Mode of actionEffect | Methylphenidate

Mode of actionEffect

Methylphenidate (Ritalin®) is a stimulant belonging to the group of amphetamines. As such it is also subject to the narcotics law. Methylphenidate has a similar effect to amphetamine or cocaine; the substances differ in their chemical structure and in their psychostimulant 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 field of ADHD and ADHD, treatment is primarily carried out with drugs containing the active substance methylphenidate.

Pain and feelings of exhaustion are reduced and the appetite is inhibited. It dispels the feeling of tiredness and has a mood-lifting and euphoric effect. In addition, methylphenidate increases alertness, performance and alertness level.The blood supply to the muscles is increased and the cells are better supplied by the simultaneous increase in the oxygen and sugar content of the blood.

Blood pressure and pulse are also increased. Methylphenidate inhibits the reuptake of dopamine into the presynaptic nerve cell. Dopamine is a messenger substance produced naturally in the body, which has a boosting and motivating effect.

Methylphenidate attaches itself to the dopamine transporter in the nerve cell and thus blocks it. If the transporter is blocked, more dopamine remains in the synaptic cleft. Its concentration is thus increased and its effect lasts longer.

The increased dopamine leads to a stronger stimulus at the receptor located at the postsynaptic nerve cell, which increases, among other things, the sympathetic tone. The term sympathetic tone refers to a state of complete excitation of the sympathetic nervous system. The body is set to “alert”, blood pressure and heart rate are increased.

Among other things, stress can trigger a sympathetic tonus. To a much lesser extent, methylphenidate ensures the release of catecholamines (dopamine, norepinephrine, adrenaline and their 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 serves as a neurotransmitter, i.e. it is a messenger substance that transmits excitation from one nerve cell to another. It also regulates the tone (tension) of the blood vessels and affects gastrointestinal activity. Methylphenidate preparations are considered to be first-choice drugs because of their good efficacy and – when used correctly in comparison to other drugs – their good tolerability.

When taken orally as a tablet, they are completely absorbed by the body. The drug has an average half-life of two hours, which means that the concentration of the drug is halved in the body within two hours. The maximum duration of action is about four hours.

After taking the drug with the active ingredient methylphenidate, the first effect is usually seen after half an hour. The active ingredient is then slowly broken down in the body. How quickly this breakdown takes place varies from one drug to another.

If a further intake is not taken in time, so-called rebound effects can occur, which are noticeable for example through increased tiredness or general worsening of symptoms. Methylphenidate is absorbed into the blood via the gastrointestinal tract and unfolds its effect by intervening in the brain metabolism. It leads to a release of certain messenger substances (hormones), which have an activating effect in various areas of the brain.

The hormone dopamine plays a special role in the mechanism of action. A high dopamine level conveys motivation, zest for life, courage, concentration and euphoria. If these feelings are artificially triggered by taking a substance like methylphenidate, addiction and dependency can quickly develop.

Young people and those who are mentally unstable are particularly at risk. People who suffer from great stress are also prone to develop addiction. In addition, the dopamine level can easily rise too high, which tends to have negative effects.

These include restlessness, headaches, tension, dizziness or abdominal pain. In addition, there can be an increase in blood pressure and heart rate, which can lead to cardiovascular stress. Contrary to widespread misconception, taking methylphenidate does not make you smarter.

Nevertheless, a positive effect on learning performance and concentration has been proven. This can be explained by the fact that the activity in areas of the brain that are not needed for learning is suppressed, allowing one to 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 dependence is also rather low. However, if methylphenidate is used without medical indication only to improve performance, both physical and mental health are at risk.