Main indications and scope
The primary field of application for anxiolytics is non-psychotic disorders. They effectively manage insomnia, acute stress, and panic attacks. At the same time, it is important to understand the limitations of this group of drugs:
- Depressive episodes: The drugs are not able to elevate lowered mood. Adding them to the treatment regimen is justified only if depression is accompanied by a pronounced anxiety component.
- Psychotic states: Delusions, hallucinatory experiences, and psychomotor agitation are not relieved by tranquilizers. Prescribing these agents to patients with schizophrenia creates only a deceptive picture of improvement due to a temporary sedative effect. Within the framework of psychosis treatment, anxiolytics are used short-term, primarily to relieve anxiety or correct side effects of neuroleptics (for example, in acute dystonia or akathisia).
- Panic disorders: Although tranquilizers are excellent for the rapid relief of an incipient panic attack, for long-term prevention of new attacks, it is preferable to use serotonergic agents (clomipramine and various SSRIs).
Mechanism of action of benzodiazepines
Most tranquilizers belong to the class of benzodiazepines, whose chemical core is formed by six- and seven-membered rings. Their pharmacodynamics is closely linked to the GABAergic system of the nervous system.
Drug molecules interact with specific receptors associated with the chloride channel. Similarly to the natural neurotransmitter (GABA), they facilitate the influx of chloride ions into the neuron. As a result, the cell enters a refractory state—its activity is inhibited.
The suppression of CNS excitability is externally manifested by muscle relaxation, decreased performance, and some memory impairment. However, in parallel, a neuroprotective effect is realized: energy processes in the cells are restored, and the resistance of nervous tissue to damaging factors increases.
Unlike other GABA-active substances (ethyl alcohol, barbiturates, general anesthetics), benzodiazepines have high selectivity, a wide therapeutic window, and relatively low toxicity. It is worth remembering that cross-tolerance exists between all GABAergic substances. This is why patients with chronic alcoholism require higher doses of tranquilizers to achieve the desired effect.
Clinical classification and additional effects
In addition to the main antianxiety effect, many drugs have the ability to relax muscles (myorelaxant effect), which is actively used in the treatment of tension headaches and osteochondrosis. A number of benzodiazepines, such as diazepam and clonazepam, demonstrate pronounced anticonvulsant activity. However, due to concomitant strong sedation, mainly clonazepam is suitable for long-term epilepsy prophylaxis.
According to the nature of the clinical effect, drugs can be divided into several profiles:
- With pronounced sedative effect: chlordiazepoxide, bromdihydrochlorophenylbenzodiazepine, lorazepam.
- "Daytime" tranquilizers (with a mild activating or weak sedative effect): medazepam, tofisopam, oxazepam, etifoxine, hydroxyzine. They have less effect on concentration and performance.
- Hypnotics: flunitrazepam, midazolam, as well as the so-called Z-drugs (zolpidem, zopiclone, zaleplon), which have a different chemical structure but a mechanism similar to benzodiazepines.
Administration features and side effects
Pharmacokinetics largely determines treatment tactics. With intravenous administration, the effect occurs immediately, but the drug must be administered slowly to avoid sudden respiratory arrest (especially when using diazepam or midazolam). When taken orally, the effect can be accelerated by placing the tablet under the tongue or dissolving it in warm water.
Important limitations and risks:
- Pulmonary pathologies: Tranquilizers depress the respiratory center and suppress the cough reflex, so they are prescribed with caution to patients with lung diseases.
- Advanced age: Due to slowed elimination in elderly people, the risk of drug accumulation increases sharply. This can lead to overdose, manifested by muscle weakness and ataxia. In such cases, 3-hydroxybenzodiazepine derivatives (lorazepam, oxazepam) are preferred, as they are better tolerated.
- Drug interactions: It is strictly forbidden to combine anxiolytics with alcohol and other sedative substances due to the risk of unpredictable mutual enhancement of effects.
- Dependence: Long-term intake naturally leads to tolerance (decreased efficacy of the usual dose), the development of physical dependence, and severe withdrawal syndrome upon abrupt discontinuation of the drug.
Finally, any tranquilizers reduce reaction speed, making driving vehicles inadmissible during the treatment period.
Briefly: answers to topical questions
Which drugs belong to the group of mood stabilizers?
The group of mood stabilizers includes two main groups of drugs: lithium salts and antiepileptic drugs.
- Lithium salts — lithium carbonate (including prolonged-release forms contemnol and micalit) and lithium oxybutyrate.
- Antiepileptic drugs — carbamazepine, valproic acid salts, topiramate, and lamotrigine.
What is the mechanism of action of mood stabilizers?
The mechanism of action of mood stabilizers depends on their group affiliation.
- Lithium preparations — alter G-protein expression and their coupling with receptors, affecting post-receptor signal transduction.
- Anticonvulsants — affect the imbalance in the "GABA-glutamate" system and the intracellular accumulation of sodium ions. They can act as GABA receptor agonists, GABA degradation inhibitors, stimulators of sodium excretion from neurons, or glutamate activity inhibitors.
What are the main indications for prescribing mood stabilizers?
The main indication for prescribing mood stabilizers is mood stabilization and the prevention of affective episodes.
- Bipolar disorder (manic-depressive psychosis) — prevention of manic and depressive phases in the interictal period (intermission).
- Recurrent forms of psychosis — prevention of attacks in periodic depression and recurrent schizophrenia.
- Behavioral disorders — correction of the tendency to uncontrolled actions, emotional outbursts, dysphoria, and autoaggressive attacks (an indication for anticonvulsants).
What side effects are characteristic of lithium salts?
Lithium salts are characterized by a number of side effects, as well as a high risk of toxicity due to a narrow therapeutic index.
- Standard side effects — nausea, thirst, polyuria, tremor, and muscle weakness.
- Toxic effect — occurs when the therapeutic concentration is exceeded by 2–3 times and manifests as vomiting, ataxia, convulsions, and in severe cases, coma is possible.
What anticonvulsants are used as mood stabilizers?
The following antiepileptic drugs are used as mood stabilizers for mood stabilization and the prevention of affective psychoses:
- Carbamazepine
- Valproic acid salts
- Topiramate
- Lamotrigine
These drugs are often prescribed in combination with lithium salts when their efficacy is insufficient.
What are the contraindications for the use of mood stabilizers?
The sources describe contraindications only for one group of mood stabilizers — lithium salts. The main contraindication to their prescription is renal pathology. This is due to the fact that lithium preparations are excreted primarily by the kidneys, and if their excretory function is impaired, there is a high risk of drug accumulation in the body. This leads to a sharp increase in toxicity, since lithium salts have a narrow therapeutic index.
Class and exam questions
Can one benzodiazepine be substituted for another without loss of efficacy?
Yes, the spectrum of action of most tranquilizers is very similar. Replacing one drug with another in an equivalent (adequate) dose usually does not lead to significant changes in the patient's well-being.
How do non-benzodiazepine anti-anxiety medications work?
They exert their effect through other receptor systems. For example, hydroxyzine has antihistamine activity, buspirone has serotinergic activity, and etifoxine stimulates the synthesis of endogenous steroids that increase the sensitivity of GABA receptors.
What is prescribed for very severe anxiety?
In such situations, the most potent benzodiazepines are indicated: alprazolam, diazepam, lorazepam, or bromdihydrochlorophenylbenzodiazepine.
What else to study on this topic
- Electroconvulsive therapy (ECT) in treatment-resistant depression
- Pharmacokinetics of long-acting keto-substituted benzodiazepines
- Z-drugs: zolpidem, zopiclone, and zaleplon
- Non-benzodiazepine hypnotics (oxylamine, chlomethiazole)
Master the entire topic in the "Psychiatry" course
This is a summary. The course covers everything tested in classes and exams.
- Full study guide on "Mood Stabilizers" and 499 more pages of the subject
- Assignments and quizzes after every topic — just like in a colloquium
- AI tutor answers questions on the topic anytime
- 7 video lessons on the subject
Other topics in "Chapter 17. Therapy of Mental Disorders. Basic Principles of Prevention and Rehabilitation"
Prepared by WhiteCoat Pro faculty in accordance with the medical school curriculum. For educational purposes only.