Adrenaline

Description overdue on 09/24/2014

• Latin name: Adrenalinum
• ATC code: C01CA24
• Active substance: Epinephrine (Epinephrine)
• Manufacturer: Moscow Endocrine Plant, Russia; Sanavita Gesundheitsmittel, Germany; ZAO "Pharmaceutical firm" Darnitsa "

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• Composition
• Product form
• Pharmacological action
• Pharmacodynamics and pharmacokinetics
• Indications
• Contraindications
• Side effects
• Instructions for use Adrenaline
• Overdose
• Cooperation
• Terms of sale
• Storage conditions
• Shelf life
• Cautions
• Ozyvy of adrenaline
• Price, where to buy

Composition

What is the adrenaline and adrenaline which is produced

Adrenaline - is a hormone that is produced in adrenal medulla   - Controlled by the nervous system structure that the organism is the main source catecholamine hormones   - Dopamine .   adrenaline   and noradrenaline .

Epinephrine, used as a drug, obtained from adrenal tissue slaughter cattle or synthetically.

Epinephrine - what is it?

The international non-proprietary name of adrenaline (INN) - epinephrine .

For medical drug produced by pharmaceutical companies in the form epinephrine hydrochloride   (Adrenalini hydrochloridum) and a epinephrine hydrogen tartrate   (Adrenalini hydrotartras).

The first is white or white with a pinkish tinge powder with a crystalline structure having the ability to change their properties when exposed to light and oxygen contained in the air.

In the process of preparation of the solution was added to the powder O, O1 n. hydrochloric acid solution. Used for the preservation of chlorobutanol and sodium metabisulfite. The final solution is clear and colorless.

Epinephrine tartrate   - It is white or white with a grayish white powder with a crystalline structure having the ability to change their properties when exposed to light and oxygen contained in the air.

The powder is easily soluble in water but slightly soluble in alcohol. Unlike adrenaline hydrochloride solutions adrenaline tartrate aqueous solutions are characterized by greater resistance, but its effect completely identical to them.

Due to the difference in molecular weight (for hydrogen tartrate it is 333, 3, and hydrochloride - 219, 66) tartrate is used at a higher dose.

Product form

Pharmaceutical companies produce a medicine in the form:

• 0, a 1% solution of epinephrine hydrochloride;
• 0, 18% solution of epinephrine hydrogen tartrate.

The agent enters the pharmacy vials made of neutral glass. The amount of funds in a vial - 1 ml.

The solution is intended for topical use, sold in hermetically-sealed bottles of orange glass. The capacity of one bottle - 30 ml.

Also encountered in pharmacies Adrenaline tablets. The drug is available in the form of homeopathic granules D3.

Pharmacological action

Wikipedia states that adrenaline belongs to a group   catabolic hormones   and affects almost all species Metabolism . It promotes raising contained in blood   sugar and stimulates the tissue metabolism .

Adrenaline belongs simultaneously to two pharmacological groups:

• Drugs that stimulate the α and α + β-adrenergic receptors.
• Hypertensive drugs.

The product is characterized by the ability to provide:

• hyperglycemic ;
• bronchodilator ;
• hypertensive ;
• antiallergenic ;
• vasoconstrictor effects .

In addition, the hormone adrenaline:

• It has an inhibitory effect on the production of glycogen in skeletal muscle and liver ;
• enhances the capture and utilization Glucose   fabrics;
• increases activity glycolytic enzymes ;
• It encourages decay and inhibits fat synthesis (a similar effect is achieved due to the ability to influence the adrenaline β1-adrenergic receptors , Localized in fat tissue );
• increases the functional activity skeletal muscle   (particularly when strong fatigue);
• stimulates CNS   (generating at the boundary (ie, carrying a risk for human life) situations hormone   provokes increase in wakefulness, improves mental alertness and mental energy, and promotes the mental mobilization);
• ons area hypothalamus Which is responsible for the production of corticotropin releasing hormone ;
• activates the system adrenal cortex hypothalamus-pituitary- ;
• stimulates adrenocorticotropic hormone ;
• stimulates the blood coagulation .

Adrenaline has antiallergic   and anti-inflammatory Preventing release mediators of allergy and inflammation   ( leukotrienes . histamine . prostaglandins   etc.) from mast cells, energizing them localized β2-adrenergic receptors   and reducing the sensitivity of different tissues to these substances.

Moderate concentrations of epinephrine have trophic effects on skeletal muscle and myocardium , In high concentrations the hormone enhances protein catabolism .

Pharmacodynamics and pharmacokinetics

Gross formula of adrenaline - C₉H₁₃NO₃.

Adrenaline and other substances that are produced adrenals They have the ability to interact with a variety of body tissues and thus prepares the body for stressful situation for the reaction (e.g., the situation of physical stress).

Reaction to severe stress is often described by the expression "fight or flight". It developed in the course of evolution and is a kind of defense mechanism that allows almost instantly react to danger.

When a person is in a dangerous situation, it hypothalamus   supplies adrenals Which is formed hormone adrenaline, the signal on the release of the latter in blood . The reaction of the organism to such emissions from developing in a few seconds: the power and speed of man has grown significantly, and sensitivity to pain at the same time significantly reduced.

This hormonal surge is called "adrenaline".

Influencing localized in liver tissues and β2-adrenergic receptors Hormone stimulates gluconeogenesis   (biochemical process of education Glucose   inorganic precursors) and the process glycogen biosynthesis from glucose   (glycogenesis).

The action of adrenaline when injected into the body is associated with the effect on α- and β-adrenergic receptors and in many ways similar to the effects arising in reflex excitation of sympathetic nerve fibers.

The mechanism of action of the drug is due to activation is responsible for the synthesis of cyclic AMP (cAMP), adenylate cyclase enzyme .

Receptors sensitive to adrenalin, localized on the outer surface cell membrane , i.e hormone   It does not penetrate into the cell. The cell is transmitted through the action of his so-called second messengers, chief among which is precisely cyclic AMP . The first intermediary in the transfer of regulatory signal is directly himself hormone .

Symptoms of adrenaline in the blood are:

• constriction vessels in the skin .   mucous As well as abdominal   (with slightly less taper in the vessels skeletal muscle );
• vasodilatation, located in brain ;
• increased frequency and amplification rate   heart muscle ;
• relief antrioventrikulyarnoy (atrioventricular) conduction ;
• increasing automaticity heart muscle ;
• improving performance Blood Pressure ;
• transient reflex bradycardia ;
• relaxation bronchial smooth muscle and gastrointestinal tract ;
• reduction Intraocular pressure ;
• mydriasis ;
• reduction of development intraocular fluid ;
• hyperkalemia   (for continuous stimulation of β2-adrenergic receptors);
• increasing concentrations plasma free fatty acids .

When Introducion adrenaline in / or under the skin of the drug is well absorbed. Maximum plasma concentration after administration under the skin or into a muscle observed after 3-10 minutes.

Adrenaline harakterizuestya ability to penetrate the placenta and in breast milk , While it is almost not able to penetrate through BBB (blood-brain barrier) .

Metabolization   it is carried out with the participation of enzyme monoamine oxidase (MAO) and catechol-O-metiltransefrazy (COMT) in sympathetic nerve endings and internal organs . The resulting products metabolism   inactive.

T1 / 2 (half-life) after the administration of adrenaline / in approximately 1-2 minutes.

Metabolites   derived mainly kidney , A small amount of substance excreted unchanged.

Indications

Epinephrine is indicated for use:

• immediately when developing allergic reactions .   including but not limited reaction to medications, food, blood, insect bites, etc. (for anaphylactic shock . hives   etc.);
• with a sharp fall in Blood Pressure   and violation of the blood supply to vital internal organs ( collapse );
• in a fit asthma ;
• at hypoglycemia Caused by overdose insulin ;
• in conditions characterized by a decrease in potassium ion concentration in blood ( hypokalemia );
• at open-angle glaucoma (elevated intraocular pressure) ;
• at cardiac arrest (ventricular asystole) ;
• during surgery on the eyes for removal   swelling of the conjunctiva ;
• at bleeding   of superficially located in the skin and mucous receptacles;
• under which developed acute atrioventricular block of 3rd degree ;
• at ventricular fibrillation ;
• at acute left ventricular failure ;
• at priapism .

Adrenaline is also used as a vasoconstrictor   in a number of ENT diseases   and to prolong the action Local anesthetic drugs .

With hemorrhoids   candles with thrombin and adrenaline allow to stop the bleeding and numb the affected area.

Epinephrine is used during surgical procedures, and is injected through the endoscope in order to reduce blood loss. In addition, the substance is included in several solutions that are used for long-term local anesthesia (particularly in dentistry).

In particular, for infiltration and conduction anesthesia   (including dental practice in extirpation of tooth . for filling cavities At grinding teeth   before setting bits) shows a drug Septanest with adrenaline.

Tablets Adrenaline quite successfully used for the treatment of angina . hypertension . In addition, the tablets may be assigned syndromes accompanied by increased anxiety, a feeling of pressure in your chest and feel of the bar lying across his chest.

Contraindications

Contraindications to the use of Adrenaline are:

• steadily increased blood pressure (hypertension) ;
• aneurysm ;
• expressed atherosclerotic vascular lesions ;
• pregnancy ;
• lactation ;
• hypertrophic cardiomyopathy (GOKMP) ;
• pheochromocytoma ;
• tachyarrhythmia ;
• thyrotoxicosis ;
• hypersensitivity epinephrine .

Because of the high risk of Arrhythmia   forbidden to use adrenaline to patients entered into a state of anesthesia   Chloroform . Cyclopropanes . Ftorotanom .

The means used with caution in the treatment of elderly patients and children.

Side effects

Adrenaline stimulates not only a significant increase in physical strength, speed and performance, but also increases the rate of breathing and sharpens attention. Often the release of this Hormone   accompanied by a distorted perception of reality, and dizziness.

In cases where the emission Hormone   It occurred, but there is no real danger, a person feels irritability and anxiety. The reason for this is that the adrenaline is accompanied by an increase in generation   Glucose   and increased blood sugar blood . That is, the human body gets extra energy, which, however, does not find a way out.

In the past, most stressful situations were resolved through the exercise in the modern world, the amount of stress has increased significantly, but at the same time to address them requires little or no physical activity. For this reason, many people are exposed to stress, to reduce the level of adrenaline is actively involved in sports.

Despite the fact that adrenaline plays a leading role in the survival of the body, over time it leads to negative consequences. Thus a prolonged increase in the level of Hormone   inhibits the activity heart muscle And in some cases may even provoke heart failure .

Elevated levels of adrenaline is also the cause of insomnia and frequent nerve disorders   ( nervous breakdowns ). Similar symptoms are an indication that the person is in a state of chronic stress.

Reaction to epinephrine may be the following side effects:

• improving performance Blood Pressure ;
• frequency increase rate heart muscle ;
• violation heart rate ;
• pain in the chest in the area hearts .

With Arrhythmia Provoked by the introduction of the drug, the patient shows the drugs pharmacological action aimed at blocking β-adrenergic receptor   (eg,   Anaprilin   or Obzidan ).

Instructions for use Adrenaline

Epinephrine hydrochloride instructions for use recommends administered subcutaneously to patients, at least - in muscle   or in vein   (slow drip). The drug is not allowed to enter into the artery As expressed by the restriction peripheral blood vessels   can trigger the development of gangrene .

Depending on the clinical picture and on the purpose for which is assigned means a single dose for an adult varies from 0, 1 to 2 ml for a child - of 0, 1 to 0, 5 ml.

With acute heart failure   intracardiac patient should enter the contents of one vial (1 ml), and ventricular fibrillation is a dose of 0, 5 to 1 ml.

Cupping asthma   solution was administered subcutaneously at a dose of 0, 3-0, 5-0, 7 ml.

Typically, the therapeutic dose solutions Epinephrine hydrochloride   and gidrotartrata   are as follows:

• 0, 3-0, 5-0, 75 ml - for adults;
• 0, 1-0, 5 ml - for children (depending on the age of the child).

Allowable highest dose subcutaneous administration: for adults - 1 ml for children - 0, 5 ml.

Overdose

Adrenaline Overdose symptoms are:

• excessive increase Blood Pressure ;
• mydriasis ( mydriasis );
• alternating with   bradycardia, tachyarrhythmia ;
• Atrial fibrillation and ventricular ;
• coldness and pale skin;
• vomiting;
• irrational fear;
• anxiety;
• tremor ;
• headache ;
• metabolic acidosis ;
• myocardial infarction ;
• cranio-cerebral hemorrhage ;
• pulmonary edema ;
• renal failure .

The minimum dose lethal dose is considered equal to 0 10 ml, 18% solution.

Treatment involves cessation of drug administration. To eliminate the symptoms of an overdose of adrenaline used α- and β-blockers As well as fast nitrates.

In cases where an overdose accompanied by severe complications, patients showed a complete cure. With Arrhythmia Associated with the use of drugs prescribed parenteral administration β-blockers .

Cooperation

Adrenaline antagonists are drugs that block α- and β-adrenergic receptors .

Non-selective β-blockers   have a potentiating effect on pressor effect epinephrine .

Simultaneous use of the drug with cardiac glycosides . tricyclic antidepressants . dopamine . quinidine As well as preparations for the inhalation anesthesia   and cocaine   It not recommended due to an increased risk of Arrhythmia . The only exceptions are cases of extreme necessity.

At simultaneous application with other sympathomimetic there is a significant increase in the severity of adverse effects arising from the Cardiovascular .

Concomitant use with antihypertensive agents   (including but not limited diuretics ) Leads to a reduction in their effectiveness.

Use of epinephrine ergot alkaloids ( ergot alkaloids ) Increases vasoconstrictor effect   (in some cases up to the onset of symptoms expressed ischemia   and development gangrene ).

Medicaments inhibitors of monoamine oxidase (MAO) reserpine . sympatholytic oktadin , Blocking agents m-cholinergic receptors . n anticholinergics , Preparations thyroid hormones   potentiate the pharmacological action epinephrine .

In its turn, epinephrine   reduces efficiency hypoglycemic agents   (including insulin); neuroleptic . holinomimeticakih   and hypnotics ; opoidnyh analgesics . muscle relaxants .

In an application with drugs prolonging the interval QT (for example, astemizole   or terfenadine ), The effect of the latter is significantly enhanced (or increase the length of the interval QT).

It is not allowed to mix in the same syringe with a solution of adrenaline solutions of acids, alkalis and oxidants due to the possibility of entry into chemical interaction with   epinephrine .

Terms of sale

The drug is intended for use in hospital and hospital emergency room. Distributed through the Inter-hospital pharmacy. Holidays made prescription.

Recipe in Latin with an indication of the dose and mode of application prescribed by a doctor.

Storage conditions

The product is included in List B. Store in a cool, it is recommended that the reach of children. Freezing is not allowed. The optimal temperature - 12-15 ° C (possible Adrenaline is recommended to put in the fridge).

Brownish solution, and the solution containing precipitate are not considered suitable for use.

Shelf life

24 months

Cautions

How to reduce the level of adrenaline in the blood

The overabundance of adrenaline that generates chromaffin tissue of the adrenal glands It expressed in such emotions as fear, rage, anger and resentment.

The hormone prepares the person to stress and improves functional capacity skeletal muscle But if it is produced for a long time at high doses, it can lead to severe debilitation and death.

For this reason, it is important to be able to control the level of adrenaline. Reducing its largely contribute to:

• Regular Weight Training (training in the gym, jogging, swimming, etc.);
• maintaining a healthy lifestyle;
• passive recreation (visiting a concert, watching a comedy, etc.);
• phytotherapy (herbal teas are very effective, has a soothing effect: mint, lemon balm, sage, etc.);
• hobbies;

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