Psychiatric%20Drugs.%20Central%20Nervous%20System%20Stimulants

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Psychiatric Drugs. Central Nervous System
Stimulants
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Analeptic

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

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Analeptics (Bemegridum, Camphora, Cordiaminum)
Camphora
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CNS Stimulants Adverse effects

• CVS Palpitation, tachycardia, hypertension,
  angina, dyshythmia
• CNS Nervousness, restlessness, anxiety
• Endocrine Hypoglycemia, hyperglycemia
• GIT Nausea, vomiting,diarrhea

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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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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.

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Chemical Properties
Molar Mass 194.19 g mol-1
Density 1.2 g/cm³ Phase Solid
Melting Point 237 C Boiling Point 178 C
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Caffeine
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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.

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Caffeine

• AP
• Hate rate
• Respiratory stimulation
• Adjunctive effect

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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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Amphetamines

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

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Amphetamines

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

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ADHD attention deficit hyperactivity disorder
more frequently in children

• Cured by potent stimulators (ritalin, adderal and
  others)
• They all can provoke addiction !!!

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Methylxanthines

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

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Anorexants

• Central acting (Benzphetamine, diethylpropion,
  Sibutramine)
• Metabolism acting (orlistat)

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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 tricyclic compounds (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 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-??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 reuptake 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 reuptake 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
  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)

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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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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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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

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

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GINSENG
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RODIOLA
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Eleutherococcus
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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