Sedative drugs

List of drugs

Sodium bromide (Natrium bromide)

Valeriana extract

Mechanism of action

Unknown

Pharmacological effects

These drugs decrease excitement state of central nervous system to normal state.

Indications

4. Neurosis (functional nervous affection with next symptoms: irritancy, tearfulness etc.)

Sodium bromide, Valeriana → decrease excitement state of central nervous system to normal state → treating of neurosis.

NB! Sedative drugs are ineffective in treatment of neurosis with anxiety syndrome.

Anxyolytics (antianxiety drugs, tranquillizers)

List of drugs

Benzodiazepines: Diazepam, Mezapam, Phenazepam

Azapirones: Buspirone

Mechanism of action

Benzodiazepines bind to the GABA-receptors (not in the active site of receptors, but in additional (allosteric) site of receptors) and potentiate GABAergic inhibition of central nervous system.

Buspirone produce direct stimulation of 5-HT_1A receptors that result in inhibition of central nervous system.

NB! GABA-receptors = receptors for gamma-aminobutyric acid

5-HT_1A receptors = receptors for serotonine

Pharmacological effects

These drugs decrease excitement state of central nervous system to normal state.

Indications

2. Neurosis with anxiety syndrome

Diazepam, Mezapam, Phenazepam → potentiation of GABAergic inhibition of central nervous system → decrease excitement state of central nervous system to normal state → treatment of neurosis with anxiety syndrome.

Buspirone → direct stimulation of 5-HT_1A receptors → decrease excitement state of central nervous system to normal state → treatment of neurosis with anxiety syndrome.

3. Premedication (decreasing of anxiety before surgery)

Diazepam, Mezapam, Phenazepam → potentiation of GABAergic inhibition of central nervous system → decrease excitement state of central nervous system to normal state → decreasing of anxiety before surgery.

4. Potentiation of effects of general anaesthetics

Diazepam, Mezapam, Phenazepam → potentiation of GABAergic inhibition of central nervous system → potentiation of inhibitory effects of general anaesthetics.

5. Acute skeletal muscle spasm (“spastic paralysis”)

Diazepam, Mezapam, Phenazepam → potentiation of GABAergic inhibition of spinal cord → relaxation of skeletal muscles.

NB! Buspirone we can use only to treat neurosis with anxiety syndrome.

Side effects

Diazepam, mezapam, phenazepam possess hypnotic activity (we should not use these drugs to treat drivers, rescue workers etc.).

Antipsychotic drugs (neuroleptics)

List of drugs

To treat psychomotor excitement: Chlorpromazine, Droperidol, Clozapine

To treat hallucinations and delusions: Trifluoperazine, Haloperidol, Sulpiride

Mechanism of action

Chlorpromazine, Droperidol, Clozapine produce the blockage of α-adrenoreceptors of reticular formation that results in inhibition of cortex → decreasing of psychomotor excitement

Trifluoperazine, Haloperidol, Sulpiride produce the blockage of D₂-receprots (dopamine receptors type 2) of substantia nigra that results in excitation of nucleus caudatus → inhibition of hallucinations and delusions.

Pharmacological effects

These drugs decrease excitement state of central nervous system below normal state thus producing inhibition of central nervous system.

Indications

2. Psychomotor excitement

Chlorpromazine, Droperidol, Clozapine → blockage of α-adrenoreceptors of reticular formation → inhibition of cortex → decreasing of psychomotor excitement.

3. Hallucinations and delusions

Trifluoperazine, Haloperidol, Sulpiride → blockage of D₂-receprots of substantia nigra → excitation of nucleus caudatus → inhibition of hallucinations and delusions.

4. Toxic vomiting (e.g. during pregnancy, during chemotherapy of cancer etc.)

Possible use any drug (Chlorpromazine, Droperidol, Clozapine, Trifluoperazine, Haloperidol, Sulpiride), but preference is given to Trifluoperazine, Haloperidol, Sulpiride → blockage of D₂-receprots of trigger zone of vomiting center → inhibition of toxic vomiting.

5. In case of small surgeries can be used specific method of anaesthesia: neuroleptanalgesia. For this we should combine neuroleptic drug (droperidol) and opioid analgesic drug (phentanyl).