Transcript Anesthetic drugs. Ethanol. Hypnotics

"Anesthetic drugs“
Ethanol. Hypnotics.
Synaptic education at various levels of the central nervous system and various
morphological and functional organization to vary in sensitivity to anesthetic drugs.
For example, activating the synapses of the reticular formation of the brain stem in
particular are highly sensitive to anesthetic drugs, whereas synapses centers of the
medulla oblongata most resistant to it. Differences in sensitivity-telnosti synapses of
different levels of the central nervous system explains the presence of certain stages in
the action of narcosis.
Allocate the following stages:
I - stage analgesia ';
II - the stage of initiation;
III- stage of surgical anesthesia:
Level 1 (III1) -poverhnostny anesthesia,
2nd level (III2) -easy anesthesia,
3rd level (III3) - deep anesthesia,
Level 4 (III4) - ultra-deep anesthesia;
IV- agonal stage.
This sequence of stages of anesthesia is valid only as a general scheme, since
the excitation step in the application of a number of drugs can be practically
absent, the severity varies stage analgesia, and so on. D .. A more detailed
description of the individual stages of anesthesia is given with respect to the
ether.
Tools for anesthesia belong to different classes of chemical compounds.
Identify common patterns between their chemical structure and drug activity
failed. Established a private individual depending series of compounds
(hydrocarbons, barbiturates).
From the point of view of practical application tools for anesthesia sub-divided
into the following groups.
I. Means for inhalation anesthesia
Liquid volatiles
Ether for anesthesia
Halothane
gaseous substances
Nitrogen oxide
cyclopropane
II. Means for not and not inhalation anesthesia
Propanidid
Sodium hydroxybutyrate
Thiopental sodium
Ketamine
By means of anesthesia impose certain requirements. Thus,
anesthesia using them should advance quickly as possible and
without the stage of initiation. There must be sufficient depth
of anesthesia, been ensured and provides optimal conditions
for the operation. The important point yaalyaetsya good
handling depth of anesthesia during the use of narcosis. Side
effects should be absent or minimal. It is desirable that the
output from anesthesia was rapid, with no aftereffects. This
facilitates after anesthetic period.
The essential characteristic of anesthetic drugs is drug latitude - between
the concentration range in which the drug causes anesthesia, and its
minimum toxic concentration at which inhibition occurs vital centers of
the medulla oblongata. About Drug latitude means for inhalation
anesthesia is judged by their concentration in the inhaled air, and means
for non-inhalation anesthesia - by the initial dose. Naturally, the more drug
latitude, the safety of the drug.
It is desirable that the use of narcosis was technically quite simple. One of
the requirements is the safety of drugs in relation to fire: they do not need
to burn and explode. Currently, it deserves special attention, since there is
a large number of operating various equipment, the slightest fault which
can cause ignition of flammable anesthetic drugs. When introducing into
medical practice new drugs should take into account their cost. Synthesis
of the drug must be affordable for its release on an industrial scale.
Means for inhalation anesthesia
For inhalation anesthesia used volatile liquids (ether anesthesia, Halothane et al.),
Easily passing into the vapor state, as well as blowing agents (nitrous oxide,
cyclopropane). Typically use special anesthetic machines, allowing to create in WdaHai air necessary concentration of substances.
By inhalation means for inhalation anesthesia they received by diffusion from the lungs
into the blood. The absorption of the drug depends on its concentration in inhaled air
volume and respiratory rate, and permeability of the alveolar surface, solubility agents
for anesthesia and the rate of blood flow in the pulmonary circulation. All this
determines the rate of increase of the concentration of drug in the blood and tissues,
which determines the speed of development of anesthesia.
Most of the inhalational anesthetic agents in the body is distributed more or less
uniformly. Some of the differences are related to uneven circulation of organs and
tissues. These substances are allocated light, mostly unchanged. Elimination rate is
dependent on the same factors as absorption. Especially quickly allocated funds for
gaseous anesthesia.
LIQUID volatiles
This group includes ether anesthesia, Halothane.
Ether for anesthesia in chemical structure is diethyl ether. It has
potent drug activity, drug sufficient latitude, relatively low toxicity.
Ether anesthesia is fairly easy to manage, but not as good as the
anesthesia caused ftorotanom or cyclopropane.
Ester concentration in inhaled air, depending on the method and
sensitivity of the patient narkotizirovaniya usually varies from 2-4
to 10-12 vol.%.
When using ether anesthesia stage clearly expressed. Stage
analgesia characterized by the suppression of pain sensitivity. This
is due, apparently, to the oppression of interneuronal transfer of
excitation in afferent pathways and decreased functional activity of
neurons in the cerebral cortex. Consciousness is thus maintained,
but the orientation is broken. Typical amnesia
For ether anesthesia characterized by prolonged excitation stage
(10-20 min). This greatly complicates the administration of
anesthesia. Stage of excitation is due to increased activity of
subcortical structures (mainly the midbrain). This is due to
inhibition of the cerebral cortex and off subordinate mechanisms
controlling the state of the underlying centers. Consciousness is lost.
There is a motor and verbal stimulation. The pupils are dilated.
Breathing usually becomes more frequent. Marked tachycardia.
Blood pressure fluctuates. Spinal reflexes may increase. In
connection with the irritating ether may occur cough, hypersecretion
of bronchial and salivary glands, and in contact with the saliva of
ether into the stomach - vomiting. It is also possible reflex (with
upper respiratory tract) decrease in breathing and heart rate until the
apnea and cardiac arrest. These effects are cautioned atropine.
Under surgical anesthesia is further depression transmission as
interneurons in the brain and the spinal cord level. Consciousness is
turned off. Pain sensitivity is absent. Reflex activity is suppressed.
Autonomic reflexes are depressed at the same time not completely.
Pupils are narrowed. In stage III, heart rate slows (compared with stage
II), blood pressure stabilized, breathing becomes regular. With the
deepening of anesthesia heart rate changes, possible cardiac arrhythmias,
blood pressure may be reduced. Breathing gradually suppressed.
Celebrate good relaxation of skeletal muscles, which facilitates the
operation. Muscle relaxation is associated not only with the effect of
ether on the central mechanisms of regulation of muscle tone, but with
some dampening effect on its neuromuscular synapses. It should also be
borne in mind that the air strengthen and prolong the blocking effect on
neuromuscular transmission antidepolyarizuyuschih curariform funds.
In applying the activated ester central links sympathoadrenal system,
which results in the release of epinephrine from the adrenal glands.
Myocardial function and liver are generally not affected. Rarely jaundice
quickly passing. Renal function is inhibited. Can albuminuria. If acidosis
develops deep anesthesia (in blood ketone bodies accumulate).
Awakening from anesthesia with ether, the light which is released in an
unmodified form, occurs gradually (about 30 min).
However, to fully restore the functions of the brain takes a few hours.
Long-term remains analgesia. In poslenarkoznom period is often a
vomiting. Irritability broadcast on airway mucosa may be the cause of
postoperative bronchopneumonia.
If overdose occurs agonal stage, due to a sharp inhibition of the
respiratory and vasomotor centers of the medulla oblongata.
Volume and respiratory rate decreases progressively and develops
asphyxia. Heart failure occurs, the blood pressure drops. Pupils in
the agonal stage dramatically expanded. If you do not take
appropriate measures, the patient dies from respiratory paralysis,
to the center and the subsequent cardiac arrest.
An important role in determining the stage of anesthesia plays
electroencephalography (EEG). When using ether in stages I and
II anesthesia observed desynchronization biopotential. Frequent
low-amplitude oscillations are recorded. Under surgical
anesthesia EEG synchronization occurs: there are high-amplitude
oscillations whose frequency decreases with depth of anesthesia.
In the agonal phase wave amplitude decreases sharply until the
complete disappearance of the bioelectric activity.
Similar EEG changes characteristic of most anesthetic drugs. However,
keep in mind that for each drug are typical features of their dynamics of
EEG in different stages of anesthesia.
Relatively common in anesthesiology received Halothane (halothane,
fluotan). Halothane relates to a fluorine-containing aliphatic compounds.
Characterized by high drug activity (3-4 times greater than air).
Anesthesia is rapid (3-5 min) with a very short step excitation.
Introduction of anesthesia ftorotanom performed at 4 vol.% (In the inhaled
air). To maintain sufficient anesthesia ingalya¬tsii 0.5-2.5 vol.%
Halothane. Anesthesia ftorotanom manageable. Upon termination of
inhalation drug the patient wakes up after 5-10 minutes. Drug
considerable latitude halothane (similar to that of ether).
Anesthesia proceeds with satisfactory muscle-relaxing tion. Halothane
mioparalitichesky enhances the effect of anti-depolarizing curariform
funds, but to a lesser extent than the air.
For action halothane is aetiology associated with high vagal tone (prevented
by administering atropine). Halothane reduces blood pressure. This occurs as
a result of the oppression of the vasomotor center and sympathetic ganglia
(Halothane markedly enhances the action ganglioblokiruyuschih substances),
as well as direct myotropic effect on blood vessels. In the application of
halothane possible heart aritmii.Obuslovleny they direct influence of
halothane on the myocardium, including its sensitization to adrenaline. In this
regard, the background ftorotanovogo anesthesia administration of
epinephrine, norepinephrine, and ephedrine is contraindicated. If there is a
need for pressor substances, it should be administered α-adrenoceptor
agonists (phenylephrine). Halothane inhibits the secretory activity of the
salivary, bronchial, gastric glands. Halothane liver function, according to
available data, violates no more frequently than other means of anesthesia.
Irritant properties has not. Acidosis causes. Nausea and vomiting in
poslenarkoznom period are rare.
In the body part of halothane significant (approximately 20%)
Biotransformation.
Enflurane (ETRAN) - hydrofluorocarbon. A volatile liquid. Has a high drug
activity. Anesthesia quickly comes and goes quickly after cessation of
inhalation of enflurane. Typical expression miorelak-sation. During the
anesthesia used about 3 vol.% Enflurane. Of adverse effects may be marked
respiratory depression and a depressing effect on the myocardium.
Furthermore, enflurane sensitizes the myocardium to act catecholamines,
which could be the cause of
cardiac arrhythmias. Adverse effect on the liver and kidneys were observed. In
the body are metabolized to a lesser extent (5-10%).
By hydrofluorocarbon is also methoxyflurane (pentran). Has a high drug and
analgesic activity. Anesthesia occurs at muscle relaxation. Characteristically
slow development of anesthesia (within 10-15 min). Output from anesthetics
also occurs gradually (15-30 min). After anesthesia, analgesia persists for a
long time. However, methoxyflurane often causes renal dysfunction (there is a
condition such as diabetes insipidus with polyuria and dehydration in the body
retained urea, creatinine). Often kidney disease is persistent and pronounced.
In connection with the use of methoxyflurane nephrotoxicity dramatically
reduced, and in some countries discontinued.
Halothane, enflurane and methoxyflurane unlike ether fireproof safe.
gaseous substances
Ketamine (ketalar, Kalipsol) -poroshkoobraznoe substance pri¬menyaetsya as
solutions for intravenous and intramuscular administration. Ketamine is a
general anesthetic and a light hypnotic effect of the loss of consciousness (state
type neuroleptanalgesia). Surgical anesthesia under the influence of ketamine
does not develop. A similar effect of ketamine is sometimes termed
"dissociative anesthesia". It is understood that such agents as ketamine, inhibit
formation of some central nervous system, and do not affect the other, ie. E.
There is a certain effect in their dissociation. When intravenously effect after
30-60 seconds and lasts 5-10 minutes and intramuscular administration - after
2-6 minutes and lasts for 15-30 minutes. Ketamine is inactivated in the liver.
Skeletal muscle on the background of ketamine did not relax; may experience
involuntary movements of the extremities. Pharyngeal, laryngeal, kaschlevoy
reflexes saved. Blood pressure increases, the heart rate increases.
Hypersalivation may occur. Slightly increased intraocular pressure.
In the postoperative period are not uncommon (especially in adults) are bright,
but often unpleasant dreams, psychomotor reactions, hallucinations.
Applied ketamine for induction of anesthesia, as well as during transient
painful manipulations (e.g., in the treatment of burn surface, etc.. P.).
Combined use of anesthetic drugs
In modern anesthesia is rarely limited to the introduction of a means of anesthesia.
Typically combine two or three drugs. Combine means for inhalation anesthesia with
inhalation or neingalyatsionnyh formulation.
The expediency of such combinations is that it eliminates the stage of excitement and
made a quick introduction to anesthesia. For example, anesthesia often start with
intravenous tiopen-tal-sodium propanidid providing very rapid development stage of
excitation without anesthesia. Especially shown combination with means for
neingalyatsionnyh anesthesia drugs with severe stage of excitation (eg, ether). For the
same reason the air is combined with nitrous oxide and ftorotanom.
The advantage of the combined anesthetic is also that the concentration (dose) of the
blend components is less than using a single agent for narcosis, therefore possible to
reduce the toxicity and to reduce the incidence of side effects. So, in order to reduce
cardiotropic action cyclopropane it can be used in conjunction with nitrous oxide and
other drugs.
One of the most commonly used at present combinations of narcosis is the following:
a barbiturate or other fast-acting drug for non-inhalation anesthetic Halothane + +
nitrous oxide.
Regardless of the nature of the combinations is important that the main stages of the
operation carried out on the background of well-managed products (gaseous means of
anesthesia, as well as Halothane, ether).
 Ethyl alcohol is a typical substance narcotic type of action.
He has a general depressant effect on the central nervous
system. In addition, ethyl alcohol has a strong antiseptic
properties.
For medical practices ethyl alcohol is of limited interest. It
is used mainly as an antiseptic. Much greater attention is
drawn to the ethyl alcohol with ¬ social dimension, as in
connection with the use of alcoholic beverages, he is often
the cause of acute and chronic poisoning.
Ingestion ethyl alcohol is rapidly absorbed mainly in the
small intestine and about 20% - in the stomach.
 The absorption rate depends largely on the nature of the
contents of the gastrointestinal tract motility and intensity.
Particularly rapid resorptive effect of ethyl alcohol comes
in the fasting state. Fats and carbohydrates significantly
delay its absorption.
In the body, 90% of the injected ethyl alcohol is
metabolized to SOG and water. The oxidation is
accompanied by liberation of ethyl ¬ tion considerable
amount of energy (7.1 kcal / g). This occurs in the liver by
approximately 10 ml / h Prolonged use of ethyl alcohol can
be observed induction of liver enzymes in which the rate of
inactivation of ethyl alcohol increased.
 Unchanged ethyl alcohol stands lungs, kidneys and
sweat glands ¬ mi.
Resorptive effect of ethyl alcohol is directed mainly to
the central nervous system. It exerts a dampening
effect, which increases with the concentration of
ethyl alcohol in the blood and tissues of the brain.
This is manifested in three major steps: 1) excitation
step 2) under anesthesia 3) atonal step.
 Stage of excitation is the result of the oppression of brake
mechanisms of the brain. It is usually well marked and longlasting. There is euphoria, increased mood, he becomes overly
sociable, talkative. Psychomotor reaction at this violated
dramatically affected human behavior, self-control, adequate
assessment of the environment, efficiency is reduced.
With an increase in the blood concentration of ethyl alcohol
come analgesia, drowsiness, then breaks out. Inhibited spinal
reflexes. The stage of anesthesia, which, however, neprodolzhi ¬
tional and soon becomes atonal stage. A small drug ¬ cal latitude
and expressed excitement stage not allow the use of ethyl
alcohol as a means of anesthesia.
 One of the manifestations of the central action of ethyl alcohol its effect on thermoregulation, manifested by increased heat
loss (due to vasodilatation of the skin, which is a consequence of
the inhibition of the vasomotor center). As a result, the cold
ethyl alcohol contributes to hypothermia, and does not preclude
it, as is often said. The subjective feeling of warmth after
receiving ethyl alcohol associated with the expansion of the
cutaneous vessels, is not accompanied by a general increase in
body temperature. In this regard, in order to create a feeling of
warmth, acceptance of ethyl alcohol can be justified only after
getting in from the cold into a warm room, when the danger of
frost is excluded.
 The diuretic action of ethyl alcohol also has a central origin
(reduced production of antidiuretic hormone of the
posterior pituitary).
Ethyl alcohol has a pronounced effect on the digestive
system. Thus, it enhances the secretory activity of the
salivary and gastric glands ¬. This is the result of his
Llyaetsya psychogenic, reflex, as well as direct action on
the gland. Increased secretion of gastric glands under
direct ethyl alcohol on the mucosa is obviously due to the
release of humoral substances (gastrin, histamine). It
should be borne in mind that ethyl alcohol increases the
secretion of acid hloristovo ¬ stout.
 Pepsin activity at low concentrations (10%) ethyl alcohol is
not changed, and decreases with increasing concentration.
Since about 20% concentration, ethyl alcohol not only
inhibits the secretion of hydrochloric acid, but also food ¬
provisional activity of gastric juice, which is particularly
pronounced when receiving alcoholic beverages with 40%
and above. In response to stimuli ¬ tal effect on the
mucous membrane of high concentrations of ethyl alcohol
gastric glands produce large amounts of mucus. It coats
the surface of the stomach, and also reduces the
concentration of ethyl alcohol.
 Changes and motility of the stomach. Ethyl alcohol in
sufficient ¬ sufficiently high concentrations cause spasm of
the pylorus and reduced gastric motility.
On bowel function ethyl alcohol has little effect. Obviously,
this is because it is diluted in the stomach and enters the
intestine gradually.
In medical practice resorptive effect of ethyl alcohol is
rarely used. Sometimes it is used as a means
protivoshokovoe (given its analgesic effect), rarely - as a
hypnotic or sedative substances. In some cases, shows the
assignment of ethyl alcohol (in low concentrations)
depleted patients
 In this case refers to its energy value. However, it
should be noted that ethyl alcohol is not a nutrient
substance ¬ tion. It does not provide a plastics
material for forming fabrics are not deposited and has
significant toxicity.
With prolonged use of ethyl alcohol develop ¬ tion
got used to it and drug abuse (physical and mental).
 Reception alcohol can lead to acute poisoning, the degree
of which depends on the concentration of ethyl alcohol in
the blood. Intoxication occurs at a concentration of
approximately 1-2 g / l (100 - 200 mg%). At 3-4 g / l (300-400
mg%) developed severe Institute ¬ intoxication. Lethal
concentration is from 5 to 8 g / l (500 - 800 mg%).
In the treatment of alcoholic coma should first establish a
hell ¬ kvatnoe breath. Held WC oral purified upper airways.
To reduce the secretion of salivary and bronchial glands
atropine.
 Assign oxygen. If necessary, carried ¬ stvlyayut mechanical
ventilation. It is also useful introduction analeptikov
(korazol, kordiamin, caffeine, etc.). When hemodynamic
disorders, symptomatic therapy. It should also wash out
the stomach. In addition, a correction of the acid-base
equilibrium (intravenous sodium bicarbonate). In severe
condition of the patient hemodialysis.
In case of severe nausea possible use of antiemetics
(metoclopramide, etc.). In connection with the violation of
thermoregulation such patients should be warm
 Chronic poisoning with ethyl alcohol (alcoholism) is
characterized by a variety of symptoms. Particularly
affected the higher nervous activity and knowledge.
Reduced mental performance, attention, and
memory. There may be mental disorders
(Delirium tremens, Korsakoff's psychosis). Affected
and peripheral innervation (polyneuritis can occur).
 Serious disorders and marked by internal organ ¬ new. For example,
accompanied by chronic gastritis, alcoholism, cirrhosis, fatty heart
and kidneys.
If alcoholism is a gradual mental and physical degradation of the
individual.
Alcoholism treatment is carried out in hospitals. The main task is to
stop accepting ethyl alcohol and in the development of a negative
attitude to it. Cancellation of ethyl alcohol must be gradual, as
abrupt discontinuation of its use can cause severe phenomenon of
deprivation, including exacerbation of mental disorders (eg, stroke,
delirium tremens). One of the drugs used in the treatment of
alcoholism is the teturam (Antabuse, disulfiram).
 Assign teturam in conjunction with the acquisition of
small amounts of ethyl alcohol. Teturama mechanism
of action is that it delays the oxidation of ethyl
alcohol to acetaldehyde level (presumably, it inhibits
the aldehyde). The accumulation of the latter ¬ him in
the body causes intoxication that followed. Extremely
painful sensations. There is a feeling of fear, pain in
the heart, headache, hypotension, diaphoresis,
nausea, and vomiting
 The course of treatment for patients Teturamom produces a
negative reflection on ethyl alcohol. Teturamom treatment
should be carried out with care, under the supervision of a
physician. The patient should be well oriented in the fact that
even a slight overdose of alcohol ethyl ¬ Vågå on the
background of teturama can lead to death. Teturam not
recommended for persons older than 50 years, as well as
cardiovascular disease, liver disease, kidney disease and
metabolism.
There is a long-acting drug teturama, called esperal (radoter).
Tablets esperal implanted in the sub ¬ cutaneous tissue.
 Sometimes to generate negative conditioned reflexes
use of centrally acting emetic - apomorphine (also
melt ¬ A combination with the reception of ethyl
alcohol).
Furthermore, in the treatment of alcoholism are
widely used various psychotropic drugs. The positive
effect in the treatment of alcoholism ¬ SRI, especially
in the development of polyneuritis, give thiamine.
 Drug treatment of alcoholism should always be
combined with psychotherapy.
Existing drugs can reduce the consumption of ethyl
alcohol ¬ Vågå only in some patients and only for a
few months. Unfortu ¬ leniyu enough effective drugs
that suppress the craving for ethyl alcohol, no.
 Hypnotics
By hypnotic include means to facilitate the
development and provision ¬ zations sleep. They
promote falling asleep and provide the necessary
amount of sleep ¬ directly.
By the nature of the influence of the central nervous
system and the lack of selective classic hypnotics
(barbiturates, Alif ¬ cal compounds) are substances
such as drugs.
 By the nature of the influence of the central nervous
system and the lack of selective classic hypnotics
(barbiturates, Alif ¬ cal compounds) are substances such as
drugs. Hypnotics
By hypnotic include means to facilitate the development
and provision ¬ zations sleep. They promote falling asleep
and provide the necessary amount of sleep ¬ directly.
By the nature of the influence of the central nervous
system and the lack of selective classic hypnotics
(barbiturates, Alif ¬ cal compounds) are substances such as
drugs.
 Hypnotics are classified based on the principle of action and chemical structure.
I. Hypnotics with narcotic
1. Heterocyclic compounds
Barbituric acid derivatives (barbiturates)
Phenobarbital
Barbital barbamyl
Barbital sodium-sodium etaminal
2. Aliphatic compounds
Chloral hydrate bromisoval
P. Hypnotics group of tranquilizers
Benzodiazepines
Nitrazepam Sibazon
(Diazepam)