Systematic (Jupak) Name: (R) -4- (1-hydroxy-2- (methyl-amino) ethyl) benzen-1,2-diol

USA: C (risk is not excluded)

Legality:

Australia: Released only on the recipe (S4)

United Kingdom: prescription only (POM)

USA: Released without a recipe

Dependency Development: Not addictive

Ways of administration of the drug: Intravenously, intramuscularly, endotracceal, in a conjunct bag, in the nasal cavity, in the eyes (in the form of droplets)

Metabolism: in adrenergic synapse (MAO and SOMT)

Half life: 2 minutes

Excretion Together with urine

Chemical formula C 9 H 13 NO 3

Epinephrine (also known as adrenaline or β, 3,4-trihydroxy-N-methyl-phenethylamine) is a hormone and part-time, neurotransmitter. Epinephrine and norepinephrine are two separate hormones that interact with each other and are distinguished by the adrenal brainstabs. Both hormones are also synthesized at the ends of the fibers of the sympathetic nerve, where they function as chemical mediators for which the nerve impulses come to the organs with the opening pharmacological properties Epinephrine, scientists, finally, figured out the work of vegetative nervous system and basic functions of the sympathetic nervous system. Epinephrine often effectively helps in critical situations when the life of the patient "hangs on the hairs", not to mention its nonspecific effect on adrenergic receptors (this property is extremely important in medicine). In everyday life, the word "adrenaline" is used to designate epinephrine, which reflects the increased activity of the sympathetic nervous system against the background of energy generation and excitation of catecholamines in response to stress. The effect of adrenaline is mainly reduced to accelerating the metabolism and armored organs, but without direct irritation of the sympathetic nervous system. I am expressed by the "chemical" language, epinephrine is a monoamine called "Catecholamine". Epinephrine is produced by separate neurons of the central nervous system and is synthesized inside chromaffine cells of adrenal brainstones (of two amino acids: phenylalanine and tyrosine).

Application in medicine

Adrenaline helps with: stopping the heart, anaphylaxis and strong bleeding. With the help of it, people have repeatedly removed bronchial spasms and increased blood sugar levels, although in modern society with these problems, the drugs of which are directed to beta-2 adrenergic receptors (for example, salbutamol, synthetic epinephrine derivative) are helped.

Heart failure

Adrenaline is used as a reanimating means when stopping the heart and to combat cardiac arrhythmias or with a decrease in the volume of the heart. The effect of epinephrine is directed to an increase in the peripheral resistance of the vessels (by α1 receptor-dependent narrowing of these vessels) and to increase the volume of the heart (by attaching to β1 - receptors). The slowdown in the peripheral blood circulation is necessary to increase the coronary and cerebral perfusion pressure and, as a result, the enhanced supply of cells with oxygen. Despite the fact that epinephrine increases blood pressure in the aorta, brain and carotid artery, it slows down the blood circulation inside the carotid artery and reduces carbon dioxide level at the end of each calm exhalation (etco2). It turns out, epinephrine enhances macro-circulation due to the kapillars, in which perfusion occurs. The concentration of carbon dioxide in the lungs with each calm exhale is a kind of marker, which is judged whether the resuscitation will be effective and the man normalizes the human circulation. With increasing macrocirculation pressure, blood circulation in the nerve endings does not always increase. ETCO2 level is a more accurate indicator of tissue perfusion than perfusion pressure markers. As it turned out, epinephrine does not contribute to the improvement of tissue perfusion and long-term survival; Moreover, it reduces the survival rate when the heart is stopped.

Anaphylaxis

Epinephrine / Adrenaline is a first-order preparation ( best tool) For the treatment of anaphylaxia. Allergies passing the course of immunotherapy, often before taking a substance causing allergies from them, intravenously pour adrenaline, thereby dulling the reaction immune system on the accepted allergen. For various emergency situations, there are its norms of administration of epinephrine (concentrations, doses and places of administration of the drug). Universal auto-injector (syringe) epinephrine accommodates 0.3 mg of epinephrine (0.3 ml, 1: 1000) and is used as an emergency medical care With severe (I type) reactions, including anaphylaxis, allergic reactions to insect bites, contrast medium, medication. One dose is designed for 30 (or a little more than) kg of weight, if necessary, a person is re-injected. In pediatrics, lower adrenaline doses are used, which cause narrowing vessels at the subcutaneous injection site, slowing the absorption of the drug. Pharmacokinetic epinephrine profile allows to enhance the inflow of plasma into the injection site (2 nanone / l); Such a concentration is achieved when using an epiphephrine inhaler and with intensive physical exertion, but it is too small to influence beta-1 adrenergic receptor or for (alpha) narrowing of vessels, although it is enough to activate beta-2 adrenergic receptor, due to which potassium concentration in The plasma decreases, and the level of glucose, on the contrary, increases (with a person against the background of brightness and bronchoprotection, the tremor fingers are intensified). Allergenic dose of epinephrine (0.1 ml / kg 1/1000 epinephrine at a maximum single dose of 0.3 ml subcutaneously or intramuscularly; the second method is preferable with weak perfusion) effectively fights skin reactions in response to subcutaneous injection Antigen. Blisters and rashes on the skin disappear under the action of beta-2 adrenergic receptors acting as mediators of this reaction. Edema disappear due to restriction of the promotion of the vessels in areas where post-capillary venules are connected to the endothelium (with irritation of receptors on the endothelium surface). With the re-administration of epinephrine, or when the dosage increases, the further narrowing of the capillaries is not excluded (due to the stimulation of alpha receptors) and, as a result, the removal of inflammatory edema. With intravenous, intraosny or intramuscular administration, the effect of epinephrine is at times amplified. Therefore, with refractory anaphylactic shock or stopping the heart, epinephrine is pre-diluted in the proportion of 1/10000, after which it is introduced intravenously or intramuscularly (so it starts to act faster). With refractory anaphylactic shock, an adult for 5 minutes is administered to 1 mg of epinephrine (1: 10,000; intravenously / intraosny), and when the heart is stopped, the inkjet injections are made 1 mg (1: 10000; intravenously and intraosnially). The principle of operation of intravenous and intra-view adrenaline injections is based on interaction with the alpha-adrenergic receptor, due to which the vessels are narrowed, the central blood pressure is rising (and the agonists of the alpha adrenergic receptor are considered alternative drugs). With intramuscular injections, the situation is more complicated, since the process itself is more laborious due to different thickness of the subcutaneous adhesive in humans, so too full people The doctor simply may not get to the bone or mistaken to get into Vienna (while often mistaken with concentration). Of course, intramuscular injections are more efficient than subcutaneous (with this method of administration of adrenaline, its pharmacokinetic profile is improved). Various modifications of α1 and β2 receptors, depending on the method of administering adrenaline, contribute to both increasing and decreasing arterial pressureDepending on whether it is achieved (due to the increase / decrease in the peripheral resistance of the vessels) the balance between the inotropic and chronotropic effect of adrenaline on the heart muscle (these effects contribute to increasing its contractility and acceleration of heartbeat, respectively). For subcutaneous and intramuscular injections, the standard concentration of adrenaline is considered to be 0.15-0.3 ml in proportion of 1: 1 000. In pharmacies, they are sold in the form of injections from allergies of the epipen brand.

Asthma

Adrenaline is used as an armor-expanding agent in the treatment of asthma, when they do not help (or there are not available) β2 receptor agonists. As a rule, astmatics are injected (intravenously and intramuscularly) 300-500 μg of adrenaline.

Croup

The racemic epinephrine of centuries is used for the treatment of cereals ( respiratory diseasemost common among children preschool age, most often aged three months to three years). The racemic adrenaline is a mixture of reducing (D) and left-hand (L) adrenaline isomers in proportion of 1: 1. L is an active ingredient. The racemic adrenaline has a stimulating effect on α-adrenergic receptors in the air flow, as a result of which the vessels of the throat of the throat are narrowed and the swelling is removed under voice ligaments, which ultimately leads to the relaxation of the smooth muscles of the bronchi.

Local anesthesia

Adrenaline is added to some local anesthetics, such as bupivacaines and lidocaine, due to which the vessels are narrowed, the absorption of anesthetic slows down, and it acts longer. Thanks to the vasoconductive properties of epinephrine, it is often added to the local anesthetics, which, among other things, helps to stop the bleeding (and reduce the overall loss of blood), when the patient is restored after an outpatient surgical intervention ("small" operations). Side effects (feeling of anxiety and fear, tachycardia and tremor) are due to the content of adrenaline in local anesthetics. Epinephrine / adrenaline is often added to dental and spinal anesthetics, after which there are particularly impressionable and sensitive people in the bouts of panic attacks, against the background of which they are often deprived of the gift of speech and frozen on the site "as inserted" (in such cases they speak of superficial anesthesia). The daily dose of the adrenaline-containing (vesseloring) dental anesthetic should not exceed 10 μg / pound of the total body weight.

Auto-injectors

Often, adrenaline is introduced using an auto-injector. Double injection "Twinjek" (currently such injections are not practiced) is an auto-injector with two syringes (in each of which - one dose of adrenaline). Despite the fact that "Epipen" and "Twinjek" is the names of trademarks, they are also used to designate any other auto-injector with adrenaline.

Side effects

Adrenaline's side reactions to adrenaline include such phenomena as rapid heartbeat, tachycardia, arrhythmia, increased anxiety, panic attacks, headache, tremor, hypertension and expressed pulmonary swelling. Adrenaline is contraindicated to people accepting non-selective β-blockers, since such a combination can cause sharp jumps (up) of blood pressure and even hemorrhagic stroke. Despite the widespread opinion that adrenaline, due to the narrowing of the coronary arteries, contributes to the development of heart failure, this is not the case. TO coronary arteries Only β2-receptors are attached, which, in the presence of adrenaline, on the contrary, cause the expansion of blood vessels. And, nevertheless, the high doses of adrenaline is by no means a way out when the heart is stopped, because it has not yet been proven that adrenaline increases the chances of a person to survive and avoid serious consequences from the CNS.

Physiology

Adrenal brainstabs makes only a minor "contribution" into the overall level of catecholamines in the blood, but this zone is responsible for the synthesis of more than 90% of circulating epinephrine. An insignificant amount of epinephrine is also contained in other tissues of the body, mainly in chromaffine cells. After resection of the adrenal glands, the level of epinephrine in the blood drops sharply to the zero mark. The adrenal glands are responsible for the production of about 7% of the circulating norepinephrine, most of which is a by-product of neurotransmission and is low-active on the hormonal level. Epinephrine has a stimulating effect on the adrenergic receptors α1, α2, β1, β2 and β3 of the sympathetic nervous system. Adrenergic receptors are considered prechet nerves (the name is associated with the special "sensitivity" of these receptors to adrenaline). The definition of "adrenergic" is often interpreted incorrectly, believing that the main neuromediator of the sympathetic nervous system is norepinephrine (norepinephrine), not epinephrine (Ulf von Yuler; 1946). Of course, epinephrine (affecting the β2 adrenergic receptor) accelerates metabolism and improves the operation of the upper respiratory tractBut at the same time, sympathetic ganglia are not related directly (neurons) with upper breathing paths. The very concept of brainstabs of adrenal glands and the sympathetic nervous system (formulated by Cannon) is directly related to the catecholamic reaction of the body for stress. However, the brainstabs of adrenal glands, in contrast to the adrenal cortex, does not affect whether the person will survive when the heart is stopped or not. After removing the adrenal glands, the hemodynamic and metabolic reaction of the body (on various stimuli, such as hypoglycemia and physical exertion) do not change. Epinephrine is an important neurotransmitter of the CNS. In the peripheral nervous system, epinephrine has a stimulating effect on the pre-synoptic β-receptor of the norepinephrine, although the degree of importance of this property is not established. The reception of beta-blockers (in humans) and resection of adrenal glands (in animals) suggest that endogenous epinephrine significantly accelerates metabolic processes in the body.

Physical exercises

The main stimulus for the extraction of epinephrine adrenalities is exercise. For the first time, it was demonstrated on the example of the denervated pupil of the cat, and later during the study of urine samples. Since 1950, biochemical methods for determining the level of catecholamines in plasma are regularly published in scientific publications. And, although the basis of the majority of such publications lay fluorescent analysis data, this method It is too generalized and allows you to accurately determine only a small share of epinephrine dissolved in plasma. With the discovery of extraction methods and radioisotope analysis (REC), it was possible to determine the level of epinephrine in the blood with an accuracy of 15. The results of the first REA tests showed that the level of epinephrine and catecholamines in the blood increases by the end of the workout when the anaerobic metabolism is launched. In physical exertion, the epinephrine concentration in the blood increases both due to the increased secretion of adrenal glands (which the epinephrine is highlighted) and due to the slowdation of metabolism against the background of slowing the hepatic blood flow. Intravenous infusion of epinephrina people at rest (in order to increase its level to such as in physical exertion) almost does not affect hemodynamics, with the exception of a minor reduction of diastolic blood pressure (due to the β2 receptor). Intravenous epinephrine injections (within physiological concentration) reduce the increased reactivity of the upper respiratory tract, sufficiently in order to inhibit the vasoconductive effect of the inhalation histamine. In 1887, the relationship between the sympathetic nervous system and the lungs was first established; This discovery is considered the merit of Grossman, which in one of its research has proven that when irritating the accelerating nerves of the heart, the upper respiratory tract, which before that narrowed under the action of Muskarin, begin to expand. In the course of simple experiments with dogs, in which a sympathetic chain was opened in the diaphragm region, Jackson showed that in this reaction, in the absence of direct stimulation of the lungs on the side of the sympathetic nervous system, allocated (adrenal brainstabs) Epinephrine stopped the process of bronchotone (narrowing of the bronchi lumen ), turning it into the opposite direction. This is a myth that after resection of adrenal glands, people become asthmatics; Those who have a predisposition to this disease, will not be superfluous to undergo corticosteroid replacement therapy, which "protects" them from the increased reactivity of the upper respiratory tract. With regular intense physical stages, the upper respiratory tract gradually expands due to the reduction of tone wandering nerve. Beta blockers containing propranolol increase the resistance of the upper respiratory tract (if they take them after workout; while the time frames are the same as when bronchial spasms appear against the background of asthma induced by physical exertion). Thus, by reducing the resistance of the upper respiratory tract during a workout, a person makes a smaller amount of breath and exhale (that is, it becomes easier to breathe).

Emotional reaction

Each emotional reaction is present behavioral, autonomous and hormonal components. The latter implies the release of epinephrine, a kind of response of the brainstabs of adrenal glands to stress, the mediator of which is a sympathetic nervous system. The main emotion that is associated with epinephrine is fear. During the experiment, with the participation of volunteers, which injected epinephrine was made, the expression of the face of these people was more often frightened than calm (they watched horror films), which you will not say about the control group of participants who have retained calm during the viewing. Those who have introduced Epinephren, were afraid in the cinema much more and they were more often manifested by bad memories than that of the representatives of the control group. The results of this experiment are a visual example that negative emotions are in one degree or another are associated with an increased concentration of epinephrine in the blood. The reason for these discoveries partly became the ability of epinephrine to cause responses of the sympathetic nervous system at the level of physiology, including a rapid heartbeat and trembling in the knees (typical signs of fear, arising independently of the actual intensity of fear caused by watching the film). Despite the fact that in the course of the studies between epinephrine and a sense of fear, a certain relationship was revealed, this regularity does not apply to other emotions. In the course of the same experiment, participants were also given to watch comedies and militants, why they did not become more fun or more aggressive. The results of this experiment were confirmed during the experiments with rodents, some of which were able to synthesize epinephrine, while others were capable of synthesize. The results of the experiments confirmed the fact that epinephrine really plays a certain role in deciphering emotional reactions, irritating the nervous system in response to fear.

Memory

Scientists have proven that adrenergic hormones, such as epinephrine, can contribute to the deterioration of long-term memory in humans. As is known, endogenous adrenaline is highlighted by the adrenal glands in response to stress, while modulating the consolidation of memory (postponement of events in long-term memory). In addition, the activity of the CNS (in terms of decoding information), one way or another depends on the concentration of epinephrine in the blood. According to some data, epinephrine plays a role in long-term adaptation of the body to stress and, in particular, in encoding emotional memory. Under the action of epinephrine, the CNS activity increases and the so-called "memory of fear" is activated (often on the background of pathological disorders, such as post-traumatic stress disorders). The results of most studies support the idea that "endogenous epinephrine, isolated by adrenal glands against mental activity, dulls long-term memory." Moreover, scientists came to the conclusion that the identification memory (on the faces, telephone numbers, etc.) is also formed under the action of epinephrine, irritating B-adrenergic receptors. Epinephrine does not immediately overcome the hematorecephalic barrier, and therefore its effect on memory is partly connected with peripheral B-adrenergic receptors. The results of the studies have shown that Satolol (antagonist B-adrenergic receptors, which, like epinephrine, does not immediately penetrate the brain) neutralizes the stimulating effect of adrenaline into memory. Based on these discovery, scientists concluded that B-adrenergic receptors are responsible for the ability of epinephrine to consolidate memory. Noraderenalin, under the influence of PNMT cells in cytosol, it is necessary to pre-clear from the granules of chromaffine cells. This is happening inside the so-called catecholamic (H +) "exchanger" of WMAD 1. WMAP-1 is also responsible for the transfer of new adrenaline from cytosoli back into chromaphhpine cell granules, from which it is later released. In the liver cell, adrenaline is attached to the β-adrenergic receptor, which changes its structure and helps Glutamine-synthase (G-protein) "exchange" GDF on GTF. This three-dimensional G - protein disintegrates on GS alpha and GS-beta derivatives, the first of which is attached to the adenil cyclase, thereby turning ATF in AMP (cyclic nucleotide). In turn, the cyclic AMF is attached to the regulatory subgroup of protein-kinase A: protein-kinase A phosphorylates phosphorylase kinase. Meanwhile, Beta / Gamma GS is embedded in a calcium channel, thereby allowing calcium ions to penetrate into the cell cytoplasm. Calcium ions are attached to calmodulin proteins (contained in eukaryotic cells), which are subsequently combined with phosphorylase kinase, thereby activating it. This kinase phosphorylates glycogen phosphorlase, which, in turn, phosphorylates glycogen himself, while turning into glucose-6-phosphate.

Pathology

Increased epinephrine secretion is observed in such pathologies as a peochromocytoma, hypoglycemia, myocardial infarction and (to a lesser extent) with a benign hereditary essential tremor. In these cases, a person, as a rule, begins to actively function the sympathetic nervous system, while the adrenal glands allocate more adrenaline; In the case of hypoxia and hypoglycemia, it is possible to talk about selectivity, since a human concentration of adrenaline (with respect to norepinenguine) significantly increases in the blood. Thus, the adrenal brainstant has a certain degree of autonomy with respect to other areas of the sympathetic nervous system (that is, separate from them). Myocardial infarction is characterized high levels Epinephren and norepinephrine in the blood (especially at the time of cardiogenic shock). Against the background of a benign hereditary tremor (DNT), blockers of peripheral β- and beta-2 adrenergic receptors, which is why human is beginning to shake hands (often the whole body). Scientists have discovered that the patients with the diagnosis of DNT in the plasma elevated the level of epinephrine (which cannot be said about Norepinefrine). Low (or zero) epinephrine concentrations are characteristic of vegetative neuropathy or the next adrenal resection behind it. In disruption of the function of the adrenal cortex (Addison disease, etc.), epinephrine synthesis is terminated, since the synthesizing enzyme (phenyl-ethanol-amine-n-methyl-transferase) is active only high concentrations Cortisol coming from adrenal cortex in the brainstant.

Terminology

"Epinephrine" is the name given by the Gormina by Americans, which is part-time is an international non-payable name, however, in everyday life, the more common name is "adrenaline". The term "epinephrine" itself (from Greek. "Above the kidneys") came up with John Abel, who used it to designate the extracts made from adrenal glands (1897). In 1901, Yokishi Takakin patented a purified extract from adrenal glands, giving him the name "adrenaline" (from Lat. "Above the kidneys"); Adrenaline went on sale under the brand name "Park, Davis & Co." in the USA. Being firmly convinced that Abel extract does not differ from the extract of Takacina (this belief caused a lot of disputes), American scientists made the "epinephrine" by the generic name of this hormone. In the UK and on the pages of European pharmacopy, the generally accepted title is "adrenaline" (in this and consists of one of the main differences between the MNN and Bon-systems). American doctors and scientists more often use the term "epinephrine", rather than "adrenaline". And yet, drugs-analogs Epinephrine is often called "adrenergics", and epinephrine receptors are "adrenergic" or "adreno-receptors". The impact of adrenaline on the body:

Heart: Following the heartbeat

Light: Increases air flow rate when breathing; Systematic vesseloring and vasodilator action

Liver: stimulates glycogenolysis (glycogen decay)

The body as a whole: causes lipolysis (splitting of fats); Enhances the contractile ability of the muscles

Being a hormone-neurotiator, epinephrine affects almost all tissues and organs. The specifics and the intensity of exposure differ depending on the type of tissue and the presence of adrenergic receptors in it. For example, in high concentrations (physiological), epinephrine helps to relax the smooth muscles of the upper respiratory tract, but it causes the smooth muscles of most small arteries. Epinephrine is attached to various adrenergic receptors (the main mechanism of action). Epinephrine is a non-selective agonist of all adrenergic receptors, including the main subgroups α1, α2, β1, β2 and β3. After attaching to receptors, adrenaline causes a number of metabolic changes. When adjusting to α-adrenergic receptors, it inhibits insulin production (pancreas), causes glycogenolysis (in the liver and muscles), glycoliz, and also interferes with muscle insulin-adjustable glycogenesis. Attaching to the β-adrenergic receptor, epinephrine stimulates the production of glucagon (pancreas), adrenocorticotropic hormone (ACTH) (pituitary) and accelerates the splitting of adipose tissue. In the aggregate, the effects described above lead to an increase in blood glucose and stimulate the synthesis of fatty acids (glucose and fatty acids are saturated with energy cells).

Biological fluids

For more accurate diagnostics various diseasesModern doctors measure the level of epinephrine in the blood, plasma or serum. In adults at rest, the concentration of endogenous epinephrine in the plasma is usually below 10 μg / l, but during exercise this indicator tends to increase 10 times, and during periods of stress and more than 50 times. In patients with a diagnosis of "Feochromocytoma", the level of adrenaline in the plasma reaches 1000-10 000 μg / l. In parenteral administration of epinephrine "Cores" as intensive therapy or emergency carePlasma concentrations increase up to 10,000 -100 000 μg / l.

Biosynthesis and regulation

Epinephrine is synthesized with adrenal brainstabs with the participation of enzymes converting tyrosine (amino acid) into some of its derivatives, which ultimately take the form of epinephrine. First, tyrosine is oxidized to the state of the L-dof, which subsequently decarboxylates, forming dopamine. Norepinephrine is a product of its oxidation. The last step in epinephrine biosynthesis is methylation of the original norepinenaline. In the role of the catalyst for this reaction, the enzyme of phenyl-ethanol-amine-n-methyl-transferase (FNMT), which uses S-adenosyl methomine (SAME) as a supplier (donor) methyl. Despite the fact that most of the FNMT focuses in the cytosol of endocrine cells of the adrenal brainstones (also known as chromaffine cells), this enzyme is also detected in the heart and brain (at low concentrations).

Regulation

The main psychological incentive for the allocation of adrenaline is stress (whether it is a threat to physical health, excitement, noise, bright light and high temperatures). All these incentives are pre-processed by the central nervous system. The adrenocorticotropic hormone (ACTH) and the sympathetic nervous system stimulate the production of adrenaline precursor substances, by increasing the activity of tyrosine hydroxylase and dopamine-β-hydroxylase, two main enzymes that are responsible for the synthesis of catecholamines. The ACTH also has a stimulating effect on the adrenal cortex, which is necessary for the release of cortisol, due to which the amount of FNMT in chromaffine cells increases and, as a result, adrenaline production increases (most often in response to stress). The sympathetic nervous system, interacting with the inner nerves with the adrenal brainstabs, stimulates the production of adrenaline. Acetylcholine, which is allocated due to the preggalionic sympathetic fibers of these nerves, affects nicotine acetylcholine receptors, which leads to depolarization (decrease in the membrane potential) of cells and the active calcium inflow by potential-dependent calcium channels. Calcium causes exocytosis of chromaffine cells and, as a result, the release of adrenaline (and norepinephrine) from adrenalines, from where they enter the bloodstream. Unlike many other hormones, adrenaline (as well as other catecholamines) does not have a negative "feedback" effect (that is, it does not interfere with its own synthesis). The concentration of adrenaline in the blood is strongly increasing under certain circumstances, in particular, due to the uncontrolled admission of epinephrine (without the appointment of a doctor), under feuohromocharcitoma and others malignant formations In sympathetic ganglia. Adrenaline temporarily ceases to act when re-entering the nerve endings (in the form of weak solutions), exposed to metabolism from monoamine-oxidase and catechol-o-methyl transferase.

History

Adrenal extracts were first obtained by Polish physiologist Napoleon Tsibulski in 1895. As part of these exhausts, which he called "Nadnerczyna", was present adrenaline and other catecholamines. The American Ophthalmologist William Bates first began to use adrenaline during the operations in the eyes (until April 20, 1896). Japanese chemist Yokishi Takakin, together with his assistant, Kazio Wenaco, opened adrenaline in 1900. In 1901, Takakin conducted a successful experiment, highlighting a pure hormone from the adrenal sheep and bulls. Adrenaline for the first time artificially synthesized in their laboratories Friedrich Stolz and Henry Drisdale Daikin (independently of each other in 1904).

Recipe (international)

RP.: SOL. EPINEPHRINI HYDROCHLORIDI 0.1% - 1 ML
D.T.D. N. 6 in AMPULLIS.
S. Entering 0.5 ml under the skin with anaphylactic shock

pharmachologic effect

Stimulates alpha and beta-blood pressure renoreceptors.

According to the peripheral sympathomimetic effect of Ephedrine is close to adrenaline. It causes a narrowing of the vessels, an increase in blood pressure, the expansion of the bronchi, the inhibition of the peristaltic (wavy movements) of the intestine, the expansion of pupils, increase the content of glucose in the blood.

Comparatively with adrenaline, ephedrine has a less sharp, but significantly longer action. Due to the greater the resistance of the ephedrine is effective when administered inward and convenient for use in course treatment (for example, allergic diseases).

In contrast to adrenaline, the ephedrine has a specific stimulating effect on the central nervous system. In this regard, it is close to the Fenamine, but the latter acts much stronger.

Mode of application

For adults: Epinephrine is introduced subcutaneously, intramuscularly, intravenously.

In an anaphylactic shock: slowly intravenously 0.1-0.25 mg diluted in 10 ml of 0.9% sodium chloride solution, if necessary, the introduction of intravenously drip at a concentration of 0.1 m / ml; If the patient's condition admits a slow action (3-5 minutes), it is preferable to introduce intramuscularly (or subcutaneously) 0.3-0.5 mg in an undivided or diluted form, if necessary, administration is repeated after 10-20 minutes (up to 3 times).

An intravenously drip at a speed of 1 μg / min (with a possible increase in the introduction rate to 2-10 μg / min) is administered as a vasoconstrictor agent.

With bronchial asthma: intravenously 0.1-0.25 mg in a diluted at a concentration of 0.1 mg / ml or subcutaneously 0.3-0.5 mg in an undivided or diluted form, repeated doses, if necessary, can be administered every 20 minutes (up to 3 times).

Asistolia: intracardiac 0.5 mg (diluted with 10 ml of 0.9% sodium chloride solution or other solution); when conducting resuscitation measures - 1 mg (in a diluted form) intravenously every 3-5 minutes; If the patient is intouted, then the endotracheal administration is possible - the optimal doses are not installed, but should be 2-2.5 times more doses for intravenous administration.

The prolongation of the action of local anesthetics: at a concentration of 5 μg / ml (dose used from the type of anesthetic used), for the spinal anesthesia - 0.2-0.4 mg.

Newborn (with asystole): intravenously, slowly, 10-30 μg / kg every 3-5 minutes; Children, older than 1 month: intravenously, 10 μg / kg (in the future, if necessary, 100 μg / kg are administered every 3-5 minutes); Perhaps the use of endotracheal administration.

Children with bronchospasm: subcutaneously 10 μg / kg (maximum - to 0.3 mg), if necessary, administration repeat every 15 minutes (up to 3-4 times) or every 4 hours.

Children with anaphylactic shock: intramuscularly or subcutaneously - 10 μg / kg (maximum - to 0.3 mg), if necessary, repeat the introduction of these doses every 15 minutes (up to 3 times).
Open-finished glaucoma - 2 times a day 1 drop 1-2% solution. To stop bleeding, locally, in the form of tampons, which are moistened with a solution of the drug.

When carrying out infusion, it is necessary to apply a device with a measuring device to control the rate of administration of the drug. Infusion should be carried out in a large vein (better in Central). Intridormo epinephrine is introduced with asistolia, only if other methods are not available, as there is a risk of pneumothorax and tamponade of the heart. During therapy, Epinephrine recommended control of the serum content in K +, measurement of diuresis, blood pressure, IOC, central venous pressure, ECG, junction pressure in pulmonary capillaries and pressure in pulmonary artery.

High doses of epinephrine with myocardial infarction due to improving the need for myocardium in oxygen can enhance ischemia. Epinephrine enhances glycemia, so sugar diabetes Higher doses of sulfonylurea and insulin derivatives are needed. With the introduction of endotragically, the absorption and final plasma content of epinephrine can be unpredictable.

You can use epinephrine in children when you stop the heart, but care must be taken, since 2 different concentrations of the drug are required in the dosing circuit. With the cessation of dose therapy, it is necessary to reduce gradually, since the sudden cancellation of treatment may cause severe hypotension.

Indications

to eliminate allergic reactions of the immediate type (quinque, anaphylactic shock, urticaria), which developed as a result of drug allergies, when overflowing blood, food use, the introduction of other allergens or insect bite;

With asistolia, including on the background of AV blockade of 3 degrees;
- relief of the attack of bronchial asthma;
- bronchospasm, which arose during the use of anesthesia;
- extension of local painkillers;
- arterial hypotension, which is not amenable to treatment with replacement liquids (after injuries, in shock, with bacteremia, open heart operations, with renal failure, overdose of drugs, heart failure);
- hypoglycemia caused by insulin overdose;
- glaucoma, if surgery in the eyes is required, in order to expand the pupil, remove the intraocular pressure;
- stop bleeding;
- Treatment of priapism.

Contraindications

Hypersensitivity, Feochromocytoma, Gokmp, arterial hypertension, coronary heart disease, ventricular fibrillation, tachyarhythmia, lactation period, pregnancy.

Side effects

angina, tachycardia, heartbeat, bradycardia, increase or decrease in blood pressure;

stomatricular arrhythmia, chest pain, cardiac
arrhythmia (high dosages means);

anxiety, tremor, headaches, dizziness;
less often than usual - feeling fatigue, feeling of heat or cold, nervousness;

insomnia, spontaneous muscle contractions, excitation of NA, failures in memory, disorientation, panic and aggression, paranoia, disorders similar to schizophrenia (rarely);

vomiting, troubles with urination, pain during urination, nausea;

rashes on the skin of an allergic nature, bronchospasm, swelling of quinque, multiform erythema;
sweating, hypokalemia - rarely;

clear, persistent and strong erection, muscle tightening.
During the intramuscular injection at the place of administration of the drug, pain and burning sensation may occur.

Form release

Powder; Tablets at 0.002; 0.003 and 0.001 g (for pediatric practice);

5% solution (for injection) in 1 ml ampoules;
2% and 3% solutions in 10 ml bottles (for otorinolaryngological practice).

ATTENTION!

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MNN: Epinephrine

Manufacturer: Pharmaceutical company Health OOO

Anatomy-therapeutic-chemical classification: Epinephrine.

Registration number in Kazakhstan: RK-LS-5№011371

Registration period: 29.05.2018 - 29.05.2023

Instruction

Tradename

Adrenalin-Health

International non-proprietary title

Epinephrine

Dosage form

Injection solution 0.18%, 1 ml

Structure

1 ml of solution contains

active substance - Hydrotater adrenaline 1,82 mg

excipients: sodium metabisulphite (E 223), sodium chloride, water for injection

Description

Transparent colorless solution

Pharmacotherapeutic group

Preparations for the treatment of heart disease. Cardiotonic means of blackcloth origin. Adreno and dopamine-stimulators. Epinephrine.

Code ATH C01S24.

Pharmacological properties

Pharmacokinetics

After intramuscular or subcutaneous administration Epinephrine is quickly absorbed; The maximum concentration in the blood is achieved after 3-10 minutes.

Therapeutic effect develops almost instantly when intravenous administration (Duration of action - 1-2 minutes), 5-10 minutes after subcutaneous administration (maximum effect - after 20 minutes), with intramuscular administration, the start time of the effect is variable.

Penetrates the placental barrier, in breast milkdoes not penetrate the hematorencephalic barrier.

Metabolized monoaminoxidase (in vanillamindal acid) and catechol-o-methyltransferase (in metanephrine) in the cells of the liver, kidney, intestinal mucosa, axon.

The half-life during intravenous administration is 1-2 minutes. The excretion of metabolites is carried out by the kidneys. Stands out with breast milk.

Pharmacodynamics

Adrenalin-Health is a pacemulatory, vasoconstrictor, hypertensive, anti-hydrcemic agent. Stimulates α- and β-adrenoreceptors of various localization. It shows a pronounced effect on the smooth muscles of the internal organs, the cardiovascular and respiratory system, activates the carbohydrate and lipid exchange.

The mechanism of action is due to the activation of adenylate cyclase of the inner surface of cell membranes, an increase in the intracellular concentration of CAMF and CA2 +. The first phase of action is due primarily to the stimulation of β-adrenoreceptors of various organs and is manifested by tachycardia, an increase in cardiac output, excitability and conductivity of myocardium, arteriolo- and brightness, decrease in the tone of the uterus, mobilization of glycogen from liver and fatty acids from fatty depots. In the second phase, the excitation of α-adrenoreceptors, which leads to narrowing of the vessels of the organs abdominal cavity, skin, mucous membranes (skeletal muscles - to a lesser extent), increase blood pressure (mainly systolic), total peripheral vessel resistance.

The effectiveness of the drug depends on the dose. In very low doses, at a rate of administration less than 0.01 μg / kg / min, it may reduce the blood pressure due to the extension of the vessels of the skeletal muscles. At the rate of administration of 0.04-0.1 μg / kg / min increases the frequency and force of heart abbreviations, the impact volume of blood and the minute volume of blood, reduces the total peripheral resistance of the vessels; Above 0.2 μg / kg / min - narrows vessels, increases blood pressure (mainly systolic) and total peripheral resistance of vessels. The press effect may cause a short-term reflector deceleration of heart rate. Relaxes the smooth muscles of the bronchi. Doses above 0.3 μg / kg / min reduce renal blood flow, blood supply to internal organs, tone and motorcyc of the gastrointestinal tract.

Increases conductivity, excitability and myocardial automatism. Increases the need of myocardium in oxygen. Inhibits antigens induced release of histamine and leukotriene, eliminates the spasm bronchiol, prevents the development of edema of their mucous membrane. Acting on α-adrenoreceptors of the skin, mucous membranes and internal organs, causes the narrowing of the vessels, reducing the suction rate of local tools, increases the duration of action and reduces the toxic effect of local anesthesia. The stimulation of β2-adrenoreceptors is accompanied by an increase in the removal of potassium from the cell and can lead to hypokalemia. In case of intracable administration, it reduces the blood flow of the cavernous bodies.

Expanding pupils, helps to reduce products intraocular fluid and intraocular pressure. Causes hyperglycemia (enhances glycogenolysis and gluconeogenesis) and increases content in plasma of free fatty acids, improves tissue exchange. Weakly stimulates the central nervous system, exhibits an anti-allergic and anti-inflammatory effect.

Indications for use

allergic reactions of immediate type: anaphylactic shock, which developed when using medicines, serum, blood transfusion, insect bite, or contact with allergens

saving sharp attacks of bronchial asthma

arterial hypotension of various genes (posthemorrhagic, intoxication, infectious)

hypokalemia, including due to insulin overdose

asistolia, Heart Stop

extension of local anesthetics

AV Blocade III degree, acutely developed

Method of application and dose

Prescribed intramuscularly, subcutaneously, intravenously (drip), intracardiac (conducting resuscitation when stopping the heart). With intramuscular administration, the effect of the drug is developing faster than with subcutaneous. Dosing mode individual.

Adults.

Anaphylactic shock: Intravenously slowly 0.5 ml, divorced in 20 ml of 40% glucose solution. In the future, if necessary, an intravenous drip administration continues with a speed of 1 μg / min, for which 1 ml of the adrenaline solution is dissolved in 400 ml of isotonic sodium chloride or 5% glucose. If the patient's condition admits, it is better to carry out intramuscular or subcutaneous administration of 0.3-0.5 ml in diluted or undersedized form.

Bronchial asthma: Enter subcutaneously 0.3-0.5 ml in diluted or undiluted form. If you need to repeat this dose, you can enter every 20 minutes (up to 3 times). It is possible intravenous administration of 0.3-0.5 ml in a diluted form.

As a vasoconstrictor Intravenously injected with a speed of 1 μg / min (with a possible increase of up to 2-10 μg / min).

Asistolia: Insertionally 0.5 ml injected, divorced in 10 ml of 0.9% sodium chloride solution. During resuscitation measures - 1 ml (in a divided form) intravenously slowly every 3-5 minutes.

Children.

ASISTOLY in newborns: We administered intravenously at 0.01 ml / kg of body weight every 3-5 minutes, slowly.

Anaphylactic shock: Enter subcutaneously or intramuscularly to children under the age of 1 year - 0.05 ml, at the age of 1 year - 0.1 ml, 2 years - 0.2 ml, 3-4 years - 0.3 ml, 5 years - 0, 4 ml, 6-12 years old - 0.5 ml. If necessary, administration is repeated every 15 minutes (up to 3 times).

Bronchospasm: 0.01 ml / kg of body weight (maximum to 0.3 ml) are injected. If necessary, administration repeat every 15 minutes (up to 3-4 times) or every 4 hours.

Side effects

Often:

headache

anxiety

• nausea, vomiting

  anorexia

  hyperglycemia

Infrequently:

stenzardia, bradycardia or tachycardia, feeling of heartbeat, decrease or enhancement of blood pressure (even with subcutaneous administration in conventional doses due to an increase in blood pressure possibly subarachnoid hemorrhage and hemiplegia)

• nervousness, dizziness, fatigue, sleep disorder

  muscular twitching

  psychoneurotic disorders (psychomotor arousal, disorientation)

  memory disorder

  aggressive or panic behavior

  schizophren-like disorders, paranoia

  increased rigidity and tremor (in patients with Parkinson's disease)

  angioedema swelling, bronchospasm

  skin rash, multiform erythema

  increased sweating, violation of thermoregulation, cooling limbs

Seldom:

ventricular arrhythmias, pain in chest

eCG changes (including a decrease in the amplitude of the tissue T)

humped and painful urination (with hyperplasia prostatic gland)

hypokalemia

pulmonary edema

pain or burning in the place of intramuscular injection, with multiple injections of adrenaline, necrosis may be marked due to adrenaline vessels

Contraindications

increased individual sensitivity to drug components

hypertrophic obstructive cardiomyopathy

heavy aortic stenosis

tahiaritimia, ventricular fibrillation

arterial or pulmonary hypertension

ischemic lung disease

expressed atherosclerosis

occlusive vascular diseases

feochromocytoma

clotched glaucoma

shock not allergenic genesis

convulsive syndrome

thyrotoxicosis

diabetes

general anesthesia using inhalation agents: fluorotan, cyclopropane, chloroform

period of pregnancy and lactation, II period of childbirth

application on the portions of the fingers and legs, in the sections of the nose, genitals

Medicinal interactions

Epinephrin antagonists are α- and β -adrenoreceptor blockers.

With the simultaneous use of the drug adrenaline-health with other drugs, it is possible:

- with narcotic analgesics and sleeping pills - the weakening of their effects;

- with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, means for inhalation anesthesia (chloroform, enfluran, galotan, isoflurane, methoxyphluran), cocaine - raising the risk of developing arrhythmias; - with other sympathomimetic means - enhancing the severity of side effects from the cardiovascular system;

- with antihypertensive means (including with diuretics) - reduction of their effectiveness;

- with monoaminoxidase inhibitors (including furazolidone, prokarbazin, selegilin) \u200b\u200b- a sudden and pronounced increase in blood pressure, hyperpyritical crisis, headache, heart arrhythmias, vomiting;

- with nitrates - the weakening of their therapeutic action;

- with phenoxybenzamin - strengthening the hypotensive effect and tachycardia;

- with phenytino - a sudden decrease in blood pressure and bradycardia, depending on the dose and the rate of administration of adrenaline;

- with hormone drugs thyroid gland - mutual strengthening of action;

- with asthyisol, cisapride, terpheneadine - the elongation of the Qt interval to the ECG;

- with diaptisoatami, iotalamova or yoxaglic acids - strengthening neurological effects;

- with alkaloids of the ardines - strengthening the vasoconstrictor effect up to pronounced ischemia and the development of gangrenes;

- with hypoglycemic drugs (including insulin) - reduction of the hypoglycemic effect;

With non-prescribing muscle relaxants - it is possible to reduce the mioryexing effect;

With hormonal contraceptives - can reduce efficiency.

special instructions

Intridially introduced with asystole if other ways to eliminate it is not available, while there is an increased risk of developing tamponads of the heart and pneumothorax.

If you need to carry out infusion, you should use a device with a measuring device in order to regulate the rate of infusion. Infusion should be carried out in large, better in the central vein. When conducting an infusion, it is recommended to monitor the concentration of potassium in serum, blood pressure, diurea, ECG, central venous pressure, pressure in the pulmonary artery.

The use of the drug with diabetes mellitus increases glycemia, and therefore higher insulin doses or sulfonylurea derivatives are required.

Adrenaline is undesirable to apply for a long time, since the narrowing of peripheral vessels can lead to the development of necrosis or gangrene.

With the cessation of treatment, the adrenaline dose should be reduced gradually, since the sudden cancellation of therapy can lead to severe hypotension.

Carefully prescribe patients with ventricular arrhythmias, ischemic disease Hearts, atrial fibrillation, arterial hypertension, pulmonary hypertension, with myocardial infarction (in case of the need to use the drug with myocardial infarction, it should be remembered that adrenaline can enhance ischemia by increasing the need of myocardium in oxygen), metabolic acidosis, hypercapper, hypoxia, hypovolemia, hypercapper, hypoxia, hypovolemia, thyrotoxicosis, in patients with occlusal diseases of vessels (arterial embolism, atherosclerosis, burgher disease, cold injury, diabetic endarterite, Reino disease, with cerebral atherosclerosis, Parkinson's disease, with convulsive syndrome, with prostate hypertrophy.

In hypovolemia, before using sympathomimetics, it is necessary to carry out the appropriate hydration of patients.

Application in pediatrics.

Special caution should be taken with the introduction of the drug to children (different dispensing). Recommendations on the dosage of the drug for children are given in the section "The method of application and dose".

Application during pregnancy and lactation

Not used during childbirth for the correction of the hypotension, since the drug can delay the second period of childbirth by relaxing the muscles of the uterus. When introduced in large doses to weaken the cutting of the uterus, a long-term atron of the uterine with bleeding can be caused.

If necessary, applying the drug should stop breastfeeding, as there is a high probability of developing side effects in a child.

Features of the drug influence on the ability to manage vehicles and work with complex mechanisms.

Overdose

Symptoms: Excessive enhancement of blood pressure, mydriasis, tachyrhythmia, replacing bradycardia, violation of heart rhythm (including atrial fibrillation and ventricular), cooling and pallor of skin, vomiting, fear, anxiety, tremor, headache, metabolic acidosis, myocardial infarction, cranial Brain hemorrhage (especially in elderly patients), pulmonary swelling, renal failure.

Treatment: Termination of the drug. Symptomatic therapy, the use of α- and β-adrenoblockers, high-speed nitrates. At arrhythmias prescribe parenteral administration of β-adrenobloclars (propranolol).

Release form and packaging

1 ml of the drug is poured into the ampoules of glass.

On the ampoule, the paint is applied marking text or stick a label.

5 or 10 ampoules along with the instructions for medical application In state and Russian languages \u200b\u200band disk cutting ceramics are placed in a cardboard box with partitions.

5 ampoules are placed in the contour cellular packaging of polyvinyl chloride film and aluminum foil.

Gross formula

Pharmacological group of substance Epinephrine

Nonological Classification (ICD-10)

CAS code

Characteristics of the substance of epinephrine

White or white with a gray-gray crystalline powder, easily soluble in water, a little soluble in alcohol, varies under the action of light and oxygen.

Application in pregnancy and breastfeeding

Typical clinical and pharmacological article 1

Pharmaceutical. Alpha and beta adrenostimulant.

At the cellular level, the action is due to the activation of adenylate cyclase on the inner surface of the cell membrane, an increase in the intracellular concentration of the CAMF and Ca 2+. In very low doses, at a rate of administration, less than 0.01 μg / kg / min can reduce the blood pressure due to the expansion of skeletal muscles vessels. At the rate of administration of 0.04-0.1 μg / kg / min increases the heart rate and the power of heart abbreviations, the uk and the IOC, reduces the OPS; Above 0.02 μg / kg / min, heals vessels, increases blood pressure (mainly systolic) and OPS. The press effect may cause a short-term reflex deceleration of heart rate. Relaxes the smooth muscles of the bronchi. Doses above 0.3 μg / kg / min, reduce the renal blood flow, blood supply to the internal organs, tone and motorcycle gastrointestinal motorcycle. Expanding pupils, helps to reduce the products of intraocular fluid and intraocular pressure. Causes hyperglycemia (enhances glycogenolysis and gluchegenesis) and increases the content in the plasma of free fatty acids. Increases conductivity, excitability and myocardial automatism. Increases the need of myocardium in oxygen. Inhibits antigens induced release of histamine and leukotriene, eliminates spasm bronchiol, prevents the development of edema of their mucous membranes. Acting on alpha-adrenoreceptors, located in the skin, mucous membranes and internal organs, causes the narrowing of the vessels, reducing the suction rate of local resources, increases the duration and reduces the toxic effect of local anesthesia. Stimulation of beta 2 -adrenoreceptors is accompanied by an increase in the elimination of K + from the cell and can lead to hypokalemia. In case of intracable administration, it reduces the blood flow of the cavernous bodies. The therapeutic effect develops almost instantly when in / in administration (duration of action - 1-2 minutes), 5-10 minutes after a p / k administration (maximum effect - after 20 minutes), with a / m administration - the start time variable.

Pharmacokinetics. With a / m or n / to administration, it is well absorbed. Inserted parenterally, quickly destroys. It is also absorbed during endotracheal and conjunctival administration. TC MAX with P / C and I / M Introduction - 3-10 minutes. Penetrates the placenta, in breast milk, does not penetrate the BGB. Metabolized mainly by Mao and CT in the end of the sympathetic nerves and other fabrics, as well as in the liver to form inactive metabolites. T 1/2 When in / in the introduction - 1-2 minutes. Excreted by kidneys in the main form of metabolites: vanillamindal acid, sulfates, glucuronides; And also in minor quantities - unchanged.

Indications. Allergic reactions of immediate type (including urticaria, angioedema, anaphylactic shock), developing when the use of drugs, serum, blood transfusion, food use, insect bite, or the introduction of other allergens; bronchial asthma (binding attack), bronchospasm during anesthesia; asistolia (including on the background of acutely developed AV blockade III Art.); bleeding from surface vessels of the skin and mucous membranes (including from gums), arterial hypotension, not amenable to adequate volumes of replaceable liquids (including shock, injury, bacteremia, operation on open heart, renal failure, hsn, an overdose of LS), the need to eliminate the action of local anesthetics; hypoglycemia (due to insulin overdose); Open-finished glaucoma, with surgical operations in the eyes - the swelling of the conjunctiva (treatment), to expand the pupil, intraocular hypertension, stopping bleeding; Priapism (treatment).

Contraindications. Hypersensitivity, GOKMP, Feochromocytoma, arterial hypertension, Tahiaritimia, IBS, ventricular fibrillation, pregnancy, lactation period.

Carefully. Metabolic acidosis, hyperkatsy, hypoxia, atrial fibrillation, ventricular arrhythmia, pulmonary hypertension, hypovolemia, myocardial infarction, shock of non-allergic genesis (including cardiogenic, traumatic, hemorrhagic), thyrotoxicosis, occlusive vascular diseases (including in history - arterial embolism, atherosclerosis, burgher disease, cold injury, diabetic endarterite, Reino disease), cerebral atherosclerosis, closed-deed glaucoma, diabetes, Parkinson disease, convulsive syndrome, prostate hypertrophy; Simultaneous use of inhalation anesthetics (halotan, cyclopropane, chloroform), elderly age, children's age.

Dosing. P / k, in / m, sometimes in / in drip.

Anaphylactic shock: V / in slowly 0.1-0.25 mg diluted in 10 ml of 0.9% NaCl solution, if necessary, continues to / in drip administration at a concentration of 0.1 m / ml. When the patient's condition admits a slow action (3-5 min), it is preferable to administer to / m (or p / k) 0.3-0.5 mg in a diluted or undivided form, if necessary, re-administration - after 10-20 minutes (up to 3 times).

Bronchial asthma: p / k 0.3-0.5 mg in a diluted or undivided form, if necessary, repeated doses can be administered every 20 minutes (up to 3 times), or in / in 0.1-0.25 mg Diluted at a concentration of 0.1 mg / ml.

As a vesseloring agent, V / in drip at a rate of 1 μg / min (with a possible increase of up to 2-10 μg / min) is introduced.

To lengthen the action of local anesthetics: at a concentration of 5 μg / ml (dose depends on the type of anesthetic used), for spinal anesthesia - 0.2-0.4 mg.

When asystolia: intracardiac 0.5 mg (diluted with 10 ml of 0.9% NaCl solution or other solution); During resuscitation activities - 1 mg (in a diluted form) in / every 3-5 minutes. If the patient is intubted by endotracheal instillation - optimal doses are not installed, should be 2-2.5 times higher than doses for in / in administration.

Newborn (asistolia): V / B, 10-30 μg / kg every 3-5 minutes, slowly. Children, older than 1 month: V / B, 10 μg / kg (subsequently, if necessary, every 3-5 min is administered by 100 μg / kg (after the introduction of at least 2 standard doses, you can use higher doses every 5 min - 200 μg / kg). It is possible to use endotracheal administration.

Children with anaphylactic shock: p / k or in / m - 10 μg / kg (maximum - to 0.3 mg), if necessary, the introduction of these doses is repeated every 15 minutes (up to 3 times).

Children with bronchospasm: p / k 10 μg / kg (maximum - to 0.3 mg), doses, if necessary, repeat every 15 min (up to 3-4 times) or every 4 hours.

Locally: to stop bleeding in the form of tampons, moistened with a solution of the drug.

With an open-angle glaucoma - 1 cap 1-2% of the solution 2 times a day.

Side effect. From the CSS side: less often - angina, bradycardia or tachycardia, heartbeat, increase or decreased blood pressure, at high doses - ventricular arrhythmias; Rarely - arrhythmia, chest pain.

From the nervous system: more often - headache, alarming state, tremor; Less often - dizziness, nervousness, fatigue, psycho-erectic disorders (psychomotor arousal, disorientation, memory disorder, aggressive or panic behavior, schizophren-like disorders, paranoia), sleep disorder, muscle twitching.

From side digestive system: more often - nausea, vomiting.

From the urinary system: rarely - difficult and painful urination (with prostate hyperplasia).

Local reactions: pain or burning in place in / m injection.

Allergic reactions: angioedema edema, bronchospasm, skin rash, multiform erythema.

Others: rarely - hypokalemia; Less often - increased sweating.

Overdose. Symptoms: Excessive increase in blood pressure, tachycardia, replacing bradycardia, rhythm disorders (including atrial fibrillation and ventricular), cooling and pallor of skin, vomiting, headache, metabolic acidosis, myocardial infarction, cranial hemorrhage (especially in the elderly patients), pulmonary swelling, death.

Treatment: stop administration, symptomatic therapy - to reduce adrenal adrenoblays (fantolamine), during arrhythmia - beta-adrenoblasts (propranolol).

Interaction. Epinephrine antagonists are alpha and beta-adrenoreceptor blockers.

Weakens the effects of narcotic analgesics and sleeping pills.

When used simultaneously with cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, means for inhalation anesthesia (chloroform, enfluran, galotan, isoflurane, methoxyphluran), cocaine increases the risk of developing arrhythmias (together should be extremely careful or not used at all); with other sympathomimetic means - strengthening the severity of side effects by the CSS; With antihypertensive means (including with diuretics) - reduction of their effectiveness.

Simultaneous appointment with Mao inhibitors (including Furazolidon, Zamazbazin, SELEGILIN) can cause a sudden and pronounced increase in blood pressure, hyperpyritical crisis, headache, heart arrhythmias, vomiting; with nitrates - the weakening of their therapeutic action; with phenoxybenzamin - strengthening the hypotensive effect and tachycardia; with phenytino - a sudden decrease in blood pressure and bradycardia (depends on the dose and the rate of administration); with drugs of thyroid hormones - mutual strengthening of action; with drugs lengthening the QT interval (including astemisol, cisapride, terpheneadine), - the elongation of the Qt interval; with diaptizoathas, iotalamova or yoxaglic acids - strengthening neurological effects; With alkaloids of the ardines - the strengthening of the vasoconstrictor effect (up to pronounced ischemia and the development of gangrenes).

Reduces the effect of insulin and other hypoglycemic drugs.

Special instructions. In case of infusion, use the instrument with the measuring device in order to regulate the rate of infusion.

Infusion should be carried out in a large (better central) vein.

Intriculturally introduced with asistolism, if other methods are not available, because There is a risk of tamponade of the heart and pneumothorax.

During the period of treatment, it was recommended that the concentration of K + in the serum, measurement of blood pressure, diurea, IOC, ECG, central venous pressure, pressure in the pulmonary artery and the pressure of the junction in pulmonary capillaries.

Excessive doses with myocardial infarction can enhance ischemia by increasing the need of myocardium in oxygen.

Increases glycemia, and therefore, with diabetes, higher doses of insulin and sulfonylurea derivatives are required.

In case of endotracheal administration, the suction and final concentration of the drug in plasma can be unpredictable.

The introduction of epinephrine at shock states does not replace blood transfusions, plasma, blood-absorbing liquids and / or saline solutions.

Epinephrine is inappropriate to apply a long time (narrowing peripheral vessels, leading to the possible development of necrosis or gangrene).

Strictly controlled studies of the use of epinephrine in pregnant women were not spent. The statistically regular interrelation of the appearance of deformities and groin hernia in children, whose mothers were used epinephrine during the I trimester or throughout the pregnancy, were also reported in one case about the occurrence of the enclosure in the fetus after the Mother of Epinephrine. Epinephrine should not be used pregnant with blood pressure above 130/80 mm Hg. Animal experiments have shown that when administered in doses, 25 times higher than the recommended dose for a person causes a teratogenic effect.

When applied during breastfeeding period, risk and benefits should be ascertained due to the high probability of side effects in the child.

Application for the correction of the hypotension during childbirth is not recommended, because it can delay the second stage of childbirth; When introduced in large doses to weaken the cutting of the uterus, a long-term atron of the uterine with bleeding can be caused.

You can use in children when you stop the heart, but care should be taken, since 2 different concentrations of epinephrine are required in the dosing pattern.

When the dose treatment should be reduced gradually, because Sudden cancellation of therapy can lead to severe hypotension.

Easily collapsed with alkalis and oxidizing agents.

If the solution acquired a pinkish or brown or brown or contains a precipitate, it is impossible to enter it. Unused part should be destroyed.

State register of medicines. Official edition: at 2 tons - M.: Medical advice, 2009. - T.2, Part 1 - 568 s.; Part 2 - 560 p.

Epinephrine preparation is used in complex treatment Bronchial asthma, arterial hypotension and other severe pathologies.

The current component of the drug is synthetic adrenaline epinephrine - neurotransmitter and a natural hormone for humans produced by chromaffine cells of the brain layer of adrenal glands and present in many tissues of the body.

By chemical structure, this substance refers to catecholamines.

The drug belongs to the pharmacological group of black-eyed cardiotonic products and is available on sale under international unatic title (INN) Epinephrine.

In medicine, it is used as a medication with a pacemulatory, vasoconductive, hypertensive, hypoglycemic, bronchological and antiallergic activity.

Wide spectrum Therapeutic action allows the use of means in the treatment of a large number of diseases.

The adrenaline present in Epinephrine has a stimulating effect on the heart and vessels.

It increases the minute and shock volume of blood flow, narrows blood vessels, reinforces heartbeat, raises systolic blood pressure, increases the latter in pulmonary veins and arteries.

The press effect of the drug is manifested in the development of short-term bradycardia in a patient, depressor - in reducing blood pressure.

In addition to the properties listed, the application leads to the relaxation of the smooth muscles of the bronchi, the elimination of the spasm of bronchiol and the edema of their mucous membrane.

The drug suppresses the release of histamine, expanding pupils, lowers intraocular pressure, enhances glukegenesis and glycogenolysis, increases the level of lipids in the blood plasma.

When introduced into Vienna, epinephrine acts almost instantly, under the skin - 5-10 minutes after the injection.

The clinical effect using the means intramuscularly depending on the individual characteristics of the human body can be observed both after a few minutes and after half an hour after the introduction.

Epinephrine instructions

Experts use epinephrine for the following purposes:

1. To remove the attack of bronchial asthma;
2. To eliminate bronchospasm used when using general anesthesia;
3. Elimination of swelling of quinque, anaphylactic shock, urticaria of generalized type and other severe allergic reactions;
4. Stopping bleeding;
5. An increase in blood pressure in situations when it is not possible to normalize it with other means;
6. Resumption of heart work during asistolia;
7. Extension of the effects of painkillers;
8. Normalization in blood level glucose, fallen as a result of insulin overdose;
9. Reduction in intraocular pressure with an open-angle glaucoma;
10. Expansion of the pupil before performing ophthalmological operations.

Epinephrine is designed for injection in the muscle, vein and under the skin. Also allowed local and intracardial use of the drug.

To obtain a vasoconstrictor effect, the drug is recommended to use intravenously, introducing a patient infusion into the body.

Reference! The speed of drip administration of adrenaline should begin with 1 μg per minute. If necessary, it can be increased to 10 μg per minute.

For urgent relief of anaphylaxis and other allergic reactions of immediate-type, epinephrine is administered intravenously by injection.

Before the procedure, the drug is mixed with 0.9% physically or glucose solution of 5%. The duration of injection during intravenous administration is 1-2 minutes.

After improving the condition, the patient continues to introduce adrenaline intravenously drip at a speed of 1 μg per minute.

With nonsense allergic reactions, epinephrine is prescribed intramuscularly or subcutaneously. The drug in such cases is used under undiluted.

In the ventricular asistol, the means is administered intracardiously, mixing before use with an elevator 0.9%

To eliminate the attack of bronchial asthma, adrenaline is recommended to apply subcutaneously. It can be administered under undiluted or mixed with a 40% glucose solution.

To stop the bleeding, epinephrine is used locally, putting a tampon moored by the undiluted solution.

Patients with open-hearted glaucoma adrenaline are injected into the eyes.

The method of using the drug while simultaneously use with anesthetics is determined depending on their type and mechanism of action.

The dosage and duration of the use of epinephrine in all cases should be installed by a doctor individually.

Composition and form of release

The therapeutic effect of epinephrine provides epinephrina hydrochloride.

The synthetic adrenaline solution is a transparent liquid without color and odor, spilled into sterile ampoules with a volume of 1 ml. Concentration active component In 1 ml of solution is 1 mg.

Additionally, the preparation of the drug: sodium chloride, sodium metabisulfit and sterile water.

Some manufacturers in the release of a solution of synthetic adrenaline use epinephrina hydrotartrate.

This form of the active ingredient has the same physical and chemical characteristics as the epinephrine in the form of hydrochloride.

Contraindications for use

Epinephrine can not be prescribed to patients suffering:

• intolerance to the substances included in its composition;
• tahiaritimia;
• stenosis aortic valve;
• obstructive form of hypertrophic cardiomyopathy;
• fibrillation of ventricles;
• arterial hypertension.

Since adrenaline penetrates through the placenta and is found in maternal milk, its use in pregnant and breastfeeding patients is contraindicated.

Epinephrine requires caution in use in hypoxia, myocardial infarction, atrial fibrillation, atherosclerosis, closed-coronal glaucoma, diabetes, Parkinson disease, suspicion, thyrotoxicosis, prostate hypertrophy.

Also, caution during the period of use of the means should be observed with patients with metabolic acidosis, articular pathologies, hypercaps, hypovolemia, cold injuries, shock of non-allergic etiology.

Children and the people of elderly, when using synthetic adrenaline, it is necessary to be under constant medical supervision.

When applying epinephrine in patients may develop side effects From the side of the cardiovascular system, the digestive tract, metabolism, etc. they are manifested in the form:

• violations in the work of the gastrointestinal tract (vomiting, nausea, reducing body weight);
• difficult urination (in men with prostate hyperplasia);
• hyperglycemia;
• hypokalemia;
• dizziness;
• anxiety;
• paranoid behavior;
• problems with sleep;
• disorientation in space;
• reduce ability to memorize;
• headache;
• blood pressure oscillations;
• heart rate disorders (heartbeat, bradycardia, tachycardia);
• muscle cramps;
• uncontrolled erection;
• liver or kidney necrosis;
• hypersensitivity reactions (angioedema edema, bronchospasm, rash, multiform erythema);
• burning, swelling and other local reactions at the injection site.

When using epinephrine, an overdose should be avoided, since it is capable of improving severity. adverse Reactions.

In case of accidental administration of a large dose of adrenaline in patients, headaches may be observed, calling for vomiting, heart rate disruption, cooling limbs, leather pale, arterial hypertension, metabolic acidosis.

Also, the development of myocardial infarction, hemorrhage to the brain, atrial fibrillation and ventricles is also not excluded.

Strong dose is able to provoke a lung edema and death in humans.

With the development of signs of overdose, the patient needs to conduct therapy aimed at eliminating the symptoms that have arisen and restoring the functions of the body.