Lorazepam

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Benjamin Clanner-Engelshofen is a freelance writer in the medical department. He studied biochemistry and pharmacy in Munich and Cambridge / Boston (USA) and noticed early on that he particularly enjoyed the interface between medicine and science. That is why he went on to study human medicine.

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Lorazepam is one of the most important active ingredients in the class of benzodiazepines, a group of sedatives. It is mainly used against anxiety disorders, but also has a calming, antispasmodic and muscle relaxing effect. The active ingredient is widely used because of its broad spectrum of activity and many years of application experience. Here you can read everything you need to know about the effects of lorazepam, dosage and use.

This is how Lorazepam works

Lorazepam is a drug from the group of benzodiazepines and as such has an anxiolytic, sedative, muscle-relaxing and anticonvulsant effect.

Like all benzodiazepines, Lorazepam wikr directly at the connection points between the nerve cells in the brain. At these so-called synapses, the nerve cells communicate with each other via messenger substances (neurotransmitters).

Some messenger substances trigger excitation (in the form of an electrical potential) in the target cell, while others inhibit the target cell's ability to excite. The latter are also called inhibitory neurotransmitters, the most common and important messenger substance in this class being GABA (gamma-aminobutyric acid).

Lorazepam binds to a sub-form of the GABA binding site (GABA-A receptor) and increases the probability of opening in the presence of GABA. In this way the inhibitory effect of GABA is increased.

Uptake, breakdown and excretion

After ingestion, lorazepam is quickly and almost completely absorbed into the blood. It can cross the blood-brain barrier and enter the central nervous system (CNS) - the brain and spinal cord.

Lorazepam is then metabolized in the body, and around twelve to 16 hours after ingestion, around half of the amount of active substance absorbed is excreted - mainly in the urine.

When is lorazepam used?

The active ingredient lorazepam is used for the short-term treatment of anxiety, tension and excitement and the associated sleep disorders. In addition, it can be used to calm down before diagnostic or surgical interventions.

Long-term use of benzodiazepines such as lorazepam often leads to addiction problems. It should therefore only be taken for as short as possible (a maximum of two to four weeks).

This is how lorazepam is used

The most common dosage form of Lorazepam is tablets for ingestion. Orodispersible tablets or injection solutions are available for patients who have difficulty swallowing or who simply refuse to take them.

Depending on the area of ​​application, a dosage of 0.5 to 2.5 milligrams is usually given over the day or in the evening.

What are the side effects of Lorazepam?

The side effects of Lorazepam mostly result directly from the desired depressant effect:

More than one in ten patients experience tiredness, sleepiness and drowsiness. More than every hundredth person treated develops fatigue, muscle weakness, confusion, depression and a feeling of dizziness.

Children, the elderly and people with brain diseases can react paradoxically to ingestion, i.e. with excitement, restlessness, sleep disorders or increased feelings of fear.

What should be considered when taking Lorazepam?

Contraindications

Lorazepam must not be used in:

  • known benzodiazepine addiction
  • Myasthenia gravis (autoimmune-mediated muscle weakness)
  • Respiratory dysfunction
  • Hypersensitivity to lorazepam

Interactions

If Lorazepam is taken at the same time as other central depressant agents, the effects can be mutually reinforcing. This applies, for example, to antipsychotics (e.g. haloperidol, promethazine), anti-anxiety drugs, antidepressants (e.g. mirtazapine, trazodone), sedatives and sleeping pills.

The same applies to pain relievers, antiallergic agents and anti-epileptic agents, as well as agents that affect the heart and blood pressure, such as beta blockers.

Avoid drinking alcohol during therapy with lorazepam, as this can increase the central depressant effect.

Age restriction

Lorazepam tablets and orodispersible tablets should only be used in children and adolescents under 18 years of age after carefully weighing the risks and benefits. Lorazepam is not recommended for children under the age of six.

In emergency medicine, for example when a status epilepticus is broken (= epileptic seizure that lasts longer than five minutes), lorazepam is approved as a solution for injection from the age of one month.

In older age, the duration of action of Lorezapam increases, which usually makes a reduction in the dosage necessary.

pregnancy and breast feeding period

Benzodiazepines as a group have been well studied, with most of the experience being with diazepam. A study with lorazepam in more than 100 evaluated pregnancies could not prove an increased risk of malformations.

If taken in the last month of pregnancy, however, the "floppy infant syndrome" (flaccid toddler syndrome) occurs more frequently, since the active ingredient can cross the placenta unhindered and thus also unfolds its effect in the child. More suitable alternatives in pregnancy are therefore promethazine (for acute anxiety states), amitriptyline (for sleep disorders) and quetiapine (for psychotic illnesses).

For breastfeeding, there is published experience on the use of lorazepam in more than 100 mother-child pairs. When a mother receives single doses of lorazepam for acute treatment, no breastfeeding break is necessary. In combination with other centrally active ingredients, there may be side effects in the infant (especially sedation).

How to get medication with lorazepam

Lorazepam requires a prescription in Germany, Austria and Switzerland. In addition, it is even listed as a narcotic (like all benzodiazepines), which means that the regulation of the active ingredient is particularly strictly regulated.

Lorazepam can only be obtained on a normal prescription if the single dose is a maximum of 2.5 milligrams and the preparation does not contain any other active ingredients.

Since when is lorazepam known?

The active ingredient Lorazepam was patented in 1963 and first launched in the USA in 1977. Since the patent protection has now expired, there are now various preparations with lorazepam from different manufacturers.

More facts about lorazepam

Lorazepam is a further development of Diazepam, another benzodiazepine. Compared to this, lorazepam has a much shorter duration of action and retention in the body, because no effective products (active metabolites) are created when it is metabolized.

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