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