ~4 hours apart)

Metabolism

Via de-esterification to inactive metabolite, d-α-phenyl-piperidine acetate (d-ritalinic acid)

Time to reach the peak

Fasting:

Immediate release: 1 to 1.5 hours; after a high-fat meal: 2.9 hours

Extended release: First peak: 1.5 hours (range: 1 to 4 hours); Second peak: 6.5 hours (range: 4.5 to 7 hours)

Distribution

Vd: 2.65 ± 1.11 L/kg

Half life

Immediate release: Children: 2 to 3 hours; Adults: 3 hours

Excretion

Urine (90%, primarily as inactive metabolite)

1-For the treatment of attention deficit hyperactivity disorder (ADHD).

2-For the treatment of attention deficit hyperactivity disorder (ADHD) in pediatric patients 6 years or older.

Usual Adult Dose for Attention Deficit Disorder

Immediate-Release:

For patients NEW to methylphenidate or on stimulants other than methylphenidate:

-Initial dose: 2.5 mg orally twice a day, at least 4 hours apart

For patients CURRENTLY on methylphenidate:

-Initial dose: One-half the total daily dose of methylphenidate; divide dose and administer orally twice a day at least 4 hours apart

Adjust dose in increments of 2.5 to 5 mg weekly according to needs and responses

Maximum dose: 20 mg/day (10 mg twice a day)

Extended Release (XR):

For patients NEW to this drug or methylphenidate, or on stimulants other than methylphenidate:

-Initial dose: 10 mg orally once a day

For patients CURRENTLY on methylphenidate:

-Initial dose: One-half of the total daily dose of methylphenidate orally once a day

For patients CURRENTLY on dexmethylphenidate immediate-release (IR):

-Initial dose: Same dexmethylphenidate IR daily dose orally once a day

Adjust dose weekly in 10 mg increments according to the needs and responses

-Maximum dose: 40 mg/day

Usual Pediatric Dose for Attention Deficit Disorder

Age 6 years or older:

Immediate-Release:

For patients NEW to methylphenidate or on stimulants other than methylphenidate:

-Initial dose: 2.5 mg orally twice a day, at least 4 hours apart

For patients CURRENTLY on methylphenidate:

-Initial dose: One-half the total daily dose of methylphenidate; divide dose and administer orally twice a day at least 4 hours apart

Adjust dose in increments of 2.5 to 5 mg weekly according to needs and responses

Maximum dose: 20 mg/day

Extended Release (XR):

For patients NEW to this drug or methylphenidate, or on stimulants other than methylphenidate:

-Initial dose: 5 mg orally once a day

For patients CURRENTLY on methylphenidate:

-Initial dose: One-half of the total daily dose of methylphenidate orally once a day

For patients CURRENTLY on dexmethylphenidate immediate-release (IR):

-Initial dose: Same dexmethylphenidate IR daily dose orally once a day

Adjust dose weekly in 5 mg increments according to the needs and responses

-Maximum dose: 30 mg/day

-Marked anxiety, tension, and agitation

-Hypersensitivity to methylphenidate or other components of the product

-Glaucoma

-Motor tics or a family history or diagnosis of Tourette's syndrome

-Concurrent or recent (within 14 days) use of monoamine oxidase inhibitors

-Safety and efficacy have not been established in patients younger than 6 years.

>10%:

Central nervous system: Headache (adults: 26% to 39%; children and adolescents: 25%), insomnia (children and adolescents: 5% to 17%), jitteriness (adults: 12%), anxiety (5% to 11%)

Gastrointestinal: Decreased appetite (children and adolescents: 30%), xerostomia (adults: 7% to 20%), abdominal pain (children and adolescents: 15%)

1% to 10%:

Central nervous system: Dizziness (adults: 6%), irritability (children and adolescents: 2% to 5%), depression (children and adolescents: 3%), emotional lability (children and adolescents: 3%)

Dermatologic: Pruritus (children and adolescents: 3%)

Gastrointestinal: Nausea (children and adolescents: 9%), dyspepsia (5% to 9%), vomiting (children and adolescents: 2% to 9%), anorexia (children and adolescents: 5% to 7%)

Respiratory: Pharyngolaryngeal pain (adults: 4% to 7%), nasal congestion (children and adolescents: 5%)

Miscellaneous: Fever (children and adolescents: 5%)

Acebrophylline, Amifampridine, Antacids, Antihypertensive Agents, AtoMOXetine, BuPROPion,Cannabinoid-Containing Products,Cocaine (Topical), Doxofylline, Esketamine, Fosphenytoin,Guanethidine, Histamine H2 Receptor Antagonists, Inhalational Anesthetics, Iobenguane Radiopharmaceutical Products, Ioflupane I 123, Iohexol, Iomeprol, Iopamidol, Monoamine Oxidase Inhibitors, PHENobarbital, Phenytoin, Primidone, Proton Pump Inhibitors, Serotonergic Agents (High Risk), Solriamfetol, Sympathomimetics, Tedizolid, Vitamin K Antagonists (eg, warfarin)

1-Dexmethylphenidate may be habit-forming. Never share dexmethylphenidate with another person, especially someone with a history of drug abuse or addiction. Keep the medication in a place where others cannot get to it. Selling or giving away this medicine is against the law.

2-Overdose symptoms may include restlessness, tremor, muscle twitches, rapid breathing, confusion, hallucinations, panic, muscle pain or weakness, and dark colored urine. These symptoms may be followed by depression and tiredness. Other overdose symptoms include nausea, vomiting, diarrhea, stomach pain, uneven heartbeats, feeling light-headed, fainting, seizure (convulsions), or coma.

3-Avoid taking dexmethylphenidate in the evening because it may cause sleep problems (insomnia).

1-You should not use dexmethylphenidate if you have glaucoma, tics or Tourette's syndrome, or severe anxiety, tension, or agitation.

2-Dexmethylphenidate may be habit-forming, and dexmethylphenidate is a drug of abuse. Tell your doctor if you have had problems with drug or alcohol abuse.

3-Stimulants have caused stroke, heart attack, and sudden death in people with high blood pressure, heart disease, or a heart defect.

4-Do not use dexmethylphenidate if you have used an MAO inhibitor in the past 14 days, such as isocarboxazid, linezolid, methylene blue injection, phenelzine, rasagiline, selegiline, or tranylcypromine.

5-Dexmethylphenidate may cause new or worsening psychosis (unusual thoughts or behavior), especially if you have a history of depression, mental illness, or bipolar disorder.

6-You may have blood circulation problems that can cause numbness, pain, or discoloration in your fingers or toes.

7-Call your doctor right away if you have: signs of heart problems--chest pain, feeling light-headed or short of breath; signs of psychosis--paranoia, aggression, new behavior problems, seeing or hearing things that are not real; signs of circulation problems--unexplained wounds on your fingers or toes.

8-You may take dexmethylphenidate with or without food. Take the regular tablet twice daily, at least 4 hours apart. Take the extended-release capsule once daily in the morning.

Storage

Store at 20°C to 25°C (68°F to 77°F); excursions permitted to 15°C to 30°C (59°F to 86°F). Protect from light and moisture.

there may be risks to fetus associated with use of CNS stimulants use during pregnancy.