Methylphenidate

Methylphenidate is a stimulant medication used primarily as a treatment for ADHD, marketed under trade names such as Ritalin and Concerta. When used recreationally, its effects resemble those of cocaine and amphetamine.
Recreational dosage:
Swallowed: 20–40 mg
Snorted: 15–30 mg

Performance-enhancing dosage:
Instant-release (IR), swallowed: 5 mg
Long-acting (LA), swallowed: 10 mg
Extended release (XR), swallowed: 18 mg
Duration:
Instant-release: 1–4 hours
Long-acting: up to 8 hours
Extended-release: up to 12 hours
Risks:
Acute toxicity: ⦿⦾⦾⦾⦾ (Very low risk)
Long-term toxicity: ⦿⦿⦾⦾⦾ (Low risk)
Dependence: ⦿⦿⦿⦾⦾ (Moderate risk)
Cognitive problems: ⦿⦿⦾⦾⦾ (Low risk)
Undesireable events: ⦿⦿⦾⦾⦾ (Low risk)
Interactions: ⦿⦿⦾⦾⦾ (Low risk)

Scroll down for the full risk profile.
1. Summary
Methylphenidate (methyl-2-phenyl-2-piperidine-2-acetate) is a central nervous stimulant drug widely used as a treatment for ADHD. It is marketed under several different trade names, including Ritalin, Concerta, Delmosart, Equasym, and Medikinet. It is also used illicitly as a recreational drug and performance-enhancing agent. It is classified as an illicit drug, albeit one with medical uses, which means it is illegal to use without a valid prescription.

Methylphenidate bears some resemblance to cocaine and amphetamine in its mechanism, but appears to be less harmful. It is usually swallowed in the form of pills or capsules, although some users prefer to insufflate (snort) crushed pills for a quicker and more intense effect. It is available in the form of instant-release pills with a short duration of effects, as well as long-acting and extended-release capsules, in which a larger dose is released continuously over several hours at a pre-determined rate.
2. Rules for sensible drug use
Please see our 10 general rules for sensible drug use. You should also be mindful of the following:

  • Never use methylphenidate at the same time as (or soon after) taking ayahuasca/pharmahuasca/changa, drugs in the 2C-T-series, or any other recreational or medical drug with strong monoamine oxidase inhibitor (MAOI) effects.

  • Be careful with using methylphenidate in combination with:

    • Tramadol, as this combination increases your risk of seizures. Avoid high
      doses of either drug.
    • SSRI-based antidepressants, as this may increase the effects of the SSRI and also increase your risk of becoming addicted to methylphenidate.
    • Central nervous depressants (including alcohol, benzodiazepines, and GHB), as the risk of overdosing on these drugs goes up rapidly once the methylphenidate wears off.
  • Avoid combining methylphenidate with other central nervous stimulants, as this can lead to dangerous over-stimulation.

  • Avoid injecting methylphenidate or repeatedly snorting higher doses, as this increases the risk of addiction.

  • Be careful with using methylphenidate if you have slept too little. Lack of sleep increases the risk of stimulant psychosis.

  • Avoid strenuous physical activity when using methylphenidate at higher doses, as this may damage your heart.

  • Be careful with using methylphenidate for performance enhancement, as this may lead to burnout over time.
    3. Risk profile
    We employ a five-step risk scale with values ranging from "very low" to "very high" within six categories: Acute toxicity, Long-term toxicity, Dependence, Cognitive problems, Unpleasant events, and Interactions.

    These values are based on qualitative reviews of available knowledge, and should only be viewed as guidelines. They are also relative, so a score of "very low risk" does not mean the substance is risk-free. The scale assumes users are normal, healthy individuals; beware that even drugs which are well-tolerated by most people may nevertheless be harmful to some users. It also assumes normal use patterns; that is, if a given drug is only harmful when used in a certain way, yet is almost never used in that way, then the drug will be considered less harmful compared to a similar drug which is commonly used in a harmful way.


    ACUTE TOXICITY

    ⦿⦾⦾⦾⦾ (Very low risk)

    Lethal overdoses of methylphenidate are exceedingly rare. Between 2000–2005, the US Toxic Exposure Surveillance System only registered two deaths attributed to methylphenidate, despite also registering more than 8000 cases of methylphenidate poisoning in 2004 alone [1]. Testing on rats indicates that medically significant overheating – a typical indication of overdose – due to methylphenidate begins to occur at serum concentrations twice as high as for amphetamine [2].


    LONG-TERM TOXICITY

    ⦿⦿⦾⦾⦾ (Low risk)

    Methylphenidate appears not to be neurotoxic, although excessive doses can indirectly cause brain damage through overheating. There is also reason to believe that frequent use of methylphenidate at high doses can put too much strain on the heart, as with amphetamine, but it is unclear whether long-term methylphenidate use increases one's risk of cardiovascular disease. Although one study of adults before and after commencing methylphenidate treatment found a 1.8-fold increase in heart attack risk, another (larger) study did not find any increased risk [8, 9]. Methylphenidate treatment does, however, appear capable of triggering heart attacks in some especially vulnerable patients [10].


    DEPENDENCE

    ⦿⦿⦿⦾⦾ (Moderate risk)

    Methylphenidate bears a strong resemblance to cocaine in its mechanism of action, and lab animals have been shown to self-administer the two drugs at comparable rates. Nevertheless, methylphenidate is assumed to carry a lower risk of addiction than cocaine and amphetamine in humans, and humans tend to self-administer the drug at low to moderate rates in similar clinical trials [20]. This may be due to methylphenidate's negligible effect on the brain's serotonin system, or possibly the fact that it is broken down in the brain more slowly than is cocaine [6]. Some users also experience more bodily discomfort and unpleasant side-effects from methylphenidate than cocaine, which might contribute to a lower prevalence of excessive use among methylphenidate users [18].


    COGNITIVE PROBLEMS

    ⦿⦿⦾⦾⦾ (Low risk)

    Use of methylphenidate in humans, at therapeutic doses and over long periods of time, is not associated with any of the structural changes in the brain that normally indicate brain damage. Experiments on mice have found a certain toxic effect on the brain's dopamine system, but it is unclear whether or to what extent this effect translates into humans [12]. Excessive methylphenidate use can nevertheless cause transient cognitive problems following cessation of use, due to tolerance build-up. There is no observed link between methylphenidate use and increased risk of psychosis, even in individuals with a history of psychosis. However, overdose and/or several-day "binge" use of any stimulant (including methylphenidate) can lead to stimulant psychosis, a transient state of psychosis resulting from severe and acute sleep deprivation [13].

    Researchers used to believe that methylphenidate had the opposite effect on individuals with and without ADHD, but this has since been disproven, and it is now known that the drug enhances cognitive performance in both groups at therapeutic doses. The effect is, however, more significant in those whose performance level is lower to begin with, which in turn levels out the observed group differences to some extent [14].


    UNDESIREABLE EVENTS

    ⦿⦿⦾⦾⦾ (Low risk)

    Some find it tempting to use methylphenidate for day-to-day performance enhancement. This often leads to users exceeding their daily work capacity and de-prioritizing sleep, increasing one's risk of burnout in the long run. Moreover, chronic sleep deprivation reliably and rapidly impairs cognitive performance, which on average cancels out any performance-enhancing effects caused by the methylphenidate itself. Thus, people who frequently or regularly use methylphenidate for performance enhancement should ideally make sure to get more sleep and rest than they would otherwise need, as well as take longer breaks from the drug on a regular basis in order to recover fully and avoid developing a tolerance. Methylphenidate tends to boost feelings of accomplishment and mastery by activating the brain's reward system. Especially at higher doses, this can lead to poor judgement and impulsive decision-making, in addition to making users less attentive to their own and others' needs. In general, for daily users of methylphenidate (whether for medical or performance-enhancing purposes), feelings of unusual satisfaction or euphoria should be taken as a sign that one's dosage is too high; if so, the dosage should be decreased to a point where only the desired medical or performance-enhancing effects are noticeable. Given that a normal prescribed dose is intended for daily users (who have developed a tolerance to the drug's effects), those who only use methylphenidate occasionally or sporadically should avoid taking more than half of a normal prescribed dose at a time.


    INTERACTIONS

    ⦿⦿⦾⦾⦾ (Low risk)

    Methylphenidate should, like all central nervous stimulants, never be used in combination with any monoamine oxidase-inhibiting drugs or medications, known as MAOIs. This includes recreational drugs such as ayahuasca, changa, and psychedelics in the 2C-T-series, atypical antidepressants such as phenelzine and moclobemide, and anti-Parkinsons drugs such as rasagiline and selegiline. Taking methylphenidate at the same time as (or soon after) a strong MAOI can result in dangerously high blood pressure; in the worst case, it can lead to serotonin syndrome, a potentially life-threatening medical emergency.

    Combining methylphenidate with tramadol in large doses of either drug significantly increases one's risk of seizures, and is thus strongly discouraged. (15) It is also best to avoid combining methylphenidate with other strong central nervous stimulants, as this can lead to dangerously high blood pressure and overheating. Combinations with central nervous depressants can effectively delay a depressant overdose until the methylphenidate wears off, at which point the overdose effects set in rapidly, often with little to no perceived warning. Anyone using methylphenidate and CNS depressants together should thus be extra cautious about their depressant intake.

    Combining methylphenidate with SSRI-based antidepressants can increase the serotonin reuptake-inhibiting effects of the latter, and may also increase one's risk of becoming addicted to methylphenidate. (19)

    Combining methylphenidate and cannabis can lead to short-term confusion and anxiety, and likely also increases the risk of psychosis associated with cannabis use. It can also increase one's heart rate to a significant degree, and should thus be avoided by users with heart problems.

    Methylphenidate in combination with psychedelics or dissociatives does not appear to carry much risk, so long as one is normally able handle each drug on its own. Users with known cardiovascular problems should nevertheless be careful with such combinations, as the central nervous stimulant effects of each drug is often mutually reinforcing, potentially causing a rapid rise in heart rate and blood pressure. Taking psychedelics on the "way down" from methylphenidate can negatively affect the psychedelic experience, and is thus discouraged.

    For a detailed list of medications known to interact with methylphenidate, see Felleskatalogen.

    4. Dosage and route of administration
    DOSAGE

    Little is known about common recreational doses of methylphenidate, but estimates range between 20 to 50 mg for instant-release formulations taken by mouth [11]. Psychonautwiki lists a normal dose as 20–40 mg (oral/swallowed) and 15–30 mg (insufflated/snorted).


    FORM

    Methylphenidate exists mainly as a legally manufactured medication in the form of pills or capsules.

    The most common trademarked forms, Ritalin and Methylphenidate Teva, are available in capsules containing either 10, 20, 40, or 60 mg of methylphenidate; these are all long-acting (modifisert frisetting) formulations, which means some of the drug is released after a delay of a few hours. Ritalin is also available as instant-release 10 mg pills.

    Methylphenidate is also available as extended-release (depotformulering) capsules under trade names such as Concerta, Delomsart, and Equasym.


    ROUTE OF ADMINISTRATION

    Methylphenidate is biologically active via all intake routes, but is most commonly swallowed or insufflated. Extended-release forms are often manufactured in such a way as to make them unsuitable for anything except oral administration.
    5. Mechanism and subjective effects
    MECHANISM OF ACTION

    Methylphenidate exists as four enantiomers (spatial reflections of the molecule), two of which are not psychoactive and hence not used medically [4]. Among the two active enantiomers, the one believed to be responsible for most of the psychoactive effects is d-threo-methylphenidate, also known as D-TMP or dexmethylphenidate [7]. In the brain, D-TMP binds to the dopamine and noradrenaline transporters DAT and NET, triggers a redistribution of the monoamine transporter VMAT-2, and activates both the 1A serotonin receptor subtype as well as ɑ2 adrenergic receptors. Increased dopamine and noradrenaline levels in the brain are assumed to be the primary mechanism behind the psychoactive effects of methylphenidate, although the activation of ɑ2 adrenergic receptors appear to also play a key role in some of the drug's performance-enhancing effects. Brain scans of patients under the influence of methylphenidate show increased cortical activity in the parietal and frontal lobes, as well as attention and context-dependent effects in other areas, including the insula, posterior cingulate cortex (PCC), and putamen [3].


    DURATION

    Instant-release methylphenidate lasts between 1–4 hours when taken by mouth. When insufflated, the effects are shorter-lived.

    Long-acting formulations taken by mouth last up to 8 hours, while extended-release forms last up to 12 hours.


    SUBJECTIVE

    Methylphenidate's effects are generally perceived as similar to those of ampheatmine or cocaine, at least when taken in moderate doses [17]. However, some find methylphenidate less pleasant than amphetamine or cocaine, likely due to its more pronounced bodily side-effects and weaker serotonergic effect.

    The most noticeable effects of taking methylphenidate include a greater sense of wakefulness, sharper focus, enhanced sensory experience, and changes in time perception. Some users also experience a sense of emotional disinterest or "dulling".


    SIDE-EFFECTS

    The most common side-effect of methylphenidate use is nausea and dry mouth.

    Less common side-effects include abdominal discomfort or pain, diarrhea, vomiting, tooth pain, high pulse and blood pressure, heart palpitations (noticeably "thumping" heart), shortness of breath, fever, and exhaustion.

    For a full list of known side-effects, see Felleskatalogen.

    More subtly, the emotional dulling effect that some users experience may impact areas of one's life which depend on emotional involvement, such as romantic relationships and artistic proclivities.
    6. Legal status
    Methylphenidate is on the narcotics list (Narkotikalisten) in Norway and is thus considered an illegal drug under legemiddelloven § 22. This means it is punishable by law to use, possess, manufacture, import, export, procure, store, or distribute methylphenidate without a special exemption for medical or scientific purposes. Patients with a valid medical precription (Norwegian reseptgruppe A, or an equivalent prescription from within the EU/EEA) are allowed to buy, posess, store, and travel internationally with limited amounts of methylphenidate for personal medical use.

    For up to 20 pills or 1 g of methylphenidate, possession or procurement without a valid exemption is punishable by a fine; any higher amounts can result in a prison sentence. This limit is halved in the case of import (smuggling) for personal use.
    7. Sources
    1. Methylphenidate poisoning: An evidence-based consensus guideline for out-of-hospital management. https://www.tandfonline.com/doi/pdf/10.1080/155636...

    2. A comparison of methylphenidate-, amphetamine-, and methamphetamine-induced hyperthermia and neurotoxicity in male Sprague–Dawley rats during the waking (lights off) cycle
    https://www.sciencedirect.com/science/article/abs/...

    3. The pharmacology of amphetamine and methylphenidate: Relevance to the neurobiology of attention-deficit/hyperactivity disorder and other psychiatric comorbidities
    https://www.sciencedirect.com/science/article/pii/...

    4. Methylphenidate: Its Pharmacology and Uses
    https://pubmed.ncbi.nlm.nih.gov/10907387/

    5. Adult ADHD Medications and Their Cardiovascular Implications
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC49927...

    6. Is methylphenidate like cocaine? Studies on their pharmacokinetics and distribution in the human brain
    https://pubmed.ncbi.nlm.nih.gov/7771915/

    7. Methylphenidate and its isomers: their role in the treatment of attention-deficit hyperactivity disorder using a transdermal delivery system
    https://pubmed.ncbi.nlm.nih.gov/16953648/

    8. Methylphenidate and Risk of Serious Cardiovascular Events in Adults
    https://ajp.psychiatryonline.org/doi/pdf/10.1176/a...

    9. ADHD Medications and Risk of Serious Cardiovascular Events In Young and Middle-Aged Adults
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC33503...

    10. Cardiovascular safety of methylphenidate among children and young people with attention-deficit/hyperactivity disorder (ADHD): nationwide self controlled case series study
    https://www.bmj.com/content/353/bmj.i2550

    11. Variables That Affect the Clinical Use and Abuse of Methylphenidate in the Treatment of ADHD
    https://www.researchgate.net/publication/9028633_V...

    12. The effect of methylphenidate intake on brain structure in adults with ADHD in a placebo-controlled randomized trial
    http://jpn.ca/wp-content/uploads/2016/10/41-6-422....

    13. Methylphenidate and the risk of psychosis in adolescents and young adults: a population-based cohort study
    https://www.thelancet.com/journals/lanpsy/article/...(19)30189-0/fulltext

    14. Responses to methylphenidate in Attention-Deficit/Hyperactivity Disorder and normal children: update 2002
    https://pubmed.ncbi.nlm.nih.gov/12685519/

    15. Drug Interactions between Ritalin and tramadol
    https://www.drugs.com/drug-interactions/ritalin-wi...

    16. Pharmacokinetics and Clinical Effectiveness of Methylphenidate
    https://pubmed.ncbi.nlm.nih.gov/10628897/

    17. Clinical potential of methylphenidate in the treatment of cocaine addiction: a review of the current evidence
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC44764...

    18. Behavioral and Cardiovascular Effects of Intravenous Methylphenidate in Normal Subjects and Cocaine Abusers
    https://www.karger.com/Article/PDF/259147

    19. Fluoxetine potentiation of methylphenidate-induced gene regulation in striatal output pathways: Potential role for 5-HT1B receptor
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC42503...

    20. Reinforcing and subjective effects of methylphenidate in adults with and without attention deficit hyperactivity disorder (ADHD)
    https://www.ncbi.nlm.nih.gov/pmc/articles/PMC26886...

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