Methylphenidate: Effects, Uses & Risks

Methylphenidate is chemically related to amphetamine and has a stimulant effect as a drug. It is also known by the trade name Ritalin. The drug is mainly used for the treatment of attention-deficit/hyperactivity disorder, known as ADHD, and narcolepsy.

What is methylphenidate?

The drug is mainly used for the treatment of ADHD. Like amphetamine, methylphenidate has a short-term performance-enhancing and stimulating effect, suppressing physical warning functions such as pain or fatigue. It also inhibits appetite. In certain mental disorders, these properties can have a short-term positive effect, so methylphenidate can also be used as an element of treatment for these conditions. Methylphenidate is rapidly absorbed by the body. It is irrelevant whether it is absorbed at the same time as food. It is up to 30 percent bioavailable, reaching its maximum plasma concentration after about 2 hours. The half-life of its elimination from plasma is again 2 hours. Methylphenidate exerts its full effect for 4 hours before it is completely degraded.

Pharmacologic effects

The action of methylphenidate is due to its inhibitory effect on the transporters of the neurotransmitters dopamine and norepinephrine. These transporters are responsible for the reuptake of these neurotransmitters into presynaptic neurons from the synaptic cleft. Since reuptake is inhibited under the influence of methylphenidate, the concentration of dopamine and norepinephrine in the synaptic cleft remains elevated for a longer period of time. This also means that the two neurotransmitters can maintain their stimulatory effect on the sympathetic nervous system for this time. The sympathetic nervous system in turn ensures an increased readiness of the body to perform, and this is also associated with increased alertness. Thus, depending on the initial situation, different and seemingly contradictory effects occur. In introverted persons, the stimulation leads to increased activity, while in persons suffering from attention disorders and at the same time undirected hyperactivity, a calming with an increase in the ability to concentrate occurs. Since the sympathetic nervous system is the antagonist of the parasympathetic nervous system, the body functions related to the activity of the parasympathetic nervous system are reduced. This affects intestinal activity, the hunger center, and the secretory and sweat glands.

Medical use and application

Methylphenidate is used primarily for two symptom complexes, ADHD and narcolepsy. While ADHD focuses on hyperactivity with attention deficit disorder, the main symptoms of narcolepsy are the extreme urge to sleep and fatigue. Both disorders can be positively influenced with methylphenidate in a well-modulating way in combination with other treatment methods. Since the causes of both disorders are extremely complex, treatment with methylphenidate alone is not sufficient. Only symptoms can be treated, but not the causes. For example, ADHD is based on a dysregulation of signal transduction due to uncoordinated different activities of certain neurotransmitters in different areas of the brain. Methylphenidate regulates and normalizes these activities during the period of its action. It should also be noted that on the basis of the symptoms reduced by medication, psychotherapeutic treatment of ADHD brings better results. Especially children from 6 years of age with the symptoms of ADHD respond well to the combined treatment methods. By dampening hyperactivity and increasing attention with medication, for example, these children’s performance at school can be improved, which in turn has a positive effect on their self-esteem. Therefore, the treatment of ADHD with methylphenidate can only be considered in the overall context. In narcolepsy, methylphenidate is often prescribed to reduce daytime sleepiness.

Risks and side effects

Taking methylphenidate must always be under medical supervision because its use can also cause many side effects. Thus, depending on the reaction to this drug, it is necessary to adjust the dosage individually. Narcolepsy patients may often experience concentration disorders, heavy sweating and sensitivity to noise.In general, a variety of psychological and neurological side effects of different types may occur. Cardiovascular disorders, such as cardiac arrhythmias, elevation of blood pressure, and even heart attacks or strokes are also observed. The multitude of different, sometimes even contradictory side effects, indicates the complex processes that take place when drugs affect the regulatory mechanisms in the body.