CNS Stimulants 1.Analeptics 2.Anorexiants 3.Antidepressants 4.Serotonin agonists.
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Transcript of CNS Stimulants 1.Analeptics 2.Anorexiants 3.Antidepressants 4.Serotonin agonists.
CNS Stimulants
1. Analeptics2. Anorexiants
3. Antidepressants4. 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 half-life 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
• 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
• 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
• ManiaMood of extreme excitement, excessive elation, hyperactivity, agitation, and increased psychomotor activity
• Bipolar Disorder
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar DisorderMood swings alternate between major depression and mania
• Unipolar Disorder
Mood Disorders
• Mania
• Bipolar Disorder
• Unipolar DisorderMajor 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
SSRIs for Depression• citalopram (Celexa)
• escitalopram (Lexapro)
• fluoxetine (Prozac, Sarafem)
• fluvoxamine
• paroxetine (Paxil)
• sertraline (Zoloft)
• venlafaxine (Effexor)
Drug List
Dispensing Issues
Look-Alike Drugs
– Prozac and Proscar (urinary drug)
– Zoloft and Zocor (high cholesterol)
– Celexa and Cerebyx (seizures) and Celebrex (arthritis)
Warning!
SSRIDispensing Issues
• Do not discontinue abruptly
• Alcohol consumption should be avoided while taking these medications
Warning!
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, obsessive-compulsive 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 obsessive-compulsive disorder
• Primary side effect is nausea
• May also cause drowsiness
citalopram (Celexa)
• Indicated for depression and obsessive-compulsive disorder
• Minimal drug interactions
escitalopram (Lexapro)
• Similar to Celexa
• More potent with fewer side effects
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
Drug List
Tricyclic Antidepressants Dispensing Issues
• Improvements are usually seen in 10 to 21 days
• Can be cardiotoxic in high doses
• May cause postural hypotension
Warning!
Tricyclic AntidepressantsDispensing Issues
Do not discontinue abruptly.Warning!
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.
MAOIs
• phenelzine (Nardil)
• selegiline (Eldepryl)
• tranylcypromine (Parnate)
Drug List
MAOI Dispensing Issues
Be cautious of many interactions with foods such as aged cheeses, concentrated yeast extracts, pickled fish, sauerkraut, broad bean pods, chocolate, and alcohol.
Warning!
MAOI Dispensing Issues
If changing to another class of antidepressant, patient must have a two-week “wash out” period before starting the new medication.
Warning!
Other Antidepressants
• bupropion (Wellbutrin, Zyban)
• mirtazapine (Remeron)
• trazodone (Desyrel)
Drug List
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
• Wellbutrin SR = BID dosing
• Wellbutrin XL = QD dosing
Warning!
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
Drugs to Treat Bipolar Disorders
• carbamazepine (Epitol, Tegretol)
• divalproex (Depakote)
• lithium (Eskalith, Lithobid)
• olanzapine-fluoxetine (Symbyax)
• valproic acid (Depakene)
Drug List
PSYCHOTROPIC DRUGS
PSYCHOTROPIC DRUGSDrugs with depressive type of action
1. Neuroleptics (antipsychotics)2. Tranquilizers (anxiolytics)3. Sedative drugs4. Normotymics (tymoleptics, tymoanaleptics)
Drug with stimulative action1. Antidepressants 2. Psychomotor stimulants3. Nootropic drugs4. Drugs which increase general tone (adaptogens)
Psychotomimetics (psychodysleptics)1. LSD 2. Cannabis sativa L.
NEUROLEPTICS• Derivatives of phenotiazine: aminasine,
triftiazine, etaperasine, tioridazine
• Derivatives of tioxanten: chlorprotixen
• Derivatives of butyrophenon: galoperidol, droperidol
• Derivatives of piperasine-dibenzodiazepine: 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, GABA-
ergic, 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• Schizophrenia• Maniac-depressive psychosis• Alcohol psychosis• Reactive psychosis
In a case of psychomotor excitationof 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• 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,
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 drugsIt 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
decreasedSYMPTOMS 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, sweat-stimulating 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
• 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. Immobility in response to noxious stimulus
2. Amnesia
3. Analgesia
4. Unconsciousness
5. Muscle relaxation
6. Loss of autonomic reflexes
7. Anxiolysis
Inhalational agentsInhalational agentsprimarily used for maintenanceprimarily used for maintenance
•Volatile agentsVolatile agentsIsofluraneIsofluraneSevofluraneSevofluraneDesfluraneDesfluraneHalothaneHalothane ( (FtorothaneFtorothane)) EnfluraneEnflurane
•Anesthetic gasesAnesthetic gasesNitrous Oxide Nitrous Oxide - currently used- currently used
CLASSIFICATION OF GENERAL ANESTHETICS
Intravenous agentsIntravenous agentsprimarily used for inductionprimarily used for induction
•Barbiturates (Thiopental-Barbiturates (Thiopental-sodium)sodium)•Benzodiazepines (Benzodiazepines (Midasolam, Midasolam, diazepam)diazepam)•EtomidateEtomidate•KetamineKetamine•PropofolPropofol•PropanididPropanidid•Sodium oxybutyrateSodium oxybutyrate•PredionPredion
CLASSIFICATION OF GENERAL ANESTHETICS
General General anesthesia can be anesthesia can be caused by a caused by a remarkable remarkable number of number of structurally structurally diverse moleculesdiverse molecules
Unitary Hypothesis
Xe
Isoflurane
Halothane
......Cellular (synapses)Cellular (synapses)
MolecularMolecular(lipids & (lipids &
receptors)receptors)
Molecular Mechanism(s) of General Molecular Mechanism(s) of General AnesthesiaAnesthesia
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 EffectsLow Dose Effects
•AmnesiaAmnesia
•EuphoriaEuphoria
•AnalgesiaAnalgesia
•HypnosisHypnosis
•ExcitationExcitation
•HyperreflexiaHyperreflexia
High Dose EffectsHigh Dose Effects
•Deep sedationDeep sedation
•Muscle relaxationMuscle relaxation
•Diminished motor responsesDiminished motor responses
•Diminished autonomic Diminished autonomic responsesresponses
•Myocardial protection from Myocardial protection from ischemiaischemia
•Cardiovascular/respiratory Cardiovascular/respiratory depressiondepression
•HypothermiaHypothermia
• MAC: MAC: mminimum inimum aalveolar lveolar cconcentration oncentration
• MAC is the concentration of MAC is the concentration of anesthetic that produces anesthetic that produces immobility in 50% of patients immobility in 50% of patients exposed to a noxious exposed to a noxious stimulus.stimulus.
• MACMACawakeawake: MAC at which response : MAC at which response to commands are lost to commands are lost
• amnesia, loss of awarenessamnesia, loss of awareness
• MACMACBARBAR: : bblunt lunt aautonomic utonomic rresponseesponse• MACMACintubationintubation: response to intubation: response to intubation
Measures of Anesthetic Potency
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 anesthesia1st level
Skeletal muscles aren’t relaxed, conjunctive and pharyngeal reflexes disappear (it is possible to perform intubations)
2nd levelReaction 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 levelDecreasing 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 levelmuscular 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 manifestationsfull 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 narcosisNarcosis 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 complicationsbright stage of excitation
Increasing of tone of n. vagiIncreasing 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 systemTachycardia, 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 oxideSmall power and width of narcosis action, stage of excitation
is present, quick entry and exit from narcosis (1-2 min)
Administration Administration as an as an analgesicanalgesic:: pregnancypregnancy,, teeth extractionteeth extraction,, bandaging in case of burnsbandaging in case of burns, , cleaning and revisions of woundscleaning and revisions of wounds,, iscemic heart attacks and iscemic heart attacks and myocardium infarctionmyocardium infarction,, colicscolics,, traumastraumas,, acute pancreatitisacute pancreatitis,, pain relief in post-operative periodpain relief in post-operative period
Induction Speed
Anesthetic of the Future: Xenon
•Rare gas extracted from airRare gas extracted from air
•Very expensive to produceVery expensive to produce
•Close to ideal anestheticClose to ideal anesthetic
•Low blood and tissue solubilityLow blood and tissue solubility
(rapid induction/recovery)(rapid induction/recovery)
•PotentPotent
•Not metabolizedNot metabolized
•NonflammableNonflammable
•Minimal side effectsMinimal side effects
Drugs for noninhalative
narcosis
Thiopental-sodiumAfter 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 effectscough, 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 introductionanaphylactic 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 effectsmotor excitationseizure twitching of extremities and tonguevomiting hypopotassiumemia.
Ketamine hydrochloride (ketalar, kalipsol)
During intravenous introduction of the drug narcosis develops after 15-30sec, 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 after-narcosis 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 manipulationsDisadvantages: 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 (multi-component, 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 analgesicsAntihistamine drugs
Scopolamine Myorelaxants
Neuroleptanalgesia
– method of general analgesia when narcoleptic (droperidol) and narcotic analgesic (fentanyl) are
combined. Combined drug - talamonal
Advantages of neuroleptanalgesia• 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)
AdvantagesTranquilizing 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