Adrenaline

Adrenaline – alpha and beta-adrenergic agonist with hypertensive, broncholitic, antiallergic action.

Form of release and structure

Dosage forms:

• Solution for injections: slabookrashenny or colourless transparent liquid with a specific smell (on 1 ml in ampoules, in a blister strip packaging on 5 ampoules, in a cardboard pack 1 or 2 packagings in a set with the scarificator or a knife ampoule (or without them); for a hospital – on 20, 50 or 100 packagings in cardboard boxes);
• Solution for topical administration of 0,1%: transparent colourless or slabookrashenny liquid with a specific smell (on 30 ml in glass bottles of dark color, in a cardboard pack 1 bottle).

For injections contains in 1 ml of solution:

• Active ingredient: Epinephrinum – 1 mg;
• Auxiliary components: sodium disulphite (sodium metabisulphite), Acidum hydrochloricum, sodium chloride, chlorobutanol гемигидрат (хлоробутанолгидрат), глицерол (glycerin), dinatrium эдетат (disodium salt of ethylene diamine tetraacetic acid), water for injections.

For topical administration contains in 1 ml of solution:

• Active ingredient: Epinephrinum – 1 mg;
• Auxiliary components: sodium metabisulphite, sodium chloride, хлоробутанолгидрат, glycerin (глицерол), disodium salt of ethylene diamine tetraacetic acid (dinatrium эдетат), acid solution of hydrochloric 0,01 M.

Indications to use

Solution for injections

• The Quincke's disease, small tortoiseshell, acute anaphylaxis and other allergic reactions of immediate type developing against the background of hemotransfusion, use of medicines and serums, the use of foodstuff, stings of insects or administration of other allergens;
• Asthma of physical effort;
• Asystolia (including at sharply developed atrioventricular block of the III degree);
• Stopping of the asthmatic status of bronchial asthma, acute management at a bronchospasm during an anesthesia;
• Morganyi-Adams-Stokes's syndrome, total atrioventricular block;
• Bleeding from superficial vessels of mucous membranes (including a gingiva) and skin;
• Arterial hypotension, in case of lack of therapeutic effect of use of adequate volumes of the replacing liquids (including shock, open heart operations, bacteremia, a renal failure).

Besides, use of drug is shown as a vasoconstrictor for a stop of bleeding and lengthening of the period of effect of local anesthetics.

Solution for topical administration of 0,1%
Solution is applied to a bleeding stop from superficial vessels of mucous membranes (including a gingiva) also by skin.

Contraindications

• Coronary heart disease, tachyarrhythmia;
• Arterial hypertension;
• Fibrillation of ventricles;
• Hypertrophic subaortic stenosis;
• Pheochromocytoma;
• Period of pregnancy and breastfeeding;
• Individual intolerance of components of drug.

In addition contraindications to use of solution for injections:

• Ventricular arrhythmias;
• Fibrillation of auricles;
• Chronic heart failure of the III-IV degree;
• Myocardial infarction;
• Chronic and acute form of arterial insufficiency (including the anamnesis – atherosclerosis, an arterial embolism, a Thrombangiitis obliterans, a Raynaud's disease, a diabetic endarteritis);
• The expressed atherosclerosis, including cerebral atherosclerosis;
• Organic injuries of a brain;
• Parkinson's disease;
• Hypovolemia;
• Thyrotoxicosis;
• Diabetes mellitus;
• Metabolic acidosis;
• Hypoxia;
• Hypercapnia;
• Pulmonary hypertensia;
• Cardiogenic, hemorrhagic, traumatic and other types of shock of not allergic genesis;
• Cold injury;
• Convulsive syndrome;
• Closed-angle glaucoma;
• Prostate hyperplasia;
• Simultaneous use with inhalation means for the general anesthesia (halothane), with local anesthetics at anesthesia of fingers of hands and legs (risk of ischemic damage of fabrics);
• Age up to 18 years.

All above-mentioned contraindications are relative at states, life-threatening the patient.

With care it is necessary to appoint solution for injections at a hyperthyroidism and the patient at advanced age.

For prevention of arrhythmias drug is recommended to be used in combination with beta adrenoblockers.

With care appoint Adrenaline in the form of solution for topical administration sick with a metabolic acidosis, a hypoxia, a hypercapnia, fibrillation of auricles, pulmonary hypertensia, ventricular arrhythmia, a hypovolemia, a myocardial infarction, shock of not allergic genesis (including cardiogenic, hemorrhagic, traumatic), occlusal diseases of vessels (including atherosclerosis, an arterial embolism, a Thrombangiitis obliterans, a diabetic endarteritis, cold injuries, a Raynaud's disease in the anamnesis), a thyrotoxicosis, a prostatauxe, closed-angle glaucoma, a diabetes mellitus, cerebral atherosclerosis, a convulsive syndrome, Parkinson's disease; at simultaneous use for the general anesthesia of inhalation drugs (Ftorotanum, chloroform, cyclopropane), at advanced or children's age.

Route of administration and dosage

Solution for topical administration
Solution is applied locally.

At a stop of bleeding it is necessary to put the tampon moistened in solution to a wound.

Solution for injections
Solution is intended for intramuscular (in oil), hypodermic (п / to), intravenous (in/in) drop or jet introduction.

The recommended dosing mode for adults:

• Acute anaphylaxis and other reactions of allergic genesis of immediate type: in/in slowly – 0,1-0,25 mg should be parted in 10 ml 0,9% of solution of sodium of chloride. For achievement of clinical effect therapy is continued in the way in/in drop by introductions, in a proportion 1:10000. In the absence of real threat of life of the patient the drug is recommended to be administered in oil or п / to in a dose of 0,3-0,5 mg, if necessary it is possible to repeat an injection with an interval of 10-20 minutes to 3 times;
• Bronchial asthma: п / to – 0,3-0,5 mg, for achievement of desirable effect repeated introduction of the same dose every 20 minutes to 3 times, or in/in – 0,1-0,25 mg, divorced from 0,9% of solution of sodium of chloride in a proportion 1:10000 is shown;
• Arterial hypotension: in/in kapelno with a speed of 0,001 mg a minute, increase in rate of administering up to 0,002-0,01 mg a minute is possible;
• Asystolia: vnutriserdechno – 0,5 mg in 10 ml of 0,9% of solution of sodium of chloride (or other solution). At resuscitation actions the drug is administered in/in, in a dose of 0,5-1 mg every 3-5 minutes, divorced in 0,9% of solution of sodium of chloride. At an intubation of a trachea of the patient introduction can be carried out by endotracheal instillation in the dose exceeding a dose for in/in introductions to 2-2,5 times;
• Vasoconstrictor: in/in kapelno with a speed of 0,001 mg a minute, it is possible to increase the speed of infusion to 0,002-0,01 mg a minute;
• Lengthening of effect of local anesthetics: the dose is appointed in concentration of 0,005 mg of drug to 1 ml of anesthetic, at spinal anesthesia – on 0,2-0,4 mg;
• Morganyi-Adams-Stokes's syndrome (bradiaritmichesky form): in/in kapelno – 1 mg in 250 ml of 5% of solution of glucose, gradually increasing infusion speed to emergence of minimum sufficient number of cordial reductions.

The recommended dosing for children:

• Asystolia: the newborn – in/in (slowly), on 0,01-0,03 mg on 1 kg of weight of the child every 3-5 minutes. To children after 1 month of life – in/in, on 0,01 mg/kg, further on 0,1 mg/kg every 3-5 minutes. After introduction of two standard doses transition to introduction of 0,2 mg/kg of weight of the child with an interval of 5 minutes is allowed. Endotracheal introduction is shown;
• Acute anaphylaxis: п / to or in oil – on 0,01 mg/kg, but no more than 0,3 mg. If necessary the procedure is repeated with an interval of 15 minutes by no more than 3 times;
• Bronchospasm: п / to – on 0,01 mg/kg, but no more than 0,3 mg, if necessary the drug is administered every 15 minutes to 3-4 times or every 4 hour.

Solution for injections Adrenaline can also be used locally, for a stop of bleedings, having put the tampon moistened in solution to a wound surface.

Side effects

• Nervous system: often – an alarming state, a headache, a tremor; infrequently – fatigue, dizziness, nervousness, frustration of the personality (a disorientation, psychomotor arousing, disturbance of memory and psychotic frustration: panic, agressive behavior, paranoia, shizofrenopodobny frustration), muscular twitchings, sleep disorder;
• Cardiovascular system: infrequently – tachycardia, stenocardia, bradycardia, a heart consciousness, decrease or increase in the arterial pressure (AP), against the background of high doses – ventricular arrhythmias (including fibrillation of ventricles); seldom – thorax pain, arrhythmia;
• Alimentary system: often – nausea, vomiting;
• Allergic reactions: infrequently – skin rash, a bronchospasm, a mnogoformny erythema, a Quincke's disease;
• Urinary system: seldom – the painful, complicated urination at patients with a prostate hyperplasia;
• Others: infrequently – the increased sweating; seldom – a hypopotassemia.

In addition, owing to use of solution for injections:

• Cardiovascular system: seldom – a fluid lungs;
• Nervous system: often – a tic; infrequently – nausea, vomiting;
• Local reactions: infrequently – burning and/or pain in the place in oil of an injection.

It is necessary to report about emergence of the specified or other undesirable effects to the doctor.

Special instructions

Accidentally entered into Epinephrinum can sharply raise the ABP.

Against the background of increase in the ABP at administration of drug development of attacks of stenocardia is possible. Action of Epinephrinum can cause reduction of a diuresis.

Infusion should be carried out to large (preferably central) vein, using the device for regulation of rate of administering of drug.

Endocardiac introduction at an asystolia is applied in case of unavailability of other ways as there is a risk of a cardiac tamponade and pheumothorax.

Treatment is recommended to be accompanied with determination of level of maintenance of potassium ions in blood serum, measurement of the ABP, minute volume of blood circulation, pulmonary pressure, jamming pressure in pulmonary capillaries, a diuresis, the central venous pressure, carrying out an electrocardiography. Use of high doses at a myocardial infarction can strengthen ischemia because of increase in oxygen requirement.

During treatment of patients with a diabetes mellitus increase in a dose of derivatives of sulphonylurea and insulin as Adrenalin increases a glycemia is required.

Absorption and final concentration of Epinephrinum in plasma at endotracheal introduction can be unpredictable.

At depressed cases use of drug does not replace transfusion of blood-substituting liquids, saline solutions, blood or plasma.

Prolonged use of Epinephrinum causes narrowing of peripheral vessels, risk of development of a necrosis or gangrene.

It is not recommended to use drug at the time of delivery for increase in the ABP, introduction of high doses for weakening of reduction of a uterus can become the reason of a long atony of a uterus with bleeding.

Use of Epinephrinum at a cardiac standstill at children is allowed on condition of respect for care.

Drug withdrawal should be carried out by a gradual dose decline not to allow development of arterial hypotension.

Adrenaline easily collapses the alkylating means and oxidizers, including bromides, chlorides, iron salts, nitrites, peroxides.

At emergence of a deposit or discoloration of solution (pinkish or brown) drug is not suitable for use. Unused drug is subject to utilization.

The doctor solves a question of the admission of the patient to control of vehicles and mechanisms individually.

Medicinal interaction

• Blockers α-and β-adrenoceptors - - - - - - - - - – antagonists of Epinephrinum (at therapy of heavy anaphylactic reactions by β-adrenoblockers efficiency of Epinephrinum at patients is reduced, it is recommended to replace it with administration of salbutamol in/in);
• Other adrenomimetik – can strengthen action of Epinephrinum and expressiveness of side effects from cardiovascular system;
• Cardiac glycosides, quinidine, tricyclic antidepressants, dopamine, means for inhalation anesthesia (a halothane, метоксифлуран, энфлуран, изофлуран), cocaine – raises probability of development of arrhythmias (combined use is allowed with respect for extreme care, or it is not allowed);
• Narcotic analgetics, somnolent, anti-hypertensive means, insulin and other hypoglycemic medicines – their efficiency decreases;
• Diuretics – increase in pressor effect of Epinephrinum is possible;
• Monoamine oxidase inhibitors (селегилин, Procarbazinum, furasolidone) – can cause the sudden and expressed increase in the ABP, a headache, cardiac arrhythmia, vomiting, hyperpyrexial crisis;
• Nitrates – weakening of their medical action is possible;
• Phenoxybenzamine – tachycardia and strengthening of hypotensive effect are probable;
• Phenytoinum – sudden decrease in the ABP and bradycardia (depending on rate of administering and a dose);
• Drugs of hormones of a thyroid gland – mutual strengthening of action;
• The medicines extending a QT interval (including астемизол, цизаприд, терфенадин) – lengthening of a QT interval;
• Diatrizoatums, yotalamovy or yoksaglovy acids – strengthening of neurologic effects;
• Ergot alkaloids – strengthening of vasopressor effect (up to the expressed ischemia and a gangrenosis).

Terms and storage conditions

To store at a temperature up to 15 °C in the place protected from light. To protect from children.

Period of validity – 3 years.