drugs effecting psychical activity. psychotropic drugs drugs with depressive type of actoin...
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DRUGS EFFECTING DRUGS EFFECTING PSYCHICAL ACTIVITYPSYCHICAL ACTIVITY
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-: 3-1010 % % of Earth population suffer from of Earth population suffer from depression (depression (adults adults - - 10 %, 10 %, teenagersteenagers – 8 % – 8 %, children, children – 3 % – 3 %))
Depression and somatic-vegetative Depression and somatic-vegetative symptoms which accompany depression are symptoms which accompany depression are quite often psychical disorders which quite often psychical disorders which happen in general medical practice.happen in general medical practice.
There areThere are::1.1. EndogenEndogen ( (psychogenicpsychogenic)) depressiondepression – –
schizophreniaschizophrenia, , maniac-depressive psychosis maniac-depressive psychosis (bipolar disorder)(bipolar disorder)
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 of patients with depressive disorders don’t realize that they have any psychological problems don’t realize that they have any psychological problems
and complain only on certain somatic dischargesand complain only on certain somatic discharges
Most frequent complaints of patients with Most frequent complaints of patients with depression: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 dyskinesia, functional motor disorders, insomnia,
toothache, disorders of sexual activity, eczema and many other disorders
Function of adrenergic synapse in Function of adrenergic synapse in physiological conditionsphysiological conditions
ANTIDEPRESSANTSANTIDEPRESSANTS
Drugs which inhibit neuronal uptakeDrugs which inhibit neuronal uptake of of monoaminesmonoamines
1.1. Nonselective actionNonselective action – tricyclic compounds – tricyclic compounds ((blockblock uptakeuptake of noradrenaline and serotonineof noradrenaline and serotonine): ): imisinimisin, , amitriptilinamitriptilin
2.2. Selective actionSelective action: а) : а) heterocyclic compoundsheterocyclic compounds ( (block block neuronalneuronal uptakeuptake of noradrenalineof noradrenaline): ): amoxapinamoxapin, , maprotilinmaprotilin ((ludiomilludiomil));; б) б) selective blockers of neuronal uptake of selective blockers of neuronal uptake of serotoninserotonin: : fluoxetinfluoxetin ( (prozak, framexprozak, framex), ), sertralinsertralin ( (zoloftzoloft), ), paroxetinparoxetin ( (rexetinrexetin))
Inhibitors of monoaminoxidaseInhibitors of monoaminoxidase ( (IMAOIMAO))1.1. nonselectivenonselective ( (blockblock МАО-А МАО-А andand МАО-В): а) МАО-В): а) irreversibleirreversible
actionaction – – nialamidnialamid; ; bb) ) reversible actionreversible action – – transamintransamin
2.2. SelectiveSelective ІМАО ( ІМАО (blockblock МАО-А): МАО-А): moklobemidmoklobemid, , pirasidolpirasidol
Blockers of neuronalBlockers of neuronal reuptake reuptake of serotonin 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)
Blockers of neuronalBlockers of neuronal reuptake of serotoninreuptake 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 reuptake of serotoninreuptake 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: 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)
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 Even small doses of adrenomimetic (sympatomimetic(sympatomimetic) ) substances in such substances in such patient can cause patient can cause hypertensive crisis:hypertensive crisis:
Nose drops for rhinitisNose drops for rhinitisIf few drops were added to solutions of If few drops were added to solutions of
local anestheticslocal anestheticsIn case of administration of drugs which In case of administration of drugs which
contain pseudoephedrine (they are widely contain pseudoephedrine (they are widely used for common cold nowadays)used for common cold nowadays)
Diet in case of administration Diet in case of administration of IMAOof IMAO
It is necessary It is necessary to excludeto exclude such products which containsuch products which contain
DOPADOPA andand thiraminethiramine ((which is formed from casein during the process which is formed from casein during the process of transforming under the influence of bacteriaof transforming under the influence of bacteria) )
aged cheese, kefiraged cheese, kefirMarinated herringMarinated herringSmoked meat, fishSmoked meat, fish
Red vine, beer, yeastRed vine, beer, yeastBeansBeans
oranges, tangerines, lemons, grape, bananas, oranges, tangerines, lemons, grape, bananas, chocolate, caviar (red and black)…chocolate, caviar (red and black)…
……Any BAA are also dangerousAny 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 In case of administration of inhibitors of uptake of serotoninof uptake of serotonin the previously the previously indicated side effects are observed indicated side effects are observed much more rarelymuch more rarely
• Administration of antidepressants with Administration of antidepressants with any other drugs should be performed any other drugs should be performed only after precise studying of possible only after precise studying of possible negative consequences of their negative consequences of their interaction interaction
PSYCHOMOTOR PSYCHOMOTOR STIMULANTSSTIMULANTS
PSYCHOMOTOR STIMULANTSPSYCHOMOTOR STIMULANTS
• Derivatives of purine – caffeinecaffeine
• Phenilalkilamines – phenaminephenamine ((amphetamineamphetamine))
• Phenilalkilsydnonimins - sydnocarbsydnocarb
ADHD – ADHD – attention deficit hyperactivity disorder – attention deficit hyperactivity disorder –
more frequently in childrenmore frequently in children
• Cured by potent stimulators (ritalin, Cured by potent stimulators (ritalin, adderal and others)adderal and others)
• They all can provoke addiction !!!They all can provoke addiction !!!
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, retardnesssubdepression, 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 vesselsContraction of brain vessels• Dilation of kidney vessels, increasing of diuresisDilation of kidney vessels, increasing of diuresis• Dilation of coronary vesselsDilation of coronary vessels
In case of depression of centers of brain In case of depression of centers of brain stem (medulla oblongata) caffeine stem (medulla oblongata) caffeine
shows stimulating propertiesshows stimulating properties, , increases increases blood pressure, stimulates breathingblood pressure, stimulates breathing – –
analeptic actionanaleptic action
SIDE EFFECTS OF CAFFEINESIDE EFFECTS OF CAFFEINE• If administered regularlyIf administered regularly – –
psychological addictionpsychological addiction – – theismtheism,, which is accompanied by which is accompanied by development of abstinent syndromedevelopment of abstinent syndrome ((retardness, fatigue, somnolence, retardness, fatigue, somnolence, depressiondepression))
• ToleranceTolerance• Teratogenic action (innate Teratogenic action (innate
abnormalities)abnormalities)• Increasing of frequency of IHD, Increasing of frequency of IHD,
essential hypertensionessential hypertension• Acute attacks of ulcer diseaseAcute attacks of ulcer disease
(it increases gastric secretion(it increases gastric secretion))• Acute poisoning in case of overdosingAcute poisoning in case of overdosing
NOOTROPIC DRUGSNOOTROPIC DRUGS
((NEUROMETABOLIC NEUROMETABOLIC CEREBROPROTECTORS)CEREBROPROTECTORS)
Neurometabolic Neurometabolic cerebroprotectorscerebroprotectors
• Derivatives of pyrrolidoneDerivatives of pyrrolidone – – pyracetampyracetam ( (nootropilnootropil))• Derivatives of GABA Derivatives of GABA – – aminalon, sodium aminalon, sodium
oxybutyrateoxybutyrate• Neuropeptides Neuropeptides – – melatoninmelatonin, , sinacten-depotsinacten-depot• Cerebrovascular drugsCerebrovascular drugs – – sermionsermion ( (nicergolinnicergolin), ),
cavintoncavinton ( (vinpocetinvinpocetin), ), stugeronstugeron ( (cinnarisincinnarisin), ), pentoxyphyllinepentoxyphylline ( (trental, agapurinetrental, agapurine), ), xantynole xantynole nicotinatenicotinate
• Derivatives of piridoxine Derivatives of piridoxine – – piritinolpiritinol ( (encephabolencephabol))• Antioxidants Antioxidants – – mexidol, tocopherole acetatemexidol, tocopherole acetate• Other Other – – cerebrolysinecerebrolysine, , actovegin, solkoseryl, plant actovegin, solkoseryl, plant
preparationspreparations
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, SchizandrumGinseng, Schizandrum, , RodiolaRodiola, , EleutherococcusEleutherococcus, , LeuseaLeusea, ,
EchinaceaEchinacea
Apilac, propolis, mumieApilac, propolis, mumie, ,
heparin, dibazolheparin, dibazol
GINSENGGINSENG
RODIOLARODIOLA
EleutherococcEleutherococcusus
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