Methylphenidate

Chemical Name:

Methyl-phenyl(piperidin-2-yl)acetate

Street Names:

Ritalin (racemic), Kiddy Coke, Focalin (dextro isomer), Concerta (long acting)

Category:

Stimulant

Subcategory:

Phenidate

Bioavailability:

~30%

Methylphenidate Dosage

Threshold

Light

Common

5 mg

5 - 20 mg

20 - 60 mg

Strong

Heavy

Fatal

60 - 90 mg

90+ mg

unknown

Warning

Remember: Always start on lower dosages! Differences in metabolism, tolerance, sensitivity, and neurochemistry can lead to higher than expected effects, and even death.

Methylphenidate Duration

Onset

Come up

Peak

15 - 60 Minutes

10 - 40 Minutes

1 - 2.5 Hours

Comedown

After effects

Total

2 -4 Hours

2 - 12 Hours

4 - 8 Hours

Interactions

This substance interacts with:

Tramadol

MAOIs

aMT

These interactions may lead to an unpleasant experiences due to substances potentiating each other unpredictably, and/or may be potentially fatal.

Methylphenidate


Methylphenidate (abbreviated as MPH, brand names Ritalin, Focalin, and Concerta) is a stimulant used for the treatment of ADHD and narcolepsy. In addition to being a very effective medicine for the mentioned conditions, methylphenidate has also found use as a study tool and, sometimes, as a recreational drug.

Harm reduction

Methylphenidate is often used at therapeutic dosages (typically in the lighter range) for productivity, a social boost, or to stay awake for extended periods. However, those who use methylphenidate recreationally for its euphoric effects have more to keep in mind before and during use.

  • The comedowns from moderate-high dosages of methylphenidate can be brutal. They range from a loss of energy, mild depression, anxiety, apathy, and insomnia to suicidal thoughts and severe depression. Due to the severity of these comedowns, users often face the urge to redose. This should be avoided for the health of the user and to keep tolerance low. During this comedown, typically good solutions would include rest, taking it easy, engaging in low-energy leisure activities such as listening to music or watching TV, and accepting that the experience is over..

  • Binging on methylphenidate can cause the negative effects listed to become exponentially worse. Due to methylphenidate's mechanism of action, the body develops a tolerance to methylphenidate extremely quickly, requiring higher dosages to continue feeling the effects. Additionally, a lack of sleep can also cause psychosis, a state in which the user cannot differentiate reality from delusion. Coupled with high doses and lack of sleep, heavy methylphenidate use can cause damage to the mind. It begins as a slow confusion of thought patterns, but quickly evolves over time, and is typically a negative experience.

  • Sleep well before dosing, and avoid pulling all-nighters. While methylphenidate may seem to give you unlimited energy and endless euphoria, these effects diminish quickly if one is sleep-deprived. Additionally, the "energy" provided after not sleeping for long periods of time (3 days+) can be extremely uncomfortable, and cause risk of stimulant psychosis.

  • Avoid overly strenuous physical activity, especially on higher doses, as this can be particularly stressful to the heart. A light workout on low doses probably won't hurt, but don't run a marathon or do HIIT while intoxicated on stimulants. Be cautious while engaging in physical activity on methylphenidate or any other stimulant.

  • Make sure you eat and stay hydrated. It can be easy to forget this. A little, light snack can go a long way into making what is a negative experience into a good one. Remember, you need fuel to create those neurotransmitters to make you feel all this stimulation.

  • Injecting, snorting, or boofing (rectal administration) methylphenidate may be more intense, but it is at the cost of a harsher and possibly longer-lasting comedown. Snorting beads in extended-release formulations can fill your nose with binders and damage your nose, so instant release is your best bet. Make sure to engage in safe practices for any ROA, particularly with IV and insufflation.

  • Avoid taking methylphenidate if you have any known heart problems. Extra strain added by methylphenidate to the heart can result in a heart attack. If you plan on heavily using any stimulant, get your heart checked by your doctor first (this does not mean that you have to admit to drug use).

  • Stimulants can lead to hyperfocusing on smaller details and small things, which can be a good or bad thing depending on the situation. Try to change activities once in a while so you don't get stuck in a loop.

  • Stimulants can lead to an artificially elated ego, abnormal confidence, and correspondingly disinhibition. Always keep this in mind when making decisions under the influence, and think hard about whether you would do or say it while sober.

  • When dosing methylphenidate, check if the formulation is Focalin/dexmethylphenidate. Dexmethylphenidate requires only half the dosage of racemic methylphenidate (brand name Ritalin) for equivalent effects.

  • Avoid drinking or using depressants such as benzodiazepines or opioids with methylphenidate. With stimulants like methylphenidate present, users often miscalculate and overdo it with depressants because they might not feel them as strongly compared to when they're sober. However, while they might not cognitively feel it, impairment is still present, and respiratory depression will be elevated once the methylphenidate wears off. Methylphenidate is also speculated to be able to chemically react with alcohol to form a different compound, as cocaine does when combined with alcohol.

  • Make sure to keep up with normal hygiene practices. Feeling great doesn't mean you look or smell great. Additionally, methylphenidate can dry out your mouth, and correspondingly may increase tooth decay, so remember to keep up on dental hygiene.

MOST IMPORTANTLY use the lowest dose possible, and don't use it consistently for extended periods of time when possible or without indication from a doctor.

Addiction potential

Methylphenidate is considered to be a moderately addictive substance, and has the potential to cause toxicity to the brain. It's dependence syndrome and accordingly withdrawal symptoms are mainly of the psychological category, with physical withdrawals (such as those found with opioids and benzodiazepines) generally not being experienced or mild in severity. The withdrawals, like with all stimulants, can last anywhere from weeks to months, and even years on rare occasions. This drug is thought to have a lower risk of chronic symptoms resulting from abuse compared to amphetamine(s) or cocaine, but it can still be addictive.

  • Lethargy

  • Flu-like body aches

  • Depression

  • Anxiety

  • Extreme increase in appetite, resulting in rebound weight gain

  • Increased sleep

  • Parkinson-like shaking

  • Forgetfulness

  • Reduced motor ability

  • Apathy

  • Boredom

  • Urges to take methylphenidate

Additionally, methylphenidate is acutely (in the short-term) addictive as well, with users frequently engaging in "binging" behavior with this drug.

Effects

Methylphenidate leaves users motivated, focused, hyper-aware of their environment, energetic, awake, confident, and in some cases, extremely anxious or jittery. Methylphenidate can also be euphoric at recreational dosages, although it's typically less intense than with other stimulants such as amphetamines.

It is also to be noted that racemic methylphenidate differs from dexmethylphenidate, the dextroratory isomer of methylphenidate. Focalin is a dexmethylphenidate formulation, making it about twice as potent without the L-isomer. 10mg of Focalin IR = 20mg of Ritalin IR, and vice-versa. Racemic mixtures tend to cause more negative side effects.

Additionally, compared to the effect duration listed, XR is about half as intense relative to dose in milligrams with about 2 times less potency, so 5mg of Focalin IR is about what you'll feel on 10mg Focalin XR, but for a significantly longer time. Methylphenidate comes in many forms, so it's good to research the differences between any formulations you are going to use.

A common myth states users with ADHD cannot derive recreational effects, or that they experience solely sedation instead of stimulation. This is untrue, and addiction and abuse are no less likely to occur in those with ADHD.

Teeth grinding is another effect of methylphenidate, so make sure to have some gum before carrying through the experience to help with this. Time may also seem as if it's going faster for the duration of the effect. Users may also feel bolder and take actions they usually wouldn't due to increased ego and confidence, the harm of this depends on the situation, and in some cases may even be seen as beneficial.

Basic Pharmacology

Methylphenidate is a central nervous stimulant that increases concentrations of the monoamine neurotransmitters norepinephrine and dopamine in your brain by preventing their reuptake/removal. Norepinephrine is a chemical related to adrenaline (epinephrine) which stimulates your sympathetic nervous system, which is responsible for the "fight or flight" response. Dopamine is a chemical mainly involved in the reward pathway and movement, and the former involvement is responsible for much of the effects on attention, motivation, etc. that methylphenidate has. This is in contrast to drugs like amphetamine, known as "releasers," which cause elevations in the aforementioned monoamines via increasing the likelihood neurons will release them. Methylphenidate, on the other hand, simply blocks the removal/reuptake of these monoamines, without releasing any more than would be normally.

Advanced Pharmacology

Methylphenidate, despite it's resemblance and similar effects to amphetamine(s), has a notably different mechanism of action, and increases neuronal firing rate rather than reduces it as amphetamine(s) do. Methylphenidate acts as an inhibitor of the dopamine transporter (DAT) and norepinephrine transporter (NET), with no significant affinity for the serotonin transporter (SERT) or any other sites. Despite similarity in mechanism to cocaine and other reuptake inhibitors, and contrary to common knowledge, methylphenidate is neurotoxic to dopaminergic neurons and accordingly, causes their death[1]. Methylphenidate also has a somewhat unexpected interaction when combined with releasers such as amphetamine, in that it actually significantly blunts the monoamine releasing ability of these drugs. This is due to it's main mechanism of action, as amphetamine's ability to induce transporter reversal, and correspondingly monoamine efflux, is blocked, as the transporters are being inhibited by methylphenidate and aren't free to pick up monoamines released into the cytosol by amphetamine(s). Amphetamine also serves as an inhibitor of these transporters, however it has a comparatively small affinity, and most of it's reuptake inhibition is theorized to be mainly produced via non-competitive reuptake inhibition via agonism of TAAR1 and subsequent transporter internalization.

Overdose

In the case of an overdose, one may experience abnormally increased heart rate (decreased is possible, but unlikely), blood pressure, temperature, and sweating. Symptoms resulting of overstimulation of the sympathetic nervous system aside from those listed such as muscle twitching and tightness, increased urination, dilated pupils, restlessness, and generalized anxiety are also likely. All of these can result from normal methylphenidate usage as well, but are more likely to occur and are of greater intensity in overdose. The user may fall into a state of state not unlike typical schizophrenic psychosis, which is aptly named stimulant psychosis. This can manifest itself in delusions, hallucinations, general paranoia, irrational thinking, and can make the user act in a violent, atypical manner. However, unlike other forms of psychosis, stimulant psychosis generally resolves on it's own after sleep and/or cessation of usage. Stimulant psychosis, while being a symptom of overdose, is also likely with normal doses, especially coupled with sleep deprivation (a known cause in and of itself). Death resulting from methylphenidate use is exceedingly rare.

If you or someone you know believes they're overdosing on methylphenidate, it's highly advised to request medical help. Deaths from methylphenidate alone are rare, but it's not impossible. Symptoms indicating increased risk of lethality include pain in the chest, left arm, left shoulder, or jaw, the feeling of intense pressure or tightness in/on the chest, convulsions, extreme lightheadedness, unconciousness, seizure, and delirium/confusion.

Legality

Methylphenidate is a controlled substance in most countries. Possession without a prescription, distribution, or manufacture is generally punishable by jail time and/or significant fines.

  • United States: Methylphenidate is a schedule 2 substance in the U.S.

  1. https://www.ncbi.nlm.nih.gov/pmc/articles/PMC3312333/ ↩︎

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