Psychiatric Drugs. Central Nervous
System Stimulants
Analeptic
 Used to stimulate respiration when natural reflex is lost
 H-cholinomimetic (reflex analeptic)
 Central analeptic (Aminophyllin, theophylline,Caffeine,
Doxapram)
Analeptics (Bemegridum, Camphora,
Cordiaminum)
Camphora
CNS Stimulants: Adverse effects
 CVS: Palpitation, tachycardia, hypertension, angina,
dyshythmia
 CNS: Nervousness, restlessness, anxiety
 Endocrine: Hypoglycemia, hyperglycemia
 GIT: Nausea, vomiting,diarrhea
Usage of psychostimulating
influence 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
vascular system
cardiac-
Vessels
1.
2.
Stimulation of vasomotor center –
contraction of vessels, increasing of AP
Peripheral myotropic spasmolytic action
– dilation of vessels, decreasing of AP
Heart
1.
2.
Central action (increasing of n. vagus
tone) – bradycardia
Peripheral action (direct influence on
heart) – tachycardia, possible
extrasystolia
Influence of caffeine on cardiovascular system
 Contraction of brain vessels
 Dilation of kidney vessels, increasing of diuresis
 Dilation of coronary vessels
In case of depression of centers of brain
stem (medulla oblongata) caffeine
shows stimulating properties, increases
blood pressure, stimulates breathing –
analeptic 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
Caffeine
Uses of Caffeine
 Caffeine 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.
Caffeine
 AP
 Hate rate
 Respiratory stimulation
 Adjunctive effect
SIDE EFFECTS OF CAFFEINE
 If administered regularly –
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psychological addiction –
theism, which is accompanied by
development of abstinent syndrome
(retardness, fatigue, somnolence,
depression)
Tolerance
Teratogenic action (innate
abnormalities)
Increasing of frequency of IHD,
essential hypertension
Acute attacks of ulcer disease
(it increases gastric secretion)
Acute 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 disorder
 Narcolepsy
TOXICITY
 Tolerance
 Psychological dependence
 High abuse potential (under Control Substance Act
ADHD –
attention deficit hyperactivity disorder –
more frequently in children
 Cured by potent stimulators (ritalin, adderal
and others)
 They all can provoke addiction !!!
Methylxanthines
 COPD (chronic obstructive pulmonary disease
 Respiratory depression in postoperative recovery period
Anorexants
 Central acting (Benzphetamine, diethylpropion, Sibutramine)
 Metabolism acting (orlistat)
Function of adrenergic synapse in physiological
conditions
ANTIDEPRESSANTS
Drugs which inhibit neuronal uptake of
monoamines
1.
2.
Nonselective action – tricyclic compounds (block uptake
of noradrenaline and serotonine): imisin, amitriptilin
Selective action: а) heterocyclic compounds (block
neuronal uptake of noradrenaline): amoxapin, maprotilin
(ludiomil); б) selective blockers of neuronal uptake of
serotonin: fluoxetin (prozak, framex), sertralin (zoloft),
paroxetin (rexetin)
Inhibitors of monoaminoxidase (IMAO)
1.
2.
nonselective (block МАО-А and МАО-В): а) irreversible
action – nialamid; b) reversible action – transamin
Selective ІМАО (block МАО-А): moklobemid, pirasidol
Blockers of neuronal reuptake 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 neuronal reuptake of serotonin
fluoxetin, sertralin, paroxetin
Mechanism of action
Increasing of active concentration of serotonin
in synaptic cleft on a level of postsynaptic
5-НТ2 serotonin receptors of cerebral
structures
Blockers of neuronal reuptake of serotonin
fluoxetin, sertralin, paroxetin
Mechanism of action of IMAO
Usage of antidepressants
Schizophrenia, MDS
Atherosclerosis of brain
Reactive depressions
Parkinsonism
Organic diseases of CNS
Oncology patients
General somatic diseases
Psychotropic action of
antidepressants
Drugs with psychosedative action:
Аmitriptilin, maprotilin, asafen, fluvoxamin
2. Drugs with psychostimulative action:
Imisin, nialamid, fluoxetin
3. Drugs with regulative influence
Pirasidol
1.
Principles 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 antidepressants
 М-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 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 antidepressants
 Acute attacks of epilepsy
 Cardiotoxic action (sudden death), three- cyclic antidepressants
increase arrhythmogenic activity of drugs for general anesthesia,
antihistamines etc.
 Combination of three-cyclic antidepressants with 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
antidepressants to another
 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
IMAO
It is necessary to exclude such products which contain
DOPA and thiramine (which is formed from casein during the process
of transforming under the influence of bacteria)
aged cheese, kefir
Marinated herring
Smoked meat, fish
Red vine, beer, yeast
Beans
oranges, tangerines, lemons, grape, bananas,
chocolate, caviar (red and black)…
…
Any BAA are also dangerous
In case of treatment with IMAO new products should be
introduced into ration very carefully
Neurometabolic
cerebroprotectors
 Derivatives of pyrrolidone – pyracetam (nootropil)
 Derivatives of GABA – aminalon, sodium
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oxybutyrate
Neuropeptides – melatonin, sinacten-depot
Cerebrovascular drugs – sermion (nicergolin),
cavinton (vinpocetin), stugeron (cinnarisin),
pentoxyphylline (trental, agapurine), xantynole
nicotinate
Derivatives of piridoxine – piritinol (encephabol)
Antioxidants – mexidol, tocopherole acetate
Other – cerebrolysine, actovegin, solkoseryl, plant
preparations
Properties of nootropic drugs
 Improvement of brain blood circulation, promotion of
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collaterals development
Psychostimulating effect, antiasthenic action
Sedative, antidepressive action
Antiepileptic, antiparkinsonic action
Nootropic action
Mnemotropic action
Vasovegetative action
Antihypoxic action
Administration of nootropic drugs
 Atherosclerosis of brain, vascular parkinsonism,
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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 (nootropil)
Cerebrolysin
Cinnarizin (stugeron)
Adaptogens
Drugs of
Ginseng, Schizandrum, Rodiola,
Eleutherococcus, Leusea, Echinacea
Apilac, propolis, mumie,
heparin, dibazol
GINSENG
RODIOLA
Eleutherococcus
Schizandrum
Echinacea purpurea Maxima
ADAPTOGENS
Increase general resistance of the organism towards
unfavorable factors
Stimulating action
Antistress action
Anabolic action
Side effects of adaptogens
Increasing of AP
disturbance of sleep if administered
in evening time, overwhelming
excitation, psychical dependence