Activating CNS agents

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• Activating CNS agents

Lector prof. Posokhova K.A.
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PSYCHOTROPIC DRUGS

• Drugs with depressive type of actoin
• Neuroleptics (antipsychotic)
• Tranquilizers (anxiolytics)
• Sedative drugs
• Normotymics (tymoleptics, tymoanaleptics)
• Drug with stimulative action
• Antidepressants
• Psychomotor stimulants
• Nootropic drugs
• Drugs which increase general tone (adaptogens)
• Psychotomimetics (psychodysleptics)
• LSD
• Cannabis sativa L.

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ANTIDEPRESSANTS
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WHO 3-6 of Earth population suffer from
depression

• Depression and somatic-vegetative symptoms
  which accompany depression are quite often
  psychical disorders which happen in general
  medical practice.
• There are
• Endogen (psychogenic) depression schizophrenia,
  maniac-depressive psychosis
• Secondary (somatogenic) depression organic
  diseases (oncology patients, hypertension, ulcer
  disease, climacteric disorders etc.)

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More than 50 of patients with depressive
disorders dont realize that they have any
psychological problems and complain only on
certain somatic discharges

• Most frequent complaints of patients with
  depression
• Feeling of hopelessness, indifference, fear,
  panic attacks,
• tiredness, weakness, headache, dizziness, dream
  disorders, dyspepsia, unpleasant feelings and
  pain in different parts of the body
• Depressive conditions mask as vegetal-vascular,
  neuro-circulative dystonia (various vegetative
  disorders), gastro-intestinal pathology,
  pathology of cardio-vascular, respiratory
  systems, manifest as diskinesia, functional motor
  disorders, insomnia, toothache, disorders of
  sexual activity, recidivate eczema and many
  other disorders

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Function of adrenergic synapse in physiological
conditions
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ANTIDEPRESSANTS

• Drugs which inhibit neuronal uptake of monoamines
• Nonselective action (block uptake of
  noradrenaline and serotonine) imisin,
  amitriptilin
• Selective action ?) heterocyclic compounds
  (block neuronal uptake of noradrenaline)
  amoxapin, maprotilin (ludiomil) ?) selective
  blockers of neuronal uptake of serotonin
  fluoxetin (prozak, framex), sertralin (zoloft),
  paroxetin (rexetin)
• Inhibitors of monoaminoxidase (IMAO)
• nonselective (block ???-? and ???-?) ?)
  irreversible action nialamid b) reversible
  action transamin
• Selective ???? (block ???-?) moklobemid,
  pirasidol

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Blockers of neuronal uptake 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-??2 receptors
• Compensatory decreasing of quantity and
  sensitivity of presynaptic 5-??1 receptors in
  hippocampus and nuclei row (these structures play
  an important role ?n development of depression)

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Blockers of neuronal uptake of serotonin
fluoxetin, sertralin, paroxetin

• Mechanism of action
• Increasing of active concentration of serotonin
  in synaptic cleft on a level of postsynaptic
• 5-??2 serotonin receptors of cerebral structures

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Blockers of neuronal uptake of serotonin
fluoxetin, sertralin, paroxetin
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Mechanism of action of IMAO
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Usage of antidepressants

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

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Psychotropic action of antidepressants

• Drugs with psychosedative action
• ?mitriptilin, maprotilin, asafen, fluvoxamin
• 2. Drugs with psychostimulative action
• Imisin, nialamid, fluoxetin
• 3. Drugs with regulative influence
• Pirasidol

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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

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Side effects of antidepressants

• ?-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
  sharp 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)

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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

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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

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It is absolutely contraindicated to administer
adreno(sympato)mimetics in case of treatment with
antidepressants

• Even small doses of adrenomimetic
  (sympatomimetic) substances in such patient can
  cause hypertensive crisis
• Nose drops for rhinitis
• If few drops were added to solutions of local
  anesthetics
• In case of administration of drugs which contain
  pseudoephedrine (they are widely used for cold at
  nowadays)

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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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• In case of administration of inhibitors of uptake
  of serotonin the previously indicated side
  effects are observed much more rarely
• Administration of antidepressants with any other
  drugs should be performed only after precise
  studying of possible negative consequences of
  their interaction

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PSYCHOMOTOR STIMULANTS
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PSYCHOMOTOR STIMULANTS

• Derivatives of purine caffeine
• Phenilalkilamines phenamine (amphetamine)
• Phenilalkilsydnonimins - sydnocarb

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Properties of psychomotor stimulants

• Stimulate intellectual activity, speed up
  thinking processes, temporarily eliminate
  tiredness, somnolence
• Eliminate such manifestations of neurosis as
  subdepression, fatigue, retardness
• Arent able to eliminate endogen depression,
  which accompanies psychical diseases

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Caffeine

• Mechanism of action
• Binds to adenosine (purine) receptors in
  brain (endogen ligand of these receptors
  adenosine decreases processes of excitation in
  CNS)
• Inhibiting of phosphodiesterase, which leads to
  accumulation of cAMP and stimulation of many
  physiological processes and metabolism

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Caffeine
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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

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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

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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

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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

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NOOTROPIC DRUGS(NEUROMETABOLIC
CEREBROPROTECTORS)
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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

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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

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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

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Piracetam (nootropil)
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Cerebrolysin
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Cinnarizin (stugeron)
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ADAPTOGENS
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Adaptogens

• Drugs of
• Ginseng, Schizandrum, Rodiola, Eleutherococcus,
  Leusea, Echinacea
• Apilac, propolis, mumie,
• heparin, dybazol

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GINSENG
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RODIOLA
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Eleutherococc
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Schizandrum
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Echinacea purpurea Maxima
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ADAPTOGENS

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

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Side effects of adaptogens

• Increasing of AP
• disturbance of sleep if administered in evening
  time, overwhelming excitation, psychical
  dependence

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Analeptics (Bemegridum, Camphora, Cordiaminum)
Camphora