Methylphenidate (MPH) is the most prescribed psychostimulant for ADHD treatment. It works by blocking the dopamine and norepinephrine transporters, thereby increasing synaptic dopamine and norepinephrine concentrations (which is said to be lacking in ADHD-diagnosed individuals). Oral effective doses of 0.25 and 1 mg/kg are estimated to being able to, respectively, block 50% and 75% of the dopamine transporter 1,2. On the other hand, a dose of 0.5 mg/kg will delay sleep start time and decrease sleep duration 3, hence care should be observed on doses near bedtime.
As Methlyphenidate has a short duration of action, other
dosage forms have emerged to prolong its effect especially when multi-dosing
throughout the day is not possible. Below is the table of comparison on three
commonly used brands. While benefits are observed during duration of action,
unwanted side effects such as decreased appetite is also observed for the
duration of the drug. For example, someone taking Concerta may not have
appetite for the entire 12 hours.
Brand name |
Ritalin 4 |
Medikinet 5 |
Concerta 6 |
Release Type |
Immediate
(IR) |
Modified (MR) |
Extended
Release |
Composition |
100%
Immediate release |
50% IR, 50% from
enteric coated pellets |
22% IR, 78%
from Osmotic Release |
Dose
equivalent to IR |
N.A. |
10 mg is for
equivalent to 5 mg, 5 mg twice dosing |
18 mg is for
equivalent 5 mg, 5 mg, 5 mg thrice dosing |
Time to peak
(hours) |
1-2 |
1st: 1-2 |
1st: 1-2 |
Duration
(hours) |
3-4 |
3-8 |
3-12 |
Effects by
meal |
No effect on
absorption. Can be taken with or without food. |
On an empty
stomach, the absorption rate is faster and extended release may not be
adequately sustained. Should be given after a meal. |
No effect on
absorption. Can be taken with or without food. |
Plasma levels
after 24h |
Close to
zero, hence no accumulation |
Close to
zero, hence no accumulation |
|
References:
- Volkow ND, Wang GJ, Fowler JS, Gatley SJ, Logan J, Ding YS, Hitzemann R, Pappas N: Dopamine transporter occupancies in the human brain induced by therapeutic doses of oral methylphenidate. Am J Psychiatry 155:1325–1331, 1998
- Spencer TJ, Biederman J, Ciccone PE, Madras BK, Dougherty DD, Bonab AA, Livni E, Parasrampuria DA, Fischman AJ: PET study examining pharmacokinetics, detection and likeability, and dopamine transporter receptor occupancy of short- and long-acting oral methylphenidate. Am J Psychiatry 163:387–395, 2006
- Santisteban JA, Stein MA, Bergmame L, Gruber R: Effect of extended-release dexmethylphenidate and mixed amphetamine salts on sleep: A double-blind, randomized, crossover study in youth with attention-deficit hyperactivity disorder. CNS Drugs 28:825–833, 2014
- Ritalin Summary of Product Characteristiscs Health Products Regulatory Authority November 2023
- Medikinet Summary of Product Characteristiscs Health Products Regulatory Authority January 2024
- Concerta Summary of Product Characteristiscs Health Products Regulatory Authority November 2022