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Benzodiazepine – Effect, Application & Risks

Benzodiazepines

Benzodiazepines are special chemical compounds (compounds of a benzene ring with a diazepine ring) that have psychotropic effects in the body. They are used in medicine as anxiolytic (anxiolytic), central muscle relaxant, calming (sedative) and sleep-inducing (hypnotic) drugs. The antispasmodic (anticonvulsant) effect of some benzodiazepines also explains their use as antiepileptics .

Was sind Benzodiazepine?

All benzodiazpines are derivatives of the same basic chemical structure. This is a bicyclic ring system made up of a benzene and diazepine ring. The benzene ring is the simplest representative of the benzenoid, aromatic hydrocarbons with the molecular formula: C6H6.

A diazepine ring is fused (connected by condensation) to these. The diazepine ring is a seven-membered, unsaturated ring with 2 nitrogen atoms. The main drugs used are diazepine rings with nitrogen atoms in the 1st and 4th position in the ring – so-called benzo-1,4-diazpines. Another six-membered ring is connected at the 5th position of the diazpin ring, but not by an annulation.

Due to different binding sites in the area of ​​the benzene ring, on the diazepine ring and the additional six-membered ring, different active ingredients are created, some of which have different effects.

Pharmacological action

Benzodiazepines have an activating effect on the gamma-aminobutyric acid (GABA) receptor A by binding and thus increase the effect of the neurotransmitter GABA . GABA-A receptors are found throughout the brain and spinal cord . The binding increases the probability of opening of the GABA-A receptor, which leads to an increased influx of chloride into the nerve cell . This hyperpolarizes the neuron membrane, resulting in reduced excitability.The GABA-A receptor consists of 6 subunits, with classic benzodiazepines showing affinity for 4 of these subunits (alpha1, alpha2, alpha3 and alpha5). An effect on the receptor is only possible if the neurotransmitter GABA is present together – these are allosteric modulators and not agonists in the narrower sense. The effect is stronger on those synapses that contain little GABA. There is an activity-dependent effect. This means that weak transmitter responses are amplified disproportionately. This could also be responsible for the specific effects of benzodiazepines.

Benzodiazepines work in the human body:

  • Anxiolytic (anxiolytic)
  • Antispasmodic (anticonvulsant)
  • Muscle relaxant (muscle relaxant)
  • Calming (sedative)
  • sleep-promoting (hypnotic)
  • Amnestic (memory lapse during duration)
  • Slightly mood-enhancing (note: if you have an underlying depressive illness, this can also get worse)
  • Partly euphoric (dose-dependent and dependent on the administration interval)

High doses of benzodiazepines do not increase the maximum effect. However, there is a reduction in the dose of GABA required to trigger the maximum effect. So the dose-response curve of gamma-aminobutyric acid is shifted to the left.

Medical Application & Use

Because of the effects that can be achieved, benzodiazepines are mainly used in emergency medicine and in psychiatry . However, the possible areas of application are clearly limited due to the high potential for dependency and the severe respiratory depression side effects .

With regular intake from about 8 weeks, withdrawal symptoms occur when the drug is stopped. It is therefore recommended not to use benzodiazepines for longer than 4 weeks (provided that the indication is strict and the dosage is as low as possible).

An exception are the antiepileptic benzodiazepines, which often have to be taken for life. The active ingredients diazepam and lorazepam are particularly suitable as drugs of first choice for the treatment of acute epileptic seizures .

In psychiatry, benzodiazepines are primarily used in the treatment of anxiety and restlessness . They are also often used as acute medication for panic attacks .

Benzodiazepines also have a firm place in the treatment of alcohol withdrawal symptoms. Benzodiazepines can also be used in the short-term therapy of problems falling asleep and staying asleep. Due to the potential for dependency, however, other substance groups (such as antihistamines ) are increasingly preferred.

In emergency medicine, benzodiazepines are also used to induce anesthesia and as part of pain therapy (analgosedation). In selective surgeries, pre-surgery premedication is often with a benzodiazepine, such as midazolam , to relieve the patient of tension and any anxiety before the procedure.

Risks & side effects

Benzodiazepines have varying degrees of respiratory depression by dampening the respiratory center in the elongated spinal cord . Although respiratory depression is dose-dependent, life-threatening intoxications from benzodiazepines alone are rare. However , there is a significantly increased risk of fatal respiratory failure , especially in the case of mixed intoxications together with alcohol or other CNS -active preparations (e.g. opiates ) .The interaction between benzodiazepines and alcohol is referred to as a so-called cross-tolerance due to the similar effect on the GABA-A receptor. The often practiced dose increase as a response to the increased tolerance leads to increased side effects.

The addictive potential of benzodiazepines is reflected in the severe physical dependence that occurs even at therapeutic doses. So it’s not surprising that benzodiazepines have the highest abuse rates in the world. Disorders of memory function , behavioral disorders , psychomotor slowdown and paradoxical effects (increase in anxiety and/or sleep disorders ) then occur under the medication.

Contraindications to taking benzodiazepines include:

  • Myasthenia gravis (disorder of the neuromuscular transmission of impulses)
  • Ataxia (impaired movement coordination)
  • angle-closure glaucoma ( glaucoma )
  • Existing addiction (also in the history)
  • Allergy to the active substance
  • Sleep apnea syndrome (pauses in breathing during sleep )
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Hello! I am Lisa Newlon, and I am a medical writer and researcher with over 10 years of experience in the healthcare industry. I have a Master’s degree in Medicine, and my deep understanding of medical terminology, practices, and procedures has made me a trusted source of information in the medical world.