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Psychiatric Drugs. Central Nervous System Stimulants
AnalepticUsed to stimulate respiration when natural
reflex is lostH-cholinomimetic (reflex analeptic)Central analeptic (Aminophyllin,
theophylline,Caffeine, Doxapram)
AnalepticsAnaleptics ( (BemegridumBemegridum,, Camphora Camphora, , CordiaminumCordiaminum))
CamphoraCamphora
CNS Stimulants: Adverse effectsCVS: Palpitation, tachycardia, hypertension,
angina, dyshythmiaCNS: Nervousness, restlessness, anxietyEndocrine: Hypoglycemia, hyperglycemiaGIT: Nausea, vomiting,diarrhea
Usage of Usage of psychostimulating psychostimulating influence of caffeineinfluence of caffeine
For stimulation of psychological processes, workability, to eliminate somnolence
Enuresis, narcolepsyIn case of poisoning with alcoholTo 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 vesselsDilation of kidney vessels, increasing of diuresisDilation of kidney vessels, increasing of diuresisDilation 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
Did You Know?Caffeine is a xanthine alkaloid compound that
acts as a stimulant in humans. Caffeine is sometimes called guaranine when found in guarana, mateine when found in mate, and theine when found in tea. It is found in the leaves and beans of the coffee plant, in tea, yerba mate, and guarana berries, and in small quantities in cocoa, the kola nut and the Yaupon Holly. Overall, caffeine is found in the beans, leaves, and fruit of over 60 plants, where it acts as a natural pesticide that paralyzes and kills certain insects feeding upon them.
Chemical Properties
Molar Mass = 194.19 g mol−1 Density: 1.2 g/cm³
Phase: Solid
Melting Point: 237 °C
Boiling Point: 178 °C
CaffeineCaffeine
Uses of CaffeineCaffeine is a central nervous system (CNS)
stimulant, having the effect of temporarily warding off drowsiness and restoring alertness. Beverages containing caffeine, such as coffee, tea, soft drinks and energy drinks enjoy great popularity: caffeine is the world's most widely consumed psychoactive substance. In North America, 90% of adults consume caffeine daily.
CaffeineAPHate rateRespiratory stimulationAdjunctive effect
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))
ToleranceToleranceTeratogenic action (innate Teratogenic action (innate
abnormalities)abnormalities) Increasing of frequency of IHD, Increasing of frequency of IHD,
essential hypertensionessential hypertensionAcute 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
Amphetamines Produce mood elevation or euphoria,
increase mental alertness and capacity for work, decrease fatigue and drowsiness, prolong wakefulness.
Amphetamines
USAGE:
ADHD (attention-deficit/hyperactivity disorderNarcolepsy
TOXICITY
TolerancePsychological dependenceHigh abuse potential (under Control Substance
Act
ADHD – ADHD – attention deficit hyperactivity disorder – attention deficit hyperactivity disorder – more frequently in childrenmore frequently in children
Cured by potent stimulators (ritalin, adderal Cured by potent stimulators (ritalin, adderal and others)and others)
They all can provoke addiction !!!They all can provoke addiction !!!
MethylxanthinesCOPD (chronic obstructive pulmonary
diseaseRespiratory depression in postoperative
recovery period
AnorexantsCentral acting (Benzphetamine,
diethylpropion, Sibutramine)Metabolism acting (orlistat)
Function of adrenergic synapse in physiological Function of adrenergic synapse in physiological conditionsconditions
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 of reuptake 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- 2НТ receptors
Compensatory decreasing of quantity and sensitivity of presynaptic 5- 1НТ 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 Combination of three-cyclic antidepressants with IMAO is absolutely antidepressants with IMAO is absolutely contraindicatedcontraindicated:: danger of development of hypertensive crisis, seizures, rapid excitation, tachycardia, cardiac arrhythmias, increasing of temperature
Rules of transferring from one Rules of transferring from one kind of antidepressants to kind of antidepressants to anotheranother
From three-cyclic to IMAO – break time– 2-3 days
From IMAO to three-cyclic – break time – not less than 2 weeks
Diet in case of administration of Diet in case of administration of IMAOIMAO
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
Neurometabolic Neurometabolic cerebroprotectorscerebroprotectors
Derivatives of pyrrolidoneDerivatives of pyrrolidone – – pyracetampyracetam ( (nootropilnootropil))Derivatives of GABA Derivatives of GABA – – aminalon, sodium aminalon, sodium
oxybutyrateoxybutyrateNeuropeptides Neuropeptides – – melatoninmelatonin, , sinacten-depotsinacten-depotCerebrovascular 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 acetateOther Other – – cerebrolysinecerebrolysine, , actovegin, solkoseryl, plant actovegin, solkoseryl, plant
preparationspreparations
Properties of nootropic Properties of nootropic drugsdrugs
Improvement of brain blood circulation, promotion of collaterals development
Psychostimulating effect, antiasthenic actionSedative, antidepressive actionAntiepileptic, antiparkinsonic actionNootropic actionMnemotropic actionVasovegetative actionAntihypoxic action
Administration of nootropic Administration of nootropic drugsdrugs
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))
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
Recommended