Methylphenidate

• Definition / explanation

Definition / explanation

Derived from the causes which, according to the current state of knowledge, may be the triggering factors for the development of ADD or ADHD, we know that “real” AD (H) D children, i.e. children with a clearly diagnosed attention deficit - Syndrome with or without hyperactivity, probably due to an imbalance of the messenger substances serotonin, dopamine and noradrenaline in the brain, which means that the transmission of information between the nerve cells of individual brain areas does not function properly.

This is exactly where the drug therapy of ADS or ADHD comes in. It aims to alleviate symptoms and enable the child to live and learn adequately.

In school, the fluctuating attention span, which is sometimes below average, can have negative effects on school grades, and symptoms of ADD are often accompanied by a weakness in reading and spelling and / or a weakness in arithmetic. In the area of ​​learning in particular, accompanying symptoms can thus also be alleviated or additionally treated through drug therapy.

An essential drug for Promotion of the ability to concentrate and perseverance with proven ADD / ADHD the active ingredient is methylphenidate.

Methylphenidate is an active ingredient in the psychotropic drugs division and is one of the so-called stimulants.
Unlike the changed behavior of an ADD child (typical Symptoms of ADD) Maybe lead to believe that there is no further calming or dampening of behavior of the child - this would certainly not be the goal with an ADD child. Rather, these drugs work improved stimulus transmission in the brain with the result that both the concentration as well as the Perseverance and attention of the child increased can be. As a result, a “dreaming” child appears “more alert”, while a child with typical ADHD symptoms Child may be “dampened” with the same medication.

It can thus be stated that Stimulants do not work equally in all affected children. The same preparations can - depending on the initial situation - cause different modes of action. In addition, there are children who do not respond at all to various drugs. This in turn can have several causes. Among other things, not every ADD or ADHD is treated with stimulants. Below it is made clear which messenger substances can incorrectly influence the transmission of stimuli in the brain and how adequately it can be treated.

The group of stimulants

The Group of stimulants, which also includes the active ingredient “methylphenidate” in many ADHD drugs, belongs to the superordinate one Group of psychotropic drugs. These are substances that primarily affect the activity of the central nervous system (CNS). In addition, they influence psychological functions such as mood, affectivity and emotionality, but also attention, impulsivity and drive.
Stimulants are those drugs that increase drive and release inhibitions in the therapy of ADD. In turn, stimulants can be divided into two groups:

1. Amphetamines
2. Non-amphetamines

Read more on the topic Psychotropic drugs

As mentioned earlier, at this point Not answered which drugs should be used in each individual case. The attending physician differentiates between first-choice drugs and second-choice drugs. Ritalin ®, or drugs with the active ingredient methylphenidate are known drugs and at the same time drugs of first choice.

Note amphetamines

Amphetamines have been covered by the Narcotics Act for some time. They are therefore prescribed on special prescriptions (so-called BTM prescriptions). Medicines that fall under the BTM law are subject to certain restrictions and / or bans on use. It is therefore also legally regulated how and to what extent a doctor can prescribe such narcotics. You must also note that special regulations apply to these medications when traveling abroad. This can work in the form of a doctor's certificate (in the case of member states of the Schengen Agreement) or it can be tied to specific provisions, which you can ask either at the responsible embassy in Germany or from your doctor

Mode of action / effect

Methylphenidate (Ritalin®) is a stimulating agent that belongs to the group of amphetamines. As such, it is also subject to the Narcotics Act. Methylphenidate works similarly to amphetamine or cocaine; the substances differ in their chemical structure and in their psychostimulating effect. It causes a short-term increase in physical performance: The drug increases nervous activity and stimulates the human organism. Stimulants (psychostimulants) are among the substances that stimulate the human organism and increase nervous activity. In the area of ​​ADD and ADHD, drugs are primarily used that contain the active ingredient methylphenidate.

Pain and feelings of exhaustion are reduced and the appetite is inhibited. It drives away the feeling of tiredness, has a mood-enhancing and euphoric effect. In addition, methylphenidate increases alertness, performance and alertness. The muscles are supplied with more blood and the cells are better supplied due to the simultaneous increase in the oxygen and sugar content in the blood. Blood pressure and pulse are also increased.

Methylphenidate inhibits the reuptake of dopamine into the presynaptic nerve cell. Dopamine is an endogenous messenger substance that increases drive and has a motivating effect. Methylphenidate attaches itself to the dopamine transporter in the nerve cell and thereby blocks it.If the transporter is blocked, more dopamine remains in the synaptic cleft. Its concentration is thus increased and its effects last longer. The increased dopamine leads to a stronger stimulus at the receptor, which is located on the postsynaptic nerve cell, which among other things increases the sympathetic tone. The term sympathetic tone is understood to mean a state of complete excitation of the sympathetic nervous system. The body is set to "alert", blood pressure and heart rate are increased.

Stress can, among other things, trigger a sympathetic tone. To a much lesser extent, methylphenidate is responsible for the release of catecholamines (dopamine, noradrenaline, adrenaline and its derivatives). In addition, the drug has an activating effect on the serotonin receptor (5-HAT 1A and 5-HT 2B). Serotonin is a hormone in the body and also acts as a neurotransmitter, i.e. it is a messenger substance that transmits excitation from one nerve cell to the other. It also regulates the tone (tension) of the blood vessels and affects gastrointestinal activity.

Methylphenidate preparations are considered to be the drugs of first choice due to their good effectiveness and - when used correctly compared to other drugs - rather good tolerance. When taken orally as a tablet, they are completely absorbed by the body. The drug has a mean half-life of two hours, which means that the drug's concentration in the body is halved within two hours. The maximum duration of action is about four hours.

After taking the drug with the active ingredient methylphenidate, the first effect usually appears after half an hour. The active ingredient is then slowly broken down in the body. How quickly this breakdown takes place varies from drug to drug. If it is not taken again in good time, so-called rebound effects can set in, which are noticeable, for example, through increased tiredness or general worsening of symptoms.

Effect in the brain

Methylphenidate is absorbed into the blood through the gastrointestinal tract and works by interfering with the brain metabolism. It leads to the release of certain messenger substances (hormones) that have an activating effect in different areas of the brain. The hormone dopamine plays a special role in the mechanism of action.

A high dopamine level conveys motivation, joie de vivre, courage, concentration and euphoria. If these feelings are artificially triggered by taking a substance such as methylphenidate, addiction and dependence can quickly develop. Young people and those who are mentally unstable are particularly at risk.

People who are under a lot of stress are also prone to develop an addiction. In addition, the dopamine level can easily rise too sharply, which is more likely to have negative effects. These include restlessness, headaches, tension, dizziness or abdominal pain.

In addition, it can lead to an increase in blood pressure and heart rate and thus to cardiovascular stress. Contrary to popular belief, taking methylphenidate doesn't make you smarter. Nevertheless, a positive effect on learning performance and the ability to concentrate was proven. This can be explained by the fact that the activity in areas of the brain that are not needed for learning is suppressed and one can thus concentrate better on one's tasks.

In people who have a disease that can be treated well with methylphenidate, hardly any side effects are to be expected in the correct dosage and the risk of addiction is also rather low. However, if you use methylphenidate only to improve performance without medical indication, you risk both your physical and mental health.

Retard medication

There are drugs, so-called Retard drugswhich, when taken only once a day, have the longest duration of action and prevent the rebound effect. The longer duration of action is due to their specific composition, which enables the active ingredient to be released gradually.

Different drugs

Except Ritalin ®, which is probably the best known ADS / ADHD - drug can be designated, there are other drugs with the same active ingredient (methylphenidate). As already mentioned, they are among the Stimulants and put the First line drugs represent.

The table is limited to essential drugs of ADD therapy (stimulants). Since some drugs are not permitted in Germany, but are administered elsewhere, we limit ourselves to those drugs that are also approved and allowed to be administered in Germany. In addition, the possible uses may vary in other countries. The table does not claim to be complete and corresponds to our level of knowledge. Any deviations are possible. The drugs mentioned are exemplary and not recommended:

Concerta® (Methylphenidate) psychoanaleptic, psychotropic drugs, Stimulants Children from 6 years and adolescents with a clear diagnosis of ADD

Equasym® (Methylphenidate) psychoanaleptic, psychotropic drugs, Stimulants Children from 6 years

Medikinet® (Methylphenidate) psychoanaleptic, psychotropic drugs, Stimulants Children from 6 years and adolescents with a clear diagnosis of ADD

Ritalin® (Methylphenidate) psychoanaleptic, psychotropic drugs, Stimulants Children from 6 years and adolescents with a clear diagnosis of ADD

Ritalin SR® (methylphenidate) psychoanaleptic, psychotropic drugs, Stimulants Children from 6 years and adolescents with a clear diagnosis of ADD

Captagon® (Fenetylline) psychoanaleptic, psychotropic drugs, Stimulants ADD in childhood: in Germany. No longer available since July 1st, 2003

Tradon® (Pemoline) sympathomimetic, Psychostimulants Children from 6 years and adolescents with a clear diagnosis of ADD

only available as raw material in Germany Amphetamine sulfate (is given as juice or in the form of tablets and produced in the pharmacy) Amphetamine preparation Children from 6 years and adolescents with a clear diagnosis of ADD

Side effects

In addition to the desired effects, drugs always have side effects that are expressed individually in different ways. A distinction must be made here between intensification of symptoms and “real” side effects. As the name suggests, intensification of symptoms is understood to mean an intensification of abnormalities that appeared before drug therapy. Such worsening of symptoms are not actually side effects.
Below you will find a list of examples of typical side effects that can occur with different frequencies. The list does not claim to be complete:

• decreased feeling of hunger

Methylphenidate inhibits appetite. However, within a few months the appetite suppressing effect wears off.

• Tendency to whine and tics

• Effects on the psyche

Methylphenidate can cause insomnia, headaches, dry mouth, feelings of anxiety, dizziness, or depression. Rare side effects are hallucinations, disorientation, or severe mood swings. Thoughts of suicide, including attempted suicide, have been observed when taking methylphenidate.

• Gastrointestinal effects

Taking methylphenidate orally without fluids may cause nausea or burning sensation in the esophagus, as well as abdominal pain and vomiting. This is because methylphenidate becomes somewhat acidic when it dissolves in the mouth or stomach area.

• allergic skin reactions

• Changes in blood count

• Skin changes

Other side effects of the preparation can be itching, increased sweating, dermatitis (inflammation of the skin), hives, flaky skin or hair loss.

• Cardiovascular changes

Those affected also report palpitations, heart stumbling, cardiac arrhythmias and changes in blood pressure.

• Growth retardation

Even with an adjusted dosage of methylphenidate, growth retardation and reduced weight gain can occur in children and adolescents. After stopping methylphenidate, this side effect will return to normal in most cases.

In children and adolescents, inflammation of the nasopharynx, fever or cough also occur.
As methylphenidate can make you dizzy, it may make it difficult to use machines or drive a car. It is generally permitted to drive a vehicle while taking methylphenidate.
Methylphenidate is not addictive with proper drug treatment. However, as a drug that affects the psyche, it should not be suddenly discontinued as this can lead to "withdrawal symptoms". Signs of this are hyperactivity, irritability, and depression.

If overdosed, methylphenidate is very dangerous. The CNS is overexcited. The consequences are convulsions, delirium and even coma. Blood pressure crises and cardiac arrhythmias can occur. Rapid medical treatment is urgently required.

In several studies and investigations it was questioned whether the active ingredient methylphenidate - for example in the form of the drug Ritalin ® - can lead to an increased risk of addiction. This does not seem to be the case even with long-term use. Some studies even confirm a lower risk of addiction.

Likewise, it does not currently appear to be proven that the intake - especially long-term intake - of methylphenidate increases the risk of Parkinson's disease (Parkinsson's disease).

Interactions

The following drugs may interact with methylphenidate. One should inform the attending physician about any medication intake. Caution should be exercised with these medicines:

• MAOIs
• Guanethidine
• Amantadine
• tricyclic Antidepressants
• Neuroleptics
• Anti-epileptic drugs
• Anticoagulants
• H2 blockers
• alcohol

Methylphenidate therapy in children

There are Guidelinesthat should be considered and adhered to in the case of drug treatment of ADD:

• Drug therapy should only be used in diagnostically clear cases.
• Drug therapy should only be considered from the age of six!
• As with other drugs, the stimulants can also have different side effects, which can vary depending on the drug being prescribed.
• The dose and the time of intake are initially prescribed in a standardized manner (based on body size and weight) and individually adjusted over the course of the first intake period (individual dosage).

Is there a prescription-free methylphenidate?

Methylphenidate is one of the amphetamines and therefore not only requires a prescription, but is also subject to the Narcotics Act in Germany. Nevertheless, there are numerous providers, especially on the Internet, from whom the drug can apparently be purchased legally, even without a prescription. However, from a medical and legal point of view, such a purchase is strongly discouraged.

Methylphenidate should only be used by people for whom it is indicated to treat a medical condition. In addition, you do not always have to fear a punishment for illegitimate purchase of the substance on the Internet, but you are violating a law that exists for good reason to protect against potentially harmful substances.

Read more on the topic here: Consequences of drugs

Methylphenidate and alcohol

Consuming alcohol in any form is not recommended when taking methylphenidate. There can be unpredictable side effects and side effects. The risk increases with the amount of alcohol drunk and life-threatening situations can arise.

For example, some people who have taken methylphenidate have already committed unintentional suicide after consuming large amounts of alcohol. In addition to these direct dangers, alcohol also interferes with the desirable effects of methylphenidate in treating conditions such as attention deficit disorder ADHD.

Methylphenidate (Ritalin®), which belongs to the group of psychotropic drugs, interacts with various drugs. In addition, psychotropic drugs and alcohol should not be taken together. By taking alcohol and methylphenidate at the same time, there is a risk of dopamine overdosing in the body. It could be shown that the breakdown of alcohol is more difficult or significantly delayed in some of those affected. Even the smallest amounts of alcohol should be avoided, as the interaction cannot be calculated and alcohol poisoning can result.

Dopamine is a messenger substance that acts as a neurotransmitter. As such, dopamine transfers excitation from one nerve cell to other cells. The hormone is responsible for the transmission of feelings and sensations. If the dopamine concentration in the brain is too high, too many impressions and feelings are perceived and the person concerned loses the ability to distinguish between important and unimportant impressions. Too high a dose of dopamine can lead to psychosis or schizophrenia. Dopamine acts as a sympathomimetic (it increases the effect of the sympathetic nervous system). It also promotes blood flow to the abdominal organs in the body and leads to increased blood flow to the kidneys. Excess dopamine can lead to high blood pressure, headaches, palpitations or sweating.

Read more on this topic under: Psychotropic Drugs and Alcohol

Drug tests

Methylphenidate can be detected in urine by a drug test. However, a special test strip that reacts to this substance must also be used for this. Even if methylphenidate is a derivative (descendant) of amphetamines, the drug test for amphetamines is negative in people who only take methylphenidate.

Drug tests can therefore be used to differentiate exactly which substances the person has ingested. However, it always depends on which substances the urine is tested for, as not all available test strips are used for every drug test. A drug test using the blood can also clearly demonstrate whether the person has taken methylphenidate or whether it is still in the body.

Prices

Since there is always talk of cost pressure in the healthcare system, I think it is important to find out the prices for drugs. (Prices are exemplary and not recommended):

Concerta® 18 mg retard 30 tablets (N1) € 67.15

Concerta® 36 mg retard 30 tablets (N1) € 81.58

Equasym® 5 mg 20 tablets (N1) € 13.50

Equasym® 10 mg 20 tablets (N1) € 15.31

Equasym® 20 mg 20 tablets (N1) € 20.13

Medicinet® 10 mg 20 tablets (N1) € 15.75

Medicinet® 10 mg 50 tablets (N2) € 24.81

Tradon® 20 mg 20 tablets (N1) € 13.35

Status: January 2004

Other forms of drug treatment

Further drug treatment options exist in therapy with Antidepressants / antidepressants
With regard to antidepressants, a distinction is made between:

1. MAO inhibitors
2. NARI (Selective Norepinephrine Reuptake Inhibitor)
3. RIMA (reversible monoamine oxidase inhibitor)
4. SNRI (Serotonin - norepinephrine - reuptake inhibitor)
5. SSRI (selective serotonin reuptake inhibitor)

Read more on the topic: Psychotropic drugs

Other ADD / ADHD therapies

1. General information on dealing with the ADD / ADHD child, especially information for parents on the therapy of ADD or therapy of ADHD in the home and family.
2. The psychotherapeutic and curative education therapy with their different forms.
3. Nutritional therapy.

As already mentioned, therapy should always be linked to several factors at the same time. An exclusively drug therapy can work, but it does not necessarily affect all areas.
Many of the package inserts for the above Medicines therefore also refer to an overall therapeutic strategy that should be carried out alongside drug therapy.