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Psychiatric Drugs. Central Nervous System Stimulants

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Presentation on theme: "Psychiatric Drugs. Central Nervous System Stimulants"— Presentation transcript:

1 Psychiatric Drugs. Central Nervous System Stimulants

2 Analeptic Used to stimulate respiration when natural reflex is lost
H-cholinomimetic (reflex analeptic) Central analeptic (Aminophyllin, theophylline,Caffeine, Doxapram)

3 Analeptics (Bemegridum, Camphora, Cordiaminum)

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6 CNS Stimulants: Adverse effects
CVS: Palpitation, tachycardia, hypertension, angina, dyshythmia CNS: Nervousness, restlessness, anxiety Endocrine: Hypoglycemia, hyperglycemia GIT: Nausea, vomiting,diarrhea

7 Usage of psychostimulating influence of caffeine
For stimulation of psychological processes, workability, to eliminate somnolence Enuresis, narcolepsy In case of poisoning with alcohol To speed up awakening after narcosis

8 Influence of caffeine on cardiac-vascular system
Vessels Stimulation of vasomotor center – contraction of vessels, increasing of AP Peripheral myotropic spasmolytic action – dilation of vessels, decreasing of AP Heart Central action (increasing of n. vagus tone) – bradycardia Peripheral action (direct influence on heart) – tachycardia, possible extrasystolia

9 Influence of caffeine on cardio-vascular system
Contraction of brain vessels Dilation of kidney vessels, increasing of diuresis Dilation of coronary vessels In case of depression of centers of brain stem (medulla oblongata) caffeine shows stimulating properties, increases blood pressure, stimulates breathing – analeptic action

10 Did You Know? Caffeine is a xanthine alkaloid compound that acts as a stimulant in humans. Caffeine is sometimes called guaranine when found in guarana, mateine when found in mate, and theine when found in tea. It is found in the leaves and beans of the coffee plant, in tea, yerba mate, and guarana berries, and in small quantities in cocoa, the kola nut and the Yaupon Holly. Overall, caffeine is found in the beans, leaves, and fruit of over 60 plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding upon them.

11 Chemical Properties Molar Mass = 194.19 g mol−1 Density: 1.2 g/cm³
Phase: Solid Melting Point: 237 °C Boiling Point: 178 °C

12 Caffeine

13 Uses of Caffeine Caffeine is a central nervous system (CNS) stimulant, having the effect of temporarily warding off drowsiness and restoring alertness. Beverages containing caffeine, such as coffee, tea, soft drinks and energy drinks enjoy great popularity: caffeine is the world's most widely consumed psychoactive substance. In North America, 90% of adults consume caffeine daily.

14 Caffeine AP Hate rate Respiratory stimulation Adjunctive effect

15 SIDE EFFECTS OF CAFFEINE
If administered regularly – psychological addiction – theism, which is accompanied by development of abstinent syndrome (retardness, fatigue, somnolence, depression) Tolerance Teratogenic action (innate abnormalities) Increasing of frequency of IHD, essential hypertension Acute attacks of ulcer disease (it increases gastric secretion) Acute poisoning in case of overdosing

16 Amphetamines Produce mood elevation or euphoria, increase mental alertness and capacity for work, decrease fatigue and drowsiness, prolong wakefulness.

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21 Amphetamines USAGE: ADHD (attention-deficit/hyperactivity disorder
Narcolepsy TOXICITY Tolerance Psychological dependence High abuse potential (under Control Substance Act

22 ADHD – attention deficit hyperactivity disorder – more frequently in children
Cured by potent stimulators (ritalin, adderal and others) They all can provoke addiction !!!

23 Methylxanthines COPD (chronic obstructive pulmonary disease
Respiratory depression in postoperative recovery period

24 Anorexants Central acting (Benzphetamine, diethylpropion, Sibutramine)
Metabolism acting (orlistat)

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27 Function of adrenergic synapse in physiological conditions

28 ANTIDEPRESSANTS Drugs which inhibit neuronal uptake of monoamines
Nonselective action – tricyclic compounds (block uptake of noradrenaline and serotonine): imisin, amitriptilin Selective action: а) heterocyclic compounds (block neuronal uptake of noradrenaline): amoxapin, maprotilin (ludiomil); б) selective blockers of neuronal uptake of serotonin: fluoxetin (prozak, framex), sertralin (zoloft), paroxetin (rexetin) Inhibitors of monoaminoxidase (IMAO) nonselective (block МАО-А and МАО-В): а) irreversible action – nialamid; b) reversible action – transamin Selective ІМАО (block МАО-А): moklobemid, pirasidol

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32 Blockers of neuronal reuptake of serotonin
Modern point of view on mechanism of development of depression Primary deficiency of serotonin in synaptic cleft Compensatory growing of quantity and sensitivity of postsynaptic 5-НТ2 receptors Compensatory decreasing of quantity and sensitivity of presynaptic 5-НТ1 receptors in hippocampus and nuclei row (these structures play an important role іn development of depression)

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34 5-НТ2 serotonin receptors of cerebral structures
Blockers of neuronal reuptake of serotonin fluoxetin, sertralin, paroxetin Mechanism of action Increasing of active concentration of serotonin in synaptic cleft on a level of postsynaptic 5-НТ2 serotonin receptors of cerebral structures

35 Blockers of neuronal reuptake of serotonin fluoxetin, sertralin, paroxetin

36 Mechanism of action of IMAO

37 Usage of antidepressants
Schizophrenia, MDS Atherosclerosis of brain Reactive depressions Parkinsonism Organic diseases of CNS Oncology patients General somatic diseases

38 Psychotropic action of antidepressants
Drugs with psychosedative action: Аmitriptilin, maprotilin, asafen, fluvoxamin 2. Drugs with psychostimulative action: Imisin, nialamid, fluoxetin 3. Drugs with regulative influence Pirasidol

39 Principles of antidepressants usage
Endogen depression – the deeper it is, the larger doses, rate of their increasing and duration of treatment should be administered Step-by-step dose increasing till obtaining of effect, administration of effective dose during 4-6 weeks – 3-6 months, gradual decreasing of dose (during 5-6 weeks) Effect can appear only after 7-14 days after beginning of therapy (this fact should be taken into consideration in patients with suicidal dispositions) In case of rapid abolishing withdrawal syndrome may develop

40 Side effects of antidepressants
М-cholinoblocking action: dry mouth, increasing of intraocular pressure, disturbance of accommodation, constipation, ischuria (important in a case of adenoma of prostatic gland!), tremor, hallucinations, disorders of consciousness, excitation Alpha-adrenoblocking, papaverine-like effect: acute hypotension, orthostatic collapse (especially in combination of amitriptiline with clopheline), for correction of which adrenomimetics cannot be used (it is necessary to increase volume of circulating blood, put the legs up)

41 Side effects of antidepressants
Acute attacks of epilepsy Cardiotoxic action (sudden death), three- cyclic antidepressants increase arrhythmogenic activity of drugs for general anesthesia, antihistamines etc. Combination of three-cyclic antidepressants with IMAO is absolutely contraindicated: danger of development of hypertensive crisis, seizures, rapid excitation, tachycardia, cardiac arrhythmias, increasing of temperature

42 Rules of transferring from one kind of antidepressants to another
From three-cyclic to IMAO – break time– 2-3 days From IMAO to three-cyclic – break time – not less than 2 weeks

43 Diet in case of administration of IMAO
It is necessary to exclude such products which contain DOPA and thiramine (which is formed from casein during the process of transforming under the influence of bacteria) aged cheese, kefir Marinated herring Smoked meat, fish Red vine, beer, yeast Beans oranges, tangerines, lemons, grape, bananas, chocolate, caviar (red and black)… Any BAA are also dangerous In case of treatment with IMAO new products should be introduced into ration very carefully

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47 Neurometabolic cerebroprotectors
Derivatives of pyrrolidone – pyracetam (nootropil) Derivatives of GABA – aminalon, sodium oxybutyrate Neuropeptides – melatonin, sinacten-depot Cerebrovascular drugs – sermion (nicergolin), cavinton (vinpocetin), stugeron (cinnarisin), pentoxyphylline (trental, agapurine), xantynole nicotinate Derivatives of piridoxine – piritinol (encephabol) Antioxidants – mexidol, tocopherole acetate Other – cerebrolysine, actovegin, solkoseryl, plant preparations

48 Properties of nootropic drugs
Improvement of brain blood circulation, promotion of collaterals development Psychostimulating effect, antiasthenic action Sedative, antidepressive action Antiepileptic, antiparkinsonic action Nootropic action Mnemotropic action Vasovegetative action Antihypoxic action

49 Administration of nootropic drugs
Atherosclerosis of brain, vascular parkinsonism, Alzheimer's disease Disorders of brain blood circulation in case of traumas and intoxications, vascular diseases of brain Diseases of CNS, accompanied by decreasing of intellect, memory Disorders of psychology (in elderly with schizophrenia, depressions) To decrease manifestations of abstinence (alcoholism, drug addiction) In neurology (neurasthenia, migraine, neuralgias, radiculitis) In pediatrics in case of mental insufficiency

50 Piracetam (nootropil)

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53 Cerebrolysin

54 Cinnarizin (stugeron)

55 Ginseng, Schizandrum, Rodiola, Eleutherococcus, Leusea, Echinacea
Adaptogens Drugs of Ginseng, Schizandrum, Rodiola, Eleutherococcus, Leusea, Echinacea Apilac, propolis, mumie, heparin, dibazol

56 GINSENG

57 RODIOLA

58 Eleutherococcus

59 Schizandrum

60 Echinacea purpurea Maxima

61 ADAPTOGENS Stimulating action Antistress action Anabolic action
Increase general resistance of the organism towards unfavorable factors Stimulating action Antistress action Anabolic action

62 Side effects of adaptogens
Increasing of AP disturbance of sleep if administered in evening time, overwhelming excitation, psychical dependence


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