Adrafinil: Effects, Uses & Risks

The drug Adrafinil was launched in 1985 by the pharmaceutical company Cephalon. The drug is used to treat narcolepsy and sleep disorders associated with narcolepsy.

What is adrafinil?

The drug is used to treat narcolepsy and sleep disorders associated with narcolepsy. The preparation Adrafinil belongs to the group of psychostimulant substances that have a stimulating effect on the organism. Its effect is similar to that of morphine-like substances, but Adrafinil differs significantly from this group of active substances in its molecular structure. The preparation is a prodrug. These are substances that have only a slight pharmacological effect. It is only during metabolism that the active substance modafinil is released, which is the main metabolite in adrafinil. Therefore, both preparations are identical in terms of their effect on the human organism. The big difference is that Adrafinil develops its effect only after a certain time delay. The drug was developed by the U.S. pharmaceutical and biotechnology company Cephalon. Because adrafinil, like modafinil, has a performance-enhancing effect, it is considered a banned doping substance.

Pharmacological effect

The mechanism of how adrafinil acts on the body and its organs has not been fully researched. However, some studies have found that after administration of adrafinil, the concentration of various neurotransmitters such as serotonin, norepinephrine, and dopamine increases significantly. It is assumed that the active part of adrafinil, i.e. modafinil, stimulates the transmission of chemical or electrical excitations in the nerve cells. A possible explanation for this effect has been found out in various tests with the organism of a mouse: Here it was found that after the administration of adrafinil, there is an increased release of histamine in the central nervous system. Histamine is a neurotransmitter that plays an important role as a neurotransmitter in a large number of organisms. In other mammals and in humans, histamine plays an important role in allergic reactions as well as in the immune system. Here, histamine is one of the messenger substances that cause tissue to swell during inflammation. Histamine also plays an important role in the central nervous system. Here it is particularly important in appetite control and in controlling the sleep-wake cycle. Histamine is formed during metabolism from the amino acid histidine, and is subsequently stored primarily in nerve cells.

Medical application and use

Adrafinil is used exclusively for the treatment of sleep disorders. It is most widely used in the treatment of narcolepsy and conditions associated with narcolepsy. This sleep disorder, popularly known as sleeping sickness, is caused by a disturbance in the sleep-wake rhythm. The causes of narcolepsy, which is estimated to affect about 40,000 people in Germany, are still largely unknown. Typical symptoms of narcolepsy include excessive daytime sleepiness, an almost complete inability to move during sleep (sleep paralysis), emotion-related and brief loss of muscle tension, and hallucinations in a hypnagogic state. Other symptoms include disturbed night sleep with many and sometimes long interruptions, as well as concentration and memory disorders. However, the latter symptoms are more likely to be a consequence of daytime sleepiness. A diagnosis of narcolepsy is difficult in that the symptomatology can vary greatly from individual to individual. In addition, many narcolepsy patients also suffer from other impairments, such as sleep-related breathing disorders or restless legs syndrome. Although this is actually a neurological disorder, it is classified as a sleep-related movement disorder. Adrafinil is administered to narcolepsy patients primarily to suppress the symptom of daytime sleepiness. The other symptoms are sometimes treated with antidepressants.

Risks and side effects

Adrafinil should not be given to patients with certain pre-existing conditions, such as addiction or liver or kidney dysfunction. The reason: side effects such as hepatotoxicity or DRESS syndrome may occur.This is a serious reaction of the immune system to the active substance, in which various organs such as the liver, kidneys or lungs can be attacked. If side effects occur, they are often manifested by allergic reactions of the skin. Thus, the skin disease Stevens-Johnson syndrome and Lyell syndrome will also be listed among the side effects of Adrafinil.