Benzodiazepines: Effects, Uses & Risks

Benzodiazepines belong to a substance class of characteristic bicyclic organic compounds that are frequently used in medicine as sedatives or sleeping pills. Their action is based on the enhancement of so-called inhibitory neurotransmitters. However, frequent applications of benzodiazepines can lead to dependence conditions.

What are benzodiazepines?

Benzodiazepines belong to a substance class of characteristic bicyclic organic compounds that are commonly used in medicine as sedatives or sleeping pills. All benzodiazepines have a basic bicyclic structure consisting of a seven-membered unsaturated ring to which a benzene ring is also fused. The unsaturated seven-membered ring contains two nitrogen atoms. Some representatives of these compounds have great importance as drugs. All benzodiazepine-based drugs have another benzene ring attached at the 5-position to the unsaturated ring and are called 1H-benzo-1,4-diazepines according to chemical nomenclature. The individual 1H-benzo-1,4-diazepines often exert a sedative effect and are therefore frequently used as tranquilizers or sleep-promoting agents. Depending on other functional groups, there are a relatively large number of drugs in this substance class. All benzodiazepines have a depressant effect on the nervous system. However, they differ in the duration and intensity of the effect. This is determined by the half-life, i.e. the decomposition time of the individual substances in the body.

Pharmacological effect

Benzodiazepines do not act directly, but they potentiate the effects of GABA (gamma-amino-butyric acid) by affecting GABA receptors. GABA is an inhibitory neurotransmitter that, when bound to the receptor, inhibits nerve excitation by increasing the influx of chloride ions into nerve cells. This inhibitory or inhibitory influence results in an overall calming of nerve function. The benzodiazepines alter the GABA receptors so that they can better bind GABA, for example, thus increasing its effectiveness. The duration of efficacy depends, of course, on the half-life of the corresponding benzodiazepine. In general, benzodiazepines have anxiety-relieving, relaxing, aggression-dampening, and sleep-promoting effects. Depending on the substance used, one or the other effect is dominant. High doses or sensitivity to benzodiazepines may also cause fatigue, drowsiness, low mood, or headache. Many benzodiazepine-based drugs with different patterns of action have been developed to cover the widest possible range of uses with few side effects. Two parameters are crucial for the use of benzodiazepines, onset of action and duration of action.

Medical application and use

The mode of action as a modulator for the inhibitory neurotransmitter GABA opens up a wide range of applications for the substance class of benzodiazepines. Thus, benzodiazepines are frequently used for anxiety disorders, restlessness, sleep disorders, states of agitation, muscle tension, and epilepsy. Benzodiazepines have also proven effective in schizophrenia and alcohol withdrawal. But benzodiazepines are also available for general use as sedatives and sleeping pills. Benzodiazepines are the most commonly used sedatives or sleeping pills. In Germany, up to 17 percent of the population takes benzodiazepine preparations each year. The choice of the right drug depends on the underlying disorder. The relationship between onset and duration of action influences certain side effects. For example, in the case of difficulty falling asleep, one wants to achieve a rapid effect. However, the duration of action should not be too long in order to avoid tiredness and drowsiness after sleep. For sleep-through problems, active ingredients with a medium duration of action are appropriate. However, if anxiety disorders, epilepsies or muscle tension are to be treated, active ingredients with a long duration of action are desirable. Benzodiazepines are also often used to relieve anxiety before surgery or diagnostic procedures, such as gastroscopy or colonoscopy. All benzodiazepine-based medications require a prescription and are usually administered in tablet form.

Risks and side effects

However, benzodiazepines also have significant side effects if used for too long or too intensively.At high concentrations of benzodiazepines, memory, perception, and reaction disorders may occur. Headache and drowsiness have also been reported. Too long treatment with benzodiazepines often leads to habituation effects and tolerance formation. Therefore, there is a risk of drug dependence. After prolonged use, even rapid discontinuation of the medication can lead to psychological disturbances and even suicidal tendencies. For these reasons, treatment with benzodiazepines should not be exaggerated. In particular, concomitant use of benzodiazepines with alcohol or barbiturates is very dangerous and often causes acute and long-term exacerbation of mental illness.