Effects of benzodiazepines
 
Benzodiazepines, commonly known as benzos, have a calming and muscle-relaxing effect. They are also anxiolytics and antispasmodics (antiepileptics) and facilitate sleep. 

Benzodiazepines produce these effects by binding to the binding sites (receptors) of the body's neurotransmitter GABA (gamma-aminobutyric acid). GABA makes it difficult for neurons to get excited, thereby preventing the transmission of nerve signals. Benzodiazepines increase the effects of GABA. This makes neurons even harder to excite.

The corresponding effect depends on which region of brain neurons is suppressed:

• Anxiolytic: Benzodiazepines inhibit nerve cells in the limbic system, a part of the brain that processes emotions such as fear.
•      calming and sleep-promoting: these effects are caused by benzodiazepines by inhibiting nerve cells in the brainstem.
•      Muscle-relaxing (muscle-relaxing): This effect is mainly due to the inhibition of the nerve cells in the spinal cord.
•      Antispasmodic (anticonvulsant): During seizures, excited nerve cells predominate.
•     Benzodiazepines dampen the nerve cells and correct the imbalance in the brain.
•      hypnotic (amnestic): benzodiazepines trigger anterograde amnesia. The patient no longer remembers, for example, surgical interventions during the effect of the drug.

In addition to the classic benzodiazepines, there are also benzodiazepine-like active ingredients, so-called Z-substances (Z-drugs). They also affect the transmitter's GABA docking sites. The best-known Z-remedies are zolpidem and zopiclone

Basically, all benzodiazepines have the same effect, but differ in duration or strength. With regard to the duration of action, substances differ according to the so-called half-life. This shows how much of the active ingredient has left the body. There are ultra-short-acting, short-acting, medium-acting, and long-acting benzodiazepines. Very short-acting and short-acting benzodiazepines. 

When benzodiazepines are “very short,” they have a half-life of less than five hours. Because of this, doctors often use them to put people to sleep or to calm them down before anesthesia. For example, midazolam or triazolam. 

With short-acting benzodiazepines, it takes up to 10 hours for the body to eliminate half of these active substances. This group includes lormetazepam or brotizolam. Intermediate-acting benzodiazepines.

After 12–24 hours, half of the amount of active ingredient is eliminated from the body. They are suitable, for example, for problems sleeping at night, i.e., when someone wakes up very often. Intermediate-acting benzodiazepines include:

Long-acting benzodiazepines

When the body breaks down some of these substances, breakdown products are produced that also have an effect. This increases their half-life. Long-acting benzodiazepines halve after 24 hours. Doctors sometimes use them for high voltage, anxiety, and epilepsy. Long-acting benzodiazepines include B.z.

• Clobazam
• Clonazepam
• Flunitrazepam
• Nitrazepam
• Flurazepam
• Diazepam

​Performance

Power is referred to as “power”. The stronger the corresponding benzodiazepine binds to GABA receptors, the greater its effect. The doctor needs less active ingredient to achieve a sufficient effect. This also means that the more often you take a certain active ingredient, the stronger its effect.

Potency is divided relative to the benzodiazepine indiazepam. That means you are administering an amount of benzodiazepine that is about as potent as, or equal to, ten milligrams of diazepam. The lower this equivalent dose, the stronger and more effective the benzodiazepine.

Side effects of benzodiazepines

Side effects are common, especially at the beginning of treatment. Patients are often tired, have headaches or dizziness. The symptoms can last all day and appear as a so-called hangover effect. 

The muscle relaxant effects of benzodiazepines lead to unsteady walking and an increased risk of falling. Therefore, caution should be exercised, especially in the elderly. 

Benzodiazepines can also cause memory loss shortly after ingestion. The patients no longer remember what they did during this time. 

Note:
If you take benzodiazepines at night, make sure you get 7–8 hours of sleep. This will help avoid dizziness or tiredness the next day. 

So-called paradoxical reactions are possible, especially in older patients or children. Therefore, the desired effect does not occur, but rather the opposite. This means that those affected are restless, irritable, suffer from hallucinations or sleep poorly.

Dosage Forms Benzodiazepines

Benzodiazepines are available in a variety of dosage forms. Which one is most appropriate depends on the patient and their condition. 

Benzodiazepines are often given to patients in tablet form. Some tablets release their active ingredient with a delay and are referred to as so-called long-acting tablets. 

Benzodiazepines in the form of drops or juices are especially good for people who have trouble swallowing. In addition, liquid dosage forms can be dosed more precisely and thus adjusted to the patient's weight, for example.

For acute attacks, prefilled benzodiazepine syringes are placed in the cheek pouch. The active ingredient then enters the blood directly through the oral mucosa and begins to take effect quickly. Benzodiazepines as nasal sprays enter the bloodstream via the nasal mucosa. 

For patients suffering from nausea and vomiting, benzodiazepines are also suitable in the form of suppositories or rectal solution. The active substance enters the bloodstream via the intestinal mucosa, and the effect sets in quickly. -

In hospital, benzodiazepines are often given directly into a vein (intravenously) or into a muscle (intramuscularly). Fields of application Benzodiazepines.

Benzodiazepines are mainly used as tranquilizers or sleep aids. The effect of the individual active ingredients varies in strength. Depending on the duration and intensity of the effect, the corresponding benzodiazepines are used:

• as a sleep aid when other measures have not been sufficiently effective
• to calm nervous or restless patients before surgery or examinations (premedication)
• to calm ventilated patients in the intensive care unit
• to induce anesthesia
• after operations (postoperative)
• seizures or certain forms of childhood epilepsy
• in patients who suffer from states of anxiety, tension or excitement

Benzodiazepines as medication

Benzodiazepines are often misused as drugs. Those affected combine them with alcohol or other antidepressants and thus increase the depressive effect. However, it also increases the risk of serious side effects. — Interactions with benzodiazepines

Benzodiazepines mainly interact with active ingredients that also have a depressant effect. These include, for example, opioids, painkillers, antidepressants, or allergy medication (antihistamines). Alcohol also increases the dampening effect. — Contraindications of benzodiazepines

Benzodiazepines can aggravate existing conditions or make concomitant medications dangerously worse. In such cases, patients should not take active substances:

Ataxia: When damaged nerves or areas of the brain prevent movement and coordination, benzodiazepines can make it worse. 

Myasthenia gravis: Because benzodiazepines relax muscles, they are not suitable for patients with the autoimmune disease myasthenia gravis, which weakens muscles.

Severe lung disease: People with, for example, advanced COPD should use benzodiazepines very carefully. Benzodiazepines can slow your breathing (respiratory depression) and make breathing problems worse, especially when combined with opioids. 

Known dependencies: Benzodiazepines become addictive after a short period of regular use. Patients who are or were addicted to alcohol, drugs, or medication have a particularly high risk of addiction. 

Allergy: If you are hypersensitive to benzodiazepines or other ingredients in the drug, the doctor will select a different preparation.

Delivery rules

Benzodiazepines are considered narcotics in Germany and psychotropic substances in Austria and Switzerland. Such funds are subject to strict distribution cones. However, individual active ingredients are exempt from this in certain quantities or dosage forms.

This means that such benzodiazepines do not require a prescription, but the drug can be obtained from the pharmacy with a standard prescription. The exception is when doctors want to prescribe benzodiazepines to patients addicted to alcohol or drugs: A prescription is then required anyway.