Transcript Phychiatric Drugs. Central Nervous System

CNS Stimulants
1. Analeptics
2. Anorexiants
3. Antidepressants
4. Serotonin agonists
CNS Stimulants: Adverse effects
• CVS: Palpitation, tachycardia,
hypertension, angina, dyshythmia
• CNS: Nervousness, restlessness, anxiety
• Endocrine: Hypoglycemia, hyperglycemia
• GIT: Nausea, vomiting,diarrhea
Analeptic
• Used to stimulate respiration when natural
reflex is lost
• H-cholinomimetic (reflex analeptic)
• Central analeptic (Aminophyllin,
theophylline,Caffeine, Doxapram)
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
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.
Metabolizing Of Caffeine
• Caffeine is completely absorbed by the stomach and small
intestine within 45 minutes of ingestion. After ingestion it
is distributed throughout all tissues of the body and is
eliminated by first-order kinetics. The half-life of caffeine
varies widely among individuals according to such factors
as age, liver function, pregnancy, some concurrent
medications, and the level of enzymes in the liver needed
for caffeine metabolism. In healthy adults, caffeine's halflife is approximately 3-4 hours. In women taking oral
contraceptives this is increased to 5-10 hours, and in
pregnant women the half-life is roughly 9-11 hours.
Caffeine can accumulate in individuals with severe liver
disease when its half-life can increase to 96 hours.
Caffeine
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AP
Hate rate
Respiratory stimulation
Adjunctive effect
Doxapram
• over dosage of CNS depressant
• COPD (chronic obstructive pulmonary
disease
• Respiratory depression in postoperative
recovery period
Doxapram: Contraindication
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Newborn
Epilepsy
Hypertension
Stroke
Amphetamines
• Produce mood elevation or euphoria,
increase mental alertness and capacity for
work, decrease fatigue and drowsiness,
prolong wakefulness.
Amphetamines usage
• Narcolepsy
• ADHD (attention-deficit/hyperactivity
disorder
Amphetamines
• Tolerance
• Psychological dependence
• High abuse potential (under Control
Substance Act
Methylxanthines
• COPD (chronic obstructive pulmonary
disease
• Respiratory depression in postoperative
recovery period
Anorexants
• Central acting (Benzphetamine,
diethylpropion, Sibutramine)
• Metabolism acting (orlistat)
Antidepressants
• Used to treat depression
• Depression, common feelings
– Pessimism
– Worry
– Intense sadness
– Loss of concentration
– Slowing of mental processes
– Problems with eating and sleeping
Serotonin agonist (Sumatriptan)
• Treatment of migraine
Antidepressants
Common Symptoms of Depression
– Loss of interest in
usual activities
– Low self-esteem
– Self-pity
– Significant weight loss
or gain
– Insomnia or
hypersomnia
– Extreme restlessness
– Loss of energy
– Feelings of
worthlessness
– Diminished ability to
think
– Feelings of guilt
– Recurrent thoughts of
death
– Suicide attempts
Antidepressants
Depression
• Women are affected more often than men
• When men are affected, it is usually later
in life
• Levels of neurotransmitters in the brain
may be a causative factor
Mood Disorders
• Mania
• Bipolar Disorder
• Unipolar Disorder
Mood Disorders
• Mania
Mood of extreme excitement, excessive elation,
hyperactivity, agitation, and increased
psychomotor activity
• Bipolar Disorder
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar Disorder
Mood swings alternate between major
depression and mania
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar Disorder
• Unipolar Disorder
Major depression with no previous occurrence
of mania
Treatment for Depression
Electroconvulsive Therapy
• Introduction of brief, but convulsive
electrical stimulation through the brain
• Can induce seizures
• Effective for major and delusional
depression
Antidepressants
• Selective Serotonin Reuptake
Inhibitors (SSRIs)
• Cyclic Antidepressants
• Monoamine Oxidase Inhibitors
(MAOIs)
Antidepressants
Selective Serotonin Reuptake
Inhibitors (SSRIs)
– Block the reuptake of serotonin, with
little effect on norepinephrine
– Fewer side effects than older meds
Treatments
Cyclic Antidepressants
– Two Types
• Tricyclic antidepressants (TCAs)
• Tetracyclic antidepressants
– Prevent reuptake of norepinephrine
and/or serotonin
– Agents in this class differ in adverse
effects, cost, and response
Treatments
Monoamine Oxidase Inhibitors
(MAOIs)
Allows for buildup of norepinephrine at the
synapse
Drug List
SSRIs for Depression
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citalopram (Celexa)
escitalopram (Lexapro)
fluoxetine (Prozac, Sarafem)
fluvoxamine
paroxetine (Paxil)
sertraline (Zoloft)
venlafaxine (Effexor)
Dispensing Issues
Warning!
Look-Alike Drugs
– Prozac and Proscar (urinary drug)
– Zoloft and Zocor (high cholesterol)
– Celexa and Cerebyx (seizures) and
Celebrex (arthritis)
SSRI
Dispensing Issues
Warning!
• Do not discontinue abruptly
• Alcohol consumption should be avoided
while taking these medications
fluoxetine (Prozac)
• Indicated for major depression and
obsessive-compulsive disorder (OCD)
• Anorexia is a possible adverse effect
• Take in the morning to avoid insomnia
paroxetine (Paxil)
• Indicated for depression, obsessivecompulsive disorder, and panic disorder
venlafaxine (Effexor)
• Blocks reuptake of serotonin and
norepinephrine
• Indicated for depression
• May cause increase in blood pressure and
blurred vision
sertraline (Zoloft)
• Indicated for depression and obsessivecompulsive disorder
• Primary side effect is nausea
• May also cause drowsiness
citalopram (Celexa)
• Indicated for depression and obsessivecompulsive disorder
• Minimal drug interactions
escitalopram (Lexapro)
• Similar to Celexa
• More potent with fewer side effects
Drug List
Cyclic
Antidepressants
Tricyclic
• amitriptyline (Elavil)
• clomipramine (Anafranil)
• desipramine (Norpramin)
• doxepin (Sinequan)
• imipramine (Tofranil)
Drug List
Cyclic
Antidepressants
Tricyclic
• nortriptyline (Aventyl, Pamelor)
• protriptyline (Vivactil)
• trimipramine (Surmontil)
Tetracyclic
• maprotiline
Tricyclic Antidepressants
Dispensing Issues
Warning!
• Improvements are usually seen in
10 to 21 days
• Can be cardiotoxic in high doses
• May cause postural hypotension
Tricyclic Antidepressants
Dispensing Issues
Warning!
Do not discontinue abruptly.
Cyclic Antidepressants Side Effects
• Sedation is
common, but
tolerance usually
occurs
• Have many
anticholinergic
effects
Discussion
Why would cyclic
antidepressants be prescribed
for bed wetting in children?
Discussion
Why would TCAs be prescribed for bed
wetting in children?
Answer
They may be prescribed
because of their anticholinergic
side effects.
Drug List
MAOIs
• phenelzine (Nardil)
• selegiline (Eldepryl)
• tranylcypromine (Parnate)
MAOI
Dispensing Issues
Warning!
Be cautious of many interactions with
foods such as aged cheeses,
concentrated yeast extracts, pickled
fish, sauerkraut, broad bean pods,
chocolate, and alcohol.
MAOI
Dispensing Issues
Warning!
If changing to another class of
antidepressant, patient must have a
two-week “wash out” period before
starting the new medication.
Drug List
Other
Antidepressants
• bupropion (Wellbutrin, Zyban)
• mirtazapine (Remeron)
• trazodone (Desyrel)
trazodone (Desyrel)
• Prevents reuptake of serotonin and
norepinephrine
• Has a better side effect profile than TCAs
• Caution: possible interaction with Ginkgo
bupropion (Wellbutrin, Zyban)
• Dopamine-uptake inhibitor
• Does not cause sedation, blood pressure
changes, or ECG changes
• Do not discontinue abruptly
• Approved in the aid of smoking cessation
Other Antidepressant
Dispensing Issues
Warning!
• Wellbutrin SR = BID dosing
• Wellbutrin XL = QD dosing
Bipolar Disorders
Signs or Symptoms
– Decreased need for sleep
– Elevated or irritable mood
– Excessive involvement in pleasurable
activities with a big potential for painful
consequences
– Grandiose ideas
– Pressure to keep talking
– Racing thoughts
Discussion
What is the drug of choice for
treating bipolar disorders?
Discussion
What is the drug of choice for treating
bipolar disorders?
Answer
Lithium
Discussion
What is the two-fold objective of
drug therapy for bipolar
disorder?
Discussion
What is the two-fold objective of drug
therapy for bipolar disorder?
Answer
Treat acute episodes
Prevent subsequent attacks
Drug List
Drugs to Treat Bipolar
Disorders
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carbamazepine (Epitol, Tegretol)
divalproex (Depakote)
lithium (Eskalith, Lithobid)
olanzapine-fluoxetine (Symbyax)
valproic acid (Depakene)
PSYCHOTROPIC DRUGS
PSYCHOTROPIC DRUGS
Drugs with depressive type of action
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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: aminasine,
triftiazine, etaperasine, tioridazine
• Derivatives of tioxanten: chlorprotixen
• Derivatives of butyrophenon:
galoperidol, droperidol
• Derivatives of piperasinedibenzodiazepine: clozapine
• Derivatives of indole: reserpin, sulpyrid
(eglonil)
NEUROPLEPTICS
“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
Aminasine (chlorpromasine)
• 1951 – aminasine was introduced into
clinical practice
• It brought considerable changes into
situations of psychiatric clinics
• Before appearance of aminasine for
treatment of psychologically sick patients
insulin or electric shock were widely used, in
some cases - lobotomy
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
with condition of consciousness
Administration of antipsychotic
action of neuroleptics
Treatment of psychosis
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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
Other properties and indications
for administration of neuroleptics
• Drugs with psychosedative action – for potentiation of
action of soporifics, 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 – aminasine, droperidol) – in case of hypertensive
crisis, lungs 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
• Aminasine has a considerable irritable action
syndrome of parkinsonism
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
• 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
Sybazon
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) sybazon is introduced intravenously
(intramuscularly) – 2-4 ml of 0,5 % solution
repeatedly (maximal 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
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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
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Sleepiness, reeling walk, retarded reactions
tranquilizers should not be administered in ambulatories to people
whose professions are connected with quick reactions
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Paradox reaction of excitation, insomnia
• Dizziness, decreasing of libido,
disturbances of menstrual cycle
• Uncontrolled urination, defecation, ataxia,
dysartria
• Acute poisoning in case of overdosing
FLUMAZENIL (ANEXAT)
ANTAGONIST OF TRANQUILIZERS
Combination of tranquilizers
with alcohol-containing
drinks is absolutely
contraindicated
(pathological alcohol intoxication)
LITHIUM DRUGS
LITHIUM CARBONATE
INDICATIONS FOR ADMINISTRATION
OF LITHIUM DRUGS
• Prophylaxis and treatment of endogen
(affective) psychosis: maniac-depressive,
schizo-affective, organic affective
• Prophylaxis and treatment of affective
disturbances in patients with epilepsy,
chronic alcoholism, in psychopaths
Method of lithium drugs
administration
• It is administered orally
• Treatment concentration of lithium in
blood – 0,6-0,8 mmol/l (not more than
1,5-1,6 mmol/l)
• The effect develops after few days – 5-6
months
• Small width of therapeutic action
(treatment with lithium drugs needs the
same attentiveness from the doctor as
treatment with insulin)
Acute poisoning with lithium drugs
It develops if the concentration is over 1,5-2 mmol/l
Development of constant nausea and tremor during
treatment with lithium means that the dose should be
decreased
SYMPTOMS OF POISONING
• Nausea, vomiting, diarrhea
• tremor, general muscular weakness, twitching muscles
• Noise in the ears, unclear vision, somnolence, dysartria
• Changes of handwriting: massive, bold
• Local neurological symptoms, meningism
• Oliguria
• Changes in ECG, arrhythmia, decreasing of BP
• Sopor, coma
• Death – from hypostatic pneumonia
Treatment of intoxication with lithium
drugs
• A lot of drinking, 10% solution of sodium chloride
(till 300 ml/day), 5% solution of sodium
hydrocarbonate (till 300 ml / day) intravenously
• Mannit, urea (saluretics are contraindicated!)
• Pyracetam, vinpocetin
• Prophylaxis of pneumonia – antibiotics
• Control of water-electrolyte balance, acid-base
balance
• Symptomatic therapy, for example, in case of
seizures - sybazon
• Haemodialysis if necessary
Prophylaxis of intoxication with
lithium drugs
• Salt in day ration should not be limited
• A lot of drinking
• Do not indicate saluretics, sweatstimulating drugs
• Heavy physical work or other situations,
accompanied by considerable sweating
should be avoided
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
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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
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
Desirable Components of
Anesthesia
1.
2.
3.
4.
5.
6.
7.
Immobility in response to noxious stimulus
Amnesia
Analgesia
Unconsciousness
Muscle relaxation
Loss of autonomic reflexes
Anxiolysis
CLASSIFICATION OF GENERAL
ANESTHETICS
Inhalational agents
primarily used for maintenance
•Volatile agents
Isoflurane
Sevoflurane
Desflurane
Halothane (Ftorothane)
Enflurane
•Anesthetic gases
Nitrous Oxide - currently used
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)
A Working Hypothesis
• Anesthetics enhance inhibitory
postsynaptic channel activity
(GABAA and glycine receptors)
• Anesthetics inhibit excitatory
synaptic channel activity (nicotinic
acetylcholine and glutamate
receptors)
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
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MACBAR: blunt autonomic response
MACintubation: response to intubation
Stages of narcosis
І. Stage of analgesia
Loss of pain feelings along with normal or
dimmed consciousness
Duration
from the beginning of inhalation of
narcosis substance and till the moment of
loss of patient’s consciousness
Sometimes during this stage small
surgical interventions are performed
(opening of abscesses, teeth extraction,
taking of the stitches etc.)
ІІ. Stage of excitation (no desirable!!!
dangerous)
Duration
from the moment of loss of patient’s consciousness
till the stage of surgical narcosis
Complications
language and motor excitement,
increasing of secretor activity of salivary and bronchial
glands,
vomiting,
variation of arterial pressure,
changes of breathing frequency
Heavy complications
Laryngospasm, bronchospasm, respiratory arrest,
cardiac arrhythmias, cardiac arrest
ІІІ. Stage of surgical anesthesia
1st level
Skeletal muscles aren’t relaxed, conjunctive and pharyngeal reflexes
disappear (it is possible to perform intubations)
2nd level
Reaction of frequent breathing as a respond cut on the skin disappear
(deep analgesia),
laryngeal reflexes disappear (it is possible to perform endotracheal
intubation);
good miorelaxation
3rd level
Decreasing of blood pressure,
Full relaxation of muscles,
step by step intercostal muscles get turned off,
Type of breathing changes into abdominal;
Corneal and pupil reflexes disappear
4th level
muscular tone is low,
full paralysis of intercostal muscles;
decreasing of blood pressure;
dilated pupil which don’t react on light
IV. Agony stage (occurs in a case of
overdosing of drugs for narcosis)
Characteristics
decreasing of breathing and vaso-motor
centers of medulla oblongata
Typical manifestations
full paralysis of breathing muscles,
respiratory arrest, collapse; cardiac arrest
Surgical interventions are
performed on 1st and 2nd
levels, approximately till half of
3rd level of third stage of
narcosis
Drugs for inhalative
narcosis
Ether for narcosis
Narcosis develops after 10-20 min, stage of excitation
- 10-20 min, strongly expressed after-narcosis
depression, high width of narcotic action (broad
therapeutic window)
Side effects and complications
bright stage of excitation
Increasing of tone of n. vagi
Increasing of secretion of salivary, bronchial glands, coughing;
laryngospasm, bronschospasm, vomiting with the following
aspiration of the masses bradycardia, stop of heart beat
Increasing of tone of sympathetic nervous system
Tachycardia, hyperglycemia
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
Ethomidate (hipnomidate)
drug of ultra-short action
During introduction into vein effect develops after 1 min and
lasts for 3-5 min
Administration
• Introduction narcosis
• Mononarcosis during short-lasting surgeries
• Performing of diagnostic manipulations
Disadvantages: doesn’t have analgesic activity,
promotes vomiting, in case of long lasting
introduction depending on dose it depresses
synthesis of hormones of adrenal cortex
Mononarcosis
(simple, single-component)
Polynarcosis (multicomponent, combined)
Induction narcosis
most frequently is achieved by
intravenous introduction of
noninhalative narcosis drugs which
don’t cause excitation stage:
ketamine, thiopental-sodium,
propofol (diprivan),
ethomidate (hypnomidate)
Basis - narcosis
– element of combined analgesia (most often it is an
intravenous narcosis, which acts during all the
surgery)
Following drugs are used:
Sodium oxybutyrate
Tiopental-sodium
Ketamine
Potentiated narcosis
– is a kind of general analgesia,during which for potentiation
of action of main narcosis substance drugs which don’t have
narcosis activity but depress CNS are used :
Neuroleptics
Tranquilizers
Opioid analgesics
Antihistamine drugs
Scopolamine
Myorelaxants
Neuroleptanalgesia
– method of general analgesia when narcoleptic
(droperidol) and narcotic analgesic (fentanyl) are
combined. Combined drug - talamonal
Advantages of neuroleptanalgesia
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inconsiderable toxicity
large therapeutical width,
deep analgesia,
anti-shock action,
considerable anti-vomiting effect,
stability of hemodynamics,
quick developing of narcosis,
quick coming out of narcosis
Ataralgesia
Combined administration of narcotic analgesic and
tranquilizer
(diazepam or midasolam)
Advantages
Tranquilizing action (until full turning off
consciousness under the influence of midasolam),
anterograde amnesia (the patient doesn’t remember
events which happened after introduction of the
drug),
relaxation of the muscles,
anti-seizure effect,
minimal influence on blood circulation