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PSYCHOTROPIC DRUGS. PSYCHOTROPIC DRUGS. Drugs with depressive type of action Neuroleptics ( antipsychotics ) Tranquilizers ( anxiolytics ) Sedative drugs Normotymics ( tymoleptics , tymoanaleptics ) Drug with stimulative action Antidepressants Psychomotor stimulants Nootropic drugs
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PSYCHOTROPIC DRUGS Drugs with depressivetype of action • Neuroleptics (antipsychotics) • Tranquilizers (anxiolytics) • Sedative drugs • Normotymics (tymoleptics, tymoanaleptics) Drug withstimulativeaction • Antidepressants • Psychomotor stimulants • Nootropic drugs • Drugs which increase general tone (adaptogens) Psychotomimetics(psychodysleptics) • LSD • Cannabis sativa L.
NEUROLEPTICS • Derivatives of phenotiazine:aminazine, triftiazine, etaperazine, tioridazine • Derivatives of tioxanten: chlorprotixen • Derivatives of butyrophenon: haloperidol, droperidol • Derivatives of piperasine-dibenzodiazepine: clozapine • Derivatives of indole: reserpin, sulpyrid (eglonil)
NEUROLEPTICS “Typical” – derivatives of phenotiazine, tioxanten, butyrophenon – they cause disorders of extrapyramidal system function –syndrome of parkinsonism “Atypical” – derivatives of indole, benzodiazepine – they cause those negative reactions very rarely
Aminazine (chlorpromazine) • 1951 – aminazine was introduced into clinical practice • It brought considerable changes into situations of psychiatric clinics • Before appearance of aminazine for treatment of psychologically sick patients insulin or electric shock were widely used, in some cases - lobotomy
piperasine-dibenzodiazepinederivatives(Clozapin, Clozapine, FazaClo, Leponex, Zaponex, Clopin Eco.)
Mechanism of action of neuroleptics Influence on dopamine (D2),noradrenergic, serotoninergic, GABA-ergic, cholinergicreceptors
Properties of neuroleptics • Antipsychotic action - they eliminate productive symptoms of psychosis (delirium and hallucinations), affective disorders • They eliminate psychomotor excitation • consciousness is present
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Administration of antipsychotic action of neuroleptics Treatment of psychosis • Schizophrenia • Maniac-depressive psychosis • Alcohol psychosis • Reactive psychosis In a case of psychomotor excitation of various etiology
Delirium tremens – alcohol psychosis
Influence of neuroleptics on psychical activity 1. Drugs with psychosedative action – they cause condition of psychomotor indifference (apathy, decreasing of moving activity, retarded emotions and wishes, disappearance of initiative) Aminazine, clozapine (leponex), chlorprotyxen, haloperidol, droperidol Peculiarities of usage: psychosis with manifestations of excitation Contraindications: psychosis with retardness, inertia, depression, stupor, apatho-abulic syndrome
Influence of neuroleptics on psychical activity 2. Drugs which stimulate psychical activity(increase mimics and liveliness, increase moving activity, improve the mood) Triftazin, ethaperazin, moditen, majeptil Peculiarities of usage: psychosis with psychomotor retardness, apatho-abulic conditions, stupor conditions Contraindications:affective disturbances, mania, psychomotor excitation
Other properties and indications for administration of neuroleptics • Drugs with psychosedative action – forpotentiation of actionof hypnotic drugs, opioid and nonopioid analgesics, drugs for general anesthesia, local anesthetics, for example, neuroleptanalgesia • Anti-emetic action (elimination of vomiting of central origin): brain tumors, radial and chemical therapy, intestinal impassability, intoxication with heart glycosides, apomorphine and other drugs • Decreasing ofbody temperature(only in the case of simultaneous hypothermia) • Decreasing of blood pressure(alpha-adrenoblocking properties – aminazine, droperidol) – in case of hypertensive crisis, lungs, brain edema
Side effects of neuroleptics • Extrapyramidal disorders:muscular hypertonus, general constraint, tremor of hands, tongue, mandible, head, seizure contractions of muscles, vegetative crisis For treatment – cyclodol(levodopa is contraindicated because it diminishes therapeutic effect of neuroleptics) • Orthostatic collapse • Complicated nose breathing, hypostatic, aspirate pneumonia • Dyspeptic disorders: anorexia, changes of taste • Abdominal pain • Constipation • Damage of the liver (cholestasis) • Granulocytopenia (especially clozapin) • Hyperglycemia, dysmenorrhea, galactorrhea, hyperthyrosis, gynecomastia, impotence • Aminazine has a considerable irritative action
Parkinsone syndrome treatment Cyclodolum Levodopa is contraindicated
TRANQUILIZERS • Agonists of benzodiazepine receptors: - derivatives of benzodiazepine – chlozepid, sybazon, phenazepam, gidazepam • Agonists of serotonine receptors: buspyrone • Drugs with other mechanisms of action: -derivatives of diphenilmethan: amisyl - derivatives of propanediole: meprotan
Properties of tranquilizers • Anxiolytic properties – eliminate feeling of anxiety, restlessness, fear, aggressiveness, irritability, cause peace, careness, decreasing of moving activity • Hypnotic (somnolent) action • Myorelaxingaction (of central genesis) • Antiseizureaction
Duration of action of tranquilizers • Drugs of long lastingaction: diazepam, phenazepam, chlozepid • Drugs of mediumaction duration: lorazepam, alprazolam • Drugs of shortaction duration: midazolam
“DAY” TRANQUILIZERS Gidazepam Mezapam (rudotel) Grandaxyn (tophizopam) Trioxazyn Buspyron
Administration of tranquilizers Anxiolytic action • Treatment of neurosis, accompanied by fear, anxiety, exertion, increased irritability, insomnia • In case of headache and heart pain of neurotic origin, so called organic neurosis • In case of abstinence in alcohol and drugs addicts • In case of diencephalons crisis (sybazon) Tranquilizers do not diminish productive symptoms of psychosis!
Usage of tranquilizers • Hypnoticaction – they cause sleep, which is very close to physiological one according to its parameters NitrazepamPhenazepam DiazepamChlozepid • Depression of CNS – foratharalgesia SibazonMidazolam
Administration of tranquilizers Anti-seizure and myorelaxing action (depression of CNS structures, braking polysynaptic spinal reflexes) sybazon, fenazepam • In a case of seizures of any etiology(epileptic status, tetanus, poisoning with seizure causing poisons)sibazon is introduced intravenously (intramuscularly) – 2-4 ml of 0,5 % solution repeatedly (maximum daily dose – 14 ml) • To eliminate muscle tension in a case of radiculitis, arthritis, myositis, bursitis
SIDE EFFECT OF TRANQUILIZERS • Psychological and physical addiction Prophylaxis: • Duration of treatment course should not be more than 2 months • Repeated course – not earlier than after 3 weeks break • Sleepiness, reeling walk, retarded reactions tranquilizers should not be administered in ambulatories to people whose professions are connected with quick reactions • Paradox reaction of excitation, insomnia • Dizziness, decreasing of libido, disturbances of menstrual cycle • Uncontrolled urination, defecation, ataxia, dysarthria • Acute poisoning in case of overdosing
Combination of tranquilizers with alcohol-containing drinks is absolutely contraindicated (pathological alcohol intoxication)
SEDATIVE DRUGS • Bromides • Drugs of plant origin: valerian, dog nettle, melissa, passiflora etc. They do not cause addiction, somnolence, myorelaxation, ataxia
ADMINISTRATION OFSEDATIVE DRUGS • Neurosis • Neurasthenia • Hysteria • Increased irritability • Insomnia • Primary stages of essential hypertension
Bromism • Cause – accumulation of bromide ions in organism in case of their prolonged administration as a result of material accumulation • Symptoms: rhinitis, cough, conjunctivitis, skin rash, general weakness, memory disorders • Treatment: sodium chloride (10-20 g / day), a lot of drinking (3-5 l / day), regular and frequent cleaning of skin and digestive tract
General anesthesia = Narcosis (from the Greek narkosis – numbness, rigidity) – Generalized reversible depression of the central nervous system such that perception of all senses is ablated, condition which is characterized by loss of consciousness, pain feelings, depression of reflexes and relaxation of skeletal muscles and which is obtained by administration of drugs for general anesthesia
“Gentlemen, this is no humbug.” 1846TG Morton: First public demonstration of ether administration for excision of neck mass
CLASSIFICATION OF GENERAL ANESTHETICS • Intravenous agents • primarily used for induction • Barbiturates (Thiopental-sodium) • Benzodiazepines (Midasolam, diazepam) • Etomidate • Ketamine • Propofol • Propanidid • Sodium oxybutyrate • Predion
Unitary Hypothesis General anesthesia can be caused by a remarkable number of structurally diverse molecules
Molecular Mechanism(s) of General Anesthesia Xe Isoflurane Halothane Cellular (synapses) ...... Molecular (lipids & receptors)
Effects of General Anesthesia • High Dose Effects • Deep sedation • Muscle relaxation • Diminished motor responses • Diminished autonomic responses • Myocardial protection from ischemia • Cardiovascular/respiratory depression • Hypothermia • Low Dose Effects • Amnesia • Euphoria • Analgesia • Hypnosis • Excitation • Hyperreflexia