PSYCHOTROPIC DRUGS

of mental illness:
Psychoses,
Neurotic and pseudoneurotic disoders, associated with stress, nervousness,

fear, anxiety.

subject without inducing sleep, though drowsiness may be produced.
Drugs: benzodiazepines,

barbiturates and alcohols
Cause dose-dependent CNS depression that extends from sedation to respiratory depression and death
BZs reach a plateau in CNS depression, barbiturates and alcohol do not.

one. It results in a decrease of internal tension, elimination

of nervousness, anxiety and fear. Besides, most anxiolytics have a sedative action. They do not affect the autonomic innervations; they do not induce extrapyramidal disorders.
Anxiolytics are divided into groups:
Agonists of benzodiazepine receptors
Agonists of serotonin receptors (Buspirone)
Drugs of different action types.

the GABA receptor–Cl¯ channel complex in limbic system.
Occupation of the

BDZ sites by BDZ receptor agonists causes a conformational change in the GABA receptor. This increases the affinity of GABA binding and enhances the actions of GABA on the Cl− conductance of the neuronal membrane. GABA activates ↑ CL- influx, which results in hyperpolarisation.
Barbiturates act at the another binding site and similarly enhance the action of GABA .
In the absence of GABA, BDZs and low doses of barbiturates do not affect Cl− conductance.

h): Lorazepam, Alprazolam
Short-term action (t1/2 ˂6 h): Midazolam

Flumazenil is a

specific antagonist of BDZs. It blocks the BDZs receptors and eliminates fully or decreases the intensity of the most central effects of BDZs.

tension, they also promote the onset of sleep. They are

used in the treatment of neuroses, neurosis-like conditions and insomnia.
There are BDZs with marked anxiolytic action and none or minimal sedative-hypnotic action. Such drugs are called “Day-time anxiolytics (tranquilizers)”. For example Medazepam.

spinal polysynaptic reflexes and disturbance of its supraspinal regulation. These

drugs are called central muscular relaxants and used in neurology.
BDZs have anticonvulsant activity. They are effective in status epilepticus.
They potentiate the CNS inhibition caused by drugs with non-selective CNS depressants action. They are administered for premedication before surgical interventions.

through the blood-brain barrier and other biological barriers.
They undergo metabolism.

Some metabolites have marked and long-term anxiolytic effect.
They bind with the plasma proteins and are deposited in the fatty tissues.
The kidneys are the main elimination route for the metabolites and conjugates of BDZs.

response, memory impairment, weakness, diplopia, headache, nausea, vomiting, dysmenorrhea, skin

rashes.
During long-term therapy: tolerance and drug dependence (psychological and physical, withdrawal syndrome).
Teratogenic effect.

anxiolytic activity. After its administration the effects develops slowly (over

1-2 weeks).
It has not sedative, anticonvulsive and muscle-relaxing action.
It has a low tendency to induce tolerance and drug dependence.
Side effects: nervousness, dizziness, headache, paresthesias, nausea, diarrhea.

drugs. They have a moderate calming action. They are administered

for the treatment of neuroses, increased irritability and sleeplessness.
Sodium bromide and potassium bromide are the most widely used bromides. Their main action is associated with the intensification of the inhibitory processes in the brain cortex. The effect of bromide depends on the type of nervous system (weak and strong type).

apathy, memory disorder, skin lesions. The irritating action of bromide

leads to the inflammation of the mucous membranes, which is associated with the cough, rhinitis, conjunctivitis and diarrhea.
The treatment: discontinuation of bromide intake, administration of large amount of sodium chloride, drinking a lot of water, introduction of diuretics.

drugs
Phenothiazine derivatives: Chlorpromazinе, Trifluoperazinе
Butyrophenone derivatives: Haloperidol, Droperidol
2. Atypical antipsychotic

drugs:
Clozаpinе, Risperidonе

and delays further progression of schisophrenia.
The effect is associated with

the block of postsynaptic dopamine D2-receptors of mesolimbic and mesocortical systems.
Haloperidol > Trifluoperazinе > Chlorpromazinе
Risperidonе blocks D2 and 5-НТ 2А receptors.

affective reactions, reduction of anxiety, nervousness, decrease in motor activity.

is associated with their effect on the ascending reticular formation of the brainstem, limbic system, hypothalamus. They block α-adrenoceptors, H-receptors, serotonin receptors and M-cholinoceptors.
Chlorpromazinе, Haloperidol, Droperidol
But Trifluoperazinе has psychostimulant action.

suppression of the striatum of the substantia nigra lead to

a change of the effect of the striatum on motor activity control. This results in the enhancement of the activity of the spinal cord α-motoneurons, increase in muscular tone and development of drug-indused parkinsonism (hypokinesia, rigidity, tremor).
Typical antipsychotics cause parkinsonism.
Atypical antipsychotics cause very rarely.

external stimuli.
Ability to potentiate action of a number of neurotropic

drugs, such as general anesthetics, hypnotics and opioid analgetics.
Antiemetic effect, which is associated with the block of the dopamine receptors of the trigger zone, located at the bottom of the 4th ventricle. They can prevent vomiting caused by antiblastomic drugs.

the temperature of the surrounding environment. Often an insignificant hypothermia

is observed (due to an increase in heat loss).
If Chlorpromazine is applied under low temperatures (physical cooling), there is a marked fall in the body temperature. This effect is used in surgery.
Chlorpromazine has a typical muscle relaxing effect, which results in a reduction of motor activity. It is associated with the inhibition of supraspinal regulation of muscular tone.

with the inhibition of hypothalamic centres, with the α-adrenoceptors blocking

effect and spasmolytic properties. Hypotension is commonly associated with reflex tachycardia.
Chlorpromazine possesses some M-cholinoceptors blocking (atropine-like) properties. They result in mild suppression of salivary, bronchial and digestive gland secretion and also tachycardia.

mask like facies, disorders of gait;
Malignant neuroleptic syndrome : It

occurs rarely with high doses of potent agents. The patient develops marked rigidity, immobility, tremor, hyperthermia, semiconsciousness, fluctuating BP and heart rate; myoglobin may be present in blood. The syndrome lasts 5–10 days after drug withdrawal and may be fatal.

amenorrhoea, infertility, galactorrhoea and gynaecomastia;
CVS Postural hypotension, tachycardia;
Dry mouth,

blurring of vision, constipation, urinary retention in elderly males;
Cholestatic jaundice;
Skin rashes, urticaria, contact dermatitis, photosensitivity;
Agranulocytosis.

reactions, aggressiveness, delirium, hallucinations.
In complex with other drugs when treating

drug dependence (opioid analgetics, alcohol)
Phenothiazine and Haloperidole are used as antiemetic drugs and in persistant hiccups.
They are used with general anesthetics, hypnotics and opioid analgetics besause they can potentiate actions.

and bipolar (manic depressive) disorder.
The mechanism of antimanic and mood

stabilizing action of lithium:
Li+ partly replaces body Na+ and is nearly equally distributed inside and outside the cells; this may affect ionic fluxes across brain cells or modify the property of cellular membranes.
Lithium decreases the presynaptic release of NA and DA.

slowly onset of effect (2-3 weeks), more selective action on

manias, and a lack of sedative effect (listlessness and apathy).
The low therapeutic window has to be considered.
Side effects: dyspeptic disorders, muscle weakness, tremor, polyuria, thirst.
Acute poisoning with the lithium salts: vomiting, diarrhea, ataxia, disarthria, and cramps.