PSYCHOTROPIC DRUGSPSYCHOTROPIC DRUGS

Lector prof. Posokhova K.A.Lector prof. Posokhova K.A.

PSYCHOTROPIC DRUGSPSYCHOTROPIC DRUGSDrugs with Drugs with depressivedepressive type of actiontype of action

1.1. Neuroleptics Neuroleptics ((antipsychoticsantipsychotics))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.

NEUROLEPTICSNEUROLEPTICSDerivatives of Derivatives of phenotiazinephenotiazine:: aminasineaminasine, , triftiazinetriftiazine, , etaperasine, tioridazineetaperasine, tioridazine

Derivatives of Derivatives of tioxantentioxanten: : chlorprotixenchlorprotixen

Derivatives of Derivatives of butyrophenonbutyrophenon: : galoperidolgaloperidol, , droperidoldroperidol

Derivatives of Derivatives of piperasine-piperasine-dibenzodiazepinedibenzodiazepine: : clozapineclozapine

Derivatives of Derivatives of indoleindole: : reserpin, sulpyrid reserpin, sulpyrid (eglonil)(eglonil)

NEUROPLEPTICSNEUROPLEPTICS““TypicalTypical”” – – derivatives of phenotiazine, derivatives of phenotiazine,

tioxanten, butyrophenon – they cause tioxanten, butyrophenon – they cause disorders of extrapyramidal system disorders of extrapyramidal system functionfunction – – syndrome of syndrome of parkinsonismparkinsonism

“ “AtypicalAtypical”” – – derivatives of indole, derivatives of indole, benzodiazepinebenzodiazepine – – they cause those they cause those negative reactions very rarelynegative reactions very rarely

Aminasine (chlorpromasine)Aminasine (chlorpromasine)

1951 – 1951 – aminasine was introduced into aminasine was introduced into clinical practiceclinical practiceIt brought considerable changes into It brought considerable changes into situations of psychiatric clinicssituations of psychiatric clinicsBefore appearance of aminasine for Before appearance of aminasine for treatment of psychologically sick patients treatment of psychologically sick patients insulin or electric shock were widely usedinsulin or electric shock were widely used, , in in some casessome cases - - lobotomylobotomy

Mechanism of action of Mechanism of action of neurolepticsneuroleptics

Influence on Influence on dopamine dopamine ((DD22),), noradrenergicnoradrenergic, , serotoninergicserotoninergic, , GABAGABA--

ergicergic, , cholinergiccholinergic receptorsreceptors

Properties of neurolepticsProperties of neuroleptics

Antipsychotic actionAntipsychotic action - - they eliminate they eliminate productive symptoms of psychosisproductive symptoms of psychosis ((delirium and hallucinationsdelirium and hallucinations), ), affective affective disordersdisorders

They eliminate psychomotor excitationThey eliminate psychomotor excitation with condition of consciousness with condition of consciousness

Administration of antipsychotic Administration of antipsychotic action of action of neurolepticsneuroleptics

Treatment of psychosisTreatment of psychosisSchizophreniaSchizophrenia

Maniac-depressive psychosisManiac-depressive psychosis

Alcohol psychosisAlcohol psychosis

Reactive psychosisReactive psychosis

In a case of psychomotor excitationIn a case of psychomotor excitationof various etiologyof various etiology

Delirium tremens Delirium tremens – – alcohol psychosisalcohol psychosis

Influence of neuroleptics on Influence of neuroleptics on psychical activitypsychical activity

1. 1. Drugs with Drugs with psychosedative actionpsychosedative action – – they they cause condition of psychomotor indifference cause condition of psychomotor indifference ((apathy, apathy, decreasing of moving activitydecreasing of moving activity,, retarded emotions and retarded emotions and wishes, disappearance of initiativewishes, disappearance of initiative) )

Aminazine, clozapineAminazine, clozapine ( (leponexleponex), ), chlorprotyxenchlorprotyxen, , haloperidolhaloperidol, , droperidoldroperidol

Peculiarities of usagePeculiarities of usage: : psychosis with manifestations psychosis with manifestations of excitationof excitation

ContraindicationsContraindications: : psychosis with retardness, inertia, psychosis with retardness, inertia, depression, stupor, apatho-abulic syndromedepression, stupor, apatho-abulic syndrome

Neuroleptics withNeuroleptics with psychosedative actionpsychosedative action

Influence of neuroleptics on Influence of neuroleptics on psychical activitypsychical activity

2. 2. Drugs which stimulate psychical Drugs which stimulate psychical activityactivity ((increase mimics and livelinessincrease mimics and liveliness, , increase increase moving activity, improve the moodmoving activity, improve the mood))

Triftazin, ethaperazin, moditen, majeptilTriftazin, ethaperazin, moditen, majeptil Peculiarities of usagePeculiarities of usage: : psychosis with psychomotor retardnesspsychosis with psychomotor retardness, ,

apatho-abulic conditionsapatho-abulic conditions, , stupor conditionsstupor conditions ContraindicationsContraindications:: affective disturbancesaffective disturbances, ,

mania, psychomotor excitation mania, psychomotor excitation

Other properties and indications Other properties and indications for administration of neurolepticsfor administration of neuroleptics

Drugs with psychosedative actionDrugs with psychosedative action – – forfor potentiationpotentiation of of actionaction of soporifics, opioid and nonopioid analgesics, drugs of soporifics, opioid and nonopioid analgesics, drugs for general anesthesia, local anestheticsfor general anesthesia, local anesthetics,, for example, for example, neuroleptanalgesianeuroleptanalgesiaAnti-emetic actionAnti-emetic action ( (elimination of elimination of vomiting of central vomiting of central originorigin): ): brain tumors, radial and chemical therapy, intestinal brain tumors, radial and chemical therapy, intestinal impassability, intoxication with heart glycosides, impassability, intoxication with heart glycosides, apomorphine and other drugsapomorphine and other drugsDecreasing ofDecreasing of body temperaturebody temperature (only in the case of (only in the case of simultaneous hypothermia)simultaneous hypothermia)Decreasing of Decreasing of blood pressureblood pressure ((alpha-adrenoblocking alpha-adrenoblocking propertiesproperties – – aminasine, droperidolaminasine, droperidol) – ) – in case of hypertensive in case of hypertensive crisis, lungs edemacrisis, lungs edema

Side effects of neurolepticsSide effects of neurolepticsExtrapyramidal disordersExtrapyramidal disorders:: muscular hypertonusmuscular hypertonus, , general constraint, tremor of hands, tongue, mandible, head, general constraint, tremor of hands, tongue, mandible, head, seizure contractions of muscles, vegetative crisisseizure contractions of muscles, vegetative crisis

For treatment For treatment – – cyclodolcyclodol (levodopa is contraindicated (levodopa is contraindicated because it diminishes therapeutic effect of neurolepticsbecause it diminishes therapeutic effect of neuroleptics))Orthostatic collapseOrthostatic collapseComplicated nose breathing, hypostatic, aspirate pneumoniaComplicated nose breathing, hypostatic, aspirate pneumoniaDyspeptic disordersDyspeptic disorders: : anorexia, changes of tasteanorexia, changes of tasteAbdominal painAbdominal painConstipationConstipationDamage of the liverDamage of the liver ( (cholestasis)cholestasis)Granulocytopenia Granulocytopenia ((especially clozapinespecially clozapin))Hyperglycemia, dysmenorrheaHyperglycemia, dysmenorrhea, , galactorrheagalactorrhea, , hyperthyrosis, hyperthyrosis, gynecomastia, impotencegynecomastia, impotenceAminasine has a considerable irritable actionAminasine has a considerable irritable action

syndrome of parkinsonismsyndrome of parkinsonism

TRANQUILIZERSTRANQUILIZERSAgonists of benzodiazepine receptorsAgonists of benzodiazepine receptors::

- - derivatives of benzodiazepinederivatives of benzodiazepine – – chlozepid, chlozepid, sybazon, phenazepam, gidazepamsybazon, phenazepam, gidazepam

Agonists of serotonine receptorsAgonists of serotonine receptors: : buspyronebuspyrone

Drugs with other mechanisms of actionDrugs with other mechanisms of action::

-- derivatives of diphenilmethanderivatives of diphenilmethan: : amisylamisyl

- - derivatives of propanediolederivatives of propanediole: : meprotanmeprotan

Properties of tranquilizersProperties of tranquilizers

Anxiolytic propertiesAnxiolytic properties – – eliminate feeling eliminate feeling of anxiety, restlessness, fear, of anxiety, restlessness, fear, aggressiveness, irritabilityaggressiveness, irritability, , cause peace, cause peace, careness, decreasing of moving activitycareness, decreasing of moving activity

Hypnotic Hypnotic ((somnolentsomnolent) ) actionaction

MyorelaxingMyorelaxing actionaction ( (of central genesisof central genesis))

AntiseizureAntiseizure actionaction

Duration of action of tranquilizersDuration of action of tranquilizers

Drugs of Drugs of long lastinglong lasting actionaction::

diazepamdiazepam, phenazepam, chlozepid, phenazepam, chlozepid

Drugs of Drugs of mediummedium action durationaction duration: :

lorazepam, alprazolamlorazepam, alprazolam

Drugs of Drugs of shortshort action durationaction duration: :

midazolammidazolam

““DAYDAY” ” TRANQUILIZERSTRANQUILIZERS

GidazepamGidazepam

MezapamMezapam ( (rudotelrudotel))

GrandaxynGrandaxyn ( (tophizopamtophizopam))

TrioxazynTrioxazyn

BuspyronBuspyron

Administration of tranquilizersAdministration of tranquilizers

Anxiolytic actionAnxiolytic actionTreatment of neurosis, accompanied by fear, Treatment of neurosis, accompanied by fear, anxiety, exertion, increased irritability, insomniaanxiety, exertion, increased irritability, insomnia

In case of headache and heart pain of neurotic In case of headache and heart pain of neurotic originorigin, , so called organic neurosisso called organic neurosis

In case of abstinence in alcohol and drugs addictsIn case of abstinence in alcohol and drugs addicts

In case of diencephalons crisisIn case of diencephalons crisis ( (sybazonsybazon))

Tranquilizers do not diminish productive Tranquilizers do not diminish productive symptoms of psychosissymptoms of psychosis!!

Usage of tranquilizersUsage of tranquilizers

HypnoticHypnotic actionaction – – they cause sleep, which they cause sleep, which is very close to physiological one is very close to physiological one according to its parametersaccording to its parameters

NitrazepamNitrazepam PhenazepamPhenazepam

DiazepamDiazepam ChlozepidChlozepid

Depression of CNSDepression of CNS – – forfor atharalgesiaatharalgesia

SybazonSybazon MidazolamMidazolam

Administration of tranquilizersAdministration of tranquilizers

Anti-seizure and myorelaxing actionAnti-seizure and myorelaxing action ((depression of CNS structures, braking polysynaptic depression of CNS structures, braking polysynaptic

spinal reflexesspinal reflexes) )

sybazonsybazon, , fenazepamfenazepamIn a case of seizures of any etiologyIn a case of seizures of any etiology (epileptic (epileptic status, tetanus, poisoning with seizure causing status, tetanus, poisoning with seizure causing poisons)poisons) sybazon is introduced intravenously sybazon is introduced intravenously (intramuscularly) – (intramuscularly) – 2-4 2-4 ml of ml of 0,5 % 0,5 % solution solution repeatedlyrepeatedly ( (maximal daily dosemaximal daily dose – 14 – 14 mlml))

To eliminate muscle tension in a case of radiculitis, To eliminate muscle tension in a case of radiculitis, arthritis, myositis, bursitisarthritis, myositis, bursitis

SeizuresSeizures(tetanus)(tetanus)

drug of a first choice drug of a first choice

- - SibazonSibazon

SIDE EFFECT OF TRANQUILIZERSSIDE EFFECT OF TRANQUILIZERSPsychological and physical addictionPsychological and physical addiction

ProphylaxisProphylaxis: :

1.1. Duration of treatment course should not be more than 2 monthsDuration of treatment course should not be more than 2 months

2.2. Repeated course Repeated course – – not earlier than after 3 weeks breaknot earlier than after 3 weeks break

Sleepiness, reeling walk, retarded reactionsSleepiness, reeling walk, retarded reactions tranquilizers should not be administered in ambulatories to people tranquilizers should not be administered in ambulatories to people

whose professions are connected with quick reactionswhose professions are connected with quick reactions

Paradox reaction of excitation, insomniaParadox reaction of excitation, insomnia

Dizziness, decreasing of libido, Dizziness, decreasing of libido, disturbances of menstrual cycle disturbances of menstrual cycle

Uncontrolled urination, defecation, ataxia, Uncontrolled urination, defecation, ataxia, dysartriadysartria

Acute poisoning in case of overdosingAcute poisoning in case of overdosing

FLUMAZENILFLUMAZENIL ( (ANEXATANEXAT)) ANTAGONIST OF TRANQUILIZERSANTAGONIST OF TRANQUILIZERS

Combination of tranquilizers Combination of tranquilizers with alcohol-containing with alcohol-containing

drinks is absolutely drinks is absolutely contraindicatedcontraindicated

(pathological alcohol intoxication)(pathological alcohol intoxication)

LITHIUM DRUGSLITHIUM DRUGS

LITHIUM CARBONATELITHIUM CARBONATE

INDICATIONS FOR ADMINISTRATION INDICATIONS FOR ADMINISTRATION OF LITHIUM DRUGSOF LITHIUM DRUGS

Prophylaxis and treatment of endogen Prophylaxis and treatment of endogen (affective) psychosis(affective) psychosis: : maniac-depressive, maniac-depressive, schizo-affective, organic affectiveschizo-affective, organic affective

Prophylaxis and treatment of affective Prophylaxis and treatment of affective disturbances in patients with epilepsydisturbances in patients with epilepsy,, chronic alcoholism, in psychopaths chronic alcoholism, in psychopaths

Method of lithium drugs Method of lithium drugs administration administration

It is administered orallyIt is administered orallyTreatment concentration of lithium in Treatment concentration of lithium in blood – blood – 0,6-0,8 0,6-0,8 mmolmmol//ll ( (not more thannot more than 1,5-1,6 1,5-1,6 mmolmmol//ll))The effect develops after few daysThe effect develops after few days – 5-6 – 5-6 monthsmonthsSmall width of therapeutic actionSmall width of therapeutic action ((treatment with lithium drugs needs the treatment with lithium drugs needs the same attentiveness from the doctor as same attentiveness from the doctor as treatment with insulintreatment with insulin))

Acute poisoning with lithium drugsAcute poisoning with lithium drugsIt develops if the concentration is overIt develops if the concentration is over 1,5-2 1,5-2 mmolmmol//ll

Development of constant nausea and tremor during Development of constant nausea and tremor during treatment with lithium treatment with lithium means that the dose should be means that the dose should be

decreaseddecreasedSYMPTOMS OF POISONINGSYMPTOMS OF POISONING

Nausea, vomiting, diarrheaNausea, vomiting, diarrheatremor, general muscular weaknesstremor, general muscular weakness, , twitching musclestwitching musclesNoise in the ears, unclear visionNoise in the ears, unclear vision, , somnolence, dysartriasomnolence, dysartria

Changes of handwritingChanges of handwriting: : massive, boldmassive, boldLocal neurological symptomsLocal neurological symptoms, , meningismmeningism

OliguriaOliguriaChanges in ECGChanges in ECG, , arrhythmiaarrhythmia, , decreasing of BPdecreasing of BP

Sopor, comaSopor, comaDeathDeath – – from hypostatic pneumoniafrom hypostatic pneumonia

Treatment of intoxication with lithium Treatment of intoxication with lithium drugsdrugs

A lot of drinking, 10% solution of sodium chloride A lot of drinking, 10% solution of sodium chloride (till 300 ml/day), 5(till 300 ml/day), 5% % solution of sodium solution of sodium hydrocarbonatehydrocarbonate ( (tilltill 300 300 mlml / / dayday)) intravenously intravenously

Mannit, ureaMannit, urea ( (saluretics are contraindicatedsaluretics are contraindicated!)!)

Pyracetam, vinpocetinPyracetam, vinpocetin

Prophylaxis of pneumoniaProphylaxis of pneumonia – – antibioticsantibiotics

Control of water-electrolyte balance, acid-base Control of water-electrolyte balance, acid-base balancebalance

Symptomatic therapy, for example, in case of Symptomatic therapy, for example, in case of seizures - sybazonseizures - sybazon

Haemodialysis if necessaryHaemodialysis if necessary

Prophylaxis of intoxication with Prophylaxis of intoxication with lithium drugslithium drugs

Salt in day ration should not be limitedSalt in day ration should not be limited

A lot of drinkingA lot of drinking

Do not indicate saluretics, sweat-Do not indicate saluretics, sweat-stimulating drugsstimulating drugs

Heavy physical work or other situations, Heavy physical work or other situations, accompanied by considerable sweating accompanied by considerable sweating should be avoidedshould be avoided

SEDATIVE DRUGSSEDATIVE DRUGS

BromidesBromides

Drugs of plant originDrugs of plant origin: : valerian, dog nettle, valerian, dog nettle, melissa, passiflora etc.melissa, passiflora etc.

They do not cause addiction, somnolence, They do not cause addiction, somnolence, myorelaxation, ataxiamyorelaxation, ataxia

ValerianaValeriana

PASSIFLORAPASSIFLORA

Leonurus L.Leonurus L. dog nettledog nettle

ADMINISTRATION OFADMINISTRATION OF

SEDATIVE DRUGSSEDATIVE DRUGS

NeurosisNeurosis

NeurastheniaNeurasthenia

Hysteria Hysteria

Increased irritabilityIncreased irritability

Insomnia Insomnia

Primary stages of essential hypertensionPrimary stages of essential hypertension

BromismBromism

Cause Cause – – accumulation of bromide ions in accumulation of bromide ions in organism in case of their prolonged organism in case of their prolonged administration as a result of material administration as a result of material accumulationaccumulation

SymptomsSymptoms: : rhinitisrhinitis, , cough, conjunctivitis, skin cough, conjunctivitis, skin rash, general weakness, memory disordersrash, general weakness, memory disorders

TreatmentTreatment: : sodium chloridesodium chloride (10-20 (10-20 gg / / dayday), ), a a lot of drinkinglot of drinking (3-5 (3-5 ll / / dayday), ), regular and regular and frequent cleaning of skin and digestive tractfrequent cleaning of skin and digestive tract

DRUGS FOR GENERAL DRUGS FOR GENERAL ANESTHESIAANESTHESIA

General anesthesia = Narcosis General anesthesia = Narcosis ((from the Greek from the Greek narkosis – narkosis – numbness numbness, , rigidityrigidity)) – –

Generalized reversible depression of the central nervous Generalized reversible depression of the central nervous system such that perception of all senses is ablated,system such that perception of all senses is ablated,condition which is characterized by loss of condition which is characterized by loss of consciousness, pain feelings, depression of reflexes and consciousness, pain feelings, depression of reflexes and relaxation of skeletal muscles and which is obtained by relaxation of skeletal muscles and which is obtained by administration of drugs for general anesthesiaadministration of drugs for general anesthesia

“Gentlemen, this is no humbug.” 1846 TG Morton: First public demonstration of ether administration

for excision of neck mass

Desirable Components of Desirable Components of AnesthesiaAnesthesia

1.1. Immobility in response to noxious stimulusImmobility in response to noxious stimulus

2.2. AmnesiaAmnesia

3.3. AnalgesiaAnalgesia

4.4. UnconsciousnessUnconsciousness

5.5. Muscle relaxationMuscle relaxation

6.6. Loss of autonomic reflexesLoss of autonomic reflexes

7.7. AnxiolysisAnxiolysis

Inhalational agentsInhalational agentsprimarily used for maintenanceprimarily used for maintenance

•Volatile agentsVolatile agentsIsofluraneIsofluraneSevofluraneSevofluraneDesfluraneDesfluraneHalothaneHalothane ( (FtorothaneFtorothane)) EnfluraneEnflurane

•Anesthetic gasesAnesthetic gasesNitrous Oxide Nitrous Oxide - currently used- currently used

CLASSIFICATION OF GENERAL CLASSIFICATION OF GENERAL ANESTHETICSANESTHETICS

Intravenous agentsIntravenous agentsprimarily used for inductionprimarily used for induction

•Barbiturates (Thiopental-Barbiturates (Thiopental-sodium)sodium)•Benzodiazepines (Benzodiazepines (Midasolam, Midasolam, diazepam)diazepam)•EtomidateEtomidate•KetamineKetamine•PropofolPropofol•PropanididPropanidid•Sodium oxybutyrateSodium oxybutyrate•PredionPredion

CLASSIFICATION OF GENERAL CLASSIFICATION OF GENERAL ANESTHETICSANESTHETICS

General General anesthesia can be anesthesia can be caused by a caused by a remarkable remarkable number of number of structurally structurally diverse moleculesdiverse molecules

Unitary HypothesisUnitary Hypothesis

Xe

Isoflurane

Halothane

......Cellular (synapses)Cellular (synapses)

MolecularMolecular(lipids & (lipids &

receptors)receptors)

Molecular Mechanism(s) of General Molecular Mechanism(s) of General AnesthesiaAnesthesia

A Working HypothesisA Working Hypothesis

Anesthetics Anesthetics enhance inhibitoryenhance inhibitory postsynaptic channel activity postsynaptic channel activity (GABA(GABAAA and glycine receptors) and glycine receptors)

Anesthetics Anesthetics inhibit excitatoryinhibit excitatory synaptic channel activity (nicotinic synaptic channel activity (nicotinic acetylcholine and glutamate acetylcholine and glutamate receptors)receptors)

Effects of General AnesthesiaEffects of General Anesthesia

Low Dose EffectsLow Dose Effects

•AmnesiaAmnesia

•EuphoriaEuphoria

•AnalgesiaAnalgesia

•HypnosisHypnosis

•ExcitationExcitation

•HyperreflexiaHyperreflexia

High Dose EffectsHigh Dose Effects

•Deep sedationDeep sedation

•Muscle relaxationMuscle relaxation

•Diminished motor responsesDiminished motor responses

•Diminished autonomic Diminished autonomic responsesresponses

•Myocardial protection from Myocardial protection from ischemiaischemia

•Cardiovascular/respiratory Cardiovascular/respiratory depressiondepression

•HypothermiaHypothermia

• MAC: MAC: mminimum inimum aalveolar lveolar cconcentration oncentration

• MAC is the concentration of MAC is the concentration of anesthetic that produces anesthetic that produces immobility in 50% of patients immobility in 50% of patients exposed to a noxious exposed to a noxious stimulus.stimulus.

• MACMACawakeawake: MAC at which response : MAC at which response to commands are lost to commands are lost

• amnesia, loss of awarenessamnesia, loss of awareness

• MACMACBARBAR: : bblunt lunt aautonomic utonomic rresponseesponse• MACMACintubationintubation: response to intubation: response to intubation

Measures of Anesthetic PotencyMeasures of Anesthetic Potency

Stages of narcosisStages of narcosis

І. І. Stage of analgesia Stage of analgesia Loss of pain feelings along with normal or Loss of pain feelings along with normal or

dimmed consciousnessdimmed consciousness

Duration Duration fromfrom the beginning of inhalation of the beginning of inhalation of

narcosis substance and till the moment of narcosis substance and till the moment of loss of patient’s consciousnessloss of patient’s consciousness

Sometimes during this stage small Sometimes during this stage small surgical interventions are performedsurgical interventions are performed ((opening of abscesses, teeth extraction, opening of abscesses, teeth extraction, taking of the stitches etc.taking of the stitches etc.))

ІІ. ІІ. Stage of excitation (no desirable!!! Stage of excitation (no desirable!!! dangerous)dangerous)

Duration Duration from the moment of loss of patient’s consciousness from the moment of loss of patient’s consciousness till the stage of surgical narcosistill the stage of surgical narcosis

Complications Complications language and motor excitement,language and motor excitement,increasing of secretor activity of salivary and bronchial increasing of secretor activity of salivary and bronchial glandsglands,,vomiting,vomiting, variation of arterial pressurevariation of arterial pressure,,changes of breathing frequencychanges of breathing frequency

Heavy complicationsHeavy complications

Laryngospasm, bronchospasm, respiratory arrest, Laryngospasm, bronchospasm, respiratory arrest, cardiac arrhythmias, cardiac arrestcardiac arrhythmias, cardiac arrest

ІІІ. ІІІ. Stage of surgical anesthesiaStage of surgical anesthesia11st levelst level

Skeletal muscles aren’t relaxedSkeletal muscles aren’t relaxed, , conjunctive and pharyngeal reflexes conjunctive and pharyngeal reflexes disappeardisappear ( (it is possible to perform intubationsit is possible to perform intubations))

22nd levelnd levelReaction of frequent breathing as a respond cut on the skin disappearReaction of frequent breathing as a respond cut on the skin disappear

((deep analgesiadeep analgesia),), laryngeal reflexes disappearlaryngeal reflexes disappear ( (it is possible to perform endotracheal it is possible to perform endotracheal

intubationintubation);); good miorelaxationgood miorelaxation

33rd levelrd levelDecreasing of blood pressureDecreasing of blood pressure,,

Full relaxation of musclesFull relaxation of muscles,, step by step intercostal muscles get turned off,step by step intercostal muscles get turned off,

Type of breathing changes into abdominalType of breathing changes into abdominal; ; Corneal and pupil reflexes disappearCorneal and pupil reflexes disappear

44thth level levelmuscular tone is lowmuscular tone is low,,

full paralysis of intercostal musclesfull paralysis of intercostal muscles;; decreasing of blood pressure;decreasing of blood pressure;

dilated pupil which don’t react on lightdilated pupil which don’t react on light

IV. IV. Agony stageAgony stage ( (occurs in a case of occurs in a case of overdosing of drugs for narcosisoverdosing of drugs for narcosis))

Characteristics Characteristics decreasing of breathing and vaso-motor decreasing of breathing and vaso-motor

centers of medulla oblongatacenters of medulla oblongata

Typical manifestationsTypical manifestationsfull paralysis of breathing muscles, full paralysis of breathing muscles,

respiratory arrest, collapse; cardiac arrestrespiratory arrest, collapse; cardiac arrest

Surgical interventions are Surgical interventions are performed on 1st and 2nd performed on 1st and 2nd

levels, approximately till half of levels, approximately till half of 3rd level of third stage of 3rd level of third stage of

narcosisnarcosis

Drugs for inhalative Drugs for inhalative narcosisnarcosis

Ether for narcosisEther for narcosisNarcosis develops afterNarcosis develops after 10-20 10-20 minmin, , stage of excitationstage of excitation - 10-20 - 10-20 minmin, , strongly expressed after-narcosis strongly expressed after-narcosis depressiondepression, , high width of narcotic action (broad high width of narcotic action (broad therapeutic window) therapeutic window)

Side effects and complicationsSide effects and complicationsbright stage of excitationbright stage of excitation

Increasing of tone of n. vagiIncreasing of tone of n. vagiIncreasing of secretion of salivary, bronchial glands, coughing; Increasing of secretion of salivary, bronchial glands, coughing; laryngospasm, bronschospasm, vomiting with the following laryngospasm, bronschospasm, vomiting with the following aspiration of the masses bradycardia, stop of heart beataspiration of the masses bradycardia, stop of heart beat

Increasing of tone of sympathetic nervous systemIncreasing of tone of sympathetic nervous systemTachycardia, hyperglycemiaTachycardia, hyperglycemia

Ftorothane Ftorothane ((halothanehalothane))Power of narcosis action of ftorothan is higher than of Power of narcosis action of ftorothan is higher than of ether, it has a large width of narcotic action, doesn’t ether, it has a large width of narcotic action, doesn’t irritate mucous membranes of breath tractsirritate mucous membranes of breath tracts, , doesn’t cause doesn’t cause laryngeal and bronchial spasm, speed of development of laryngeal and bronchial spasm, speed of development of narcosisnarcosis – 3-5 – 3-5 min., after narcosis depression is not min., after narcosis depression is not expressedexpressed

Side effects and complicationsSide effects and complications

hypotension and cardiac arresthypotension and cardiac arrest,, sensitizationsensitization ( (increased sensitivityincreased sensitivity) ) of myocardium of myocardium

towards catecholaminestowards catecholamines acute damage of liveracute damage of liver – – halothane hepatitishalothane hepatitis,, teratogenic actionteratogenic action

Nitrogenous oxideNitrogenous oxideSmall power and width of narcosis actionSmall power and width of narcosis action,, stage of excitation stage of excitation

is presentis present, , quick entry and exit from narcosisquick entry and exit from narcosis (1-2 (1-2 minmin))

Administration Administration as an as an analgesicanalgesic:: pregnancypregnancy,, teeth extractionteeth extraction,, bandaging in case of burnsbandaging in case of burns, , cleaning and revisions of woundscleaning and revisions of wounds,, iscemic heart attacks and iscemic heart attacks and myocardium infarctionmyocardium infarction,, colicscolics,, traumastraumas,, acute pancreatitisacute pancreatitis,, pain relief in post-operative periodpain relief in post-operative period

Induction SpeedInduction Speed

Anesthetic of the Future: Anesthetic of the Future: XenonXenon

•Rare gas extracted from airRare gas extracted from air

•Very expensive to produceVery expensive to produce

•Close to ideal anestheticClose to ideal anesthetic

•Low blood and tissue solubilityLow blood and tissue solubility

(rapid induction/recovery)(rapid induction/recovery)

•PotentPotent

•Not metabolizedNot metabolized

•NonflammableNonflammable

•Minimal side effectsMinimal side effects

Drugs for Drugs for noninhalative noninhalative

narcosisnarcosis

ThiopentalThiopental--sodiumsodiumAfter administration of the drug narcosis develops in After administration of the drug narcosis develops in 1-2 1-2 min.min., , awakening awakening occurs inoccurs in 20-30 20-30 minmin..

Administration Administration introduction narcosisintroduction narcosis,, basis narcosisbasis narcosis,, mononarcosis in case of short-lasting mononarcosis in case of short-lasting

operative interventions operative interventions ((dentistry, gynecologydentistry, gynecology,, traumatologytraumatology),),

anti-seizure druganti-seizure drug..

Side effectsSide effectscoughcough, , laryngeal and bronchial spasmlaryngeal and bronchial spasm

In case of rapid introductionIn case of rapid introduction – – depression of centers of medulla depression of centers of medulla oblongataoblongata

. . In case of contact of the drug with skin, it’s separation may occur, In case of contact of the drug with skin, it’s separation may occur, contact with nervous trunk or near it – irreversible paralysis, contact contact with nervous trunk or near it – irreversible paralysis, contact with an artery – thrombosis with the following gangrene of the with an artery – thrombosis with the following gangrene of the extremityextremity

Propanidid Propanidid ((sombrevinsombrevin))Narcosis develops afterNarcosis develops after 30-40 30-40 sec from the beginning of intravenous sec from the beginning of intravenous

introduction of the drugintroduction of the drug (“ (“on the edge of the needle”on the edge of the needle”). ). Stage of Stage of surgical narcosis lasts forsurgical narcosis lasts for 3-4 3-4 minmin

AdministrationAdministration for mononarcosis during short operative interventions in surgery, for mononarcosis during short operative interventions in surgery, dentistry, gynecology, urologydentistry, gynecology, urology,, painful diagnostic procedurespainful diagnostic procedures,, sometimes sometimes – – for introduction into narcosisfor introduction into narcosis

Side effects and complicationsSide effects and complications

Frequent breathing (tachypnoe) with the following stopping of Frequent breathing (tachypnoe) with the following stopping of breathingbreathing ( (apnoeapnoe),),phlebitis and thrombosis in the place of introductionphlebitis and thrombosis in the place of introductionanaphylactic reactionsanaphylactic reactions

Sodium oxybutyrateSodium oxybutyrate in case of intravenous introduction narcosis develops afterin case of intravenous introduction narcosis develops after 15-40 15-40 minmin. . id id administered orally sleep comes afteradministered orally sleep comes after 30-60 30-60 minmin. . duration of narcosis isduration of narcosis is 1,5-3 1,5-3 hourshours. . It manifestsIt manifests antihypoxia propertiesantihypoxia properties

Administration Administration mononarcosis – to perform long-lasting surgeries but with small traumatic mononarcosis – to perform long-lasting surgeries but with small traumatic

effecteffect premedicationpremedication,, introduction and basis narcosisintroduction and basis narcosis.. drug of choice for narcosis in case of intoxications, sepsisdrug of choice for narcosis in case of intoxications, sepsis,,

disturbance of functions of parenchymatous organsdisturbance of functions of parenchymatous organs,, analgesia during child-deliveryanalgesia during child-delivery. . to decrease psycho-motor excitation, seizures,to decrease psycho-motor excitation, seizures, insomniainsomnia

Side effectsSide effectsmotor excitationmotor excitationseizure twitching of extremities and tongueseizure twitching of extremities and tonguevomitingvomiting hypopotassiumemiahypopotassiumemia..

Ketamine hydrochlorideKetamine hydrochloride ( (ketalar, kalipsolketalar, kalipsol))

During intravenous introduction of the drug narcosis develops afterDuring intravenous introduction of the drug narcosis develops after 15- 15-3030secsec, , lasts forlasts for 8-10 8-10 minmin, , during intramuscular introduction – after during intramuscular introduction – after 2-3 2-3 minmin, , lasts forlasts for 20-30 20-30 minmin

Administration Administration introduction and basis narcosisintroduction and basis narcosis mononarcosis during surgeries which don’t need muscular relaxationmononarcosis during surgeries which don’t need muscular relaxation as a part of combined narcosisas a part of combined narcosis

Side effectsSide effects during coming out of narcosis – unpleasant dreamsduring coming out of narcosis – unpleasant dreams,, deliriumdelirium, , hallucinationhallucination,, seizures,seizures, nausea, vomiting,nausea, vomiting, increasing of blood pressureincreasing of blood pressure,, increasing of frequency and power of heart contractionsincreasing of frequency and power of heart contractions The drug is able to raise intracranial pressureThe drug is able to raise intracranial pressure,, oxygen consumption by brain and intraoccular pressureoxygen consumption by brain and intraoccular pressure

PROPOFOLPROPOFOL ( (DIPRIVANDIPRIVAN))drug with ultra-short actiondrug with ultra-short action

Narcosis develops afterNarcosis develops after 30-40 30-40 sec after intravenous introductionsec after intravenous introduction, , lasts forlasts for 3-5 3-5 minmin

Administration Administration Mononarcosis Mononarcosis

Polycomponent narcosisPolycomponent narcosis

Artificial ventilation of lungsArtificial ventilation of lungs

Positive Positive momentsmoments:: can’t be accumulated, doesn’t have after-can’t be accumulated, doesn’t have after-narcosis depressionnarcosis depression, , possesses anti-vomiting actionpossesses anti-vomiting action

Negative Negative momentsmoments:: doesn’t have analgesic actiondoesn’t have analgesic action

((it is often combined with fentanil, ketamineit is often combined with fentanil, ketamine),),

possible hypotension, short apnoepossible hypotension, short apnoe

Ethomidate Ethomidate ((hipnomidatehipnomidate))drug of ultra-short actiondrug of ultra-short action

During introduction into vein effect develops after 1 min and During introduction into vein effect develops after 1 min and lasts for lasts for 3-5 3-5 minmin

AdministrationAdministrationIntroduction narcosisIntroduction narcosisMononarcosis during short-lasting surgeriesMononarcosis during short-lasting surgeriesPerforming of diagnostic manipulationsPerforming of diagnostic manipulations

DisadvantagesDisadvantages: : doesn’t have analgesic activitydoesn’t have analgesic activity, , promotes vomiting, in case of long lasting promotes vomiting, in case of long lasting introduction depending on dose it depresses introduction depending on dose it depresses synthesis of hormones of adrenal cortexsynthesis of hormones of adrenal cortex

MononarcosisMononarcosis((simplesimple,, single-component single-component))

Polynarcosis Polynarcosis ((multi-multi-componentcomponent, , combinedcombined))

Induction narcosisInduction narcosis most frequently is achieved by most frequently is achieved by

intravenous introduction of intravenous introduction of noninhalative narcosis drugs which noninhalative narcosis drugs which

don’t cause excitation stagedon’t cause excitation stage::

ketamineketamine, , thiopental-sodium, thiopental-sodium, propofol (diprivan), propofol (diprivan),

ethomidate (hypnomidate)ethomidate (hypnomidate)

Basis - narcosisBasis - narcosis– – element of combined analgesiaelement of combined analgesia (most often it is an (most often it is an intravenous narcosisintravenous narcosis, , which acts during all the which acts during all the surgerysurgery))

Following drugs are usedFollowing drugs are used::

Sodium oxybutyrateSodium oxybutyrate

Tiopental-sodiumTiopental-sodium

KetamineKetamine

Potentiated narcosisPotentiated narcosis– – is a kind of general analgesia,during which for potentiation is a kind of general analgesia,during which for potentiation of action of main narcosis substance drugs which don’t have of action of main narcosis substance drugs which don’t have

narcosis activity but narcosis activity but depress CNS depress CNS are used are used ::

Neuroleptics Neuroleptics Tranquilizers Tranquilizers

Opioid analgesicsOpioid analgesicsAntihistamine drugsAntihistamine drugs

Scopolamine Scopolamine Myorelaxants Myorelaxants

NeuroleptanalgesiaNeuroleptanalgesia

– – method of general analgesia when narcolepticmethod of general analgesia when narcoleptic ((droperidoldroperidol) ) and narcotic analgesic (and narcotic analgesic (fentanylfentanyl)) are are

combinedcombined. . Combined drugCombined drug - - talamonaltalamonal

Advantages of neuroleptanalgesiaAdvantages of neuroleptanalgesia inconsiderable toxicityinconsiderable toxicity large therapeutical width,large therapeutical width, deep analgesiadeep analgesia,, anti-shock actionanti-shock action,, considerable anti-vomiting effectconsiderable anti-vomiting effect,, stability of hemodynamicsstability of hemodynamics,, quick developing of narcosisquick developing of narcosis,, quick coming out of narcosisquick coming out of narcosis

Ataralgesia Ataralgesia Combined administration of narcotic analgesic and Combined administration of narcotic analgesic and

tranquilizertranquilizer

((diazepam or midasolamdiazepam or midasolam))

AdvantagesAdvantagesTranquilizing actionTranquilizing action ( (until full turning off until full turning off

consciousness under the influence of midasolamconsciousness under the influence of midasolam),), anterograde amnesiaanterograde amnesia ( (the patient doesn’t remember the patient doesn’t remember

events which happened after introduction of the events which happened after introduction of the drugdrug),),

relaxation of the musclesrelaxation of the muscles,, anti-seizure effectanti-seizure effect,,

minimal influence on blood circulationminimal influence on blood circulation