Barbiturates: Effects, Uses & Risks

Barbiturates were once considered miracle drugs and were used extensively. Today, their use is severely restricted and they are considered dangerous. There are a number of good reasons for this. The following overview of the effects of barbiturates on the body, their uses, and risks and side effects shows why.

What are barbiturates?

Barbiturate is the generic term for a variety of different drugs that have narcotic, hypnotic, anticonvulsant, and sedative effects. Barbiturate is the generic term for a variety of different drugs that have narcotic, hypnotic, anticonvulsant, and sedative effects. Their name is derived from barbituric acid, from which they form derivatives. The chemist Johann Friedrich Wilhelm Adolf Ritter von Baeyer successfully produced barbituric acid for the first time in 1864. On this basis, Hermann Emil Fischer then developed the first barbiturate with a sedative effect in 1903 and named it Barbital. Since this development, barbiturates have been among the most widely used sleeping pills and sedatives in German-speaking countries for many decades. However, because they are very quickly addictive and there have been many cases of poisoning due to overdoses and misuse, they have no longer been approved as sleeping pills and sedatives in Germany since the early 1990s. Since then, they have only been used in the treatment of epilepsy and as anesthetics during surgery. There are three types of barbiturates: short-acting, which have an effect for only a few minutes; medium-acting, whose effect lasts for several hours; and long-acting, whose effect lasts for many hours. Thus, the classification is based on the duration of each effect.

Pharmacological action

The pharmacological effects of barbiturates on the body and organs are enormously complex. They exert their effects via various receptors in the organism, the so-called GABA-A receptors. These are located in the nerve cells and bind the neurotransmitter γ-aminobutyric acid there. In this way, they directly influence the messenger substances responsible for the transmission of stimuli and excitation between nerve cells. After the barbiturate binds to these receptors, they practically take over their task and act as agonists to control signal transmission between individual nerve cells. They practically mimic γ-aminobutyric acid and take over its functions. In this way, barbiturates can inhibit or suppress pain signals, for example. In addition, the dosage of the barbiturate plays an important role in the effect. At lower doses, for example, they inhibit the AMPA receptor, which has an excitatory effect, and thus provide sedation. In higher doses, they also inhibit sodium channels, which in turn are important for many other processes in the body. Ultimately, barbiturates lead to total anesthesia.

Medical application and use

In the past, barbiturates were prescribed mainly as sleep aids or sedatives. However, as experience and studies soon revealed the extremely high addictive potential as well as the dangerously high toxicity, these uses were eventually banned. Barbiturates were replaced by far less dangerous drugs such as benzodiazepines. Because of this fact, barbiturates are now basically used for only two applications: as an anesthetic and as an antiepileptic. As an anesthetic, it is used in the form of thiopental in the induction of anesthesia. The short-acting barbiturate thiopental has a duration of action of just under 10 minutes and acts enormously quickly, which is why it is injected intravenously into the patient to induce anesthesia. In the treatment of epilepsy, the long-acting phenobarbital is used, which is effective for around 10 to 18 hours. Because of its anticonvulsant effect, it is popular for both preventing and treating seizures associated with epileptic disorder. Furthermore, it can also be used to combat seizures triggered by exposure to certain poisons such as strychnine or DDT. In Switzerland, certain barbiturates such as pentobarbital are also used in active euthanasia, which is permitted there. In veterinary medicine, it is used as an agent for euthanasia.

Risks and side effects

As mentioned earlier, the risks and side effects of taking barbiturates are enormous. Regular use leads very quickly to severe dependence.Withdrawal is difficult and associated with sometimes severe symptoms such as anxiety, seizures and overexcitability. The liver also reacts to regular use and breaks down the barbiturate more and more quickly over time, which is why the effect becomes weaker and shorter. In the course of this, other drugs are also broken down more quickly and therefore no longer work properly. Too high a dosage can also lead to severe poisoning, with symptoms ranging from impaired consciousness and dizziness to nausea, vomiting, amnesia and coma. The worst toxic effect, however, is central respiratory paralysis and cardiac arrest, which, without immediate treatment, result in the brain being deprived of oxygen and ultimately death. Other sedating agents such as alcohol or opiates also potentiate the effects of barbiturates. Because of these severe side effects, barbiturates are now subject to the Narcotic Prescription Regulation (BtMVV). Although barbiturates act very quickly and effectively, they are unfortunately associated with many, sometimes even life-threatening, risks and side effects that far exceed their inherently positive properties. For this reason, their use is now prohibited for understandable reasons, with only a few exceptions. Self-medication is therefore strongly discouraged.