Activating CNS agentsActivating CNS agents
Lector prof. Posokhova K.A.Lector prof. Posokhova K.A.
PSYCHOTROPIC DRUGSPSYCHOTROPIC DRUGSDrugs withDrugs with depressivedepressive type of actointype of actoin
1.1. Neuroleptics Neuroleptics ((antipsychoticantipsychotic))2.2. Tranquilizers Tranquilizers ((anxiolyticsanxiolytics))3.3. Sedative drugsSedative drugs4.4. Normotymics Normotymics ((tymolepticstymoleptics, , tymoanalepticstymoanaleptics))
Drug withDrug with stimulativestimulative actionaction1.1. Antidepressants Antidepressants 2.2. Psychomotor stimulantsPsychomotor stimulants3.3. Nootropic drugsNootropic drugs4.4. Drugs which increase general tone Drugs which increase general tone
((adaptogensadaptogens))
PsychotomimeticsPsychotomimetics ((psychodyslepticspsychodysleptics))1.1. LSD LSD 2.2. Cannabis sativa L.Cannabis sativa L.
ANTIDEPRESSANTSANTIDEPRESSANTS
WHOWHO: 3-6 % : 3-6 % of Earth population suffer from of Earth population suffer from depressiondepression
Depression and somatic-vegetative symptoms Depression and somatic-vegetative symptoms which accompany depression are quite often which accompany depression are quite often psychical disorders which happen in general psychical disorders which happen in general medical practice.medical practice.
There areThere are::
1.1. EndogenEndogen ( (psychogenicpsychogenic)) depressiondepression – – schizophreniaschizophrenia, , maniac-depressive psychosismaniac-depressive psychosis
2.2. Secondary Secondary ((somatogenicsomatogenic)) depressiondepression – – organic diseasesorganic diseases ( (oncology patientsoncology patients, , hypertensionhypertension, , ulcer diseaseulcer disease, , climacteric disorders etc.climacteric disorders etc.))
More thanMore than 50 % 50 % of patients with depressive disorders don’t of patients with depressive disorders don’t realize that they have any psychological problems and realize that they have any psychological problems and
complain only on certain somatic dischargescomplain only on certain somatic discharges
Most frequent complaints of patients with depressionFeeling 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
Function of adrenergic synapse in Function of adrenergic synapse in physiological conditionsphysiological conditions
ANTIDEPRESSANTSANTIDEPRESSANTS
Drugs which inhibit neuronal uptake of monoamines
1. Nonselective action (block uptake of noradrenaline and serotonine): imisin, amitriptilin
2. 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)1. nonselective (block МАО-А and МАО-В): а) irreversible
action – nialamid; b) reversible action – transamin
2. Selective ІМАО (block МАО-А): moklobemid, pirasidol
Blockers of neuronalBlockers of neuronal uptake of uptake of serotonin 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)
Blockers of neuronalBlockers of neuronal uptake of serotoninuptake of serotonin
fluoxetinfluoxetin, , sertralinsertralin, , paroxetinparoxetin
Mechanism of actionMechanism of actionIncreasing of active concentration of serotonin in synaptic cleft on a level
of postsynaptic
5-НТ2 serotonin receptors of cerebral structures
Blockers of neuronalBlockers of neuronal uptake of serotoninuptake of serotonin
fluoxetinfluoxetin, , sertralinsertralin, , paroxetinparoxetin
Mechanism of action of IMAOMechanism of action of IMAO
Usage of antidepressantsUsage of antidepressants
SchizophreniaSchizophrenia, , MDSMDS
Atherosclerosis of brainAtherosclerosis of brain
Reactive depressionsReactive depressions
Parkinsonism Parkinsonism
Organic diseases of CNSOrganic diseases of CNS
Oncology patientsOncology patients
General somatic diseasesGeneral somatic diseases
Psychotropic action of Psychotropic action of antidepressantsantidepressants
1. Drugs with psychosedativepsychosedative action:
ААmitriptilinmitriptilin, , maprotilinmaprotilin,, asafen asafen, , fluvoxaminfluvoxamin
2. Drugs with psychostimulativepsychostimulative action:
ImisinImisin, , nialamidnialamid, , fluoxetinfluoxetin
3. Drugs with regulativeregulative influence
PirasidolPirasidol
Principles of antidepressants usagePrinciples 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
Side effects of antidepressantsSide effects of antidepressants
• ММ-cholinoblocking action-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 effectAlpha-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)
Side effects of antidepressantsSide effects of antidepressants
• Acute attacks of epilepsy epilepsy
• CardiotoxicCardiotoxic action (sudden death), three- cyclic antidepressants increase arrhythmogenic activity of drugs for general anesthesia, antihistamines etc.
• Combination of three-cyclic antidepressants Combination of three-cyclic antidepressants with IMAO is absolutely contraindicatedwith IMAO is absolutely contraindicated:: danger of development of hypertensive crisis, seizures, rapid excitation, tachycardia, cardiac arrhythmias, increasing of temperature
Rules of transferring from one kind of Rules of transferring from one kind of antidepressants to anotherantidepressants to another
• From three-cyclic to IMAO – break time– 2-3 days
• From IMAO to three-cyclic – break time – not less than 2 weeks
It is absolutely contraindicated to It is absolutely contraindicated to administer adreno(sympato)mimetics in administer adreno(sympato)mimetics in case of treatment with antidepressantscase of treatment with antidepressants
Even small doses of adrenomimetic (sympatomimetic) substances in such patient
can cause hypertensive crisis: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)
Diet in case of administration Diet in case of administration of IMAOof 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, kefirMarinated herringSmoked meat, fish
Red vine, beer, yeastBeans
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 In case of treatment with IMAO new products should be introduced intointroduced into ration very carefullyration very carefully
• 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
PSYCHOMOTOR PSYCHOMOTOR STIMULANTSSTIMULANTS
PSYCHOMOTOR STIMULANTSPSYCHOMOTOR STIMULANTS
• Derivatives of purine – caffeinecaffeine
• Phenilalkilamines – phenaminephenamine ((amphetamineamphetamine))
• Phenilalkilsydnonimins - sydnocarbsydnocarb
Properties of psychomotor Properties of psychomotor stimulantsstimulants
• Stimulate intellectual activity, speed up thinking processes, temporarily eliminate tiredness, somnolence
• Eliminate such manifestations of neurosis neurosis as:as: subdepression, fatigue, retardness subdepression, fatigue, retardness
• Aren’t able to eliminate endogen depression, which accompanies psychical diseases
Caffeine Caffeine
Mechanism of action
• Binds to adenosine adenosine (“(“purinepurine”) ”) receptorsreceptors in brain (endogen ligand of these receptors – adenosine decreases processes of excitation in CNS)
• Inhibiting of phosphodiesteraseInhibiting of phosphodiesterase, which leads to accumulation of cAMP and stimulation of many physiological processes and metabolism
CaffeineCaffeine
Usage of psychostimulating Usage of psychostimulating influence of caffeineinfluence 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
Influence of caffeine on Influence of caffeine on cardiac-vascular systemcardiac-vascular system
Vessels Vessels 1. Stimulation of vasomotor center –
contraction of vessels, increasing of AP2. Peripheral myotropic spasmolytic action
– dilation of vessels, decreasing of AP
HeartHeart1. Central action (increasing of n. vagus
tone) – bradycardia2. Peripheral action (direct influence on
heart) – tachycardia, possible extrasystolia
Influence of caffeine on cardio-Influence of caffeine on cardio-vascular systemvascular 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 actionanaleptic action
SIDE EFFECTS OF CAFFEINESIDE 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
NOOTROPIC DRUGSNOOTROPIC DRUGS
((NEUROMETABOLIC NEUROMETABOLIC CEREBROPROTECTORS)CEREBROPROTECTORS)
Neurometabolic Neurometabolic cerebroprotectorscerebroprotectors
• 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
Properties of nootropic drugsProperties 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
Administration of nootropic drugsAdministration 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
Piracetam Piracetam ((nootropilnootropil))
CerebrolysinCerebrolysin
CinnarizinCinnarizin ( (stugeronstugeron))
ADAPTOGENSADAPTOGENS
AdaptogensAdaptogensDrugs of
Ginseng, Schizandrum, Rodiola, Eleutherococcus, Leusea,
Echinacea
Apilac, propolis, mumie, heparin, dybazol
GINSENGGINSENG
RODIOLARODIOLA
EleutherococcEleutherococc
Schizandrum
Echinacea purpurea MaximaEchinacea purpurea Maxima
ADAPTOGENSIncrease general resistance of the organism
towards unfavorable factors
Stimulating actionAntistress action Anabolic action
Side effects of adaptogens
Increasing of AP
disturbance of sleep if administered in evening time, overwhelming
excitation, psychical dependence
AnalepticsAnaleptics ( (BemegridumBemegridum,, Camphora Camphora, , CordiaminumCordiaminum))
CamphoraCamphora