Psychotropic drugs

Август 1, 2022

Главная
Медицина
Psychotropic drugs

Содержание

3. Sedative - a drug that subdues excitement and calms the subject without inducing sleep, though drowsiness
5. Anxiolytics (tranquilizers) The main effect of these drugs is the anxiolytic one. It results in a
6. BDZs activate their receptor, which is an integral part of the GABA receptor–Cl¯ channel complex in
9. BDZs have anxiolytic, hypnotic, muscle relaxant, anticonvulsant and amnesic actions.
10. Long-term action (t1/2 =24-48 h): Diazepam, Phenazepam, Medazepam Medium-term action (t1/2=6-24 h): Lorazepam, Alprazolam Short-term action
11. BDZs have marked anxiolytic and sedative properties. By reducing emotional tension, they also promote the onset
12. BDZs cause muscle relaxation due to the depression of the spinal polysynaptic reflexes and disturbance of
13. BDZs are well absorbed from the digestive tract, easily pass through the blood-brain barrier and other
14. Side effects In high doses they can cause amnesia. Drowsiness, delayed motor response, memory impairment, weakness,
15. Buspironе is the agonist of serotonin receptors. It has marked anxiolytic activity. After its administration the
16. Sedatives Bromide salts, valerian and motherwort preparations belong to the sedative drugs. They have a moderate
17. Bromism – chronic poisoning This is manifested by general lethargy, apathy, memory disorder, skin lesions. The
18. Antipsychotic drugs (neuroleptic drugs) have antipsycotic and sedative action. Classification 1.Typical antipsychotic drugs Phenothiazine derivatives: Chlorpromazinе,
19. Antipsychotic effect reduces the productive symptoms of psychoses (delusions, hallucinations) and delays further progression of schisophrenia.
20. Psychosedative action is characterized by general sedation – elimination of affective reactions, reduction of anxiety, nervousness,
21. Parkinsonism The inhibition of the nigrostriatal transmission and reduction of the suppression of the striatum of
22. Other effects Hypnotic effect: superficial sleep, which is easily interrupted by external stimuli. Ability to potentiate
23. Chlorpromazine inhibits the center of termoregulation. The outcome depends on the temperature of the surrounding environment.
24. Cardiovascular system: Chlorpromazine decreased arterial pressure. This effect is associated with the inhibition of hypothalamic centres,
26. Side effects. Extrapyramidal disturbances Parkinsonism with typical manifestations— rigidity, tremor, hypokinesia, mask like facies, disorders of
27. Side effects. CNS: Drowsiness, lethargy, mental confusion; Hyperprolactinemia (due to D2 blockade), amenorrhoea, infertility, galactorrhoea and
28. Use Antipsychotics drugs are administered in psychoses with marked excitation, affective reactions, aggressiveness, delirium, hallucinations. In
29. Lithium salts are mainly used to manage and prevent mania and bipolar (manic depressive) disorder. The
31. Скачать презентацию

Слайд 2

Слайд 3

Sedative - a drug that subdues excitement and calms the 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.

Слайд 4

Слайд 5

Anxiolytics (tranquilizers)
The main effect of these drugs is the anxiolytic 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.

Слайд 6

BDZs activate their receptor, which is an integral part of 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.

Слайд 7

Слайд 8

Слайд 9

BDZs have anxiolytic, hypnotic, muscle relaxant, anticonvulsant and amnesic actions.

Слайд 10

Long-term action (t1/2 =24-48 h): Diazepam, Phenazepam, Medazepam
Medium-term action (t1/2=6-24 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.

Слайд 11

BDZs have marked anxiolytic and sedative properties. By reducing emotional 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.

Слайд 12

BDZs cause muscle relaxation due to the depression of the 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.

Слайд 13

BDZs are well absorbed from the digestive tract, easily pass 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.

Слайд 14

Side effects
In high doses they can cause amnesia.
Drowsiness, delayed motor 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.

Слайд 15

Buspironе is the agonist of serotonin receptors. It has marked 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.

Слайд 16

Sedatives
Bromide salts, valerian and motherwort preparations belong to the sedative 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).

Слайд 17

Bromism – chronic poisoning
This is manifested by general lethargy, 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.

Слайд 18

Antipsychotic drugs (neuroleptic drugs) have antipsycotic and sedative action.
Classification
1.Typical antipsychotic drugs

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

Слайд 19

Antipsychotic effect reduces the productive symptoms of psychoses (delusions, hallucinations) 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.

Слайд 20

Psychosedative action
is characterized by general sedation – elimination of 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.

Слайд 21

Parkinsonism
The inhibition of the nigrostriatal transmission and reduction of the 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.

Слайд 22

Other effects
Hypnotic effect: superficial sleep, which is easily interrupted by 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.

Слайд 23

Chlorpromazine inhibits the center of termoregulation. The outcome depends on 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.

Слайд 24

Cardiovascular system: Chlorpromazine decreased arterial pressure. This effect is associated 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.

Слайд 25

Слайд 26

Side effects. Extrapyramidal disturbances
Parkinsonism with typical manifestations— rigidity, tremor, hypokinesia, 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.

Слайд 27

Side effects.
CNS: Drowsiness, lethargy, mental confusion;
Hyperprolactinemia (due to D2 blockade), 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.

Слайд 28

Use
Antipsychotics drugs are administered in psychoses with marked excitation, affective 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.

Слайд 29

Lithium salts are mainly used to manage and prevent mania 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.

Psychotropic drugs

Содержание

Sedative - a drug that subdues excitement and calms the subject

Anxiolytics (tranquilizers) The main effect of these drugs is the anxiolytic one.

BDZs activate their receptor, which is an integral part of the

BDZs have anxiolytic, hypnotic, muscle relaxant, anticonvulsant and amnesic actions.

Long-term action (t1/2 =24-48 h): Diazepam, Phenazepam, MedazepamMedium-term action (t1/2=6-24 h):

BDZs have marked anxiolytic and sedative properties. By reducing emotional tension,

BDZs cause muscle relaxation due to the depression of the spinal

BDZs are well absorbed from the digestive tract, easily pass through

Side effectsIn high doses they can cause amnesia.Drowsiness, delayed motor response,

Buspironе is the agonist of serotonin receptors. It has marked anxiolytic

SedativesBromide salts, valerian and motherwort preparations belong to the sedative drugs.

Bromism – chronic poisoning This is manifested by general lethargy, apathy,

Antipsychotic drugs (neuroleptic drugs) have antipsycotic and sedative action.Classification1.Typical antipsychotic drugs

Antipsychotic effect reduces the productive symptoms of psychoses (delusions, hallucinations) and

Psychosedative action is characterized by general sedation – elimination of affective

Parkinsonism The inhibition of the nigrostriatal transmission and reduction of the suppression

Other effectsHypnotic effect: superficial sleep, which is easily interrupted by external