Lorazepam: What It Is And How It Works

Lorazepam is a drug from the group benzodiazepines (BZD) that is used to fight anxiety and nervousness. Depending on the case, consumption can be prescribed for specific time periods (short-term treatment) or seasonal (long-term treatment).

Have you ever heard it mentioned or do you have a prescription for it? In that case, it would be good for you to know a little more about the mechanism of action and its pharmacological effects, as well as its side effects and pharmacokinetics. First, we need to know what we mean when we talk about anxiety.

What is anxiety?

As experts point out, anxiety is a natural adaptation mechanism that, when it becomes too much and affects a person in various ways, can be considered a disorder. They also add that “anxiety disorders as a whole are the most common psychiatric illness.”

In other words, in normal situations, anxiety is a component of normal mental activity that is involved in defense mechanisms and can be linked to stressful situations. This situation becomes pathological when the limits are exceeded, which cancels out or prevents adaptation to the stressful situation.

In these cases, the feeling of anxiety can be described as a feeling of threat, of tense anticipation of the future and of a change in the psychosomatic balance in the absence of real danger.

When affected by anxiety, different emotions coexist in the patient, such as anxiety, fear or nausea in the face of something “threatening” or a state of irritability, and together these can cause different symptoms such as the following:

• Exhaustion
• Insomnia
• Headache
• Sweat
• Palpitations

What is an anti-anxiety drug?

Drugs used to combat anxiety, such as lorazepam, are called anti-anxiety medications. These relieve or suppress the feeling of anxiety without producing sedation or sleep. In small doses, they are usually only able to produce a feeling of calm.

However, as the dose is increased, the effects of sedation, coma and even death due to poisoning may appear in some cases.

Mechanism of action of lorazepam

Lorazepam is a short-acting drug for the treatment of anxiety. To achieve its anti-anxiety effect, this drug has two complementary mechanisms.

It facilitates the transition from GABA

GABA is a neutral transmitter with the ability to inhibit or reduce neuronal activity. Therefore, the binding of lorazepam to the GABA receptor will result in a change in it which will result in a better binding to the neurotransmitter. By strengthening this bond, its inhibitory capacity is improved.

Binding of lorazepam to specific sites in the GABA-BZD receptor complex

This complex has several domains: α1, ß2 and γ2. It is very important to achieve the right selectivity for these receptors to distinguish the hypnotic effect from the anxiolytic. Particularly for anti-anxiety effect, the sub-receptor involved is BZ2 (ω2).

Pharmacological effects

Depending on the properties of the benzodiazepines, one or both of these actions may take place, or even both at the same time. Lorazepam has anti-anxiety and anticonvulsant effects.

The anti-anxiety effect is characteristic of the BZ2 receptor, as we have mentioned earlier. By binding to this complex, it triggers actions that reduce anxiety and aggression.

Healthy people and people with anxiety

So it is important that we distinguish between healthy people taking lorazepam and patients with anxiety:

• In healthy people, at therapeutic doses, the performance of physical or mental processes does not change. At higher doses it can cause drowsiness, lethargy, ataxia and muscle weakness. The biggest drawback is “remaining sleep”.
• In patients with anxiety, lorazepam relieves both subjective tension and subjective symptoms. However, it is not very effective in situations of panic, phobias and non-neurotic anxiety.

It can also affect aggression and memory, depress the cardiovascular system and reduce the ability to speak and express oneself.

Pharmacokinetics of Lorazepam

This substance, like the other benzodiazepines, is well absorbed orally. In addition, it is highly bound to plasma proteins. Therefore , caution should be exercised, as it may interact with other drugs that present these properties.

It is also a very fat-soluble substance, a necessary property to be able to cross the blood-brain barrier that protects the brain, and trigger its action at the central level.

It is also a molecule that has already been oxidized. Therefore, in its metabolism, it will only undergo conjugation reactions. This is very useful in geriatric patients, as liver function at this age is usually reduced, and by requiring fewer metabolic reactions, patients at this age will easily eliminate it.

Side effects

Side effects come from a long-acting effect of lorazepam. The central nervous system is usually affected and gives reactions such as:

• Paradoxical effects
• Dysarthria (difficulty speaking)
• Sedation and ataxia (impaired coordination of movements)
• Anterograde memory loss (recent memories are not remembered, but events before memory loss are remembered).
• Tolerance dependence with rebound effect  (lorazepam treatment should not be stopped abruptly, it should be done gradually).

Therefore , caution should be exercised in people with allergies to benzodiazepines, asthmatics and patients with severe renal failure. It can also be dangerous for pregnant women, as lorazepam is able to cross the placenta due to its high fat solubility.

Lorazepam should be taken under medical supervision

Under no circumstances should anxiolytics (or other forms) be taken without first consulting a doctor. Many people also require a prescription from their doctor, because they are not available without a prescription.

It is also necessary to always keep in mind that only healthcare professionals can decide whether a person needs to take a particular medication or not. So if you think you need help, go to a consultation with a doctor or specialist and follow their instructions.