Dexmethylphenidate Stats & Data
COC(=O)C(C1CCCCN1)c1ccccc1DUGOZIWVEXMGBE-CHWSQXEVSA-NPharmacology
DrugBankDescription
Dexmethylphenidate is the dextrorotary form of methylphenidate introduced in 2002. It is a norepinephrine-dopamine reuptake inhibitor (NDRI) and thus a psychostimulant. It is used for treatment of Attention Deficit Hyperactivity Disorder (ADHD). The d-isomer is thought to have greater effect with fewer side effects than the l-isomer or the racemic mixture.
Mechanism of Action
Methylphenidate inhibits dopamine and norepinephrine reuptake transporters in synapses, especially in the thalamus and striatum. One study shows no detectable difference in the caudal prefrontal cortex of treated or untreated monkeys, though multiple rat studies show activity on the prefrontal cortex. Imaging of human brains after administration of methylphenidate shows changes to blood flow of various regions of the brain including the striatum, supplementary motor area, and posterior parietal cortex.
Pharmacodynamics
Dexmethylphenidate is the d-enantiomer of methylphenidate. This enantiomer is more pharmacologically active than the racemic mixture and may block norepinephrine and dopamine reuptake in synapses.
Metabolism
Dexmethylphenidate is metabolised to the inactive metabolite ritalinic acid by carboxylesterase 1A1 in the liver. Other minor pathways metabolise dexmethylphenidate to the inactive metabolites 6-oxo-methylphenidate and p-hydroxy-methylphenidate which are de-esterified and conjugated into other unknown metabolites.
Absorption
Taking dexmethylphenidate with or without food does not affect patients in a clinically relevant way. 90% of an oral dose is absorbed but as a result of hepatic first pass metabolism, oral bioavailability of dexmethylphenidate is 23% compared to l-methylphenidate with an oral bioavailability of 5% . Maximum concentration is generally reached in 1-1.5 hours.
Toxicity
There is no difference in effect across genders. The difference in effect across racial groups, patients under 6 years, renal impairment, hepatic impairment, pregnancy, lactation, and geriatric patients has not been well studied. Patients with renal impairment are not expected to need dose adjustment as the drug is not mainly cleared renally. Animal studies in pregnant and lactating rats showed delayed fetal skeletal ossification, and reduced weight gain in male offspring. Due to these studies, caution must be exercised and the benefits and risks of taking this drug must be weighed. It is unlikely that dexmethylphenidate is carcinogenic but B6C3F1 mice, which are sensitive to the development of hepatic tumours, developed hepatoblastomas at 2 times the maximum recommended human dose. Methylpheidate was not found to be mutagenic but is weakly clastogenic in Chinese Hamster Ovary cells. Methylphenidate does not impair fertility in animal studies.
Indication
Dexmethylphenidate is used as a treatment for ADHD, ideally in conjunction with psychological, educational, behavioral or other forms of treatment.
Half-life
The mean terminal half life is approximately 2.2 hours. However other studies have shown 3.8-3.9 hours, or 5.96 hours after intravenous administration and 5.69 hours following an oral dose.
Protein Binding
12-15% of dexmethylphenidate is protein bound. However, other studies have observed 15.2±5.2% protein binding in children and 16.2±1.1% in adults.
Elimination
Dexmethylphenidate is mainly eliminated renally. After 48 hours, 90% of the dose is collected in the urine and 3.3% is collected from feces.
Clearance
0.40L/hr/kg following an intravenous dose and a renal clearance of 0.005L/hr/kg.
History & Culture
Dexmethylphenidate is the dextrorotatory enantiomer of methylphenidate, isolated and developed as a separate pharmaceutical product. It received approval for medical use in the United States in 2001 and was subsequently introduced to the market in 2002 under the brand name Focalin. The rationale for its development was that the d-isomer was believed to be the more pharmacologically active component of the racemic methylphenidate mixture. Since its introduction, dexmethylphenidate has become widely prescribed for the treatment of attention deficit hyperactivity disorder. Generic formulations have become available, expanding access beyond the original brand-name product. By 2023, it had become the 127th most commonly prescribed medication in the United States, with more than 4 million prescriptions written annually.
Effect Profile
Curated + 15 ReportsStrong euphoria with moderate anxiety/jitters, mild stimulation
Tolerance & Pharmacokinetics
drugs.wikiTolerance Decay
Cross-Tolerances
Experience Report Analysis
ErowidDemographics
Gender Distribution
Age Distribution
Reports Over Time
Effect Analysis
ErowidEffects aggregated from 15 experience reports (15 Erowid)
Effect Sentiment Distribution
Confidence Distribution
Positive Effects 6
Adverse Effects 5
Real-World Dose Distribution
62K DosesFrom 30 individual dose entries
Insufflated (n=14)
Oral (n=16)
Form / Preparation
Most common forms and preparations reported
Body-Weight Dosing
Dose relative to body weight from reports with weight data
Redose Patterns
Redosing behavior across 11 reports
Legal Status
| Country | Status | Notes |
|---|---|---|
| United States | Prescription medication | Marketed as a prescription product under the brand name Focalin since November 2001. Generic formulations (Dexmethylphenidate HCl) are also available from multiple pharmaceutical manufacturers including Sandoz and Adare Pharmaceuticals. |