What are anxiolytics?

Anxiolytics are a group of drugs used for anxiety disorders. These medicines help to get rid of the constant feeling of fear and anxiety, reduce long-term emotional stress.

There are various anxiolytic options on the pharmaceutical market: prescription and over-the-counter, with anti-anxiety effect and with a combined (sedative and anxiolytic) effect, old-generation drugs and the latest medicines. Previously, the group of anxiolytics included only benzodiazepines, which have a wide range of side effects, since that time a negative attitude and distrust towards the pharmaceutical group as a whole has been preserved. Anxiolytics have now been developed that are highly effective and, if used correctly, do not harm health.

The biomechanism of anxiolytics is mainly due to the effect on the work of the GABAergic system of the brain. Gamma-aminobutyric acid (GABA) is a biogenic substance that regulates the balance of the processes of excitation and inhibition of the activity of brain nerve cells. Anxiolytics affect the GABA system and reduce the excitability of the subcortical zones responsible for emotional reactions. Violation of the proper functioning of these zones (thalamus, hypothalamus, limbus) just becomes the culprit of an anxiety or depressive disorder. Less pronounced effects of anxiolytics are realized due to their influence on three hormonal cascades of the central nervous system: norepinephrine (norepinephrine, adrenaline), dopaminergic (dopamine) and serotoninergic (serotonin)

What are the effects of anxiolytics?

  • Actually anxiolytic, or anti-anxiety, is the main effect of drugs in this group. It is achieved by strengthening inhibitory processes, reducing the excitability of the subcortical areas of the brain - as a result, emotional tension decreases, feelings of anxiety and fear weaken.
  • Sedative. This effect, as well as the subsequent ones, is not mandatory for anxiolytics. As a result of exposure to the reticular formation of the brain stem, psychomotor excitability decreases, concentration of attention and reaction speed decrease. Muscle relaxant. The inhibitory effect on the spinal reflexes provides relaxation of the skeletal muscles.
  • Vegetostabilizing. Some anxiolytics, acting on the autonomic nervous system, prevent the progression of autonomic manifestations of anxiety, such as gastrointestinal dysfunction, tachycardia, and sweating.

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Pharmachologic effect

Tranquilizer, anxiolytic. It has hypnotic, sedative, muscle relaxant, anxilotic, anticonvulsant effects.

Pharmacodynamics and pharmacokinetics

The mechanism of action of the drug is based on an increase in the inhibitory effect of the GABA mediator on the transmission of impulses along the nerve roots.

The drug stimulates benzodiazepine receptors of the allosteric center, reduces the excitability of the subcortical structures of the brain (hypothalamus, limbic system, thalamus), inhibits spinal, polysynaptic reflexes.

The anxiolytic effect is caused by exposure to the amygdala complex in the limbic system, a decrease in emotional stress, a weakening of feelings of anxiety, worry and fear.

The sedative effect is explained by the influence on the nonspecific nuclei of the thalamus, the reticular pharmacy of the brain stem, which leads to a decrease in the severity of neurological symptoms (fear, anxiety).

The hypnotic effect is achieved due to the inhibition of reticular pharmacy cells in the brain stem.

By providing enhanced presynaptic inhibition, an anticonvulsant effect is achieved.

The drug does not relieve excitation in the focus, but suppresses the spread of epileptogenic activity.

Muscle relaxant action of central origin occurs as a result of inhibition of spinal, polysynaptic, afferent inhibitory pathways. Direct inhibition of motor nerves, functions of the muscular system is allowed.

The drug does not affect psychotic symptoms (hallucinations and affective disorders), in rare cases, a decrease in the severity of delusional disorders, affective tension is recorded.


Lorazepam is prescribed for neurosis and anxiety, somatic disorders, worsening sleep, increased irritability.

As part of complex therapy, the drug is used for anxiety caused by a depressive state.

The drug is effective for psychosomatic disorders, catatonic, manic states, endogenous psychoses, withdrawal symptoms, drug addiction, alcoholic delirium.

In anesthetic practice, it is used for sedation.

The drug is prescribed for essential, senile tremor, muscle rigidity, muscle spasm, contractures (trauma, arthritis, moisitis), tetanus, athetosis.


Lorazepam is not prescribed for angle-closure glaucoma, severe myasthenia gravis, intolerance to benzodiazepine derivatives, acute drug intoxication, addiction to drugs, alcohol.

The drug is contraindicated in severe COPD, pregnancy, acute respiratory failure, breastfeeding, sleep apnea syndrome.

With cerebral ataxia, insufficiency of the renal, hepatic systems, spinal ataxia, severe depression, with organic diseases of the brain, hyperkinesis, psychosis, sleep apnea, hypoproteinemia are prescribed with caution.

In pediatrics, they are used after reaching the age of 12.

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Side effects

Nervous system: ataxia, dullness of emotions, lethargy, decreased concentration, fatigue, increased drowsiness. Extrapyramidal disorders, catalepsy, confusion, anterograde amnesia, depressed mood, myasthenia gravis, paradoxical reactions (acute agitation, hallucinations, confusion, muscle spasm, suicidal tendencies, outbursts of aggression, fear) are rarely noted.

Sense organs: visual disturbances, diplopia.

Organs of hematopoiesis: neutropenia, anemia.

Digestive system: jaundice, increased liver transaminases, dry mouth, diarrhea, loss of appetite.

Genitourinary system: dysmenorrhea, decreased libido, pathology of the renal system, urinary retention, urinary incontinence.

Lorazepam has a teratogenic effect on the fetus, the use of breastfeeding causes suppression of the sucking reflex in the child, breathing is disturbed.

The development of drug dependence, a drop in blood pressure, and depression of the respiratory center are noted.

The withdrawal syndrome is accompanied by the appearance of a feeling of fear, dysphoria, myalgia, increased sweating, tremor.

Method of application and dosage

Take three times a day, 1 mg. For a hypnotic effect, the drug is taken half an hour before bedtime at a dose of 1-2 mg. With anxiety and increased excitability, take up to 6 mg per day.

For the purpose of premedication, Lorazepam is prescribed an hour before surgery at a dose of 2.5-5 mg, for children the dosage is calculated according to the scheme: 0.05 mc / kg.

To prevent the risk of developing a convulsive syndrome, drug withdrawal should be carried out gradually. Duration of therapy - no more than 7 days.

For patients with pathology of the renal, hepatic system, the dosage is reduced.

Maximum daily tablets - no more than 10 mg, solution no more than 4 mg.


Stupefaction, decreased reflexes, paradoxical excitement, confusion, increased drowsiness, nystagmus, ataxia, dysarthria, deep sleep, tremor, coma, depression of the cardiac, respiratory systems, collapse, drop in blood pressure, shortness of breath, bradycardia.

Emergency forced diuresis is recommended, flumazenil is used as an antidote. Hemodialysis is not effective.

Drug interactions

When conducting premedication with Lorazepam, in some cases, a reduction in the dosage of Fentanyl derivatives is required.

The drug reduces the effectiveness of levodopa in the treatment of patients with parkinsonism.

The drug enhances the toxic effect of zidovudine.

Barbiturates, narcotic analgesics, phenothiazines, antidepressants, MAO inhibitors increase the inhibitory effect on the nervous system, increase neurotropic activity.

Narcotic analgesics enhance the effect of euphoria, causing an increase in psychological dependence.

Clozapine may cause respiratory depression when taken concomitantly with lorazepam.

Special instructions

Patients with cerebral sclerosis, arterial hypotension, with reduced body weight, with CHF require adjustment of the dosing regimen.

During the treatment period, it is strictly forbidden to take alcoholic beverages.

Taking large doses for a long time causes the formation of drug dependence.

Abrupt discontinuation of Lorazepam is unacceptable.

The drug adversely affects the management of complex mechanisms, driving vehicles, performing complex work related to concentration.

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