Also known as
Concerta, Methylin, Ritalin, Medikinet, Equasym XL, mph, smart pills, ritties, vitamin r, kiddie coke, skittles, smarties, diet coke
Classification
Stimulanta drug that acts on the Central Nervous System, increasing some rates of function such as heart-rate
Overview
Methylphenidate is a psychostimulant drug approved for treatment of ADHDattention deficit hyperactivity disorder - a group of behavioural symptoms that include inattentiveness, hyperactivity and impulsiveness More, postural orthostatic tachycardiarapid pulse rate syndrome, and narcolepsy. It may also be prescribed for off-label use in treatment-resistant cases of lethargy, depression, neural insult and obesity. It is similar in structure as amphetamines however only produce mild effects of amphetamines 1.
Street price
Currently, it is being sold for 50p to £1 per tablet 2.
Why take it?
Sought after effects
Undesired effects
- increased body temperature,
- tachycardiarapid pulse rate,
- hypertensionhigh blood pressure,
- dehydration,
- paranoiasuspicion, distrust or fear of other people,
- racing thoughts,
- insomniadifficulty in going to sleep or in getting enough sleep 3.
How long do its effects last?
Onset of effects
Come up
- oral – 20 – 60 minutes 4.
Peak
- oral – 90 – 150 minutes 4.
Offset
- oral – 1 – 2 hours 4.
Duration of effects
After-effects
- oral – 2 – 6 hours 4.
- insufflatedInsufflating, commonly referred to as snorting, is a method of drug administration where powdered substances are inhaled through the nose. More – 1 – 24 hours 5.
Pharmacology
Pharmacodynamics
Methylphenidate is a central nervous systembrain and spinal cord stimulanta drug that acts on the Central Nervous System, increasing some rates of function such as heart-rate used most commonly in the treatment of attention-deficit disorders in children and for narcolepsy. Methylphenidate also blocks the reuptake of norepinephrine and dopamine. Its mechanisms appear to be similar to those of dextroamphetamine. Furthermore, it is a racemic mixture comprised of the d- and l-threo enantiomers. The d-threo enantiomer is more pharmacologically active than the l-threo enantiomer 6.
Pharmacokinetics
The pharmacokinetics of the methylphenidate capsule (CD) methylphenidate hydrochloride formulation have been studied in healthy adult volunteers and in children with ADHDattention deficit hyperactivity disorder - a group of behavioural symptoms that include inattentiveness, hyperactivity and impulsiveness More 7.
Metabolism
Methylphenidate is hepatically metabolised. More specifically, it is rapidly and extensively metabolised by carboxylesterase CES1A1. Via this enzyme, methylphenidate undergoes de-esterification to ritalinic acid (a-phenyl-2-piperidine acetic acid, PPAA), which has little to no pharmacologic activity 6.
Half-life
- d-methylphenidate = 3 – 4 hours,
- l-methylphenidate = 1 – 3 hours,
- Ritalinic acid = 3 – 4 hours 6.
Elimination
After oral administration of an immediate release formulation of methylphenidate, 78% – 97% of the dose is excreted in the urine and 1% – 3% in the faeces in the form of metabolites within 48 – 96 hours. Only small quantities (<1%) of unchanged methylphenidate appear in the urine. Most of the dose is excreted in the urine as ritalinic acid (60% – 86%), the remainder being accounted for by minor metabolites 6.
Lethal dosage
The LD50the amount of a material, given all at once, which causes the death of 50% (one half) of a group of test animals. The LD50 is one way to measure the short-term poisoning potential (acute toxicity) of a material of methylphenidate in rats is 190mg/kg. In humans it is estimated to be 250mg+ for a 75kg (130lb) person 3.
Mechanism of action
Methylphenidate is a norepinephrine and dopamine reuptake inhibitor. It inhibits the Dopamine Transporter enzyme that pumps out dopamine from a synapse for reuse, this leads to increased activation of dopamine receptorsnerve endings that sense changes in the body More. It has a similar effect on the norepinephrine transporter. The latter is responsible for it’s feelings of energy and bodily stimulationcan be defined as any changes in a person's energy levels which are interpreted as stimulating and encouraging when it comes to movement and physical activities such as running, walking, cleaning, socializing, dancing, and climbing More, whilst the former accounts for euphoriafeelings of joy and happiness 1. Methylphenidate blocks dopamine uptake in central adrenergic neurons by blocking dopamine transport or carrier proteins. Methylphenidate acts at the brain stem arousal system and the cerebral cortex and causes increased sympathomimetic activity in the central nervous systembrain and spinal cord. Alteration of serotonergic pathways via changes in dopamine transport may result 6.
Signs of usage
- abnormal movements (similar to tourette’s),
- agitation and anxiety,
- altered sexual desire,
- chest pain,
- difficulty breathing,
- dilated pupils,
- dizziness,
- general nervousness,
- gastrointestinal distress,
- hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind,
- headaches,
- nausea and vomiting,
- OCD-like syndrome,
- social withdrawal,
- thoughts of suicide 8.
Effects
Short-term effects
- excitation,
- formicationa tactile hallucination involving the belief that something is crawling on the body or under the skin. More,
- facial flushing,
- perseverationexcessive repetition of meaningless tasks. More 8,
- wakefulness,
- exhilaration,
- agitation,
- headache,
- muscle twitches,
- dilated pupils,
- dry mouth,
- sweating,
- increased heart rate and body temperature,
- nausea 9.
Long-term effects
- delusions,
- grandiosity,
- hallucinationswhere someone sees, hears, smells, tastes or feels things that don't exist outside of their mind,
- mania,
- paranoiasuspicion, distrust or fear of other people,
- suicidal thoughts,
- violence 8.
Physical effects
- stimulationcan be defined as any changes in a person's energy levels which are interpreted as stimulating and encouraging when it comes to movement and physical activities such as running, walking, cleaning, socializing, dancing, and climbing More,
- appetite suppression,
- dehydration,
- increased heart rate,
- increased perspiration,
- teeth grinding 4.
Cognitive effects
- anxiety,
- cognitive euphoriastate of intense well-being, happiness, and excitement More,
- depression,
- irritability,
- time distortion,
- analysis enhancementbest described as a subtle to distinct enhancement of one's overall ability to process information and logically or creatively analyse concepts, ideas and scenarios. The experience of this leads onto deep and complex states of contemplation which often result in an abundance of new and insightful ideas. This gives the person a powerful ability to dissect and rationally analyse concepts and problems, allowing them to gain insights and reach new conclusions, perspectives and solutions which would have been otherwise difficult to conceive of. More,
- focus enhancement,
- increased music appreciation,
- memory enhancement,
- motivation enhancement,
- thought acceleration,
- thought organisation,
- wakefulness,
- cognitive fatiguethe decline in the ability to think effectively and maintain focus. More,
- motivation suppression,
- thought deceleration 4.
After effects
- anxiety,
- cognitive fatiguethe decline in the ability to think effectively and maintain focus. More,
- depression,
- irritability,
- motivation suppression,
- thought deceleration,
- wakefulness 4.
Minor effects
More common
- abdominal or stomach pain,
- headache,
- loss of appetite,
- nervousness,
- stuffy nose,
- trouble sleeping,
- unusually warm skin 7.
Less common
- anger,
- decreased appetite,
- dizziness,
- drowsiness,
- fear,
- irritability,
- muscle aches,
- nausea,
- runny nose,
- scalp hair loss,
- talking, feeling, and acting with excitement,
- vomiting 7.
Major effects
More common
- fast heartbeat 7.
Less common
- chest pain,
- fever,
- joint painJoint pain is unpleasant and difficult to deal with, in addition to the other effects of drug abuse on your body. Intravenous drug users in particular are at an increased risk for joint damage. More,
- skin rash or hivesThis is an allergic skin reaction causing localised redness, swelling, and itching. 7.
Rare
- black, tarry stools,
- blood in the urine or stools,
- blurred vision or other changes in vision,
- convulsionswhen your body shakes violently without you meaning it to,
- crusting, dryness, or flaking of the skin,
- muscle cramps,
- pinpointthe pupils are very small. More red spots on the skin,
- scaling, severe redness, soreness, or swelling of the skin,
- uncontrolled vocal outbursts,
- uncontrolled tics,
- unusual bleeding or bruising 7.
Incidence not known
- confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation,
- depression,
- feeling like surroundings are not real,
- jaundiceyellowing of your skin or the whites of your eyes,
- numbness of the hands,
- painful or difficult urination,
- pale skin,
- paleness or cold feeling in the fingertips and toes,
- red, irritated eyes,
- red, swollen, or scaly skin,
- seeing, hearing, or feeling things that are not there,
- severe or sudden headache,
- shortness of breath,
- sores, ulcers, or white spots on the lips or in the mouth,
- sudden loss of coordination,
- sudden slurring of speech,
- tingling or pain in the fingers or toes when exposed to cold,
- unusual behaviour,
- unusual tiredness or weakness,
- weight loss 7.
Abuse
Positive
Neutral
- reduced appetite,
- flushing of the face 3.
Negative
- increased body temperature,
- tachycardiarapid pulse rate,
- hypertensionhigh blood pressure,
- dehydration,
- paranoiasuspicion, distrust or fear of other people,
- racing thoughts
- insomniadifficulty in going to sleep or in getting enough sleep 3.
Overdose
- vomiting,
- agitation,
- uncontrollable shaking of a part of the body,
- muscle twitching,
- seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More,
- loss of consciousness,
- inappropriate happiness,
- confusiontrouble focusing, slow or disorganised thinking, poor short-term memory, unsure of time or place, or having difficulty following a conversation,
- hallucinating,
- sweating,
- flushing,
- headache,
- fever,
- fast, pounding, or irregular heartbeat,
- widening of pupils,
- dry mouth or nose 10,
- euphoriafeelings of joy and happiness,
- delirium,
- hyperpyrexiaan excessive elevation of body temperature above the average normal temperature. More,
- tachycardiarapid pulse rate,
- palpitations,
- cardiac arrhythmias,
- hypertensionhigh blood pressure 6.
Interactions
Although many drugs are safe on their own, they can become dangerous and even life-threatening when combined with other substances. The list below contains some common potentially dangerous combinations, but may not include all of them. Certain combinations may be safe in low doses of each but still increase the potential risk of death. Independent research should always be done to ensure that a combination of two or more substances is safe before consumption 4.
- 25x-NBOMe – Both the NBOMe series and this compound induce powerful stimulationcan be defined as any changes in a person's energy levels which are interpreted as stimulating and encouraging when it comes to movement and physical activities such as running, walking, cleaning, socializing, dancing, and climbing More and their interaction may cause severe side-effects. These can include thought loops, seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More, increased blood pressure, vasoconstrictionnarrowing of the blood vessels resulting from contraction of the muscular wall of the vessels (in particular the large arteries and small arterioles), increased heart rate, and heart failure (in extreme cases).
- Alcohol – It is dangerous to combine alcohol, a depressant, with stimulants due to the risk of excessive intoxication. Stimulants decrease the sedativeOne of a diverse group of drugs manufactured for medical purposes to relax the central nervous system. More effect of alcohol which is the main factor most people consider when determining their level of intoxication. Once the stimulanta drug that acts on the Central Nervous System, increasing some rates of function such as heart-rate wears off, the effects of alcohol will be significantly increased, leading to intensified disinhibition as well as respiratory depressionslowing the drive and effectiveness of breathing More. If combined, one should strictly limit themselves to only drinking a certain amount of alcohol per hour.
- DXM – This combination may cause increased heart rate and panic attacks.
- MXE – Increased heart rate and blood pressure may occur.
- Tramadol – This combination can increase the risk of seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More.
- MDMA – The neurotoxic effects of MDMASee Ecstasy More may be increased when combined with other stimulants.
- MAOIsMAOIs may be used to treat the symptoms of depression. More – This combination may increase the amount of neurotransmitters such as dopamine to dangerous or even fatal levels. Examples include syrian rue, banisteriopsis caapi, 2C-T-2, 2C-T-7, αMT, and some antidepressants 11.
- Cocaine – This combination may increase strain on the heart 4.
Dangerous
- αMT,
- Tramadol – Tramadol and stimulants both increase the risk of seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More.
- MAOIsMAOIs may be used to treat the symptoms of depression. More – MAO-B inhibitors can increase the potency and duration of phenethylamines unpredictably. MAO-A inhibitors with amphetamine can lead to hypertensive crises 5.
Unsafe
- DOx – The combined stimulating effects of the two can lead to an uncomfortable body-load, while the focusing effects of amphetamine can easily lead to thought loops. Coming down from amphetamines while the DOx is still active can be quite anxiogenicsomething that causes anxiety More.
- NBOMes – Amphetamines and NBOMes both provide considerable stimulationcan be defined as any changes in a person's energy levels which are interpreted as stimulating and encouraging when it comes to movement and physical activities such as running, walking, cleaning, socializing, dancing, and climbing More. When combined they can result in tachycardiarapid pulse rate, hypertensionhigh blood pressure, vasoconstrictionnarrowing of the blood vessels resulting from contraction of the muscular wall of the vessels (in particular the large arteries and small arterioles) and in extreme cases heart failure. The anxiogenicsomething that causes anxiety More and focusing effects of stimulants are also not good in combination with psychedelics as they can lead to unpleasant thought loops. NBOMes are known to cause seizuresthe outward effect can vary from uncontrolled jerking movement (tonic-clonic seizure) to as subtle as a momentary loss of awareness More and stimulants can increase this risk.
- 2C-T-x – Stimulants increase anxiety levels and the risk of thought loops which can lead to negative experiences. In extreme cases, they can result in severe vasoconstrictionnarrowing of the blood vessels resulting from contraction of the muscular wall of the vessels (in particular the large arteries and small arterioles), tachycardiarapid pulse rate, hypertensionhigh blood pressure, and in more extreme cases heart failure.
- 5-MeO-xxT – The anxiogenicsomething that causes anxiety More and focusing effects of stimulants increase the chance of unpleasant thought loops. The combination is generally unnecessary because of the stimulating effects of psychedelics.
- DXM – Both substances raise heart rate, in extreme cases, panic attacks caused by these drugs have led to more serious heart issues.
- PCP – This combination can easily lead to hypermanic states 5.
Withdrawal
- aggression,
- anxiety,
- depression,
- hunger,
- inability to concentrate,
- hypersomniaexcessive daytime sleepiness More,
- mood swings,
- paranoiasuspicion, distrust or fear of other people 8.
Drug testing
The timetable for detecting MethylPhenidate in the system is also dependent upon each individual’s metabolism, body mass, age, hydration level, physical activity, health conditions and other factors, making it almost impossible to determine an exact time MethylPhenidate will show up on a drug test 10.
The following is an estimated range of times, or detection windows, during which MethylPhenidate can be detected by various testing methods –
How long does methylphenidate stay in the urine?
MethylPhenidate can be detected in the urine for 1 – 2 days 10.
How long can methylphenidate be detected in blood?
There is currently no data available concerning the detection of MethylPhenidate in blood tests 10.
How long can a saliva test detect methylphenidate?
A saliva test can detect MethylPhenidate for up to 1 – 2 days 10.
How long can a hair test detect methylphenidate?
MethylPhenidate, like many other drugs, can be detected with a hair follicle drug test for up to 90 days 10.
Harm reduction
- abuse or binging on methylphenidate can lead to heavy comedown effects which can, in extreme cases, result in psychosis. Get some sleep every night,
- methylphenidate has been shown to be habit-forming, take care with repeated use,
- drinking alcohol (ethanol) also increases the blood plasma levels of d-methylphenidate by up to 40% 3.
As with all stimulants, remain hydrated and stay healthy 3.
History
Methylphenidate was first synthesised by the Ciba Pharmaceutical Company in 1944, and after human testing which began in 1954 it first became available in 1957 under the brand name ‘Ritalin’ – marketed as a treatment for several conditions including chronic fatiguea feeling of weariness, tiredness, or lack of energy. More, depression and narcolepsy.
In the 1960s it was popularly used to reverse the effects of a barbiturate overdose, meanwhile also being sold in combination with other substances in ‘health tonics’ – the most notable of which being ‘Ritonic’ 3.
Footnotes:
Methylphenidate, 2013, http://wiki.bluelight.org/index.php/Methylphenidate
Wren, A., Misusing prescription drugs, 2015, http://www.themix.org.uk/drink-and-drugs/drugs-and-your-body/misusing-prescription-drugs-9575.html
Methylphenidate, 2017, https://wiki.tripsit.me/wiki/Methylphenidate
Methylphenidate, 2017, https://psychonautwiki.org/wiki/Methylphenidate
Methylphenidate, 2017, http://drugs.tripsit.me/methylphenidate
Methylphenidate, 2017, https://www.drugbank.ca/drugs/DB00422
Methylphenidate, 2017, https://www.drugs.com/methylphenidate.html
Lautieri, A., Methylphenidate Abuse, 2017, http://drugabuse.com/library/methylphenidate-abuse/
Ritalin (an overview of abuse, addiction, signs, symptoms, treatment), 2016, https://www.addictions.com/ritalin-an-overview-of-abuse-addiction-signs-symptoms-treatment/
How Long Does Methylphenidate Stay in Your System?, 2016, https://www.verywell.com/how-long-does-methylphenidate-stay-in-your-system-80285
Gillman, P. K., Monoamine oxidase inhibitors, opioid analgesics and serotonin toxicityThis is when too much of something is taken over a short period of time More, British Journal of Anaesthesiathe state in which someone does not feel pain, usually because of drugs they have been given. More, 2005, 95, 4, 434-441, https://doi.org/10.1093/bja/aei210, https://www.ncbi.nlm.nih.gov/pubmed/16051647