Transcript Neuroleptics

PSYCHOTROPIC DRUGS
PSYCHOTROPIC DRUGS
Drugs with depressive type of action
1.
2.
3.
4.
Neuroleptics (antipsychotics)
Tranquilizers (anxiolytics)
Sedative drugs
Normotymics (tymoleptics, tymoanaleptics)
Drug with stimulative action
1.
2.
3.
4.
Antidepressants
Psychomotor stimulants
Nootropic drugs
Drugs which increase general tone (adaptogens)
Psychotomimetics (psychodysleptics)
1.
2.
LSD
Cannabis sativa L.
NEUROLEPTICS
Derivatives of phenotiazine: aminazine,
triftiazine, etaperazine, tioridazine
Derivatives of tioxanten: chlorprotixen
Derivatives of butyrophenon:
haloperidol, droperidol
Derivatives of piperasinedibenzodiazepine: 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
Phenothiazine derivatives
Thioxanten derivateves
Butyrophenon derivatives
piperasine-dibenzodiazepine derivatives
(Clozapin, Clozapine, FazaClo, Leponex, Zaponex,
Clopin Eco.)
Mechanism of action of
neuroleptics
Influence on dopamine (D2),
noradrenergic, serotoninergic, GABAergic, cholinergic receptors
Properties of neuroleptics
Antipsychotic action - they eliminate
productive symptoms of psychosis
(delirium and hallucinations), affective
disorders
They eliminate psychomotor excitation
consciousness is present
1 Lung Cancer, 2 Criminality, 3 Stroke, 4 Breast Cancer, 5 Same
Sex Attraction, 6 Leukemia, 7 Malformation, 8 Alzheimer’s, 9
Ulcerative Colitis, 10 Rheumatoid Arthritis, 11 Alcoholism,
12 Schizophrenia, 13 Depression, 14 Suicide attempt,
15 Diabetes type I, 16 Divorce, 17 Crohn’s disease, 18 Asthma,
19 Hypertension, 20 Co twin is best friend, 21 Diabetes type II,
22 Autism, 23 Opposite Sex Attraction, 24 Phenylketonuria
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
Neuroleptics with psychosedative action
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
Drugs which stimulate psychical
activity
Other properties and indications
for administration of neuroleptics
Drugs with psychosedative action – for potentiation of
action of 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 of body 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
syndrome of parkinsonism
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
TRANQUILIZERS
Properties of tranquilizers
Anxiolytic properties – eliminate feeling
of anxiety, restlessness, fear,
aggressiveness, irritability, cause peace,
careness, decreasing of moving activity
Hypnotic (somnolent) action
Myorelaxing action (of central genesis)
Antiseizure action
Duration of action of tranquilizers
Drugs of long lasting action:
diazepam, phenazepam, chlozepid
Drugs of medium action duration:
lorazepam, alprazolam
Drugs of short action 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
Hypnotic action – they cause sleep, which
is very close to physiological one
according to its parameters
Nitrazepam
Phenazepam
Diazepam
Chlozepid
Depression of CNS – for atharalgesia
Sibazon
Midazolam
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
Seizures
(tetanus)
drug of a first choice
- Sibazon
SIDE EFFECT OF TRANQUILIZERS
Psychological and physical addiction
Prophylaxis:
1.
Duration of treatment course should not be more than 2 months
2.
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
FLUMAZENIL (ANEXAT)
ANTAGONIST OF TRANQUILIZERS
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
Valeriana
PASSIFLORA
Leonurus L.
dog nettle
ADMINISTRATION OF
SEDATIVE 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
Hypnotic agents
DRUGS FOR GENERAL
ANESTHESIA
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.”
1846
TG 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
......
Molecular
(lipids &
receptors)
Cellular (synapses)
Effects of General Anesthesia
Low Dose Effects
High Dose Effects
•Amnesia
•Deep sedation
•Euphoria
•Muscle relaxation
•Analgesia
•Diminished motor responses
•Hypnosis
•Diminished autonomic
responses
•Excitation
•Hyperreflexia
•Myocardial protection from
ischemia
•Cardiovascular/respiratory
depression
•Hypothermia
Measures of Anesthetic Potency
•
MAC: minimum alveolar concentration
• MAC is the concentration of
anesthetic that produces
immobility in 50% of patients
exposed to a noxious stimulus.
•
MACawake: MAC at which response to
commands are lost
• amnesia, loss of awareness
•
•
MACBAR: blunt autonomic response
MACintubation: response to intubation
Surgical interventions are
performed on 1st and 2nd
levels, approximately till half of
3rd level of third stage of
narcosis
Ftorothane (halothane)
Power of narcosis action of ftorothan is higher than of
ether, it has a large width of narcotic action, doesn’t
irritate mucous membranes of breath tracts, doesn’t cause
laryngeal and bronchial spasm, speed of development of
narcosis – 3-5 min., after narcosis depression is not
expressed
Side effects and complications
hypotension and cardiac arrest,
sensitization (increased sensitivity) of myocardium
towards catecholamines
acute damage of liver – halothane hepatitis,
teratogenic action
Nitrogenous oxide
Small power and width of narcosis action, stage of excitation
is present, quick entry and exit from narcosis (1-2 min)
Administration as an analgesic:
pregnancy,
teeth extraction,
bandaging in case of burns,
cleaning and revisions of wounds,
iscemic heart attacks and
myocardium infarction,
colics,
traumas,
acute pancreatitis,
pain relief in post-operative period
Induction Speed
Anesthetic of the Future:
Xenon
•Rare gas extracted from air
•Very expensive to produce
•Close to ideal anesthetic
•Low blood and tissue solubility
(rapid induction/recovery)
•Potent
•Not metabolized
•Nonflammable
•Minimal side effects
Drugs for
noninhalative
narcosis
Thiopental-sodium
After administration of the drug narcosis develops in 1-2 min., awakening
occurs in 20-30 min.
Administration
introduction narcosis,
basis narcosis,
mononarcosis in case of short-lasting
operative interventions (dentistry, gynecology,
traumatology),
anti-seizure drug.
Side effects
cough, laryngeal and bronchial spasm
In case of rapid introduction – depression of centers of medulla
oblongata
.
In case of contact of the drug with skin, it’s separation may occur,
contact with nervous trunk or near it – irreversible paralysis, contact
with an artery – thrombosis with the following gangrene of the
extremity
Propanidid (sombrevin)
Narcosis develops after 30-40 sec from the beginning of intravenous
introduction of the drug (“on the edge of the needle”). Stage of
surgical narcosis lasts for 3-4 min
Administration
for mononarcosis during short operative interventions in surgery,
dentistry, gynecology, urology,
painful diagnostic procedures,
sometimes – for introduction into narcosis
Side effects and complications
Frequent breathing (tachypnoe) with the following stopping of
breathing (apnoe),
phlebitis and thrombosis in the place of introduction
anaphylactic reactions
Sodium oxybutyrate
in case of intravenous introduction narcosis develops after 15-40 min. id
administered orally sleep comes after 30-60 min. duration of narcosis is 1,5-3
hours. It manifests antihypoxia properties
Administration
mononarcosis – to perform long-lasting surgeries but with small traumatic
effect
premedication,
introduction and basis narcosis.
drug of choice for narcosis in case of intoxications, sepsis,
disturbance of functions of parenchymatous organs,
analgesia during child-delivery.
to decrease psycho-motor excitation, seizures,
insomnia
Side effects
motor excitation
seizure twitching of extremities and tongue
vomiting
hypopotassiumemia.
Ketamine hydrochloride (ketalar, kalipsol)
During intravenous introduction of the drug narcosis develops after 1530sec, lasts for 8-10 min, during intramuscular introduction – after 2-3
min, lasts for 20-30 min
Administration
introduction and basis narcosis
mononarcosis during surgeries which don’t need muscular relaxation
as a part of combined narcosis
Side effects
during coming out of narcosis – unpleasant dreams,
delirium,
hallucination,
seizures,
nausea, vomiting,
increasing of blood pressure,
increasing of frequency and power of heart contractions
The drug is able to raise intracranial pressure,
oxygen consumption by brain and intraoccular pressure
PROPOFOL (DIPRIVAN)
drug with ultra-short action
Narcosis develops after 30-40 sec after intravenous introduction,
lasts for 3-5 min
Administration
Mononarcosis
Polycomponent narcosis
Artificial ventilation of lungs
Positive moments: can’t be accumulated, doesn’t have afternarcosis depression, possesses anti-vomiting action
Negative moments: doesn’t have analgesic action
(it is often combined with fentanil, ketamine),
possible hypotension, short apnoe